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Sample records for oral contraceptive tablets

  1. Oral Contraceptives and Cancer Risk

    MedlinePlus

    ... oral contraceptives are available in the United States today? How could oral contraceptives influence cancer risk? How ... oral contraceptives are available in the United States today? Two types of oral contraceptives (birth control pills) ...

  2. Estrogen and Progestin (Oral Contraceptives)

    MedlinePlus

    ... syndrome [AIDS]) and other sexually transmitted diseases.Some brands of oral contraceptives are also used to treat ... your doctor.Oral contraceptives come in many different brands. Different brands of oral contraceptives contain slightly different ...

  3. Oral Contraceptive Pill and PCOS

    MedlinePlus

    ... Health Gynecology Medical Conditions Nutrition & Fitness Emotional Health PCOS: The Oral Contraceptive Pill Posted under Health Guides . ... of oral contraceptive pills for young women with PCOS? Regular and Lighter Periods: Oral contraceptive pills can ...

  4. Oral contraceptive drug interactions.

    PubMed

    Baciewicz, A M

    1985-01-01

    Approximately 50 million women use oral contraceptives (OC). Studies and case reports demonstrate that OC failure may be caused by rifampin, anticonvulsant drugs, and possibly some antibiotics. Contraceptive steroids may interfere with the metabolism of the benzodiazepines, theophylline, and the glucocorticoids. Future investigation will document the clinical significance of other OC interactions as well as give rise to new interactions. PMID:2859674

  5. History of oral contraception.

    PubMed

    Dhont, Marc

    2010-12-01

    On the 50th birthday of the pill, it is appropriate to recall the milestones which have led to its development and evolution during the last five decades. The main contraceptive effect of the pill being inhibition of ovulation, it may be called a small miracle that this drug was developed long before the complex regulation of ovulation and the menstrual cycle was elucidated. Another stumbling block on its way was the hostile climate with regard to contraception that prevailed at the time. Animal experiments on the effect of sex steroids on ovulation, and the synthesis of sex steroids and orally active analogues were the necessary preliminaries. We owe the development of oral contraceptives to a handful of persons: two determined feminists, Margaret Sanger and Katherine McCormick; a biologist, Gregory Pincus; and a gynaecologist, John Rock. Soon after the introduction of the first pills, some nasty and life-threatening side effects emerged, which were due to the high doses of sex steroids. This led to the development of new preparations with reduced oestrogen content, progestins with more specific action, and alternative administration routes. Almost every decade we have witnessed a breakthrough in oral contraception. Social and moral objections to birth control have gradually disappeared and, notwithstanding some pill scares, oral contraceptives are now one of the most used methods of contraception. Finally, all's well that ends well: recent reports have substantiated the multiple noncontraceptive health benefits paving the way for a bright future for this 50-year-old product. PMID:21091163

  6. Progestin-Only Oral Contraceptives

    MedlinePlus

    Progestin-only oral contraceptives are used to prevent pregnancy. Progestin is a female hormone. It works by preventing the ... mucus and the lining of the uterus. Progestin-only oral contraceptives are a very effective method of ...

  7. Diabetes and oral contraception.

    PubMed

    Gourdy, Pierre

    2013-02-01

    The prevalence of diabetes mellitus is increasing dramatically worldwide, resulting in more and more women of reproductive age being affected by either type 1 or type 2 diabetes. Management of contraception is a major issue due to the specific risks associated with pregnancy and those potentially induced by hormonal contraceptives in diabetic women. This review emphasizes the urgent need to improve the use of contraception in women with diabetes. There is no consistent evidence that combined oral contraceptives significantly influence the risk of developing diabetes, even in women with a history of gestational diabetes. Furthermore, although data from specific studies remain sparse, no worsening effect has been reported in diabetic women, either in glycemic control or on the course of microvascular complications. Thus, the use of estroprogestive pills is now recognized as a safe and effective option for preconception care of women with uncomplicated diabetes. According to recent guidelines, these contraceptives must be avoided in case of associated cardiovascular risk factors, cardiovascular disease or severe microvascular complications such as nephropathy with proteinuria or active proliferative retinopathy. Prescription of combined hormonal contraception in type 2 diabetic women must also be considered with caution due to a frequent association with obesity and vascular risk factors which increase both thromboembolic and arterial risks. Thanks to their metabolic and vascular safety profile, progestin-only contraceptives, as well as non-hormonal methods, represent alternatives according to patient wishes. PMID:23384747

  8. Antibiotics and oral contraceptives.

    PubMed

    Rubin, D F

    1981-04-01

    Dermatologists often prescribe oral tetracycline for the control of acne, primarily, and to a much lesser extent, for the treatment of cutaneous infections. A number of the patients taking tetracycline are also taking birth control pills. A recent article in the British Medical Journal (1980;1:293) indicates that this combination can lead to a failure of the (OC) oral contraceptive. Such failure had been associated with ampicillin as well. It is believed that the mechanism for this was the disturbance in normal gut flora, with consequent effects on bacterial hydrolysis of steroid conjugates. This would interrupt the enterohepatic circulation of contraceptive steroids, resulting in a less than normal concentration of circulating steroids. It was recommended that women taking low-dose OCs take extra precautions against pregnancy during any cycle in which antibiotics are given. In regard to our care of and responsibilities to our patients, and in an era when malpractice suits for all types of reasons are more common, it certainly behooves dermatologists to recognize and be concerned about this potential consequence of prescribing oral antibiotics. PMID:7212735

  9. Adolescents and oral contraceptives.

    PubMed

    Sanfilippo, J S

    1991-01-01

    Oral contraceptive (OC) options for adolescents are provides. Clarification for those desiring a birth control method is necessary and the benefits of decreased acne and dysmenorrhea with low dose OCs should be stressed along with the importance of compliance. A community effort is suggested to communicate the sexual and contraceptive alternatives, including abstinence and outercourse (sexual stimulation to orgasm without intercourse). Attention is given to concerns associated with teenage sexual activity, prevention of adolescent pregnancy, contraceptive options for the adolescent patient, adolescent attitudes toward birth control OCs, management of the adolescent OC user, manipulation of steroid components of OCs to respond to adolescent concerns, and other hormonal contraceptive options such as minipills or abstinence. The text is supplemented with tables: the % of US women by single years of age for 1971, 1976, 1979, and 1982; comparative pregnancy and abortion rates for the US and 5 other countries; federal cost for teen childbearing; adolescent nonhormonal contraceptive methods (advantages, disadvantages, and retail cost); checklist to identify those at risk for noncompliance with OCs; hormonal side effects of OCs; risks from OCs to adolescents; and benefits of OCs. Concern about adolescent pregnancy dates back to Aristotle. A modern profile shows girls form single-parent families are sexually active at an earlier age, adolescent mothers produce offspring who repeat the cycle, victims of sexual abuse are more likely to be sexually active, and teenagers in foster care are 4 times more likely to be sexually active and 8 times more likely to become pregnant. Prevention involves a multifaceted approach. OCs are the most appropriate contraceptive choice for adolescents. Frequency of intercourse is closely associated with OC use after approximately 15 months of unprotected sexual activity. At risk for noncompliance variables are scales of personality development

  10. Progestin-Only Oral Contraceptives

    MedlinePlus

    ... oral contraceptives are a very effective method of birth control, but they do not prevent the spread of ... on another day, use a backup method of birth control (such as a condom and/or a spermicide) ...

  11. Oral contraceptives and exercise.

    PubMed

    Mostardi, R A; Woebkenberg, N R; Jarrett, M T

    1980-01-01

    A laboratory study was undertaken with volunteer females (aged 20-25) to determine the effect of OCs (oral contraceptives) on hematologic and metabolic variables during exercise. 5 of the women studied were naturally cycling and 7 were taking OCs. The women worked at 2 workloads on a bicycle ergometer at 50% and 90% of their maximal aerobic capacity during 3 different phases of their menstrual cycle. There was no better time of the month for doing the 50% or the 90% workload in either group. Heartrate for the OC group was significantly higher at the 50% maximal capacity. Results of the test indicate tha women on OCs have somewhat reduced cardiac efficiency and are ventilating more to carry out a given amount of work when compared to women who are naturally cycling. Possible explanations for the higher heart rate are put forward. The main limitation of the study is that the subject numbers involved are small and the number of cycles studied is also small. PMID:12278397

  12. [Effect of oral contraceptives on vaginal flora].

    PubMed

    Batashki, I; Markova, D; Milchev, N; Uchikova, E; Gŭrova, A

    2006-01-01

    The contraceptive and non contraceptive advantages of oral chormonal contraceptives as well as the good control on fertility, make it one of the most preffered method of contraception. The normal vaginal flora is a dynamic ecosystem and itsequilibrium and status of eubyosis amongst its inhabitants is an important mechanism against exogenous infections. The use of oral contraceptives is not associated with significant changes in the vaginal microbial flora; the normal concentration of the lactobacillli is preserved. PMID:16889189

  13. Nomegestrol acetate/estradiol: in oral contraception.

    PubMed

    Yang, Lily P H; Plosker, Greg L

    2012-10-01

    Nomegestrol acetate/estradiol is a combined oral contraceptive with approval in many countries. This fixed-dose combination tablet contains nomegestrol acetate, a highly selective progestogen, and estradiol, a natural estrogen. It is the first monophasic combined oral contraceptive to contain estradiol, and is taken in 28-day cycles, consisting of 24 active therapy days with 4 placebo days (i.e. 24/4-day cycles). In two large, 1-year, randomized, open-label, multicentre, phase III trials in healthy adult women (aged 18-50 years), nomegestrol acetate/estradiol was at least as effective as drospirenone/ethinylestradiol as contraceptive therapy, as the pregnancy rates in women aged 18-35 years (primary efficacy population) in terms of the Pearl Index (primary endpoint) were numerically lower with nomegestrol acetate/estradiol, although the between-group difference was not statistically significant. In both trials, nomegestrol acetate/estradiol was given in a 24/4-day cycle, and drospirenone/ethinylestradiol was given in a 21/7-day cycle. The criteria for using condoms in case of forgotten doses were less stringent in the nomegestrol acetate/estradiol group than in the drospirenone/ethinylestradiol group. Nomegestrol acetate/estradiol therapy for up to 1 year was generally well tolerated in healthy adult women, with an acceptable tolerability profile in line with that expected for a combined oral contraceptive. The most commonly reported adverse events were acne and abnormal withdrawal bleeding (most often shorter, lighter or absent periods). Overall, compared with drospirenone/ethinylestradiol, nomegestrol acetate/estradiol appeared to be associated with less favourable acne-related outcomes, and shorter, lighter or absent periods. PMID:22950535

  14. [The acceptability of different oral contraceptive methods].

    PubMed

    Klinger, G; Fritzsche, H; Hempel, E; Carol, W; Böhme, W; Scholz, B; Grass, M; Chemnitius, K H

    1975-05-01

    Results of a survey of contraceptive acceptability are reported. In formation on oral and depot hormonal contraceptives was distributed to 1064 Ovosiston or Nonovlon users, 110 women using depot contraceptives, and 609 women who had never used hormonal contraception. The women's preferences with regard to administration schedule, and their perceptions of effectiveness and safety were noted. Non-users considered daily, weekly, or monthly administration acceptable, while only 2/3 of those taking oral contraceptives thought daily administration convenient. 90.2% of Deposiston patients did not care for daily administration. Deposiston patients also had the greatest confidence in their method. The authors believe on the basis of this survey that weekly administration may be highly acceptable alternative t o conventional oral contraception. PMID:1140078

  15. Non-Contraceptive Benefits of Oral Hormonal Contraceptives

    PubMed Central

    Schindler, Adolf E

    2012-01-01

    Abstract It is becoming evident that oral hormonal contraceptives-besides being well established contraceptives-seem to become important medications for many functional or organic disturbances. So far, clinical effectiveness has been shown for treatment as well as prevention of menstrual bleeding disorders and menstrual-related pain symptoms. Also this is true for premenstrual syndrome (PMS) and premenstrual disphoric disorder (PMDD). Particular oral contraceptives (OCs) containing anti-androgenic progestogens were shown to be effective medications for treatment of androgenisation symptoms (seborrhea, acne, hirsutism, alopecia). Through perfect suppression of the hypothalamic-pituitary-ovarian axis OCs have proven to be effective in elimination of persistent follicular cysts. Endometriosis/adenomyosis related pain symptoms are well handled similar to other drugs like Gonadotropine Releasing Hormone agonists but are less expensive, with less side effects, and possibility to be used for longer periods of time. This is also true for myoma. Pelvic inflammatory disease, rheumatoid arthritis, menstrual migraine, and onset of multiple sclerosis are prevented or delayed. Bone density is preserved and asthma symptoms improved. Endometrial hyperplasia and benign breast disease can be controlled. There is definitely a significant impact on risk reduction regarding endometrial, ovarian, and colon cancers. In conclusion, it needs to be recognized that oral combined hormonal contraceptives (estrogen/ progestogen combination) are - besides being reliable forms of contraception - are cost-effective medications for many medical disorders in women. Therefore, these contraceptives drugs are important for female and global health and should be used in clinical practice. PMID:23853619

  16. Combination oral contraceptives and cancer risk.

    PubMed

    Gast, K; Snyder, T

    1990-07-01

    Substantial evidence exists to suggest that the use of oral contraceptives alters the risk for some types of cancer. Use of oral contraceptives for one year or more will reduce the risk of endometrial cancer and epithelial ovarian cancer by 50%, with the protective effect lasting for at least 10 years. The risk for developing cervical cancer in women who have used oral contraceptives appears to be slightly increased, although two independent studies actually found a protective effect associated with oral contraceptive use. The protective effect was probably related to the increased screening frequency found in oral contraceptive users and not related to a biologically protective effect. Therefore, women should be encouraged to undergo regular Pap tests. Data regarding breast cancer, in general, show no increased risk associated with oral contraceptive use. The latency associated with the development of breast cancer does not allow a definitive conclusion, and further study will be required. Oral contraceptives appear to increase the risk for developing benign hepatocellular adenoma, but not hepatocellular carcinoma. PMID:2202849

  17. Pharmacokinetic drug interactions with oral contraceptives.

    PubMed

    Back, D J; Orme, M L

    1990-06-01

    Oral contraceptive steroids are used by an estimated 60 to 70 million women world-wide. Over the past 20 years there have been both case reports and clinical studies on the topic of drug interactions with these agents. Some of the interactions are of definite therapeutic relevance, whereas others can be discounted as being of no clinical significance. Pharmacological interactions between oral contraceptive steroids and other compounds may be of 2 kinds: (a) drugs may impair the efficacy of oral contraceptive steroids, leading to breakthrough bleeding and pregnancy (in a few cases, the activity of the contraceptive is enhanced); (b) oral contraceptive steroids may interfere with the metabolism of other drugs. A number of anticonvulsants (phenobarbital, phenytoin, carbamazepine) are enzyme-inducing agents and thereby increase the clearance of the oral contraceptive steroids. Valproic acid has no enzyme-inducing properties, and thus women on this anticonvulsant can rely on their low dose oral contraceptive steroids for contraceptive protection. Researchers are now beginning to unravel the molecular basis of this interaction, with evidence of specific forms of cytochrome P450 (P450IIC and IIIA gene families) being induced by phenobarbital. Rifampicin, the antituberculous drug, also induces a cytochrome P450 which is a product of the P450IIIA gene subfamily. This isozyme is one of the major forms involved in 2-hydroxylation of ethinylestradiol. Broad spectrum antibiotics have been implicated in causing pill failure; case reports document the interaction, and general practitioners are convinced that it is real. The problem remains that there is still no firm clinical pharmacokinetic evidence which indicates that blood concentrations of oral contraceptive steroids are altered by antibiotics. However, perhaps this should not be a surprise, given that the incidence of the interaction may be very low. It is suggested that an individual at risk will have a low bioavailability

  18. [Interactions between oral contraceptives and other drugs].

    PubMed

    Hansen, T H; Jensen, S B

    1991-10-28

    Failures of oral contraceptives are possible when combined with rifampicin or antiepileptics, especially phenobarbitone and phenytoin. The mode of action is shown by clinical trials to be due to induction of hepatic enzymes thus increasing the steroid metabolism. Failure or oral contraceptives has occurred with the concomitant use of antibiotics, i.e. ampicillin and sulfonamides. Clinical trials have focused upon the changes in the intestinal flora induced by antibiotics. This might influence the enterohepatic circulation of estrogen and thereby decrease reabsorption of estrogen, but this has not been definitely proved. The failures may be caused by individual pharmacokinetics of oral contraceptives. Oral contraceptives are able to influence the pharmacodynamics of various other drugs metabolized by oxidation or conjugation but besides an increased pharmacological effect of prednisolone and increased toxicity of imipramine the clinical importance is uncertain. PMID:1949335

  19. Oral contraceptives and birth defects.

    PubMed

    Smithells, R W

    1981-06-01

    Although OCs (oral contraceptives) are not designed to be taken during pregnancy, in Europe and the U.S. they are taken by 2-5% of women in early pregnancy and by 1/4-1/3 of women 3-4 months prior to conception. The effects of OCs on folic acid and other vitamin metabolism are well known and provide a theoretical basis for possible teratogenicity, even when stopped prior to conception. Both hormone support therapy for threatened abortions and hormonal pregnancy tests have been abandoned in recent years, the first because it proved inefficacious, the second because there are better alternatives available. In neither of these cases were sex hormones shown to be teratogenic. Most cohort (prospective) and many case-control (retrospective) studies have shown no association between OC use and birth defects. Case-control methodology can be criticized because of recall bias and because of the difficulty of choosing entirely matched controls. Several studies have shown OC users to have characteristics slightly different from the general population, e.g., they are younger, more often unmarried, and are more likely to smoke during pregnancy. Any of these characteristics might influence the occurrence of teratogenicity. It is impossible to prove that OCs constitute a low-level teratogen. The author considers them nonteratogenic. PMID:7250546

  20. Oral contraceptives and liver cancer.

    PubMed

    1997-11-01

    To date, nine case-control studies conducted in developed countries have identified an association between oral contraceptives (OCs) and liver cancer. The most recent population-based data from both developed and developing countries failed to confirm such an association, however. A study conducted by the World Health Organization in eight developing countries (Chile, China, Colombia, Israel, Kenya, Nigeria, Philippines, and Thailand), in which 122 women with liver cancer were matched with 802 controls, found no elevated risk for OC users compared with never-users (relative risk, 0.7; 95% confidence interval, 0.4-1.2). This study is particularly significant since it was conducted in countries where hepatitis B virus infection, an important risk factor for primary liver cancer, is widespread. In addition, population mortality data from the US, UK, Japan, and Sweden have failed to document increases in liver cancer cases coincident with increases in OC use. Given that population statistics can detect changes on the magnitude of a 40-50% decrease in the risk of ovarian and endometrial cancer related to OC use, they should be able to detect increases of two to 20 times the risk of liver cancer. The increased risk of liver cancer found in the case-control studies may reflect bias resulting from the small size of these studies. PMID:12348250

  1. Pharmacologic considerations for patients taking oral contraceptives.

    PubMed

    Hassan, T

    1987-03-01

    This is a brief review of the theoretical and known drug reactions with oral contraceptives. There are at least 6 possible types of drug reactions that may affect the action of oral contraceptives, not including malabsorption related to changes in intestinal motility or flora. Ampicillin is an example of an antibiotic that may cause diarrhea, thereby reducing absorption of pill steroids. The steroids in orals are subject to enterohepatic circulation, which is in turn affected by the gut flora. Antibiotics known to suppress gut flora include: penicillins, cephalosporins, tetracyclines, sulfas, neomycin and erythromycin. Although controlled clinical trials of antibiotic intake with oral contraception have not shown significant interactions, anecdotal reports of pill failures have been published. The other important drug interaction affecting contraception by orals is enhanced hepatic degradation, as seen with rifampicin. Other drugs such as cimetidine, MAO-inhibitor antidepressants, chloramphenicol, influenza or BCG vaccine, isoniazid, warfarin, metronidazole and disulfiram may delay steroid metabolism and possibly increase side effects. When prescribing drugs it is important to realize that certain drugs decrease oral contraceptive concentrations: antibiotics anticonvulsants, griseofulvin, purgatives and rifampicin. PMID:3155374

  2. Choosing a combined oral contraceptive pill

    PubMed Central

    Stewart, Mary; Black, Kirsten

    2015-01-01

    Summary The combined oral contraceptive pill is an effective contraceptive method which can also offer other benefits. However, other contraceptive options should be discussed. If the pill is the chosen method, prescribe a pill with the lowest effective dose of oestrogen and progestogen. Pills containing levonorgestrel or norethisterone in combination with ethinyloestradiol 35 microgram or less are considered first-line. They are effective if taken correctly, have a relatively low risk of venous thromboembolism, and are listed on the Pharmaceutical Benefits Scheme. The pill is usually taken in a monthly cycle. Some women may prefer an extended pill regimen with fewer or no inactive pills. PMID:26648603

  3. Assessment of Incremental Dosage Regimen of Combined Oestrogen-Progestogen Oral Contraceptive

    PubMed Central

    Brosens, I. A.; Robertson, W. B.; Van Assche, F. A.

    1974-01-01

    Eighty-six women of proved fertility used an incremental dosage regimen of a combined oral contraceptive for a total of 570 cycles over one year. A daily tablet containing 50 μg of ethinyloestradiol and 50 μg D-norgestrel was taken for 11 days and a daily tablet containing 50 μg ethinyloestradiol and 125 μg D-norgestrel for the next 10 days. Withdrawal bleeding occurred during the tabletfree interval of seven days. The new preparation proved to be an efficient contraceptive, well tolerated, and with few side effects. Women who had gained weight while taking other oral contraceptives lost weight when they changed to the new preparation. The regimen allowed a significant reduction in the cycle dose of progestogen, and these results suggest that a further reduction in the cycle dose of both oestrogen and progestogen may be possible without losing contraceptive efficiency. PMID:4441832

  4. [Oral contraceptives: knowledge and compliance].

    PubMed

    Koch, T; Marslew, U; Nielsen, M R

    1993-11-01

    One hundred and twenty (120) women, taking contraceptive pills, underwent a structured interview with a view elucidating their knowledge of the physiology of menstruation, the action and side effects of contraceptive pills and their compliance in the taking of contraceptive pills. The most important sources of information were the medical letters in magazines and the women's own doctors, while the teaching in the Folkeskole (primary and lower secondary school) had not had any major influence on the level of information. Well over one third of the interviewed women knew the most important action mechanism of the contraceptive pill, and half of the women could give a satisfactory explanation of the physiology of menstruation. Twenty-four percent (24%) thought that pregnancy could not occur until 1-2 months after the woman had ceased taking the pill. There was high compliance among the women i.e. that their behavior was correct when they had forgotten to take one or two contraceptive pills, when bleeding was irregular, and when beginning on a new package of pills. Eighty-three percent (83%) had experienced side effects that could be related to contraceptive pills. The investigation shows that there is a need for more efficient information about the effects of the Pill and about the physiology of menstruation. PMID:8236575

  5. Oral contraceptive marketing in Ibadan, Nigeria.

    PubMed

    Bamgboye, E A; Ladipo, O A

    1992-10-01

    The demographic transition in Nigeria is gradually moving towards the second stage. There is clear evidence of a declining mortality but the fertility rate remains exceptionally high. A realistic approach towards reducing fertility rate is the use of oral contraceptive. This study assesses the distribution system of oral contraceptive in Ibadan, the second largest city in Nigeria. The findings revealed that the people are aware of modern oral contraceptives as they purchase them freely at chemist shops. But effective distribution is hampered by existing channels and high costs. A local source recommended is the proprietary medicine stores, often at convenient locations to the potential users of contraceptives. The current cost which is between $1.3 and $19.5 per couple-years of protection is exorbitant, consuming 0.5-7.8% of the gross annual income of the average individual. Therefore, the government should subsidize the prices of oral contraceptives, to facilitate freedom from the tyranny of excessive fertility. PMID:1411690

  6. Reassessment of the metabolic effects of oral contraceptives.

    PubMed

    Franklin, M

    1990-01-01

    During the 30 years of experience with oral contraceptives, dramatic changes have occurred in their formulations and in prescribing practices. This article analyzes the latest information on the metabolic effects of oral contraceptives and makes recommendations for practice. PMID:2286849

  7. In vitro uptake of oral contraceptive steroids by magnesium trisilicate.

    PubMed

    Khalil, S A; Iwuagwu, M

    1978-02-01

    Some steroids used in oral contraceptives were adsorbed significantly by magnesium trisilicate. The adsorption affinity followed the sequence: ethindrone greater than mestranol greater than norethindrone greater than ethinyl estradiol. Adsorption data obtained at relatively low initial concentrations fitted a Langmuir plot; the values for monolayer adsorption ranged between 0.24 and 0.32 mg/g. At higher concentrations of the steroids, multilayer adsorption occurred. The results of desorption experiments made at 37 degrees in water and 0.05 N HCl suggested that desorption was incomplete and depended on the amount of steroid adsorbed. During the dissolution testing of a brand of contraceptive tablets containing norethindrone acetate, the presence of 0.5% (w/v) magnesium trisilicate in the medium resulted in almost complete reduction in the amount of the steroid remaining in solution after 1 hr. PMID:202691

  8. The Emotional Responses of Married Women Receiving Oral Contraceptives

    PubMed Central

    Ringrose, C. A. Douglas

    1965-01-01

    One hundred women taking oral contraceptives were questioned concerning their opinions about personal and sociological effects of this method of conception control. Fifty-three per cent reported improved coital satisfaction while 4% noted the opposite effect. Libido was increased in 22% and decreased in 13%. One woman in five believed that an increase in premarital and extramarital sexual activity would take place in the general population as a result of tablet-induced infertility. The problem of population control is discussed. It is paradoxical that the incidence of unplanned pregnancies continues to increase despite the availability of completely reliable conception control. This reflects present inability to communicate contraceptive knowledge to the appropriate people. PMID:14292887

  9. Oral contraceptives in polycystic ovary syndrome.

    PubMed

    Helvaci, N; Yildiz, B O

    2014-09-01

    Polycystic ovary syndrome (PCOS) is the most common endocrine disorder of women of reproductive age and combined oral contraceptives (OCs) are often the first-line treatment of the syndrome by improving hyperandrogenism and regulating menstrual cycles. Oral contraceptives have some cardiovascular and metabolic effects that varies among different formulations depending upon the dose and type of the both estrogen and progestin components. These cardiometabolic effects of OCs raise some concerns about their long-term use in PCOS, but available data suggest that the benefits outweigh the risks. More studies are needed to clarify the safety of long-term use of OCs in PCOS. PMID:25003228

  10. Benefits and risks of oral contraceptives.

    PubMed

    Sherif, K

    1999-06-01

    The major benefits of modern low-dose oral contraceptives include relative safety and a high degree of efficacy, decreasing the need for abortion or surgical sterilization; reduced risks of bacterial (but not viral) pelvic inflammatory disease and of endometrial and ovarian cancer; improved menstrual regularity, with less dysmenorrhea and blood flow; and, when low-dose combination (not progestogen-only) oral contraceptives are used, reduced acne and hirsutism. Major risks are cardiovascular. Preliminary data from nonrandomized studies suggest that oral contraceptives containing third-generation progestogens are associated with increased risk of venous thromboembolism, particularly in carriers of the coagulation factor V Leiden mutation. The risk of arterial thrombosis, such as myocardial infarction or stroke, may be directly related to estrogen dose, particularly in women who have hypertension, smoke, or are >35 years old. Considering that only users aged >/=30 years who smoke >/=25 cigarettes/d have a higher estimated mortality rate than that of pregnant women, the benefits of oral contraceptives appear to outweigh their risks. PMID:10368519

  11. An Oral Contraceptive Drug Interaction Study

    ERIC Educational Resources Information Center

    Bradstreet, Thomas E.; Panebianco, Deborah L.

    2004-01-01

    This article focuses on a two treatment, two period, two treatment sequence crossover drug interaction study of a new drug and a standard oral contraceptive therapy. Both normal theory and distribution-free statistical analyses are provided along with a notable amount of graphical insight into the dataset. For one of the variables, the decision on…

  12. Zoely: a new combined oral contraceptive.

    PubMed

    2014-08-01

    ▼Zoely is the second estradiol-containing oral contraceptive formulated as an 'extended regimen' (pill-free interval <7 days) to be licensed in the UK. However, unlike the quadraphasic estradiol-containing contraceptive Qlaira, it is a monophasic preparation.1,2 It is postulated that combined oral contraceptives (COCs) containing synthetic estradiol, which is structurally identical to endogenous oestrogen,3 are potentially safer and better tolerated than those containing ethinylestradiol, the synthetic oestrogen most commonly used in COCs.4 The progestogen in Zoely is nomegestrol acetate, which is structurally related to progesterone,5 in contrast to the majority of progestogens in COCs that are derived from 19-nortestosterone6 and associated with androgenic effects.7 It is suggested that nomegestrol acetate, with its greater specificity for progesterone receptors, may minimise the potential for androgenic, oestrogenic and glucocorticoid effects.7 The company considers Zoely an option for women "who want a contraceptive with hormones similar to her own", and claims that it has a high level of contraceptive efficacy, produces shorter, lighter periods compared with a 21-day regimen of drospirenone 3mg/ethinylestradiol 30µg (Yasmin) and that most women report no negative impact on weight and skin.8 Here we review the effectiveness and place of Zoely. PMID:25104773

  13. [Emergency oral contraception policy: the Peruvian experience].

    PubMed

    Pretell-Zárate, Eduardo A

    2013-07-01

    Emergency oral contraception is part of the sexual and reproductive rights of women. In 2001, this health policy was incorporated into the Rules of the National Family Planning Program of the Ministry of Health, primarily to prevent unwanted pregnancy and its serious consequences, induced abortion and the high associated maternal mortality rate, which are major public health problems. Scientific research has confirmed that the main mechanism of action of levonorgestrel, component of emergency oral contraception (EOC) is to inhibit or delay ovulation, preventing fertilization of the egg; additionally, it increases the thickening of the cervical mucus, making the sperm migration more difficult. No study has found endometrial abnormalities that may interfere with the implantation of the fertilized egg or embryo development of an implanted egg. However, despite the support of medical science and legal backing, the EOC is available only to users with economic resources, but its use has not been fully implemented in public sector services, due to obstacles created by groups opposed to contraception under claim of an alleged abortive effect that has already been ruled out scientifically. This article describes the administrative experience and legal confrontations between groups of power that prevent the proper implementation of an emergency contraception policy in Peru. PMID:24100827

  14. Intracranial venous thrombosis complicating oral contraception

    PubMed Central

    Dindar, F.; Platts, M. E.

    1974-01-01

    Four days after the onset of a severe headache a 22-year-old woman who had been taking oral contraceptives for less than three weeks had a convulsion, followed by right hemiparesis. Other focal neurologic signs and evidence of raised intracranial pressure appeared, and she became comatose on the seventh day. A left craniotomy revealed extensive cerebral venous thrombosis. She died the next day. On postmortem examination extensive thrombosis of the superior sagittal sinus and draining cerebral veins, and multiple areas of cerebral hemorrhage and hemorrhagic infarction were seen. Some of the superficial cerebral veins showed focal necrosis of their walls, and the lateral lacunae of the superior sagittal sinus contained proliferating endothelial cells. The adrenal veins were also thrombosed. The significance of these findings is discussed. The literature on cerebrovascular complications of oral contraception, particularly cerebral venous thrombosis, is reviewed. ImagesFIG. 1FIG. 2FIG. 3FIG. 4FIG. 5FIG. 6 PMID:4413961

  15. Vertebral artery occlusion and oral contraceptives.

    PubMed Central

    Ask-Upmark, E; Bickerstaff, E R

    1976-01-01

    If vertebral artery occlusion occurs in degenerative arterial disease it is almost invariably left-sided, but in vertebral artery deficiency syndromes associated with oral contraceptives a striking preponderance of right-sided involvement has been shown. This observation adds support to the view that causes other than changes in the wall of the vessel at the site of occlusion must be sought as an explanation of the occlusion. PMID:1252812

  16. Changing convention in combination oral contraceptives: estradiol and nomegestrol acetate in a monophasic 24/4 regimen.

    PubMed

    Shulman, Lee P

    2013-07-01

    Initial oral contraceptive regimens were characterised by high doses of ethinylestradiol (EE) and a progestogen in a 21-day regimen that either included seven additional hormone-free tablets or simply the 21 days of combination hormonal tablets. These regimens were developed to ensure high contraceptive effectiveness, regular and predictable withdrawal bleeding episodes to mimic a menstrual cycle, and minimal unscheduled vaginal bleeding. However, these regimens were associated with adverse tolerability and safety issues resulting from the dose and characteristics of their hormonal components. Attempts to ameliorate these adverse issues included the development of lower-dose EE regimens, the incorporation of new progestogens, multiphasic regimens, and reduced hormone-free interval regimens. However, the EE component has remained a constant until the recent approval of combination oral contraceptives with an estrogen component other than EE. The development and introduction of an estradiol-based oral contraceptive regimen is presented in this review. PMID:23709606

  17. Communication about Contraception and Knowledge of Oral Contraceptives amongst Norwegian High School Students.

    ERIC Educational Resources Information Center

    Hansen, Thomas; Skjeldestad, Finn Egil

    2003-01-01

    Examines communication about contraception and specific knowledge of oral contraceptives (OCs) in a sample of Norwegian high school students. More females than males discussed contraception at least monthly. Discussions were predominantly held with peers and not adults. Females were far more knowledgeable about OCs than males. The most significant…

  18. The Current Status of Oral Contraceptives: Progress and Recent Innovations.

    PubMed

    Golobof, Alexandra; Kiley, Jessica

    2016-05-01

    Millions of women in the United States and abroad use oral contraceptive pills. These popular contraceptives are the most common reversible birth control method in the United States, and a wide variety of pills are available for prescription. Oral contraceptives provide safe and effective protection against pregnancy and offer several noncontraceptive benefits. Over the years, advances in the laboratory and knowledge gained through epidemiologic data promoted the development of new contraceptive preparations. Generations of oral contraceptives emerged over time, containing lower doses of estrogens and new and novel progestins. The current review discusses the clinical characteristics of oral contraceptives, with emphasis on basic pharmacology and the evolution of various contraceptive formulations and regimens. PMID:26960906

  19. Effects of Administration of Fostamatinib on Blood Concentrations of an Oral Contraceptive in Healthy Female Subjects

    ClinicalTrials.gov

    2012-02-17

    Scientific Terminology Rheumatoid Arthritis, Healthy Female Volunteers, Pharmacokinetics, Oral Contraceptive, Drug-drug Interaction; Laymen Terminology Level of Oral Contraceptive in Blood, Oral Contraceptive, Rheumatoid Arthritis, Drug -Drug Interaction

  20. Factors related to choosing oral contraception at age 15.

    PubMed

    Kosunen, E; Laippala, P

    1996-12-01

    This report aims to identify factors which are related to use of oral contraceptives at an early age. A self-administered questionnaire was completed at schools in 1988 and 1992 in southern and western Finland (N = 1339). Sexually experienced girls (mean age 15.8 years) who had answered the question concerning their oral contraceptive use were included (N = 389). Logistic regression analysis was used to compare oral contraceptive users (N = 121) with the group of non-users. Total number of coital experiences was associated with oral contraceptive use: the odds ratio for those having at least 10 coital experiences was 6.30 compared with those with only one intercourse. The proportion was 73% among oral contraceptive users and 30% among non-users. Girls using oral contraceptives perceived more often (67%) that parents accept their sexual relationship (30% among non-users). Oral contraceptive users were less afraid of getting pregnant (9% compared with 31% among non-users) and felt more often that sex was very important in their life (31 and 13%, respectively). Other factors that entered the model were age at menarche, having a steady partner and frequency of disco visits. When a young girl asks for oral contraceptives, she is probably at true risk of pregnancy, and regular contraception should be considered both in view of effective prevention of pregnancies and sexually transmitted diseases. PMID:10163954

  1. Perceptions of contraceptive effectiveness and health effects of oral contraception.

    PubMed

    Tessler, S L; Peipert, J F

    1997-01-01

    The hypothesis that misperceptions about the effectiveness of contraceptive methods and the risks and benefits of oral contraceptive (OC) use are widespread in the US, even among the most educated population groups, was investigated in 147 women presenting to the Brown University (Providence, Rhode Island) health service and 189 students solicited by female volunteers on the campus. 90% of respondents correctly estimated the effectiveness of OCs in preventing pregnancy, but 32-34% inflated the pregnancy rates associated with subdermal implants and Depo-Provera. 60% overestimated the failure rate of the IUD. On the other hand, a majority underestimated the failure rates of barrier methods and spermicides. 41% believed OCs increase the risk of breast cancer and 33% thought the pill increases cervical cancer risk. 66% knew that OCs reduce dysmenorrhea and 50% were aware the pill decreases menstrual bleeding. However, the majority were unaware OCs reduce the risk of benign breast disease (95%), ectopic pregnancy (91%), pelvic inflammatory disease (90%), and anemia (89%). 81% were unaware of the protective effects of OCs against uterine cancer and 77% did not know they have a protective effect against ovarian cancer. In general, OC users were more aware of the health benefits of OCs than condom users. Finally, respondents were asked to rate their satisfaction with their current birth control method on a scale of 1-12. Mean satisfaction scores were significantly higher among OC users (10.3) than condom users (7.1). These findings indicate that, even among highly educated US women, misperceptions persist about the reliability of birth control, the risks of pregnancy, and the health effects of OCs. PMID:9439201

  2. Oral contraceptives in the immediate postpartum period.

    PubMed

    Hume, A L; Hijab, J C

    1991-04-01

    Although there is a critical need for effective contraception in the immediate postpartum period for women who are not breastfeeding, this need must be balanced against the inherent risks. The most effective form of contraceptive protection--oral contraceptives (OCs)--can present an increased risk of thromboembolism in the period after delivery. The thrombotic changes associated with pregnancy, and the statistics and vascular damage following a delivery, can combine to create greater potential for thromboembolism after delivery than during pregnancy. Reported here is the case of a 21-year-old woman who, 4 weeks postpartum, developed pain and swelling in the right lower calf and mottled discoloration extending from the proximal thigh to the toes. A diagnosis of deep venous thrombosis was made and heparin was administered. In the hospital, the patient experienced pleuritic chest pain and diaphoresis. A ventilation-perfusion scan indicated a pulmonary embolism. 1 week after delivery, the patient had initiated use of Triphasil. Although this woman had other risk factors (obesity, light cigarette smoking, and a sedentary life-style), OC use in the immediate postpartum period may have been the final factor precipitating the thromboembolic event. It is recommended that OC use should be delayed until at least 2 weeks postpartum in women without other risk factors for thromboembolism and until 4-6 weeks postpartum in those with such factors. PMID:2010744

  3. Spontaneous hepatic hemorrhage secondary to prolonged use of oral contraceptives.

    PubMed

    Jaffar, Reema; Pechet, Liberto; Whalen, Giles Francis; Banner, Barbara F

    2010-05-15

    Oral contraceptive pills (OCP) are the most commonly used form of contraception throughout the United States of America. The prolonged usage of oral contraceptives leads to a variety of complications, ranging from subclinical modifications of liver function tests to the development of benign and malignant tumors of the liver. Spontaneous hepatic hemorrhage secondary to oral contraceptive use was only reported once in the early 1980s. We report a case of spontaneous hepatic hemorrhage secondary to prolonged ingestion of combined OCPs followed by multiple pulmonary emboli without underlying thrombophilia. PMID:19577854

  4. Striae distensae of augmented breasts after oral contraceptive therapy.

    PubMed

    Har-Shai, Y; Barak, A; Taran, A; Weissman, A

    1999-02-01

    A case of striae distensae (SD) of bilateral augmented breasts following oral contraceptive therapy is presented. Striae maturation and the prevention of additional skin marks was achieved with immediate cessation of oral contraceptive pill therapy and long-term daily topical application of tretinoin cream. It is suggested that patients who are candidates for breast augmentation surgery should be informed of the possible risk of developing SD if they are taking or planning to take the contraceptive pill. PMID:10029486

  5. Affective and Physical Changes Associated with Oral Contraceptive Use.

    ERIC Educational Resources Information Center

    Wiener, Alane L.; And Others

    Although investigations of the physiological effects of oral contraceptives suggest that affective changes may accompany their use, empirical documentation of these effects has not been consistent. This study examined physiological and affective changes accompanying use of a low-dosage oral contraceptive while controlling for possible expectancy…

  6. [Inefficacy of oral contraception during use of minocycline].

    PubMed

    de Groot, A C; Eshuis, H; Stricker, B H

    1990-06-23

    A healthy woman aged 21 years who used the oral contraceptive Trigynon became pregnant while being treated with Minocin (minocycline; 100 mg per day) for acne conglobata. While the risk of use of antibiotics such as this one reducing the efficacy of oral contraceptives is small, patients should nevertheless be informed that the risk exists. PMID:2143563

  7. Evaluation of extended and continuous use oral contraceptives

    PubMed Central

    Wright, Kristen Page; Johnson, Julia V

    2008-01-01

    Oral contraceptives are classically given in a cyclic manner with 21 days of active pills followed by 7 days of placebo. In the past 4 years, new oral contraceptives have been introduced which either shorten the placebo time, lengthen the active pills (extended cycle), or provide active pills every day (continuous). These concepts are not new; extended and continuous pills were first studied in the 1960s and 1970s and have been provided in an off-label manner by gynecologists to treat menstrual disorders, such as menorrhagia and dysmenorrhea, and gynecologic disorders, such as endometriosis. Now that extended and continuous combined oral contraceptives are available for all patients, it is critical for providers to understand the physiology, dosing, side effects, and benefits of this form of oral contraceptive. This article reviews the history and the potential uses of the new continuous combined oral contraceptive. PMID:19209272

  8. [Cholestatic icterus due to oral contraceptives].

    PubMed

    Pestel, M; Lambert, C; Jeanmougin, M

    1973-03-01

    A case report of cholestatic jaundice in a 25 year old woman, who had had jaundice at age 4 years, and had taken Stediril (a combined oral contraceptive) for 1 month, implicates either the pill or a possibly hereditary hyperlipidemia. The jaundice developed in 2 weeks with vomiting, epigastric pain, anorexia, then discolored urine and feces, and intense pruritus. On hospitalization the patient had moderate bilirubinemia (56 mg/1), low alkaline phosphatase (13 U.K.) and slightly high serum glutamate pyruvate transaminase (270 U.W.). There were elevated serum cholesterol (3 gm/1), triglycerides (2.05 gm/1), total lipids (10.6 gm/1), and a definitely increased pre-beta lipoprotein, suggesting hyperlipidemia type IV (Frederickson classification). Liver biopsy showed fibrosis of the portal spaces lymphocytic infiltration, canalicular and intrahepatocytic thrombi. On laparoscopy the liver had a regular lower border, normal volume color and surface. Albumin, prothrombin and flocculation tests were normal. The patient's jaundice lasted about 1 month, then liver function slowly improved, although pruritus remained intense. Probably this jaundice was due to oral contraceptives, in a patient predisposed either by jaundice in childhood or endogenous hyperlipidemia. PMID:4268576

  9. Contraceptives.

    PubMed

    1997-01-01

    This chart sets forth brief descriptions of 14 contraceptive methods: male condom, female condom, vaginal diaphragm and cap, spermicides, oral contraceptives, hormonal implants, injectables, IUD, natural family planning, fertility awareness, breast feeding, withdrawal, sterilization, and emergency contraception. After presenting a short description of each method, the chart rates its degree of protection from pregnancy, the protection provided against HIV and other sexually transmitted diseases, its availability, and the method's advantages and disadvantages. PMID:12348240

  10. Nomegestrol acetate-17b-estradiol for oral contraception

    PubMed Central

    Burke, Anne

    2013-01-01

    Oral contraceptives remain a popular method of contraception over 50 years after their introduction. While safe and effective for many women, the failure rate of oral contraception is about 8%. Concerns about the risk of venous thromboembolism continue to drive the search for the safest oral contraceptive formulations. The oral contraceptive NOMAC-E2 contains nomegestrol acetate (NOMAC) 2.5 mg + 17b-estradiol (E2) 1.5 mg. The approved dosing regimen is 24 days of active hormone, followed by a 4-day hormone-free interval. NOMAC is a progestin derived from testosterone, which has high bioavailability, rapid absorption, and a long half-life. Estradiol, though it has a lower bioavailability, has been successfully combined with NOMAC in a monophasic oral contraceptive. Two recently published randomized controlled trials demonstrate that NOMAC-E2 is an effective contraceptive, with a Pearl Index less than one pregnancy per 100 woman-years. The bleeding pattern on NOMAC-E2 is characterized by fewer bleeding/spotting days, shorter withdrawal bleeds, and a higher incidence of amenorrhea than the comparator oral contraceptive containing drospirenone and ethinyl estradiol. The adverse event profile appears to be acceptable. Few severe adverse events were reported in the randomized controlled trials. The most common adverse events were irregular bleeding, acne, and weight gain. Preliminary studies suggest that NOMAC-E2 does not seem to have negative effects on hemostatic and metabolic parameters. While no one oral contraceptive formulation is likely to be the optimum choice for all women, NOMAC-E2 is a formulation with effectiveness comparable with that of other oral contraceptives, and a reassuring safety profile. PMID:23836965

  11. Nomegestrol acetate-17b-estradiol for oral contraception.

    PubMed

    Burke, Anne

    2013-01-01

    Oral contraceptives remain a popular method of contraception over 50 years after their introduction. While safe and effective for many women, the failure rate of oral contraception is about 8%. Concerns about the risk of venous thromboembolism continue to drive the search for the safest oral contraceptive formulations. The oral contraceptive NOMAC-E2 contains nomegestrol acetate (NOMAC) 2.5 mg + 17b-estradiol (E2) 1.5 mg. The approved dosing regimen is 24 days of active hormone, followed by a 4-day hormone-free interval. NOMAC is a progestin derived from testosterone, which has high bioavailability, rapid absorption, and a long half-life. Estradiol, though it has a lower bioavailability, has been successfully combined with NOMAC in a monophasic oral contraceptive. Two recently published randomized controlled trials demonstrate that NOMAC-E2 is an effective contraceptive, with a Pearl Index less than one pregnancy per 100 woman-years. The bleeding pattern on NOMAC-E2 is characterized by fewer bleeding/spotting days, shorter withdrawal bleeds, and a higher incidence of amenorrhea than the comparator oral contraceptive containing drospirenone and ethinyl estradiol. The adverse event profile appears to be acceptable. Few severe adverse events were reported in the randomized controlled trials. The most common adverse events were irregular bleeding, acne, and weight gain. Preliminary studies suggest that NOMAC-E2 does not seem to have negative effects on hemostatic and metabolic parameters. While no one oral contraceptive formulation is likely to be the optimum choice for all women, NOMAC-E2 is a formulation with effectiveness comparable with that of other oral contraceptives, and a reassuring safety profile. PMID:23836965

  12. Oral contraception for women of middle age.

    PubMed

    Ruan, Xiangyan; Mueck, Alfred O

    2015-11-01

    Women at middle age have decreased fertility and their pregnancies are higher risk. Combined oral contraceptives (COC) are effective but confer increased risk of age-related diseases, especially cardiovascular diseases. These risks are lower, however, with progestogen-only pills (POP). Therefore, other than the levonorgestrel intrauterine device (LNG-IUD), POP are usually the first choice, even though they do often lead to bleeding problems, which are already frequent in the perimenopause. However, the main risk of COC, venous thromboembolism, seems not to be relevant in (non-hospitalized) Chinese women and perhaps also other Asian women. COC may therefore be in fact a better choice than POP for these groups. In contrast to POP and IUDs, they have a variety of benefits especially important for middle-aged women, including a large decrease of the risk of ovarian, endometrial and colorectal cancer, an improvement in bleeding irregularities, a reduction of climacteric symptoms and some protection against bone loss. Further research is needed into individualized and safe contraception that takes into account ethnicity, as well as other factors. PMID:26163075

  13. Do antibiotics decrease effectiveness of oral contraceptives?

    PubMed

    Cottet, C

    1996-09-01

    The number of accidental pregnancies occurring in oral contraceptive (OC) users who are concurrently taking certain antibiotics and antifungal agents exceeds the 1% failure rate associated with OCs, suggesting some form of drug interaction. Two mechanisms of action have been proposed to explain this phenomenon. First, drugs such as rifampin and griseofulvin induce liver enzymes that break down the estrogen and progestin contained in OCs, reducing plasma hormone levels. Second, changes in the intestinal bacterial flora induced by penicillin and tetracycline may reduce the gut's absorption of hormones, also compromising efficacy. Since rifampin and griseofulvin are the medications most frequently implicated in accidental pregnancies in OC users, the induction of liver enzymes is the more probable, potent cause of failure. Although the risk of pregnancy due to OC-antibiotic interactions is extremely small, OC users prescribed antibiotics should be warned to use condoms or spermicides until the antibiotics are discontinued. PMID:9006212

  14. [Hormonal contraception using the oral depot preparation, Deposiston].

    PubMed

    Vasilev, D

    1978-01-01

    The efficacy of a new contraceptive delayed-action preparation, Deposiston is reviewed. Deposiston is the estrogen-progestin preparation with predominant estrogen activity. The estrogen and progestin eomponents of the preparation are ehtinyl estradiol and norethindrone acetate, respectively. Contraceptive effect is associated with gonadotropic stimulation by estrogen component, while progestin component provides the thermogenic effect. Mutagenicity, carcinogenicity, and toxicity tests show safety of Deposiston. Clinical trials of Deposiston in 815 women over the period of 16,207 cycles (18.1 cycles/woman) confirm contraceptive efficacy of the preparation: pregnancy occurred in only 12 women. Side effects of Deposiston include nausea (16.06%), vomiting (3.7%), headache (5.08%), and vaginal discharge (11.86%). Each Deposiston package contains 3 white estrogen tablets and 2 red progestin tablets. A woman starts to take Deposiston on day 4 of the cycle: white tablets are taken on days 4, 11, and 18 and 2 red tablets are taken on day 25. On day 2-7 after the red progestin tablets, the woman experiences hemorrhage. Average duration of and the amount of blood loss during the hemorrhage do not differ from those during the normal menstruation. Deposiston is indicated for women with recurrent uterine hemorrhages, gastrointestinal disorders, and decreased libido. The preparation is contraindicated for adolescents younger than 16 years of age, for women with hormonal active tumors, thromboembolism, chronic liver diseases, and idiopathic jaundice. PMID:350070

  15. First time issue of oral hormonal contraception by nurses.

    PubMed

    Presho, M; Leadbetter, C

    1999-10-01

    This study aimed to assess whether introducing the issue of first time oral hormonal contraception by nurses could expand the role of the family planning nurse and improve the service to the client group. Nurse acceptability of, and adherence to, the protocol were examined. Results indicate that with appropriate training the first time issue of oral hormonal contraception is a valuable skill in enhancing the nurses' role, reduces waiting time for clients and is acceptable to clients. PMID:10567062

  16. Does the use of oral contraception depress DZ twinning rates?

    PubMed

    Campbell, D; Thompson, B; Pritchard, C; Samphier, M

    1987-01-01

    Data based on total births from a geographically defined population with zygosity determined from blood samples and placentation and with data on the use of oral contraceptives routinely collected in early pregnancy showed no association between oral contraceptive use prior to pregnancy in either MZ or DZ twinning. Three mutually exclusive control groups of singletons were used to take account of age, parity and secular trends. PMID:3451649

  17. [Individualization of low-dose oral contraceptives. Pharmacological principles and practical indications for oral contraceptives].

    PubMed

    Cianci, A; De Leo, V

    2007-08-01

    The contraceptive pill has been a revolution of the last 40 years. In Italy, however, it is much less widely used than in other countries. Explanations for this phenomenon range from religious implications and customs to misinformation and word-of-mouth communication of negative experiences. The oral contraceptive pill is often used to correct menstrual disorders, leading to poor results and side-effects. Recent advances in oral contraception have led to a substantial reduction in doses and side-effects. Low-dose pills contain minimal doses of progesterones and estrogens and ensure good control of the menstrual cycle. Although reduction of ethinyl estradiol (EE) concentrations has reduced the incidence of negative systemic side effects such as water retention, edema and swollen breasts, the low estrogen dose may be associated with spotting and hypomenorrhea or amenorrhea in the long term, as well as dyspareunia due to reduced vaginal trophism, which may induce women to suspend use of the drug. It is also true that only one type of estrogen is used in the pill, albeit at different doses, whereas the progesterone may differ and in many cases is the cause of common side-effects. The choice of progesterone therefore involves not only its effect on the endometrium in synergy with estrogen, but also possible residual androgenic activity which may have negative metabolic repercussions. Indeed, addition of a progesterone, especially androgen-derived, attenuates the positive metabolic effects of estrogen. Two new monophasic oral contraceptives were recently released. They contain 30 microg (Yasmin) or 20 muicrog (Yasminelle) EE and a new progesterone, drospirenone, derived from spirolactone, which has antiandrogenic and antimineralcorticoid activity similar to endogenous progesterone. Like progesterone, the drospirenone molecule is an aldosterone antagonist and has a natriuretic effect that opposes the sodium retention effect of EE. It may, therefore, help to prevent the

  18. Pharmacokinetic and pharmacodynamic drug interactions between antiretrovirals and oral contraceptives.

    PubMed

    Tittle, Victoria; Bull, Lauren; Boffito, Marta; Nwokolo, Nneka

    2015-01-01

    More than 50 % of women living with HIV in low- and middle-income countries are of reproductive age, but there are limitations to the administration of oral contraception for HIV-infected women receiving antiretroviral therapy due to drug-drug interactions caused by metabolism via the cytochrome P450 isoenzymes and glucuronidation. However, with the development of newer antiretrovirals that use alternative metabolic pathways, options for contraception in HIV-positive women are increasing. This paper aims to review the literature on the pharmacokinetics and pharmacodynamics of oral hormonal contraceptives when given with antiretroviral agents, including those currently used in developed countries, older ones that might still be used in salvage regimens, or those used in resource-limited settings, as well as newer drugs. Nucleos(t)ide reverse transcriptase inhibitors (NRTIs), the usual backbone to most combined antiretroviral treatments (cARTs) are characterised by a low potential for drug-drug interactions with oral contraceptives. On the other hand non-NRTIs (NNRTIs) and protease inhibitors (PIs) may interact with oral contraceptives. Of the NNRTIs, efavirenz and nevirapine have been demonstrated to cause drug-drug interactions; however, etravirine and rilpivirine appear safe to use without dose adjustment. PIs boosted with ritonavir are not recommended to be used with oral contraceptives, with the exception of boosted atazanavir which should be used with doses of at least 35 µg of estrogen. Maraviroc, an entry inhibitor, is safe for co-administration with oral contraceptives, as are the integrase inhibitors (INIs) raltegravir and dolutegravir. However, the INI elvitegravir, which is given in combination with cobicistat, requires a dose of estrogen of at least 30 µg. Despite the growing evidence in this field, data are still lacking in terms of large cohort studies, randomised trials and correlations to real clinical outcomes, such as pregnancy rates, in women

  19. 21 CFR 310.501 - Patient package inserts for oral contraceptives.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... comparing the effectiveness of oral contraceptives to other methods of contraception. (4) A boxed warning... indications in addition to contraception that are identified in the professional labeling for the drug...

  20. 21 CFR 310.501 - Patient package inserts for oral contraceptives.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... comparing the effectiveness of oral contraceptives to other methods of contraception. (4) A boxed warning... indications in addition to contraception that are identified in the professional labeling for the drug...

  1. 21 CFR 310.501 - Patient package inserts for oral contraceptives.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... comparing the effectiveness of oral contraceptives to other methods of contraception. (4) A boxed warning... indications in addition to contraception that are identified in the professional labeling for the drug...

  2. 21 CFR 310.501 - Patient package inserts for oral contraceptives.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... comparing the effectiveness of oral contraceptives to other methods of contraception. (4) A boxed warning... indications in addition to contraception that are identified in the professional labeling for the drug...

  3. 21 CFR 310.501 - Patient package inserts for oral contraceptives.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... comparing the effectiveness of oral contraceptives to other methods of contraception. (4) A boxed warning... indications in addition to contraception that are identified in the professional labeling for the drug...

  4. Teenagers' perceptions of unplanned adolescent pregnancies and oral contraceptive use.

    PubMed

    White, J E; Kellinger, K G

    1989-01-01

    Adolescent women who are sexually active often do not use contraceptives consistently and correctly. Adolescents are sexually active for an average of 15 months before initiating regular contraceptive use and the majority of young women who initiate use discontinue within the first year after initiation. This study enrolled 50 young women who initiated oral contraceptive use and was designed to provide more understanding of their perceptions about the possibility of an unplanned pregnancy and about contraceptive use. They were again contacted 6 weeks after initiation of oral contraceptives to assess continuation. Findings revealed that 90% of the subjects were sexually active at the time of the first visit; the mean period of sexual activity was 15 months. Only 30% had used a nonprescription birth control method during this period. While perceiving themselves to be highly susceptible to pregnancy, many young women continue to have psychosocial barriers to contraceptive use. Follow-up contact revealed more than 10% of the subjects were not using oral contraceptives. PMID:2631927

  5. Factors affecting the enterohepatic circulation of oral contraceptive steroids.

    PubMed

    Orme, M L; Back, D J

    1990-12-01

    Oral contraceptive steroids may undergo enterohepatic circulation, but it is relevant for only estrogens, because these compounds can be directly conjugated in the liver. Animal studies show convincing evidence of the importance of the enterohepatic circulation, but studies in humans are much less convincing. The importance of the route and the rate of metabolism of ethinyl estradiol are reviewed. Some antibiotics have been reported anecdotally to reduce the efficacy of oral contraceptive steroids, but controlled studies have not confirmed this observation. Although gut flora are altered by oral antibiotics, the blood levels of ethinyl estradiol are not reduced, and one antibiotic at least (cotrimoxazole) enhances the activity of ethinyl estradiol. PMID:2256523

  6. Influence of combined oral contraceptives on the periodontal condition

    PubMed Central

    DOMINGUES, Roberta Santos; FERRAZ, Bruna Fidêncio Rahal; GREGHI, Sebastião Luiz Aguiar; de REZENDE, Maria Lúcia Rubo; PASSANEZI, Euloir; SANT'ANA, Adriana Campos Passanezi

    2012-01-01

    Most studies investigating the impact of oral contraceptives have been performed some years ago, when the level of sexual hormones was greater than the actual formulations. Objective The aim of this study was to evaluate the effects of current combined oral contraceptives (COC) on periodontal tissues, correlating the clinical parameters examined with the total duration of continuous oral contraceptive intake. Material and methods Twenty-five women (19-35 years old) taking combined oral contraceptives for at least 1 year were included in the test group. The control group was composed by 25 patients at the same age range reporting no use of hormone-based contraceptive methods. Clinical parameters investigated included pocket probing depth (PD), clinical attachment level (CAL), sulcular bleeding index (SBI) and plaque index (Pl.I). Data were statistically evaluated by unpaired t test, Pearson's correlation test and Spearman's correlation test. Results The test group showed increased PD (2.228±0.011 x 2.154±0.012; p<0.0001) and SBI (0.229±0.006 x 0.148±0.005, p<0.0001) than controls. No significant differences between groups were found in CAL (0.435±0.01 x 0.412±0.01; p=0.11). The control group showed greater Pl.I than the test group (0.206±0.007 x 0.303±0.008; p<0.0001). No correlation between the duration of oral contraceptive intake, age and periodontal parameters was observed. Conclusions These findings suggest that the use of currently available combined oral contraceptives can influence the periodontal conditions of the patients, independently of the level of plaque accumulation or total duration of medication intake, resulting in increased gingival inflammation. PMID:22666846

  7. Chlamydia trachomatis and oral contraceptive use: a quantitative review.

    PubMed Central

    Cottingham, J; Hunter, D

    1992-01-01

    OBJECTIVES--Chlamydia trachomatis is now recognised as a major sexually transmitted disease; oral contraceptive use is rapidly increasing particularly in developing countries. There are thus important public health implications of the many reports that isolation of C trachomatis is more frequent among users of oral contraceptives. The aim of this analysis was to assess the strength and consistency of this association by summarising published studies between 1972 and 1990. DESIGN--Studies identified were grouped according to whether they were prospective or case-control studies. Data were extracted and pooled estimates of the unadjusted odds ratios were made for all studies, as well as for sub-groups defined by an index of study quality, background prevalence of C trachomatis, and the contraceptive comparison being made. LOCATION--Studies in the analysis were mainly conducted in Europe and North America; the meta-analysis was done at the Harvard School of Public Health, Boston, MA, USA. RESULTS--The pooled estimated unadjusted odds ratio for 29 case-control studies examined was 1.93 (95% CI, 1.77-2.11), indicating an almost twofold increased risk of chlamydial infection for oral contraceptive users. Neither study quality nor prevalence of C trachomatis modified this risk. When compared to the use of barrier contraceptives, however, the risk of infection for women using oral contraceptives increased to 2.91 (95% CI, 1.86-4.55). The pooled estimated protective effect of barrier methods in these studies was 0.34 (95% CI, 0.22-0.54). CONCLUSIONS--Cross-study comparisons of the relationship between oral contraceptive use and chlamydial infection are limited by the design and analysis of many component studies which did not control for confounding factors such as sexual behaviour and age. The almost twofold risk of increased chlamydial infection for oral contraceptive users, supported by the findings of two prospective studies, however, points to the importance of

  8. How can we improve oral contraceptive success in obese women?

    PubMed Central

    Cherala, Ganesh; Edelman, Alison

    2015-01-01

    Summary A rapid increase in obesity rates worldwide further underscores the importance of better understanding the pharmacokinetic alterations in this sub-population and the subsequent effects on pharmaco-therapeutics. Pharmacokinetics of contraceptive steroids are altered in obese oral contraceptive users which may in turn impact efficacy. Our work has identified several dosing strategies that offset these pharmacokinetic changes and may improve effectiveness for obese OC users. PMID:25354219

  9. Physiologic and psychologic symptoms associated with use of injectable contraception and 20 µg oral contraceptive pills

    PubMed Central

    Berenson, Abbey B.; Odom, Susan D.; Radecki Breitkopf, Carmen; Rahman, Mahbubur

    2013-01-01

    Objective To compare menstrual, physiologic, and psychologic symptoms over 2 years among women initiating use of depot medroxyprogesterone acetate or an oral contraceptive pill with a reduced pill-free interval, and those not using hormonal contraception. Methods A total of 608 women reported their experience regarding 17 symptoms prior to initiating contraception and every 6 months thereafter for 24 months. Longitudinal relationships between symptoms and contraceptives were assessed after adjusting for age, visits, and baseline status of symptoms. Results Oral contraceptive pills were protective against mastalgia (OR = 0.7), cramping (OR = 0.5), hair loss (OR = 0.6), acne (OR = 0.4), nervousness (OR = 0.5), and mood swings (OR = 0.7). DMPA was protective against bloating (OR = 0.5) and mood swings (OR = 0.7), but caused weight gain (OR = 2.3), bleeding episodes >20 days (OR = 13.4), and missed periods (OR = 96.9). Both methods caused intermenstrual bleeding. Conclusion Evidence-based data regarding beneficial and adverse symptoms associated with these methods may help clinicians counsel patients appropriately prior to contraceptive initiation. PMID:18599013

  10. Comparison of recalled and validated oral contraceptive histories.

    PubMed

    Nischan, P; Ebeling, K; Thomas, D B; Hirsch, U

    1993-11-01

    From a case-control study of the relation between oral contraceptives and breast cancer carried out in East Germany during 1982-1986, the authors obtained information on oral contraceptive use through interviews of study subjects and from the records of prescribing gynecologists. The degree of agreement regarding information from these two sources was assessed for 234 breast cancer cases and 524 controls who had ever used oral contraceptives. Agreement between information obtained from medical records and that from interviews on total duration of use, number of episodes of use, and time since first and last use was reasonably good, and levels of agreement did not differ appreciably between cases and controls. Lower levels of agreement were observed for individual brand names and the duration of use of specific brands. Attempts should be made to obtain information on specific brands from medical records when investigating the effects of individual preparations. PMID:8237985

  11. Nonspecific side effects of oral contraceptives: nocebo or noise?

    PubMed

    Grimes, David A; Schulz, Kenneth F

    2011-01-01

    Side effects of combined oral contraceptives are the most common reason why women discontinue them. Over the past half century, an elaborate mythology about these ill effects has evolved, fueled by rumor, gossip and poor-quality research. In contrast, placebo-controlled randomized trials document that nonspecific side effects are not significantly more common with combined oral contraceptives than with inert pills. These reported nonspecific side effects may reflect the nocebo phenomenon (the inverse of a placebo): if women are told to expect noxious side effects, these complaints occur because of the power of suggestion. Alternatively, nonspecific complaints may simply reflect their background prevalence in the population. Because Level I evidence documents no important increase in nonspecific side effects with oral contraceptives, counseling about these side effects or including them in package labeling is unwarranted and probably unethical. When in doubt, clinicians should err on the side of optimism. PMID:21134497

  12. Serum lipids and proteins during treatment with a new oral contraceptive combination containing desogestrel.

    PubMed

    Penttilä, I M; Bergink, E W; Holma, P; Hulkko, S; Makkonen, M; Pyörälä, T; Castrén, O

    1983-12-01

    The present study was carried out to measure lipid and protein levels in serum of healthy women during treatment with a new oral contraceptive combination containing 0.075 mg desogestrel (Org 2969, 17 alpha-ethinyl-18-methyl-11-methylene-4-estren-17-ol) plus 0.050 mg ethinyloestradiol per tablet. All 30 volunteers took 1 tablet daily for 21 consecutive days, followed by a tablet-free period of 7 days. Treatment lasted 3 months. At the end of treatment serum total cholesterol had increased by 0.26 mmol/l (5.0%), high-density lipoprotein-cholesterol by 0.22 mmol/l (15.2%) and triglycerides by 0.43 mmol/l (50%); the calculated low-density lipoprotein cholesterol had decreased by 0.16 mmol/l (4.9%). All lipid concentrations had returned to initial levels 2 months after treatment stopped. After 3 months treatment serum ceruloplasmin, cortisol-binding globulin capacity, sex-hormone-binding globulin capacity and thyroxine-binding globulin had significantly increased by 85.2, 133, 206 and 101%, respectively. All protein levels returned to normal 2 months after treatment stopped. The relationship between serum lipids and hormone-binding proteins has been discussed, as well as the significance of the high-density lipoprotein level with regard to contraceptive treatment. PMID:6232161

  13. Ziprasidone and the pharmacokinetics of a combined oral contraceptive

    PubMed Central

    Muirhead, G J; Harness, J; Holt, P R; Oliver, S; Anziano, R J

    2000-01-01

    Aims To determine whether multiple doses of ziprasidone alter the steady-state pharmacokinetics of the component steroids, ethinyloestradiol and levonorgestrel, of an oral contraceptive; to evaluate the tolerability of a co-administered combined oral contraceptive and ziprasidone; and to compare plasma concentrations of prolactin in subjects taking a combined oral contraceptive with placebo or ziprasidone. Methods Nineteen women taking a combined oral contraceptive (ethinyloestradiol 30 µg day−1 and levonorgestrel 150 µg day−1) were enrolled into a double-blind, placebo-controlled, two-way crossover study. They received ziprasidone 40 mg day−1 in two divided daily doses or placebo for 8 days (days 8–15) in one of two 21 day treatment periods separated by a 7 day washout period. Venous blood samples were collected immediately before and up to 24 h after the morning dose of oral contraceptive and ziprasidone or placebo on day 15 of each 21 day treatment period. These were assayed for ethinyloestradiol and levonorgestrel and the resulting data used to derive pharmacokinetic data for these steroids. Additional samples were collected immediately before and 4 h after the morning dose of oral contraceptive and ziprasidone or placebo on day 15 of each 21 day treatment period for prolactin assay. All observed and volunteered adverse events were recorded throughout the study. Results The mean AUC(0,24 h), Cmax and tmax for ethinyloestradiol and the mean AUC(0,24 h) and Cmax for levonorgestrel during ziprasidone co-administration were not statistically significantly different from corresponding values occurring during placebo co-administration. The tmax for levonorgestrel was approximately 0.5 h longer. Concomitant therapy with a combined oral contraceptive and ziprasidone did not result in adverse events not previously seen with either preparation alone. Conclusions The findings of this study suggest that, based on pharmacokinetic and tolerability data, ziprasidone

  14. Iron supplementation: oral tablets versus intramuscular injection.

    PubMed

    Dawson, Brian; Goodman, Carmel; Blee, Tanya; Claydon, Gary; Peeling, Peter; Beilby, John; Prins, Alex

    2006-04-01

    Non-anemic, iron depleted women were randomly assigned to an injection group (IG) or oral group (OG) to assess which method is more efficient for increasing iron stores over a short time period. IG received a course of 5 x 2 mL intramuscular injections over 10 d, and OG received one tablet daily for 30 d. Fourteen, 21 and 28 d after commencing supplementation, ferritin concentration in OG significantly increased from baseline (means +/- standard error: 27 +/- 3 to 40 +/- 5 to 41 +/- 5 to 41 +/- 5 microg/L; P < 0.01). Similarly, on days 15, 20, and 28 post the first injection, ferritin concentration in IG significantly increased from baseline (means +/- standard error: 20 +/- 2 to 71 +/- 17 to 63 +/- 11 to 63 +/- 7 microg/L; P < 0.01), and was also significantly greater than OG at day 15 and 28 (P < 0.05). Iron injections are significantly more effective (both in time and degree of increase) in improving ferritin levels over 30 d than oral tablets. PMID:16779924

  15. Oral contraceptives and venous thrombosis: end of the debate?

    PubMed

    Skouby, S O

    1998-06-01

    During the more than 30-year history of oral contraceptives, clinicians have received several official warnings issued by regulating agencies on cardiovascular risks. These have affected not only gynecological practice, but also generated research activities resulting in the refined third-generation products marketed in the 1970s. The alert sent out by the UK Committee on Safety of Medicines (CSM), October 1995, on increased risk of deep venous thrombosis during use of these compounds was, therefore, very much unexpected. The statements were referring to unpublished data and, thus, indicated new and highly alarming findings. However, during the following months, although four epidemiological studies reported a 2-4 fold relative increase compared with the second-generation oral contraceptives. This relative increase means, looking at absolute risks, an excess of 1-2 cases of deep venous thrombosis per 10,000 oral contraceptive users per year. In the academic discussions following the primary publication of the four papers, the possibility of confounding factors and bias was strongly emphasized and follow-up studies together with re-analysis of the original studies have not generated evidence for the suspicion of the increased risk with third-generation oral contraceptives. In contrast, a decreasing tendency was demonstrated for more serious events such myocardial infarction. Also, the biological plausibility for increased risk of deep venous thrombosis with third-generation products is lacking, although one study has pointed to a change in the natural anticoagulatory mechanism. Obviously, the authorities have a right to react on suspicion, but the psychological and social effects of the abrupt stopping of oral contraceptive use should not be ignored, and the public understanding of scientific results is manipulated by the mass media. Following confirmed evidence from both epidemiological and biological studies, with full acknowledgement of the contraceptive and non-contraceptive

  16. Laryngeal Aerodynamics Associated with Oral Contraceptive Use: Preliminary Findings

    ERIC Educational Resources Information Center

    Gorham-Rowan, Mary; Fowler, Linda

    2009-01-01

    The purpose of this study was to examine possible differences in laryngeal aerodynamic measures during connected speech associated with oral contraceptive (OC) use. Eight women taking an OC, and eight others not taking an OC, participated in the study. Three trials of syllable /p[subscript alpha] /repetitions were obtained using a…

  17. Adherence to a flexible extended regimen for oral hormonal contraception provided in blister packaging compared with an adherence-supporting digital tablet dispenser: historical comparison of data from two clinical studies

    PubMed Central

    Elliesen, Jörg; Trummer, Dietmar

    2016-01-01

    Background The Clyk™ digital pill dispenser helps ensure correct and consistent administration of a flexible extended regimen of the combined oral contraceptive, ethinylestradiol (EE) 20 μg/drospirenone 3 mg (EE/drospirenone ; YAZ® Flex Flex), guiding users through the intake cycle and 4-day pill break and providing visible and acoustic daily reminders when pill intake is due. A study showed that the audible alarm function of the dispenser could help reduce the number of missed pills, but it lacked an appropriate “non-dispenser” group for a meaningful assessment of the impact of the dispenser on adherence. This study indirectly assessed the overall effect of the digital dispenser on adherence by comparing data from a treatment with standard blister packaging. Materials and methods One-year adherence data were compared from two similarly designed, Phase III, open-label, randomized trials of EE/drospirenoneFlex. In study 1, women used diary cards to record adherence with EE/drospirenoneFlex dispensed in blister packs (n=640), and in study 2 the dispenser was used with the alarm activated (n=250) or deactivated (n=248) in addition to using diary cards. Results A mean (±SD) of 4.3 (±4.24) missed pills over 1 year were recorded in diary cards among women who dispensed their pills from the blister packages (study 1) compared with 1.0 (±2.4) recorded by the alarm-activated dispenser (study 2). In study 2, a mean of 1.9 (±4.2) missed pills were reported in the diaries over 1 year compared with 4.4 (±9.1) from automatic recording by the dispenser (both arms of study 2), indicating underreporting of missed pills in diary cards vs the digital dispenser. Adjusting for this rate of underreporting, an estimated mean of ten pills were missed over 1 year by women using EE/drospirenoneFlex in blister packs, or ten times more than with the digital dispenser with activated acoustic alarm. Conclusion The digital dispenser helps reduce the number of missed pills and

  18. Fibrinolytic response in women on low-dose oral contraceptive.

    PubMed

    Ishak, R; Ahmad, R; Gudum, H R; Hassan, K; Ang, E S

    1992-06-01

    Long term use of low doses of combination oral contraceptives appears to increase plasminogen level, thereby increasing fibrinolytic activity and reducing the risk of thromboembolism. Blood levels of plasminogen, tissue plasminogen activator (tPA), and plasminogen activator inhibitor (PAI), were measured before and after stress (5 minutes of stair climbing) in a group of 30 women, 23-40 years old, who had taken 30 mcg of ethinyl estradiol with 150 mcg of desogestrel or levonorgestrel for at least 1 year. Similar measurements were taken from a control group of 30 women matched for age, height, and weight. Plasminogen and tPA levels in both groups increased significantly after exercise. The level of PAI did not change significantly with stress in either group. The level of plasminogen was significantly higher in the group taking contraceptives, whether before or after exercise, when compared to the control group. Levels of tPA and PAI, although slightly increased in the oral contraceptive group, were not significantly different between the two groups. The increase in plasminogen may be due to the estrogen component of the contraceptives. Stress seems to increase fibrinolytic response. PMID:12345026

  19. Anatomical and Functional Changes Induced by Oral Contraception

    PubMed Central

    Lefebvre, Yves

    1970-01-01

    The hormonal contraceptives seem to have no direct effect on cervical carcinoma or dysplasia, but they are responsible for the appearance of glandular adenomatous hyperplasia of the endocervix. The long-term use of progestins is responsible for the inactive appearance of the ovaries, with thickening of the tunica albuginea, rare follicle growth, occasional fibrosis of the stroma and a decreased DNA formation. After stopping oral and injectable hormonal contraceptives the first cycle is usually long and cases of amenorrhea have been reported. The causes of secondary amenorrhea probably lie in the hypothalamus and/or the ovaries. The time lapse between cessation of oral contraception and conception is between 5.8 and 6.5 months. No increase in abortion has been noted, but abortuses and ova have an increased polyploid tendency and incidence of chromosome breaks. Further investigations of larger series are necessary to provide definite proof. Meanwhile it would seem advisable that after cessation of hormonal contraception there should be a time lapse of six to eight months before a patient becomes pregnant. ImagesFIG. 1FIG. 2 PMID:4908561

  20. Pharmacokinetic interaction study between riociguat and the combined oral contraceptives levonorgestrel and ethinylestradiol in healthy postmenopausal women

    PubMed Central

    Unger, Sigrun; van der Mey, Dorina; Becker, Corina; Saleh, Soundos; Wensing, Georg; Mück, Wolfgang

    2016-01-01

    Abstract Female patients requiring treatment for pulmonary arterial hypertension (PAH) are advised to avoid pregnancy because of the high associated mortality rate. Oral contraception is one of the main methods of preventing pregnancy in this context, mandating pharmacokinetic and safety studies for new agents in this setting. Riociguat is a soluble guanylate cyclase stimulator approved for treatment of PAH and inoperable and persistent or recurrent chronic thromboembolic pulmonary hypertension. This single-center, randomized, nonblinded study involving healthy postmenopausal women investigated the effect of riociguat on plasma concentrations of levonorgestrel (0.15 mg) and ethinylestradiol (0.03 mg) in a combined oral contraceptive. Treatment A was a single oral tablet of levonorgestrel-ethinylestradiol. In treatment B, subjects received 2.5 mg riociguat 3 times daily for 12 days. On the eighth day, they also received a single oral tablet of levonorgestrel-ethinylestradiol. Subjects received both regimens in a crossover design. There was no change in area under the plasma concentration–time curves of levonorgestrel or ethinylestradiol or maximum concentration in plasma (Cmax) of levonorgestrel during combined administration versus levonorgestrel-ethinylestradiol alone. A 20% increase in the Cmax of ethinylestradiol was noted during coadministration; this is not anticipated to adversely impact the contraceptive efficacy or to require any dose adjustment for ethinylestradiol. Plasma concentrations and exposures of riociguat were within the expected range and were not influenced by coadministration with levonorgestrel-ethinylestradiol. Combined treatment was safe and well tolerated. In conclusion, riociguat did not change the exposure to levonorgestrel or ethinylestradiol relative to oral contraceptive administered alone. PMID:27162633

  1. Incidence of depressive symptoms in users of the oral contraceptive.

    PubMed

    Fleming, O; Seager, C P

    1978-05-01

    Evidence is presented that the incidence of depression among users of oral contraceptives is no higher than that among matched controls not taking such medication. There is an association between high depression scores and high neuroticism scores, more marked in controls than takers. Intensity of depression is related more to age, personality and occupation than to the use of oral contraceptives. A higher proportion of users than of controls experience sexual satisfaction. Past takers include a large number of individuals with a high neuroticism score. The incidence of depression symptoms in women increases with age. A higher proportion of housewives than of women going out to full-time work show depressive symptoms. PMID:656705

  2. A New and Practical Oral Contraceptive Agent: Norethindrone with Mestranol

    PubMed Central

    Dickinson, J. H.; Smith, G. G.

    1963-01-01

    The usefulness of a new oral contraceptive compound containing norethindrone 5 mg. and mestranol 0.075 mg. (Ortho-Novum) was studied. One hundred and seventeen private patients used this preparation for a total of 998 menstrual cycles. There were no pregnancies. Side effects were minimal and caused few (11 patients) to discontinue use. The most significant of these was weight gain and a premenstrual tension syndrome including nausea, breakthrough bleeding and skin effects. Other symptoms were minor and easily controlled. Instruction in use of the preparation is easy. Patient acceptance is excellent. Possible masculinizing effects, liver damage, or harmful effects on the uterus were checked specifically by laboratory evaluation; no significant abnormal findings were noted. This appears to be an effective oral contraceptive which is well accepted by the patient and which produced no serious side effects as used in this study. PMID:14027723

  3. Letter: Kilopascals. Control of oral contraceptive clinical trails.

    PubMed

    Mitchell, G D

    1975-02-01

    To deal with the confusion surrounding clinical acceptability of specific oral contraceptive preparations, a single set of forms for use in clinical research, together with a set of definitions, was recommended. Senior representatives of major pharmaceutical companies engaging in clinical trials in the United Kingdom were invited to cooperate. The Family Planning Research Unit of the University of Exeter was requested to provide facilities for meetings which began in 1972. An agreed set of forms has been designed and set of definitions has been developed to make the collection and interpretation of data more efficient. Organizations carrying out oral contraceptive clinical trials are invited to contact this unit. Forms, definitions, and further information will be provided on request. PMID:1089453

  4. The effect of a contraceptive vaginal ring and oral contraceptives on the vaginal flora.

    PubMed

    Roy, S; Wilkins, J; Mishell, D R

    1981-10-01

    Premenopausal women seeking a steroid contraceptive method were allowed to choose between a contraceptive vaginal ring (CVR) containing levonorgestrel and estradiol used in a 3-week in, 1-week out regimen (n=20) and an oral contraceptive (OC) containing levonorgestrel and ethinyl estradiol in a 28-day regimen (n = 10). Cultures from the posterior vaginal fornix were obtained before therapy in both groups and monthly for 6 months for the CVR group and after 1, 3, and 6 months for the OC group. These cultures were streaked on specific media to provide quantitative aerobic and anaerobic, lactobacillus, Candida sp., Gardnerella vaginalis and Neisseria gonorrhoeae counts in micro-organisms per milliliter. A comparison of the number and types of organisms isolated from vaginal cultures obtained initially and at 6 months demonstrated no statistically significant differences in colony counts between CVR and OC users. The results of this study suggest that the use of the CVR is not associated with a greater growth of pathogens than is oral administration of a progestin and estrogen combination. PMID:6797788

  5. Cerebral venous and sinus thrombosis associated with subcutaneous immunoglobulin injection and oral contraceptive use.

    PubMed

    Min, Jiangyong; Bhatt, Archit; Aburashed, Rany; Burton, Stephen

    2012-06-01

    Although patients of cerebral sinus thrombosis after intravenous immunoglobulin (IVIG) has been previously reported; reports of cerebral venous thrombosis secondary to subcutaneous injection of immunoglobulin (SIG) in conjunction with oral contraceptives are nonexistent in the current literature. We describe here a patient of cerebral venous and sinus thrombosis occurring after the combination of SIG and oral contraceptive use. Furthermore, we shall explore proper clinical precautions for someone who receives IG therapy, especially in conjunction with the use of oral contraceptives. PMID:21915646

  6. It's all about money: oral contraception alters neural reward processing.

    PubMed

    Bonenberger, Martina; Groschwitz, Rebecca C; Kumpfmueller, Daniela; Groen, Georg; Plener, Paul L; Abler, Birgit

    2013-12-01

    Mating preferences in phases of the natural menstrual cycle with a low probability to conceive have been associated with lower interest in characteristics promising genetic benefits but increased search for safety and future security. We hypothesized that this effect would also be evident under oral contraception and may therefore alter neural processing of monetary rewards as a proxy for potential safety. Our aim was to assess the activation of reward-related brain areas using a monetary incentive task in women with functional MRI (fMRI). We compared fMRI activation of 12 young women taking oral contraceptives with 12 women with a natural hormonal cycle in their follicular phase during the expectation of monetary rewards. Women under hormonal contraception who have already shown decreased anterior insula activation upon erotic stimulation in a previous study of the same sample now showed enhanced activation during monetary reward expectation in the anterior insula/inferior lateral prefrontal cortex (t=2.84; P<0.05) relative to young normal cycling women in the follicular phase. Our finding supports the notion that the switch in mating preferences related to different hormonal states in women is mirrored by a switch in the stimulus-dependent excitability of reward-related brain regions. Beyond highlighting hormonal effects on reward processing, our data underline the importance of monitoring hormonal states in fMRI research in women. PMID:24136199

  7. Jordanian Muslim women's intention to use oral contraceptives.

    PubMed

    Kridli, Suha Al-Oballi; Schott-Baer, Darlene

    2004-01-01

    Oral contraceptives (OCs) are the second most popular method of contraception in Jordan; however, their use remains low compared with the intrauterine device. The purpose of this article is to report the effect of factors identified by The Theory of Planned Behavior (TPB) on Jordanian Muslim women's intention to use OCs. TPB was used to develop an investigator-developed instrument, the Intention to Use Oral Contraceptive Tool (IUOCT). The IUOCT measured attitude (general attitude and attitudinal beliefs), social norms and perceived behavioral control factors in a total of 83 women participants. A stepwise regression analysis was calculated using the IUOCT subscales as predictors of Jordanian Muslim women's intention to use OCs. The findings demonstrated that the attitude, specifically general attitude and positive beliefs, about OC use affect Jordanian Muslim women's intention to use OCs. However, the findings provide limited support for social norms and perceived behavioral control as factors influencing Jordanian Muslim women's intention to use OCs. The findings indicate that more attention should be devoted to health education programs on the benefits of using OCs rather than focusing only on correcting misinformation. Nursing implications and recommendations for future research are discussed. PMID:15776755

  8. Transcortin as an indicator of estrogenic potency in oral contraceptives.

    PubMed

    Carol, W; Börner, A; Klinger, G; Greinke, C

    1980-03-01

    Serum cortisol-binding globulin (CBG) was measured before, during and following a 21-day application period of 5 oral contraceptives used in the GDR. In a second group of patients determinations were carried out at the end of a 24-month treatment period and the end of the first post-treatment cycle. From a third group of volunteers blood samples were taken at the end of the first, second and third treatment cycles. All the drugs tested produced a marked increase of CBG in serum, reaching its maximum at the end of the second treatment cycle. Within four weeks following termination of application the level fell to the control range. There were no significant differences between the various contraceptives. PMID:6156820

  9. Seizure facilitating activity of the oral contraceptive ethinyl estradiol.

    PubMed

    Younus, Iyan; Reddy, Doodipala Samba

    2016-03-01

    Contraceptive management is critical in women with epilepsy. Although oral contraceptives (OCs) are widely used by many women with epilepsy, little is known about their impact on epileptic seizures and epileptogenesis. Ethinyl estradiol (EE) is the primary component of OC pills. In this study, we investigated the pharmacological effect of EE on epileptogenesis and kindled seizures in female mice using the hippocampus kindling model. Animals were stimulated daily with or without EE until generalized stage 5 seizures were elicited. EE treatment significantly accelerated the rate of epileptogenesis. In acute studies, EE caused a significant decrease in the afterdischarge threshold and increased the incidence and severity of seizures in fully-kindled mice. In chronic studies, EE treatment caused a greater susceptibility to kindled seizures. Collectively, these results are consistent with moderate proconvulsant-like activity of EE. Such excitatory effects may affect seizure risk in women with epilepsy taking OC pills. PMID:26874323

  10. Risk of cancer with combined oral contraceptive use among Iranian women.

    PubMed

    Vaisy, Afasaneh; Lotfinejad, Shirin; Zhian, Faegh

    2014-01-01

    Oral contraceptive use is the most common type of contraception. More than 300 million women worldwide take oral contraceptives every day. However, there is a concern about the relationship with the incidence of cancer. This analytical retrospective study aimed to investigate the relationship between the incidence of cervical and breast cancers and oral contraceptive use in 128 Iranian patients with cervical cancer, 235 with breast cancer and equal numbers of controls. Data were collected through interviews with an organized set of questions. Details were also extracted from patient files. Data were analyzed using Student's t-test, chi-square and Fisher's exact tests, and Pearson's correlation analysis. The result revealed correlations between both cervical and breast cancers and history of contraceptive pills use. While cervical cancer significantly correlated with duration of use of pills, breast cancer had significant correlations with the type of oral contraceptive and age at first use. No significant relationships were found between the two types of cancer and age at discontinuation of oral contraceptives, patterns of use, and intervals from the last use. The use of oral contraceptives may triple the incidence of cervical cancer and doubles the incidence of breast cancer. Therefore, performing Pap smears every six months and breast cancer screening are warranted for long-term oral contraceptive users. PMID:25081657

  11. Mesenteric venous thrombosis associated with oral contraceptives: a case report.

    PubMed

    Milne, P Y; Thomas, R J

    1976-05-01

    Small-bowel infarction resulting from mesenteric venous thrombosis is a rare but life-threatening complication to which young women taking oral contraceptives are liable. The patient characteristically presents with an "acute abdomen" after a variable prodromal period of vague abdominal pain. The correct diagnosis can be made from the macroscopic appearance at laparotomy, provided the surgeon is alert to the condition. An accurate diagnosis is important, as anticoagulation measures must be instituted early to counter the commonly associated thromboembolic phenomena. PMID:1067070

  12. Oral contraceptives and polyp regression in familial adenomatous polyposis.

    PubMed

    Giardiello, Francis M; Hylind, Linda M; Trimbath, Jill D; Hamilton, Stanley R; Romans, Katharine E; Cruz-Correa, Marcia; Corretti, Mary C; Offerhaus, G Johan A; Yang, Vincent W

    2005-04-01

    Epidemiologic and experimental reports suggest that female hormones protect against the development of colorectal cancer, but studies are limited. We describe a patient in the placebo arm of a 4-year primary chemoprevention trial who developed adenomatous polyps and then had eradication of polyps after the administration of oral contraceptives. No change in the prostaglandin levels in the colonic mucosa was noted after polyp elimination, making nonsteroidal anti-inflammatory drug ingestion unlikely as a cause. This report represents the regression of colorectal adenomas with the use of estrogen/progesterone compounds. PMID:15825088

  13. Perceived side effects of oral contraceptives among adolescent girls.

    PubMed

    Herold, E S; Goodwin, M S

    1980-11-22

    Knowledge and attitudes of adolescent females regarding the side effects of oral contraceptives were investigated. The data source was a large study of sexual and contraceptive attitudes and experience. The questionnaire responses of 486 single females attending 10 birth control and pregnancy counseling centers in Ontario, Canada were examined. The age range of the subjects was from 13-20; 71% were attending school and 69% were living at home. They were attending the centers in order to obtain contraceptives (55%), to renew OC prescriptions (20%), or to receive pregnancy counseling (25%). 29% of the subjects had used OCs before coming to the clinic, but 91% planned to use OC after their clinic visit. 8% were planning to use an IUD; 1% were planning to use a diaphragm; and less than 1% were planning to have their boyfriend use condoms. 85% of the subjects indicated that they had heard abut side effcts of OCs with weight gain as the best known side effect. Other side effects familiar to many included nausea, circulatory disorders, headaches, emotional changes, menstrual problems and cancer. About 1/2 of the subjects had learned about these side effects from the mass media or female friends, 25% from a school sex education class, 15% from their mothers, and 3% from a physician. Despite knowledge regarding side effects, most of the subjects had positive attitudes toward OCs with 59% believing that the advnatages outweighed any disadvantages. PMID:7448666

  14. [Zoely, a combined oral contraceptive, monophasic pill containing estradiol and nomegestrol acetate].

    PubMed

    Pintiaux, A; Gaspard, U; Nisolle, M

    2012-03-01

    A new combined oral contraceptive called Zoely has just been marketed in Belgium. It contains nomegestrol acetate, a progestin known for its high contraceptive reliability based on its antigonadotropic power and long half-life. This progestin is associated with estradiol and Zoely is devoid of ethinyl estradiol, which is the usual component of the majority of combined oral contraceptives and is primarily responsible for thrombotic side effects of the pill. The compositon and type of regimen of this new oral contraceptive contribute to its efficacy and excellent clinical tolerance. PMID:22611833

  15. [ORAL CONTRACEPTIVES AND MOOD/SEXUAL DISORDERS IN WOMEN].

    PubMed

    Sirakov, M; Tomova, E

    2015-01-01

    Oral contraceptives are used since more than 50 years and are very popular due to offering more than 99% confidence in preventing pregnancy. Over 100 million women worldwide use oral contraceptives. In the UK 27% of women between 16 and 49 y. use pills. In the United States they are about 30%, in Germany - 40%, and in The Netherlands - 60%. According to a study by B. Pehlivanov, 2008, in Bulgaria only 4% of women use OC. (1) Despite the convenience and security, in the U.S.A. 29% of women taking OC interrupt prematurely their use (2), while the percentage of adolescents appears to be higher (3) Earlier studies of the reasons for refusal of OC focus on their influence on the menstrual cycle, as well as on some physical side effects such as the appearance of hair growth, weight gain, bloating etc. They paid very little attention to their impact on mood and sexual behavior of women (4). Newer studies suggest that the side effects associated with mood and sexual behavior proved more powerful factor leading to early termination of the use of OC (5). This paper is a review of the literature and evaluation of the facts presented in studies from different countries. They found a high incidence of symptoms such as anxiety, susceptibility to stress, mood changes, incl. depression, anxiety, increased irritability and affection of sexual desire of women. (6) There are many indications that OC-users are at increased risk of suicide and mental illnesses. (9). PMID:26411194

  16. Effect of Oral and Vaginal Hormonal Contraceptives on Inflammatory Blood Biomarkers

    PubMed Central

    Divani, Afshin A.; Luo, Xianghua; Datta, Yvonne H.; Flaherty, James D.; Panoskaltsis-Mortari, Angela

    2015-01-01

    The use of combined hormonal contraceptives has been reported to increase the level of C-reactive protein (CRP). We assessed the effect of hormonal contraceptive use on inflammatory cytokines including CRP, monocyte chemotactic protein-1, soluble tumor necrosis factor (sTNF), interleukin-6 (IL-6), and soluble CD40 ligand. We used 79 female subjects (19 to 30 years old) who were combined oral contraceptives users (n = 29), combined vaginal contraceptive users (n = 20), and nonusers (n = 30) with CRP values of ≤1 (n = 46) or ≥3 (n = 33). Information on medical history, physical activities, and dietary and sleeping habits were collected. Both oral and vaginal contraceptive users had higher levels of CRP (P < 0.0001), compared to nonusers. Only oral contraceptive users exhibited elevated sCD40L (P < 0.01). When comparing the groups with CRP ≤ 1 and CRP ≥ 3, levels of IL-6 and sTNF-RI were positively correlated with CRP among oral contraceptive users. We did not observe the same elevation for other inflammatory biomarkers for the CRP ≥ 3 group among vaginal contraceptive users. The clear cause of elevation in CRP level due to the use of different hormonal contraceptive formulations and methods is not well understood. Longitudinal studies with larger sample size are required to better assess the true cause of CRP elevation among hormonal contraceptive users. PMID:25861161

  17. Efficacy and safety of metformin or oral contraceptives, or both in polycystic ovary syndrome

    PubMed Central

    Yang, Young-Mo; Choi, Eun Joo

    2015-01-01

    Background Polycystic ovary syndrome (PCOS) is an endocrinopathy that affects approximately 10% of reproductive-aged women throughout their lives. Women with PCOS present with heterogeneous symptoms including ovulatory dysfunction, hyperandrogenism, and polycystic ovaries. Therefore, lifelong individualized management should be considered. Pharmacological agents commonly used to manage the symptoms are metformin and oral contraceptive pills. Although these medications have been beneficial in treating PCOS symptoms, their efficacy and safety are still not entirely elucidated. This study aimed to report the efficacy and safety of metformin, oral contraceptives, or their combination in the treatment of PCOS and to define their specific individual roles. Methods A literature search of original studies published in PubMed and Scopus was conducted to identify studies comparing metformin with oral contraceptives or evaluating the combination of both in PCOS. Results Eight clinical trials involving 313 patients were examined in the review. The intervention dosage of metformin ranged from 1,000 to 2,000 mg/d and that of oral contraceptives was ethinylestradiol 35 µg and cyproterone acetate 2 mg. Lower body mass index was observed with regimens including metformin, but increased body mass index was observed in monotherapy with oral contraceptives. Administration of metformin or oral contraceptives, especially as monotherapy, had a negative effect on lipid profiles. In addition, there are still uncertainties surrounding the effects of metformin or oral contraceptives in the management of insulin level, although they improved total testosterone and sex hormone-binding globulin levels. In the included studies, significant side effects due to metformin or oral contraceptives were not reported. Conclusion The clinical trials suggest that metformin or oral contraceptives are at least patient convenient, efficacious, and safe for the treatment of PCOS. However, well

  18. Ginger Orally Disintegrating Tablets to Improve Swallowing in Older People.

    PubMed

    Hirata, Ayumu; Funato, Hiroki; Nakai, Megumi; Iizuka, Michiro; Abe, Noriaki; Yagi, Yusuke; Shiraishi, Hisashi; Jobu, Kohei; Yokota, Junko; Hirose, Kahori; Hyodo, Masamitsu; Miyamura, Mitsuhiko

    2016-01-01

    We previously prepared and pharmaceutically evaluated ginger orally disintegrating (OD) tablets, optimized the base formulation, and carried out a clinical trial in healthy adults in their 20 s and 50s to measure their effect on salivary substance P (SP) level and improved swallowing function. In this study, we conducted clinical trials using the ginger OD tablets in older people to clinically evaluate the improvements in swallowing function resulting from the functional components of the tablet. The ginger OD tablets were prepared by mixing the excipients with the same amount of mannitol and sucrose to a concentration of 1% ginger. Eighteen healthy older adult volunteers aged 63 to 90 were included in the swallowing function test. Saliva was collected before and 15 min after administration of the placebo and ginger OD tablets. Swallowing endoscopy was performed by an otolaryngologist before administration and 15 min after administration of the ginger OD tablets. A scoring method was used to evaluate the endoscopic swallowing. Fifteen minutes after taking the ginger OD tablets, the salivary SP amount was significantly higher than prior to ingestion or after taking the placebo (p<0.05). Among 10 subjects, one scored 1-3 using the four evaluation criteria. Overall, no aspiration occurred and a significant improvement in the swallowing function score was observed (p<0.05) after taking the ginger OD tablets. Our findings showed that the ginger OD tablets increased the salivary SP amount and improved swallowing function in older people with appreciably reduced swallowing function. PMID:27374286

  19. Pharmacists' knowledge and interest in developing counseling skills relating to oral contraceptives.

    PubMed

    Amin, Mohamed E K

    2016-04-01

    Background Possessing correct therapeutic information on oral contraceptives is an important prerequisite for the provision of sound advice to women who are using these products. Objectives This study examines Egyptian pharmacists' knowledge of pharmacotherapeutic aspects of oral contraceptives as well as interest in developing skills in providing counseling on oral contraceptive pills. Setting Community pharmacies throughout Alexandria, Egypt. Methods A cross-sectional survey was self-administered by a random sample of community pharmacists in Alexandria, Egypt. Five multiple choice questions likely to arise when counseling women on oral contraceptives were constructed. Questions covered compatibility with breastfeeding, precautions, health risks and managing missed pills of oral contraceptives. Using ordered logistic regression, a model was estimated to predict pharmacists' interest in developing skills in providing counseling on oral contraceptives. Main outcome measure Pharmacists' aggregate scores for knowledge questions and pharmacists' interest in developing skills in providing counseling on oral contraceptive pills. Results Of the 181 approached pharmacists, 92 % participated. Twenty one pharmacists (13 %) did not know the correct answer to any question, 122 (73 %) answered one-two correctly, 23 (14 %) answered three-four correctly. No pharmacist answered all five questions correctly. For pharmacists' interest in developing skills in providing counseling on oral contraceptives, the percentage values for answers were: not interested at all (10.2 %), slightly interested (27.0 %), somewhat interested (23.4 %), interested (30.0 %) and extremely interested (9.6 %). Pharmacists' interest in developing skills in providing counseling on oral contraceptives was significantly associated with the number of women who requested advice from the pharmacists on oral contraceptives (OR 1.54, CI 1.24-1.91). In terms of the learning method of preference, percentage

  20. Nomegestrol acetate, a novel progestogen for oral contraception.

    PubMed

    Mueck, Alfred O; Sitruk-Ware, Regine

    2011-05-01

    Nomegestrol acetate (NOMAC) is a potent, highly selective progestogen, which is structurally similar to 19-norprogesterone and characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors. In animal models, NOMAC demonstrated moderate antiandrogenic activity and strong antiestrogenic activity. In clinical studies, the progestogen was associated with effective suppression of gonadotropic activity and ovulation in premenopausal women, and a neutral impact on hemostasis, lipids, and carbohydrate metabolism. In normal and cancerous human breast tissue, NOMAC has shown favorable effects on estrogen metabolism, and in human breast cancer cell lines in vitro, it does not stimulate cell proliferation. The pharmacologic profile of NOMAC suggested that it would be well suited for combination with a physiologic estrogen in a combined oral contraceptive (COC), with the aim of achieving effective contraception with good cycle control and a favorable safety profile. A monophasic COC containing NOMAC 2.5mg and 17β-estradiol (E2) 1.5mg, administered in a 24/4-day regimen, is currently under clinical investigation. In a phase III study, NOMAC/E2 provided consistent and robust ovulation inhibition, with contraceptive effects that compared favorably with those of drospirenone 3mg/ethinyl estradiol (EE) 30 μg. Investigators for a second phase III study reported less overall impact with NOMAC/E2 on hemostatic, lipid, inflammatory, and carbohydrate metabolism parameters than with levonorgestrel 150 μg/EE 30 μg. These clinical findings are promising; however, full publication of results from the pivotal phase III trials of NOMAC/E2 is pending. PMID:21335021

  1. Oral contraceptives as an over-the-counter medication.

    PubMed

    Halperin, E C

    1994-05-01

    Five physicians debate the pros and cons of changing the prescription requirement for oral contraceptives (OCs) to an over-the-counter (OTC) status. Three of the physicians are in favor of changing the present policy, while the other 2 physicians are in favor of keeping the present policy. Reasons supporting a change to OTC OCs are: the health risks from an unwanted pregnancy are greater than the risks from OC use; the prescription requirement puts an expensive and unnecessary burden on women; and other countries (e.g., India and South Africa) dispense OCs OTC. Reasons for keeping the prescription requirement are: the potential risks of self medication; the possibility of inappropriate use by relatively uninformed patients; and the loss of opportunity for women to obtain a health evaluation, physical examination, and counseling. One family practice physician supports OTC status because this change may reduce the teenage pregnancy rate. She acknowledges, however, that the change will not solve the problem of teenage pregnancy. An advantage of OTC OCs is that women could use them as a postcoital contraceptive. Another physician in favor of OTC status for OCs suggests that the US health department and Planned Parenthood clinics could offer OCs at lower than retail cost to women who undergo an annual health examination. Another physician calls for randomized clinical trials to generate sufficient data to make an informed decision about public and medical policy changes. PMID:8035888

  2. Consensus conference on combination oral contraceptives and cardiovascular disease.

    PubMed

    1999-06-01

    At the June 1998 conference of the International Federation of Fertility Societies (IFFS), a consensus was reached that there is no reason to advise selective prescribing of oral contraceptives (OCs) containing different progestins on the basis of their effects on cardiovascular disease. All currently available low-dose OCs, regardless of their progestin component, are more beneficial for a woman's short- or long-term health than the alternative of use of no contraception or use of a less effective method. The usual precautions in selecting appropriate candidates for OC use should be applied. This consensus was reached after several investigators presented the results of their studies on OC use and cardiovascular risk to an IFFS panel. Consolidation of the available research evidence produced annual cardiovascular mortality rates per 100,000 among women 15-24 years old of 1.2 in OC non-users, 2.1 in users of second-generation OCs, and 1.8-2.3 in users of third-generation OCs; among women 35-44 years old, these rates were 9.2, 20.4, and 15.5-17.8, respectively. PMID:10360623

  3. Effects of smoking and oral contraception on plasma beta-carotene levels in healthy women.

    PubMed

    Palan, P R; Romney, S L; Vermund, S H; Mikhail, M G; Basu, J

    1989-10-01

    Oral contraceptive use and smoking have been known to affect plasma vitamin levels. Total carotenoids have been studied with spectrophotometry, a relatively insensitive technique. In this study plasma concentrations of beta-carotene and retinol were measured in coded samples by sensitive high-pressure liquid chromatography in a cross-sectional study of 149 normal healthy women attending a family planning clinic. At the time of recruitment in the morning, a general health questionnaire was administered for patient age, methods of contraception, smoking habits, and food intake at breakfast. Of the 149 enrolled volunteers, 88 were oral contraceptive users and 61 were not users. Among users, 21 smoked cigarettes, and there were 18 smokers among nonusers. Oral contraceptive users had significantly lower plasma concentrations of beta-carotene (p less than 0.001) and higher retinol levels (p less than 0.0001). Plasma beta-carotene or retinol levels did not differ among users of intrauterine contraceptive devices or barrier methods of contraception. No association was noted between the plasma levels of these two micronutrients and age greater than or less than 30 years. Cigarette smoking alone was associated with significantly reduced plasma beta-carotene levels in nonusers (p less than 0.001). Combined cigarette smoking and oral contraceptive usage were associated with low plasma beta-carotene levels; the results appear to be additive. These findings suggest a possible synergistic effect on plasma beta-carotene levels from the use of both cigarette smoking and oral contraception. PMID:2801833

  4. Treating acne with oral contraceptives: use of lower doses.

    PubMed

    Huber, Johannes; Walch, Katharina

    2006-01-01

    Oral contraceptives (OCs) have been shown to effectively treat acne. Clinical trials of various doses of ethinyl estradiol (EE) combined with progestins such as levonorgestrel, desogestrel, norgestimate, gestodene, cyproterone acetate and drospirenone in monophasic, triphasic and combiphasic formulations used to treat acne in women are reviewed here. Open-label and comparative studies beginning in the 1980s were the first to demonstrate objective and subjective reductions in the incidence of acne, severity of existing acne and seborrhea. Placebo-controlled trials have corroborated these findings with a trend toward effective acne treatment with declining doses of EE. Significant reductions in total, inflammatory and noninflammatory lesions compared with placebo have been demonstrated with an OC containing the low dose of 20 microg of EE. Collectively, these findings support the use of low-dose OCs for the treatment of acne. PMID:16371290

  5. Oral contraceptive use and female genital arousal: methodological considerations.

    PubMed

    Seal, Brooke N; Brotto, Lori A; Gorzalka, Boris B

    2005-08-01

    This study explored effects of oral contraceptive pill (OCP) use on physiological sexual arousal as measured by a vaginal photoplethysmograph. Sixteen women aged 18-29 viewed audiovisual neutral and erotic stimuli before and an average of 6 weeks following the onset of OCP use. Although subjective measures of sexual arousal, including perceptions of genital arousal, significantly increased in response to erotic stimuli both before and after OCP onset, physiological sexual arousal only increased before OCP use. A comparison of individual responses before and after OCP onset reveals a much higher degree of intrasubject variability after OCP onset. We discuss these findings as they relate to OCP use as a confounding methodological variable to consider in future investigations employing vaginal photoplethysmography. PMID:19817038

  6. Hypertension among oral contraceptive users in El Paso, Texas.

    PubMed

    White, Kari; Potter, Joseph E; Hopkins, Kristine; Amastae, Jon; Grossman, Daniel

    2013-11-01

    On the U.S.-Mexico border, residents frequently cross into Mexico to obtain medications or medical care. We previously reported relatively high prevalence of hypertension among Latina oral contraceptive users in El Paso, particularly those obtaining pills over the counter (OTC) in Mexico. Here, we examine factors associated with having hypertension among 411 OTC users and 399 clinic users. We also assess hypertension awareness and interest in using blood pressure kiosks. Women age 35 to 44 and who had BMI ≥ 30 kg/m2 had higher odds of having hypertension. 59% of hypertensive women had unrecognized hypertension, and 77% of all participants would use a blood pressure kiosk; there were no significant differences between clinic and OTC users. Alternative approaches to increase access to health screenings are needed in this setting, where OTC pill use among women with unrecognized hypertension confers unique health risks. PMID:24185148

  7. Oral Contraceptives and Multiple Sclerosis/Clinically Isolated Syndrome Susceptibility

    PubMed Central

    Hellwig, Kerstin; Chen, Lie H.; Stancyzk, Frank Z.; Langer-Gould, Annette M.

    2016-01-01

    Background The incidence of multiple sclerosis (MS) is rising in women. Objective To determine whether the use of combined oral contraceptives (COCs) are associated with MS risk and whether this varies by progestin content. Methods We conducted a nested case-control study of females ages 14–48 years with incident MS or clinically isolated syndrome (CIS) 2008–2011 from the membership of Kaiser Permanente Southern California. Controls were matched on age, race/ethnicity and membership characteristics. COC use up to ten years prior to symptom onset was obtained from the complete electronic health record. Results We identified 400 women with incident MS/CIS and 3904 matched controls. Forty- percent of cases and 32% of controls had used COCs prior to symptom onset. The use of COCs was associated with a slightly increased risk of MS/CIS (adjusted OR = 1.52, 95%CI = 1.21–1.91; p<0.001). This risk did not vary by duration of COC use. The association varied by progestin content being more pronounced for levenorgestrol (adjusted OR = 1.75, 95%CI = 1.29–2.37; p<0.001) than norethindrone (adjusted OR = 1.57, 95%CI = 1.16–2.12; p = 0.003) and absent for the newest progestin, drospirenone (p = 0.95). Conclusions Our findings should be interpreted cautiously. While the use of some combination oral contraceptives may contribute to the rising incidence of MS in women, an unmeasured confounder associated with the modern woman’s lifestyle is a more likely explanation for this weak association. PMID:26950301

  8. Oral contraceptives as anti-androgenic treatment of acne.

    PubMed

    Lemay, André; Poulin, Yves

    2002-07-01

    Although acne is seldom associated with high serum levels of androgens, it has been shown that female acne patients have definite increases in ovarian and adrenal androgen levels when compared to appropriate controls. As shown in several pilot and in multiple open and comparative studies, oral contraceptives (OCs) are effective in causing a significant regression of mild to moderate acne. These results have been confirmed by multicentre randomized trials where low-dose OCs did not cause side effects different from those of the placebo-controlled group. The beneficial effect of OCs is related to a decrease in ovarian and adrenal androgen precursors; to an increase in sex hormone-binding globulin (SHBG), which limits free testosterone; and to a decrease in 3a-androstenediol glucuronide conjugate, the catabolite of dihydrotestosterone (DHT) formed in peripheral tissues. The estrogen-progestin combination containing cyproterone acetate (CPA) is particularly effective in treating acne, since this progestin also has a direct peripheral anti-androgenic action in blocking the androgen receptor. Only two open studies and one randomized study on small numbers of patients have reported some efficacy of spironolactone used alone or in combination with an OC in the treatment of acne. The new non-steroidal anti-androgens flutamide and finasteride are being evaluated for the treatment of hirsutism. Oral antibiotics are prescribed to patients with inflammatory lesions, where they are effective in decreasing the activity of microbes, the activity of microbial enzymes, and leukocyte chemotaxis. Concomitant intake of an OC and an antibiotic usually prescribed for acne does not impair the contraceptive efficacy of the OC. A second effective contraceptive method should be used whenever there would be decreased absorption or efficacy of the OC (digestive problems, breakthrough bleeding), lack of compliance and use of a type or dose of antibiotic different from that usually prescribed

  9. The return of fertility after discontinuation of oral contraception in Malaysian women.

    PubMed

    Hassan, J; Kulenthran, A; Thum, Y S

    1994-12-01

    The return of fertility after discontinuation of oral contraception was studied in a cross-sectional survey of 61 patients who were desirous of a further pregnancy. For controls, 380 women who did not take any oral contraception were used. Cumulative conception rates in the pill users were reduced but not significantly during the first three (p = 0.15) and six months (p = 0.20). By 12 months this difference was negligible (p = 0.28). We conclude that there is no significant delay in return of fertility following cessation of oral contraception in our group of Malaysian women. PMID:7674970

  10. New contraceptive eligibility checklists for provision of combined oral contraceptives and depot-medroxyprogesterone acetate in community-based programmes.

    PubMed Central

    Stang, A.; Schwingl, P.; Rivera, R.

    2000-01-01

    Community-based services (CBS) have long used checklists to determine eligibility for contraceptive method use, in particular for combined oral contraceptives (COCs) and the 3-month injectable contraceptive depot-medroxyprogesterone acetate (DMPA). As safety information changes, however, checklists can quickly become outdated. Inconsistent checklists and eligibility criteria often cause uneven access to contraceptives. In 1996, WHO produced updated eligibility criteria for the use of all contraceptive methods. Based on these criteria, new checklists for COCs and DMPA were developed. This article describes the new checklists and their development. Several rounds of expert review produced checklists that were correct, comprehensible and consistent with the eligibility requirements. Nevertheless, field-testing of the checklists revealed that approximately half (48%) of the respondents felt that one or more questions still needed greater comprehensibility. These findings indicated the need for a checklist guide. In March 2000, WHO convened a meeting of experts to review the medical eligibility criteria for contraceptive use. The article reflects also the resulting updated checklist. PMID:10994285

  11. Bioequivalence study of levothyroxine tablets compared to reference tablets and an oral solution.

    PubMed

    Koytchev, Rossen; Lauschner, Reinhard

    2004-01-01

    The study was designed to evaluate the bioequivalence of three levothyroxine sodium (CAS 51-48-9) formulations, i.e. a test and a reference tablet and an oral solution. A bioequivalence study was carried out in 25 healthy volunteers, who were administered a single dose of 600 microg levothyroxine in the form of the test formulation (levothyroxine sodium tablets 200 microg; Eferox), the originator product, and an oral solution. The trial was performed in one study center according to an open, randomized, three-way cross-over design with wash-out periods of 35 days between administration. Blood samples were taken up to 48 h post dose, the plasma was separated and the concentrations of levothyroxine and triiodothyronine were determined by radioimmunoassay with I125 labeling method. The levothyroxine mean Cmax were 112.0+/-17.3 ng/ml, 113.4+/-18.5 ng/ ml and 111.3+/-15.1 ng/ml, while the mean AUC0-24 were 2263.7+/-332.8 ng x h/ ml, 2307.3+/-351.3 ng x h/ml and 2286.1+/-331.0 ng x h/ml for the test and reference tablets as well as for the oral solution, respectively. No significant differences were found of principal pharmacokinetic parameters between the studied formulations. The 90%-confidence interval for the primary target parameters, intra-individual ratios of AUC0-24 and Cmax of levothyroxine were within the acceptance ranges for bioequivalence trials, i.e. AUC0-24 0.954-1.016 and 0.966-1.011 as well as Cmax 0.948-1.027 and 0.968-1.032 for test tablets versus reference tablets and the oral solution, respectively. Similar results were observed for triiodothyronine. In the light of the present study it can be concluded that the levothyroxine test tablet is bioequivalent to the reference formulation in respect of extent and rate of absorption. The results of the present trial confirm the findings of a previous study, performed under steady-state conditions with Eferox tablets 100 microg in patients without thyroid function. PMID:15553108

  12. A chewable low-dose oral contraceptive: a new birth control option?

    PubMed Central

    Weisberg, Edith

    2012-01-01

    A new chewable combined oral contraceptive pill containing ethinyl estradiol (EE) 0.025 mg and norethindrone (NE) 0.8 mg in a 24/4 regimen was approved for marketing in December 2010. Each of the four inactive tablets contains 75 mg ferrous fumarate, which has no therapeutic benefit. The tablet can be taken with food but not water as this affects the absorption of EE. The Pearl index based on intention to treat women aged 18–35 years has been reported at 2.01 (confidence interval [CI] 1.21, 3.14) and for the whole population 1.65 (CI 1.01, 2.55). The effect of a body mass index of >35 was not studied. Regular withdrawal bleeding occurred for 78.6% of women in Cycle 1, but by Cycle 13 almost half the women failed to have a withdrawal bleed. This new formulation provides an intermediate dose of an EE/NE combination that will be useful for women experiencing breakthrough bleeding on the lower-dose EE/NE pill. The convenience of a low-dose pill, which can be chewed without the need for water, will be useful to enable women who have forgotten a pill to take one whenever they remember, provided they carry it with them. The advantage of a 24/4 regimen is better suppression of follicular development in the pill-free interval and may be beneficial for women who experience menstrual cycle-related problems, such as heavy bleeding or dysmenorrhea. PMID:22573934

  13. Oral contraception in the former Czech and Slovak Federal Republic: attitudes and use.

    PubMed

    Ketting, E; Visser, A P; Uzel, R; Lehert, P

    1993-06-01

    This paper presents and discusses data on oral contraception from a national representative survey (n = 1072) on knowledge, attitudes and practice with regard to contraceptive use in the Czech and Slovak Federal Republic (CSFR). Only 7% of the women at risk of unplanned pregnancy used the pill. The low rate of use seems to be due to the general negative image of oral contraception, reinforced by the experiences of past users and opinions expressed by relative, friends, doctors, and the media. In particular, perceived psychological disadvantages have an important bearing on the decision not to use the method, whereas perceived advantages have hardly any impact. It is likely that this negative image is closely linked with the types of oral contraceptives that have been available in the country and also with the limited choice. Second- and third-generation oral contraceptives have only very recently become available. It is recommended that balanced information on the advantages and disadvantages of oral contraception be made available to doctors and to the general public on a large scale and through a variety of channels. PMID:8237567

  14. Treatment of recurrent toxic shock syndrome with oral contraceptive agents.

    PubMed

    McIvor, M E; Levin, M L

    1982-09-01

    The case of a 20-year old woman who was hospitalized for toxic shock syndrome (TSS) for 4 consecutive months despite use of conventional therapy for prevention of recurrence is described. Following discharge after the 4th episode she was started on oral contraceptives (OCs), and her next 8 menstrual cycles were uneventful despite continued use of tampons. She since discontinued use of tampons and remains asymptomatic. TSS recurrences occur in 30-64% of patients and can follow the initial episode by up to 41 months. The experience of this patient demonstrates the limitations of using antistaphyloccal antibiotics at the end of each menstrual cycle but suggests that hormonal manipulation may be an effective alternative therapy for TSS recurrences. Epidemiological studies show TSS patients use OCs less frequently than controls. Whether OCs suppress the vaginal flora, as some evidence suggests, or make conditions less favorable for the development of TSS in some other way is unknown. OC therapy for recurrences of TSS should receive further study. PMID:7144265

  15. Hypertriglyceridemic Pancreatitis Caused by the Oral Contraceptive Agent Estrostep.

    PubMed

    Abraham, Mary; Mitchell, Jennifer; Simsovits, Debra; Gasperino, James

    2015-07-01

    Norethindrone acetate/ethinyl estradiol (Estrostep; Warner Chilcott, Rockaway, New Jersey) is an "estrophasic" type of oral contraceptive, which combines a continuous low progestin dose with a gradually increasing estrogen dose. In clinical trials, this medication failed to produce clinically significant changes in serum lipid levels. We report a case of severe hypertriglyceridemia-induced acute pancreatitis in a 24-year-old woman caused by Estrostep, occurring nearly 10 years after she began using the drug. The patient was admitted to the medical intensive care unit (ICU) for aggressive volume resuscitation and management of severe electrolyte abnormalities. Laboratory studies obtained on admission indicated severe hypertriglyceridemia (2,200 mg/dL), hyponatremia (120 mEq/L), and hypocalcemia (0.78 mmol/L). Amylase and lipase levels were also elevated (193 and 200 U/L, respectively). Ranson score calculated after 48 hours of admission was 4, and her Acute Physiology and Chronic Health Evaluation (APACHE) IV score was 35. Treatment included an insulin infusion, ω-3 fatty acid esters, and gemfibrozil. The insulin infusion reduced serum triglyceride levels by 50% after 1 day of treatment and to 355 mg/dL by day 7 of her ICU course. We believe that this is the first reported case of severe, acute hypertriglyceridemia-induced pancreatitis caused by this medication. PMID:24671004

  16. Affective responsiveness is influenced by intake of oral contraceptives.

    PubMed

    Radke, Sina; Derntl, Birgit

    2016-06-01

    Despite the widespread use of oral contraceptive pills (OCs), little is known about their impact on psychological processes and emotional competencies. Recent data indicate impaired emotion recognition in OC users compared to naturally cycling females. Building upon these findings, the current study investigated the influence of OC use on three components of empathy, i.e., emotion recognition, perspective-taking, and affective responsiveness. We compared naturally cycling women to two groups of OC users, one being tested in their pill-free week and one in the phase of active intake. Whereas groups did not differ in emotion recognition and perspective-taking, an effect of pill phase was evident for affective responsiveness: Females currently taking the pill showed better performance than those in their pill-free week. These processing advantages complement previous findings on menstrual cycle effects and thereby suggest an association with changes in endogenous and exogenous reproductive hormones. The current study highlights the need for future research to shed more light on the neuroendocrine alterations accompanying OC intake. PMID:27039036

  17. Using Changes in Binding Globulins to Assess Oral Contraceptive Compliance

    PubMed Central

    Westhoff, Carolyn; Petrie, K.A.; Cremers, S.

    2012-01-01

    Background Validity of oral contraceptive pill (OCP) clinical trial results depends on participant compliance. Ethinyl estradiol (EE2) induces increases in hepatic binding globulin (BG) levels. Measuring these BG increases may provide an effective and convenient approach to distinguishing non-compliant from compliant OCP users in research settings. This analysis evaluated the usefulness of measuring increases in corticosteroid, sex hormone and thyroxine binding globulins (CBG, SHBG, TBG) as measures of OCP compliance. Methods We used frozen serum from a trial that compared ovarian suppression between normal weight and obese women randomized to one of two OCPs containing EE2 and levonorgestrel (LNG). Based on serial LNG measurements during the trial, 17% of participants were non-compliant. We matched non-compliant participants with compliant participants by age, BMI, ethnicity and OCP formulation. We measured CBG, SHBG and TBG levels, and compared change from baseline to 3-month follow-up between the non-compliant and compliant participants. Construction of receiver operator characteristic (ROC) curves allowed comparison of various BG measures. Results Changes in CBG and TBG distinguished OCP non-compliant users from compliant users (area under the ROC curve (AUROC), 0.86 and 0.89, p < 0.01). Changes in SHBG were less discriminating (AUROC 0.69) Conclusions EE2 induced increases in CBG and TBG provide a sensitive integrated marker of compliance with an LNG-containing OCP. PMID:22795088

  18. Clinical utility of folate-containing oral contraceptives

    PubMed Central

    Lassi, Zohra S; Bhutta, Zulfiqar A

    2012-01-01

    Folate is a generic term for a water-soluble B-complex vitamin which plays an important role in protein synthesis and metabolism and other processes related to cell multiplication and tissue growth. Pregnant and lactating women are at increased risk of folic acid deficiency because generally their dietary folate is insufficient to meet their physiological requirements and the metabolic demands of the growing fetus. The evidence pertaining to the reduction of the risk of neural tube defects (NTDs) due to folate is so compelling that supplementation with 400 μg of folic acid to all women trying to conceive until 12 weeks of pregnancy has been recommended by every relevant authority. A recent Cochrane review has also found protective effects of folate supplementation in occurrence and reoccurrence of NTDs. Despite food fortification and targeted public health campaigns promoting folic acid supplementation, 4,300,000 new cases occur each year worldwide resulting in an estimated 41,000 deaths and 2.3 million disability-adjusted life years (DALYS). This article will review the burden and risk factors of NTDS, and the role of folate in preventing NTDs. It will also describe different modes of supplementing folate and the newer evidence of the effectiveness of adding folate in oral contraceptives for raising serum and red blood cell folate levels. PMID:22570577

  19. Development of oral acetaminophen chewable tablets with inhibited bitter taste.

    PubMed

    Suzuki, Hiroyuki; Onishi, Hiraku; Takahashi, Yuri; Iwata, Masanori; Machida, Yoshiharu

    2003-01-30

    Various formulations with some matrix bases and corrigents were examined for development of oral chewable tablets which suppressed the bitter taste of acetaminophen, often used as an antipyretic for infants. Corn starch/lactose, cacao butter and hard fat (Witepsol H-15) were used for matrix bases, and sucrose, cocoa powder and commercial bitter-masking powder mixture made from lecithin (Benecoat BMI-40) were used for corrigents against bitter taste. The bitter taste intensity was evaluated using volunteers by comparison of test samples with standard solutions containing quinine at various concentrations. For the tablets made of matrix base and drug, Witepsol H-15 best inhibited the bitter taste of the drug, and the bitter strength tended to be suppressed with increase in the Witepsol H-15 amount. When the inhibitory effect on the bitter taste of acetaminophen solution was compared among the corrigents, each tended to suppress the bitter taste; especially, Benecoat BMI-40 exhibited a more inhibitory effect. Further, chewable tablets were made of one matrix base and one corrigent, and of one matrix base and two kinds of corrigents, their bitter taste intensities after chewing were compared. As a result, the tablets made of Witepsol H-15/Benecoat BMI-40/sucrose, of Witepsol H-15/cocoa powder/sucrose and of Witepsol H-15/sucrose best masked the bitter taste so that they were tolerable enough to chew and swallow. The dosage forms best masking bitter taste showed good release of the drug, indicating little change in bioavailability by masking. PMID:12527182

  20. The effect of elevated ovarian hormones on periodontal health: oral contraceptives and pregnancy.

    PubMed

    Zachariasen, R D

    1993-01-01

    The most common oral manifestation of elevated levels of ovarian hormones, as seen in pregnancy or oral contraceptive usage, is an increase in gingival inflammation with an accompanying increase in gingival exudate. This gingivitis can be avoided or at least minimized by establishing low plaque levels at the beginning of pregnancy or the beginning of oral contraceptive therapy. It would appear that bacteria are not solely responsible for the gingivitis seen during these times, nor are the ovarian hormones solely responsible for the condition. Data from numerous studies suggest that the ovarian hormones alter the microenvironment of the oral bacteria so as to promote their growth and shifts in their populations. The present article reviews the current state of knowledge concerning the relationship of gingivitis to elevated levels of ovarian hormones, and describes the role that these hormones may play in the gingivitis associated with pregnancy or oral contraceptive usage. PMID:8372477

  1. Oral thyroxine: variation in biologic action and tablet content.

    PubMed

    Sawin, C T; Surks, M I; London, M; Ranganathan, C; Larsen, P R

    1984-05-01

    Thirty-two patients with primary hypothyroidism were given oral thyroxine as Levothroid or Synthroid to see if the two preparations had similar effects. The serum thyroxine was used as an index of bioavailability and the serum thyrotrophin as an index of biologic activity. The serum thyroxine was lower in all 32 patients when taking Synthroid than when taking Levothroid. In 15 patients the serum thyroxine level fell low enough to raise the serum thyrotrophin; in all 15 the serum thyrotrophin rose when taking Synthroid. Direct measurement of thyroxine in the tablets showed that the tablets of Synthroid contained 20% to 30% less thyroxine than their stated content. Thus, the decreased bioavailability (lower serum thyroxine) and decreased biologic action (higher serum thyrotrophin) of Synthroid were due to the lower content of thyroxine. An incidental observation is that the range of serum thyroxine in treated hypothyroid patients is 7.6 to 16.6 micrograms/dL, higher than in normal persons. Because oral thyroxine is widely used, a cooperative effort among manufacturers, the United States Pharmacopeia and Food and Drug Administration, and clinicians to ensure the potency and biologic action of oral thyroxine is in order. Meanwhile, it seems reasonable to use oral thyroxine that is close to the stated content. PMID:6546843

  2. Bioprostethic mitral valve thrombosis due to oral contraceptive drug use and management with ultra-slow thrombolytic therapy.

    PubMed

    Yesin, Mahmut; Kalçik, Macit; Gündüz, Sabahattin; Astarcioğlu, Mehmet Ali; Gürsoy, Mustafa Ozan; Karakoyun, Süleyman; Özkan, Mehmet

    2016-03-01

    Prosthetic valve thrombosis is a severe complication, which usually occurs in inadequately anticoagulated patients. Mechanical valve thrombosis is more common than bioprosthetic valve thrombosis (BVT). Oral contraceptive drugs are associated with increased risk of thromboembolism in women. The possible association between oral contraceptive drug use and BVT has never been reported before. We present a case of obstructive BVT occurring after the use of an oral contraceptive drug and successful management with ultra-slow thrombolytic therapy. PMID:26378817

  3. Reproductive Health Outcomes of Insured Women Who Access Oral Levonorgestrel Emergency Contraception

    PubMed Central

    Raine-Bennett, Tina; Merchant, Maqdooda; Sinclair, Fiona; Lee, Justine W.; Goler, Nancy

    2015-01-01

    Objectives To assess the level of risk for women who seek emergency contraception through various clinical routes and the opportunities for improved care provision. Methods This study looked at a retrospective cohort to assess contraception and other reproductive health outcomes among women aged 15-44 who accessed oral levonorgestrel emergency contraception through an office visit or the call center at Kaiser Permanente Northern California from 2010 to 2011. Results Of 21,421 prescriptions, 14,531(67.8%) were accessed through the call center. In the subsequent 12 months, 12,127(56.6%) women had short-acting contraception (pills, patches, rings, depot medroxyprogesterone) dispensed and 2,264(10.6%) initiated very effective contraception (intrauterine contraception, implants, sterilization). Initiation of very effective contraception was similar for women who accessed it through the call center -1,569(10.8%) and office visits – 695(10.1%) (adjusted OR 1.02 95% confidence interval (CI) 0.93-1.13). In the subsequent 6 months, 2,056(9.6%) women became pregnant. Women who accessed emergency contraception through the call center were less likely to become pregnant within 3 months of accessing emergency contraception than woman who accessed it through office visits (adjusted OR 0.82 95% CI 0.72-0.94); however they were more likely to become pregnant within 4-6 months (adjusted OR 1.37 95%CI 1.16-1.60). Among women who were tested for chlamydia and gonorrhea, 689(7.8%) and 928(7.9%) were positive in the 12 months before and after accessing emergency contraception, respectively. Conclusions Protocols to routinely address unmet need for contraception at every call for emergency contraception and all office visits including visits with primary care providers should be investigated. PMID:25751211

  4. Greater Beta-Adrenergic Receptor Mediated Vasodilation in Women Using Oral Contraceptives

    PubMed Central

    Limberg, Jacqueline K.; Peltonen, Garrett L.; Johansson, Rebecca E.; Harrell, John W.; Kellawan, Jeremy M.; Eldridge, Marlowe W.; Sebranek, Joshua J.; Walker, Benjamin J.; Schrage, William G.

    2016-01-01

    Background: β-adrenergic receptors play an important role in mitigating the pressor effects of sympathetic nervous system activity in young women. Based on recent data showing oral contraceptive use in women abolishes the relationship between muscle sympathetic nervous system activity and blood pressure, we hypothesized forearm blood flow responses to a β-adrenergic receptor agonist would be greater in young women currently using oral contraceptives (OC+, n = 13) when compared to those not using oral contraceptives (OC–, n = 10). Methods: Women (18–35 years) were studied during the early follicular phase of the menstrual cycle (days 1–5) or placebo phase of oral contraceptive use. Forearm blood flow (FBF, Doppler ultrasound) and mean arterial blood pressure (MAP, brachial arterial catheter) were measured at baseline and during graded brachial artery infusion of the β-adrenergic receptor agonist, Isoproterenol (ISO), as well as Acetylcholine (ACH, endothelium-dependent vasodilation) and Nitroprusside (NTP, endothelium-independent vasodilation). Forearm vascular conductance was calculated (FVC = FBF/MAP, ml/min/100 mmHg) and the rise in FVC from baseline during infusion quantified vasodilation (ΔFVC = FVCinfusion − FVCbaseline). Results: ISO increased FVC in both groups (p < 0.01) and ISO-mediated ΔFVC was greater in OC+ compared to OC– (Main effect of group, p = 0.02). Expressing data as FVC and FBF resulted in similar conclusions. FVC responses to both ACH and NTP were also greater in OC+ compared to OC–. Conclusions: These data are the first to demonstrate greater β-adrenergic receptor-mediated vasodilation in the forearm of women currently using oral contraceptives (placebo phase) when compared to those not using oral contraceptives (early follicular phase), and suggest oral contraceptive use influences neurovascular control. PMID:27375493

  5. The influence of humidity, temperature, and oral contraceptive in tear

    NASA Astrophysics Data System (ADS)

    Sousa, Raul A. R. C.; Ribeiro, Tânia L. C.; Moreira, Sandra M. B.; Baptista, António M. G.

    2013-11-01

    The aim of this study is to ascertain whether the quantity and quality of tear and eye subjective comfort are influenced by the temperature, humidity and oral Contraceptives Taking or Non-taking (CTNT). Forty-one students, females, from the University of Minho, Braga, Portugal, aged (mean+/-1standard deviation) of 21.51+/-1.85 years, ranging from 20 to 30 years, participated in this study. The McMonnies Questionnaire (MMQ), Break Up Time (BUT) and Phenol Red Test (PRT) were accessed between 14-17 hours in four sets of visits throughout the year: Visit 1, Visit 2, Visit 3 and Visit 4. The PRT and BUT values (mean+/-1standard deviation) for Visit 1, Visit 2, Visit 3 and Visit 4 were respectively 23.88+/-6.50mm, 22.29+/-8.00mm, 23.61+/-6.75mm, 22.88+/-7.00mm and 6.02+/-1.58s, 5.62+/-1.22s, 5.23+/-0.88s, 5.53+/-1. 42s. The MMQ scores for Visit 1, Visit 2, Visit 3 and Visit 4 ranged from 2-13, 2-15, 1-14 and 2-14 with medians of 6, 7, 6 and 6, respectively. The influence of temperature, humidity and CTNT on PRT, BUT and MMQ were evaluated using generalized linear mixed model. For BUT and MMQ statistical significant effects were found regarding temperature and humidity. The temperature and humidity influenced the tear quality and subjective comfort but did not influence the tear quantity. The CTNT did not influence tear quantity, quality or subjective eye comfort.

  6. Oral contraceptives and the risk of endometrial cancer.

    PubMed

    Levi, F; La Vecchia, C; Gulie, C; Negri, E; Monnier, V; Franceschi, S; Delaloye, J F; De Grandi, P

    1991-03-01

    The relationship between the use of combination oral contraceptives (OCs) and the risk of endometrial cancer was assessed in a case-control study conducted in the Swiss Canton of Vaud between 1 January 1988 and 31 July 1990. Subjects included 122 women aged 75 or less with histologically confirmed endometrial cancer, and 309 control women in hospital for acute conditions unrelated to OC use. Overall, 14 percent of cases and 27 percent of controls had ever used OCs, corresponding to a multivariate relative risk (RR) of 0.5 (95 percent confidence interval [CI]: 0.3, 0.8). The risk of endometrial cancer was found to be related inversely to duration of OC use: RR = 1.0 for less than two years of OC use; 0.5 for two to five years; and 0.3 (95 percent CI: 0.1, 0.7) for more than five years. The protection appeared greater within 20 years since last use, and the RR rose to 0.8 after 20 or more years since last use; numbers are too small, however, for reliable inference from these subanalyses. No significant interaction or modifying effect was observed with other major factors related to endometrial cancer, including parity, body mass index, estrogen replacement therapy, and cigarette smoking. While this study provides further evidence for the protective effect of OCs against risk of endometrial cancer, the relationship requires continued evaluation to assess the long-term implications and public health impact of OC use. PMID:1873443

  7. Use of Oral Contraceptives for Management of Acne Vulgaris: Practical Considerations in Real World Practice.

    PubMed

    Harper, Julie C

    2016-04-01

    Acne vulgaris may be effectively treated with combination oral contraceptive pills (COCs) in women. COCs may be useful in any woman with acne in the absence of known contraindications. When prescribing a COC to a woman who also desires contraception, the risks of the COC are compared with the risks associated with pregnancy. When prescribing a COC to a woman who does not desire contraception, the risks of the COC must be weighed against the risks associated with acne. COCs may take 3 cycles of use to show an effect in acne lesion count reductions. PMID:27015775

  8. The in vitro effect of aspirin on increased whole blood platelet aggregation in oral contraceptive users.

    PubMed

    Norris, L A; Bonnar, J

    1994-05-01

    The effects of triphasic oral contraceptives on whole blood platelet aggregation in 36 Italian women are reported here. Aspirin's effects on platelet aggregation were also studied. 18 women took a triphasic oral contraceptive; 10 women took Trinordiol, while 8 took Trinovum for at least 90 days. The remaining 18 women took nothing and served as controls. The study was aligned with each woman's birth control pill cycle. Blood was taken daily on days 15-21 of their cycle. Either saline solution or acetylsalicylic acid was added to the blood samples and compared. All data was statistically analyzed using unpaired student's t-test. Effects of 3 aggregating agents, ADP, PAF, and EDTA, on platelet aggregation were studied. Arachidonic acid and adrenalin bitartrate were also studied in this manner. An increase in platelet aggregation was observed in women taking oral contraceptives. No difference was found between patients taking Trinordiol and those taking Trinovum. The results of this study indicate an increase in whole blood platelet sensitivity to collagen, adrenalin, and arachidonic acid when using oral contraceptives. Aspirin, at low doses, may have a role in preventing early thrombus formation in women taking oral contraceptives. PMID:8042198

  9. Development of sildenafil-loaded orally disintegrating tablet with new lactate salt.

    PubMed

    Jung, Si-Young; Kim, Dong-Wuk; Seo, Youn Gee; Woo, Jong Soo; Yong, Chul Soon; Choi, Han-Gon

    2012-05-01

    To develop a sildenafil lactate-loaded orally disintegrating tablet with a faster drug effect onset and immediate action of erection, the orally disintegrating tablets were prepared with various amounts of menthol and colloidal silica using the direct compression technique followed by vacuum drying. Their tablet properties such as friability, hardness, wetting time and disintegration time were investigated. The oral bioavailability of sildenafil in the orally disintegrating tablet was then compared with the sildenafil citrate-loaded commercial tablet (Viagra(®)) in rabbits. Sildenafil lactate was a new salt form with more improved solubility and alleviated bitterness compared with commercial salt, sildenafil citrate. As the amount of menthol in the orally disintegrating tablet increased, the friability increased and hardness decreased, resulting in a shorter wetting time and disintegration time. Colloidal silica did the opposite. The sildenafil lactate-loaded orally disintegrating tablet prepared with 45 mg/tab of menthol and 1.5 mg/tab of colloidal silica gave a hardness of 3-4 KP, friability less than 0.5% and disintegration time less than 30 s, suggesting that it was a practical and commercial product with good tablet property and excellent efficacy. Furthermore, it gave higher AUC and C(max), and shorter T(max) values than did the commercial tablet, indicating that it improved the oral bioavailability of sildenafil in rabbits compared with the commercial tablet. Thus, the sildenafil lactate-loaded orally disintegrating tablet might induce a fast onset of action and immediate erection compared with the sildenafil citrate-loaded commercial tablet. PMID:22010981

  10. Statement on postcoital contraception.

    PubMed

    1981-12-01

    For the woman exposed to a single unexpected and unprotected act of sexual intercourse, postcoital contraception can be used to avoid an unwanted pregnancy. Since the mid-1960s postcoital contraception using orally administered hormones has been found to be highly effective. This should be, however, considered as a 1-time procedure rather than a routine approach to contraception. The recommended oral methods are combined oral contraceptives (OCs) containing ethinyl estradiol 50 mcg and levonorgestrel 0.25 mg. Other similar formulations may also have high efficacy. The dosage schedule is 2 tablets at once followed by 2 tablets after 12 hours. This method is indicated in women exposed to unexpected and unprotected sexual intercourse, such as in cases of rape. It is effective only if it is instituted within 72 hours of the exposure. Data suggest this regime is as effective as that using diethylstilbestrol but with fewer side effects. As with all hormonal contraceptives, the method is contraindicated where a pregnancy is already established. Possible side effects include nausea and vomiting, irregular uterine bleeding, breast tenderness, and headache. The woman should be advised to return after 1 month to reinforce the need for elective contraception or, in the case of failure, to diagnose pregnancy and initiate counseling. In the event of a pregnancy, the woman should be reassured that no evidence exists to associate this regime of OC steroid administration with teratogenesis. Recent evidence indicates that effective postcoital contraceptive can be achieved by the insertion of a copper-containing IUD within 5 days of unprotected, mid-cycle sexual intercourse. PMID:12263975

  11. 77 FR 1695 - Determination That AVALIDE (Hydrochlorothiazide and Irbesartan), Oral Tablets, 25 Milligrams/300...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-01-11

    ...The Food and Drug Administration (FDA) has determined that AVALIDE (hydrochlorothiazide and irbesartan), oral tablets, 25 milligrams (mg)/300 mg and 12.5 mg/75 mg, were not withdrawn from sale for reasons of safety or effectiveness. This determination will allow FDA to approve abbreviated new drug applications (ANDAs) for hydrochlorothiazide and irbesartan, oral tablets, 25 mg/300 mg and 12.5......

  12. Early Impact Of The Affordable Care Act On Oral Contraceptive Cost Sharing, Discontinuation, And Nonadherence.

    PubMed

    Pace, Lydia E; Dusetzina, Stacie B; Keating, Nancy L

    2016-09-01

    The oral contraceptive pill is the contraceptive method most commonly used by US women, but inconsistent use of the pill is a contributor to high rates of unintended pregnancy. The relationship between consumer cost sharing and consistent use of the pill is not well understood, and the impact of the elimination of cost sharing for oral contraceptive pills in a mandate in the Affordable Care Act (ACA) is not yet known. We analyzed insurance claims for 635,075 women with employer-sponsored insurance who were initiating use of the pill, to examine rates of discontinuation and nonadherence, their relationship with cost sharing, and trends before and during the first year after implementation of the ACA mandate. We found that cost sharing for oral contraceptives decreased markedly following implementation, more significantly for generic than for brand-name versions. Higher copays were associated with greater discontinuation of and nonadherence to generic pills than was the case with zero copayments. Discontinuation of the use of generic or brand-name pills decreased slightly but significantly following ACA implementation, as did nonadherence to brand-name pills. Our findings suggest a modest early impact of the ACA on improving consistent use of oral contraceptives among women initiating their use. PMID:27605641

  13. Partner choice, relationship satisfaction, and oral contraception: the congruency hypothesis.

    PubMed

    Roberts, S Craig; Little, Anthony C; Burriss, Robert P; Cobey, Kelly D; Klapilová, Kateřina; Havlíček, Jan; Jones, Benedict C; DeBruine, Lisa; Petrie, Marion

    2014-07-01

    Hormonal fluctuation across the menstrual cycle explains temporal variation in women's judgment of the attractiveness of members of the opposite sex. Use of hormonal contraceptives could therefore influence both initial partner choice and, if contraceptive use subsequently changes, intrapair dynamics. Associations between hormonal contraceptive use and relationship satisfaction may thus be best understood by considering whether current use is congruent with use when relationships formed, rather than by considering current use alone. In the study reported here, we tested this congruency hypothesis in a survey of 365 couples. Controlling for potential confounds (including relationship duration, age, parenthood, and income), we found that congruency in current and previous hormonal contraceptive use, but not current use alone, predicted women's sexual satisfaction with their partners. Congruency was not associated with women's nonsexual satisfaction or with the satisfaction of their male partners. Our results provide empirical support for the congruency hypothesis and suggest that women's sexual satisfaction is influenced by changes in partner preference associated with change in hormonal contraceptive use. PMID:24818612

  14. Oral contraception, parity, breast feeding, and severity of rheumatoid arthritis.

    PubMed Central

    Jorgensen, C; Picot, M C; Bologna, C; Sany, J

    1996-01-01

    OBJECTIVE: To investigate the influence of breast feeding, use of the oral contraceptive pill (OCP), and parity on rheumatoid arthritis (RA). METHODS: One hundred and seventy six women with RA were compared with 145 control subjects; all had at least one child. RA patients were classified as having severe (n = 82) or mild disease (n = 89) according to clinical joint evaluation, radiological score, biological inflammation, and the presence of HLA-DR1 or -DR4 alleles. RESULTS: The mean age of RA patients was 58 years, and the mean age at the time of diagnosis of RA was 46 years. The mean time between onset of RA and the first birth was 23.6 (SD 3.8) years. The OCP user rates were 33% in the RA group and 47.6% in the control group (p < 0.02). OCP use was related to the mother's year of birth. The relative risk for developing RA was 0.598 (95% confidence interval (CI) 0.33 to 1.1) in women who had used OCP for more than five years compared with those who had never used OCPs. In contrast, the age at which the first pregnancy occurred, the number of children breast fed, and the duration of breast feeding were comparable in RA patients and healthy subjects. Among the RA patients, parity, duration of breast feeding, and the number of breast fed children were significantly increased in those with severe disease. Having more than three children increased the risk of developing severe disease 4.8-fold when adjusted for age and OCP use. Forty six percent of women with severe RA had a history of breast feeding duration greater than six months before disease onset, compared with 26% of patients with mild disease (p < 0.008). Having more than three breast fed children increased the risk of poor disease prognosis 3.7-fold. In contrast, OCP use had a protective role in the course of RA (44% of RA patients with mild disease were OCP users, compared with 21.7% of those with severe RA; p < 0.001). Among those using OCP for more than five years, the relative risk of developing severe

  15. Examining the use of oral contraceptives in the management of acne

    PubMed Central

    Salvaggio, Heather L; Zaenglein, Andrea L

    2010-01-01

    Combined oral contraceptive pills (cOCPs) are often used in the treatment of acne in females. They are effective, safe, and easy to use in appropriate patients in combination with more conventional acne therapies. This article will briefly address the physiologic rationale for the use of cOCPs in the treatment of acne. It will also review efficacy by examining relevant clinical trials. Safety considerations and the adverse event profile for oral contraceptives will be presented. Finally, practical considerations for prescribing cOCPs will be discussed. PMID:21072299

  16. Cerebral venous sinus thrombosis with ophthalmic manifestations in 18-year-olds on oral contraceptives.

    PubMed

    Tan, Jeffrey J; Hassoun, Ameer; Elmalem, Valerie I

    2014-08-01

    Cerebral venous sinus thrombosis (CVST) is a rare and potentially life-threatening cause of stroke. In the past few decades, the incidence and patient demographics have changed because of many factors, including the widespread use of oral contraceptives, improved detection of prothrombotic conditions, and advancement of imaging technology. The presentation of CVST is varied and can include ocular signs and symptoms. We present 2 cases of oral contraceptive-induced CVST in 18-year-old women, whose main presenting findings were ophthalmologic. PMID:24803635

  17. Timing of oral contraceptive use and the risk of breast cancer in BRCA1 mutation carriers.

    PubMed

    Kotsopoulos, Joanne; Lubinski, Jan; Moller, Pal; Lynch, Henry T; Singer, Christian F; Eng, Charis; Neuhausen, Susan L; Karlan, Beth; Kim-Sing, Charmaine; Huzarski, Tomasz; Gronwald, Jacek; McCuaig, Jeanna; Senter, Leigha; Tung, Nadine; Ghadirian, Parviz; Eisen, Andrea; Gilchrist, Dawna; Blum, Joanne L; Zakalik, Dana; Pal, Tuya; Sun, Ping; Narod, Steven A

    2014-02-01

    It is not clear if early oral contraceptive use increases the risk of breast cancer among young women with a breast cancer susceptibility gene 1 (BRCA1) mutation. Given the benefit of oral contraceptives for the prevention of ovarian cancer, estimating age-specific risk ratios for oral contraceptive use and breast cancer is important. We conducted a case-control study of 2,492 matched pairs of women with a deleterious BRCA1 mutation. Breast cancer cases and unaffected controls were matched on year of birth and country of residence. Detailed information about oral contraceptive use was collected from a routinely administered questionnaire. Conditional logistic regression was used to estimate the odds ratios (OR) and 95 % confidence intervals (CI) for the association between oral contraceptive and breast cancer, by age at first use and by age at diagnosis. Among BRCA1 mutation carriers, oral contraceptive use was significantly associated with an increased risk of breast cancer for women who started the pill prior to age 20 (OR 1.45; 95 % CI 1.20-1.75; P = 0.0001) and possibly between ages 20 and 25 as well (OR 1.19; 95 % CI 0.99-1.42; P = 0.06). The effect was limited to breast cancers diagnosed before age 40 (OR 1.40; 95 % CI 1.14-1.70; P = 0.001); the risk of early-onset breast cancer increased by 11 % with each additional year of pill use when initiated prior to age 20 (OR 1.11; 95 % CI 1.03-1.20; P = 0.008). There was no observed increase for women diagnosed at or after the age of 40 (OR 0.97; 95 % CI 0.79-1.20; P = 0.81). Oral contraceptive use before age 25 increases the risk of early-onset breast cancer among women with a BRCA1 mutation and the risk increases with duration of use. Caution should be taken when advising women with a BRCA1 mutation to take an oral contraceptive prior to age 25. PMID:24458845

  18. A consumer intercept study of oral contraceptive users in the Dominican Republic.

    PubMed

    Green, E C

    1988-01-01

    Purchasers of a low-cost oral contraceptive were intercepted and interviewed in a sample of Santo Domingo pharmacies that represented the highest sales of the product, yet also reflected the socioeconomic profile of the city's entire population. Users of the contraceptive were later interviewed in greater depth in their homes. The survey of users showed that the Dominican Republic's social marketing program, implemented by PROFAMILIA, was reaching an appropriate target market--that is, younger, lower-middle-class women of low parity. The program was, in addition, successful in attracting first-time adopters, and it was also expanding the overall commercial market for all contraceptives. The marketing campaign was successful in part because a mass audience was reached, through brief television spots. Program impact on contraceptive prevalence can be assessed from sales data. PMID:3381225

  19. The effect of a biphasic desogestrel-containing oral contraceptive on carbohydrate metabolism and various hormonal parameters.

    PubMed

    Kuhl, H; Jung-Hoffmann, C; Weber, J; Boehm, B O

    1993-01-01

    During 6 cycles of treatment of 19 women, the effect of a low-dose biphasic oral contraceptive containing 40 micrograms ethinylestradiol + 25 micrograms desogestrel (7 tablets) and 30 micrograms ethinylestradiol + 125 micrograms desogestrel (15 tablets) on various hormonal parameters and glucose metabolism was compared with the values of the pre- and post-treatment cycle. There was a profound reduction in gonadotropin secretion and ovarian steroid synthesis. The serum levels of testosterone were reduced by 35%, free testosterone by 55%, and DHEA-S by 30%. Cortisol increased by 100%, SHBG by 250%, and TBG by 60%, while FT3 and FT4 were only marginally influenced. Fasting levels of glucose and insulin did not change significantly, but the glucose load revealed a slight impairment of glucose tolerance. Three weeks after termination of pill intake, the various parameters returned to pretreatment levels, except for SHBG and TBG which were still elevated by 20 to 30%. The results demonstrate a marked preponderance of the effect of the estrogen component, a reliable inhibition of ovulation and very good cycle control during treatment with the biphasic formulation. PMID:8436002

  20. Orally disintegrating mini-tablets (ODMTs)--a novel solid oral dosage form for paediatric use.

    PubMed

    Stoltenberg, I; Breitkreutz, J

    2011-08-01

    The new European regulations on paediatric medicines and recent WHO recommendations have induced an increased need for research into novel child-appropriate dosage forms. The aim of this study was the development of orally disintegrating mini-tablets (ODMTs) as a suitable dosage form for paediatric patients. The suitability of five commercially available ready-to-use tableting excipients, Ludiflash, Parteck ODT, Pearlitol Flash, Pharmaburst 500 and Prosolv ODT, to be directly compressed into mini-tablets, with 2 mm in diameter, was examined. All of the excipients are based on co-processed mannitol. Drug-free ODMTs and ODMTs with a child-appropriate dose of hydrochlorothiazide were investigated. ODMTs could be produced with all investigated excipients. ODMTs with a sufficient crushing strength >7 N and a low friability <1% could be obtained, as well as ODMTs with a short simulated wetting test-time <5 s. ODMTs made of Ludiflash showed the best results with crushing strengths from 7.8 N up to 11.8 N and excellent simulated wetting test-times from 3.1 s to 5.0 s. For each excipient, ODMTs with accordance to the pharmacopoeial specification content uniformity could be obtained. The promising results indicate that orally disintegrating mini-tablets may serve as a novel platform technology for paediatrics in future. PMID:21324357

  1. [Pregnancy under oral contraceptives after treatment with tetracycline].

    PubMed

    Lequeux, A

    1980-01-01

    A 35 year old woman on hormonal contraception became pregnant during prolonged tetracycline treatment to cure acne. There is only 1 similar case published in the literature. Tetracycline may have been responsible for alterations in the intestinal flora, thus impairing the enterohepatic cycle of mestranol. An enzymatic microsomal induction is also possible, with acceleration of estrogen metabolization at the hepatic level. PMID:12336602

  2. Mortality among oral contraceptive users: 20 year follow up of women in a cohort study.

    PubMed Central

    Vessey, M. P.; Villard-Mackintosh, L.; McPherson, K.; Yeates, D.

    1989-01-01

    OBJECTIVE--To see whether the use of oral contraceptives influences mortality. DESIGN--Non-randomised cohort study of 17,032 women followed up on an annual basis for an average of nearly 16 years. SETTING--17 Family planning clinics in England and Scotland. SUBJECTS--Women recruited during 1968-74. At the time of recruitment each woman was aged 25-39, married, a white British subject, willing to participate, and either a current user of oral contraceptives or a current user of a diaphragm or intrauterine device (without previous exposure to the pill). MAIN OUTCOME MEASURES--Overall mortality and cause specific mortality. RESULTS--238 Deaths occurred during the follow up period. The main analyses concerned women entering the study while using either oral contraceptives or a diaphragm or intrauterine device. The overall relative risk of death in the oral contraceptive users was 0.9 (95% confidence interval 0.7 to 1.2). Though the numbers of deaths were small in most individual disease categories, the trends observed were generally consistent with findings in other reports. Thus the relative risk of death in the oral contraceptive users was 4.9 (95% confidence interval 0.7 to 230) for cancer of the cervix, 3.3 (95% confidence interval 0.9 to 17.9) for ischaemic heart disease, and 0.4 (95% confidence interval 0.1 to 1.2) for ovarian cancer. There was a linear trend in the death rates from cervical cancer and ovarian cancer (in opposite directions) with total duration of oral contraceptive use. Death rates from breast cancer (relative risk 0.9; 95% confidence interval 0.5 to 1.4) and suicide and probable suicide (relative risk 1.1; 95% confidence interval 0.3 to 3.6) were much the same in the two contraceptive groups. In 1981 the relative risk of death in oral contraceptive users from circulatory diseases as a group was reported to be 4.2 (95% confidence interval 2.3 to 7.7) in the Royal College of General Practitioners oral contraception study. The corresponding

  3. An Ethinyl Estradiol-Levonorgestrel Containing Oral Contraceptive Does Not Alter Cytochrome P4502C9 In Vivo Activity

    PubMed Central

    Pearson, Jacob; Maslen, Cheryl; Edelman, Alison

    2014-01-01

    Oral contraceptives have been in wide use for more than 50 years. Levonorgestrel, a commonly employed progestin component of combined oral contraceptives, was implicated in drug–drug interactions mediated via CYP2C9. Although in vitro studies refuted this interaction, there are no confirmatory in vivo studies. In the current study, we examined the phenotypic status of CYP2C9 using low-dose (125 mg) tolbutamide before and after oral contraceptive use in reproductive age women. Blood was collected 24 hours after the tolbutamide oral dose was administered, plasma was isolated, and tolbutamide concentration (C24) was measured using liquid chromatography–mass spectrometry. The natural logarithm of tolbutamide C24, a metric for CYP2C9 phenotype, was found to be equivalent (within 80%–125% equivalency boundaries) before and after oral contraceptive use. In conclusion, levonorgestrel-containing oral contraceptives, the most commonly used form of oral contraception, do not affect the status of the CYP2C9 enzyme. This suggests that it is safe to coadminister levonorgestrel-containing oral contraceptives and CYP2C9 substrates, which include a wide array of drugs. PMID:24368832

  4. Cerebral arterial occlusion and intracranial venous thrombosis in a woman taking oral contraceptives.

    PubMed Central

    Montón, F.; Rebollo, M.; Quintana, F.; Berciano, J.

    1984-01-01

    Occlusion of the middle cerebral artery and thrombosis of the superior sagittal sinus are reported in a 30-year-old woman taking oral contraceptives (OC). The coexistence of arterial and venous cerebral pathology as a complication of OC use has only been previously reported in one case. The pathogenesis of this rare association is briefly discussed. Images Fig. 1 Fig. 2 PMID:6462985

  5. Effects of the Menstrual Cycle and Oral Contraception on Singers' Pitch Control

    ERIC Educational Resources Information Center

    La, Filipa M. B.; Sundberg, Johan; Howard, David M.; Sa-Couto, Pedro; Freitas, Adelaide

    2012-01-01

    Purpose: Difficulties with intonation and vibrato control during the menstrual cycle have been reported by singers; however, this phenomenon has not yet been systematically investigated. Method: A double-blind randomized placebo-controlled trial assessing effects of the menstrual cycle and use of a combined oral contraceptive pill (OCP) on pitch…

  6. Menstrual and oral contraceptive use patterns among deployed military women by race and ethnicity.

    PubMed

    Deuster, Patricia A; Powell-Dunford, Nicole; Crago, Mark S; Cuda, Amanda S

    2011-01-01

    Menstrual cycle patterns and concerns and oral contraceptive use in the combat environment were examined in Caucasian, Asian, Hispanic, and African American women to guide the development of educational resources for women soldiers. An anonymous, questionnaire was completed by 455 U.S. Army women-Caucasian (CA: n = 141); Asian (AS: n = 67); Hispanic (HIS: n = 67); and African American (AA: n = 184) to compare menstrual patterns and concerns, dysmenorrhea, and oral contraceptive patterns. Total menstrual concerns were significantly lower among African Americans relative to Caucasians, Asians, or Hispanics; Asians and Hispanics reported the greatest concern. Overall, secondary amenorrhea was noted by 14.9% of women. Severe dysmenorrhea rates were significantly lower in African American (6.1%) compared to Caucasian (11.6%), Asian (20.9%) and Hispanic (19.7%) women. Asian women reported missing less work-only 9.3% with moderate to severe dysmenorrhea missed work compared to 25.1% of all other women. Only 9.2% of women with mild, compared to 25.8% with moderate to severe (OR = 3.44; p ≤ 0.0001) dysmenorrhea sought health care. Less than 50% of women took oral contraceptive, and less than half of those women took oral contraceptive continuously. African Americans seemed to experience menstruation as less bothersome than others, despite no difference in the proportion with menstrual irregularities, mean duration of menses, and/or mean time between cycles. PMID:21391160

  7. Factor V Leiden: should we screen oral contraceptive users and pregnant women?

    PubMed Central

    Vandenbroucke, J. P.; van der Meer, F. J.; Helmerhorst, F. M.; Rosendaal, F. R.

    1996-01-01

    The factor V Leiden mutation is the most common genetic risk factor for deep vein thrombosis: it is present in about 5% of the white population. The risk of deep vein thrombosis among women who use oral contraceptives is greatly increased by the presence of the mutation. The same seems to be true of the risk of postpartum thrombosis. Several authors have called for all women to be screened before prescription of oral contraceptives and during pregnancy. Such a policy might deny effective contraception to a substantial number of women while preventing only a small number of deaths due to pulmonary emboli. Moreover, in pregnancy the ensuing use of oral anticoagulation prophylaxis might carry a penalty of fatal bleeding that is equal to or exceeds the risk of death due to postpartum thrombosis. It might pay, however, to take a personal and family history of deep vein thrombosis when prescribing oral contraceptives or at a first antenatal visit to detect women from families with a tendency to multiple thrombosis. Images p1129-a PMID:8916702

  8. [Objective and perceived knowledge of oral contraceptive methods among adolescent mothers].

    PubMed

    Sousa, Michelle Chintia Rodrigues de; Gomes, Keila Rejane Oliveira

    2009-03-01

    The high rate of early pregnancy in Brazil and particularly in Teresina (21.5%), Piauí State, motivated the current study, the aim of which was to identify levels of objective and perceived knowledge on oral contraceptives, as well as predictive reproductive and socio-demographic variables for high knowledge. A cross-sectional study was performed including 278 teenage mothers (15-19 years), with their childbearing history, admitted to four maternity hospitals in Teresina in 2006. Logistic regression provided the basis for the statistical analysis. Nearly 98% of the adolescent mothers showed low objective and perceived knowledge of oral contraceptives. High parity was the only predictor of increased objective knowledge on oral contraceptives. The adolescents' low level of objective and perceived knowledge on use of oral contraceptives emphasized their susceptibility to risky sexual behavior. The findings emphasize the need for a more interactive approach with adolescents concerning their level of objective and perceived knowledge, to reduce the occurrence and repetition of unwanted teenage pregnancy and its negative consequences for the lives of these young mothers and their children. PMID:19300853

  9. A double-blind, placebo-controlled evaluation of the effect of oral doses of rizatriptan 10 mg on oral contraceptive pharmacokinetics in healthy female volunteers.

    PubMed

    Shadle, C R; Liu, G; Goldberg, M R

    2000-03-01

    Rizatriptan (MAXALT), a potent, oral 5-HT1B/1D agonist with a rapid onset of action, is available now for the acute treatment of migraine. This study examined the pharmacokinetic and clinical interaction between rizatriptan 10 mg and the components (ethinyl estradiol [EE] 35 micrograms and norethindrone [NET] 1.0 mg) of a well-established oral contraceptive combination product, ORTHO-NOVUM 1/35. Levels of sex hormone binding globulin (SHBG), a protein increased by EE to which NET binds, were also examined. In this two-period crossover study, 20 healthy young female subjects received a coadministration of 8 days of rizatriptan treatment (6 days of single-dose 10 mg rizatriptan and 2 days of multiple-dose rizatriptan, 10 mg q 4 hours for three doses, giving a total daily dose of 30 mg on Days 7 and 8) or matching placebo along with their daily dose (one tablet) of ORTHO-NOVUM 1/35 within their oral contraceptive cycle. Plasma was sampled for EE, NET, and SHBG concentrations. Safety evaluations included routine laboratory safety studies, physical examinations, and monitoring for ECG, vital signs, and adverse events. There were no statistically significant differences in any of the pharmacokinetic parameters of EE or NET between the rizatriptan and placebo treatment periods, thus indicating that rizatriptan had no meaningful effect on the disposition of either the EE or the NET component of ORTHO-NOVUM 1/35. The SHBG concentration did not change throughout the entire study. Clinically, coadministration of rizatriptan with ORTHO-NOVUM 1/35 was well tolerated. Blood pressure, heart rate, and temperature showed no consistent trend or clinically important changes. Adverse events following coadministration of rizatriptan with ORTHO-NOVUM 1/35 were similar to those reported when placebo was given with ORTHO-NOVUM 1/35. The findings of this study indicate that there is little potential for dosages as high as 30 mg/day, the maximum recommended dosing schedule, of rizatriptan

  10. Combining oral contraceptives with a natural nuclear factor-kappa B inhibitor for the treatment of endometriosis-related pain.

    PubMed

    Maia, Hugo; Haddad, Clarice; Casoy, Julio

    2013-01-01

    Endometriosis is a chronic disease in which a persistent state of heightened inflammation is maintained by nuclear factor-kappa B (NF-κB) activation. The progestins present in oral contraceptives are potent inhibitors of NF-κB translocation to cell nuclei, while Pycnogenol® (Pinus pinaster) acts by blocking post-translational events. In this study, the effects of Pycnogenol on pain scores were investigated in patients with endometriosis using oral contraceptives containing either gestodene or drospirenone in extended regimens. Pain scores were determined using a visual analog scale before and after 3 months of treatment. Oral contraceptives, used alone (groups 1 and 3) or in association with Pycnogenol (groups 2 and 4), resulted in significant decreases in pain scores after 3 months of treatment; however, this reduction was significantly greater in the groups using oral contraceptives + Pycnogenol (groups 2 and 4) compared with those using oral contraceptives alone (groups 1 and 3). In the groups using oral contraceptives alone, 50% of patients became pain-free by the end of the third month of treatment. These results suggest that Pycnogenol increases the efficacy of oral contraceptives for the treatment of endometriosis-related pain. PMID:24379702

  11. Effect of formulated ingredients on rapidly disintegrating oral tablets prepared by the crystalline transition method.

    PubMed

    Sugimoto, Masaaki; Narisawa, Shinji; Matsubara, Koji; Yoshino, Hiroyuki; Nakano, Minoru; Handa, Tetsurou

    2006-02-01

    The aim of this article was to determine the optimal ingredients for the rapidly disintegrating oral tablets prepared by the crystalline transition method (CT method). The effect of ingredients (diluent, active drug substance and amorphous sugar) on the characteristics of the tablets was investigated. The ingredients were compressed and the resultant tablets were stored under various conditions. The oral disintegration time of the tablet significantly depended on diluents, due to differences in the penetration of a small amount of water in the mouth and the viscous area formed inside the tablet. The oral disintegration time was 10-30 s for tablets with a tensile strength of approximately 1 MPa, when erythritol, mannitol or xylitol was used as the diluent. The increase in the tensile strength of tablets containing highly water-soluble active drug substances during storage was as large as that of tablets without active drug substances, while the increase in the tensile strength of tablets containing low water-soluble active drug substances was small. It was therefore found that highly water-soluble active drug substances were more suitable for the formulation prepared by the CT method than low water-soluble active drug substances. Irrespective of the type of amorphous sugar (amorphous sucrose, lactose or maltose) used, the porosity of tablets with 1 MPa of tensile strength was 30-40%, and their oral disintegration time was 10-20 s. The optimal ingredients for rapidly disintegrating oral tablets with reasonable tensile strength and disintegration time were therefore determined from these results. PMID:16462059

  12. [A comparative study of the incidence of Gardnerella vaginalis in users of IUD and oral contraceptives].

    PubMed

    Aleixo Neto, A; Peixoto, M L; Cabral, A C

    1987-07-01

    Leukorrhea constitutes one of the most frequent complaints by women visiting out-patient gynecological clinics. The most common etiological agents are Gardnerella vaginalis, Trichomonas vaginalis, Neisseria gonorrhoea and Candida albicans. Some authors have been able to verify an increased presence of certain pathogenic germs in the vaginal flora for users of contraceptive methods, e.g., for users of IUD, Kivijarvi et al. demonstrated a significantly increased presence of Gardnerella vaginalis considered responsible for a large number of inflammatory diseases of the pelvis in woman. In order to establish the frequency of colpo-cervicitis in users of contraceptive methods a study was initiated of women attending the Family Planning Clinic of the Department of Medicine at UFMG during the period January-December 1986. 305 cytological smears obtained from 111 users of oral hormonal contraceptives and from 194 users of IUD were studied by using the Papanicolaou staining method. A microscopic examination enabling the detection of cells that indicate the presence of Gardnerella vaginalis, trichomonas, Candida, papilloma, and dysplastic cells was performed. The results are listed in two tables. In 34.5% of cases a significant association was established between users of IUD and cells indicating the presence of Gardnerella vaginalis. For users of oral contraceptives that figure was lower, 28.8%. This circumstance has been attributed to probable epithelial lesions caused by incorrect insertion of the IUD and more abundant menstrual flux provoked b the IUD in combination with the hemophilic characteristics of Gardnerella vaginalis. A significant prevalence of papilloma and trichomonas was also noted for women using IUD as opposed to those oral contraceptives. The results demonstrate the necessity of frequent clinical attendance and laboratory tests for women using contraceptive methods, particularly the IUD. PMID:12282423

  13. The link between oral contraceptive use and prevalence in autism spectrum disorder.

    PubMed

    Strifert, Kim

    2014-12-01

    Autism spectrum disorder (ASD) is a group of developmental disabilities that include full syndrome autism, Asperger's syndrome, and other pervasive developmental disorders. The identified prevalence of ASD has increased in a short time period across multiple studies causing some to conclude that it has reached epidemic proportions in the U.S. Many possible explanations for the rise in numbers of individuals diagnosed with ASD have been offered and yet, causes and contributing factors for ASD are inadequately understood. Current evidence suggests that both genetics and environment play a part in causing ASD. One possible risk factor for the increase in prevalence has been profoundly overlooked in the existing biomedical and epidemiologic literature. As the prevalence of ASD has risen in the last sixty years, so has the prevalence of the usage of the oral contraceptives and other modern hormonal delivery methods. In 1960 about one million American women were using oral contraceptives, today close to 11 million women in the U.S. use oral contraceptives. Eighty-two percent of sexually active women in the U.S. have used oral contraceptives at some point during their reproductive years. Thus, the growth in use of progesterone/estrogen-based contraceptives in the United State has reached near-ubiquitous levels among women in the child-bearing age range. The suppression of ovulation produced by estrogen-progesterone is an indisputable abnormality. It is logical to consider the outcome of the ovum that would have been normally released from the ovary during ovulation. To date there is no comprehensive research into the potential neurodevelopmental effects of oral contraceptive use on progeny. The issue has been only sparsely considered in the biomedical literature. This article hypothesizes that the compounds, estrogen and progesterone, used in oral contraceptives modify the condition of the oocyte and give rise to a potent risk factor that helps explain the recent increase

  14. Oral contraceptive use and mortality after 36 years of follow-up in the Nurses’ Health Study: prospective cohort study

    PubMed Central

    Charlton, Brittany M; Rich-Edwards, Janet W; Colditz, Graham A; Missmer, Stacey A; Rosner, Bernard A; Hankinson, Susan E; Speizer, Frank E

    2014-01-01

    Objective To determine whether use of oral contraceptives is associated with all cause and cause specific mortality. Design Prospective cohort study. Setting Nurses’ Health Study, data collected between 1976 and 2012. Population 121 701 participants were prospectively followed for 36 years; lifetime oral contraceptive use was recorded biennially from 1976 to 1982. Main outcome measures Overall and cause specific mortality, assessed throughout follow-up until 2012. Cox proportional hazards models were used to calculate the relative risks of all cause and cause specific mortality associated with use of oral contraceptives. Results In our population of 121 577 women with information on oral contraceptive use, 63 626 were never users (52%) and 57 951 were ever users (48%). After 3.6 million person years, we recorded 31 286 deaths. No association was observed between ever use of oral contraceptives and all cause mortality. However, violent or accidental deaths were more common among ever users (hazard ratio 1.20, 95% confidence interval 1.04 to 1.37). Longer duration of use was more strongly associated with certain causes of death, including premature mortality due to breast cancer (test for trend P<0.0001) and decreased mortality rates of ovarian cancer (P=0.002). Longer time since last use was also associated with certain outcomes, including a positive association with violent or accidental deaths (P=0.005). Conclusions All cause mortality did not differ significantly between women who had ever used oral contraceptives and never users. Oral contraceptive use was associated with certain causes of death, including increased rates of violent or accidental death and deaths due to breast cancer, whereas deaths due to ovarian cancer were less common among women who used oral contraceptives. These results pertain to earlier oral contraceptive formulations with higher hormone doses rather than the now more commonly used third and fourth generation formulations

  15. Enhanced oral bioavailability of felodipine by novel solid self-microemulsifying tablets.

    PubMed

    Jing, Boyu; Wang, Zhiyuan; Yang, Rui; Zheng, Xia; Zhao, Jia; Tang, Si; He, Zhonggui

    2016-01-01

    The novel self-microemulsifying (SME) tablets were developed to enhance the oral bioavailability of a poor water-soluble drug felodipine (FDP). Firstly, FDP was dissolved in the optimized liquid self-microemusifying drug delivery systems (SMEDDS) containing Miglyol® 812, Cremophor® RH 40, Tween 80 and Transcutol® P, and the mixture was solidified with porous silicon dioxide and crospovidone as adsorbents. Then after combining the solidified powders with other excipients, the solid SME tablets were prepared by wet granulation-compression method. The prepared tablets possessed satisfactory characterization; the droplet size of the SME tablets following self-emulsification in water was nearly equivalent to the liquid SMEDDS (68.4 ± 14.0 and 64.4 ± 12.0 nm); differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) analysis demonstrated that FDP in SME tablets had undergone a polymorphism transition from a crystal form to an amorphous state, which was further confirmed by transmission electron microscopy (TEM). A similar dissolution performance of SME tablets and liquid SMEDDS was also obtained under the sink condition (85% within 10 min), both significantly higher than commercial tablets. The oral bioavailability was evaluated for the SME tablets, liquid SMEDDS and commercial conventional tablets in the fasted beagle dogs. The AUC of FDP from the SME tablets was about 2-fold greater than that of conventional tablets, but no significant difference was found when compared with the liquid SMEDDS. Accordingly, these preliminary results suggest that this formulation approach offers a useful large-scale producing method to prepare the solid SME tablets from the liquid SMEDDS for oral bioavailability equivalent enhancement of poorly soluble FDP. PMID:26177197

  16. Contraceptive knowledge and attitudes of Austrian adolescents after mass media reports linking third-generation oral contraceptives with an increased risk of venous thromboembolism.

    PubMed

    Egarter, C; Strohmer, H; Lehner, R; Földy, M; Leitich, H; Berghammer, P

    1997-09-01

    We performed a representative survey to determine the level of knowledge of 1,010 Austrian adolescents aged 14 to 24 years about selected facts relating to the recent massive news coverage of the increase in the risk of venous thromboembolism in users of third-generation oral contraceptives and to assess the contraceptive behavior of this population. The overall use rate of oral contraceptives and condoms had increased significantly between 1991 and 1996. Sixty-six percent of the adolescents surveyed stated not having heard or read any media reports on oral contraceptives. Only 8% of those who had knew that most reports focused on the pill as a possible cause of venous thromboembolism, whereas the majority of respondents indicated that the media conveyed doubts regarding the health safety of oral contraceptives in general. Nearly half of adolescents were unable to define what a thrombosis was. Thus, although the mass media play an important role in transmitting medical information, the dissemination of practical, accurate advice on the risks of a drug and competent patient counseling is reserved for the health care professionals. PMID:9347204

  17. Efficacy and safety of a 24-day regimen of drospirenone-containing combined oral contraceptive in Korean women

    PubMed Central

    Kim, Nayoung; Yoo, Ha-Na; Hyun, Hye Sun; Yoon, Byung-Koo; Choi, Doo-Seok

    2015-01-01

    This study assesses the efficacy and safety of a 24-day regimen of drospirenone-containing combined oral contraceptive, and demonstrates that it is an effective and safe option for contraception, releasing symptom of premenstrual dysphoric disorder and acne in Korean women. PMID:26430665

  18. Contraceptive Development.

    ERIC Educational Resources Information Center

    Troen, Philip; And Others

    This report provides an overview of research activities and needs in the area of contraceptive development. In a review of the present state, discussions are offered on the effectiveness and drawbacks of oral contraceptives, intrauterine devices, barrier methods, natural family planning, and sterilization. Methods of contraception that are in the…

  19. Formulation development, evaluation and comparative study of effects of super disintegrants in cefixime oral disintegrating tablets.

    PubMed

    Remya, Ks; Beena, P; Bijesh, Pv; Sheeba, A

    2010-07-01

    The present work was aimed at formulation development, evaluation and comparative study of the effects of superdisintegrants in Cefixime 50 mg oral disintegrating tablets. The superdisintegrants used for the present study were sodium starch glycolate and crosscarmellose sodium. The formulated tablets were evaluated for various tableting properties, like hardness, thickness, friability, weight variation, disintegration time and dissolution rate. Comparative evaluation of the above-mentioned parameters established the superiority of the tablets formulated with crosscarmellose sodium to those formulated with sodium starch glycolate. PMID:21042477

  20. Formulation Development, Evaluation and Comparative Study of Effects of Super Disintegrants in Cefixime Oral Disintegrating Tablets

    PubMed Central

    Remya, KS; Beena, P; Bijesh, PV; Sheeba, A

    2010-01-01

    The present work was aimed at formulation development, evaluation and comparative study of the effects of superdisintegrants in Cefixime 50 mg oral disintegrating tablets. The superdisintegrants used for the present study were sodium starch glycolate and crosscarmellose sodium. The formulated tablets were evaluated for various tableting properties, like hardness, thickness, friability, weight variation, disintegration time and dissolution rate. Comparative evaluation of the above-mentioned parameters established the superiority of the tablets formulated with crosscarmellose sodium to those formulated with sodium starch glycolate. PMID:21042477

  1. Why do inadvertent pregnancies occur in oral contraceptive users? Effectiveness of oral contraceptive regimens and interfering factors.

    PubMed

    Fraser, I S; Jansen, R P

    1983-06-01

    Inadvertent pregnancies in combined pill users are not uncommon, and are usually due to errors of tablet taking. However, many factors may contribute to 'pill failure'. In this review the endocrine pharmacology of pill use and the changes reported with missed pills have been considered in detail. The influences of other factors including drug interactions have been reviewed and a series of recommendations made for reducing the risk of pregnancy in each of these circumstances. PMID:6413129

  2. The influence of formulation and manufacturing process parameters on the characteristics of lyophilized orally disintegrating tablets.

    PubMed

    Jones, Rhys J; Rajabi-Siahboomi, Ali; Levina, Marina; Perrie, Yvonne; Mohammed, Afzal R

    2011-01-01

    Gelatin is a principal excipient used as a binder in the formulation of lyophilized orally disintegrating tablets. The current study focuses on exploiting the physicochemical properties of gelatin by varying formulation parameters to determine their influence on orally disintegrating tablet (ODT) characteristics. Process parameters, namely pH and ionic strength of the formulations, and ball milling were investigated to observe their effects on excipient characteristics and tablet formation. The properties and characteristics of the formulations and tablets which were investigated included: glass transition temperature, wettability, porosity, mechanical properties, disintegration time, morphology of the internal structure of the freeze-dried tablets, and drug dissolution. The results from the pH study revealed that adjusting the pH of the formulation away from the isoelectric point of gelatin, resulted in an improvement in tablet disintegration time possibly due to increase in gelatin swelling resulting in greater tablet porosity. The results from the ionic strength study revealed that the inclusion of sodium chloride influenced tablet porosity, tablet morphology and the glass transition temperature of the formulations. Data from the milling study showed that milling the excipients influenced formulation characteristics, namely wettability and powder porosity. The study concludes that alterations of simple parameters such as pH and salt concentration have a significant influence on formulation of ODT. PMID:24310589

  3. Oral contraceptive pill use and menstrual cycle phase are associated with altered resting state functional connectivity.

    PubMed

    Petersen, Nicole; Kilpatrick, Lisa A; Goharzad, Azaadeh; Cahill, Larry

    2014-04-15

    At rest, brain activity can be characterized not by an absence of organized activity but instead by spatially and temporally correlated patterns of activity. In this experiment, we investigated whether and to what extent resting state functional connectivity is modulated by sex hormones in women, both across the menstrual cycle and when altered by oral contraceptive pills. Sex hormones have been shown to have important effects on task-related activity, but few studies have investigated the extent to which they can influence the behavior of functional networks at rest. These hormones are dramatically altered by the use of hormonal contraception, which is used by approximately 100 million women worldwide. However, potential cognitive side effects of hormonal contraception have been given little attention. Here, we collected resting state data for naturally-cycling women (n=45) and women using combined oral contraceptive pills (n=46) and evaluated the differences in resting state activity between these two groups using independent component analysis. We found that in the default mode network and in a network associated with executive control, resting state dynamics were altered both by the menstrual cycle and by oral contraceptive use. Specifically, the connectivity of the left angular gyrus, the left middle frontal gyrus, and the anterior cingulate cortex were different between groups. Because the anterior cingulate cortex and left middle frontal gyrus are important for higher-order cognitive and emotional processing, including conflict monitoring, changes in the relationship of these structures to the functional networks with which they interact may have important consequences for attention, affect, and/or emotion regulation. PMID:24365676

  4. MHC-correlated odour preferences in humans and the use of oral contraceptives

    PubMed Central

    Roberts, S. Craig; Gosling, L. Morris; Carter, Vaughan; Petrie, Marion

    2008-01-01

    Previous studies in animals and humans show that genes in the major histocompatibility complex (MHC) influence individual odours and that females often prefer odour of MHC-dissimilar males, perhaps to increase offspring heterozygosity or reduce inbreeding. Women using oral hormonal contraceptives have been reported to have the opposite preference, raising the possibility that oral contraceptives alter female preference towards MHC similarity, with possible fertility costs. Here we test directly whether contraceptive pill use alters odour preferences using a longitudinal design in which women were tested before and after initiating pill use; a control group of non-users were tested with a comparable interval between test sessions. In contrast to some previous studies, there was no significant difference in ratings between odours of MHC-dissimilar and MHC-similar men among women during the follicular cycle phase. However, single women preferred odours of MHC-similar men, while women in relationships preferred odours of MHC-dissimilar men, a result consistent with studies in other species, suggesting that paired females may seek to improve offspring quality through extra-pair partnerships. Across tests, we found a significant preference shift towards MHC similarity associated with pill use, which was not evident in the control group. If odour plays a role in human mate choice, our results suggest that contraceptive pill use could disrupt disassortative mate preferences. PMID:18700206

  5. Acceptability of emergency contraception in Brazil, Chile, and Mexico: 1 - Perceptions of emergency oral contraceptives.

    PubMed

    Díaz, Soledad; Hardy, Ellen; Alvarado, Gloria; Ezcurra, Enrique

    2003-01-01

    This article presents the results of a study on the acceptability of emergency contraception (EC) in Brazil, Chile, and Mexico. Opinions of potential users and possible providers were obtained through discussion groups and those of authorities and policy-makers through semi-structured interviews. Most participants had a positive opinion of EC, based on the view that it can help reduce unplanned pregnancy, adolescent pregnancy, and unsafe abortion. Several interviewees felt that all women should be informed about EC, while others viewed it as a method for special situations such as rape and unprotected first sexual intercourse. Concern was expressed that its introduction might be associated with a decrease in condom use, increase in sexually transmitted diseases, and irresponsible or promiscuous sexual behavior among adolescents. The need for EC was clearly perceived by most participants, leading to the conclusion that health authorities have the responsibility of implementing programs for its introduction. Training of health care personnel should include the discussion of reproductive health problems that could be prevented by EC. PMID:14666232

  6. [Monoclonal human immunoglobulin (IgG lambda) with antiethinylestradiol activity, oral contraceptives, and arterial pulmonary thrombosis].

    PubMed

    Beaumont, J L; Lemort, N

    1975-06-23

    In a 36-year-old woman taking an oral contraceptive containing 50 mug of ethinyloestradiol each day, a pulmonary arterial thrombosis and a monoclonal gammapathia were associated. The monoclonal IgI lambda Mai... was prepared. When purified, this IgG lambda binds ethinyloestradiol with strong affinity (Ka= 2.7 times 10(7)M-1) and also 17-beta-oestradiol with a little less affinity (Ka = 0.4 times 10(7)M-1. For those ligands each IgG lambda Mai... molecule has two sites of same affinity and specificity so that a Scatchard plot of the experimental values gives a straight line. It is likely that the antibody sites of the IgG lambda Mai... are the binding sites. These facts support the hypothesis of an immunological mechanism of the thromboembolic disease which may be induced by oral contraceptives. PMID:808320

  7. A case-series study of cerebral venous thrombosis in women using short course oral contraceptive

    PubMed Central

    Khomand, Payam; Hassanzadeh, Kambiz

    2016-01-01

    Background: We report a case series of cerebral vein thrombosis (CVT) in women who used oral contraceptive pill (OCP) in the Muslims Ramadan and fasting month. Methods: This study was a retrospective case series of 9 patients with diagnosis of CVT, who admitted in the neurology ward of Tohid Hospital of Sanandaj, Iran, in July-August 2014-2015. Results: Patients had no history of thrombosis before. They were treated with oral contraceptive more than 1 month to be able to fast during Ramadan. They did not have other possible risk factors for CVT. A headache was the most common in 9/9 patients (100%) followed by vomiting and vertigo. Conclusion: We found that high rate of CVT in female population during Ramadan indicates that it needs be considered as a specific risk factor and should be considered by healthcare system. PMID:27326364

  8. Resting state alpha frequency is associated with menstrual cycle phase, estradiol and use of oral contraceptives.

    PubMed

    Brötzner, Christina P; Klimesch, Wolfgang; Doppelmayr, Michael; Zauner, Andrea; Kerschbaum, Hubert H

    2014-08-19

    Ongoing intrinsic brain activity in resting, but awake humans is dominated by alpha oscillations. In human, individual alpha frequency (IAF) is associated with cognitive performance. Noticeable, performance in cognitive and emotional tasks in women is associated with menstrual cycle phase and sex hormone levels, respectively. In the present study, we correlated frequency of alpha oscillation in resting women with menstrual cycle phase, sex hormone level, or use of oral contraceptives. Electroencephalogram (EEG) was recorded from 57 women (aged 24.07 ± 3.67 years) having a natural menstrual cycle as well as from 57 women (aged 22.37 ± 2.20 years) using oral contraceptives while they sat in an armchair with eyes closed. Alpha frequency was related to the menstrual cycle phase. Luteal women showed highest and late follicular women showed lowest IAF or center frequency. Furthermore, IAF as well as center frequency correlated negatively with endogenous estradiol level, but did not reveal an association with endogenous progesterone. Women using oral contraceptives showed an alpha frequency similar to women in the early follicular phase. We suggest that endogenous estradiol modulate resting alpha frequency. PMID:25010817

  9. Noncontraceptive benefits of the estradiol valerate/dienogest combined oral contraceptive: a review of the literature

    PubMed Central

    Nappi, Rossella E; Serrani, Marco; Jensen, Jeffrey T

    2014-01-01

    Combined oral contraceptives formulated to include estradiol (E2) have recently become available for the indication of pregnancy prevention. A combined estradiol valerate and dienogest pill (E2V/DNG), designed to be administered using an estrogen step-down and a progestin step-up regimen over 26 days of active treatment followed by 2 days of placebo (26/2-day regimen), has also undergone research to assess the potential for additional noncontraceptive benefits. Randomized, placebo-controlled studies have demonstrated that E2V/DNG is an effective treatment for heavy menstrual bleeding – a reduction in median menstrual blood loss approaching 90% occurs after 6 months of treatment. To date, E2V/DNG is the only oral contraceptive approved for this indication. Comparator studies have also demonstrated a reduction in hormone withdrawal-associated symptoms in users of E2V/DNG compared with a conventional 21/7-day regimen of ethinylestradiol/levonorgestrel. Other potential noncontraceptive benefits associated with E2V/DNG, like improvement in dysmenorrhea, sexual function, and quality of life, are comparable with those associated with other combined oral contraceptives and are discussed further in this review. PMID:25120376

  10. Sexual and reproductive life events in relation to duration of oral contraceptive use.

    PubMed

    Lidegaard, O; Helm, P

    1988-07-01

    In order to disclose differences between users and non-users of oral contraceptives (OC), 620 women aged 15-54 were invited to participate in an in depth interview about sexual, contraceptive, and reproductive life events. Of the 585 women who participated, 459 were consecutive gynecological in- or outpatients, and 126 were selected from visitors in general practice. Data was analysed by multivariate test statistics. After correction for present age and social class, the duration of use of OC (DOC) among women 15-34 years of age correlated negatively to age at menarche and coital debut and positively to number of sexual partners, oral-genital sexual practice, and number of pelvic inflammatory diseases. Among women over 35, DOC was positively associated only to cigarette smoking. No correlation was found to coital frequency (whether earlier, present or during pregnancy or menstruation), number of births and abortions, or to social classification. In epidemiological research on benefits and risks of oral contraceptives, confounding influence of one or more variables is of crucial importance. The present findings point at sexual and life-style habits as potential confounders in the study of OC and associated diseases. PMID:3168446

  11. Comparative study of the effects of combined oral contraceptives in hemostatic variables: an observational preliminary study.

    PubMed

    Stocco, Bianca; Fumagalli, Helen F; Franceschini, Silvio A; Martinez, Edson Z; Marzocchi-Machado, Cleni M; de Sá, Marcos Felipe S; Toloi, Maria Regina T

    2015-01-01

    Thrombotic risk is associated with the estrogen dose and type of progestin in combined oral contraceptives. Studies published since 1990 showed that third-generation progestins have larger risk to contribute to thrombosis development than the second-generation. However, there are conflicts in the literature regarding the thrombotic risk associated to the drospirenone progestin. So, this study aimed to evaluate the effects of 3 formulations of contraceptives containing ethinylestradiol (EE) (20 and 30 μg) combined with drospirenone versus levonorgestrel combined with EE (30 μg) in hemostatic parameters. This cross-sectional study included 70 healthy women between 18 and 30 years, BMI 19 to 30 kg/m², not pregnant, non-smokers, and users or non-users (control) of contraceptives for a minimum period of 6 months. The following parameters were assessed: prothrombin time (PT), Factor VII, activated partial thromboplastin time (aPTT), Factor XII, fibrinogen, Factor 1 + 2, Protein C, Protein S, antithrombin, D-dimers, and plasminogen activator inhibitor-1. Significant alterations were found in PT, aPTT, fibrinogen, D-dimers, and protein S, all favoring a state of hypercoagulation for contraceptive containing DRSP/20EE. Both contraceptives containing DRSP/30EE and LNG/30EE promoted changes that favor the hypercoagulability in the coagulant variable PT and in the anticoagulant variables Protein S and Protein C, respectively. We suggest that the progestin drospirenone can contribute to an inadequate balance among procoagulant, anticoagulant, and fibrinolytic factors, since that the contraceptive containing the lowest dose of estrogen and drospirenone (DRSP/20EE) caused a higher number of hemostatic changes. PMID:25634167

  12. Effect of preparation method on properties of orally disintegrating tablets made by phase transition.

    PubMed

    Kuno, Yoshio; Kojima, Masazumi; Ando, Shuichi; Nakagami, Hiroaki

    2008-05-01

    In order to evaluate the effect of preparation method on the properties of orally disintegrating (OD) tablets, OD tablets were prepared by compressing a mixture of high melting point sugar alcohol (HMP-SA) and low melting point sugar alcohol (LMP-SA) and subsequent heating. In the direct compression method (DCM) where the LMP-SA was added as a powder, both hardness and disintegration time were increased by decreasing the particle size of the LMP-SA. In the wet granule compression method (WGCM), where the LMP-SA was added as an aqueous binder solution, the tablets became harder with less heating compared to tablets prepared by DCM. Using 1% xylitol as the LMP-SA provided tablets with sufficient hardness when prepared by WGCM, as opposed to DCM where 5% xylitol was necessary to prepare tablets with similar hardness. These results suggest that uniformly distributed LMP-SA on the surface of HMP-SA particles in WGCM might diffuse more easily during the heating process compared to mechanically mixed LMP-SA in DCM, resulting in an increase in tablet hardness even with a short heating time and low content of LMP-SA. In addition, disintegration and hardness stability of the tablets were affected by the LMP-SA content when prepared by WGCM, suggesting that the LMP-SA content should be regulated to assure the stability of OD tablet characteristics. PMID:18182258

  13. The effect of pycnogenol on patients with dysmenorrhea using low-dose oral contraceptives

    PubMed Central

    Maia, Hugo; Haddad, Clarice; Casoy, Julio

    2014-01-01

    Objective Menstrual symptoms such as dysmenorrhea usually occur during the hormone-free interval in oral contraceptive users. Progestin withdrawal activates NF-κB transcription factor, which upregulates both vascular endothelial growth factor (VEGF) and Cox-2 expression in the endometrium. The use of natural NF-κB inhibitors such as pycnogenol may block this response, improving dysmenorrhea. Patients and methods Twenty-four patients with severe dysmenorrhea were allocated to one of two treatment groups. In Group A (n=13), women were treated with an oral contraceptive containing 15 μg of ethinyl estradiol and 60 mg of gestodene (Adoless®) in a 24/4 regimen for three consecutive cycles. Women in Group B (n=11) used the same contraceptive regimen together with 100 mg of pycnogenol (Flebon®) continuously for 3 months. Pain scores were graded using a visual analog scale (VAS) before and during the hormone-free interval at the end of the third treatment cycle. Results Before treatment, VAS pain scores for dysmenorrhea were 8 and 9 in Groups A and B, respectively. However, by the end of the third treatment cycle, pain scores had decreased significantly (P<0.05) both in groups A and B. The final pain scores were 6 in Group A and 2 in Group B, a difference that was statistically significant (P<0.0001). In Group B, 27% of the patients became pain-free, while in Group A, none of the women reported complete disappearance of this symptom. The number of bleeding days was also lower in Group B. Discussion Pycnogenol effectively decreased pain scores and the number of bleeding days when administered concomitantly with a low-dose 24/4 oral contraceptive containing gestodene. PMID:25525393

  14. Efficacy of oral powder compared with chewable tablets for lanthanum carbonate administration in hemodialysis patients.

    PubMed

    Sakurada, Tsutomu; Oishi, Daisuke; Shibagaki, Yugo; Yasuda, Takashi; Kimura, Kenjiro

    2013-10-01

    Lanthanum carbonate (LC) has been administered in a chewable tablet form for patients with hyperphosphatemia undergoing dialysis. However, some patients have difficulty chewing the tablets. LC oral powder has recently been released in Japan. The purpose of this study was to clarify the efficacy of LC oral powder form compared with that of chewable tablet form. The efficacy and safety of LC oral powder was retrospectively assessed in hemodialysis patients who switched from chewable tablet form to oral powder form without dose modification. Thirty-six patients (mean age, 66.8 ± 10.5 years; male, 64%; 39% with diabetes; mean duration of dialysis treatment, 99.2 ± 95.6 months) were enrolled in this study between June and July of 2012. Changes in clinical data and adverse events after the switch to oral powder form were investigated. The average dose of LC was 1180 ± 520 mg/day. Serum phosphorus levels were significantly decreased after the switch from chewable tablet form to oral powder form (5.3 ± 1.7 mg/dL at baseline vs. 4.9 ± 1.2 mg/dL at after 1 month after, P = 0.038). In contrast, no significant differences were observed in serum calcium and parathyroid hormone levels. Furthermore, no significant differences were evident in weight gain after the switch to oral powder form (2.5 ± 1.2 kg at baseline vs. 2.4 ± 1.1 kg at 1 month after the switch, P = 0.29). No serious adverse events were recorded. Our results suggest that LC is more effective in oral powder form than chewable tablet form for hemodialysis patients. PMID:24134326

  15. Oral Disintegration Tablets of Stavudine for HIV Management: A New Technological Approach.

    PubMed

    Sankar, V; Ramakrishna, B; Devi, P Shalini; Karthik, S

    2012-11-01

    Stavudine oral disintegration tablets were formulated to minimize the bitter taste and to reduce the first-pass hepatic metabolism. The various precompression parameters like the angle of repose, bulk density, compressibility index and Hausner's ratio were determined for the powder blend. In this study, 14 formulations of stavudine oral disintegration tablet were prepared by direct compression method. The tablets were evaluated for weight variation, percentage friability, disintegration time, hardness, wetting time and water absorption ratio. The in vitro dissolution study results of the batch S1 (stavudine+crospovidone+sodium starch glycollate) are encouraging as highest dissolution rate (99.2% in 100 min) and lowest time of disintegration (56 s) was achieved. The in vivo drug release studies were carried out in rabbits and the relative bioavailability of formulation S1 was found to be 2.83 times greater than that of conventional tablets. PMID:23798782

  16. Relationship between premenstrual symptoms and oral contraceptive use: a controlled study.

    PubMed

    Walker, A; Bancroft, J

    1990-01-01

    Patterns of menstrual cycle-related change were compared in three groups of women differing in their use of oral contraceptives and being matched for age, occupation, and parity. These groups were: a "monophasic group" (n = 35) established on low dose "combined" pills with stable levels of estrogen and progestagen. a "triphasic group" (n = 30) on low dose pills with escalating progestagen dosage, and a "non-pill control group" (n = 57) using nonsteroidal contraceptives. Each woman kept visual analogue ratings of mood, irritability, energy, tension, breast tenderness, bloating, and sexual interest for two or three cycles. Cyclicity was evident in all variables assessed, but the only variable to show a clear difference between groups was breast tenderness; the "monophasic group" showed less premenstrual breast tenderness than the other two groups. The monophasic group also showed a tendency to menstrual rather than premenstrual symptoms. In view of the similarity of timing of most cyclical symptoms in the three groups, it is difficult to attribute such cyclical phenomena to the effects of either ovulation or variation in corpus luteum function. For most subjects, the cyclical changes were relatively mild, and these findings need to be replicated in women suffering from severe premenstrual syndrome. However, alternative explanations need to account for changes in women both taking and not taking oral contraceptives. PMID:2305025

  17. Effect of Oral Contraceptive Pills on the Blood Serum Enzymes and DNA Damage in Lymphocytes Among Users.

    PubMed

    Naz, Falaq; Jyoti, Smita; Rahul; Akhtar, Nishat; Siddique, Yasir Hasan

    2016-07-01

    The continuous use of synthetic hormones as contraceptive pill or hormonal replacement therapy among women is increasing day by day. The widespread use of different formulations as oral contraceptives by women throughout their reproductive cycle has given rise to a serious concern for studying the effects of oral contraceptives on enzymatic profile and DNA damage in peripheral blood lymphocytes among users. The present study was carried out on women taking oral contraceptives. The study was based on the questionnaire having the information of reproductive history, fasting, age, health, nature of menstrual cycle, bleeding and other disease. The profile of the blood serum enzymes i.e. alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), lactate dehydrogenase (LDH), aminotransferases (SGOT and SGPT), serum proteins (albumin and globulin) and DNA damage in lymphocytes was studied among users and non-users. The results of the present study suggest that OCs not only effects enzymatic activity but also results in DNA damage that may vary with the duration of using oral contraceptives. A significant increase in LDH, GGT, SGPT, SGOT, globulin and decrease in ALP as well as albumin was found among users as compared to non-users. The observed DNA damage was more in users as compared to non-users. Hormonal contraceptives seem to exert DNA damage and also have significant effects on blood serum enzymes. PMID:27382200

  18. Development of oral dispersible tablets containing prednisolone nanoparticles for the management of pediatric asthma

    PubMed Central

    Chen, Yi-Dan; Liang, Zhong-Yuan; Cen, Yan-Yan; Zhang, He; Han, Mei-Gui; Tian, Yun-Qiao; Zhang, Jie; Li, Shu-Jun; Yang, Da-Sheng

    2015-01-01

    The purpose of the present study was to develop oral dispersible tablets containing prednisolone (PDS)-loaded chitosan nanoparticles using microcrystalline cellulose (MCC 101), lactose, and croscarmellose sodium (CCS). The PDS-loaded chitosan nanoparticles were formulated by ionotropic external gelation technique in order to enhance the solubility of PDS in salivary pH. Prepared nanoparticles were used for the development of oral fast disintegrating tablets by direct compression method. The prepared tablets were evaluated for disintegration time (DT), in vitro drug release (DR), thickness, weight variation, drug content uniformity, friability, and hardness. The effect of concentrations of the dependent variables (MCC, lactose, CCS) on DT and in vitro DR was studied. Fast disintegrating tablets of PDS can be prepared by using MCC, CCS, and lactose with enhanced solubility of PDS. The minimum DT was found to be 15 seconds, and the maximum DR within 30 minutes was 98.50%. All independent variables selected for the study were statistically significant. Oral fast disintegrating tablets containing PDS nanoparticles could be the better choice for the pediatric patients that would result in better patient compliance. From this study, it can be concluded that fast disintegrating tablets could be a potential drug delivery technology for the management of asthma in pediatrics. PMID:26640367

  19. Development of oral dispersible tablets containing prednisolone nanoparticles for the management of pediatric asthma.

    PubMed

    Chen, Yi-Dan; Liang, Zhong-Yuan; Cen, Yan-Yan; Zhang, He; Han, Mei-Gui; Tian, Yun-Qiao; Zhang, Jie; Li, Shu-Jun; Yang, Da-Sheng

    2015-01-01

    The purpose of the present study was to develop oral dispersible tablets containing prednisolone (PDS)-loaded chitosan nanoparticles using microcrystalline cellulose (MCC 101), lactose, and croscarmellose sodium (CCS). The PDS-loaded chitosan nanoparticles were formulated by ionotropic external gelation technique in order to enhance the solubility of PDS in salivary pH. Prepared nanoparticles were used for the development of oral fast disintegrating tablets by direct compression method. The prepared tablets were evaluated for disintegration time (DT), in vitro drug release (DR), thickness, weight variation, drug content uniformity, friability, and hardness. The effect of concentrations of the dependent variables (MCC, lactose, CCS) on DT and in vitro DR was studied. Fast disintegrating tablets of PDS can be prepared by using MCC, CCS, and lactose with enhanced solubility of PDS. The minimum DT was found to be 15 seconds, and the maximum DR within 30 minutes was 98.50%. All independent variables selected for the study were statistically significant. Oral fast disintegrating tablets containing PDS nanoparticles could be the better choice for the pediatric patients that would result in better patient compliance. From this study, it can be concluded that fast disintegrating tablets could be a potential drug delivery technology for the management of asthma in pediatrics. PMID:26640367

  20. Extended regimen combined oral contraception: A review of evolving concepts and acceptance by women and clinicians

    PubMed Central

    Nappi, Rossella E.; Kaunitz, Andrew M.; Bitzer, Johannes

    2016-01-01

    ABSTRACT Objectives: The clinical utility of extended regimen combined oral contraceptives (COCs) is increasingly being recognised. Our objective was to understand the attitudes of women and clinicians about the use of these regimens. We present the rationale for extended regimen COCs from a historical perspective, and trace their evolution and growing popularity in light of their clinical benefits. We conclude by offering potential strategies for counselling women about extended regimen COC options. Methods: We conducted a MEDLINE search to identify and summarise studies of extended regimen COCs, focusing on attitudes of women and clinicians regarding efficacy, safety/tolerability and fewer scheduled bleeding episodes and other potential benefits. Results: The body of contemporary literature on extended regimen COCs suggests that their contraceptive efficacy is comparable to that of conventional 28-day (i.e., 21/7) regimens. For women seeking contraception that allows infrequent scheduled bleeding episodes, particularly those who suffer from hormone withdrawal symptoms and cyclical symptoms (e.g., headache, mood changes, dysmenorrhoea, heavy menstrual bleeding), extended regimen COCs are an effective and safe option. Although satisfaction with extended regimen COCs in clinical trials is high, misperceptions about continuous hormone use may still limit the widespread acceptance of this approach. Conclusions: Despite the widespread acceptance among clinicians of extended regimen COCs as an effective and safe contraceptive option, these regimens are underused, likely due to a lack of awareness about their availability and utility among women. Improved patient education and counselling regarding the safety and benefits of extended regimen COCs may help women make more informed contraceptive choices. PMID:26572318

  1. Bioavailability, pharmacokinetics, and safety of riociguat given as an oral suspension or crushed tablet with and without food

    PubMed Central

    Frey, Reiner; Becker, Corina; Unger, Sigrun; Wensing, Georg; Mück, Wolfgang

    2016-01-01

    Abstract Riociguat is approved for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. Some patients have difficulty swallowing tablets; therefore, 2 randomized, nonblinded, crossover studies compared the relative bioavailability of riociguat oral suspensions and immediate-release (IR) tablet and of crushed-tablet preparations versus whole IR tablet. In study 1, 30 healthy subjects received 5 single riociguat doses: 0.3 and 2.4 mg (0.15 mg/mL suspensions), 0.15 mg (0.03 mg/mL), and 1.0 mg (whole IR tablet) under fasted conditions and 2.4 mg (0.15 mg/mL) after a high-fat, high-calorie American-style breakfast. In study 2, 25 healthy men received 4 single 2.5-mg doses: whole IR tablet and crushed IR tablet suspended in applesauce and water, respectively, under fasted conditions, and whole IR tablet after a continental breakfast. In study 1, dose-normalized pharmacokinetics of riociguat oral suspensions and 1.0-mg whole IR tablet were similar in fasted conditions; 90% confidence intervals for riociguat area under the curve (AUC) to dose and mean maximum concentration (Cmax) to dose were within bioequivalence criteria. After food, dose-normalized AUC and Cmax decreased by 15% and 38%, respectively. In study 2, riociguat exposure was similar for all preparations; AUC ratios for crushed-IR-tablet preparations to whole IR tablet were within bioequivalence criteria. The Cmax increased by 17% for crushed IR tablet in water versus whole IR tablet. Food intake decreased Cmax of the whole tablet by 16%, with unaltered AUC versus fasted conditions. Riociguat bioavailability was similar between the oral suspensions and the whole IR tablet; exposure was similar between whole IR tablet and crushed-IR-tablet preparations. Minor food effects were observed. Results suggest that riociguat formulations are interchangeable. PMID:27162630

  2. Formulation and in vivo evaluation of ondansetron orally disintegrating tablets using different superdisintegrants.

    PubMed

    Sheshala, Ravi; Khan, Nurzalina; Chitneni, Mallikarjun; Darwis, Yusrida

    2011-11-01

    The aim of this study was to formulate cost effective taste-masked orally disintegrating tablets of ondansetron, a bitter drug using different superdisintegrants by a wet granulation technique. Microcrystalline cellulose (Avicel) as a diluent and disintegrant in addition to aspartame as a sweetener were used in all formulations. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. The tablets' hardness was maintained in the range of 2-3 kg and friability was <1% for all batches. All tablet formulations disintegrated rapidly in vitro within 5.83 to 33.0 sec. The optimized formulation containing 15% Polyplasdone XL-10 released more than 90% of drug within 5 min and the release was comparable to that of a commercial product. In human volunteers, optimized formulation was found to have a pleasant taste and mouth feel and they disintegrated in the oral cavity within 12 sec. The stability results were also satisfactory. A pharmacokinetic study with the optimized formulation was performed in comparison with a reference (Zofer MD 8®) and they were found to be bioequivalent. In conclusion, a cost effective ondansetron orally disintegrating tablet was successfully prepared with acceptable hardness, desirable taste and rapid disintegration in the oral cavity. PMID:22139694

  3. How does Intimate Partner Violence Affect Condom and Oral Contraceptive Use in the United States? A Systematic Review of the Literature

    PubMed Central

    Bergmann, Julie N.; Stockman, Jamila K.

    2015-01-01

    INTRODUCTION Intimate partner violence (IPV) is estimated to affect 25% of adult women in the US alone. IPV directly impacts women’s ability to use contraception, resulting in many of unintended pregnancies and STIs. This review examines the relationship between IPV and condom and oral contraceptive use within the United States at two levels: the female victim’s perspective on barriers to condom and oral contraceptive use, in conjunction with experiencing IPV (Aim 1) and the male perpetrator’s perspective regarding condom and oral contraceptive use (Aim 2). STUDY DESIGN We systematically reviewed and synthesized all publications meeting the study criteria published since 1997. We aimed to categorize the results by emerging themes related to each study aim. RESULTS We identified 42 studies that met our inclusion criteria. We found 37 studies that addressed Aim 1. Within this we identified three themes: violence resulting in reduced condom or oral contraceptive use (n=15); condom or oral contraceptive use negotiation (n=15); which we further categorized as IPV due to condom or oral contraceptive request, perceived violence (or fear) of IPV resulting in decreased condom or oral contraceptive use, and sexual relationship power imbalances decreasing the ability to use condoms or oral contraceptives; and reproductive coercion (n=7). We found 5 studies that addressed Aim 2. Most studies were cross-sectional, limiting the ability to determine causality between IPV and condom or oral contraceptive use; however, most studies did find a positive relationship between IPV and decreased condom or oral contraceptive use. CONCLUSIONS Quantitative, qualitative, and mixed methods research has demonstrated the linkages between female IPV victimization/male IPV perpetration and condom or oral contraceptive use. However, additional qualitative and longitudinal research is needed to improve the understanding of dynamics in relationships with IPV and determine causality between IPV

  4. Effects of menstrual cycle phase and oral contraceptives on alertness, cognitive performance, and circadian rhythms during sleep deprivation

    NASA Technical Reports Server (NTRS)

    Wright, K. P. Jr; Badia, P.; Czeisler, C. A. (Principal Investigator)

    1999-01-01

    The influence of menstrual cycle phase and oral contraceptive use on neurobehavioral function and circadian rhythms were studied in healthy young women (n = 25) using a modified constant routine procedure during 24 h of sleep deprivation. Alertness and performance worsened across sleep deprivation and also varied with circadian phase. Entrained circadian rhythms of melatonin and body temperature were evident in women regardless of menstrual phase or oral contraceptive use. No significant difference in melatonin levels, duration, or phase was observed between women in the luteal and follicular phases, whereas oral contraceptives appeared to increase melatonin levels. Temperature levels were higher in the luteal phase and in oral contraceptive users compared to women in the follicular phase. Alertness on the maintenance of wakefulness test and some tests of cognitive performance were poorest for women in the follicular phase especially near the circadian trough of body temperature. These observations suggest that hormonal changes associated with the menstrual cycle and the use of oral contraceptives contribute to changes in nighttime waking neurobehavioral function and temperature level whereas these factors do not appear to affect circadian phase.

  5. Evaluation of a unique oral contraceptive in the treatment of premenstrual dysphoric disorder.

    PubMed

    Freeman, E W; Kroll, R; Rapkin, A; Pearlstein, T; Brown, C; Parsey, K; Zhang, P; Patel, H; Foegh, M

    2001-01-01

    Premenstrual dysphoric disorder (PMDD) is a severe form of premenstrual syndrome (PMS). This is the first trial of a unique oral contraceptive containing a combination of drospirenone (DRSP, 3 mg) and ethinyl estradiol (EE, 30 microg) for the treatment of PMDD. DRSP is a spironolactone-like progestin with antiandrogenic and antimineralocorticoid activity. Spironolactone has been shown to be beneficial in PMS, whereas oral contraceptives have shown conflicting results. In this double-blind, placebo-controlled trial, 82 women with PMDD (Diagnostic and Statistical Manual of Mental Disorders, 4th ed. [DSM IV]) were randomized to receive DRSP/EE or placebo for three treatment cycles. The primary end point was change from baseline in luteal phase symptom scores as assessed on the Calendar of Premenstrual Experiences (COPE) scale. Patients treated with DRSP/EE showed a numerically greater change from baseline compared with those treated with placebo on each of the 22 COPE items and each of the 4 symptom factors. Between-group differences in symptom improvement reached statistical significance in factor 3 only (appetite, acne, and food cravings, p = 0.027). The secondary end points, Beck Depression Inventory (BDI) and Profile of Mood States (PMS), were consistent with the primary end point in that patients treated with the oral contraceptive showed a numerically greater improvement from baseline compared with those treated with placebo. The results of this study show a consistent trend in the reduction of symptoms that suggested a beneficial effect of DRSP/EE for the treatment of PMDD, despite limitations of the study design. PMID:11559453

  6. Formulation and Characterization of Oral Mucoadhesive Chlorhexidine Tablets Using Cordia myxa Mucilage

    PubMed Central

    Moghimipour, Eskandar; Aghel, Nasrin; Adelpour, Akram

    2012-01-01

    Background The dilution and rapid elimination of topically applied drugs due to the flushing action of saliva is a major difficulty in the effort to eradicate infections of oral cavity. Utilization a proper delivery system for incorporation of drugs has a major impact on drug delivery and such a system should be formulated for prolonged drug retention in oral cavity. Objectives The aim of the present study was the use of mucilage of Cordia myxa as a mucoadhesive material in production of chlorhexidine buccal tablets and its substitution for synthetic polymers such as HPMC. Materials and Methods The influence of mucilage concentration on the physicochemical responses (hardness, friability, disintegration time, dissolution, swelling, and muco-adhesiveness strength) was studied and swelling of mucilage and HPMC were compared. The evaluated responses included pharmacopoeial characteristics of tablets, the force needed to separate tablets from mucosa, and the amount of water absorbed by tablets. Results In comparison to HPMC, the rise of mucilage concentration in the formulations increased disintegration time, drug dissolution rate, and reduced MDT. Also, compared to 30% HPMC, muco-adhesiveness strength of buccal tablets containing 20% mucilage was significantly higher. Conclusions It can be concluded that the presence of Cordia myxa powdered mucilage may significantly affect the tablet characteristics, and increasing in muco-adhesiveness may be achieved by using 20% w/w mucilage. PMID:24624170

  7. Latent structure analysis of the process variables and pharmaceutical responses of an orally disintegrating tablet.

    PubMed

    Hayashi, Yoshihiro; Oshima, Etsuko; Maeda, Jin; Onuki, Yoshinori; Obata, Yasuko; Takayama, Kozo

    2012-01-01

    A multivariate statistical technique was applied to the design of an orally disintegrating tablet and to clarify the causal correlation among variables of the manufacturing process and pharmaceutical responses. Orally disintegrating tablets (ODTs) composed mainly of mannitol were prepared via the wet-granulation method using crystal transition from the δ to the β form of mannitol. Process parameters (water amounts (X(1)), kneading time (X(2)), compression force (X(3)), and amounts of magnesium stearate (X(4))) were optimized using a nonlinear response surface method (RSM) incorporating a thin plate spline interpolation (RSM-S). The results of a verification study revealed that the experimental responses, such as tensile strength and disintegration time, coincided well with the predictions. A latent structure analysis of the pharmaceutical formulations of the tablet performed using a Bayesian network led to the clear visualization of a causal connection among variables of the manufacturing process and tablet characteristics. The quantity of β-mannitol in the granules (Q(β)) was affected by X(2) and influenced all granule properties. The specific surface area of the granules was affected by X(1) and Q(β) and had an effect on all tablet characteristics. Moreover, the causal relationships among the variables were clarified by inferring conditional probability distributions. These techniques provide a better understanding of the complicated latent structure among variables of the manufacturing process and tablet characteristics. PMID:22878814

  8. Stability of cilazapril in pediatric oral suspensions prepared from commercially available tablet dosage forms.

    PubMed

    Stanisz, Beata J; Paszun, Sylwia K; Zalewska, Anna

    2014-01-01

    Abstract: Cilazapril is a drug commonly used in management of heart failure in pediatric population. On pharmaceutical market it is available only in inconvenient for pediatric use tablet dosage forms. Until now, no oral liquid formulation containing cilazapril has been evaluated. Therefore, the aim of this study was to prepare easy to made and palatable 1 mg/mL oral liquid formulation with cilazapril (with consideration of original and generic cilazapril tablet and different packages) and subsequent investigation of physicochemical stability of these suspensions. Formulations were compounded using cilazapril obtained from original or generic cilazapril marketed tablet formulations and Ora-Blend" suspending agent. Stability of prepared suspensions stored in closed amber glass or amber plastic PET bottles in the temperature of 298 K was estimated throughout 28 day shelf-life period. Chemical stability was assessed by HPLC cilazapril stability indicating method. Physical stability was evaluated by appearance, taste, smell, pH and theological assessments. Cilazapril oral suspensions at concentration of 1 mg/mL demonstrated satisfactory stability over 28 day long storage at room temperature. Cilazapril concentrations remained within acceptable limit (+/- 10%) stored in closed amber bottles made of glass or PET material. Moreover, suspensions physical properties remained unaffected. Cilazapril - Ora-Blend* pediatric oral liquid is easy to made, palatable and stable when stored at room temperature for 28 days. Stability of cilazapril oral liquid remains unchanged while using cilazapril tablets produced by different manufacturers and bottles made of amber glass or PET material. PMID:25272892

  9. Combined oral contraceptives for the treatment of acne: a practical guide.

    PubMed

    Arrington, Elizabeth A; Patel, Nishit S; Gerancher, Karen; Feldman, Steven R

    2012-08-01

    Many therapies exist in the arsenal of drugs available to dermatologists for the treatment of acne vulgaris. Among them, hormonal therapy stands out as a unique and highly efficacious treatment modality. Although some dermatologists may be hesitant to prescribe hormonal therapies, they can be safely and appropriately used in eligible female patients to treat acne vulgaris. Herein, current issues regarding the hormonal treatment of acne in the form of combined oral contraceptives (COCs) are presented, and a practical method for implementing this therapy is proposed. Specifically, drug selection, associated risks, benefits, monitoring, and counseling are discussed, with emphasis on the practicality of use in the clinical setting. PMID:22988652

  10. Ovarian Follicular Development During the Use of Oral Contraception: A Review

    PubMed Central

    Baerwald, Angela R.; Pierson, Roger A.

    2010-01-01

    Over the past 40 years, alterations to the composition of oral contraceptives (OCs) have been made in attempts to reduce adverse effects and to improve patient compliance while maintaining contraceptive efficacy. However, there is growing evidence to indicate that reducing the estrogen dose to minimize adverse effects may have compromised the degree of hypothalamo-pituitary-ovarian suppression, particularly during the hormone-free interval (HFI) or following missed doses. Follicle development during OC use appears to occur in association with a loss of endocrine suppression during the HFI. This information provides a rationale for reducing or eliminating the HFI in OC regimens. There is also evidence for an increased risk of follicle development and ovulation in women who use delayed OC initiation schemes, such as the “Sunday Start” method. It is not currently known why some follicles ovulate during OC use while others regress or form anovulatory follicle cysts. Continued research about follicle development during OC use would provide insight into understanding the precise mechanisms of action underlying combined OCs, as well as those of continuous OC formulations and emergency contraceptive regimens. PMID:14715122

  11. The dynamics of oral contraceptive use in The Netherlands 1990-1993.

    PubMed

    Oddens, B J; Arnolds, H T; Van Maris, M G; Van Lunsen, H W

    1994-09-01

    Data from an ongoing series of surveys on contraceptive use in the Netherlands were analyzed with respect to the percentages of oral contraceptive (OC) users who annually started use, discontinued use or switched to another OC type. The surveys had been conducted between 1990 and 1993 among samples of women aged 15-49 who belonged to a survey panel. Response rates of the surveys were 89-90% and the sample sizes ranged from 4560 to 4621 women. The assessed OC use rates reflected those of the Dutch population reasonably well. Of all respondents who had used OCs during the 12 months prior to the surveys, 12-15% discontinued use within this period, mainly in order to get pregnant, 12-16% were starters and 9-14% switchers. Of all starters 37% switched to another OC type within the first 12 months after starting. Switching was mainly related to the experience of perceived side-effects and wishes for better cycle control. The results highlighted the relevance of closely monitoring the individual woman's satisfaction with her OC. Since OC use appeared in many cases to be characterized by an active seeking for the most acceptable OC type, a wide range of OC types available and the development and introduction of new types is highly relevant for tailoring contraceptive use to individual needs. PMID:7863842

  12. Relationship satisfaction and outcome in women who meet their partner while using oral contraception

    PubMed Central

    Roberts, S. Craig; Klapilová, Kateřina; Little, Anthony C.; Burriss, Robert P.; Jones, Benedict C.; DeBruine, Lisa M.; Petrie, Marion; Havlíček, Jan

    2012-01-01

    Hormonal variation over the menstrual cycle alters women's preferences for phenotypic indicators of men's genetic or parental quality. Hormonal contraceptives suppress these shifts, inducing different mate preference patterns among users and non-users. This raises the possibility that women using oral contraception (OC) choose different partners than they would do otherwise but, to date, we know neither whether these laboratory-measured effects are sufficient to exert real-world consequences, nor what these consequences would be. Here, we test for differences in relationship quality and survival between women who were using or not using OC when they chose the partner who fathered their first child. Women who used OC scored lower on measures of sexual satisfaction and partner attraction, experienced increasing sexual dissatisfaction during the relationship, and were more likely to be the one to initiate an eventual separation if it occurred. However, the same women were more satisfied with their partner's paternal provision, and thus had longer relationships and were less likely to separate. These effects are congruent with evolutionary predictions based on cyclical preference shifts. Our results demonstrate that widespread use of hormonal contraception may contribute to relationship outcome, with implications for human reproductive behaviour, family cohesion and quality of life. PMID:21993500

  13. Knowledge and attitudes of Latin American gynecologists regarding unplanned pregnancy and use of combined oral contraceptives

    PubMed Central

    Bahamondes, Luis; Lira-Plascencia, Josefina; Martin, Ricardo; Marin, Victor; Makuch, Maria Y

    2015-01-01

    Background Unintended pregnancy is a public health problem and unmet medical need worldwide. It is estimated that in the year 2012, almost 213 million pregnancies occurred, and the global pregnancy rate decreased only slightly from 2008 to 2012. It was also estimated that 85 million pregnancies (40% of all pregnancies) were unintended and that 38% ended in an unintended birth. Objectives To assess knowledge and attitudes of Latin American (LA) obstetricians and gynecologists (OBGYNs) regarding unintended pregnancies and aspects of combined oral contraceptive (COC) use. Methods A survey was conducted during a scientific meeting about contraception in 2014, in which OBGYNs from 12 LA countries who provide attention in contraception were invited to respond to a multiple-choice questionnaire to assess their knowledge and attitudes regarding unplanned pregnancy and some aspects regarding COC use. Results A total of 210 OBGYNs participated in the study. Their knowledge regarding COC failure was low. The participants reported they believed that their patients habitually forgot to take a pill and that their patients did not know what to do in these situations. They were aware of the benefits of COC use; however, they were less prone to prescribe COCs for the purpose of protecting against ovarian and endometrial cancer, and one-quarter of them had doubts about the association between COC use and cancer risk. Conclusion The interviewed LA OBGYNs showed some flaws in terms of knowledge of COC failure rates and the non-contraceptive benefits and risks of COCs. To adequately counsel their patients regarding COC intake, OBGYNs must be updated regarding all aspects of COC use. PMID:25999766

  14. The underrated benefits of oral contraception: consequences of pregnancy and induced abortion in teenagers.

    PubMed

    Dreyfus, R

    1992-01-01

    If complications occur within a pregnancy planned and brought to term, they often can be dealt with and accepted. They are even more traumatic when they occur in an unwanted pregnancy that could have been prevented through contraception. Teenagers, because of their physical and psychological immaturity and also because of their social environment, seem to suffer with undue frequency from the complications of induced abortion. Its result, for the teenager, is a handicapped future in comparison to other women. Hence, access to contraception is important for all women, and especially for teenagers, in order to avoid such prejudicial situations. It is important, then, to prescribe oral contraception for its efficacy and its short- and long-term innocuousness. Because of her immaturity, the pregnant teenager is at risk: of spontaneous abortion, pre-eclampsia, anemia, hemorrhage, and prematurity. She is also at risk because of the social difficulties she will be facing. This is particularly true in families from developing countries. From birth, the child is also at risk: of low birth weight for the term, mortality in the first year of life, and all risks linked to abandonment, or education by a third party. In a proportion of 13 to 30% in western countries and in a proportion of 3% in East Asia or in Northwest Africa (Maghreb), induced abortions are a reflection of the following: early sexual activity without contraception even if fertility is still low in very young teenagers, absence of social protection or social independence, refusal of forced marriage, and presence or absence of liberal legislation.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:1362187

  15. Lyophilized mucoadhesive-dendrimer enclosed matrix tablet for extended oral delivery of albendazole.

    PubMed

    Mansuri, Shakir; Kesharwani, Prashant; Tekade, Rakesh Kumar; Jain, Narendra Kumar

    2016-05-01

    Dendrimers are multifunctional carriers widely employed for delivering drugs in a variety of disease conditions including HIV/AIDS and cancer. Albendazole (ABZ) is a commonly used anthelmintic drug in human as well as veterinary medicine. In this investigation, ABZ was formulated as a "muco-dendrimer" based sustained released tablet. The mucoadhesive complex was synthesized by anchoring chitosan to fifth generation PPI dendrimer (Muco-PPI) and characterized by UV, FTIR, (1)H NMR spectroscopy and electron microscopy. ABZ was entrapped inside Muco-PPI followed by lyophilization and tableting as matrix tablet. A half-life (t1/2) of 8.06±0.15, 8.17±0.47, 11.04±0.73, 11.49±0.92, 12.52±1.04 and 16.9±1.18h was noted for ABZ (free drug), conventional ABZ tablet (F1), conventional ABZ matrix tablet (F2), PPI-ABZ complex, PPI-ABZ matrix tablet (F3) and Muco-PPI-ABZ matrix tablet (F4), respectively. Thus the novel mucoadhesive-PPI based formulation of ABZ (F4) increased the t1/2 of ABZ significantly by almost twofold as compared to the administration of free drug. The in vivo drug release data showed that the Muco-PPI based formulations have a significantly higher Cmax (2.40±0.02μg/mL) compared with orally administered free ABZ (0.19±0.07μg/mL) as well as conventional tablet (0.20±0.05μg/mL). In addition, the Muco-PPI-ABZ matrix tablet displayed increased mean residence time (MRT) and is therefore a potential candidate to appreciably improve the pharmacokinetic profile of ABZ. PMID:26563727

  16. Mirtazapine orally disintegrating tablet versus sertraline: a prospective onset of action study.

    PubMed

    Behnke, Kirsten; Søgaard, Jesper; Martin, Stephen; Bäuml, Josef; Ravindran, Arun V; Agren, Hans; Vester-Blokland, Estelle D

    2003-08-01

    This multinational, randomized, double-blind study was specifically designed to prospectively compare the onset of antidepressant efficacy of mirtazapine orally disintegrating tablets and sertraline at dosages commonly used in clinical practice. A total of 345 patients with major depressive episode (DSM-IV) received mirtazapine (30-45 mg/d) or sertraline (50-150 mg/d) for 8 weeks. Mirtazapine was administered in the newly developed fast dissolving, orally disintegrating tablet formulation. Assessments were performed at baseline and on days 4, 7, 10, 14, 28, 42, and 56. The primary efficacy variable (mean absolute change from baseline in the Hamilton Depression Rating Scale [HAMD] total score [17 items]) showed that mirtazapine was significantly (P < 0.05) more effective than sertraline at all assessments during the first 2 weeks of the study. After this time, HAMD total scores were similar in both groups. These findings were supported by analysis of the HAMD response rate (ie, > or =50% reduction in HAMD total score from baseline), HAMD remission rate (HAMD total score of < or =7), and the Montgomery-Asberg Depression Rating Scale (MADRS). Both treatments were well tolerated. In addition, mirtazapine had a greater effect than sertraline on sexual functioning. In conclusion, this first prospective onset of action study using the orally disintegrating tablet indicates that mirtazapine has a faster onset of therapeutic effect than sertraline. The orally disintegrating tablet formulation of mirtazapine used in this study is known to enhance the convenience and compliance by the patient. PMID:12920411

  17. Masculinizing effects on otoacoustic emissions and auditory evoked potentials in women using oral contraceptives.

    PubMed

    McFadden, D

    2000-04-01

    The otoacoustic emissions (OAEs) and auditory evoked potentials (AEPs) measured in two separate large scale studies were examined retrospectively for potential differences between those women using, and those not using, oral contraception (OC). Fourteen dependent variables were examined, all of which exhibited substantial sex differences. For 13 of those 14 dependent variables, the means for the users of OC were shifted away from the means of the non-users in the direction of the males. Specifically, for four different measures of OAE strength, for seven of eight measures of AEP latency or amplitude, and for two cognitive tests (mental rotation and water level), the means for the users of OC were located intermediate to those of the non-users of OC and the males. Few of these differences between users and non-users of OC achieved statistical significance, but the near universality of the direction of the difference suggests that oral contraceptives do produce a weak masculinizing effect on some auditory structures. These weak masculinizing effects appear to run contrary to the facts that the levels of both free testosterone and estradiol are lower in women using OC than in normal-cycling women. Past findings on auditory sex differences may have underestimated those sex differences. PMID:10748325

  18. Exogenous Hormone Use: Oral Contraceptives, Postmenopausal Hormone Therapy, and Health Outcomes in the Nurses’ Health Study

    PubMed Central

    Grodstein, Francine; Stampfer, Meir J.; Willett, Walter C.; Hu, Frank B.; Manson, JoAnn E.

    2016-01-01

    Objectives. To review the contribution of the Nurses’ Health Study (NHS) to our understanding of the complex relationship between exogenous hormones and health outcomes in women. Methods. We performed a narrative review of the publications of the NHS and NHS II from 1976 to 2016. Results. Oral contraceptive and postmenopausal hormone use were studied in relation to major health outcomes, including cardiovascular disease and cancer. Current or recent oral contraceptive use is associated with a higher risk of cardiovascular disease (mainly among smokers), melanoma, and breast cancer, and a lower risk of colorectal and ovarian cancer. Although hormone therapy is not indicated primarily for chronic disease prevention, findings from the NHS and a recent analysis of the Women’s Health Initiative indicate that younger women who are closer to menopause onset have a more favorable risk–benefit profile than do older women from use of hormone therapy for relief of vasomotor symptoms. Conclusions. With updated information on hormone use, lifestyle factors, and other variables, the NHS and NHS II continue to contribute to our understanding of the complex relationship between exogenous hormones and health outcomes in women. PMID:27459451

  19. Adiponectin and bone metabolism markers in female rowers: eumenorrheic and oral contraceptive users.

    PubMed

    Jürimäe, J; Vaiksaar, S; Mäestu, J; Purge, P; Jürimäe, T

    2011-12-01

    This study investigated whether adiponectin, bone formation (osteocalcin) and bone resorption [type I carboxyterminal telopeptide (ICTP)] values are influenced by menstrual cycle phase and oral contraceptive use in female rowers. Twenty-four rowers divided into normally cycling athletes (NOC; no.=15) and athletes taking oral contraceptive pills (OC; no.=9) participated in this study. Fasting blood samples, body composition and aerobic capacity measurements were taken during the follicular (FP) and the luteal (LP) phases of the menstrual cycle. Adiponectin, insulin, glucose, insulin resistance, body composition and aerobic capacity did not fluctuate significantly during menstrual cycle in both groups. Osteocalcin and ICTP were lower (p<0.05) in OC compared with NOC, but did not change significantly across menstrual cycle phases in both groups. Estradiol and progesterone were not related to adiponectin, osteocalcin or ICTP (r<0.147; p>0.05). Adiponectin was correlated (p<0.05) with osteocalcin (r=0.452) and fat free mass (r=0.428), and osteocalcin was related (p<0.05) to insulin (r=-0.413), glucose (r=-0.486) and insulin resistance (r=-0.528). In conclusion, adiponectin was not affected by menstrual cycle phase and OC use in female rowers, while bone metabolism markers were lower in OC compared to NOC groups. Adiponectin and osteocalcin were interrelated and may characterise energy homeostasis in female athletes. PMID:21169728

  20. The effects of short-term jump training on bone metabolism in females using oral contraceptives.

    PubMed

    Reiger, Jamie; Yingling, Vanessa R

    2016-01-01

    The purpose of this study was to determine the effect of oral contraceptive use on bone serum markers following a 3-week jumping protocol. Twenty-three females (18-25 years) were grouped as oral contraceptive users (OC+) or non-users (OC-). Following a 3-week observation period, participants completed a 3-week (15-day) jump protocol. Jump sessions consisting of ten 42 cm drop jumps with a 30 s rest interval between jumps were completed each day, 5 days per week. Peak vertical ground reaction force and loading rate were measured and the osteogenic index was calculated. Serum markers for bone formation, bone alkaline phosphatase (BAP) and bone resorption, C-terminal telopeptides of type I collagen (CTX) were measured at three time points (pre-, mid-, post-jump). BAP and CTX increased significantly (P = 0.0017, 0.0488) in both groups post-jump; however, bone metabolic markers were not different between the OC+ and OC- groups. Osteogenic index, ground reaction force and vertical jump height were similar between groups. Correlations between markers of bone metabolism and participants' age at menarche, weight, loading rate and years on OC were not significant. A 3-week jumping protocol was found to be effective in stimulating bone metabolism in both OC+ and OC- groups. PMID:26008875

  1. Paracetamol interaction with oral contraceptive steroids: increased plasma concentrations of ethinyloestradiol.

    PubMed Central

    Rogers, S M; Back, D J; Stevenson, P J; Grimmer, S F; Orme, M L

    1987-01-01

    The effect of a single dose of paracetamol (1 g) on plasma concentrations of the oral contraceptive steroids ethinyloestradiol (EE2) and levonorgestrel (LNG) has been studied in six healthy female volunteers. The area under the plasma concentration-time curve (AUC0-24) of EE2 was significantly increased following paracetamol administration by 22% (control 2221 +/- 291; following paracetamol, 2702 +/- 452 pg ml-1 h; mean +/- s.d.; P less than or equal to 0.05). The greatest effect was evident in the time period 0-3 h. There was a significant decrease in the AUC of EE2-sulphate after paracetamol (7736 +/- 3791 pg ml-1 h) compared with control (13161 +/- 4535 pg ml-1 h; P less than or equal to 0.05). Plasma concentrations of LNG were unaltered by concurrent paracetamol administration. We conclude that the administration of a single 1 g dose of paracetamol causes an increase in plasma concentrations of EE2 as a result of a reduction in the sulphation of the steroid. This interaction may be of clinical significance in women on oral contraceptive steroids who regularly take paracetamol. PMID:3111513

  2. Effects of the oral contraceptive pill cycle on physiological responses to hypoxic exercise

    NASA Technical Reports Server (NTRS)

    Sandoval, Darleen A.; Matt, Kathleen S.

    2003-01-01

    To test whether the oral contraceptive pill cycle affects endocrine and metabolic responses to hypoxic (fraction of inspired oxygen = 13%, P(IO2): 95 mmHg; H) versus normoxic (P(IO2):153 mmHg; N) exercise, we examined eight women (28 +/- 1.2 yr) during the third (PILL) and placebo (PLA) weeks of their monthly oral contraceptive pill cycle. Cardiopulmonary, metabolic, and neuroendocrine measurements were taken before, during, and after three 5-min consecutive workloads at 30%, 45%, and 60% of normoxic V(O2peak) in H and N trials. Heart rate response to exercise was greater in H versus N, but was not different between PILL and PLA. Lactate levels were significantly greater during exercise, and both lactate and glucose levels were significantly greater for 30 min after exercise in H versus N (p < 0.0001). When expressed relative to baseline, lactate levels were lower in PILL versus PLA, but glucose was greater in PILL versus PLA (p < 0.001). Cortisol levels were also significantly greater in PILL versus PLA (p < 0.001). Norepinephrine levels were significantly increased during exercise (p < 0.0001) and in H versus N (p < 0.0001). However, epinephrine levels were not different over time or with trial. Thus, the presence of circulating estradiol and progesterone during the PILL phase reduces glucose and lactate responses to hypoxic exercise.

  3. Influence of Body Weight, Ethnicity, Oral Contraceptives, and Pregnancy on the Pharmacokinetics of Azithromycin in Women of Childbearing Age

    PubMed Central

    Habibi, Mitra; Kilpatrick, Sarah J.; Tuomala, Ruth E.; Shier, Janice M.; Wollett, Lori; Fischer, Patricia A.; Khorana, Kinnari S.; Rodvold, Keith A.

    2012-01-01

    Women of childbearing age commonly receive azithromycin for the treatment of community-acquired infections, including during pregnancy. This study determined azithromycin pharmacokinetics in pregnant and nonpregnant women and identified covariates contributing to pharmacokinetic variability. Plasma samples were collected by using a sparse-sampling strategy from pregnant women at a gestational age of 12 to 40 weeks and from nonpregnant women of childbearing age receiving oral azithromycin for the treatment of an infection. Pharmacokinetic data from extensive sampling conducted on 12 healthy women were also included. Plasma samples were assayed for azithromycin by high-performance liquid chromatography. Population data were analyzed by nonlinear mixed-effects modeling. The population analysis included 53 pregnant and 25 nonpregnant women. A three-compartment model with first-order absorption and a lag time provided the best fit of the data. Lean body weight, pregnancy, ethnicity, and the coadministration of oral contraceptives were covariates identified as significantly influencing the oral clearance of azithromycin and, except for oral contraceptive use, intercompartmental clearance between the central and second peripheral compartments. No other covariate relationships were identified. Compared to nonpregnant women not receiving oral contraceptives, a 21% to 42% higher dose-adjusted azithromycin area under the plasma concentration-time curve (AUC) occurred in non-African American women who were pregnant or receiving oral contraceptives. Conversely, azithromycin AUCs were similar between pregnant African American women and nonpregnant women not receiving oral contraceptives. Although higher levels of maternal and fetal azithromycin exposure suggest that lower doses be administered to non-African American women during pregnancy, the consideration of azithromycin pharmacodynamics during pregnancy should guide any dose adjustments. PMID:22106226

  4. Comparison of Glucosamine Absorption After Administration of Oral Liquid, Chewable, and Tablet Formulations to Dogs.

    PubMed

    Maxwell, Lara K; Regier, Penny; Achanta, Satyanarayana

    2016-01-01

    Glucosamine (GS) is commonly administered as a nutritional supplement to support joint function. Although many supplements are available, the effect of formulation on oral absorption in dogs is unknown. The purpose of this study was to determine the relative bioavailability of GS for liquid, chewable, and tablet formulations containing GS sulfate or hydrochloride and chondroitin sulfate. In a randomized cross-over design, supplements were administered daily for 8 days with a 1 wk washout period between treatments. Liquid or Tablet A was administered to four dogs, whereas Liquid or Tablet B was administered to four additional dogs. When nutraceutical exposure was normalized to the administered dose of GS free base, similar relative bioavailabilities were determined for all three formulations. However, the dose-normalized maximum plasma GS concentration was higher for the liquid supplement (5.5 ± 0.5 μg/mL) than for the two tablets (3.1 ± 0.6 and 2.1 ± 0.6 μg/mL, P < 0.001). Similarly, the time at which maximal plasma GS concentrations occurred was shorter for the liquid formulation (0.7 ± 0.5 hr) than for the two tablets (4.2 ± 0.6 and 5.0 ± 0.6 hr, P < 0.001). These data show that the formulation of joint supplements affects the oral absorption of GS in dogs. PMID:26808433

  5. Effectiveness and acceptability of progestogens in combined oral contraceptives – a systematic review

    PubMed Central

    Kulier, Regina; Helmerhorst, Frans M; Maitra, Nandita; Gülmezoglu, A Metin

    2004-01-01

    Background The progestogen component of oral contraceptives (OCs) has undergone changes since it was recognized that their chemical structure can influence the spectrum of minor adverse and beneficial effects. Methods The objective of this review was to evaluate currently available low-dose OCs containing ethinylestradiol and different progestogens in terms of contraceptive effectiveness, cycle control, side effects and continuation rates. The Cochrane Controlled Trials Register, MEDLINE and EMBASE databases were searched. Randomized trials reporting clinical outcomes were considered for inclusion and were assessed for methodological quality and validity. Results Twenty–two trials were included in the review. Eighteen were sponsored by pharmaceutical companies and in only 5 there was an attempt for blinding. Most comparisons between different interventions included one to three trials, involving usually less than 500 women. Discontinuation was less with second-generation progestogens compared to first–generation (RR 0.79; 95% CI 0.69–0.91). Cycle control appeared to be better with second-compared to first-generation progestogens for both, mono-and triphasic preparations (RR 0.69; 95% CI 0.52–0.91) and (RR 0.61; 95% CI 0.43–0.85), respectively. Intermenstrual bleeding was less with third- compared to second-generation pills (RR 0.71; 95% CI 0.55–0.91). Contraceptive effectiveness of gestodene (GSD) was comparable to that of levonorgestrel (LNG), and had similar pattern of spotting, breakthrough bleeding and absence of withdrawal bleeding). Drospirenone (DRSP) was similar compared to desogestrel (DSG) regarding contraceptive effectiveness, cycle control and side effects. Conclusion The third- and second-generation progestogens are preferred over first generation in all indices of acceptability. Current evidence suggests that GSD is comparable to LNG in terms of contraceptive effectiveness and for most cycle control indices. GSD is also comparable to DSG

  6. [The choice of oral contraception in 1984: general indications and specific cases].

    PubMed

    Gaspard, U

    1984-04-01

    Oral contrceptives (OCs), usd by over 30% of reproductive aged women in Belgium, are by far the most widely used contraceptive in that country. The various types of OCs include monophasic, biphasic, and triphasic combinations of an estrogen and a progestin, sequentials containing estrogen only for 7-14 days followed by a progestin through the 21st day; macrodose or microdose progestin only formulations, 3-month injectable progestins, and the morning after pill. Side effects of OCs are mainly due to metabolic effects on coagulation factors, the renin-angiotensin system, glucose tolerance, or the lipid profile. Users of OCs face increased risks of cholelithiases, thrombophlebitis, thromboembolism, cerebrovascular accidents, myocardial infarcts (among smokers over 35 years of age), and hepatic adenomas. The most troubling secondary effect is the excess cardiovascular morbidity and mortality show by contraceptive users, not just those who are obese, hypertensive, or who have histories of vascular pathology, but also those over 40 years of age and smokers. Lenght of use of OCs does not increase vascular risks. Epidemiologic studies demonstrate that vascular risks are reduced in lower dose formulations. Absolute contraindications to OC use include serious cardiovascular problems, severe hepatic pathology, estrogen-dependent tumors, pregnancy and undiagnosed gynecologic problems, and significant hyperlipidemia. Relative contraindications include severe headaches, cholelithiase, previous cholestasis of pregnancy, severe renal disease, fibromyomas, benign breast disease, age over 40 years, smoking, surgery anticipated within 4 weeks, infectious mononucleosis, falciform anemia, and immediate postpartum and lactation. Epilepsy, diabetes, depression, and varicose veins are not strictly speaking contraindications but require additonal surveillance. Lower dose formulations should be prescribed if possible. OC users should be followed up every 6-12 months. Among other steroidal

  7. The effects of oral contraceptives on well-being and sexuality.

    PubMed

    Bancroft, J; Sartorius, N

    1990-01-01

    The extent to which the high discontinuation rate for oral contraceptives is due to adverse effects of mood, well-being and sexuality is explored, taking into account early studies on high dose combined and sequential pills, recent studies on low-dose combined and triphasics, experimental design factors, effects of OCs on free androgen levels, psychosocial factors and reasons for choosing or stopping pills, effects on depressive illness, premenstrual syndrome, sexuality, and possible mechanisms for direct effects of steroids on mood and sexuality. Study design is complicated by selection of early or late oral contraceptive users, types of controls, and unknown confounding factors such as reason for choice of pills, effect of a reliable contraceptive on the sexual relationship, prior history of depression and premenstrual tension. Furthermore virtually all topics reviewed here resulted in inconsistent or contradictory findings, making a case for individual variation and subgroups of women with different responses regarding the end point being examined. Examples include whether progestogen alter female sexual desire or male attraction; and whether rising or falling free testosterone levels affect sexual response. Factors affecting experimental design include culture, language, life-cycle, type of relationship, personal qualities affecting contraceptive choice, manner of eliciting reports of side effects, steroid dose, whether ovulation was blocked, initial or established pill-use, possibility of missed pills, and type of controls. Current pill users seem to discontinue for depression and low libido less frequently than did users of higher dose pills, and severity scores of adverse effects are lower. Premenstrual and other cyclic events may be altered in timing, and premenstrual symptoms are relieved in most women, but worsened in some who take pills. It is likely that women with depressive and premenstrual complaints tend to discontinue pills, leaving the remaining

  8. Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability.

    PubMed

    Desai, Samixa; Poddar, Aditi; Sawant, Krutika

    2016-01-01

    The present investigation was aimed towards developing a beta-cyclodextrin (β-CD) solid dispersion (SD) based orally disintegrating tablet (ODT) of eslicarbazepine acetate (ESL), for improving the dissolution and providing fast onset of anti-epileptic action. Optimum ratio of ESL and β-CD was determined by Job's plot. Thereafter, solid dispersions were prepared by solvent evaporation method and evaluated for yield, assay, Differential scanning calorimetry (DSC), Fourier transform infra red spectroscopy (FTIR), X-ray diffraction (XRD), and in vitro dissolution. Optimized SD was compressed into ODT by direct compression using super disintegrants and evaluated for wetting time, drug content, in vitro drug release and in vivo studies. The results of DSC, FTIR and XRD analysis supported the formation of inclusion complex. An improved dissolution with 99.95 ± 2.80% drug release in 60 min was observed in comparison to 24.85 ± 2.96% release from a plain drug suspension. Tablets with crosspovidone as a super disintegrant showed the least disintegration time of 24.66 ± 1.52 s and higher in vitro drug release against marketed tablets. In vivo studies indicated that the formulated tablets had 2 times higher bioavailability than marketed tablets. Thus, the developed β-CD-ESL SD-ODT could provide faster onset of action and higher bioavailability, which would be beneficial in case of epileptic seizures. PMID:26478377

  9. Oral contraceptives, reproductive history and risk of colorectal cancer in the European Prospective Investigation into Cancer and Nutrition

    PubMed Central

    Tsilidis, K K; Allen, N E; Key, T J; Bakken, K; Lund, E; Berrino, F; Fournier, A; Olsen, A; Tjønneland, A; Overvad, K; Boutron-Ruault, M-C; Clavel-Chapelon, F; Byrnes, G; Chajes, V; Rinaldi, S; Chang-Claude, J; Kaaks, R; Bergmann, M; Boeing, H; Koumantaki, Y; Stasinopoulou, G; Trichopoulou, A; Palli, D; Tagliabue, G; Panico, S; Tumino, R; Vineis, P; Bueno-de-Mesquita, H B; van Duijnhoven, F J B; van Gils, C H; Peeters, P H M; Rodríguez, L; González, C A; Sánchez, M-J; Chirlaque, M-D; Barricarte, A; Dorronsoro, M; Borgquist, S; Manjer, J; van Guelpen, B; Hallmans, G; Rodwell, S A; Khaw, K-T; Norat, T; Romaguera, D; Riboli, E

    2010-01-01

    Background: Oral contraceptive use and reproductive factors may initiate long-term changes to the hormonal milieu and thereby, possibly influence colorectal cancer risk. Methods: We examined the association of hormonal and reproductive factors with risk of colorectal cancer among 337 802 women in the European Prospective Investigation into Cancer and Nutrition, of whom 1878 developed colorectal cancer. Results: After stratification for center and age, and adjustment for body mass index, smoking, diabetes mellitus, physical activity and alcohol consumption, ever use of oral contraceptives was marginally inversely associated with colorectal cancer risk (hazard ratio (HR), 0.92; 95% confidence interval (CI), 0.83–1.02), although this association was stronger among post-menopausal women (HR, 0.84; 95% CI: 0.74–0.95). Duration of oral contraceptive use and reproductive factors, including age at menarche, age at menopause, type of menopause, ever having an abortion, parity, age at first full-term pregnancy and breastfeeding, were not associated with colorectal cancer risk. Conclusion: Our findings provide limited support for a potential inverse association between oral contraceptives and colorectal cancer risk. PMID:21045829

  10. Localization of fluconazole in oral cavity by preferential coating of buccoadhesive tablet for treatment of oral thrush

    PubMed Central

    Pathak, Kamla; Sharma, Vijay; Akhtar, Nida; Rastogi, Pragya

    2016-01-01

    Background: The present research work was aimed at localization of fluconazole in the oral cavity by preferential coating of buccoadhesive tablet for the treatment of oral thrush. Materials and Methods: In order to achieve the aim, buccoadhesive tablets were optimized using 32 full factorial design to study the influence of varying content of chitosan and carbopol 934P (input variables) on the responses. Results: Perturbation plots revealed high sensitivity of the input variables to ex vivo mucoadhesion force and percent cumulative drug release (CDR) whereas the ex vivo mucoadhesion time was less sensitive to the input variables. Based on the highest desirability factor of 0.693 the formulation F9 was identified as the optimized formulation and was preferentially coated with ethyl cellulose (3% w/v) on one tablet face to get F9C. In reference to F9, F9C showed superior mucoadhesive features (P < 0.05) but the % CDR was comparable (f2 = 50.80). The preferential coating (F9C, Jss = 0.812 μg/cm2/h) limited the permeation of fluconazole across goat buccal mucosa by almost half the value of F9 (Jss = 1.34 μg/cm2/h) that could serve as an advantage in establishing high local concentration of drug in the oral cavity, thereby facilitating faster attainment of minimum inhibitory concentration. Scanning electron microscopy and histological analysis established nonirritant potential. The developed formulation was stable and demonstrated antifungal activity against Candida albicans. Conclusion: Thus it can be concluded that preferentially coated buccoadhesive tablets of fluconazole might be considered as a precise approach to localize the drug delivery in oral cavity. PMID:27051630

  11. Formulation and evaluation of clozapine orally disintegrating tablets prepared by direct compression.

    PubMed

    Olmez, S S; Vural, I; Sahin, S; Ertugrul, A; Capan, Y

    2013-02-01

    In this study, clozapine orally disintegrating tablets (ODTs) were prepared by direct compression method. Disintegration time, resistance to crushing of tablets, porosity, friability, dissolution tests were performed and dissolution profiles of ODTs were investigated. Morphological and interaction studies were also performed. Friability values were found to be less than 1%. All tablet formulations disintegrated within 1 min and fulfilled the 3 min disintegration time required for ODTs given in the European Pharmacopoeia. More than 85% of the labeled amount of clozapine was dissolved in 15 min from the ODTs. No interaction or changes were found between active substance and excipients. As a result of the studies, ODT formulations developed in this study can be suggested as promising formulations, which assist development and manufacturing a generic product of clozapine. PMID:23469682

  12. PREPARATION AND CHARACTERIZATION OF ORALLY DISINTEGRATING LORATADINE TABLETS MANUFACTURED WITH CO-PROCESSED MIXTURES.

    PubMed

    Amelian, Aleksandra; Szekalska, Marta; Wilczewska, Agnieszka Zofia; Basa, Anna; Winnicka, Katarzyna

    2016-01-01

    The aim of this study was to develop orally disintegrated tablets (ODT) with loratadine using Parteck ODT and Ludiflash--new commercially available tableting excipients based on co-processed mannitol. ODT containing loratadine were prepared with 3% addition of various superdisintegrants (AcDiSol, Kollidon CL-F and Kollidon CL-SF) by direct compression method. Obtained tablets were characterized for friability, pore structure, and wetting and disintegration time measured by four independents methods. In order to identify possible interactions between loratadine and the excipients, differential scanning calorimetry was used. The results showed that all formulated ODT were characterized by appropriate mechanical properties (friability < 1%), the uniform content of the drug substance and pleasant mouth feeling. Disintegration time below 30 s was observed in formulations with crospovidones as disintegrant. PMID:27180438

  13. A combined oral contraceptive affects mucosal SHIV susceptibility factors in a pigtail macaque model

    PubMed Central

    Ostergaard, Sharon Dietz; Butler, Katherine; Ritter, Jana M.; Johnson, Ryan; Sanders, Jeanine; Powell, Nathaniel; Lathrop, George; Zaki, Sherif R.; McNicholl, Janet M.; Kersh, Ellen N.

    2015-01-01

    Background Injectable hormonal contraception may increase women’s risk of HIV acquisition, and can affect biological risk factors in animal models of HIV. We established, for the first time, a model to investigate whether combined oral contraceptives (COC) alter SHIV susceptibility in macaques. Methods Seven pigtail macaques were administered a monophasic levonorgestrel (LNG)/ethinyl estradiol (EE) COC at 33% or 66% of the human dose for 60 days. Menstrual cycling, vaginal epithelial thickness and other SHIV susceptibility factors were monitored for a mean of 18 weeks. Results Mean vaginal epithelial thicknesses was 290.8 μm at baseline and 186.2 μm during COC (p=0.0141, Mann Whitney test). Vaginal pH decreased from 8.5 during to 6.5 post- treatment (0.0176 two-tailed t-test). Measured microflora was unchanged. Conclusions COC caused thinning of the vaginal epithelium and vaginal pH changes, which may increase SHIV susceptibility. 0.033 mg LNG + 0.0066 mg EE appeared effective in suppressing ovulation. PMID:25536296

  14. Cancers in Australia in 2010 attributable to and prevented by the use of combined oral contraceptives

    PubMed Central

    Jordan, Susan J; Wilson, Louise F; Nagle, Christina M; Green, Adele C; Olsen, Catherine M; Bain, Christopher J; Pandeya, Nirmala; Whiteman, David C; Webb, Penelope M

    2015-01-01

    Objectives To estimate the proportion and number of cancers occurring in Australia in 2010 attributable to combined oral contraceptive pill (OCP) use. Methods We estimated the population attributable fraction (PAF) for cancers causally associated with combined OCP use (breast, cervix), and the proportion of endometrial and ovarian cancers prevented (prevented fraction [PF]). We used standard formulae incorporating prevalence of combined OCP use in the Australian population, relative risks of cancer associated with this exposure and cancer incidence. Results An estimated 105 breast and 52 cervical cancers (0.7% and 6.4% of each cancer, respectively) in Australia in 2010 were attributable to current use of combined OCP. Past combined OCP use was estimated to have prevented 1,032 endometrial and 308 ovarian cancers in 2010, reducing the number of cancers that would otherwise have occurred by 31% and 19%, respectively. Conclusions A small proportion of breast and cervical cancers is attributable to combined OCP use; OCP use is likely to have prevented larger numbers of endometrial and ovarian cancers. Implications Women seeking contraceptive advice should be told of potential adverse effects, but should also be told that – along with reproductive health benefits – combined OCP use can reduce long-term risks of ovarian and endometrial cancers. PMID:26437729

  15. No association between body size and frequency of sexual intercourse among oral contraceptive users

    PubMed Central

    Brunner Huber, Larissa R.; Stanley, Whitney A.; Broadhurst, Leah; Dmochowski, Jacek; Vick, Tara M.; Scholes, Delia

    2014-01-01

    Purpose This study aimed to describe frequency of sexual intercourse and whether body size was associated with weekly sexual intercourse among a diverse group of women using oral contraceptives. Methods This longitudinal, prospective cohort study recruited participants (n=185) from several clinics in Charlotte, NC. Body mass index (BMI) and waist-to-hip ratio (WHR) were used as measures of body size and sexual intercourse frequency was determined from self-reported information provided on daily diaries. Mean monthly frequencies of sexual intercourse were calculated and linear mixed models were used to assess if means remained constant over time. Generalized estimating equations were used to calculate odds ratios (ORs) and 95% confidence intervals (CIs). Results Mean monthly frequency of sexual intercourse was similar for women classified as normal/underweight or obese by BMI during each month of data collection, but was highest for women classified as overweight. After adjustment, obesity-sexual intercourse associations were attenuated (BMI ≥30 vs. <25.0: OR=0.78, 95% CI: 0.43, 1.42 and WHR ≥0.85 vs. <0.85: OR=1.11; 95% CI: 0.62, 2.01). Conclusions This study found no association between BMI or WHR and weekly sexual intercourse. However, more research is warranted given the importance of this possible relationship for future studies of fertility, contraceptive effectiveness, and sexual health. PMID:25034574

  16. [Medication of the month. A new combined oral contraceptive containing estradiol valerate and dienogest (Qlaira)].

    PubMed

    Gaspard, U; Pintiaux, A; Kridelka, F

    2010-12-01

    In combined oral contraception (OC), a drastic reduction of both ethinylestradiol and androgenic progestins mostly derived from 19 NOR testosterone, allowed to moderately reduce the adverse impact of classical combined pills on metabolism and circulation (both arterial and venous). However, the marked hepatic action of ethinylestradiol, even in small dosages, lessens the expected risk reduction. For the first time, an OC has been developed, which contains estradiol valerate (with reduced hepatic action because of lack of a 17alpha ethinyl group) with dienogest, a 19 NOR testosterone-derived nonandrogenic progestin, which powerfully inhibits endometrial proliferation. Thanks to a dynamic modulation of estrogen and progestin doses (26 active days + 2 placebo days), an adequate contraceptive effectiveness, a good cycle control and drug tolerance are achieved, similar to those obtained with a classical low-dose OC. Recent data indicate that this new combination reduces the usually observed metabolic impact. An adequate cycle control (with 20% amenorrhea) is achieved for the first time with estradiol valerate + progestin,, in opposition with prior catastrophic results with other formulations containing 17beta-estradiol. A second combination containing estradiol + nomegestrol acetate (monophasic, 24 active days + 4 placebo days) is under study and seems also to yield promising results. Of course, in-depth study of metabolic and vascular effects of these new combinations is mandatory - and ongoing. PMID:21287768

  17. A case-control study of the possible association between oral contraceptives and malignant melanoma.

    PubMed Central

    Adam, S. A.; Sheaves, J. K.; Wright, N. H.; Mosser, G.; Harris, R. W.; Vessey, M. P.

    1981-01-01

    In a case-control study, we investigated 169 women aged 15-49 years with malignant melanoma notified to the Oxford and South Western cancer registries during the years 1971-1976, together with 507 matched controls. Data about medical, reproductive, drug and smoking histories were obtained both by reviewing general practitioner (GP) records and from the women themselves by postal questionnaires. There was no significant evidence of any overall increase in the risk of melanoma in oral contraceptive (OC) users (data from GP records-ever use vs never use, relative risk (RR) 1.34, 95% confidence limits 0.92-1.96; corresponding data from postal questionnaires-RR 1.13, limits 0.73-1.75). However, although not significant, the risk estimated from data in the postal questionnaires was higher in women who had used OCs for 5 years or more (use greater than or equal to 5 years vs never use, RR 1.57, limits 0.83-3.03). Previously demonstrated risk factors for melanoma, such as fair skin, blond or red hair and Celtic origin were found to be commoner in the cases than in the controls. Data from the Oxford/Family Planning Association contraceptive study were also examined. Unexpectedly there was a strong suggestion of a negative association between OC use and melanoma risk, but the analysis was based on only 12 women with the disease. PMID:7259960

  18. Bone Mineral Density in Adolescent Females Using Injectable or Oral Contraceptives: A 24 Month Prospective Study

    PubMed Central

    Cromer, Barbara A.; Bonny, Andrea E.; Stager, Margaret; Lazebnik, Rina; Rome, Ellen; Ziegler, Julie; Camlin-Shingler, Kelly; Secic, Michelle

    2008-01-01

    Study Objective To determine whether bone mineral density (BMD) is lower in hormonal contraceptive users than that in an untreated, comparison group. Design Observational, prospective cohort; duration: 24 months. Setting Adolescent clinics in a midwestern, metropolitan setting. Patients 433 postmenarcheal girls, aged 12–18 years, on depot medroxyprogesterone acetate (DMPA) [n=58], oral contraceptives (OC) [n=187], or untreated (n=188). Intervention DMPA and OC containing 100 mcg levonorgestrel and 20 mcg ethinyl estradiol. Main Outcome Measure BMD measurements at spine and femoral neck were obtained with dual x-ray absorptiometry (DXA) at baseline and 6-month intervals. Results Over 24 months, mean percent change in spine BMD was: DMPA −1.5%, OC +4.2%, and untreated +6.3%. Mean percent change in femoral neck BMD was: DMPA −5.2%, OC +3.0%, untreated +3.8%. Statistical significance was found between the DMPA group and other two groups (p<.001). In the DMPA group, mean percent change in spine BMD over the first 12 months was −1.4%; the rate of change slowed to −0.1% over the second 12 months. No bone density loss reached the level of osteopenia. Conclusions Adolescent girls receiving DMPA had significant loss in BMD compared with bone gain in the OC and untreated group. However, its clinical significance is mitigated by slowed loss after the first year of DMPA use and general maintenance of bone density values within the normal range. PMID:18222431

  19. Effects of oral contraceptive pill use on vaginal flora and vaginal epithelium.

    PubMed

    Eschenbach, D A; Patton, D L; Meier, A; Thwin, S S; Aura, J; Stapleton, A; Hooton, T M

    2000-09-01

    The objective of this study was to examine the effect of oral contraceptive (OC) use on vaginal discharge, epithelium, and flora. Thirty women who planned to use OC for contraception were evaluated before and 2 months after the start of OC use. At both visits, genital symptoms and exposures were assessed by questionnaire; vaginal signs were assessed by speculum examination and colposcopy; vaginal microflora was evaluated by quantitative culture; and a vaginal biopsy was obtained for histopathologic evaluation. Variables were compared between the initial visit and after 2 months of OC use. It was found that OC use did not change the gross, colposcopic, or histologic appearance of the vaginal epithelium or characteristics of vaginal or cervical discharge. Vaginal flora essentially remained unchanged after 2 months of OC use, except that a small decrease occurred in the number of subjects with > or =10(5) colony forming units/mL of H(2)O(2) producing Lactobacillus from 16 at baseline to 9 (p = 0.04) and in the total number of subjects with Ureaplasma urealyticum from 17 at baseline to 10 of 29 (p = 0.04). The results indicate minimal effect of OC use on the vaginal epithelium and vaginal and cervical discharge, and a small effect on vaginal flora. PMID:11124356

  20. Development and optimization of buspirone oral osmotic pump tablet.

    PubMed

    Derakhshandeh, K; Berenji, M Ghasemnejad

    2014-01-01

    The aim of the current study was to design a porous osmotic pump-based drug delivery system for controlling the release of buspirone from the delivery system. The osmotic pump was successfully developed using symmetric membrane coating. The core of the tablets was prepared by direct compression technique and coated using dip-coating technique. Drug release from the osmotic system was studied using USP paddle type apparatus. The effect of various processing variables such as the amount of osmotic agent, the amount of swellable polymer, concentration of the core former, concentration of the plasticizer, membrane thickness, quantum of orifice on drug release from osmotic pump were evaluated. Different kinetic models (zero order, first order and Higuchi model) were applied to drug release data in order to establish the kinetics of drug release. It was found that the drug release was mostly affected by the amount of NaCl as osmotic agent, the swellable polymer; hydroxy propyl methyl cellulose (HPMC), the amount of PEG-400 and cellulose acetate in the coating solution and thickness of the semipermeable membrane. The optimized formulation released buspirone independent of pH and orifice quantum at the osmogen amount of 42%, hydrophilic polymer of 13% and pore size of 0.8 mm on the tablet surface. The drug release of osmotic formulation during 24 h showed zero order kinetics and could be suggested that this formulation as a once-daily regimen improves pharmacokinetic parameters of the drug and enhances patient compliance. PMID:25657794

  1. The Combined Influence of Oral Contraceptives and Human Papillomavirus Virus on Cutaneous Squamous Cell Carcinoma

    PubMed Central

    Efird, Jimmy T.; Toland, Amanda E.; Lea, C. Suzanne; Phillips, Christopher J.

    2011-01-01

    The vast majority of cutaneous squamous cell carcinoma (CSCC) will occur in those with fair complexion, tendency to burn, and high ultraviolet radiation (UVR) exposure. Organ transplant recipients also are an important population at great risk for CSCC. An association has been reported between oral contraceptive (OC) use, human papillomavirus virus (HPV) and cervical cancer, and there could be a similar association for CSCC. The cutaneous HPV β-E6 protein, a close cousin of the transformative E6 protein underlying anogenital cancers, has been shown to inhibit apoptosis in response to UVR damage and stimulate morphologic transformation in rodent fibroblast cell lines. Furthermore, OC use has been shown to enhance HPV transcription and may contribute to CSCC risk through this pathway. PMID:21499554

  2. The relationship between oral contraceptive use and sensitivity to olfactory stimuli.

    PubMed

    Renfro, Kaytlin J; Hoffmann, Heather

    2013-03-01

    The present study examined differences in olfactory sensitivity between 16 naturally cycling (NC) women and 17 women taking monophasic oral contraceptives (OCs) to six odors: lemon, peppermint, rose, musk, androstenone and androsterone. Thresholds were assessed twice for both groups of women (during the periovulatory and luteal phases of their cycles) via a forced-choice discrimination task. NC women in the periovulatory phase were significantly more sensitive to androstenone, androsterone, and musk than women taking OCs. These findings give support to odor-specific hormonal modulation of olfaction. Further, due to the social and possibly sexual nature of these odors, future work should address whether there is a relationship between decreased sensitivity to these odors and reported behavioral side effects among women taking OCs. PMID:23321429

  3. Influence of menstrual cycle, parity and oral contraceptive use on steroid hormone receptors in normal breast.

    PubMed Central

    Battersby, S.; Robertson, B. J.; Anderson, T. J.; King, R. J.; McPherson, K.

    1992-01-01

    Steroid receptor was assessed immunohistochemically in 158 samples of normal breast for variation through the menstrual cycle. Patterns and intensity of reaction were used in a semi-quantitative scoring system to examine the influence of cycle phase, cycle type, parity and age. The changes in oestrogen receptor for natural cycle and oral contraceptive (OC) cycles indicated down-regulation by progestins. Progesterone receptor did not vary significantly in natural cycles, but increased steadily through OC cycles. This study provides strong evidence that both oestrogen and progesterone influence breast epithelium, but dissimilarities from the endometrium are apparent. The interval since pregnancy had a significant negative effect on frequency and score of oestrogen receptor and score of progesterone receptor. Multivariate analysis established the phase of cycle and OC use as independent significant influences on oestrogen receptor. The interval since pregnancy was an independent significant factor for both oestrogen and progesterone receptor presence. Images Figure 1 Figure 2 PMID:1562470

  4. Combined oral contraceptive synergistically activates mineralocorticoid receptor through histone code modifications.

    PubMed

    Igunnu, Adedoyin; Seok, Young-Mi; Olatunji, Lawrence A; Kang, Seol-Hee; Kim, Inkyeom

    2015-12-15

    Clinical studies have shown that the use of combined oral contraceptive in pre-menopausal women is associated with fluid retention. However, the molecular mechanism is still elusive. We hypothesized that combined oral contraceptive (COC) ethinyl estradiol (EE) and norgestrel (N) synergistically activates mineralocorticoid receptor (MR) through histone code modifications. Twelve-week-old female Sprague-Dawley rats were treated with olive oil (control), a combination of 0.1µg EE and 1.0µg N (low COC) or 1.0µg EE and 10.0µg N (high COC) as well as 0.1 or 1.0µg EE and 1.0 or 10.0µg N daily for 6 weeks. Expression of MR target genes in kidney cortex was determined by quantitative real-time polymerase chain reaction. MR was quantified by western blot. Recruitment of MR and RNA polymerase II (Pol II) on promoters of target genes as well as histone code modifications was analyzed by chromatin immunoprecipitation assay. Treatment with COC increased renal cortical expression of MR target genes such as serum and glucocorticoid-regulated kinase 1 (Sgk-1), glucocorticoid-induced leucine zipper (Gilz), epithelial Na(+)channel (Enac) and Na(+)-K(+)-ATPase subunit α1 (Atp1a1). Although COC increased neither serum aldosterone nor MR expression in kidney cortex, it increased recruitment of MR and Pol II in parallel with increased H3Ac and H3K4me3 on the promoter regions of MR target genes. However, treatment with EE or N alone did not affect renal cortical expression of Sgk-1, Gilz, Enac or Atp1a1. These results indicate that COC synergistically activates MR through histone code modifications. PMID:26506558

  5. Sucralose as co-crystal co-former for hydrochlorothiazide: development of oral disintegrating tablets.

    PubMed

    Arafa, Mona F; El-Gizawy, Sanaa A; Osman, Mohamed A; El Maghraby, Gamal M

    2016-08-01

    Development of oral disintegrating tablets requires enhancement of drug dissolution and selection of sweetener. Co-crystallization of drugs with inert co-former is an emerging technique for enhancing dissolution rate. The benefit of this technique will become even greater if one of the sweeteners can act as co-crystal co-former to enhance dissolution and mask the taste. Accordingly, the objective of this work was to investigate the efficacy of sucralose as a potential co-crystal co-former for enhancing the dissolution rate of hydrochlorothiazide. This was extended to prepare oral disintegrating tablets. Co-crystallization was achieved after dissolving hydrochlorothiazide with increasing molar ratios of sucralose in the least amount of acetone. The co-crystallization products were characterized using Fourier transform infrared spectroscopy, differential thermal analysis and powder X-ray diffraction. These measurements indicated that co-crystallization process started at a drug sucralose molar ratio of 1:1 and completed at 1:2. The developed co-crystals exhibited faster drug dissolution compared with the control, with co-crystal containing the drug with sucralose at 1:2 molar ratio being optimum. The later was used to prepare fast disintegrating tablets. These tablets had acceptable physical characteristics and showed fast disintegration with subsequent rapid dissolution. The study introduced sucralose as co-crystal co-former for enhanced dissolution and masking the taste. PMID:26555927

  6. Hypertensive Crisis and Left Ventricular Thrombi after an Upper Respiratory Infection during the Long-term Use of Oral Contraceptives.

    PubMed

    Suzuki, Natsuko; Suzuki, Keisuke; Mizuno, Tomofumi; Kato, Yukari; Suga, Norihiro; Yoshino, Masabumi; Miura, Naoto; Banno, Shogo; Imai, Hirokazu

    2016-01-01

    A 34-year-old woman who had been using oral contraceptives for 10 years developed hypertensive crisis with papilloedema after an upper respiratory infection. Laboratory data showed hyperreninemic hyperaldosteronism and elevated levels of fibrinogen, fibrin, and fibrinogen degradation products. Echocardiography demonstrated two masses (18 mm) in the left ventricle. On the fourth hospital day, cerebral infarction, renal infarction, and upper mesenteric artery occlusion suddenly occurred despite the blood pressure being well-controlled using anti-hypertensive drugs. Echocardiography revealed the disappearance of the left ventricular masses, which suggested left ventricular thrombi. Cessation of the contraceptives and administration of heparin, warfarin, and anti-platelets drugs improved her general condition. PMID:26726092

  7. Cycle-Related Changes in Mood, Sexual Desire, and Sexual Activity in Oral Contraception-Using and Nonhormonal-Contraception-Using Couples.

    PubMed

    Elaut, Els; Buysse, Ann; De Sutter, Petra; Gerris, Jan; De Cuypere, Griet; T'Sjoen, Guy

    2016-01-01

    Findings on women's sexuality across the menstrual cycle are inconsistent. One relatively consistent finding is a midcycle and premenstrual peak in sexual desire in freely cycling women. Results on the cycle-related effects on sexual behavior are less clear. Large proportions of reproductive-aged women use combined oral contraception (COC), but studies on potential cycle-related shifts in sexual desire and behavior are sparse. A prospective diary study assessed sexual desire, sexual behavior, and mood in 89 heterosexual couples. Women were using one of four contraceptive methods: (1) nonhormonal contraception, (2) low-dose COC containing 20 mcg ethinylestradiol and 75 mcg gestoden or desogestrel, (3) COC containing 35 mcg ethinylestradiol and 2 mg cyproteronacetate, and (4) COC containing 30 mcg ethinylestradiol and 3 mg drospirenone. No cycle effects of sexual desire were established in the COC group, but frequency of sexual intercourse declined in the last days of active pill taking. These results were similar in both female and male partners. Negative affect did not covary with sexual desire. PMID:25420716

  8. In vitro and in vivo evaluation of oral tablet formulations prepared with ketoconazole and hydroxypropyl-beta-cyclodextrin.

    PubMed

    Taneri, Filiz; Ozcan, Ipek; Guneri, Tamer

    2010-04-01

    The objective of this study was to enhance the solubility, dissolution rate, and oral bioavailability of a very poorly water-soluble anti-fungal agent, ketoconazole (KET), by inclusion complexation with a highly-soluble cyclodextrin derivative, hydroxypropyl-beta cyclodextrin (HP-beta-CD). Two groups of tablets containing KET alone and KET:HP-beta-CD (1:2) kneaded product (KP) including magnesium stearate and lactopress (anhydrous and spray-dried) as excipients were prepared by direct compression method. After the characterization studies, the in vitro dissolution studies of these tablets in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were carried out. To evaluate the in vivo bioavailability, the tablets were administered orally to rabbits and drug levels in serum were determined by HPLC. Tablets containing the cyclodextrin complex showed a higher in vitro dissolution rate and bioavailability compared to the tablets containing KET alone. PMID:20148713

  9. Iron supplement tablet embedded in the oral cavity mimicking neoplasm: a case report

    PubMed Central

    2016-01-01

    The detection of foreign bodies in the upper-aerodigestive tract is a fairly frequent event and can occur in various areas and for various reasons. In rare cases, foreign bodies can simulate a neoplasia. We evaluated similar cases during emergency regimen with an oral cavity mucosal lesion, causing lockjaw, sore throat, dysphagia, and swelling of the submandibular and laterocervical region. Physical examination revealed an extensive mucosal ulceration in the floor of the mouth and the lateral surface of the tongue, comparable to oral cancer. During a second, more accurate assessment, a partially deteriorated iron supplement tablet was found embedded in a mucosal pocket. After removing the tablet, gradual normalization of the tissue was observed without any sequelae. This is one of the many reasons why it is advisable and useful in cases of oral lesions to collect a detailed medical history and to perform an accurate clinical evaluation, including inspection and palpation of the lesion, before proceeding to further diagnostic assessments, especially in elderly patients taking many medications. However unlikely, it is possible that difficulty in swallowing pills or tablets could generate tumorlike lesions. PMID:27162752

  10. New Generation of Orally Disintegrating Tablets for Sustained Drug Release: A Propitious Outlook.

    PubMed

    Elwerfalli, Arwa Matoug; Ghanchi, Zabir; Rashid, Fatema; Alany, Raid G; ElShaer, Amr

    2015-01-01

    Orally disintegrating tablets (ODTs) or orodispersible tablets are solid dosage forms that disintegrate within 3 minutes in the mouth into a paste that can be easily swallowed. ODTs have improved over the past years, in an attempt to produce a safe and efficient substitute to the conventional oral dosage forms, particularly for dysphagia patients. Since its introduction in the market in the 1980s, ODTs expanded rapidly and achieved revenues over $3 billion in 2006 and sustaining 20% annual growth. It is therefore evident that ODTs carry good commercial value, however there is potential for improvement. Current sustained-release technologies may be exploited and incorporated into an ODT to provide greater therapeutic value by reducing the need for multiple daily dosing regimens and improving patient adherence. A number of technologies such as polymer coated nanoparticles, stimuli-responsive polymers and ion-exchange resins have emerged to produce robust, sustained release orally disintegrating tablets (SR-ODT). The purpose of this review is to highlight these various approaches and techniques and how they have been utilised in an ODT formulation to extend differentiated line, market exclusivity and patent life. The review also explores future perspective and the potential challenges that SR-ODTs will face. PMID:25760951

  11. Modern trends in contraception.

    PubMed

    Burkman, R T

    1990-12-01

    Substantial improvements have been made in oral contraceptives, a new injectable contraceptive (Norplant), and the intrauterine device (IUD). Major risks with oral contraceptives have declined substantially, and a number of noncontraceptive health benefits have been discovered. Norplant is probably the first new contraceptive in recent years, and offers long-term contraception with high efficacy and modest risks. The IUD, by carefully selecting users, is a safe and efficacious contraceptive method. The major risk, pelvic inflammatory disease (PID), is far less common if one avoids use in the presence of risk factors for PID. PMID:2128711

  12. Relative bioavailability of diclofenac potassium from softgel capsule versus powder for oral solution and immediate-release tablet formulation.

    PubMed

    Bende, Girish; Biswal, Shibadas; Bhad, Prafulla; Chen, Yuming; Salunke, Atish; Winter, Serge; Wagner, Robert; Sunkara, Gangadhar

    2016-01-01

    The oral bioavailability of diclofenac potassium 50 mg administered as a soft gelatin capsule (softgel capsule), powder for oral solution (oral solution), and tablet was evaluated in a randomized, open-label, 3-period, 6-sequence crossover study in healthy adults. Plasma diclofenac concentrations were measured using a validated liquid chromatography-mass spectrometry/mass spectrometry method, and pharmacokinetic analysis was performed by noncompartmental methods. The median time to achieve peak plasma concentrations of diclofenac was 0.5, 0.25, and 0.75 hours with the softgel capsule, oral solution, and tablet formulations, respectively. The geometric mean ratio and associated 90%CI for AUCinf, and Cmax of the softgel capsule formulation relative to the oral solution formulation were 0.97 (0.95-1.00) and 0.85 (0.76-0.95), respectively. The geometric mean ratio and associated 90%CI for AUCinf and Cmax of the softgel capsule formulation relative to the tablet formulation were 1.04 (1.00-1.08) and 1.67 (1.43-1.96), respectively. In conclusion, the exposure (AUC) of diclofenac with the new diclofenac potassium softgel capsule formulation was comparable to that of the existing oral solution and tablet formulations. The peak plasma concentration of diclofenac from the new softgel capsule was 67% higher than the existing tablet formulation, whereas it was 15% lower in comparison with the oral solution formulation. PMID:27119581

  13. Lack of Pharmacokinetic Interactions Between Macitentan and a Combined Oral Contraceptive in Healthy Female Subjects.

    PubMed

    Hurst, Noémie; Pellek, Matthias; Dingemanse, Jasper; Sidharta, Patricia N

    2016-06-01

    Macitentan, a dual endothelin receptor antagonist used in pulmonary arterial hypertension, induces cytochrome P450 (CYP) 3A at supratherapeutic concentrations in vitro. Most combined oral hormonal contraceptives (OCs) are CYP3A substrates and their efficacy can be affected by CYP3A inducers. This randomized crossover study assessed possible pharmacokinetic (PK) interactions between macitentan and an OC containing ethinyl estradiol and norethindrone (or norethisterone). Twenty-six healthy women received a single oral dose of OC alone (reference) and concomitantly with 10 mg macitentan at steady state (test). No PK interaction was concluded if the 90% confidence intervals (CIs) of geometric mean ratios (GMRs; test/reference) of the peak plasma concentration (Cmax ) and the exposure from 0 to infinity (AUC0 - ∞ ) to the OC components were within the equivalence limits of 0.8 to 1.25. Cmax and AUC0-∞ of the OC were within the equivalence limits. For ethinyl estradiol, GMRs (90%CIs) of Cmax and AUC0-∞ were 0.92 (0.85-0.99) and 0.95 (0.90-0.99). For norethindrone, these values were 1.02 (0.95-1.09) and 1.04 (0.98-1.09), respectively. Overall, study treatments were well tolerated. No major changes from baseline in safety parameters were reported in either treatment. Macitentan does not affect the PK of OCs. PMID:26381054

  14. Pro/antioxidant status in young healthy women using oral contraceptives.

    PubMed

    Kowalska, Katarzyna; Milnerowicz, Halina

    2016-04-01

    The aim of the study was to analyze the effects of oral contraceptives (OCs) on pro/antioxidant status in the blood of healthy women aged 20-25 years. Individuals were divided into OCs users and OCs nonusers. Markers of oxidative stress in the blood such as Cu, Cu/Zn ratio, malondialdehyde (MDA), glutathione oxidized (GSSG), and gamma-glutamyl transpeptidase (GGT) were determined. Antioxidants such as glutathione reduced (GSH), catalase (CAT), glutathione reductase (GR), glutathione peroxidase (GPx), glutathione S-transferase (GST), and superoxide dismutase (SOD) were estimated. Higher Cu concentrations, Cu/Zn ratio and GGT activity in women taking OCs were noted. A significant increase in MDA concentrations in oral OCs users was observed. Heightened activity of CAT in plasma was observed in OCs users, whereas SOD activity remained unchanged in plasma and erythrocyte lysate. A decline of GSH and GSSG in whole blood and glutathiono-dependent enzymes (GPx in plasma, GR in plasma and GST in lysate) was shown. Use of OCs leads to a pro/antioxidant imbalance. The results in the present study confirmed that GGT is an early marker of oxidative stress. Catalase is the main antioxidant, involved in the removal of free radicals in OCs users. PMID:26921793

  15. Matched-pairs analysis of ovarian suppression during oral versus vaginal hormonal contraceptive use

    PubMed Central

    Petrie, Kelsey A.; Torgal, Anu H.; Westhoff, Carolyn L.

    2011-01-01

    Background This study was conducted to compare ovarian suppression during oral versus vaginal hormonal contraceptive use. Secondary aims included comparison of endometrial thickness and bleeding patterns. Methods In two open-label trials assessing ovarian suppression, 33 compliant women completed both studies. They first used OCs [randomized to either 20 mcg ethinyl estradiol (EE)/100 mcg levonorgestrel (LNG) or 30 mcg EE/150 mcg LNG] and subsequently used contraceptive vaginal rings (CVR) (daily release of 15 mcg EE/120 mcg etonogestrel), all 21/7 day regimens. Participants had at least one run-in cycle using each contraceptive method prior to evaluation. During one cycle of each method, women underwent bi-weekly transvaginal sonography to measure ovarian follicular diameters and endometrial thickness. We also noted presence of a corpus luteum or a ruptured follicle as a marker of ovulation. Participants recorded bleeding days on paper calendars. We used matched pairs analyses as appropriate. Results During follow-up, we identified at least one ovarian follicle ≥8 mm in 20/33 (61%) OC users and 12/33 (36%) CVR users (matched pairs analysis, p=0.02). Similar trends were seen for larger follicles; however we had limited statistical power to evaluate these differences. Median follicular diameter among OC users was larger than median follicular diameter among CVR users (p=0.01). We did not observe a corpus luteum or ruptured follicle in any participant during either study. Endometrial thickness was similar during OC and CVR use (mean 4.1 ± 1.4 mm versus 4.1 ± 1.6 mm, p=0.9) as was the number of bleeding or spotting days (mean 2.1 ± 2.4 versus 1.9 ± 2.1, p=0.8). OC dose was unrelated to follicle diameter, endometrial thickness, or bleeding. Conclusions Ovarian follicles ≥8 mm were more common in 33 compliant women during OC use than during CVR use indicating CVR use results in greater ovarian suppression than OC use. PMID:22018131

  16. Serum metabolomic profiles suggest influence of sex and oral contraceptive use

    PubMed Central

    Ruoppolo, Margherita; Campesi, Ilaria; Scolamiero, Emanuela; Pecce, Rita; Caterino, Marianna; Cherchi, Sara; Mercuro, Giuseppe; Tonolo, Giancarlo; Franconi, Flavia

    2014-01-01

    Aim: Considering that the effects of sex and oral contraceptives (OCs) on blood metabolites have been scarcely studied and the fact that protocol designs for clinical trials emphasise the use of contraception for women of childbearing potential, we examined if OCs and sex affect the serum levels of the physiologically relevant amino acids, carnitine and acylcarnitines, using metabolomics approaches. Methods: Healthy adult men and women were enrolled. They were drug free with the exception of women taking cyclic format OCs (ethinylestradiol + different progestins). OCs-free women were analysed during the follicular phase, and amino acids, free carnitine and acylcarnitines were measured using HPLC or LC-MS/MS, respectively. Results: Men had significantly higher leucine, isoleucine, methionine, asparagine, proline, valine, tyrosine, glutamine+glutamate, glutamate, histidine and citrulline than OCs-free women, while tryptophan was significantly lower in men. OCs use significantly decreased the levels of glycine, proline, histidine, lysine, hydroxyproline and ornithine and increased isoleucine levels when compared with non-user women. OCs use reduced, although not significantly, carnitine levels in women. Total esterified carnitines were higher in untreated women than in OCs users. Globally, the effect of OCs and sex was specific for the individual esterified carnitine. The observed metabolic changes were not attributable to renal or hepatic functions or to differences in body weight. Conclusions: The assessed parameters were specifically influenced by sex, highlighting the need to have reference values for women and men. The major novelty of this study is the demonstration that OCs specifically change the profiles of serum amino acids and carnitine, which suggests that OCs users and non-users should be represented in clinical trials. PMID:25360225

  17. Pre-gravid oral contraceptive use in relation to birth weight: a prospective cohort study.

    PubMed

    Hatch, Elizabeth E; Hahn, Kristen A; Mikkelsen, Ellen M; Riis, Anders H; Sorensen, Henrik Toft; Rothman, Kenneth J; Wise, Lauren A

    2015-11-01

    Few studies have evaluated the association between pregravid oral contraceptive (OC) use and birth weight, and findings have been conflicting. We conducted a prospective cohort study of 5921 pregnancy planners in Denmark to evaluate recency, duration, and type of OC used before conception in relation to infant birth weight. Participants completed online questionnaires and reported detailed information on contraceptive history and covariates at baseline. Participants completed bimonthly follow-up questionnaires to update their pregnancy status for up to 12 months or until conception occurred. Birth weight data were ascertained from the Danish Medical Birth Registry for 4046 live births delivered by study participants between 2008 and 2010. We used multivariable linear and log-binomial regression analyses to control for confounding. Mean birth weight was higher among women who had used OCs within 0-1 months (mean difference = 97 g, CI 26, 168) or 2-6 months (mean difference = 40 g, CI -5, 85) before conception, compared with more than 12 months before conception. Mean birth weight was lower among women who had used OCs for long durations (mean difference comparing ≥12 with <4 years of OC use = -85 g, CI -158, -11). Our findings indicate that pregravid OC use within 6 months of conception may be associated with a small increase in birth weight, but that long duration of use may have the opposite effect. Results were stronger among male infants, among 2nd and 4th generation OC users, and among users of OCs with a higher estrogen dose. PMID:26076921

  18. Oral Contraceptive Use, Muscle Sympathetic Nerve Activity, and Systemic Hemodynamics in Young Women.

    PubMed

    Harvey, Ronee E; Hart, Emma C; Charkoudian, Nisha; Curry, Timothy B; Carter, Jason R; Fu, Qi; Minson, Christopher T; Joyner, Michael J; Barnes, Jill N

    2015-09-01

    Endogenous female sex hormones influence muscle sympathetic nerve activity (MSNA), a regulator of arterial blood pressure and important factor in hypertension development. Although ≈80% of American women report using hormonal contraceptives sometime during their life, the influence of combined oral contraceptives (OCs) on MSNA and systemic hemodynamics remains equivocal. The goal of this study was to determine whether women taking OCs have altered MSNA and hemodynamics (cardiac output and total peripheral resistance) at rest during the placebo phase of OC use compared with women with natural menstrual cycles during the early follicular phase. We retrospectively analyzed data from studies in which healthy, premenopausal women (aged 18-35 years) participated. We collected MSNA values at rest and hemodynamic measurements in women taking OCs (n=53; 25±4 years) and women with natural menstrual cycles (n=74; 25±4 years). Blood pressure was higher in women taking OCs versus those with natural menstrual cycles (mean arterial pressure, 89±1 versus 85±1 mm Hg, respectively; P=0.01), although MSNA was similar in both groups (MSNA burst incidence, 16±1 versus 18±1 bursts/100 heartbeats, respectively; P=0.19). In a subset of women in which detailed hemodynamic data were available, those taking OCs (n=33) had similar cardiac output (4.9±0.2 versus 4.7±0.2 L/min, respectively; P=0.47) and total peripheral resistance (19.2±0.8 versus 20.0±0.9 U, respectively; P=0.51) as women with natural menstrual cycles (n=22). In conclusion, women taking OCs have higher resting blood pressure and similar MSNA and hemodynamics during the placebo phase of OC use when compared with naturally menstruating women in the early follicular phase. PMID:26101348

  19. Oral contraceptive use, muscle sympathetic nerve activity, and systemic hemodynamics in young women

    PubMed Central

    Harvey, Ronee E.; Hart, Emma C.; Charkoudian, Nisha; Curry, Timothy B.; Carter, Jason R.; Fu, Qi; Minson, Christopher T.; Joyner, Michael J.; Barnes, Jill N.

    2015-01-01

    Endogenous female sex hormones influence muscle sympathetic nerve activity (MSNA), a regulator of arterial blood pressure and important factor in hypertension development. While nearly 80% of American women report using hormonal contraceptives sometime during their life, the influence of combined oral contraceptives (OCs) on MSNA and systemic hemodynamics remains equivocal. The goal of this study was to determine if women taking OCs have altered MSNA and hemodynamics (cardiac output and total peripheral resistance) at rest during the placebo phase of OC use compared to women with natural menstrual cycles during the early follicular phase. We retrospectively analyzed data from studies in which healthy, premenopausal women (ages 18–35 years old) participated. We collected MSNA values at rest and hemodynamic measurements in women taking OCs (n=53, 25±4 yr) and women with natural menstrual cycles (n=74, 25±4 yr). Blood pressure was higher in women taking OCs versus those with natural menstrual cycles (mean arterial pressure: 89±1 vs. 85±1 mmHg, respectively; p=0.01), although MSNA was similar in both groups (MSNA burst incidence: 16±1 vs. 18±1 bursts/100 heartbeats, respectively, p=0.19). In a subset of women in which detailed hemodynamic data were available, those taking OCs (n=33) had similar cardiac output (4.9±0.2 vs. 4.7±0.2 L/min, respectively; p=0.47) and total peripheral resistance (19.2±0.8 vs. 20.0±0.9 units, respectively; p=0.51) as women with natural menstrual cycles (n=22). In conclusion, women taking OCs have higher resting blood pressure and similar MSNA and hemodynamics during the placebo phase of OC use compared to naturally menstruating women in the early follicular phase. PMID:26101348

  20. Determination of the in vitro disintegration profile of rapidly disintegrating tablets and correlation with oral disintegration.

    PubMed

    Abdelbary, G; Eouani, C; Prinderre, P; Joachim, J; Reynier, Jp; Piccerelle, Ph

    2005-03-23

    The assessment of the in vitro disintegration profile of rapidly disintegrating tablets (RDT) is very important in the evaluation and the development of new formulations of this type. So far neither the US Pharmacopoeia nor the European Pharmacopoeia has defined a specific disintegration test for RDT; currently, it is only possible to refer to the tests on dispersible or effervescent tablets for the evaluation of RDT's disintegration capacity. In the present study, we have evaluated the disintegration profile of RDT manufactured by main commercialised technologies, using the texture analyser (TA). In order to simulate as much as possible the oral disintegration of these dosage forms, a new operating structure was developed. This structure mimics the situation in the patient's mouth and provides a gradual elimination of the detached particles during the disintegration process. The obtained time-distance profiles or disintegration profiles enabled the calculation of certain quantitative values as the disintegration onset (t1) and the total disintegration time (t2). These values were used in the characterisation of the effect of test variables as the disintegration medium and temperature on the disintegration time of RDT. Moreover, the oral disintegration time of the same products was evaluated by 14 healthy volunteers. Results obtained when artificial saliva at 37 degrees C was employed as disintegration medium were used to correlate the in vitro (t2) and oral disintegration times. Excellent correlation was found and in addition, we were able to achieve a qualitative measure of the mouthfeel by comparing the thickness of the tablets and the penetration distance obtained from the disintegration profile. This method also permitted the discrimination between different RDT, where differences in the disintegration mechanism were reflected on the disintegration profile achieved for each tablet. PMID:15725551

  1. Emergency contraception.

    PubMed

    Grimes, David A; Raymond, Elizabeth G

    2002-08-01

    Emergency contraception is used to prevent pregnancy after a coital act not adequately protected by a regular method of contraception. In contrast to early medical abortion, emergency contraception prevents a pregnancy from starting and does not disrupt an established pregnancy. The most commonly used approaches consist of two oral doses of contraceptive steroids. The levonorgestrel-only regimen (levonorgestrel, 0.75 mg, repeated in 12 hours) appears to be more effective and better tolerated than the Yuzpe regimen (ethinyl estradiol, 100 microg, and levonorgestrel, 0.5 mg, repeated in 12 hours). In the largest randomized, controlled trial to date, levonorgestrel prevented about 85% of pregnancies that would have occurred without its use. Hormonal emergency contraception has no known medical contraindications, although it is not indicated for suspected or confirmed pregnancy. However, if hormonal emergency contraception is inadvertently taken in early pregnancy, neither the woman nor the fetus will be harmed. Nausea and vomiting associated with the Yuzpe regimen can be reduced by prophylactic use of meclizine. A strong medical and legal case exists for making hormonal emergency contraception available over the counter, as has happened in countries other than the United States. Easier access to and wider use of emergency contraception could dramatically lower the high rates of unintended pregnancy and induced abortion in the United States. PMID:12160366

  2. Effects of oral contraceptives, or lanosterol, on ADP-induced aggregation and binding of /sup 125/I-fibrinogen to rat platelets

    SciTech Connect

    McGregor, L.; Toor, B.; McGregor, J.L.; Renaud, S.; Clemetson, K.J.

    1984-03-01

    The aggregation to ADP and the binding of /sup 125/I-fibrinogen to platelets from rats treated with oral contraceptives or normal platelets treated in vitro with lanosterol were compared to their respective controls. Both types of platelets showed a significant increase in ADP-induced aggregation and in binding of fibrinogen, indicating that the effect of oral contraceptives could be partly due to increased levels of lanosterol in platelet membrane.

  3. Effect of oral contraceptives and hormone replacement therapy on bone mineral density in premenopausal and perimenopausal women: a systematic review

    PubMed Central

    Liu, S L; Lebrun, C M

    2006-01-01

    Seventy five articles on the effect of oral contraceptives and other hormone replacement on bone density in premenopausal and perimenopausal women were reviewed. The evidence was appraised using the Oxford Centre for Evidence‐Based Medicine levels of evidence. There is good evidence for a positive effect of oral contraceptives on bone density in perimenopausal women, and fair evidence for a positive effect in “hypothalamic” oligo/amenorrhoeic premenopausal women. There is limited evidence for a positive effect in healthy and anorexic premenopausal women. In hypothalamic oligo/amenorrhoeic women, baseline bone density has been shown to be significantly lower than that in healthy controls, therefore the decision to treat is clinically more important. The ideal formulation(s) and duration of treatment remain to be determined by further longitudinal and prospective randomised controlled trials in larger subject populations. PMID:16371485

  4. [Technical scheme of real-time evaluation of traditional Chinese medicine orally disintegrating tablets].

    PubMed

    Qin, Dong; Chen, Xu-dong; Feng, Liang; Gu, Jun-fei; Yuan, Jia-rui; Jia, Xiao-bin

    2014-12-01

    Orally disintegrating tablets (ODT), a kind of new solid tablet that rapidly disintegrates to work in the mouth, has became the hot form of new drug research in recent years with many advantages, such as the convenient taking, a widely applicable people, fast acting, high bioavailability, good compliance, and so on. ODT has been widely used in chemical medicines, while the application of it in traditional Chinese medicines (TCMs) is still in the stage of development The development of TCMs ODT provides a new direction for the research of Chinese medicine new dosage, accelerates the pace of connecting to the world and modernization of Chinese medicine. This dosage has a broad market prospect, and its quality control and assessment standards, taste, the disintegration time in vitro and evaluation method are the key factors that affect the industrialization, standardization of Chinese medicine ODT. Therefore, this paper reviewed the characteristics, preparation, taste masking technology and quality evaluation with new technology of ODT. Meantime, numerous application examples of ODT used in traditional Chinese medicine were described. We expect to provide the reference and utilization for the development of traditional Chinese medicine orally disinteeratine tablets. PMID:25898566

  5. A new modified wetting test and an alternative disintegration test for orally disintegrating tablets.

    PubMed

    Hooper, Patrick; Lasher, Jason; Alexander, Kenneth S; Baki, Gabriella

    2016-02-20

    Industrial manufacturing of solid oral dosage forms require quality tests, such as friability, hardness, and disintegration. The United States Pharmacopeia (USP) disintegration test uses 900mL of water. However, recent studies of orally disintegrating tablets (ODTs) have shown that this volume does not accurately portray the oral environment. In our study, various tests were conducted with a more moderate amount of water that accurately resembles the oral environment. A simulated wetting test was performed to calculate the water absorption ratio. Results showed that wetting was comparable to disintegration. Although the wetting test worked for most types of ODTs, it had limitations that produced inaccurate results. This led to the use of a modified shaking water bath test. This test was found to work for all types of ODT products and was not subject to the limitations of the wetting test. The shake test could provide disintegration times rather than water permeation times; however, it could not be used to calculate the water absorption ratio. A strong correlation was observed between the standardized shake test and the USP disintegration times for the tablets. This shake test could be used during the development stages and quality tests for ODTs with relative ease. PMID:26774944

  6. [Benefit of the Internet as an information tool in case of oral contraceptive miss. Survey of 1964 women visiting the website www.g-oubliemapilule.com].

    PubMed

    Lemaître, Sophie; Collier, Francis; Hulin, Vincent

    2009-12-20

    The aim of the study is to evaluate the utility of the website http://www.g-oubliemapilule.com/ that contains the recommendations of the French Haute Autorité de santé in case of oral contraceptive pill missing. This epidemiologic prospective study was conducted using an online questionnaire available at http://www.g-oubliemapilule.com/. The results emphasize the poor quality of information provided by the physicians. 40% of the physicians don't provide information about what to do in case of oral contraceptive pill missing during the first medical visit for oral contraceptive prescription and the physicians don't inquire about oral contraceptive pill missing during the follow-up in 3/4 of the cases. Furthermore, when women find information about what to do in case of oral contraceptive pill missing, a majority of them won't follow the advice provided even if it is fully understood. 60% of the women who should use the condom during the 7 days following the oral contraceptive pill missing don't use it and 86% of the women who should use the emergency contraceptive pill don't use it. The reason mostly invoked (1/3 of the cases) to support that behaviour is the assumption that the risk of pregnancy is too low. The results help to understand the gap between theoretical efficacy (Pearl Index: 0.3%) and real efficacy (8%) of the oral contraceptive pill. Finally, the website http://www.g-oubliemapilule.com/ is a useful well understood additional tool but can't replace the medical follow-up. PMID:20085215

  7. Bioequivalence of ondansetron oral soluble film 8 mg (ZUPLENZ) and ondansetron orally disintegrating tablets 8 mg (ZOFRAN) in healthy adults.

    PubMed

    Dadey, Eric

    2015-01-01

    Oral formulations of ondansetron are used to prevent nausea and vomiting associated with chemotherapy, radiotherapy, and surgery. An oral soluble film formulation of ondansetron (OND OSF) was developed using MonoSol Rx's proprietary PharmFilm technology and was formulated to dissolve rapidly on the tongue, without the need for water. This product provides an oral antiemetic treatment option for patients who experience difficulty swallowing. The purpose of this study was to compare the bioequivalence of OND OSF 8 mg (ZUPLENZ, Monosol Rx, Warren, NJ) with ondansetron orally disintegrating tablets (OND ODT) 8 mg (ZOFRAN, GlaxoSmithKline, Research Triangle Park). In 3 individual open-label, randomized studies, healthy adult subjects received a single dose of OND OSF 8 mg and a single dose of OND ODT 8 mg, under fasted conditions (study 1, n = 48), fed conditions (study 2, n = 48), and fasted with and without water (study 3, n = 18). Each dosing period was followed by a 3- or 7-day washout period. Ondansetron pharmacokinetics were assessed predose to 24 hours postdose for the single 8-mg doses of OND OSF and OND ODT. All analyses were conducted on natural log-transformed pharmacokinetic parameters for OND OSF and OND ODT. Under both fasted and fed conditions, the 90% confidence interval for the comparisons of OND OSF and OND ODT plasma ondansetron area under the curve from time 0 to the last measured concentration (AUC0-t), area under the concentration vs. time curve from time 0 to infinity (AUC0-∞), and maximum plasma concentration (Cmax) were within the 80%-125% range, indicating bioequivalence between the formulations. With features designed to make it portable and easy to take, OND OSF 8 mg provides an alternative treatment option, particularly for patients with dysphagia and others who find it difficult to take oral tablets. PMID:25581856

  8. Design, development, and optimization of orally disintegrating tablets of etoricoxib using vacuum-drying approach.

    PubMed

    Patel, Dharmesh; Shah, Mohit; Shah, Sunny; Shah, Tejal; Amin, Avani

    2008-01-01

    Etoricoxib is a cyclooxygenase 2 (COX-2) inhibitor that selectively inhibits the COX-2 enzyme and decreases the incidences of side effects associated with these agents. It is commonly prescribed for acute pain, gouty arthritis, and rheumatoid arthritis. Conventional tablets of etoricoxib are not capable of rapid action, which is required for faster drug effect onset and immediate relief from pain. Thus, the aim of the present investigation is to formulate orally disintegrating tablets (ODTs) of etoricoxib. A combination of the superdisintegrants with a sublimation technique was used to prepare the tablets. Tablets were prepared using a direct compression method employing superdisintegrants such as low substituted hydroxylpropyl methyl cellulose (L-HPMC), low substituted hydroxyl-propyl cellulose (L-HPC), crospovidone, croscarmellose sodium, and sodium starch glycolate. Tablets of etoricoxib prepared using L-HPC exhibited the least friability and disintegration time (approximately 65 s). To decrease the disintegration time further, a sublimation technique was used along with the superdisintegrants for the preparation of ODTs. The use of sublimating agents including camphor, menthol, and thymol was explored. The addition of camphor lowered the disintegration time (approximately 30 s) further, but the percent friability was increased. A 3(2) full factorial design was employed to study the joint influence of the amount of superdisintegrant (L-HPC) and the amount of sublimating agent (camphor) on the percent of friability and the disintegration time. The results of multiple linear regression analysis revealed that for obtaining an effective ODT of etoricoxib, higher percentages of L-HPC and camphor should be used. Checkpoint batches were prepared to validate the evolved mathematical model. A response surface plot is also presented to graphically represent the effect of the independent variables on the percent of friability and the disintegration time. The approach using

  9. Formulation design for orally disintegrating tablets containing enteric-coated particles.

    PubMed

    Okuda, Yutaka; Okamoto, Yasunobu; Irisawa, Yosuke; Okimoto, Kazuto; Osawa, Takashi; Yamashita, Shinji

    2014-01-01

    The purpose of this study was to investigate the applicability of our newly developed technology (RACTAB® technology) for preparing orally disintegrating tablets (ODTs) containing enteric-coated particles. Tamsulosin hydrochloride (TAM) was used as a model drug contained in the enteric-coated particles. Enteric-coated particles containing TAM (ECP-T) were prepared by spray coating a mixture of TAM with controlled-release materials. ECP-T was then mixed with rapidly disintegrating granules (RDGs), which were prepared using the suspension spray-coating method, and was tableted to form ODTs (ODTRAC). ODTRAC was evaluated for its hardness, thickness, internal structure (X-ray-CT scanning), functional properties (controlled-release profile), and in vivo disintegration time. Since RDGs with micronized ethylcellulose (MEC) increased tablet hardness by increasing the contact frequency between granules, ODTRAC containing ECP-T exhibited high hardness (>50 N) and low friability (<0.5%) with a relatively low compression force. After tableting, the structure of ECP-T in ODTRAC remained intact and no damage was observed on the surface. ECP-T recovered from ODTRAC showed the same dissolution profile of TAM in Japanese Pharmacopoeia (JP) 1st and JP 2nd media as that of intact ECP-T, which indicated that the tableting process did not affect the acid-resistibility of the particle. In addition, ODTRAC rapidly disintegrated in vivo (< 30 s), even at a high compression force (at 9 kN). These findings clearly suggest that RACTAB® technology is a useful approach to prepare ODTs containing enteric-coated particles. PMID:24789923

  10. Effects of Orally Administered Lactoferrin and Lactoperoxidase-Containing Tablets on Clinical and Bacteriological Profiles in Chronic Periodontitis Patients

    PubMed Central

    Shimizu, Eiju; Kobayashi, Tetsuo; Wakabayashi, Hiroyuki; Yamauchi, Koji; Iwatsuki, Keiji; Yoshie, Hiromasa

    2011-01-01

    This study was undertaken to evaluate the effect of oral administration of lactoferrin (LF) and lactoperoxidase-(LPO-)containing tablet on periodontal condition. Seventy-two individuals with chronic periodontitis were randomly assigned to take either bovine LF and LPO-containing tablets (test group, n = 37) or control tablets (control group, n = 35) every day for 12 weeks. Periodontal parameters and levels of subgingival plaque bacteria, human and bovine LF, and endotoxin in gingival crevicular fluid (GCF) were evaluated at baseline, 1 week, 4 weeks, and 12 weeks. Significant differences were observed in GCF levels of bovine LF between the test and control groups throughout the study (P < .05). However, clinical and bacteriological parameter values proved comparable between the two groups at 1 week to 12 weeks. Therefore, the effect of oral administration of LF and LPO-containing tablets might be weak on periodontal and bacteriological profile in this study. PMID:21747858

  11. Prevalence Rates of Uterine Cervical Carcinoma in situ for Women Using the Diaphragm or Contraceptive Oral Steroids*

    PubMed Central

    Melamed, Myron R.; Koss, Leopold G.; Flehinger, Betty J.; Kelisky, Richard P.; Dubrow, Hilliard

    1969-01-01

    Study of the prevalence rates of uterine cervical carcinoma in situ among women attending centres of Planned Parenthood of New York City, Inc., showed a small but statistically significant difference between the population choosing and using the diaphragm and the population choosing and using oral steroids for contraception. This can be attributed either to a decreased prevalence rate for women using the diaphragm or to an increased rate for women using oral steroids. The reason for the difference is not apparent from these data. PMID:5792609

  12. Influence of oral contraceptives on endogenous pain control in healthy women.

    PubMed

    Rezaii, Taraneh; Ernberg, Malin

    2010-06-01

    This study investigated the influence of oral contraceptives (OC) on diffuse noxious inhibitory control (DNIC) in healthy women. Fifteen women taking OC and 17 normally menstruating women (No-OC) were tested during high and low endogenous estrogens sessions. Saliva was sampled for analysis of endogenous estradiol level. Mechanical pressure (test stimuli) was applied to the masseter muscle and finger. The pain induced by this pressure was assessed on a 0-10 numerical rating scale (NRS) before, during, and after immersion of the contralateral hand in ice-cold water (cold pressor test, CPT) to induce DNIC. For all subjects, pain induced by the test stimuli decreased significantly during the CPT (P < 0.001). The decrease in general was larger in the No-OC group, with a significant difference between groups in the masseter muscle in the low session (P < 0.027). There were no significant differences between groups or sessions in estradiol levels. These results indicate that endogenous pain modulation may be less effective in OC users. PMID:20419369

  13. Oral contraceptive pill use is associated with localized decreases in cortical thickness

    PubMed Central

    Petersen, Nicole; Touroutoglou, Alexandra; Andreano, Joseph M.; Cahill, Larry

    2015-01-01

    Oral contraceptive pills (OCs), which are used to prevent pregnancy by the majority of women in the United States, contain steroid hormones that may affect the brain’s structure and function. In this investigation, we tested the hypothesis that OC use is associated with differences in brain structure using a hypothesis-driven, surface-based approach. In 90 women, (44 OC users, 46 naturally-cycling women), we compared the cortical thickness of brain regions that participate in the salience network and the default mode network, as well as the volume of subcortical regions in these networks. We found that OC use was associated with significantly lower cortical thickness measurements in the lateral orbitofrontal cortex and the posterior cingulate cortex. These regions are believed to be important for responding to rewards and evaluating internal states/incoming stimuli, respectively. Further investigations are needed to determine if cortical thinning in these regions are associated with behavioral changes, and also to identify whether OC use is causally or only indirectly related to these changes in brain morphology. PMID:25832993

  14. Elevated eating disorder symptoms in women with a history of oral contraceptive side effects.

    PubMed

    Bird, Jessica L; Oinonen, Kirsten A

    2011-08-01

    Previous research suggests a link between gonadal hormones and eating disorder symptomatology. This study examined the role of gonadal hormones and hormonal sensitivity in eating disorder (ED) symptoms by using oral contraceptive (OC) side effect history as an indicator of hormonal sensitivity. A questionnaire containing two scales of the Eating Disorder Inventory-2 and an OC side effect scale was completed by 174 healthy women who had used OCs. Histories of emotional and physical OC side effects were evaluated as predictors of body dissatisfaction and drive for thinness. Women with a history of negative OC side effects had higher levels of ED symptoms. After controlling for body mass index (BMI) and depression scores, OC side effect history remained a significant predictor of body dissatisfaction and drive for thinness. The experience of OC side effects may indicate a greater risk for increased eating disorder symptoms. The findings provide further support for a hormonal link to ED symptoms, as women who are more "sensitive" to exogenous gonadal hormones also experience more ED symptoms. PMID:21725835

  15. Oral contraceptive use by teenage women does not affect peak bone mass: a longitudinal study.

    PubMed

    Lloyd, T; Taylor, D S; Lin, H M; Matthews, A E; Eggli, D F; Legro, R S

    2000-10-01

    This longitudinal observational study determined the effect of oral contraceptive (OC) use during adolescence on peak bone mass (PBM). The sample comprised 62 non-Hispanic, White females in The Penn State Young Women's Health Study, who were studied for 8 years between the ages of 12 and 20. There were 28 OC users who used OCs for a minimum of 6 months and were still using them at age 20, and 34 nonusers who had never used the regimen. Total body bone, dedicated hipbone, and body composition measurements were made by dual-energy roentgenogram absorptiometry. There was no difference between OC users and nonusers in the anthropometric, body composition, or total body bone measurements. By age 20, the average duration of OC use by the user group was 22 months. At this age, the groups remained indistinguishable in anthropometric, body composition, total body, and hipbone measurements, and in age of menarche and sports exercise scores. These findings suggest that OC use by healthy, White, teenage females does not affect acquisition of PBM. PMID:11020515

  16. A comparative study of two low-dose combined oral contraceptives: results from a multicenter trial.

    PubMed

    Dunson, T R; McLaurin, V L; Israngkura, B; Leelapattana, B; Mukherjee, R; Perez-Palacios, G; Saleh, A A

    1993-08-01

    A comparative multicenter clinical trial of two low-dose combined oral contraceptives (OCs) was conducted in Malaysia, Egypt, Thailand, and Mexico. Efficacy, safety and acceptability were investigated in women taking either a norgestrel-based (NG) OC or a norethindrone acetate-based (NA) OC. This paper includes analysis of 892 women, all of whom were at least 42 days but within 26 weeks postpartum and randomly allocated to one of the above OCs. Follow-up visits were scheduled at 1, 4, 8 and 12 months after admission. Baseline sociodemographic characteristics were similar for both groups, as well as compliance. There were nine unintended pregnancies reported; eight of these occurring in the NA group. Adverse experiences were minor with headaches and dizziness being the most common complaints; frequency of reports was similar in both groups. The group taking the NG-based OC had significantly (p < .05) fewer menstrual-related complaints. Discontinuations due to menstrual problems were significantly more common among NA users (primarily amenorrhea). Discontinuations in the NG group were primarily for other personal reasons, e.g. unable to return to the clinic. There was also a significant difference between the two groups for the 11-month gross cumulative life table discontinuation rates due to menstrual problems (p < .01); the NA group had the higher rate. PMID:8403908

  17. Oral contraceptive use and bone density in adolescent and young adult women

    PubMed Central

    Scholes, Delia; Ichikawa, Laura; LaCroix, Andrea Z.; Spangler, Leslie; Beasley, Jeannette M.; Reed, Susan; Ott, Susan M.

    2009-01-01

    Background Most of the millions of oral contraceptive (OC) users are under age 30 years and in the critical period for bone mass accrual. Study Design This cross-sectional study of 606 women aged 14–30 years examined both OC duration and estrogen dose and their association with bone mineral density (BMD) at the hip, spine, and whole-body (DEXA). Results Of 389 OC users and 217 nonusers enrolled, 50% were adolescents (14–18 years). Of OC users, 38% used “low-dose” OCs [<30 mcg ethinyl estradiol (EE)]. In adolescents, mean BMD differed by neither OC duration nor EE dose. However, 19–30 year-old women’s mean BMD was lower with longer OC use for spine and whole-body (p=0.004, p=0.02, respectively) and lowest for >12 months of low-dose OCs for the hip, spine and whole-body (p=0.02, 0.003 and 0.002, respectively). Conclusions Prolonged use of today’s OCs, particularly <30 mcg EE, may adversely impact young adult women’s bone density while ingesting these agents. PMID:20004271

  18. Efficacy and safety of combined ethinyl estradiol/drospirenone oral contraceptives in the treatment of acne.

    PubMed

    Tan, Jerry Kl; Ediriweera, Chemanthi

    2010-01-01

    Acne is a common disorder affecting the majority of adolescents and often extends into adulthood. The central pathophysiological feature of acne is increased androgenic stimulation and/or end-organ sensitivity of pilosebaceous units leading to sebum hypersecretion and infundibular hyperkeratinization. These events lead to Propionibacterium acnes proliferation and subsequent inflammation. Hormonal therapy, including combined oral contraceptives (OCs), can attenuate the proximate androgenic trigger of this sequence. For many women, hormonal therapy is a rational option for acne treatment as it may be useful across the spectrum of severity. Drospirenone (DRSP) is a unique progestin structurally related to spironolactone with progestogenic, antimineralocorticoid, and antiandrogenic properties. It is available in 2 combined OC preparations (30 μg EE/3 mg DRSP; Yasmin(®) in a 21/7 regimen; and 20 μg EE/3 mg DRSP; Yaz(®) in a 24/4 regimen). These preparations are bereft of the fluid retentional side effects typical of other progestins and their safety has been demonstrated in large epidemiological studies in which no increased risk of vascular thromboembolic disease or arrhythmias was observed. In acne, the efficacy of DRSP-containing OCs has been shown in placebo-controlled superiority trials and in active-comparator non-inferiority trials. PMID:21072290

  19. Evaluation of cerebral venous thrombosis secondary to oral contraceptive use in adolescents.

    PubMed

    Özdemir, Hasan H; Varol, Sefer; Akıl, Eşref; Acar, Abdullah; Demir, Caner F

    2015-01-01

    Our goal was to evaluate the clinical patterns, additional risk factors, treatment and outcome of cerebral venous thrombosis (CVT) related to adolescent oral contraceptive pill (OCP) usage. We evaluated 22 patients with CVT related to OCPs admitted to Firat and Dicle University Hospitals from January 2008 to January 2013. We assessed the clinical features, risk factors, imaging results and prognosis. Magnetic resonance imaging (MRI) and magnetic resonance were the preferred procedures for the diagnosis of CVT. MRI revealed parenchymal lesions in 11 (50 %) patients, and the remaining patients had normal MRIs. The sinuses most frequently affected by thrombosis were the superior sagittal sinus and the transverse sinus. The additional risk factors identified for CVT were antiphospholipid syndrome, protein C deficiency, protein C and S deficiency, factor V Leiden associated with heterozygous antithrombin III deficiency, methylenetetrahydrofolate reductase and prothrombin gene mutations. CVT may be overlooked in adolescents because it is more common among middle-aged and elderly adults. CVT should be suspected in the presence of neurological symptoms in adolescents, especially in those using OCPs. PMID:25092566

  20. Sex steroids, sexual behavior, and selection attention for erotic stimuli in women using oral contraceptives.

    PubMed

    Alexander, G M; Sherwin, B B

    1993-01-01

    The relationship between sex steroids and sexual behavior was examined in 19 oral contraceptive users. Retrospective assessment of sexual attitudes were obtained and women completed daily ratings of sexual behavior and well-being for 28 days. Plasma levels of free testosterone (T), estradiol, and progesterone were measured at weekly intervals. In addition, women performed a novel selective attention task designed to measure the strength of the tendency to be distracted by sexual stimuli. Multiple regression analyses using average sexual behavior variables as dependent variables, and hormone levels sexual attitudes and well-being as predictor variables, showed that free T was strongly and positively associated with sexual desire, sexual thoughts, and anticipation of sexual activity. A role for T in attention to sexual stimuli was also supported by the positive correlation between free T and the bias for sexual stimuli in a subgroup of women. These results are consistent with the hypothesis that T may enhance cognitive aspects of women's sexual behavior. PMID:8493300

  1. Relative impact of smoking and oral contraceptive use on women in the US

    SciTech Connect

    Goldbaum, G.M.; Kendrick, J.S.; Hogelin, G.C.; Gentry, E.M.

    1987-09-11

    Women who smoke and use oral contraceptives (OCs) are at increased risk for cardiovascular and cerebrovascular disease. To study the prevalence of smoking and OC use and of other behaviors affecting health, 28 states and the District of Columbia conducted telephone surveys during 1981 through 1983. More than 22,000 US adults were interviewed, of whom 5779 women aged 18 to 44 years were studied. Data were weighted to represent the US population. Overall, 7.4% of US women aged 18 to 44 years reported smoking and using OCs' 1.1% reported smoking 25 or more cigarettes per day while using OCs. Although women aged 18 to 24 years were most likely to smoke and use OCs, combined smoking and OC use contributed substantially to the number of excess cases of myocardial infarctions occurring among US women aged 35 to 44 years. However, regardless of OC use, smoking accounted for most of the excess cases. Therefore, health care providers need to intensity their efforts to reduce smoking among their patients.

  2. Ultrasound image attributes of human ovarian dominant follicles during natural and oral contraceptive cycles

    PubMed Central

    Birtch, Rebecca L; Baerwald, Angela R; Olatunbosun, Olufemi A; Pierson, Roger A

    2005-01-01

    Background Computer-assisted analyses were used to examine ultrasound image attributes of human dominant ovarian follicles that developed during natural and oral contraceptive (OC) cycles. We hypothesized that image attributes of natural cycle follicles would quantitatively differ from those in OC cycles and that OC cycle follicles would possess image attributes indicative of atresia. Methods Dominant ovarian follicles of 18 clinically normal women were compared using transvaginal ultrasonography for the 7 days before ovulation during a natural cycle (n = 9) or the 7 days before peak estradiol in women using OC (n = 11). Follicles were analyzed using region and line techniques designed to compare the image attributes numerical pixel value (NPV), pixel heterogeneity (PH) and area under the curve (AUC). Results NPV was higher in OC cycle follicles with region analysis and tended to be higher with line analysis (p = 0.005 and p = 0.06, respectively). No differences were observed in two other image attributes (AUC and PH), measured with either technique, between natural and OC cycle follicles. Conclusion The increased NPV value of OC cycle follicles and lack of differences in PH and AUC values between natural cycle and OC cycle follicles did not support the hypothesis that OC cycle follicles would show ultrasonographically detectable signs of atresia. Image attributes observed in OC cycle follicles were not clearly indicative of atresia nor were they large enough to preclude preovulatory physiologic status in OC cycle follicles. PMID:15829004

  3. Diminished nap effects on memory consolidation are seen under oral contraceptive use.

    PubMed

    Genzel, Lisa; Bäurle, Anna; Potyka, Alina; Wehrle, Renate; Adamczyk, Marek; Friess, Elisabeth; Steiger, Axel; Dresler, Martin

    2014-01-01

    Many young females take exogenous hormones as oral contraceptive (OC), a condition rarely controlled for in studies on sleep and memory consolidation even though sex hormones influence consolidation. This study investigated the effects of OCs on sleep-related consolidation of a motor and declarative task, utilizing a daytime nap protocol. Fifteen healthy, young females taking OCs came to the sleep lab for three different conditions: nap with previous learning, wake with previous learning and nap without learning. They underwent each condition twice, once during the "pill-active" weeks and once during the "pill-free" week, resulting in 6 visits. In all conditions, participants showed a significant off-line consolidation effect, independent of pill week or nap/wake condition. There were no significant differences in sleep stage duration, spindle activity or spectral EEG frequency bands between naps with or without the learning condition. The present data showed a significant off-line enhancement in memory irrespective of potential beneficial effects of a nap. In comparison to previous studies, this may suggest that the use of OCs may enhance off-line memory consolidation in motor and verbal tasks per se. These results stress the importance to control for the use of OCs in studies focusing on memory performance. PMID:25720656

  4. Design Features of Drug-Drug Interaction Trials Between Antivirals and Oral Contraceptives.

    PubMed

    Ayala, Ruben C; Arya, Vikram; Younis, Islam R

    2016-05-01

    The aim of this work was to explore the major design features of drug-drug interaction trials between antiviral medications (AVs) and oral contraceptives (OCs). Information on these trials (n = 27) was collected from approved drug labels and clinical pharmacology reviews conducted by the U.S. Food and Drug Administration. The primary objective of all trials was to evaluate changes in OC exposure following the coadministration of AVs. In addition, an evaluation of potential pharmacodynamic interaction was performed in 10 of these trials. Twenty-two trials were open label with a fixed-sequence design, and 5 trials used a double-blind crossover design. The trials were conducted using one, two, or three 28-day ovulatory cycles in 10, 8, and 9 trials, respectively. Only 1 trial enrolled HIV-infected women. The median number of women in a trial was 20 (range, 12 to 52). Norethindrone/ethinyl estradiol (EE) combination was the most commonly used OC (n = 16, 59%) followed by norgestimate/EE (n = 9, 33%). Labeling recommendations were based on exposure changes in 25 cases and on safety observations in the trial in 2 cases. In conclusion, a wide variety of trial designs was used, and there is no preferred design. The answer to the exposure question can be achieved using multiple designs. PMID:26384089

  5. Seeing things differently: expert and consumer mental models evaluating combined oral contraceptives.

    PubMed

    Vogt, Claudia; Schaefer, Marion

    2012-01-01

    Communication regarding the benefits and risks of combined oral contraceptives (COCs) remains a challenge in view of persistent misconceptions about the 'pill'. The aim of this study was to investigate how women understand the benefits and risks of COCs, comparing their assessments with an expert model created from literature- and guideline-based research and reviewed by a sample of gynaecologists using the mental models approach. Two qualitative studies were conducted in Germany - a questionnaire-based study involving 30 gynaecologists with a mean of 218 COC prescriptions on average per month, and in-depth interviews (plus the use of a questionnaire) with 21 women aged 18-24 years. As expected, women reported only a few concepts of benefits and risks unprompted, but further prompting revealed beliefs of many other associations. The women stated an overall positive valence even if the number of negative concepts predominated indicating a latent cognitive dissonance. The major differences compared with the expert model included: (a) a negative association with weight gain, subfertility and teratogenicity, (b) only a partial association of COC intake with thromboembolic conditions, (c) a confusing, rather negative perception of a COC-related effect on cancer and (d) a partial lack of basic knowledge of the active ingredients, time to excretion and mode of action of COCs. Appropriate COC counselling should cover these discrepancies. PMID:22519728

  6. Differential effects of isoniazid and oral contraceptive steroids on antipyrine oxidation and acetaminophen conjugation.

    PubMed

    Ochs, H R; Greenblatt, D J; Verburg-Ochs, B; Abernethy, D R; Knüchel, M

    1984-01-01

    Factors influencing hepatic oxidation of antipyrine and conjugation of acetaminophen were evaluated in volunteers who received 1.0 g of antipyrine intravenously and on a different occasion a 650 mg intravenous dose of acetaminophen. In study one, subjects received both drugs in the control state and at another time during coadministration of isoniazid (INH), 180 mg daily. In control versus INH conditions, mean clearance of antipyrine was reduced from 0.67 to 0.60 ml/min/kg as was clearance of acetaminophen from 4.97 to 4.23 ml/min/kg, but these differences were not statistically significant. In study two, females on low-dose estrogen oral contraceptives (OC) and drug-free controls matched for age received both drugs. Compared to controls, OC users had reduced total clearance of antipyrine (0.71 vs. 0.50 ml/min/kg; p less than 0.005) and prolonged antipyrine t1/2 (9.6 vs. 13.3 h; p less than 0.005). For acetaminophen, however, OC users had higher clearance (5.2 vs. 6.1 ml/min/kg) and shorter t1/2 (2.2 vs. 1.9 h) although differences did not attain statistical significance. Clearance of antipyrine and acetaminophen across both studies was not statistically significantly correlated within individuals (r = 0.22). The capacities for drug oxidation and conjugation appear to be controlled by different mechanisms. PMID:6728897

  7. Thrombotic microangiopathy caused by oral contraceptives in a kidney transplant recipient.

    PubMed

    Shirai, Hiroyuki; Yashima, Jun; Tojimbara, Tamotsu; Honda, Kazuho

    2016-07-01

    Thrombotic microangiopathy (TMA) after kidney transplantation has various aetiologies, including acute antibody-mediated rejection, bacterial or viral infection and immunosuppressive drugs, particularly calcineurin inhibitors. We present the case of a 28-year-old woman who developed TMA 30 months after the transplantation of an ABO-incompatible kidney from a living unrelated donor. The patient developed a sudden onset of allograft renal dysfunction and became uremic. She was transferred to our institution from a community hospital with strongly suspected acute allograft rejection. Intensive treatments for both T- and B-cell mediated acute rejection, including steroid pulse therapy, double-filtration plasmapheresis, antithymocyte globulin (1.5 mg/kg × 14 days) and rituximab (100 mg), were initiated during haemodialysis. However, her renal allograft function did not improve. Histopathological analysis 8 days after the treatment indicated TMA, despite the absence of apparent acute T-cell- or acute antibody-mediated rejection. There were no symptoms of infectious diseases, such as intestinal haemorrhagic colitis or viral infection. We concluded that the use of oral contraceptives, which had been initiated 3 weeks before TMA onset for the treatment of irregular vaginal bleeding, was the aetiologic agent. PMID:26970708

  8. Salivary SIgA responses to acute moderate-vigorous exercise in monophasic oral contraceptive users.

    PubMed

    Hayashida, Harumi; Dolan, Nicola J; Hounsome, Charlotte; Alajmi, Nawal; Bishop, Nicolette C

    2015-09-01

    The purpose of this study was to examine the effect of oral contraceptive (OC) use on salivary secretory immunoglobulin A (SIgA) levels at rest and in response to an acute bout of moderate-vigorous exercise during 2 phases of the 4-week OC cycle corresponding to different phases of the synthetic menstrual cycle. Ten healthy active females completed a cycling at 70% peak oxygen uptake for 45 min at 2 time points of an OC cycle: during the equivalent in time to the mid-follicular phase (day 8 ± 2) and the mid-luteal phase (day 20 ± 2). Timed unstimulated saliva samples were obtained before, immediately postexercise, and 1 h postexercise and analyzed for salivary SIgA. Salivary SIgA secretion rate was 26% (95% confidence limits (CI) 6-46) lower at postexercise compared with pre-exercise during the synthetic follicular phase (p = 0.019) but no differences were observed during the synthetic luteal trial. Saliva flow rate was 11% (95% CI, 8-30) lower at postexercise compared with pre-exercise (main effect for time; p = 0.025). In conclusion, the pattern of salivary SIgA secretion rate response to moderate-vigorous exercise varies across the early and late phases of a monophasic OC cycle, with a transient reduction in salivary SIgA responses during the synthetic follicular phase. These findings indicate that monophasic OC use should be considered when assessing mucosal immune responses to acute exercise. PMID:26300012

  9. Comparison of prospective daily diaries and retrospective recall to measure oral contraceptive adherence

    PubMed Central

    Huber, Larissa R. Brunner; Broel, Elizabeth C.; Mitchelides, Ashley N.; Dmochowski, Jacek; Dulin, Michael; Scholes, Delia

    2013-01-01

    BACKGROUND The purpose of this study was to determine if retrospective recall of oral contraceptive (OC) adherence provides data that are similar to data collected via daily diaries over the same time period. Factors associated with inconsistent agreement between prospective and retrospective measurements of adherence also were explored. STUDY DESIGN A total of 185 women participated in a longitudinal, prospective cohort of OC users and 113 of these women provided complete information on OC adherence during follow-ups. Concordance beyond chance was assessed using weighted kappa statistics and logistic regression was used to identify factors associated with inconsistent reporting of adherence. RESULTS There was substantial agreement between prospective and retrospective adherence information (weighted kappa=0.64; 95% CI: 0.52, 0.77). Participants with a high school education or less and those who had problems with feeling sad while using OCs had increased odds of inconsistent reporting of adherence (OR=4.38, 95% CI: 1.41, 13.61 and OR=3.52, 95% CI: 1.25, 9.94; respectively). CONCLUSION While prospective data collection via diaries may improve accuracy, the added expense and burden on study participants may not be necessary. However, the use of retrospective recall may not be appropriate for all study populations. PMID:23582236

  10. Oral Contraceptive Use and the ECG: Evidence of an Adverse QT Effect on Corrected QT Interval

    PubMed Central

    Sedlak, Tara; Shufelt, Chrisandra; Iribarren, Carlos; Lyon, Liisa L; Merz, C. Noel Bairey

    2013-01-01

    Background A prolonged corrected QT (QTc) interval is a marker for an increased risk of sudden cardiac death. We evaluated the relationship between oral contraceptive (OC) use, type of OC, and QTc interval. Methods We identified 410,782 ECGs performed at Northern California Kaiser Permanente on female patients between 15–53 years from January, 1995 to June, 2008. QT was corrected for heart rate using log-linear regression. OC generation (first, second and third) was classified by increasing progestin androgenic potency, while the fourth generation was classified as anti-androgenic. Results Among 410,782 women, 8.4% were on OC. In multivariate analysis after correction for comorbidities, there was an independent shortening effect of OCs overall (slope = −0.5ms; SE = 0.12, p<0.0002). Users of first and second generation progestins had a significantly shorter QTc than non-users (p<0.0001), while users of fourth generation had a significantly longer QTc than non-users (slope = 3.6ms, SE = 0.35, p<0.0001). Conclusion Overall, OC use has a shortening effect on the QTc. Shorter QTc is seen with first and second generation OC while fourth generation OC use has a lengthening effect on the QTc. Careful examination of adverse event rates in fourth generation OC users is needed. PMID:23879279

  11. Duration of oral contraceptive use predicts women's initial and subsequent subjective responses to sexual stimuli.

    PubMed

    Renfro, Kaytlin J; Rupp, Heather; Wallen, Kim

    2015-09-01

    Recent work suggests that a woman's hormonal state when first exposed to visual sexual stimuli (VSS) modulates her initial and subsequent responses to VSS. The present study investigated whether women's initial hormonal state was related to their subjective ratings of VSS, and whether this relationship differed with VSS content. We reanalyzed previously collected data from 14 naturally cycling (NC) women and 14 women taking oral contraceptives (OCs), who subjectively rated VSS at three hormonal time-points. NC women's ratings of 216 unique sexual images were collected during the menstrual, periovulatory, and luteal phases of their menstrual cycles, and OC women's ratings were collected at comparable time-points across their pill-cycles. NC women's initial hormonal state was not related to their ratings of VSS. OC women's initial hormonal state predicted their ratings of VSS with minimal contextual information and of images depicting female-to-male oral sex. Specifically, women who entered the study in the third week of their pill-cycle (OC-3 women) rated such images as less attractive at all testing sessions than did all other women. OC-3 women were also the only women to rate decontextualized VSS as unattractive at all testing sessions. These results corroborate previous studies in which women's initial hormonal state was found to predict subsequent interest in sexual stimuli. Future work, with larger samples, should more directly investigate whether OC-3 women's negative assessment of specific types of VSS reflects a reaction to the laboratory environment or a broader mechanism, wherein OC women's sexual interests decrease late in their pill-cycle. PMID:26204805

  12. Review of the safety, efficacy and patient acceptability of the combined dienogest/estradiol valerate contraceptive pill.

    PubMed

    Guida, Maurizio; Bifulco, Giuseppe; Di Spiezio Sardo, Attilio; Scala, Mariamaddalena; Fernandez, Loredana Maria Sosa; Nappi, Carmine

    2010-01-01

    The aim of this review is to define the role of the combined dienogest (DNG)/estradiol valerate (E2V) contraceptive pill, in terms of biochemistry, metabolic and pharmacological effects and clinical application as well. E2V is the esterified form of 17β-estradiol (E2), while dienogest is a fourth-generation progestin with a partial antiandrogenic effect. The cycle stability is achieved with 2 to 3 mg DNG, supporting contraceptive efficacy. In this new oral contraceptive, E2V is combined with DNG in a four-phasic dose regimen (the first two tablets contain 3 mg E2V; the next five tablets include 2 mg E2V + 2 mg DNG, followed by 17 tablets with 2 mg E2V + 3 mg DNG; followed by two tablets with 1 mg E2V only, and finally two placebo tablets). Duration and intensity of scheduled withdrawal bleeding are lower with this contraceptive pill, whereas the incidence and the intensity of intra-cyclic bleeding are similar to the other oral contraceptive. With this new pill the levels of high density lipoprotein increased, while the levels of prothrombin fragment 1 + 2 and D-dimer remained relatively unchanged; the levels of sex hormone binding globulin, cortisol binding globulin, thyroxine binding globulin increased. The most frequently reported adverse events are: breast pain, headache, acne, alopecia, migraine, increase of bodyweight. The satisfaction rate is about 79.4%. PMID:21151673

  13. An assessment of the quality of advice provided by patent medicine vendors to users of oral contraceptive pills in urban Nigeria

    PubMed Central

    Ujuju, Chinazo; Adebayo, Samson B; Anyanti, Jennifer; Oluigbo, Obi; Muhammad, Fatima; Ankomah, Augustine

    2014-01-01

    Introduction In Nigeria about 50% of oral contraceptive pill users obtain their products from proprietary patent medicine vendors (PPMVs). This group of service providers are poorly trained and have very limited knowledge about contraception. This paper investigated the nature of the advice offered to simulated current and potential users of oral contraceptive pills. The main objective was to assess the nature and quality of advice provided by PPMVs to pill users. Method This study is based on findings from a ‘mystery client’ approach in which three scenarios related to contraceptive pill use were simulated. Each of the 12 mystery clients simulated one of the following three scenarios: new pill users (new to family planning or switching from condom to pills); user seeking a resupply of pills; and dissatisfied pill users intending to discontinue use. Simple random sampling was used to select 410 PPMVs from a total of 1,826 in four states in Nigeria. Qualitative study using in-depth interviews was also conducted. Results A majority of the PPMVs had pills in stock on the day of the survey and resupplied pills to the clients. PPMVs also understood the reason and importance of referring clients who were new adopters of oral contraceptive methods to a health facility; 30% of the PPMVs referred new adopters to a health facility. However, demand from clients who do not want to go to health care facilities (for various reasons) necessitated the provision of oral contraceptive pills to 41% of the first time users. Some PPMVs prescribed treatment to mystery clients who presented with perceived complications arising from the use of pills, while 49% were referred to a health facility. Conclusion The advice given by PPMVs often falls short of safety guidelines related to the use of oral contraceptive pills. There is a need to continuously update knowledge among the PPMVs to ensure that they provide quality oral contraceptive services as PPMVs bridge the gap between medical

  14. Oral contraceptive use in women changes preferences for male facial masculinity and is associated with partner facial masculinity.

    PubMed

    Little, Anthony C; Burriss, Robert P; Petrie, Marion; Jones, Benedict C; Roberts, S Craig

    2013-09-01

    Millions of women use hormonal contraception and it has been suggested that such use may alter mate preferences. To examine the impact of oral contraceptive (pill) use on preferences, we tested for within-subject changes in preferences for masculine faces in women initiating pill use. Between two sessions, initiation of pill use significantly decreased women's preferences for male facial masculinity but did not influence preferences for same-sex faces. To test whether altered preference during pill use influences actual partner choice, we examined facial characteristics in 170 age-matched male partners of women who reported having either been using or not using the pill when the partnership was formed. Both facial measurements and perceptual judgements demonstrated that partners of women who used the pill during mate choice have less masculine faces than partners of women who did not use hormonal contraception at this time. Our data (A) provide the first experimental evidence that initiation of pill use in women causes changes in facial preferences and (B) documents downstream effects of these changes on real-life partner selection. Given that hormonal contraceptive use is widespread, effects of pill use on the processes of partner formation have important implications for relationship stability and may have other biologically relevant consequences. PMID:23528282

  15. The efficacy and safety of clotrimazole vaginal tablet vs. oral fluconazole in treating severe vulvovaginal candidiasis.

    PubMed

    Zhou, Xiaofang; Li, Ting; Fan, Shangrong; Zhu, Yuxia; Liu, Xiaoping; Guo, Xuedong; Liang, Yiheng

    2016-07-01

    To compare the efficacy and safety of two doses of clotrimazole vaginal tablet 500 mg with two doses of oral fluconazole 150 mg in treating severe vulvovaginal candidiasis (SVVC), 240 consecutive patients with SVVC were studied at the Department of Obstetrics and Gynaecology of Peking University Shenzhen Hospital between June 2014, and September 2015. Patients were randomly assigned in a 1 : 1 ratio to receive treatment with either two doses of clotrimazole vaginal tablet or two doses of oral fluconazole. The clinical cure rates in the clotrimazole group and the fluconazole group at days 7-14 follow-up were 88.7% (102/115) and 89.1% (98/110) respectively; the clinical cure rates at days 30-35 in the two groups were 71.9% (82/114) and 78.0% (85/109) respectively. The mycological cure rates at days 7-14 follow-up in the two groups were 78.3% (90/115) and 73.6% (81/110) respectively. The mycological cure rates of the patients at days 30-35 in the two groups were 54.4% (62/114) and 56.0% (61/109) respectively (P > 0.05). The adverse events of clotrimazole were mainly local. This study demonstrated that two doses of clotrimazole vaginal tablet 500 mg were as effective as two doses of oral fluconazole 150 mg in the treatment of patients with SVVC and could be an appropriate treatment for this disorder. PMID:27073145

  16. Coated dextrin microcapsules of amlodipine incorporable into orally disintegrating tablets for geriatric patients.

    PubMed

    Jang, Dong-Jin; Bae, Soo Kyung; Oh, Euichaul

    2014-10-01

    To improve oral absorption and patient compliance when using amlodipine, novel coated dextrin microcapsules incorporable into orally disintegrating tablets (ODT's) were investigated. Amlodipine-loaded dextrin microcapsules (ADM) were prepared by spray-drying a mixture of amlodipine free base dissolved in ethanol and aqueous dextrin solution. The ADM were suspended in Eudragit(®) EPO solution in ethanol and subsequently spray-dried to collect coated ADM (CADM). The ADM or CADM were blended with ODT excipients and then directly compressed into ODTs. The ADM and CADM used were both spherical with smooth surfaces and had mean particle sizes of 13.3 and 18.5μm, respectively. Amlodipine was dispersed in an amorphous state and was readily encapsulated within ADM or CADM. Unlike the ADM, the tableted CADM remained intact without rupture during tableting, which was consistent with no loss of ethanol (0.82%) entrapped in the ODTs containing the CADM (ODTs-CADM). The amlodipine content appeared to be uniformly maintained as designed in all the dextrin microcapsules and ODTs. The ODTs-CADM compressed with 3kp of hardness showed acceptable ODT characteristics: fast disintegration time (29.8s) and low friability (0.1%). Drug dissolution from the ODTs-CADM was much faster than that of amlodipine free base itself at both pH 1.2 and 6.8 over the tested time. CADM demonstrated significantly higher plasma concentrations (2.7 fold in AUC0-24h and 2.5 fold in Cmax) in SD rats than did amlodipine free base. These results indicate that CADM substantially increased the oral absorption of amlodipine and can be incorporated into ODTs while maintaining their original physicochemical features. The dextrin microcapsules coated using Eudragit(®) EPO may be applied to the development of an amlodipine ODT formulation for improving geriatric patient compliance. PMID:25458788

  17. [Time course of inhibition of caffeine elimination in response to the oral depot contraceptive agent Deposiston. Hormonal contraceptives and caffeine elimination].

    PubMed

    Meyer, F P; Canzler, E; Giers, H; Walther, H

    1991-01-01

    In the course of six months, the influence of the oral depot contraceptive, Deposiston (3 mg ethinylestradiol sulphonate and 10 mg norethisterone acetate per menstrual cycle) on the pharmacokinetics of caffeine as a model substance was studied in seven women in intraindividual comparison. The first examination began prior to administration of Deposition. The women were subjected to little challenge as saliva was used as the measuring compartment. Deposiston was found markedly delay the elimination half-life life of caffeine (p less than 0.05): t1/2 prior to therapy 4.9 +/- 2.6 h and, after as little as 2 mg ethinylestradiol sulphonate 8.0 +/- 3.5 h. In contrast to the effect observed for preparations containing less estrogen, these longer half-lives persisted throughout the trial. As expected, the AUC values were slightly elevated during this period, whereas clearance values were reduced. PMID:2058339

  18. Biotransformation of oral contraceptive ethynodiol diacetate with microbial and plant cell cultures

    PubMed Central

    2012-01-01

    Background Biotransformation by using microbial and plant cell cultures has been applied effectively for the production of fine chemicals on large scale. Inspired by the wealth of literature available on the biotransformation of steroids, we decided to investigate the biotransformation of ethynodiol diacetate (1) by using plant and microbial cultures. Results The biotransformation of ethynodiol diacetate (1) with Cunninghamella elegans and plant cell suspension cultures of Ocimum basilicum and Azadirachta indica is being reported here for the first time. Biotransformation of 1 with Cunninghamella elegans yielded three new hydroxylated compounds, characterized as 17α-ethynylestr-4-en-3β,17β-diacetoxy-6α-ol (2), 17α-ethynylestr-4-en-3β,17β-diacetoxy-6β-ol (3), and 17α-ethynylestr-4-en-3β,17β-diacetoxy-10β-ol (4) and a known metabolite, 17α-ethynyl-17β-acetoxyestr-4-en-3-one (5). The biotransformation of 1 with Ocimum basilicum included hydrolysis of the ester group, oxidation of alcohol into ketone, and rearrangement of the hydroxyl group. Thus four major known metabolites were characterized as 17α-ethynyl-17β-acetoxyestr-4-en-3-one (5), 17α-ethynyl-17β-hydroxyestr-4-en-3-one (6), 17α-ethynyl-3 β-hydroxy-17β-acetoxyestr-4-ene (7) and 17α-ethynyl-5α,17β-dihydroxyestr-3-ene (8). Biotransformation of 1 with Azadirachta indica culture yielded compounds 5 and 6. Spectroscopic data of compound 8 is being reported for the first time. Structure of compound 6 was unambiguously deduced through single-crystal x-ray diffraction studies. Conclusion Biotransformation of an oral contraceptive, ethynodiol diacetate (1), by using microbial and plant cell cultures provides an efficient route to the synthesis of a library of new steroids with potential contraceptive properties. These methods can be employed in the production of such compounds with high stereoselectivity. PMID:23021311

  19. Pre-gravid oral contraceptive use and time to pregnancy: a Danish prospective cohort study

    PubMed Central

    Mikkelsen, Ellen M.; Riis, Anders H.; Wise, Lauren A.; Hatch, Elizabeth E.; Rothman, Kenneth J.; Toft Sørensen, Henrik

    2013-01-01

    STUDY QUESTION Is there an association between oral contraceptive (OC) use (age at the start of use, duration of use, ethinylestradiol dose and generation) and time to pregnancy (TTP)? SUMMARY ANSWER Although OC use was associated with a transient delay in the return of fertility, we found no evidence that long-term OC use deleteriously affects fecundability. WHAT IS KNOWN ALREADY Studies using retrospective data on TTP have reported a short-term delay in the return of fertility after OC use. However, little is known about the long-term OC use and TTP. STUDY DESIGN, SIZE, DURATION Data were derived from ‘Snart Gravid.dk’, a prospective cohort study that enrolled participants from 1 June 2007 to 31 May 2010. The final study population consisted of 3727 women. PARTICIPANTS, SETTING, METHODS Eligible women were Danish pregnancy planners, aged 18–40 years, who completed a baseline questionnaire and bimonthly follow-up questionnaires until conception or for 12 months, whichever came first. Cohort retention was 80%. We used proportional probability regression models to estimate fecundability ratios (FRs) and 95% confidence intervals (CIs), with adjustment for potential confounders. MAIN RESULTS AND ROLE OF CHANCE Compared with barrier methods, the use of OCs as the last contraception method before attempting to conceive was associated with a short-term delay in return of fertility (FR = 0.87, 95% CI: 0.79–0.96). Longer term OC use was associated with higher fecundability: compared with OC use for less than 2 years; FRs were 0.98 (95% CI: 0.83–1.15) for 2–3 years, 1.16 (95% CI: 0.98–1.37) for 4–5 years, 1.10 (95% CI: 0.93–1.29) for 6–7 years, 1.17 (95% CI: 0.99–1.38) for 8–9 years, 1.23 (95% CI: 1.04–1.46) for 10–11 years and 1.28 (95% CI: 1.07–1.53) for ≥12 years of OC use. LIMITATIONS, REASONS FOR CAUTION Because this was a non-experimental study, where study volunteers provided information about their history of contraceptive use at

  20. The 1998 Canadian Contraception Study.

    ERIC Educational Resources Information Center

    Fisher, William A.; Boroditsky, Richard; Bridges, Martha L.

    1999-01-01

    Describes the 1998 Canadian Contraception Study, a mailed survey which asked women about contraceptive practices past, present, and future (including use of oral contraceptives, condoms, and sterilization); familiarity with and opinion about different contraception methods; and general sexual and reproductive health. The paper also examines…

  1. Maltodextrin: a novel excipient used in sugar-based orally disintegrating tablets and phase transition process.

    PubMed

    Elnaggar, Yosra Shaaban R; El-Massik, Magda A; Abdallah, Ossama Y; Ebian, Abd Elazim R

    2010-06-01

    The recent challenge in orally disintegrating tablets (ODT) manufacturing encompasses the compromise between instantaneous disintegration, sufficient hardness, and standard processing equipment. The current investigation constitutes one attempt to fulfill this challenge. Maltodextrin, in the present work, was utilized as a novel excipient to prepare ODT of meclizine. Tablets were prepared by both direct compression and wet granulation techniques. The effect of maltodextrin concentrations on ODT characteristics--manifested as hardness and disintegration time--was studied. The effect of conditioning (40 degrees C and 75% relative humidity) as a post-compression treatment on ODT characteristics was also assessed. Furthermore, maltodextrin-pronounced hardening effect was investigated using differential scanning calorimetry (DSC) and X-ray analysis. Results revealed that in both techniques, rapid disintegration (30-40 s) would be achieved on the cost of tablet hardness (about 1 kg). Post-compression conditioning of tablets resulted in an increase in hardness (3 kg), while keeping rapid disintegration (30-40 s) according to guidance of the FDA for ODT. However, direct compression-conditioning technique exhibited drawbacks of long conditioning time and appearance of the so-called patch effect. These problems were, yet, absent in wet granulation-conditioning technique. DSC and X-ray analysis suggested involvement of glass-elastic deformation in maltodextrin hardening effect. High-performance liquid chromatography analysis of meclizine ODT suggested no degradation of the drug by the applied conditions of temperature and humidity. Overall results proposed that maltodextrin is a promising saccharide for production of ODT with accepted hardness-disintegration time compromise, utilizing standard processing equipment and phenomena of phase transition. PMID:20405257

  2. Pre-exposure Prophylaxis Adherence Measured by Plasma Drug Level in MTN-001: Comparison Between Vaginal Gel and Oral Tablets in Two Geographic Regions.

    PubMed

    Minnis, Alexandra M; van der Straten, Ariane; Salee, Parichat; Hendrix, Craig W

    2016-07-01

    Despite strong evidence that daily oral pre-exposure prophylaxis (PrEP) reduces HIV risk, effectiveness across studies has varied. Inconsistent adherence constitutes one explanation. Efforts to examine adherence are limited when they rely on self-reported measures. We examined recent adherence as measured by plasma tenofovir (TFV) concentration in participants of MTN-001, a phase 2 cross-over trial comparing oral tablet and vaginal gel formulations of TFV among 144 HIV-uninfected women at sites in the United States (U.S.) and sub-Saharan Africa (SSA). Adherence to daily product use was higher in the U.S. than in the SSA sites. Within region, however, adherence was similar between products. In the U.S., gel adherence was higher among married women, and lower among women using male condoms and injectable contraceptives. At the SSA sites, gel adherence was lower for younger women. Inconsistent adherence points to challenges in use of daily PrEP, even during a trial of short duration. PMID:25969178

  3. Bleeding patterns of women using Lunelle monthly contraceptive injections (medroxyprogesterone acetate and estradiol cypionate injectable suspension) compared with those of women using Ortho-Novum 7/7/7 (norethindrone/ethinyl estradiol triphasic) or other oral contraceptives.

    PubMed

    Garceau, R J; Wajszczuk, C J; Kaunitz, A M

    2000-12-01

    Persistent and/or unpredictable bleeding is a common reason for discontinuation of hormonal contraceptive methods. An open-label, nonrandomized, parallel, controlled study compared the efficacy, safety, and cycle control of the new, highly efficacious monthly injectable contraceptive containing 25 mg medroxyprogesterone acetate (MPA) and 5 mg estradiol cypionate (E(2)C) (MPA/E(2)C) (Lunelle Monthly Contraceptive Injection) with that of the frequently used norethindrone 0.5, 0.75, 1.0 mg/0.035 mg ethinyl estradiol (NET/EE) triphasic oral contraceptive (Ortho-Novum 7/7/7). This report directly compares the bleeding patterns of women on MPA/E(2)C to those of women on NET/EE and untreated women. Overall, breakthrough bleeding occurred less frequently in women using MPA/E(2)C than in women using NET/EE (p < or =0.01). However, more women using MPA/E(2)C experienced amenorrhea/missed periods than those on NET/EE (p < or =0.01). In addition, the percentage of women experiencing breakthrough bleeding or amenorrhea while using other oral contraceptives is compared to that of women using MPA/E(2)C. A rapidly reversible method, MPA/E(2)C, combines the high contraceptive efficacy of surgical sterilization with the convenience of monthly administration. These data suggest that, for a large proportion of women, MPA/E(2)C offers predictability in bleeding patterns comparable to or greater than that experienced by ovulatory untreated women or those using combination oral contraceptives. PMID:11239615

  4. Effects of Food Thickeners on the Inhibitory Effect of Voglibose Oral-disintegrating Tablets on Post-prandial Elevation of Blood Sugar Levels.

    PubMed

    Tomita, Takashi; Goto, Hidekazu; Sumiya, Kenji; Yoshida, Tadashi; Tanaka, Katsuya; Kohda, Yukinao

    2016-01-01

    The aim of this study was to examine the effects of food thickeners on the pharmacodynamics of voglibose, an α-glucosidase inhibitor. The pharmacodynamics of voglibose were examined in an open-label study in 9 healthy participants after the ingestion of a single oral dose of a voglibose oral-disintegrating tablet, with and without food thickener immersion. The area under the incremental blood sugar concentration-time curve was larger and the rate of increments in the blood sugar concentration was higher with the voglibose oral-disintegrating tablets immersed in the food thickener than with the tablets that were not immersed. Immersing the voglibose oral-disintegrating tablets in the food thickener possibly delayed their disintegration rate. This suggests that commercially available food thickeners may be associated with changes in the disintegration of voglibose oral-disintegrating tablets and should therefore be used carefully in certain clinical situations. PMID:27477734

  5. Effect of combined low-dose oral contraceptives on blood viscosity and haematocrit.

    PubMed

    Ishak, R; Loh Chooi Khim

    1991-06-01

    Researchers compared the results of hematocrit and blood viscosity tests of 16 women using a combined oral contraceptive (COC) with 30 mcg ethinyl estradiol/150 mcg desogestrel (group 1), 11 women using a COC with 30 mcg ethinyl estradiol/150 mcg levonorgestrel (group 2), and 16 women who did not use any OCs (control group), all who attended the National Population and Family Development Clinic at the General Hospital in Kuala Lumpur, Malaysia. They wanted to examine the effects of COCs on blood viscosity, which is inversely related to blood flow, and hematocrit. The women were matched for age. The hematocrit level of women who took the ethinyl estradiol/desogestrel COC was significantly higher than that of the control group (41.5% vs. 37.4%; p.001). On the other hand, the hematocrit level of women who took the ethinyl estradiol/levonorgestrel COC was close to that of the control group (38.5% vs. 37.4%). Even though the mean whole blood viscosity for group 2 was higher than that of group 1 and the control group (6.6 cps vs. 5.5 cps), the difference was insignificant. Yet whole blood viscosity of group 2 at the higher shear rates (46, 115, and 230 per second) was significantly higher than the control group (p.05). The whole blood viscosities of group 1 and the control group did not differ considerably. This supported the theory that hematocrit contributes to blood viscosity. Further these results agreed with those of another study which also showed increased blood viscosity and hematocrit in healthy women taking OCs. Thus thromboembolic events in women taking OCs could be a result of a drop in rate of blood flow which at the lower shear rates could increase red cell aggregation and clotting. In conclusion, health providers could use these indicators to monitor women who have used OCs over a considerable period for thrombotic risks to determine if OC use should continue. PMID:12317443

  6. Use of Simulated Patients to Evaluate Combined Oral Contraceptive Dispensing Practices of Community Pharmacists

    PubMed Central

    Obreli-Neto, Paulo Roque; Pereira, Leonardo Régis Leira; Guidoni, Camilo Molino; Baldoni, André de Oliveira; Marusic, Srecko; de Lyra-Júnior, Divaldo Pereira; de Almeida, Kelsen Luis; Pazete, Ana Claudia Montolezi; do Nascimento, Janaina Dutra; Kos, Mitja; Girotto, Edmarlon; Cuman, Roberto Kenji Nakamura

    2013-01-01

    Background Combined oral contraceptive (COC) use is the most commonly used reversible method of birth control. The incorrect use of COCs is frequent and one of the most common causes of unintended pregnancies. Community pharmacists (CPs) are in a strategic position to improve COC use because they are the last health professional to interact with patients before drug use. Objective To evaluate the COC dispensing practices of CPs in a developing country. Method A cross-sectional study was conducted in community pharmacies of Assis and Ourinhos microregions, Brazil, between June 1, 2012, and October 30, 2012. Four simulated patients (SPs) (with counseled audio recording) visited community pharmacies with a prescription for Ciclo 21® (a COC containing ethinyl estradiol 30 mcg + levonorgestrel 15 mcg). The audio recording of every SP visit was listened to independently by 3 researchers to evaluate the COC dispensing practice. The percentage of CPs who performed a screening for safe use of COCs (i.e., taking of patients’ medical and family history, and measuring of blood pressure) and provided counseling, as well as the quality of the screening and counseling, were evaluated. Results Of the 185 CPs contacted, 41 (22.2%) agreed to participate in the study and finished the study protocol. Only 3 CPs asked the SP a question (1 question asked by each professional), and all of the questions were closed-ended, viz., “do you smoke?” (n = 2) and “what is your age?” (n = 1). None of the CPs measured the patient’s blood pressure. Six CPs provided counseling when dispensing COCs (drug dosing, 5 CPs; possible adverse effects, 2 CPs), and one CP provided counseling regarding both aspects. Conclusion The CPs evaluated did not dispense COC appropriately and could influence in the occurrence of negatives therapeutic outcomes such as adverse effects and treatment failure. PMID:24324584

  7. FDA moves to permit oral contraceptive prescriptions without initial pelvic exam.

    PubMed

    1993-05-28

    The Planned Parenthood Federation of America (PPFA) submitted recommendations to the US Food and Drug Administration's (FDA) Fertility and Maternal Health Drugs Advisory Committee. The PPFA wanted the FDA to remove requirements for a pelvic examination and blood tests before an oral contraceptive (OC) is prescribed. Two representatives of the Family Planning Council of Southeastern Pennsylvania told the FDA advisory committee about the evaluation results of its Smart Start program. 23% of teenagers wanting to use OCs opted to delay the pelvic examination, and 40% opted to delay the blood tests. 83% of these same teenagers were already sexually active. 69% returned for pelvic exams at 3 months. Increased education and counseling over several sessions probably explained why more study participants used condoms and fewer of them became pregnant during the 6-month study. Physicians from the American College of Obstetricians and Gynecologists and the American Fertility Society also attended the committee hearing and supported PPFA's recommendations. The National Women's Health Network wanted to delay the discussion until the committee could also address the sale of OCs over-the-counter. The statements convinced the committee to allow physicians to defer to full physical examination as long as there are no contraindications. This May 20, 1993 approval emphasized the need for physicians to continue taking a complete medical history and conducting other tests that may uncover contraindications (e.g. pregnancy and blood pressure). FDA staff now must write the exact language needed for the OC labeling change to be approved by the FDA commissioner. PMID:12286460

  8. Oral Contraceptive Use and Colorectal Cancer in the Nurses’ Health Study I and II

    PubMed Central

    Charlton, Brittany M.; Wu, Kana; Zhang, Xuehong; Giovannucci, Edward L.; Fuchs, Charles S.; Missmer, Stacey A.; Rosner, Bernard; Hankinson, Susan E.; Willett, Walter C.; Michels, Karin B.

    2015-01-01

    Background It remains unclear if oral contraceptive (OC) use is associated with the incidence of colorectal cancer. Few studies have examined this association by duration of OC use, time since last OC use, and different cancer subsites. Methods Among 88,691 participants of the Nurses’ Health Study I (NHSI) and 93,080 participants of the Nurses’ Health Study II (NHSII), we assessed OC use every 2 years between 1976-2010 and categorized it as ever use, duration of use, and time since last use. We included incident colorectal cancer cases through 2010 (NHSI: age at diagnosis=36-88, N=1,764, NHSII: age at diagnosis=33-64, N=206). Multivariable hazard ratios and 95% confidence intervals [HR (95% CIs)] were estimated using Cox proportional hazards regression models. Results Ever OC use was not associated with colorectal cancer in NHSI [1.01 (0.91, 1.12)] nor NHSII [1.03 (0.69, 1.53)]. In NHSII, when compared to never-users, longer durations (5+ years) of OC use were inversely associated with the risk of colon cancers (test for trend p=0.02) but the number of endpoints was limited. No other colorectal cancer subsites were associated with OC durations or times since last OC use in either cohort. Conclusions In two large prospective cohorts, we found little evidence that OC use may be protective for colorectal cancer, except potentially with longer durations of use among younger women. Impact Our results do not support the previous initial studies that reported an inverse association of recent OC use with colorectal cancer but instead support newer, larger studies demonstrating no such association. PMID:26063479

  9. Oral contraception does not alter single dose saquinavir pharmacokinetics in women

    PubMed Central

    Fröhlich, Margit; Burhenne, Jürgen; Martin-Facklam, Meret; Weiss, Johanna; von Wolff, Michael; Strowitzki, Thomas; Walter-Sack, Ingeborg; Haefeli, Walter E

    2004-01-01

    Aims Women experience more adverse drug reactions (ADR) to antiretroviral therapy than men. This may be attributed to higher plasma concentrations of protease inhibitors due to pharmacokinetic interactions with hormonal preparations. Thus, in the present study we aimed to investigate the influence of oral contraceptives (OC) on the pharmacokinetics of the protease inhibitor saquinavir. Methods Saquinavir was administered in a hard gelatin capsule formulation (Invirase®) to rule out confounding by pharmaceutical aids of the more frequently used soft gelatin capsule. After an overnight fast, eight healthy female participants ingested a single oral dose of 600 mg saquinavir immediately before and after the 19th dose of a combined, low dose OC (0.03 mg ethinylestradiol, 0.075 mg gestodene) in a prospective, fixed sequence study design. The first saquinavir application was scheduled on day 1, 2, or 3 of the individual menstrual cycle. Plasma concentrations of saquinavir and relative concentrations of its M2&M3-hydroxy metabolites were determined by LC/MS/MS for 48 h. Results Intake of OC resulted in a significant decrease in morning serum concentrations (before intake of OC, compared to day 19 of OC therapy) of 17β-estradiol by −23.4 pg ml−1 (57%, 95%CI: −76% to −37.4%); progesterone by −0.25 ng ml−1 (33%, 95%CI: −45.3% to −21.5%); follicle-stimulating hormone by −4.06 U l−1 (82%, 95%CI: −96.5% to −67.7%); and luteinizing hormone by −3.49 U l−1 (74%, 95%CI: −93 to −54.6%). Conversely, sexual hormone binding globulin serum concentrations increased by 83.6 nmol l−1 (205%, 95%CI: 32.2% to 377%). Pharmacokinetic parameters of saquinavir (AUC, Cmax, tmax, t1/2, CLR) were not affected by OC, nor was the relative metabolic ratio of saquinavir/M2&M3-hydroxy saquinavir. Furthermore, there was no association of serum hormone concentrations or MDR1-polymorphisms (C3435T and G2677T) with pharmacokinetic parameters of saquinavir. Conclusions There

  10. Comparison of Postprandial Lipemia between Women who are on Oral Contraceptive Methods and Those who are not

    PubMed Central

    Petto, Jefferson; Vasques, Leila Monique Reis; Pinheiro, Renata Leão; Giesta, Beatriz de Almeida; dos Santos, Alan Carlos Nery; Gomes Neto, Mansueto; Ladeia, Ana Marice Teixeira

    2014-01-01

    Background: Postprandial Lipemia (PPL) is a physiological process that reflects the ability of the body to metabolize lipids. Even though the influence of oral contraceptives (OC) on PPL is not known, it is a known fact that their use increases fasting lipid values. Objective: To compare the PPL between women who are on OC and those who are not. Methods: A prospective analytical study which assessed eutrophic women, aged between 18 and 28 years old, who were irregularly active and with fasting triglycerides ≤150 mg/dL. They were divided into two groups: oral contraceptive group (COG) and non-oral contraceptive group (NCOG). Volunteers were submitted to the PPL test, in which blood samples were collected in time 0 (12-hour fasting) and after the intake of lipids in times 180 and 240 minutes. In order to compare the triglyceride deltas, which reflect PPL, the two-tailed Mann-Whitney test was used for independent samples between fasting collections and 180 minutes (∆1) and between fasting and 240 minutes (∆2). Results: Forty women were assessed and equally divided between groups. In the fasting lipid profile, it was observed that HDL did not present significant differences and that triglycerides in COG were twice as high in comparison to NCOG. Medians of ∆1 and ∆2 presented significant differences in both comparisons (p ≤0.05). Conclusion: The results point out that women who are irregularly active and use OC present more PPL in relation to those who do not use OC, which suggests that in this population, its chronic use increases the risk of heart conditions. PMID:25317941

  11. Normal vaginal microbiology of women of childbearing age in relation to the use of oral contraceptives and vaginal tampons.

    PubMed

    Morris, C A; Morris, D F

    1967-07-01

    The vaginal microbiology of women attending a family planning clinic was found to be unrelated to the use of oral contraceptives and vaginal tampons. Beta haemolytic streptococci isolated from this ;normal' population were compared with those from 1,104 women attending general practitioners complaining of vaginal discharge. There is a caution regarding the indications for antibiotic therapy. Observations were made on the effects of contamination of vaginal swabs with yeasts and beta-haemolytic streptococci from the vulva. The persistent character of the vaginal flora over a six-month period is described. PMID:5602581

  12. Development and optimization of taste-masked orally disintegrating tablets (ODTs) of clindamycin hydrochloride.

    PubMed

    Cantor, Stuart L; Khan, Mansoor A; Gupta, Abhay

    2015-01-01

    The purpose of this research was to develop an orally disintegrating tablet (ODT) dosage form containing taste-masked beads of clindamycin HCl. Several formulation strategies were evaluated and a taste-masked ODT of clindamycin HCl was prepared without the use of a waxy cushioning agent. Clindamycin HCl (ca. 46% w/w) was coated onto microcrystalline cellulose beads (Cellets® 200) followed by the addition of a taste-masking layer of amino methacrylate copolymer, NF (Eudragit EPO® (EPO)) coating suspension. The efficiency of both the drug coating process and the taste-masking polymer coating process, as well as the taste masking ODTs was determined using potency and drug release analysis. Magnesium stearate was found to be advantageous over talc in improving the efficiency of the EPO coating suspension. A response surface methodology using a Box-Behnken design for the tablets revealed compression force and levels of both disintegrant and talc to be the main factors influencing the ODT properties. Blending of talc to the EPO-coated beads was found to be the most critical factor in ensuring that ODTs disintegrate within 30 s. The optimized ODTs formulation also showed negligible (<0.5%) drug release in 1 min using phosphate buffer, pH 6.8 (which is analogous to the residence time and pH in the oral cavity). By carefully adjusting the levels of coating polymers, the amounts of disintegrant and talc, as well as the compression force, robust ODTs can be obtained to improve pediatric and geriatric patient compliance for clindamycin oral dosage forms. PMID:25000481

  13. An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate/dienogest

    PubMed Central

    Fruzzetti, Franca; Trémollieres, Florence; Bitzer, Johannes

    2012-01-01

    Natural estrogens such as estradiol (E2) or its valerate ester (E2V) offer an alternative to ethinyl estradiol (EE). E2-containing combined oral contraceptives (COCs) have demonstrated sufficient ovulation inhibition and acceptable contraceptive efficacy. However, earlier formulations were generally associated with unacceptable bleeding profiles. Two E2V-containing preparations have been approved to date for contraceptive use: E2V/cypro-terone acetate (CPA) (Femilar®; only approved in Finland and only in women >40 years or women aged 35–40 years in whom a COC containing EE is not appropriate) and E2V/dienogest (DNG; Qlaira®/Natazia®). The objective of the current review is to provide an overview of the development of COCs containing natural estrogen, highlighting past issues and challenges faced by earlier formulations, as well as the current status and future directions. The majority of information to date pertains to the development of E2V/DNG. PMID:22468839

  14. Osteoporosis in anorexia nervosa: the influence of peak bone density, bone loss, oral contraceptive use, and exercise.

    PubMed

    Seeman, E; Szmukler, G I; Formica, C; Tsalamandris, C; Mestrovic, R

    1992-12-01

    Anorexia nervosa occurs early in life and predisposes to osteoporosis. Exercise may be protective. We asked: (1) Does failure to attain peak bone density contribute to the deficit in bone density? (2) Does oral contraceptive use protect against osteoporosis? (3) Is any protective effect of exercise confined to weight-bearing sites? Areal bone density (g/cm2) and body composition were measured by dual x-ray absorptiometry in 65 patients with anorexia nervosa and 52 controls. Comparing the 12 patients with primary amenorrhea and the 37 patients with secondary amenorrhea, bone density (mean +/- SEM) at the lumbar spine was 0.88 +/- 0.04 versus 1.06 +/- 0.03 (P = 0.001), respectively. Bone density at the femoral neck was 0.80 +/- 0.04 versus 0.92 +/- 0.03 (P < 0.05), respectively. These values differed before, but not after, adjusting for the respective duration of illness (73.0 +/- 10.3 versus 34.1 +/- 4.8 months, P < 0.001) and fat-free mass (31.6 +/- 1.3 versus 35.4 +/- 0.5 kg, P < 0.01). Bone density at the lumbar spine in the 16 patients with 31.8 +/- 8.3 months of contraceptive exposure was higher than in the 49 patients with no contraceptive exposure (1.14 +/- 0.05 versus 1.02 +/- 0.02 P < 0.02) but was lower than in controls (1.14 +/- 0.05 versus 1.27 +/- 1.02, P < 0.01). No protective effect of contraceptive exposure was detectable at the femoral neck.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:1481732

  15. Formulation and Evaluation of a Novel Matrix-Type Orally Disintegrating Ibuprofen Tablet

    PubMed Central

    Tayebi, Hoda; Mortazavi, Seyed Alireza

    2011-01-01

    Orally disintegrating tablets (ODTs) are capable of turning quickly into a liquid dosage form in contact with the saliva, thus possessing the advantages of both the solid dosage forms particularly stability and liquid dosage forms specially ease of swallowing and pre-gastric absorption of drug. The aim of this study was to prepare a novel matrix-type buccal fast disintegrating ibuprofen tablet formulation using special polymers, water soluble excipients, super-disintegrants and quickly soluble granules. For this purpose different tablet formulations of ibuprofen were prepared. The amount of ibuprofen in each formulation was 100 mg. Eight groups of formulation were prepared (A-H series), accounting for a total number of 45 formulations. Formulations prepared were examined in terms of different physicochemical tests including powder/granule flowability, appearance, thickness, uniformity of weight, hardness, friability and disintegration time. Results of formulation F22a (in series F), was found to be acceptable, making it the chosen formulation for further studies. Then, by adding various flavorants and sweeteners to this formulation, complementary series of formulations, named G and H, were prepared. Following the comparison of their taste with each other through asking 10 volunteers, the most suitable formulation regarding the taste, being formulation F22s, was chosen as the ultimate formulation. This formulation had PVP, ibuprofen and croscarmellose as the intra-granular components and xylitol and saccharin as the extra-granular ingredients. Formulation F22s was found to be acceptable in terms of physicochemical tests conducted, showing quick disintegration within the buccal cavity, appropriate hardness and rather low friability. Hence formulation F22s was selected as the final formulation. PMID:24250378

  16. Evidence-Based Nanoscopic and Molecular Framework for Excipient Functionality in Compressed Orally Disintegrating Tablets

    PubMed Central

    Al-khattawi, Ali; Alyami, Hamad; Townsend, Bill; Ma, Xianghong; Mohammed, Afzal R.

    2014-01-01

    The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mechanisms responsible for powder densification and optimum product functionality. Atomic force microscopy (AFM) contact mode analysis was performed to measure nano-adhesion forces and surface energies between excipient-drug particles (6-10 different particles per each pair). Moreover, surface topography images (100 nm2–10 µm2) and roughness data were acquired from AFM tapping mode. AFM data were related to ODT macro/microscopic properties obtained from SEM, FTIR, XRD, thermal analysis using DSC and TGA, disintegration testing, Heckel and tabletability profiles. The study results showed a good association between the adhesive molecular and physical forces of paired particles and the resultant densification mechanisms responsible for mechanical strength of tablets. MCC micro roughness was 3 times that of D-mannitol which explains the high hardness of MCC ODTs due to mechanical interlocking. Hydrogen bonding between MCC particles could not be established from both AFM and FTIR solid state investigation. On the contrary, D-mannitol produced fragile ODTs due to fragmentation of surface crystallites during compression attained from its weak crystal structure. Furthermore, AFM analysis has shown the presence of extensive micro fibril structures inhabiting nano pores which further supports the use of MCC as a disintegrant. Overall, excipients (and model drugs) showed mechanistic behaviour on the nano/micro scale that could be related to the functionality of materials on the macro scale. PMID:25025427

  17. Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.

    PubMed

    Al-Khattawi, Ali; Alyami, Hamad; Townsend, Bill; Ma, Xianghong; Mohammed, Afzal R

    2014-01-01

    The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mechanisms responsible for powder densification and optimum product functionality. Atomic force microscopy (AFM) contact mode analysis was performed to measure nano-adhesion forces and surface energies between excipient-drug particles (6-10 different particles per each pair). Moreover, surface topography images (100 nm2-10 µm2) and roughness data were acquired from AFM tapping mode. AFM data were related to ODT macro/microscopic properties obtained from SEM, FTIR, XRD, thermal analysis using DSC and TGA, disintegration testing, Heckel and tabletability profiles. The study results showed a good association between the adhesive molecular and physical forces of paired particles and the resultant densification mechanisms responsible for mechanical strength of tablets. MCC micro roughness was 3 times that of D-mannitol which explains the high hardness of MCC ODTs due to mechanical interlocking. Hydrogen bonding between MCC particles could not be established from both AFM and FTIR solid state investigation. On the contrary, D-mannitol produced fragile ODTs due to fragmentation of surface crystallites during compression attained from its weak crystal structure. Furthermore, AFM analysis has shown the presence of extensive micro fibril structures inhabiting nano pores which further supports the use of MCC as a disintegrant. Overall, excipients (and model drugs) showed mechanistic behaviour on the nano/micro scale that could be related to the functionality of materials on the macro scale. PMID:25025427

  18. Depo-Provera in adolescents: effects of early second injection or prior oral contraception.

    PubMed

    Harel, Z; Biro, F M; Kollar, L M

    1995-05-01

    The capability of an early second injection or prior use of oral contraceptives (OCs) to improve satisfaction and long-term continuation of Depo-Provera in adolescents was investigated in a clinical trial involving 78 females 12-20 years of age (average, 15.9 years) recruited from a hospital-based adolescent health clinic. 36 subjects received injection of 150 mg of Depo-Provera every three months (Group 1), 27 received the second injection after only six weeks (Group 2), and 15 switched directly from OCs to the standard Depo-Provera regimen (Group 3). There was no difference between Groups 1 and 2 in terms of duration or frequency of menstrual bleeding; however, prior OC users experienced a significant reduction in the duration and intensity of bleeding in the first six months of Depo-Provera use (when estrogen was still present in the women's systems). Overall, 64% of study subjects reported less dysmenorrhea while on Depo-Provera. A slightly greater change in body mass index was observed among girls in Group 2 than in Groups 1 and 3; moreover, 70% of those in the early injection group reported increased appetite and weight gain compared to 39% of those on the standard schedule. The most commonly reported side effects included initial pain and soreness at the injection site (27%), decreased libido (56%), mood changes (31%), depression (26%), frequent headache (25%), fatigue (24%), and increase in acne (15%); there were no significant differences by group. 17 adolescents (22%) discontinued Depo-Provera, generally after two injections and due to bleeding irregularities or weight gain. 87% of adolescents who were prior OC users, 52% of those on the regular schedule, and 39% of those who received an early injection stated they were very satisfied with Depo-Provera. These findings indicate that early second Depo-Provera injection offers no advantages; use of OCs immediately prior to Depo-Provera should be further investigated, however, given its potential to minimize

  19. Low dosage monophasic oral contraceptive use and intermittent exercise performance and metabolism in humans.

    PubMed

    Lynch, N J; De Vito, G; Nimmo, M A

    2001-04-01

    Nine untrained women using low dosage monophasic oral contraceptives (OC) performed an intermittent treadmill test on two different occasions within one pill-cycle to determine the effect of OC on performance and some commonly used metabolic markers. The first test was performed after 5-8 days of resuming the OC agents after menstrual bleeding while the other test was performed after 19-21 days. Performance time on the final exhausting run of six intermittent high intensity 20 s runs was no different between trials [mean days 5-8: 22.3 (SEM 1.2) s vs days 19-21: 22.7 (SEM 1.1) s]. There was no difference in heart rate [peak heart rate days 5-8: 183 (SEM 3) beats.min-1 vs days 19-21: 186 (SEM 2) beats.min-1], oxygen consumption during any run [run 5 of days 5-8: 1,392 (SEM 51) ml.min-1 vs run 5 of days 19-21: 1,494 (SEM 3) ml.min-1] or in any of the metabolic variables measured at any time in venous blood [peak blood lactate concentration days 5-8: 8.4 (SEM 0.3) mmol.l-1 vs days 19-21: 8.1 (SEM 0.5) mmol.l-1; peak blood glycerol concentration days 5-8: 0.39 (SEM 0.02) mmol.l-1 vs days 19-21: 0.38 (SEM 0.02) mmol.l-1; resting free fatty acids concentration days 5-8: 0.25 (SEM 0.05) mmol.l-1 vs days 19-21: 0.29 (SEM 0.07) mmol.l-1; peak blood glucose concentration days 5-8: 6.7 (SEM 0.5) mmol.l-1 vs days 19-21: 6.6 (SEM 0.2) mmol.l-1; peak capillary blood ammonia concentration days 5-8: 139 (SEM 18.3) mumol.l-1 vs days 19-21: 170 (SEM 18.0) mumol.l-1]. These results suggest neither intermittent high intensity exercise performance nor energy metabolism change between days 5-8 and days 19-21 of a low dosage monophasic OC pill during one pill-cycle. PMID:11374113

  20. Oral contraception following abortion: A systematic review and meta-analysis.

    PubMed

    Che, Yan; Liu, Xiaoting; Zhang, Bin; Cheng, Linan

    2016-07-01

    Oral contraceptives (OCs) following induced abortion offer a reliable method to avoid repeated abortion. However, limited data exist supporting the effective use of OCs postabortion. We conducted this systematic review and meta-analysis in the present study reported immediate administration of OCs or combined OCs postabortion may reduce vaginal bleeding time and amount, shorten the menstruation recovery period, increase endometrial thickness 2 to 3 weeks after abortion, and reduce the risk of complications and unintended pregnancies.A total of 8 major authorized Chinese and English databases were screened from January 1960 to November 2014. Randomized controlled trials in which patients had undergone medical or surgical abortions were included. Chinese studies that met the inclusion criteria were divided into 3 groups: administration of OC postmedical abortion (group I; n = 1712), administration of OC postsurgical abortion (group II; n = 8788), and administration of OC in combination with traditional Chinese medicine postsurgical abortion (group III; n = 19,707).In total, 119 of 6160 publications were included in this analysis. Significant difference was observed in group I for vaginal bleeding time (P = 0.0001), the amount of vaginal bleeding (P = 0.03), and menstruation recovery period (P < 0.00001) compared with the control groups. Group II demonstrated a significant difference in vaginal bleeding time (P < 0.00001), the amount of vaginal bleeding (P = 0.0002), menstruation recovery period (P < 0.00001), and endometrial thickness at 2 (P = 0.003) and 3 (P < 0.00001) weeks postabortion compared with the control group. Similarly, a significant difference was observed in group III for reducing vaginal bleeding time (P < 0.00001) and the amount of vaginal bleeding (P < 0.00001), shortening the menstruation recovery period (P < 0.00001), and increasing endometrial thickness 2 and 3 weeks after surgical abortion (P < 0.00001, all

  1. [Improving oral contraception compliance. The "ringing card": memory aid or new ritual?].

    PubMed

    Lachowsky, M; Levy-Toledano, R

    2000-04-01

    compliance card is an easy and reliable device that improves the compliance of women using oral contraceptives by helping them to establish a ritual. PMID:10859894

  2. Correcting oral contraceptive pharmacokinetic alterations due to obesity. A randomized controlled trial

    PubMed Central

    Edelman, Alison B; Cherala, Ganesh; Munar, Myrna Y.; McInnis, Martha; Stanczyk, Frank Z.; Jensen, Jeffrey T

    2014-01-01

    Objective To determine if increasing the hormone dose or eliminating the hormone-free interval improves key pharmacokinetic (PK) alterations caused by obesity during oral contraceptive (OC) use. Study design Obese (BMI ≥ 30 kg/m2), ovulatory, otherwise healthy, women received an OC containing 20 mcg ethinyl estradiol (EE)/100 mcg levonorgestrel (LNG) dosed cyclically (21 days active pills with 7-day placebo week) for two cycles and then were randomized for two additional cycles to: Continuous Cycling [CC, a dose neutral arm using the same OC with no hormone-free interval] or Increased Dose [ID, a dose escalation arm using an OC containing 30 mcg EE/150 mcg LNG cyclically]. During Cycle 2, 3, and 4, outpatient visits were performed to assess maximum serum concentration (Cmax), area under the curve (AUC0-∞), and time to steady state as well as pharmacodynamics. These key PK parameters were calculated and compared within groups between baseline and treatment cycles. Results A total of 31 women enrolled and completed the study (CC group n = 16; ID group n = 15). Demographics were similar between groups [mean BMI: CC 38kg/m2 (SD 5.1), ID 41kg/m2 (SD 7.6)]. At baseline, the key LNG PK parameters were no different between groups; average time to reach steady-state was 12 days in both groups; Cmax were CC: 3.82 ± 1.28 ng/mL and ID: 3.13 ± 0.87 ng/mL; and AUC0-∞ were CC: 267 ± 115 hr*ng/mL and ID: 199±75 hr*ng/mL. Following randomization, the CC group maintained steady-state serum levels whereas the ID group had a significantly higher Cmax (p< 0.001) but again required 12 days to achieve steady-state. However, AUC was not significantly different between CC (412 ± 255 hr*ng/mL) and ID (283 ± 130 hr*ng/mL). Forty-five percent (14/31) of the study population had evidence of an active follicle-like structure prior to randomization and afterwards this decreased to 9% (3/31). Conclusion Both increasing the OC dose and continuous dosing appear to counteract the impact

  3. Effect of granule properties on rough mouth feel and palatability of orally disintegrating tablets.

    PubMed

    Kimura, Shin-Ichiro; Uchida, Shinya; Kanada, Ken; Namiki, Noriyuki

    2015-04-30

    In this study, we evaluated the palatability of orally disintegrating tablets (ODTs) containing core granules with different particle sizes, coating, and types of materials using visual analog scales (VAS). Tableting the core granules into ODTs reduced rough mouth feel and improved overall palatability compared to the ingestion of core granules alone. Moreover, the evaluation performed immediately after spitting out ODTs demonstrated differences in rough mouth feel between ODTs containing placebo and core granules. Rough mouth feel was found to be significantly more intense with core granules with particle sizes ≥ 200 μm. Since ODTs may contain taste-masked particles, palatability of ODTs containing coated core granules was also evaluated. Although coating with polymers impairs palatability, it was improved by coating the outer layer with d-mannitol. The effects on palatability of materials constituting core granules were also evaluated, with reduced rough mouth feel observed with core granules composed of water-soluble additives. Based on these data, receiver operating characteristic analysis was performed to determine the threshold VAS scores at which the subjects felt roughness and discomfort. In addition, the threshold particle size of the core granule contained within the ODT required for feeling roughness was determined to be 244 μm. This study elucidated the effect of the properties of masking particles on the rough mouth feel and palatability of ODTs. PMID:25681720

  4. Bioequivalence assay between orally disintegrating and conventional tablet formulations in healthy volunteers.

    PubMed

    Armando, Yara Popst; Schramm, Simone Grigoleto; Silva, Marina de Freitas; Kano, Eunice Kazue; Koono, Eunice Emiko Mori; Porta, Valentina; Serra, Cristina Helena dos Reis

    2009-01-21

    The purpose of this study was to evaluate bioequivalence of two commercial 8 mg tablet formulations of ondansetrona available in the Brazilian market. In this study, a simple, rapid, sensitive and selective liquid chromatography-tandem mass spectrometry method is described for the determination of ondansetron in human plasma samples. The method was validated over a concentration range of 2.5-60 ng/ml and used in a bioequivalence trial between orally disintegrating and conventional tablet ondansetron formulations, to assess its usefulness in this kind of study. Vonau flash (Biolab Sanus Farmacêutica, Brazil, as test formulations) and Zofran (GlaxoSmithKline, Brazil, as reference formulation) were evaluated following a single 8 mg dose to 23 healthy volunteers of both genders. The dose was administered after an overnight fast according to a two-way crossover design. Bioequivalence between the products was determinated by calculating 90% confidence interval (90% CI) for the ratio of C(max), AUC(0-t) and AUC(0-infinity) values for the test and reference products, using logarithmically transformed data. The 90% confidence interval for the ratio of C(max) (87.5-103.8%), AUC(0-t) (89.3-107.2%) and AUC(0-infinity) (89.7-106.0%) values for the test and reference products is within the 80-125% interval, proposed by FDA, EMEA and ANVISA. It was concluded that two ondansetron formulations are bioequivalent in their rate and extent of absorption. PMID:18848869

  5. Increased dissolution rate and oral bioavailability of hydrophobic drug glyburide tablets produced using supercritical CO₂ silica dispersion technology.

    PubMed

    Guan, Jibin; Han, Jihong; Zhang, Dong; Chu, Chunxia; Liu, Hongzhuo; Sun, Jin; He, Zhonggui; Zhang, Tianhong

    2014-04-01

    The aim of this study was to design a silica-supported solid dispersion of a water-insoluble drug, glyburide, to increase its dissolution rate and oral absorption using supercritical fluid (SCF) technology. DSC and PXRD results indicated that the encapsulated drug in the optimal solid dispersion was in an amorphous state and the product was stable for 6 months. Glyburide was adsorbed onto the porous silica, as confirmed by the SEM images and BET analysis. Furthermore, FT-IR spectroscopy confirmed that there was no change in the chemical structure of glyburide after the application of SCF. The glyburide silica-based dispersion could also be compressed into tablet form. In vitro drug release analysis of the silica solid dispersion tablets demonstrated faster release of glyburide compared with the commercial micronized tablet. In an in vivo test, the AUC of the tablets composed of the new glyburide silica-based solid dispersion was 2.01 times greater than that of the commercial micronized glyburide tablets. In conclusion, SCF technology presents a promising approach to prepare silica-based solid dispersions of hydrophobic drugs because of its ability to increase their release and oral bioavailability. PMID:24184803

  6. Mucoadhesive elementary osmotic pump tablets of trimetazidine for controlled drug delivery and reduced variability in oral bioavailability.

    PubMed

    Alam, Naushad; Beg, Sarwar; Rizwan, Mohammad; Ahmad, Akifa; Ahmad, Farhan Jalees; Ali, Asgar; Aqil, Mohammad

    2015-04-01

    The objectives of this work was preparation and evaluation of the mucoadhesive elementary osmotic pump tablets of trimetazidine hydrochloride to achieve desired controlled release action and augmentation of oral drug absorption. The drug-loaded core tablets were prepared employing the suitable tableting excipients and coated with polymeric blend of ethyl cellulose and hydroxypropyl methylethylcellulose E5 (4:1). The prepared tablets were characterized for various quality control tests and in vitro drug release. Evaluation of drug release kinetics through model fitting suggested the Fickian mechanism of drug release, which was regulated by osmosis and diffusion as the predominant mechanism. Evaluation of mucoadhesion property using texture analyzer suggested good mucoadhesion potential of the developed osmotic systems. Solid state characterization using Fourier-transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffraction spectroscopy confirmed the absence of any physiochemical incompatibilities between drug and excipients. Scanning electron microscopy analysis showed the smooth surface appearance of the coated tablets with intact polymeric membrane without any fracture. In vivo pharmacokinetic studies in rabbits revealed 3.01-fold enhancement in the oral bioavailability vis-à-vis the marketed formulation (Vastarel MR®). These studies successfully demonstrate the bioavailability enhancement potential of the mucoadhesive elementary osmotic pumps as novel therapeutic systems for other drugs too. PMID:24669975

  7. [Frequency and reasons for switching/stopping use of oral contraceptives. Results of the German Cohort Study on Women Health].

    PubMed

    Heinemann, L A; Thiel, C; Assmann, A; Möhner, S

    2001-10-01

    Frequency and reasons for switching/stopping use of oral contraceptives. Results of the German Cohort Study on Women Health. Use of oral contraceptives is the safest and most commonly used method of contraception. The frequency of use underscores the importance of research on benefits, risks, and acceptability of long-term use. - An interim analysis of the German Cohort Study on Women's Health (aged 15-65 years) was performed to analyse frequency and reason of switching or stop of OC-use. We got for this analysis over 10 000 women with almost 100 000 years of observation from first to last (or current) OC use. - The prevalence of ever use of OCs was 85.5 % in our cohort. Switching or stop of OC use was observed in 93 % of the women. The frequency of switching increased with age and duration of use. Social parameter such as education, employment status, and living in the old or the new Federal States were not materially associated with the frequency of switching or stopping OC use. Satisfaction with general health, psychic stability, and sexual life was slightly associated with the frequency of switching: The better satisfaction the lower frequency of switching, but the sequence of cause and consequence is unclear. The most frequent categories of reasons for switching were observed side effects and personal reasons. Desire to get pregnant was the number one single reason, followed by headache/migraine, and bleeding problems. The frequency of more than 50 single reasons is listed. - The frequency and the knowledge of reason for switching or stopping OC use underlines the need for a good collaboration between physician and treated woman. However, also research on long-term compliance is required and the development of OCs with even less side effects. PMID:11753811

  8. Comparison of efficacy of metformin and oral contraceptive combination of ethinyl estradiol and drospirenone in polycystic ovary syndrome

    PubMed Central

    Suvarna, Yashasvi; Maity, Nivedita; Kalra, Pramila; Shivamurthy, MC

    2016-01-01

    Objective The 2013 Endocrine Society guidelines state that hormonal contraceptives should be used for treating both menstrual irregularity and hirsutism in patients with polycystic ovary syndrome (PCOS). Metformin should be reserved for the treatment of women presenting with only menstrual irregularity because it has limited benefits in treating hyperandrogenism associated with PCOS. A high prevalence of insulin resistance is noted among the South Asians, and these guidelines may not hold good for this population. Thus, this study was conducted to investigate and compare the effects of metformin and an oral contraceptive containing drospirenone on menstrual pattern, body mass index, serum testosterone levels, and dehydroepiandrosterone sulfate (DHEAS) levels at baseline to 6 months of therapy in the treatment groups. Material and Methods This was a prospective observational study that was conducted over a year in patients visiting the Endocrinology outpatient department at a tertiary care center in a south Indian city. Forty-six subjects diagnosed with PCOS as per the Rotterdam criteria were included. They received either metformin twice daily or an oral contraceptive containing drospirenone once daily as a monthly regimen for 6 months. Results Metformin regularized menstrual cycles in 72% of patients who were followed up at 6 months. No significant difference was observed between the two treatment groups with respect to decreasing the body mass index, serum testosterone levels, and DHEAS levels (p=0.40, p=0.65, and p=0.22, respectively). Conclusion Metformin is effective in regularizing menstrual cycles, decreasing body mass index, and treating hyperandrogenism in Indian women diagnosed with PCOS. PMID:27026772

  9. Comparative safety, efficacy, and cycle control of Lunelle monthly contraceptive injection (medroxyprogesterone acetate and estradiol cypionate injectable suspension) and Ortho-Novum 7/7/7 oral contraceptive (norethindrone/ethinyl estradiol triphasic). Lunelle Study Group.

    PubMed

    Kaunitz, A M; Garceau, R J; Cromie, M A

    1999-10-01

    An open-label, nonrandomized, parallel, controlled study compared the efficacy, safety, and cycle control of a new monthly injectable contraceptive containing 25 mg of medroxyprogesterone acetate (MPA) and 5 mg of estradiol cypionate (E2C) (MPA/E2C) (Lunelle Monthly Contraceptive Injection) with that of a norethindrone 0.5, 0.75, 1.0 mg/0.035 mg ethinyl estradiol (NET/EE) triphasic oral contraceptive (Ortho-Novum 7/7/7). At study enrollment, women chose either the injections or the oral contraceptive. A higher proportion of women in the NET/EE group (65.1%) than in the MPA/E2C group (48.7%) had used hormonal contraception during the month before the study (p < 0.01). Overall, 55.5% (434/782) of MPA/E2C users and 67.6% (217/321) of NET/EE users completed the 60-week trial. One-year contraceptive efficacy (13 cycles of 28 days) for MPA/E2C and NET/EE was based on 8008 and 3434 woman-cycles of use, respectively. During the first year, one pregnancy occurred in an NET/EE user for a life table rate of 0.3; no pregnancies occurred in users of MPA/E2C. One additional pregnancy in the NET/EE group occurred during the 15th treatment cycle. After the first treatment cycle, women in both groups experienced regular menses, with an average cycle length of 28 days in MPA/E2C users and 27 days in NET/EE users. Although MPA/E2C users were more likely to experience bleeding irregularities, only 2.5% (19/775) cited metrorrhagia as a reason for discontinuing treatment. The adverse events reported in both treatment groups are consistent with those expected with the use of combined hormonal contraceptives. Overall, the results of this first Phase III US clinical trial of MPA/E2C confirm this method's high contraceptive efficacy and safety, as shown in previous studies by the World Health Organization. These results suggest that a monthly combination injectable would represent a welcome new contraceptive option for women in the US. PMID:10640164

  10. Contraception today.

    PubMed

    Benagiano, Giuseppe; Bastianelli, Carlo; Farris, Manuela

    2006-12-01

    Modern contraceptive methods represent more than a technical advance: they are the instrument of a true social revolution-the "first reproductive revolution" in the history of humanity, an achievement of the second part of the 20th century, when modern, effective methods became available. Today a great diversity of techniques have been made available and-thanks to them, fertility rates have decreased from 5.1 in 1950 to 3.7 in 1990. As a consequence, the growth of human population that had more than tripled, from 1.8 to more than 6 billion in just one century, is today being brought under control. At the turn of the millennium, all over the world, more than 600 million married women are using contraception, with nearly 500 million in developing countries. Among married women, contraceptive use rose in all but two developing countries surveyed more than once since 1990. Among unmarried, sexually active women, it grew in 21 of 25 countries recently surveyed. Hormonal contraception, the best known method, first made available as a daily pill, can today be administered through seven different routes: intramuscularly, intranasally, intrauterus, intravaginally, orally, subcutaneously, and transdermally. In the field of oral contraception, new strategies include further dose reduction, the synthesis of new active molecules, and new administration schedules. A new minipill (progestin-only preparation) containing desogestrel has been recently marketed in a number of countries and is capable of consistently inhibiting ovulation in most women. New contraceptive rings to be inserted in the vagina offer a novel approach by providing a sustained release of steroids and low failure rates. The transdermal route for delivering contraceptive steroids is now established via a contraceptive patch, a spray, or a gel. The intramuscular route has also seen new products with the marketing of improved monthly injectable preparations containing an estrogen and a progestin. After the first

  11. [Contraception news].

    PubMed

    Vincent-Rohfritsch, A; Pernin, E; Chabbert-Buffet, N

    2012-04-01

    Although contraception is widely available in France, contraceptive failure remains high. However a number of modifications in contraceptive methods have been developed and should help reduce contraceptive failure. Among those, information and improvement of access to contraception are very important. Recent advances in contraceptive practice have also contributed to improve clinical tolerance and subsequently compliance. Finally, emergency contraception has evolved as well. PMID:22079029

  12. Emergency contraception with a Copper IUD or oral levonorgestrel: an observational study of 1-year pregnancy rates

    PubMed Central

    Turok, David K.; Jacobson, Janet C.; Dermish, Amna I.; Simonsen, Sara E.; Gurtcheff, Shawn; McFadden, Molly; Murphy, Patricia A.

    2014-01-01

    Objective We investigated the one-year pregnancy rates for emergency contraception (EC) users who selected the copper T380 IUD or oral levonorgestrel (LNG) for EC. Study Design This prospective study followed women for 1 year after choosing either the copper T380 IUD or oral LNG for EC. The study was powered to detect a 6% difference in pregnancy rates within the year after presenting for EC. Results Of the 542 women who presented for EC, agreed to participate in the trial, and meet inclusion criteria, 215 (40%) chose the copper IUD and 327 (60%) chose oral LNG. In the IUD group, 127 (59%) were nulligravid. IUD insertion failed in 42 women (19%). The 1-year follow-up rate was 443/542 (82%); 64% of IUD users contacted at 1 year still had their IUDs in place. The 1-year cumulative pregnancy rate in women choosing the IUD was 6.5% vs. 12.2% in those choosing oral LNG (HR= 0.53, 95% CI: 0.29–0.97, p=0.041). By type of EC method actually received, corresponding values were 5.2% for copper IUD users vs. 12.3% for oral LNG users, HR 0.42 (95% CI: 0.20–0.85, p= 0.017). A multivariable logistic regression model controlling for demographic variables demonstrates that women who chose the IUD for EC had fewer pregnancies in the following year than those who chose oral LNG (HR 0.50, 95% CI: 0.26–0.96, p=0.037). Conclusion One year after presenting for EC women choosing the copper IUD for EC were half as likely to have a pregnancy compared to those choosing oral LNG. PMID:24332433

  13. Oral liquid L-thyroxine (L-t4) may be better absorbed compared to L-T4 tablets following bariatric surgery.

    PubMed

    Pirola, Ilenia; Formenti, Anna M; Gandossi, Elena; Mittempergher, Francesco; Casella, Claudio; Agosti, Barbara; Cappelli, Carlo

    2013-09-01

    Drug malabsorption is a potential concern after bariatric surgery. We present four case reports of hypothyroid patients who were well replaced with thyroxine tablets to euthyroid thyrotropin (TSH) levels prior to Roux-en-Y gastric bypass surgery. These patients developed elevated TSH levels after the surgery, the TSH responded reversibly to switching from treatment with oral tablets to a liquid formulation. PMID:23824980

  14. Formulation and In-vitro Evaluation of Orally Disintegrating Tablets of Olanzapine-2-Hydroxypropyl-β-Cyclodextrin Inclusion Complex

    PubMed Central

    Ajit Shankarrao, Kulkarni; Dhairysheel Mahadeo, Ghadge; Pankaj Balavantrao, Kokate

    2010-01-01

    The aim of this study was to design orally disintegrating tablets of Olanzapine and to complex Olanzapine with 2-hydroxypropyl-β- cyclodextrin with special emphasis on disintegration and dissolution studies. Phase solubility studies demonstrated the formation of 1:1 molar inclusion complex by kneading method. Tablets were prepared by using superdisintegrants namely, sodium starch glycolate, croscarmellose sodium, crospovidone, tulsion 339, and indion 414. Complex was characterized using infrared spectroscopy, drug content estimation, saturated solubility study, diffrerential scanning calorimetry and X-ray diffractometry. 5% w/w croscarmellose sodium showed the minimum disintegration time 39 ± 1.76 sec and in-vitro drug release 99.19 ± 0.18% within 6 min. In general, solubility of Olanzapine can be improved by complexing with 2-hydroxypropyl-β- cyclodextrin. Croscarmellose sodium can be used for faster disintegration of tablets. PMID:24381598

  15. Efficacy and tolerability of a monophasic combined oral contraceptive containing nomegestrol acetate and 17β-oestradiol in a 24/4 regimen, in comparison to an oral contraceptive containing ethinylestradiol and drospirenone in a 21/7 regimen

    PubMed Central

    Mansour, Diana; Verhoeven, Carole; Sommer, Werner; Weisberg, Edith; Taneepanichskul, Surasak; Melis, Gian Benedetto; Sundström-Poromaa, Inger; Korver, Tjeerd

    2011-01-01

    Objectives The primary objective was to assess the efficacy, cycle control and tolerability of a monophasic combined oral contraceptive (COC) containing nomegestrol acetate (NOMAC) and 17β-oestradiol (E2). Effects on acne were evaluated as a secondary objective. Results were compared to those of a COC containing drospirenone (DRSP) and ethinylestradiol (EE). Methods Women (aged 18-50 years) were randomised to receive NOMAC/E2 (2.5 mg/1.5 mg) in a 24/4-day regimen (n = 1591) or DRSP/EE (3 mg/30 μg) in a 21/7-day regimen (n = 535) for 13 cycles. Results Estimated Pearl Indices for NOMAC/E2 and DRSP/EE were 0.38 and 0.81 in women aged ≤ 35 years and 0.31 and 0.66 for all women (18–50 years), respectively. Scheduled withdrawal bleedings were shorter and lighter among users of NOMAC/E2 and were sometimes absent altogether. Intracyclic bleeding/spotting was infrequent in both groups, and decreased over time. Type and frequency of adverse events were similar to those typically reported for COCs. Conclusions These data show that NOMAC/E2 provides high contraceptive efficacy with acceptable cycle control as well as an overall adverse event profile similar to that of DRSP/EE. PMID:21995590

  16. Contraception and Diabetes.

    PubMed

    Afsana, Faria

    2016-09-01

    Contraception for women with diabetes mellitus is an important issue mainly as the pregnancy outcome depends on glycaemic control before conception among women with diabetes. Type of diabetes as type 1 or type 2 Diabetes, women with history of gestational diabetes and breast feeding diabetic mothers may be a consideration in selecting a contraceptive .On the other hand presence of diabetic complications is a significant determinant. Different methods of contraception as oral, injectable, implant, intrauterine devices are available. Patient\\'s choice and health issues both should be considered while prescribing a contraceptive to a woman with diabetes. Emergency contraception is sometimes required in situations where there is chance of contraceptive failure. This review article highlights different contraceptive methods, their use and limitations and will guide to make a rational choice for a woman with diabetes. PMID:27582166

  17. Intra-gastric performance and bioavailability study of a new per-oral bioadhesive Verapamil HCl matrix tablet in dogs.

    PubMed

    Yassin, Alaa Eldeen B; Alkhaled, F; al-Suwayeh, S; Elkheshen, S

    2003-09-01

    In a previous study, we developed a per-oral extended--release bioadhesive matrix tablet for verapamil HCl (VP). The system combined both strong bioadhesion and sustained release properties in vitro. The purpose of this study is to evaluate the in vivo performance of the prepared bioadhesive tablets (B). The conduction of a periodic X-ray imaging of the abdomen of beagle dogs, after administration of B containing 12% barium sulfate, was used to evaluate the intra-gastric performance. The VP concentrations in blood samples taken at specified times after oral administration of B to fasted beagle dogs were determined and compared with those obtained after administration of a commercial sustained release VP tablets (Manidon 120 R). The X-ray images showed that bioadhesive tablets remained almost at the same place in the stomach for at least 6 hours while it disappeared after 1 hour in case of the control tablets. No statistical difference was seen between the Cmax, tmax, AUC, t1/2, and MRT for B compared to Manidon. The Cmax was found to be 51.4 +/- 15.5 and 48.6 +/- 17.9 (ng/ml) for Manidon and B, respectively and the corresponding tmax were 7.0 +/- 1.9 and 6.0 +/- 0, respectively. The AUCO-. for Manidon and B were 949.84 +/- 245.11 and 722.92 +/- 144.42 ng.h/ml, respectively. So, the prepared B tablets can be considered bioequivalent to the commercial Manidon Retard product. PMID:14677272

  18. Per-oral extended-release bioadhesive tablet formulation of verapamil HCl.

    PubMed

    Elkheshen, Seham; Yassin, Alaa Eldeen B; Alkhaled, Fayza

    2003-06-01

    The objective of this study was to formulate a hydrogel-forming bioadhesive drug delivery system for oral administration of verapamil HCl (VP). This system is a non-distintegrating gastro-retentive tablet to allow continuous slow release of VP in the stomach medium where it is more soluble. Different formulate of VP tablets were prepared by compression using various proportions of hydroxypropyl cellulose (HPC) and carbopol 934p (CP). The effect of polymer concentration on the release profile, water uptake and in vitro bioadhesion was studied. Five formulae (F3-F7) exhibited slow release profiles. Formulations F6 (40% HPC and 30% CP) and F7 (40% HPC and 40% CP) had the slowest. They showed 63.6 and 52.2% drug release, respectively, after 12 hours. The kinetic analysis of the release data demonstrated that the bigbest linearity were achieved when data fitted in Higuchi equation rather than zero or first order equations. They had n values close to 0.5 that confirming their Higuchi diffusion. F3 showed the highest swelling index (101.2%), however, the detachment force was intermediate (1.427 N/cm2). Formulae (F4-F7) showed relatively strong in-vitro bioadhesive force. They had detachment forces higher than 1 N/cm2. In general, a delay in drug release and an increase in the in-vitro bioadhesion was seen with the increase in both polymer concentrations. The in vitro data revealed that Formulae F4-F7 served the dual purpose of bioadhesion and sustained release. PMID:14526657

  19. [The statement of Polish Gynecological Society experts on oral use of contraceptive 75 microg desogestrel minipill in different clinical cases--state of art in 2008].

    PubMed

    Debski, Romuald; Kotarski, Jan; Paszkowski, Tomasz; Pawelczyk, Leszek; Skrzypulec, Violetta; Tomaszewski, Jacek

    2009-01-01

    Recent epidemiologic studies indicate that use of combined oral contraception is associated with a increase in the incidence of cardiovascular disease (venous thromboembolism, pulmonary embolism, myocardial infarction and stroke). The risk of cardiovascular disease is strongly related to estrogen dose, progestogen type and other factors for example thrombogenic mutations and cigarette smoking among female over age 35. The progestogen only contraception is safe alternative to combined hormonal contraception. Progestogen only pill (POP) has different levels of action (local and/or central) which may vary from one drug to another. As for the cardiovascular disease risk, progestogens are not considered to be risk factors. Desogestrel containing POP is advised in the following cases: bad tolerance of exogenous oestrogens; in order to counteract an endogenous hyperoestrogenosis; medical, metabolic or cardiovascular contraindications to estroprogestogen contraception. Lastly, POP should be used as a prime contraception in some particular situations (breast feeding, endometriosis, adenomyosis, cigarette smoking, contraception for older women). These recommendations present the actual system of care in that population of women in Poland. PMID:19323063

  20. Effect of a high-fat meal on the pharmacokinetics of 300-milligram posaconazole in a solid oral tablet formulation.

    PubMed

    Kersemaekers, Wendy M; Dogterom, Peter; Xu, Jialin; Marcantonio, Eugene E; de Greef, Rik; Waskin, Hetty; van Iersel, Marlou L P S

    2015-01-01

    Posaconazole in oral suspension must be taken multiple times a day with food (preferably a high-fat meal) to ensure adequate exposure among patients. We evaluated the effect of food on the bioavailability of a new delayed-release tablet formulation of posaconazole at the proposed clinical dose of 300 mg once daily in a randomized, open-label, single-dose, two-period crossover study with 18 healthy volunteers. When a single 300-mg dose of posaconazole in tablet form (3 tablets × 100 mg) was administered with a high-fat meal, the posaconazole area under the concentration-time curve from 0 to 72 h (AUC0-72) and maximum concentration in plasma (Cmax) increased 51% and 16%, respectively, compared to those after administration in the fasted state. The median time to Cmax (Tmax) shifted from 5 h in the fasted state to 6 h under fed conditions. No serious adverse events were reported, and no subject discontinued the study due to an adverse event. Six of the 18 subjects reported at least one clinical adverse event; all of these events were mild and short lasting. The results of this study demonstrate that a high-fat meal only modestly increases the mean posaconazole exposure (AUC), ∼1.5-fold, after administration of posaconazole tablets, in contrast to the 4-fold increase in AUC observed previously for a posaconazole oral suspension given with a high-fat meal. PMID:25824210

  1. A Pharmacokinetic Study Comparing Eslicarbazepine Acetate Administered Orally as a Crushed or Intact Tablet in Healthy Volunteers.

    PubMed

    Sunkaraneni, Soujanya; Kharidia, Jahnavi; Schutz, Ralph; Blum, David; Cheng, Hailong

    2016-07-01

    The relative bioequivalence of crushed versus intact eslicarbazepine acetate (ESL) tablets (800 mg) administered orally in healthy adults was evaluated in an open-label, randomized, 2-period crossover study with a 5-day washout between treatments. Sample blood levels of eslicarbazepine and (R)-licarbazepine were determined; pharmacokinetic parameters were derived for eslicarbazepine. Bioequivalence was established if the 90% confidence intervals (CIs) for the geometric mean treatment ratios of eslicarbazepine AUC(0-∞) and Cmax were within the prespecified 80%-125% range. Twenty-seven subjects in the intent-to-treat population (n = 28) completed both treatment periods. Eslicarbazepine exposure measures were similar for crushed versus intact ESL tablets: average Cmax , 11 700 versus 11 500 ng/mL; AUC(0-∞) , 225 000 versus 234 000 ng·h/mL; AUC(0-last) , 222 000 versus 231 000 ng·h/mL, respectively. Geometric least squares mean ratios (90%CIs) comparing eslicarbazepine exposure measures were within the 80%-125% range (Cmax , 102.63% [97.07%-108.51%]; AUC(0-∞) , 96.72% [94.36%-99.13%]; AUC0-last , 96.69% [94.24%-99.21%]). In conclusion, ESL administered orally as a crushed tablet sprinkled on applesauce, or intact were bioequivalent in healthy subjects. Eslicarbazepine bioavailability was not significantly altered by crushing, indicating that ESL tablets can be administered intact or crushed. PMID:27249205

  2. A prospective study of a monophasic oral contraceptive containing 30 mcg ethinyl oestradiol and 150 mcg desogestrel (Marvelon).

    PubMed

    Ismail, M T

    1994-06-01

    Marvelon, a monophasic oral contraceptive (OC) containing 30 mcg of ethinyl estradiol and 150 mcg of desogestrel, has been available to Malaysian women through the national family planning program since 1982. To assess the safety, effectiveness, and side effects associated with this OC, 247 women who requested the pill were enrolled in a multicenter prospective study that included follow-up after the first, third, and sixth cycles of use. 81% of participants had never used any form of contraception before Marvelon. 194 women (79%) completed the 6-month study. There were no pregnancies recorded. Although women reported a slightly increased incidence of nausea, breast tenderness, and headache in the first treatment cycle, these side effects had abated by the end of the third cycle. After six cycles, mean body weight had decreased by an average of 0.4 kg. Both systolic and diastolic blood pressure were unaffected. An unexpected finding was a decrease in the severity of acne with continuous use of Marvelon. Although both spotting and breakthrough bleeding increased slightly in the first two cycles, irregular bleeding returned to pretreatment levels by the third cycle. The length of the withdrawal bleed in the pill-free week was reduced. The incidence of irregular bleeding and other side effects was substantially lower in this sample of Malaysian women than in Asian and Caucasian Marvelon users surveyed in other studies. PMID:12320338

  3. Nomegestrol acetate/estradiol hormonal oral contraceptive and breast cancer risk.

    PubMed

    Del Pup, Lino; Berretta, Massimiliano; Di Francia, Raffaele; Cavaliere, Carla; Di Napoli, Marilena; Facchini, Gaetano; Fiorica, Francesco; Mileto, Mario; Schindler, Adolf E

    2014-08-01

    Combined hormonal contraceptives (CHCs) contain estrogen and progestin, which can stimulate estrogen-sensitive and/or progesterone-sensitive breast cancer growth. Until recently, ethinylestradiol had been almost the only estrogen used for decades, and its dose has been greatly reduced over time. The first generations of birth control pills contained approximately five times more estrogen and four times more progestin than the latest contraceptives. Newer CHCs also contain steroids that more closely mimic the physiological estradiol (E2) and progesterone effects. The newer CHC formulations are thus expected to have less influence on the breast, although it is very difficult to demonstrate any difference among the recent available preparations in human studies. Recently, nomegestrol acetate (NOMAC), a neutral, nonandrogenic, progesterone-like profile progestin, has become available in combination with the 'natural' estrogen, E2. According to the literature, NOMAC/E2 is expected to have either a lesser stimulating effect or a neutral effect on estrogen-sensitive breast cancers. We performed an analysis of the available studies and a bibliographical review. The endocrine and metabolic effects of NOMAC/E2 formulation might lead to a lesser breast tissue stimulation. The data reported, confirmed through clinical studies, should be considered when choosing a hormonal contraceptive, especially when breast stimulation is a concern. PMID:24346139

  4. New contraceptive choices across reproductive life.

    PubMed

    Foran, Therese M

    2003-06-16

    The range of contraceptive options and consumer awareness of new contraceptive methods have both increased significantly over the past 10 years. New methods available in Australia include lower-dose oral contraceptive pills, new oral progestogens, progestogen implants, a progestogen-bearing intrauterine device and polyurethane female condoms. Contraceptive options which may soon be introduced in Australia include novel methods of administering combined (oestrogen-progestogen) contraception, such as dermal patches and vaginal rings. PMID:12797848

  5. [Hemoperitoneum caused by rupture of a benign tumor of the liver in women taking oral contraceptives. 2 cases].

    PubMed

    Nicodeme, J P; Levy, J B; Gendrel, T; Costet, H; Prestat, J; Reynes, M; James, J M

    1976-06-01

    2 cases of rupture of benign liver tumors in women who had received oral contraceptive (OC) treatment for over 7 years are reported. Although the number of cases of benign liver tumor is very small, it has been increasing in recent years. The role of OCs in determining them is still unproven, and the risk appears to be extremely low (between 1 in 500,000 and 1 in 1,000,000); however, it is possible that favor the growth of preexisting lesions or the occurrence of rupture with hemorrhages. It is concluded that the possibility of such cases must be considered by physicians, and that early detection and surgery are required in order to remove the tumor before its rupture and consequent hemorrhage. PMID:934872

  6. [Oral combined hormonal contraception containing nomegestrol acetate and 17beta-oestradiol--the statement of Polish Gynecological Society Experts Group].

    PubMed

    Debski, Romuald; Kotarski, Jan; Paszkowski, Tomasz; Pawelczyk, Leszek; Poreba, Ryszard; Skrzypulec-Plinta, Violetta; Tomaszewski, Jacek

    2012-04-01

    Nomegestrol acetate (NOMAC) combined with E2 (Zoely) is a monophasic oral contraceptive (OC) which safety and efficacy was confirmed in a number of level I evidence clinical trials. Zoely is highly effective OC, especially in overweight and obese patients, with good cycle control, safe and well tolerated. NOMAC/E2 combination causes no or minimal weight gain and is characterized by minimal influence on bone mineral density or blood pressure and presence of acne. Moreover lipids profile, carbohydrates metabolism, haemostasis and endocrine glands functioning were not affected. High tolerance and acceptance of NOMAC/E2 combination by women, low adverse event profile, fast recovery of ovarian activity and ovulation is a reasonable treatment tool in everyday practice. PMID:22712267

  7. Metabolism and pharmacokinetics of major polyphenol components in rat plasma after oral administration of total flavonoid tablet from Anemarrhenae Rhizoma.

    PubMed

    Xie, Yuan-Yuan; Wang, Xiu-Ming; Wang, Si-Huan; Wang, Yi-Ming; Tian, Hui-Fang; Yuan, Yong-Sheng; Li, Hong-Yan; Liang, Qiong-Lin; Luo, Guo-An

    2016-07-15

    Total flavonoid tablet from Anemarrhenae Rhizoma (Zhimu tablet), which was made of total polyphenol components extracted from the dried rhizome of Anemarrhena asphodeloides Bge. (Zhimu in Chinese), is a novel traditional Chinese medicine prescribed for the treatment of diabetes. Mangiferin (MF) and neomangiferin (NMF) are the two main components detected and determined in Zhimu tablet, accounting for 8.9% of the total weight of each tablet. In the present study, high performance liquid chromatography (HPLC) coupled with time-of-flight (TOF) tandem mass spectrometry (MS) was applied to characterize the metabolites of MF and NMF in rat plasmas collected at different time points after oral administration of Zhimu tablet at a dose of 3.63g/kg (corresponding to 270mg/kg MF). Accurate mass measurement was used to determine the elemental composition of metabolites and thus to confirm the proposed structures of identified metabolites. Time points of appearance of some metabolites, such as isomers, were also taken into account during the structure confirmation. A total of 21 potential metabolites were found in rat plasma at different time points, and the metabolic pathways in vivo were involved in hydrolysis, methylation, glucuronide conjugation, glycoside conjugation, sulphation, dehydration and isomerisation. Furthermore, a selective and accurate LC-MS assay method was developed and validated for the quantification of MF in plasma. Semi-quantification of main conjugated metabolites was also performed in order to describe the dynamic metabolism profiles of polyphenol components in Zhimu tablet. MF concentration in plasma reached 1.36±0.47μgmL(-1) about 5.0h after oral administration of Zhimu tablet, which showed a 3.24- and 4.91-fold increase in plasma maximum concentration and area under the concentration-time curve (AUC) from 0 to 24h of MF compared with those for rats administered with free MF, respectively. The results indicated that the pharmacokinetic processes and

  8. Emergency Contraception.

    PubMed

    Batur, Pelin; Kransdorf, Lisa N; Casey, Petra M

    2016-06-01

    Emergency contraception (EC) may help prevent pregnancy in various circumstances, such as contraceptive method failure, unprotected sexual intercourse, or sexual assault, yet it remains underused. There are 4 approved EC options in the United States. Although ulipristal acetate requires a provider's prescription, oral levonorgestrel (LNG) is available over the counter for women of all ages. The most effective method of EC is the copper intrauterine device, which can be left in place for up to 10 years for efficacious, cost-effective, hormone-free, and convenient long-term primary contraception. Ulipristal acetate tends to be more efficacious in pregnancy prevention than is LNG, especially when taken later than 72 hours postcoitus. The mechanism of action of oral EC is delay of ovulation, and current evidence reveals that it is ineffective postovulation. Women who weigh more than 75 kg or have a body mass index greater than 25 kg/m(2) may have a higher risk of unintended pregnancy when using oral LNG EC; therefore, ulipristal acetate or copper intrauterine devices are preferable in this setting. Providers are often unaware of the range of EC options or are unsure of how to counsel patients regarding the access and use of EC. This article critically reviews current EC literature, summarizes recommendations, and provides guidance for counseling women about EC. Useful tips for health care providers are provided, with a focus on special populations, including breast-feeding women and those transitioning to long-term contraception after EC use. When treating women of reproductive age, clinicians should be prepared to counsel them about EC options, provide EC appropriately, and, if needed, refer for EC in a timely manner. PMID:27261868

  9. Combination effect of physical and gustatory taste masking for propiverine hydrochloride orally disintegrating tablets on palatability.

    PubMed

    Matsui, Rakan; Uchida, Shinya; Namiki, Noriyuki

    2015-01-01

    Orally disintegrating tablets (ODTs) containing propiverine hydrochloride (which is extremely bitter and leaves a feeling of numbness in the mouth) were prepared with a combined use of physical and organoleptic taste masking. Propiverine-loaded masking particles (PLMPs) were prepared with different amounts of gastric-soluble coatings as physical masking. ODTs without organoleptic masking were prepared by mixing each group of PLMPs with Ludiflash®, crospovidone, and magnesium stearate. ODTs with organoleptic masking were also prepared by addition of L-menthol, aspartame, thaumatin, and cinnamon. Fifteen-minute dissolution of propiverine in solutions with pH 1.2 was ≥ 85% for all ODTs, whereas that in pH 6.8 solutions was ≤ 85% and increased with physical masking. A single blind randomized crossover trial was conducted. Ten healthy volunteers were asked to quantify the bitterness, numbness, and overall palatability using a 100-mm visual analog scale (VAS) at the period of disintegration as well as 1 and 5 min later. VAS scores of bitterness, numbness, and overall palatability improved along with increasing amounts of physical masking, and the effects persisted for 5 min. VAS scores for numbness increased over time regardless of the amount of physical masking. Bitterness, numbness, and overall palatability were significantly improved by organoleptic masking if the amount of physical masking was small. Combined use of physical and organoleptic masking is useful for improving palatability of ODTs containing propiverine. PMID:25744453

  10. Orally disintegrating vardenafil tablets for the treatment of erectile dysfunction: efficacy, safety, and patient acceptability

    PubMed Central

    Green, Roger; Hicks, Rodney W

    2011-01-01

    Background: Erectile dysfunction (ED) is a well-documented medical condition that is expected to increase significantly over the next several decades, especially as men live longer and the prevalence of diabetes and cardiovascular diseases increase. Pharmacology agents are often the first line treatment approach. Newer solid dosage forms, known as orally disintegrating tablets (ODT), are now available as one treatment option. Objectives: To review the drug delivery mechanisms of ODTs in general and to review safety and efficacy of vardenafil ODT (a PDE-5 inhibitor) as a treatment option for management of ED. Method: Literature reviews were performed of pharmaceutical dosage forms and the POTENT I (n = 358 subjects) and POTENT II (n = 337 subjects) studies that investigated vardenafil ODT. Results: Vardenafil ODT has been successfully used in multiple age groups and in multiple settings with men from various ethnic backgrounds. Efficacy of vardenafil ODT, as measured using the International Index of Erectile Function (IIEF-EF) and from the Sexual Encounter Profile (SEP) was significantly greater than placebo (P < 0.0001) at 12 weeks. Safety profiles were similar to film-coated dosage forms with no patient deaths reported. Conclusion: Vardenafil ODT offers a convenient, ready-to-use approach for combating ED. Safety concerns are similar to other PDE-5 inhibitors and practitioners should counsel patients accordingly. PMID:21573049

  11. Biopharmaceutical characterization of oral theophylline and aminophylline tablets. Quantitative correlation between dissolution and bioavailability studies.

    PubMed

    Varshosaz, J; Ghafghazi, T; Raisi, A; Falamarzian, M

    2000-09-01

    Considering the narrow therapeutic index of theophylline and the low range between the safe and toxic serum concentrations of this drug, the study of its pharmacokinetic properties is necessary. However, considering the time consuming and expensive in vivo tests, quantitative correlation between in vivo bioavailability and in vitro dissolution tests can be used routinely in quality control tests of these drug products to predict the in vivo pharmacokinetic parameters. For this reason healthy human volunteers were used for in vivo studies and serum samples were analyzed by a fluorescence polarization immunoassay analysis (FPIA) method. The results showed that an open one compartmental model could best describe the pharmacokinetic properties of orally administered theophylline and aminophylline tablets. Linear regression analysis by least-square method showed a good correlation between some in vivo and in vitro parameters obtained from dissolution studies by rotating basket and paddle methods. D(30)% (percentage of drug dissolved in vitro after 30 min) and F(0.5)% (drug absorbed in vivo after half an hour calculated by Wagner-Nelson equation) showed best correlation (r=0. 99036). C(max) (maximum serum concentration) of this drug also correlates well with t(25%) (time required to dissolve 25% of the drug). The calculated correlation coefficients could best predict the actual values of some pharmacokinetic parameters; AUC(0-->infinity), AUC(0-->1), F(0.5)% and C(max). PMID:10962242

  12. The prediction of the palatability of orally disintegrating tablets by an electronic gustatory system.

    PubMed

    Nakamura, Hideshi; Uchida, Shinya; Sugiura, Takeshi; Namiki, Noriyuki

    2015-09-30

    In this study, the human gustatory palatability sensation of taste-masked famotidine and amlodipine orally disintegrating tablets (ODTs) was quantitatively predicted by an electronic gustatory system (α-Astree e-Tongue). Furthermore, its use in formulation design was evaluated. The famotidine- and amlodipine-containing ODTs, which were bitter- and highly bitter-tasting, respectively, were prepared using a physical (granules spray-coated with ethyl cellulose) or organoleptic (the addition of a sweetener and a flavor) masking method and combinations thereof. The taste-masking effects of different masking methods on the ODTs were investigated in a human gustatory sensation test. In the test, volunteers scored the overall palatability using a 100mm visual analog scale (VAS). The electronic gustatory system was evaluated using the Euclidean distance (the distance between each drug-containing ODT and its corresponding placebo) and partial least squares (PLS) regression analysis of the sensor response values. A good linear relationship was observed between each ODT's Euclidean distance analysis, PLS regression analysis, and clinical VAS scores. Cross-validation verification of each analysis confirmed the model's predictive power. This study suggests that the α-Astree can quantitatively evaluate physical and organoleptic taste masking and that the palatability of unknown formulations can be predicted by Euclidean distance and PLS regression data analysis. PMID:26216412

  13. Single, Escalating Dose Pharmacokinetics, Safety and Food Effects of a New Oral Androgen Dimethandrolone Undecanoate in Man: A prototype oral male hormonal contraceptive

    PubMed Central

    Swerdloff, Ronald S.; Nya-Ngatchou, Jean Jacques; Liu, Peter Y.; Amory, John K.; Leung, Andrew; Hull, Laura; Blithe, Diana L.; Woo, Jason; Bremner, William J.; Wang, Christina

    2014-01-01

    The novel androgen, dimethandrolone (DMA) has both androgenic and progestational activities, properties that may maximize gonadotropin suppression. We assessed the pharmacokinetics of dimethandrolone undecanoate (DMAU), an orally bioavailable, longer-acting ester of DMA, for male contraceptive development. Our objective was to examine the safety and pharmacokinetics of single, escalating doses of DMAU (powder in capsule formulation) administered orally with or without food in healthy men. We conducted a randomized, double-blind Phase 1 study. For each dose of DMAU (25 to 800 mg), ten male volunteers received DMAU and two received placebo at two academic medical centers. DMAU was administered both fasting and after a high fat meal (200–800 mg doses). Serial serum samples were collected over 24h following each dose. DMAU was well tolerated without significant effects on vital signs, safety laboratory tests or electrocardiograms. When administered while fasting, serum DMA (active compound) was detectable in only 4/10 participants after the 800mg dose. When administered with a 50% fat meal, serum DMA was detectable in all participants given 200mg DMAU and showed a dose-incremental increase up to 800mg, with peak levels 4 to 8h after taking the dose. Serum gonadotropins and sex hormone concentrations were significantly suppressed 12h after DMAU administration with food at doses above 200mg. This first-in-man study demonstrated that a single, oral dose of DMAU up to 800 mg is safe. A high-fat meal markedly improved DMAU/DMA pharmacokinetics. PMID:24789057

  14. [Contraceptive pancreopathy].

    PubMed

    Riederer, J

    1973-01-26

    In a private practice an increasing number of young women or girls are being observed with sudden onset of acute stomach pains of unknown origin. Clinically the pancreas is sensitive to pressure and there is an alpha-amylase elevation in the urine often accompanied by moderate leukocytosis. A slight elevation of the transaminase count is usual in such cases. There are no indications of alchohol abuse or pancreatic disorders in the anamnese and x-rays reveal an adequately functionning gall bladder without stones. Without exception all the women have been on oral contraceptives. With spasmolytics and a diet low in fats the symptoms disappear, often without discontinuation of the contraceptive. More data are needed on this problem, and prospective research should determine which additional factors must be present for the activation of such pancreatic disorders. PMID:4684016

  15. [Pharmacological, metabolic and clinical aspects of new oral contraceptive associations containing natural estrogens].

    PubMed

    Ferrari, S; Piacenti, I; Napolitano, A; Cagnacci, A

    2014-02-01

    Introduction of new compounds containing natural estrogens represented a major development in the field of hormonal contraception. Micronized estradiol (E2) and its estere valerate (EV), is more easily metabolized by the liver than ethynylestradiol (EE). This causes minimal metabolic impact, but the weak estrogenic activity needs not be antagonized by androgenic progestin and requires progestin capable to stabilize the endometrium. Dienogest (DNG), an antiandrogenic progestin with a short half-life, is associated with estradiol valerate (EV) in a quadriphasic fashion. In comparison to EE/levonorgestrel (LNG), EV/DNG is more neutral on metabolism and coagulation. Furthermore, it does not seem to negatively affect the cardiovascular system and breast. Cycle control is optimal with a higher prevalence of amenorrhea and reduction of menstrual flow. For this reason EV/DNG can be tehrapeutic for heavy menstrual bleedings. Nomegestrol acetate (NOMAc), an anti-andogen progestin with a long half-life is combined in monophasic regimen with micronized E2. E2/NOMAc is more neutral than EE/LNG on metabolism and more neutral than EE/DRSP on coagulation. NOMAc reduces peripheral tissue estrogen formation, and this may be beneficial for the breast. The two formulations exert a high contraceptive efficacy similar to the ones containing EE, but with less estrogen-related side-effects. The additional benefits due to DNG and NOMAc need to be further explored. PMID:24569408

  16. Metabolic effects of low-dose fluconazole in healthy female users and non-users of oral contraceptives.

    PubMed

    Devenport, M H; Crook, D; Wynn, V; Lees, L J

    1989-06-01

    1. Azole antifungal agents such as ketoconazole act by inhibiting cytochrome P-450 mediated sterol synthesis in the fungal cell membrane and thus have the potential to interfere with mammalian steroidogenesis. Fluconazole is a novel orally-effective antifungal triazole which has been reported to have more specific effects on the cytochrome P-450 enzymes involved in fungal sterol synthesis. 2. Due to the potential value of systemic antifungal agents in the treatment of infections commonly occurring in women, we assessed the effect of oral fluconazole on the metabolic profile of 18 healthy premenopausal women, 10 of whom were taking combined oral contraceptives (OC). Each woman acted as her own control, being studied both before and 21-28 days after fluconazole therapy (50 mg daily), in the luteal phase of consecutive menstrual cycles. 3. The endocrinological profile included measurement of serum oestradiol, progesterone, testosterone and sex hormone binding globulin (SHBG) concentrations, short tetracosactrin adrenal stimulation test and thyroid function tests. Carbohydrate metabolism was investigated by means of an oral glucose tolerance test with measurement of plasma glucose, insulin and C-peptide concentrations. Serum lipids, lipoproteins and apolipoproteins were analysed on samples taken after an overnight fast. 4. Minor biochemical changes associated with fluconazole treatment included increases in serum thyroxine and testosterone concentrations (but not in women taking OC as well as fluconazole) and in insulin and apolipoprotein B levels (but only in women taking OC as well as fluconazole). In general, these changes were small and of no clinical significance with the values remaining within the laboratory normal range. There were no adverse side-effects.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:2547410

  17. Application of water-insoluble polymers to orally disintegrating tablets treated by high-pressure carbon dioxide gas.

    PubMed

    Ito, Yoshitaka; Maeda, Atsushi; Kondo, Hiromu; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2016-09-10

    The phase transition of pharmaceutical excipients that can be induced by humidifying or heating is well-known to increase the hardness of orally disintegrating tablets (ODTs). However, these conditions are not applicable to drug substances that are chemically unstable against such stressors. Here, we describe a system which enhances the hardness of tablets containing water-insoluble polymers by using high-pressure carbon dioxide (CO2). On screening of 26 polymeric excipients, aminoalkyl methacrylate copolymer E (AMCE) markedly increased tablet hardness (+155N) when maintained in a high-pressure CO2 environment. ODTs containing 10% AMCE were prepared and treatment with 4.0MPa CO2 gas at 25°C for 10min increased the hardness to +30N, whose level corresponded to heating at 70°C for 720min. In addition, we confirmed the effects of CO2 pressure, temperature, treatment time, and AMCE content on the physical properties of ODTs. Optimal pressure of CO2 gas was considered to be approximately 3.5MPa for an AMCE formula, as excessive pressure delayed the disintegration of ODTs. Combination of high-pressure CO2 gas and AMCE is a prospective approach for increasing the tablet hardness for ODTs, and can be conducted without additional heat or moisture stress using a simple apparatus. PMID:27374202

  18. High-amylose sodium carboxymethyl starch matrices: development and characterization of tramadol hydrochloride sustained-release tablets for oral administration.

    PubMed

    Nabais, Teresa; Leclair, Grégoire

    2014-01-01

    Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol. PMID:25006518

  19. A bioequivalence study of levothyroxine tablets versus an oral levothyroxine solution in healthy volunteers.

    PubMed

    Yannovits, N; Zintzaras, E; Pouli, A; Koukoulis, G; Lyberi, S; Savari, E; Potamianos, S; Triposkiadis, F; Stefanidis, I; Zartaloudis, E; Benakis, A

    2006-01-01

    Probably for genetic reasons a substantial part of the Greek population requires Levothyroxine treatment. Since commercially available Levothyroxine was first marketed, the manufacture and storage of the drug in tablet form has been complicated and difficult; and as cases of therapeutic failure have frequently been reported following treatment with this medicinal agent, quality control is an essential factor. Due to the unreliability of Levothyroxine-based commercial products, in the present study we decided to follow the Food and Drug Administration (FDA) guidelines*, and use a Levothyroxine solution as reference product. The bioavailability of the Levothyroxine sodium tablet formulation THYROHORMONE/Ni-The Ltd (0.2 mg/tab) and that of a reference oral solution (0.3 mg/100 ml) under fasting conditions were compared in an open, randomized, single-dose two-way crossover study. Twenty four healthy Caucasian volunteers (M/F=15/9, mean age=32.9+/-7.4yr) participated in the study. Bioavailability was assessed by pharmacokinetic parameters such as the area under plasma concentration-time curve from time zero up to the measurable last time point (AUC(last)) and the maximum plasma concentration (Cmax). Heparinized venous blood samples were collected pre-dose and up to a 48-hour period post-dose. Levothyroxine sodium in plasma samples was assayed by a validated electrochemiluninescent immunoassay technique. Statistical analysis showed that the post-dose thyrotropin-stimulating hormone (TSH) levels decreased significantly (p<0.05). Regarding Levothyroxine (T4), the point estimate of the test formulation to the reference formulation ratios (T/R) for AUC(last) and Cmax was 0.92 with 90% confidence limits (0.90, 0.94) and 0.93 with 90% confidence limits (0.91, 0.94), respectively. Regarding triiodo-L-thyronine (T3), the point estimate for the T/R ratios of AUC(last) and Cmax was 0.92 with 90% confidence limits (0.90, 0.95) and 0.94 with 90% confidence limits (0.92, 0

  20. Influence of Prosolv and Prosolv:Mannitol 200 direct compression fillers on the physicomechanical properties of atorvastatin oral dispersible tablets.

    PubMed

    Gowda, Veeran; Pabari, Ritesh M; Kelly, John G; Ramtoola, Zebunnissa

    2015-06-01

    The objective of the present study was to evaluate the influence of Prosolv® and Prosolv®: Mannitol 200 direct compression (DC) fillers on the physicomechanical characteristics of oral dispersible tablets (ODTs) of crystalline atorvastatin calcium. ODTs were formulated by DC and were analyzed for weight uniformity, hardness, friability, drug content, disintegration and dissolution. Three disintegration time (DT) test methods; European Pharmacopoeia (EP) method for conventional tablets (Method 1), a modification of this method (Method 2) and the EP method for oral lyophilisates (Method 3) were compared as part of this study. All ODTs showed low weight variation of <2.5%. Prosolv® only ODTs showed the highest tablet hardness of ∼ 73 N, hardness decreased with increasing mannitol content. Friability of all formulations was <1% although friability of Prosolv®:Mannitol ODTs was higher than for pure Prosolv®. DT of all ODTs was <30 s. Method 2 showed the fastest DT. Method 3 was non-discriminatory giving a DT of 13-15 s for all formulations. Atorvastatin dissolution from all ODTs was >60% within 5 min despite the drug being crystalline. Prosolv® and Prosolv®:Mannitol-based ODTs are suitable for ODT formulations by DC to give ODTs with high mechanical strength, rapid disintegration and dissolution. PMID:24397821

  1. Enhancement of the Oral Bioavailability of Fexofenadine Hydrochloride via Cremophor® El-Based Liquisolid Tablets

    PubMed Central

    Yehia, Soad Ali; El-Ridi, Mohamed Shafik; Tadros, Mina Ibrahim; El-Sherif, Nolwa Gamal

    2015-01-01

    Purpose: The current work aimed to develop promising Fexofenadine hydrochloride (FXD) liquisolid tablets able to increase its oral bioavailability and shorten time to reach maximum plasma concentrations (Tmax). Methods: Eighteen liquisolid powders were developed based on 3 variables; (i) vehicle type [Propylene glycol (PG) or Cremophor® EL (CR)], (ii) carrier [Avicel® PH102] to coat [Aerosil® 200] ratio (15, 20, 25) and (iii) FXD concentration in vehicle (30, 35, 40 %, w/w). Pre-compression studies involved identification of physicochemical interactions and FXD crystallinity (FT-IR, DSC, XRD), topographic visualization (SEM) and estimation of flow properties (angle of repose, Carr’s index, Hausner’s ratio). CR-based liquisolid powders were compressed as liquisolid tablets (LST 9 – 18) and evaluated for weight-variation, drug-content, friability-percentage, disintegration-time and drug-release. The pharmacokinetics of LST-18 was evaluated in healthy volunteers relative to Allegra® tablets. Results: Pre-compression studies confirmed FXD dispersion in vehicles, conversion to amorphous form and formation of liquisolid powders. CR-based liquisolid powders showed acceptable-to-good flow properties suitable for compaction. CR-based LSTs had appropriate physicochemical properties and short disintegration times. Release profile of LST-18 showed a complete drug release within 5 min. Conclusion: LST-18 succeeded in increasing oral FXD bioavailability by 62% and reducing Tmax to 2.16 h. PMID:26819931

  2. Investigation on the association between breast cancer and consumption patterns of combined oral contraceptive pills in the women of Isfahan in 2011

    PubMed Central

    Ehsanpour, Soheila; Nejad, Fahime Seyed Ahmadi; Rajabi, Fariborz Mokarian; Taleghani, Fariba

    2013-01-01

    Background: Oral contraceptive pills are among the most popular contraceptive methods, but the fear of cancer and cardiovascular disease overshadows its continuous use among women. This study aimed to define the association between consumption patterns of combined oral contraceptives among women with breast cancer. Materials and Methods: This is an analytical case–control study conducted on 175 women with breast cancer, referring to Seyed al Shohada Medical Center and private clinics in Isfahan to be treated and followed up in 2011, as well as 350 healthy women who were identical with the subjects in the study group regarding age and residential location. The data were collected using a researcher-made questionnaire. Content validity and Cronbach's alpha were employed to confirm validity and scientific reliability of the questionnaire, respectively. The data were analyzed by descriptive and analytical statistical methods through SPSS. Results: The findings showed that there was a significant association between history of contraceptive pills’ consumption and incidence of breast cancer (P < 0.001). It was shown that the risk of developing breast cancer is increased by 2.27-fold among those with pills’ consumption compared to those with no history of that. It was also shown that pills’ consumption for 36-72 months increased the risk of breast cancer by 2.18-fold, the age of the first use being less than 20 years increased the risk by 3.28-fold, and time since the last use of less than 25 years increased the risk by 2.63-fold. There was no significant association between duration of use, age of the first and last use, and time since the first and last use in the study and control groups. Conclusion: The results showed that history of pills’ consumption is associated with incidence of breast cancer regardless of the consumption pattern. Use of oral contraceptives pills at any age and for any duration can increase the risk of breast cancer. PMID:23983752

  3. Formulation and bioequivalence of two Valsartan/Amlodipine immediate release tablets after a single oral administration.

    PubMed

    Zaid, Abdel Naser; Natur, Salam; Qaddomi, Aiman; Abualhasan, Murad; Al-Ramahi, Rowa; Shraim, Naser; Khammash, Saed; Jaradat, Nidal

    2014-07-01

    The aim of this study was to formulate a film-coated Valsartan/Amlodipine (VS/AM) immediate release tablets and to evaluate their in vivo release profile. VS/AM core tablets were manufactured using dry granulation method. Opadry aqueous coating dispersion was used as film coating material. Dissolution of the film coated tablets was tested in 900 ml of 0.5% SLS media, bioequivalence of tablets was tested by comparisons against the reference brand product. The ICH guidelines were used to evaluate the stability of the obtained tablets. The coated tablets were subjected to gastric pH, and drug release was analyzed using HPLC system to evaluate the efficiency of the film coat. The coated tablets had no defects. VS/AM release met the FDA guidelines for bioequivalence studies. Statistical comparison of the main pharmacokinetic parameters showed no significant difference between test and reference. These findings suggest that aqueous film coating with Opadry system is an easy and economical approach for preparing stable film coated VS/AM tablets without compromising their in vivo drugs release. PMID:25015436

  4. Pharmacokinetic profile of rizatriptan 10-mg tablet and 10-mg orally disintegrating tablet administered with or without water in healthy subjects: an open-label, randomized, single-dose, 3-period crossover study.

    PubMed

    Swan, Suzanne K; Alcorn, Harry; Rodgers, Anthony; Hustad, Carolyn M; Ramsey, Karen E; Woll, Susan; Skobieranda, Franck

    2006-02-01

    This open-label, 3-period crossover study compared the plasma concentration profiles of rizatriptan tablet, orally disintegrating tablet with water (ODTc), and ODT without water (ODTs) in 24 healthy volunteers aged 18 to 45 years. At each period, subjects received a single dose of either 10-mg rizatriptan tablet, 10-mg rizatriptan ODTs, or 10-mg rizatriptan ODTc. The authors hypothesized that ODTc has a greater geometric mean AUC(0-2h) than ODTs and that ODTc has a greater geometric mean AUC(0-1h) than tablet. A secondary end point was to compare the time of occurrence of the maximum rizatriptan plasma concentration (t(max)) of each dosing method. ODTc had a statistically significantly greater geometric mean AUC(0-2h) compared with ODTs (33.84 h x ng/mL vs 18.83 h x ng/mL; P < .001). ODTc had a slightly, but not statistically significantly, greater geometric mean AUC(0-1h) compared with rizatriptan tablet (17.07 h x ng/mL vs 13.32 h x ng/mL). The median t(max) was 0.67 hours for ODTc and tablet and 1.33 hours for ODTs. ODTc showed a slightly, but not significantly, faster rate of absorption compared with tablet. ODTs with water had a faster rate of absorption than ODTc. Future studies are needed to determine whether this pharmacokinetic difference produces differential efficacy in a clinical setting. PMID:16432269

  5. A randomized comparative trial of a combined oral contraceptive and azelaic acid to assess their effect on sleep quality in adult female acne patients.

    PubMed

    Albuquerque, Rachel Gimenes; da Rocha, Marco Alexandre Dias; Hirotsu, Camila; Hachul, Helena; Bagatin, Edileia; Tufik, Sergio; Andersen, Monica Levy

    2015-12-01

    Several studies have reported an increase in the prevalence of adult female acne. This subtype of acne presents particular characteristics, and can be triggered by several factors such as smoking, stress, the use of oily cosmetics and even by poor sleep. Sleep quality is related to well-being and the maintenance of body homeostasis. In addition, several skin diseases present a bidirectional relationship with sleep, demonstrating an important connection between skin and the central nervous system. With this in mind, we aimed to compare the effect of two types of treatment for adult female acne (azelaic acid or a combined oral contraceptive) on sleep quality and on concentrations of stress hormones. Also, we proposed to assess the correlation of sleep and hormonal parameters with acne severity. In order to do this, 32 women underwent a clinical evaluation, completed the Pittsburgh Sleep Quality Index (PSQI) questionnaire and had their blood collected for hormone assays. These procedures were performed at baseline and after 6 months of treatment. At baseline there were no differences between the groups in terms of body mass index, age, acne severity and hormone concentrations. Results showed that both treatments demonstrated effectiveness but that women treated with azelaic acid presented a better sleep quality after the treatment compared to baseline and to the group treated with the combined oral contraceptive. The combined oral contraceptive group presented an increase in cortisol and a decrease in free testosterone concentration in relation to baseline. These data suggest that both azelaic acid and combined oral contraceptive are effective in the treatment of adult female acne but, azelaic acid seems to be a more suitable option for those women who may benefit from a better subjective sleep quality. PMID:26472098

  6. The Drop That Spilled the Cup: Acute Myocardial Infarction in a Young Woman with Underlying Thrombophilic Polymorphisms and Oral Contraceptive Use

    PubMed Central

    Capilli, Gianfranco; Patané, Anella Antonietta

    2014-01-01

    We present the case of a 28-year-old woman who was admitted to our cardiology unit for acute coronary syndrome. Her history was notable for cardiovascular disease familiarity, active smoking, and oral contraceptive use. On further analysis, she was noted to have thrombophilic polymorphisms involving the plasminogen activator inhibitor (PAI), angiotensin-converting enzyme (ACE), and methylenetetrahydrofolate reductase (MTHFR) genes. We discuss the implications that these cofactors may have had in the genesis of the disease. PMID:25587456

  7. The drop that spilled the cup: acute myocardial infarction in a young woman with underlying thrombophilic polymorphisms and oral contraceptive use.

    PubMed

    Russo, Nunzio; Franzì, Enrico; Capilli, Gianfranco; Patané, Anella Antonietta; Russo, Silvia Paola; Evola, Rosario

    2014-01-01

    We present the case of a 28-year-old woman who was admitted to our cardiology unit for acute coronary syndrome. Her history was notable for cardiovascular disease familiarity, active smoking, and oral contraceptive use. On further analysis, she was noted to have thrombophilic polymorphisms involving the plasminogen activator inhibitor (PAI), angiotensin-converting enzyme (ACE), and methylenetetrahydrofolate reductase (MTHFR) genes. We discuss the implications that these cofactors may have had in the genesis of the disease. PMID:25587456

  8. Population pharmacokinetics of levodopa in subjects with advanced Parkinson's disease: levodopa-carbidopa intestinal gel infusion vs. oral tablets

    PubMed Central

    Othman, Ahmed A; Dutta, Sandeep

    2014-01-01

    Aims Levodopa-carbidopa intestinal gel (LCIG) provides continuous levodopa-carbidopa delivery through intrajejunal infusion. This study characterized the population pharmacokinetics of levodopa following a 16 h jejunal infusion of LCIG or frequent oral administration of levodopa-carbidopa tablets (LC-oral) in subjects with advanced Parkinson's disease (PD). Methods A non-linear mixed-effects model of levodopa pharmacokinetics was developed using serial plasma concentrations from an LCIG phase 1 study and a phase 3 double-blind, double-dummy study of the efficacy and safety of LCIG compared with LC-oral in advanced PD patients (n = 68 for model development; 45 on LCIG and 23 on LC-oral). The final model was internally evaluated using stochastic simulations and bootstrap and externally evaluated using sparse pharmacokinetic data from 311 subjects treated in a long term safety study of LCIG. Results The final model was a two compartment model with a transit compartment for absorption, first order elimination, bioavailability for LCIG (97%; confidence interval = 95% to 98%) relative to LC-oral, different first order transit absorption rate constants (LCIG = 9.2 h–1 vs. LC-oral = 2.4 h–1; corresponding mean absorption time of 7 min for LCIG vs. 25 min for LC-oral) and different residual (intra-subject) variability for LCIG (15% proportional error, 0.3 μg ml−1 additive error) vs. LC-oral (29% proportional error, 0.59 μg ml−1 additive error). Estimated oral clearance and steady-state volume of distribution for levodopa were 24.8 l h−1 and 131 l, respectively. Conclusions LCIG administration results in faster absorption, comparable levodopa bioavailability and significantly reduced intra-subject variability in levodopa concentrations relative to LC-oral administration. PMID:24433449

  9. Multinational, multicentre, randomised, open-label study evaluating the impact of a 91-day extended regimen combined oral contraceptive, compared with two 28-day traditional combined oral contraceptives, on haemostatic parameters in healthy women

    PubMed Central

    Paoletti, Anna Maria; Volpe, Annibale; Chiovato, Luca; Howard, Brandon; Weiss, Herman; Ricciotti, Nancy

    2014-01-01

    Objectives To evaluate the impact of a 91-day extended regimen combined oral contraceptive (150 μg levonorgestrel [LNG]/30 μg ethinylestradiol [EE] for 84 days, followed by 10 μg EE for seven days [Treatment 1]) compared with two traditional 21/7 regimens (21 days 150 μg LNG/30 μg EE [Treatment 2] or 150 μg desogestrel [DSG]/30 μg EE [Treatment 3], both with seven days’ hormone free), on several coagulation factors and thrombin formation markers. Methods Randomised, open-label, parallel-group comparative study involving healthy women (18–40 years). The primary endpoint was change from baseline in prothrombin fragment 1 + 2 (F1 + 2) levels over six months. Results A total of 187 subjects were included in the primary analysis. In all groups, mean F1 + 2 values were elevated after six months of treatment. Changes were comparable between Treatments 1 and 2 (least squares mean change: 170 pmol/L and 158 pmol/L, respectively) but noticeably larger after Treatment 3 (least squares mean change: 592 pmol/L). The haemostatic effects of Treatment 1 were comparable to those of Treatment 2 and noninferior to those of Treatment 3 (lower limit of 95% confidence interval [− 18.3 pmol/L] > − 130 pmol/L). Conclusions The LNG/EE regimens had similar effects on F1 + 2. Noninferiority was demonstrated between extended regimen LNG/EE and DSG/EE. PMID:24923685

  10. Acute effects of bright light and caffeine on nighttime melatonin and temperature levels in women taking and not taking oral contraceptives

    NASA Technical Reports Server (NTRS)

    Wright, K. P. Jr; Myers, B. L.; Plenzler, S. C.; Drake, C. L.; Badia, P.; Czeisler, C. A. (Principal Investigator)

    2000-01-01

    Caffeine and bright light effects on nighttime melatonin and temperature levels in women were tested during the luteal phase of the menstrual cycle (n=30) or the pseudo luteal phase for oral contraceptive users (n=32). Participants were randomly assigned to receive either bright (5000 lux) or dim room light (<88 lux) between 20:00 and 08:00 h under a modified constant routine protocol. Half the subjects in each lighting condition were administered either caffeine (100 mg) or placebo in a double-blind manner at 20:00, 23:00, 02:00 and 05:00 h. Results showed that the combination of bright light and caffeine enhanced nighttime temperature levels to a greater extent than did either caffeine or bright light alone. Both of the latter groups had higher temperature levels relative to the dim light placebo condition and the two groups did not differ. Temperature levels in the bright light caffeine condition were maintained at near peak circadian levels the entire night in the luteal and pseudo luteal phase. Melatonin levels were reduced throughout the duration of bright light exposure for all women. Caffeine reduced the onset of melatonin levels for women in the luteal phase, but it had little effect on melatonin levels for oral contraceptive users. The results for women in the luteal phase of the menstrual cycle are consistent with our previous findings in men. The results also suggest that oral contraceptives may alter the effects of caffeine on nighttime melatonin levels.

  11. Contraception in the 1990s.

    PubMed

    Shoupe, D

    1996-06-01

    Contraceptive technology has recently provided the market place with new barrier methods, new progestin oral contraceptives, an injectable contraceptive, the female condom, new male condoms, and the contraceptive implant. During the last decade, epidemiologists have clearly defined the non-contraceptive benefits of current contraceptive methods that include decreased infections, protection from various cancers, protection from many gynecologic problems that lead to surgery, as well as symptomatic relief from many gynecologic conditions. In conjunction with medical specialists, contraceptive researchers have established the increased safety and benefits of various contraceptive choices in women with medical conditions that, until recently, were contra-indications for their use. That these advances have occurred despite multiple legal and scientific assaults gives hope that the field will continue to grow. PMID:8818532

  12. Exposure to combined oral contraceptives and risk of venous thromboembolism: a protocol for nested case–control studies using the QResearch and the CPRD databases

    PubMed Central

    Vinogradova, Yana; Coupland, Carol; Hippisley-Cox, Julia

    2014-01-01

    Introduction Many studies have found an increased risk of venous thromboembolism (VTE) associated with the use of combined hormonal contraceptives, but various methodologies have been used in the study design relating to definition of VTE event and the selection of appropriate cases for analysis. This study will focus on common oral hormonal contraceptives, including compositions with cyproterone because of their contraceptive effect and will perform a number of sensitivity analyses to compare findings with previous studies. Methods and analysis 2 nested case–control studies will be based on the general population using records from UK general practices within the QResearch and Clinical Practice Research Datalink databases. Cases will be female patients aged 15–49 with primary VTE diagnosed between 2001 and 2013. Each case will be matched by age, year of birth and practice to five female controls, who are alive and registered with the practice at the time of diagnosis of the case (index date). Exposure to different hormonal contraceptives will be defined as at least one prescription for that contraceptive in the year before the index date. The effects of duration and the length of any gap since last use will also be investigated. Conditional logistic regression will be applied to calculate ORs adjusted for smoking, ethnicity, comorbidities and use of other medications. Possible indications for prescribing hormonal contraceptives, such as menstrual disorders, acne or hirsutism will be included in the analyses as confounding factors. A number of sensitivity analyses will be carried out. Ethics and dissemination The initial protocol has been reviewed and approved by ISAC (Independent Scientific Advisory Committee) for Medicine and Healthcare Products Regulatory Agency Database Research. The project has also been reviewed by QResearch and meets the requirements of the Trent Research Ethics Committee. The results will be published in a peer-reviewed journal. PMID

  13. Use of combined oral contraceptives and risk of venous thromboembolism: nested case-control studies using the QResearch and CPRD databases

    PubMed Central

    Coupland, Carol; Hippisley-Cox, Julia

    2015-01-01

    Objective To investigate the association between use of combined oral contraceptives and risk of venous thromboembolism, taking the type of progestogen into account. Design Two nested case-control studies. Setting General practices in the United Kingdom contributing to the Clinical Practice Research Datalink (CPRD; 618 practices) and QResearch primary care database (722 practices). Participants Women aged 15-49 years with a first diagnosis of venous thromboembolism in 2001-13, each matched with up to five controls by age, practice, and calendar year. Main outcome measures Odds ratios for incident venous thromboembolism and use of combined oral contraceptives in the previous year, adjusted for smoking status, alcohol consumption, ethnic group, body mass index, comorbidities, and other contraceptive drugs. Results were combined across the two datasets. Results 5062 cases of venous thromboembolism from CPRD and 5500 from QResearch were analysed. Current exposure to any combined oral contraceptive was associated with an increased risk of venous thromboembolism (adjusted odds ratio 2.97, 95% confidence interval 2.78 to 3.17) compared with no exposure in the previous year. Corresponding risks associated with current exposure to desogestrel (4.28, 3.66 to 5.01), gestodene (3.64, 3.00 to 4.43), drospirenone (4.12, 3.43 to 4.96), and cyproterone (4.27, 3.57 to 5.11) were significantly higher than those for second generation contraceptives levonorgestrel (2.38, 2.18 to 2.59) and norethisterone (2.56, 2.15 to 3.06), and for norgestimate (2.53, 2.17 to 2.96). The number of extra cases of venous thromboembolism per year per 10 000 treated women was lowest for levonorgestrel (6, 95% confidence interval 5 to 7) and norgestimate (6, 5 to 8), and highest for desogestrel (14, 11 to 17) and cyproterone (14, 11 to 17). Conclusions In these population based, case-control studies using two large primary care databases, risks of venous thromboembolism associated with combined oral

  14. Emergency Contraception

    MedlinePlus

    ... contraception are available: emergency contraceptive pills and the copper-containing intrauterine device (IUD). Emergency contraceptive pills include ... for emergency use, talk to your doctor. The copper-containing IUD (brand name: Paragard) is a small, ...

  15. Emergency Contraception

    MedlinePlus

    f AQ FREQUENTLY ASKED QUESTIONS FAQ114 CONTRACEPTION Emergency Contraception • What is emergency contraception (EC)? • How does EC work? • What are the different types of EC? • What is the most ...

  16. Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram.

    PubMed

    Ramadhani, Nisrina; Shabir, Mehwish; McConville, Christopher

    2014-11-20

    The oral route of administration is the most common and preferred route of drug delivery due to its ease of administration, cost-effectiveness and flexibility in design. However, limited aqueous solubility of the active pharmaceutical ingredient can result in poor bioavailability, which is a major issue for the pharmaceutical industry. Increasing numbers of new drugs are falling into class II of the Biopharmaceutical Classification System (BCS), where they have a low solubility and high tissue permeability, meaning that bioavailability is solubility dependent. Here we demonstrate the development and characterisation of solid dispersion oral tablets, containing the poorly water-soluble drug disulfiram, prepared using both the hot melt and solvent evaporation methods and manufactured from two different polymers, Kolliphor(®) P 188 and P 237, specifically designed for the manufacture of solid dispersions. This paper demonstrates that the disulfiram solid dispersions tablets have an enhanced release rate of disulfiram compared to the control tablets. The Kolliphor(®) P 188 polymer control tablets released approximately 48.8% of their disulfiram content over 8h, with the solvent evaporated tablets releasing approximately 65.8%, while the 60 and 80 °C hot melt tablets released approximately 73.2 and 100% of their disulfiram content respectively. A similar trend was seen with Kolliphor(®) P 237 as the control tablets released approximately 50.5% of their disulfiram content over 8h, while the solvent evaporated tablets released approximately 79.5% and the 60 and 80 °C hot melt tablets released 100.2 and 100.3% respectively. Depending on what method and polymer is used to manufacture the solid dispersions the disulfiram is either maintained completely or partially in its amorphous state and it is this which enhances its solubility and release rate from the tablets. The disulfiram in the Kolliphor(®) P 188 solvent evaporated and 60 °C hot melt tablets retained 50

  17. Preparation of Orally Disintegrating Tablets Containing Powdered Tea Leaves with Enriched Levels of Bioactive Compounds by Means of Microwave Irradiation Technique.

    PubMed

    Tanaka, Hironori; Iwao, Yasunori; Izumikawa, Masahiro; Sano, Syusuke; Ishida, Hitoshi; Noguchi, Shuji; Itai, Shigeru

    2016-01-01

    In the present study, a microwave treatment process has been applied to prepare orally disintegrating tablets (ODTs) containing powdered tea leaves with enriched levels of the anti-inflammatory compounds such as chafuroside A (CFA) and chafuroside B (CFB). The use of distilled water as the adsorbed and granulation solvents in this preparation process afforded tablets with a long disintegration time (more than 120 s). The CFA and CFB contents of these tablets did not also change after 4 min of microwave irradiation due to the tablet temperature, which only increased to 100°C. In contrast, the tablet temperature increased up to 140°C after 3 min of microwave irradiation when a 1.68 M Na2HPO4 solution instead of distilled water. Notably, the disintegration time of these tablets was considerably improved (less than 20 s) compared with the microwave-untreated tablets, and there were 7- and 11-fold increases in their CFA and CFB contents. In addition, the operational conditions for the preparation of the tablets were optimized by face-centered composite design based on the following criteria: tablet hardness greater than 13 N, disintegration time less than 30 s and friability less than 0.5%. The requirements translated into X1 (the amount of granulation solvent), X2 (tableting pressure) and X3 (content of the powdered tea leaves) values of 45%, 0.43 kN and 32%, respectively, and the ODTs containing powdered tea leaves prepared under these optimized conditions were found to show excellent tablet properties and contain enriched levels of CFA and CFB. PMID:27581633

  18. Effect of the oral contraceptive pill on protein S and antithrombin-III levels in Malaysian women.

    PubMed

    Wong, K K; Ng, S C; Koong, P L

    Studies focusing on the relationship between oral contraceptive (OC) usage and occurrence of thromboembolism have been conducted for over 3 decades. Those studies centered on the effects OC use has on blood proteins and on measurable physiological changes that occurred in women with venous thrombosis. This article reports the findings of a study that investigated the effects of OC use on the levels of the anticoagulants antithrombin-III (AT-III), protein C (PC), and protein S (PS) in a group of Asian women. Previous studies had mostly been based on Caucasian women. Of the 21 women studied, 16 were Malaysian, 3 were Chinese, and 2 were Indian. Low-dose OCs containing 30 mcg of ethinyl estradiol and 150 mcg of either desogestrel or levonorgestrel were used. Blood was tested before OC use and 3 and 6 months after starting OC use. Levels of AT-III and PS were measured using the Laurell rocket immunoelectrophoresis technique. Statistical analysis was performed using the paired Student's t-test and an analysis of variance test. No statistically significant differences were found for the mean levels of AT-III and total PS when comparing the pre-OC with the 3- and 6-month post-OC values. Earlier studies based mostly on Caucasian women have reported lower levels of both total PS and free PS in OC users. PMID:12288974

  19. Oral contraceptive use and breast cancer in young women. A joint national case-control study in Sweden and Norway.

    PubMed

    Meirik, O; Lund, E; Adami, H O; Bergström, R; Christoffersen, T; Bergsjö, P

    1986-09-20

    The possible association between oral contraceptive (OC) use and the risk of breast cancer developing before the age of 45 was investigated by means of a population based case-control study in Sweden and Norway. Information was obtained by personal interview from 422 (89.2%) of all eligible patients with a newly diagnosed breast cancer from May, 1984, to May, 1985, and from 722 (80.6%) of all contacted age-matched controls. A multivariate analysis, which accounted for several possible confounding factors, revealed a significant (p = 0.03) association between total duration of OC use and breast cancer risk. The relative risk (RR) of breast cancer after 12 or more years of OC use was 2.2 (1.2-4.0). OC use for more than 7 years before first full-term pregnancy entailed an increased breast cancer risk (RR = 2.0 [1.0-4.2]) which was of borderline significance. When total duration of use was considered, the risk of breast cancer was virtually unrelated to age at first OC use and latency from first use. The results suggest that long-term use of OCs may increase the risk of breast cancer in young women. PMID:2876135

  20. Hormone replacement therapy and oral contraceptives and risk of oesophageal adenocarcinoma: a systematic review and meta-analysis.

    PubMed

    Lagergren, Katarina; Lagergren, Jesper; Brusselaers, Nele

    2014-11-01

    There is an unexplained strong male predominance in the aetiology of oesophageal adenocarcinoma (OAC). The hypothesis that oestrogens are protective, deserves attention. A potential protective influence of exogenous oestrogen exposure, that is, hormone replacement therapy (HRT) and oral contraceptives (OC) has been addressed only in studies of limited statistical power, and the individual studies have not provided conclusive results. We conducted a systematic literature search and meta-analysis on HRT and OC and the risk of OAC. We used the databases PubMed and the Web of Science. Odds ratios (ORs) and 95% confidence intervals (CIs) were estimated by the Mantel-Haenszel random-effect method. A total of five studies were included. Compared to never users, ever users of HRT had a statistically significantly decreased risk of OAC (pooled OR = 0.75; 95% CI: 0.58-0.98), and ever users of OC had a borderline significantly decreased risk of this cancer (pooled OR = 0.76; 95% CI: 0.57-1.00). In conclusion, HRT and OC use seems to be associated with a decreased risk of OAC. However, further research is warranted. PMID:24676860

  1. A Comparison of Self-reported Oral Contraceptive Use and Automated Pharmacy Data in Peri- and Early Postmenopausal Women

    PubMed Central

    Spangler, Leslie; Ichikawa, Laura; Hubbard, Rebecca; Operskalski, Belinda; LaCroix, Andrea; Ott, Susan; Scholes, Delia

    2014-01-01

    Purpose Oral contraceptive (OC) use can occur throughout a woman’s reproductive lifespan with the potential for long- term impacts on health. To assess potential measurement error in prior OC use, this study compared level of agreement between self-reported prior OC use and pharmacy dispensing data in peri-/early postmenopausal women. Methods The study’s 1,399 women (ages 45–59 years) were participants in a population based case-control study of the association between OC use and fracture risk. Episodes of lifetime self-reported OC use (in months) were collected, by telephone interview, for 1/1/2008 through 11/25/2012. Pharmacy fills, back to 1980, were collected from automated data. Agreement was measured using the Prevalence Adjusted and Bias Adjusted Kappa Index (PABAK). Results The number of women with OC pharmacy fills was 11–45% higher than those who reported OC use during each time period. Between-measures agreement was better for more recent use. PABAK values ranged from 0.88 (95% CI 0.85–0.90) within 5 years from the reference date to 0.65 (95% CI 0.59–0.71) within 15–20 years. Conclusion For studies designed to assess the long term effects of OC use, the current results are reassuring in noting moderate agreement between self-reported OC use and pharmacy data for up to 15–20 years before the interview. PMID:25453353

  2. Combined Oral Contraception and Obesity Are Strong Predictors of Low-Grade Inflammation in Healthy Individuals: Results from the Danish Blood Donor Study (DBDS)

    PubMed Central

    Sørensen, Cecilie J.; Pedersen, Ole B.; Petersen, Mikkel S.; Sørensen, Erik; Kotzé, Sebastian; Thørner, Lise W.; Hjalgrim, Henrik; Rigas, Andreas S.; Møller, Bjarne; Rostgaard, Klaus; Riiskjær, Mads; Ullum, Henrik; Erikstrup, Christian

    2014-01-01

    Background C-reactive protein (CRP) is a well-established marker of inflammation. The level of CRP is affected by several lifestyle factors. A slightly increased CRP level, also known as low-grade inflammation (LGI), is associated with increased risk of several diseases, especially cardiovascular disease. The aim of this study was to identify predictors of increased CRP levels in healthy individuals. We therefore assessed CRP in a large cohort of blood donors. Methods We measured plasma CRP levels in 15,684 participants from the Danish Blood Donor Study. CRP was measured by a commercial assay. Furthermore, all participants completed a standard questionnaire on smoking status, alcohol consumption, physical activity, diet, and various body measurements. Female participants also reported the use of contraception, childbirth, and menopausal status. The relationship between LGI (defined here as a plasma CRP level between 3 mg/L and 10 mg/L) and predictors was explored by multivariable logistic regression analysis. Results were presented as odds ratios (OR) with 95% confidence intervals (CI). Results We found LGI in a total of 1,561 (10.0%) participants. LGI was more frequent in women using combined oral contraception (OC) (29.9%) than in men (6.1%) and women not using OC (7.9%). Among premenopausal women, OC was the strongest predictor of LGI (odds ratio = 8.98, p<0.001). Additionally, body mass index (BMI) and waist circumference were positively associated with LGI. Conclusion High BMI and abdominal obesity strongly predicted LGI among healthy individuals. However, the most striking finding was the high prevalence of LGI among premenopausal women who used combined oral contraception. Although the significance of CRP as a marker of inflammation is well known, the role of CRP in pathogenesis is still uncertain. The impact of oral contraception on CRP levels should nevertheless be considered when CRP is used in risk assessment. PMID:24516611

  3. Semaglutide, a Once-Weekly Human GLP-1 Analog, Does Not Reduce the Bioavailability of the Combined Oral Contraceptive, Ethinylestradiol/Levonorgestrel

    PubMed Central

    Kapitza, Christoph; Nosek, Leszek; Jensen, Lene; Hartvig, Helle; Jensen, Christine B; Flint, Anne

    2015-01-01

    The effect of semaglutide, a once-weekly human glucagon-like peptide-1 (GLP-1) analog in development for type 2 diabetes (T2D), on the bioavailability of a combined oral contraceptive was investigated. Postmenopausal women with T2D (n = 43) on diet/exercise ± metformin received ethinylestradiol (0.03 mg)/levonorgestrel (0.15 mg) once daily for 8 days before (semaglutide-free) and during (steady-state 1.0 mg) semaglutide treatment (subcutaneous once weekly; dose escalation: 0.25 mg 4 weeks; 0.5 mg 4 weeks; 1.0 mg 5 weeks). Bioequivalence of oral contraceptives was established if 90%CI for the ratio of pharmacokinetic parameters during semaglutide steady-state and semaglutide-free periods was within prespecified limits (0.80–1.25). The bioequivalence criterion was met for ethinylestradiol area under the curve (AUC0–24 h) for semaglutide steady-state/semaglutide-free; 1.11 (1.06–1.15). AUC0–24 h was 20% higher for levonorgestrel at semaglutide steady-state vs. semaglutide-free (1.20 [1.15–1.26]). Cmax was within bioequivalence criterion for both contraceptives. Reductions (mean ± SD) in HbA1c (–1.1 ± 0.6%) and weight (–4.3 ± 3.1 kg) were observed. Semaglutide pharmacokinetics were compatible with once-weekly dosing; the semaglutide dose and dose-escalation regimen were well tolerated. Adverse events, mainly gastrointestinal, were mild to moderate in severity. Asymptomatic increases in mean amylase and lipase were observed. Three subjects had elevated alanine aminotransferase levels ≥3x the upper limit of normal during semaglutide/oral contraceptive coadministration, which were reported as adverse events, but resolved during follow-up. Semaglutide did not reduce the bioavailability of ethinylestradiol and levonorgestrel. PMID:25475122

  4. [Pharmacokinetic study on peoniflorin, astilbin, rosmarinic acid, isofraxidin and liquiritin in rat blood after oral administration of shaolin xiaoyin tablets].

    PubMed

    Zhao, Rui-Zhi; Wang, Yin-Jie; Feng, Li-Min; Lu, Chuan-Jian

    2014-07-01

    To establish a method for the determination of astilbin, peoniflorin, rasmarinci acid, isofraxidin and liquiritin contained in Shaolin Xiaoyin tablets, in order to lay a foundation for designing late-stage dosage forms and clinical medication schemes. In this paper, efforts were made to establish a method for the determination of the blood concentration of the five components and study the in vivo pharmacokinetics in rats. The blood concentration was determined by HPLC. Phenomenex C18 column (4.6 mm x 250 mm, 5 microm) was adopted and eluted with methanol-acetonitrile-0.05% formic acid, the flow rate was 0.8 mL x min(-1), and the wavelength was 275 nm. The samples were processed by the solid phase extraction method. After oral administration of Shaoling Xiaoyin tablets, the rat bloods were collected at different time points to determine the blood concentrations. The experimental results showed that the baseline separation could be adopted for the five components, and astilbin, peoniflorin, rasmarinci acid, isofraxidin and liquiritin showed good linear relations within ranges of 2.48-248, 0.213 6-21.36, 0.531-53.1, 0.704-70.4, 0.253-25.3 mg x L(-1). All the five components could be absorbed in blood and excreted quickly. The method established in this paper is rapid and accurate, and could be used for in vivo analysis on preparations containing similar components. The main components in Shaoling Xiaoyin tablets could be absorbed and excreted quickly, and thus suitable to be made into sustained release tablets. Common preparations are required to be taken for 4-6 times a day. PMID:25276982

  5. Views and attitudes of oral contraceptive users towards their availability without a prescription in the Republic of Ireland

    PubMed Central

    Barlassina, Luigi

    2015-01-01

    Background: Previous studies show that provision of oral contraceptive pill (OCs) without a prescription is safe, feasible and effective and that users are interested in obtaining contraception in this way, especially if a pharmacist screening is involved. A recent national survey conducted in the Republic of Ireland has highlighted that unintended pregnancy resulting from the failure of OCs could be linked to poor compliance due to costs and difficulty of access. Objective: To evaluate views and attitudes of OC users towards the availability of OCs without a prescription in the Republic of Ireland. Methods: A cross sectional survey was conducted using an opportunistic sample of OC users aged 18 to 50 years. Sixty community pharmacists were recruited nationwide. Data were collected using self-completed questionnaires. The questionnaires comprised information on: demographic data, need of the service, views on the availability of OCs without prescription, advantages and concerns around the service, role of pharmacists and cost implications for private and public patients. Results: A total of 488 eligible OC users completed the survey. The majority of the respondents (71.7%;n = 350/488) reported to have missed a pill for reasons connected to the OCs prescription status and 55.5% (n = 268/488) of the respondents reported to have felt distressed on at least one occasion because they could not renew their OC prescription. A total of 87.9% (n = 429/488) of the respondents said they were in favour of OCs being available without prescription and 92% (n = 448/488) said they were likely to obtain OCs without prescription if available. Convenience and ease of access were indicated as the main advantages of availing of OCs without prescription, while safety was the biggest concern reported. Over 88% (n = 430/488) of the respondents indicated that pharmacists would be able to safely supply OCs without prescription. Private patients expected to save an average of 27.3% on their

  6. A prospective, open-label, single arm, multicentre study to evaluate efficacy, safety and acceptability of pericoital oral contraception using levonorgestrel 1.5 mg

    PubMed Central

    Festin, Mario P.R.; Bahamondes, Luis; Nguyen, Thi My Huong; Habib, Ndema; Thamkhantho, Manopchai; Singh, Kuldip; Gosavi, Arundhati; Bartfai, Gyorgy; Bito, Tamas; Bahamondes, M. Valeria; Kapp, Nathalie

    2016-01-01

    STUDY QUESTION Will the use of levonorgestrel (LNG) 1.5 mg taken at each day of coitus by women who have relatively infrequent sex be an efficacious, safe and acceptable contraceptive method? SUMMARY ANSWER Typical use of LNG 1.5 mg taken pericoitally, before or within 24 h of sexual intercourse, provides contraceptive efficacy of up to 11.0 pregnancies per 100 women-years (W-Y) in the primary evaluable population and 7.1 pregnancies per 100 W-Y in the evaluable population. WHAT IS KNOWN ALREADY LNG 1.5 mg is an effective emergency contraception following unprotected intercourse. Some users take it repeatedly, as their means of regular contraception. STUDY DESIGN, SIZE, DURATION This was a prospective, open-label, single-arm, multicentre Phase III trial study with women who have infrequent coitus (on up to 6 days a month). Each woman had a follow-up visit at 2.5, 4.5 and 6.5 months after admission or until pregnancy occurs if sooner, or she decided to interrupt participation. The study was conducted between 10 January 2012 and 15 November 2014. PARTICIPANTS/MATERIALS, SETTING, METHODS A total of 330 healthy fertile women aged 18–45 years at risk of pregnancy who reported sexual intercourse on up to 6 days a month, were recruited from four university centres located in Bangkok, Thailand; Campinas, Brazil; Singapore and Szeged, Hungary to use LNG 1.5 mg pericoitally (24 h before or after coitus) as their primary method of contraception. The participants were instructed to take one tablet every day she had sex, without taking more than one tablet in any 24-h period, and to maintain a paper diary for recording date and time for every coital act and ingestion of the study tablet, use of other contraceptive methods and vaginal bleeding patterns. Anaemia was assessed by haemoglobin evaluation. Pregnancy tests were performed monthly and pregnancies occurring during product use were assessed by ultrasound. At the 2.5-month and final visit at 6.5 months, acceptability

  7. Unexpected sequelae of contraception.

    PubMed

    Dunn, H P

    1996-01-01

    Dissident Roman Catholic theologians who promote the use of contraception have ignored the fact that contraception separates the loving aspect of sex from its fertile nature (which does not imply fecundity). While there is no obligation for Roman Catholics to achieve pregnancy, no interference with fertility is allowed. The importance of this seeming technicality can be seen when considering that contraception offers sex without babies and in vitro fertilization allows babies to be conceived without sexual intercourse. Barrier methods of contraception make sexual intercourse impure in a way similar to masturbation, oral contraceptives generally suppress ovulation but may also act as an abortifacient, and the IUD is an abortifacient, as are other hormonal methods and menstrual extraction. Sterilization and abortion are serious moral faults. Contraception is the first step towards the prevailing antinatalism that will cause demographic collapse in rich countries because there is a progression from contraception to sterilization to abortion. Rather than leading to fewer abortions, acceptance of contraception leads to more. This distressing sequence can be extended to include masturbation at one end and homosexuality at the other. Acceptance of contraception encourages all premarital and extramarital sexual intercourse and has depreciated the value of marriage. Rejection of child-bearing has exacerbated the estrangement of teenagers from parents who chose sterile sex and money over siblings for their children. Contraception fuels fears about a population explosion when people should be regarded as important resources. Finally, contraception has contributed to the shortage of those choosing religious vocations because it has demeaned their sacrifice of celibacy. The only permitted method of family limitation, therefore, is ovulation detection. PMID:12320545

  8. [Topical contraceptives].

    PubMed

    Alipov, V I; Korkhov, V V

    1982-02-01

    Recently there has been little interest in topical contraceptives. The most popular are the cervical cap and the diaphragm. Other types of mechanical contraceptive devices are being investigated. Standley and Kessler have developed a device for introduction into the cervical canal with a reservoir of spermatocide, it does not block the flow of blood during menstruation. New models of vaginal rings are also being developed which are simple enough for self-insertion and also contain a reservoir of spermatocide. Work is being done on spermatocide-containing sponges in many countries. Another project being investigated is the possibility of using natural proteins, collagens, and other substances which absorb spermatozoids. The ancients used various vaginal suppositories to kill spermatozoids; in the late 19th century quinine sulfate was used for this, and a variety of substances have been used recently. These spermicidal creams also have the advantage of acting as anti-infectious agents in many cases. But they do have some negative effects. They are about 85% effective, are local irritants, and some cause discomfort during intercourse. And it is possible that some are resorbed by the body and act on the liver and other organs. Vaginal globules and suppositories are also popular. The "Kontraceptin-T" brand contains quinosol, boric acid, and tannin. There are also foaming tablets which are mixed with water and then introduced. New locally-active chemical substances are being developed in Japan, West Germany, and the USSR. Kontraceptin-E contains paranonyl-phenoxypolyethylene glycol and sodium dioctylsulfosuccinate. The "Norforks" and other preparations contain mercurial compounds which may turn out to be harmful. The future promises the development of products which will act to prevent fertilization by acting on the hyaluronidase and the acrosine of the spermatozoid, thus preventing it from penetrating the ovum. It would be best to find enzyme inhibitors which are

  9. [Contraception and obesity].

    PubMed

    Lobert, M; Pigeyre, M; Gronier, H; Catteau-Jonard, S; Robin, G

    2015-11-01

    The prevalence of obesity is increasing massively over several decades in industrialized countries. Obese women are sexually active but they use fewer contraceptive methods and are at high risk of unintended pregnancy. In addition, obesity is an important risk factor for venous thromboembolism events and arterial thrombosis (myocardial infarction and ischemic stroke). All of these data are to be considered in choosing a contraceptive method for obese women. Except depot medroxyprogesterone acetate injection, the progestin-only contraceptives (progestin only pills and etonogestrel subdermal implant) and the intra-uterine devices are the preferred contraceptive methods in obese women. The combined estrogen-progestin contraceptives (pill, patch and vaginal ring) may be proposed in very strict conditions (no other associated vascular risk factor). Obesity does not increase the risk of failure of most contraceptive methods. Bariatric surgery is a complex situation. It requires to program a possible pregnancy and contraception is needed for several months. Some bariatric surgical techniques such as by-pass can induce gastrointestinal malabsorption. In this situation, all oral contraceptives are not recommended because of a higher risk of failure. PMID:26527416

  10. Albizia procera gum as an excipient for oral controlled release matrix tablet.

    PubMed

    Pachuau, Lalduhsanga; Mazumder, Bhaskar

    2012-09-01

    The purpose of this research was to develop and evaluate controlled release matrix tablets of paracetamol based on natural gum exudates of Albizia procera. Procera gum was characterized of its properties like compressibility index, angle of repose, viscosity and moisture content. The interaction between the gum and paracetamol was also studied through differential scanning calorimetry (DSC) and FTIR spectroscopy. Matrix tablets were then prepared by wet granulation method with different concentrations of procera gum and hydroxypropyl methylcellulose (HPMC) and evaluated for their physical properties like weight variation, hardness, friability and content uniformity. Dissolution study was conducted to characterize release mechanism from the matrix system and data were fitted to various kinetic models. The mechanism of drug release from both types of matrix tablets was found to be anomalous type. Results from various evaluations suggested that A. procera gum could be used as drug release retardant in controlled release matrix systems. PMID:24751043

  11. Users of withdrawal method in the Islamic Republic of Iran: are they intending to use oral contraceptives? Applying the theory of planned behaviour.

    PubMed

    Rahnama, P; Hidarnia, A; Shokravi, F A; Kazemnejad, A; Montazeri, A; Najorkolaei, F R; Saburi, A

    2013-09-01

    Many couples in the Islamic Republic of Iran rely on coital withdrawal for contraception. The purpose of this cross-sectional study was to use the theory of planned behaviour to explore factors that influence withdrawal users' intent to switch to oral contraception (OC). Participants were 336 sexually active, married women, who were current users of withdrawal and were recruited from 5 public family planning clinics in Tehran. A questionnair included measures of the theory of planned behaviour: attitude (behavioural beliefs, outcome evaluations), subjective norms (normative beliefs, motivation to comply), perceived behaviour control, past behaviour and behavioural intention. Linear regression analyses showed that past behaviour, perceived behaviour control, attitude and subjective norms accounted for the highest percentage of total variance observed for intention to use OC (36%). Beliefs-based family planning education and counsellingshould to be designed for users of the withdrawal method. PMID:24313039

  12. Development and Efficacy Assessment of an Enteric Coated Porous Tablet Loaded With F4 Fimbriae for Oral Vaccination of Piglets against F4+ Escherichia coli Infections.

    PubMed

    Srivastava, Atul; Gowda, D V; Madhunapantula, SubbaRao V; Siddaramaiah

    2016-01-01

    Enterotoxigenic Escherichia coli (ETEC) infection is one of the major causes contributing to the development of diarrhoea and mortality in new born, suckling and newly weaned piglets. To date, no preventive/treatment strategy showed promising results, which could be due to the lack of potent vaccines, and/or due to the development of resistance of ETEC to antibiotics. Therefore, in the present investigation, a novel porous sodium alginate (SA) tablet formulation loaded with F4 fimbriae antigen was developed and tested for efficacy against ETEC infections in piglet models. Precompression parameters of the powder mixes and post compression parameters of tablets have been evaluated and results were found to be satisfactory. Loading of F4 fimbrial antigens into the tablets was achieved by inducing pores in the tablets via the sublimation of camphor followed by incubation with purified F4 fimbriae. The loaded tablets have been coated with Eudragit L100 to protect the F4 fimbriae from (a) highly acidic gastric environment; (b) proteolytic cleavage by pepsin; and (c) to promote subsequent release in the intestine. Evaluation of developed F4 fimbrial tablets in a Pig model demonstrated induction of mucosal immunity, and a significant reduction of F4+ E. coli in faeces. Therefore, F4 fimbriae loaded porous tablets could be a novel oral vaccination candidate to induce mucosal and systemic immunity against ETEC infections. PMID:26212139

  13. Contraception in Turkey.

    PubMed

    1967-01-01

    Population control and the use of contraceptives were discusses at the biannual meeting of the Turkish Academy of Medicine in September 1966. This was of special importance because contraception and dissemination of information about it were illegal in Turkey for many years before 1965. Thus, until quite recently Turkish doctors had only limited experience of modern contraceptive methods. Oral contraceptives and IUDs were discussed at the Academy meeting, and Dr Nusret Fisek has sent the Bulletin a summary of the main points raises. Oral contraceptives: Only minor side-effects were found and were ignored or easily treated; they disappeared when the oral contraception was stopped. Serious conditions such as liver dysfunction, thromboembolic phenomena, and diabetes have not been found. Intra-uterine devices: Endometritis requiring treatment is infrequent. In 23 of 45 women who had used IUDs for six months, endometrial histology showed diffuse bleeding, endometrial oedema or lymphocyctic endometritis. Expulsion and medical removal rates for IUDs over a six-month period were 5% in one clinic and 12% in another, with a pregnancy rate of between 1.2%. There was only one perforation in 6000 insertions. The doctor's attitude had a great influence on removal and discontinuation rates. In a large maternity hospital the Medical Board accepted, as a medical reason for induced abortion, accidental pregnancies that occurred in women wearing IUDs. PMID:12304991

  14. Effect of the hepatitis C virus protease inhibitor faldaprevir on the pharmacokinetics of an oral contraceptive containing ethinylestradiol and levonorgestrel in healthy female volunteers.

    PubMed

    Sabo, John P; Lang, Benjamin; Elgadi, Mabrouk; Huang, Fenglei

    2015-01-01

    Faldaprevir is a potent hepatitis C virus (HCV) NS3/4A protease inhibitor. Faldaprevir is known to inhibit P-glycoprotein, CYP3A4, and UDP-glucuronosyltransferase 1A1. This study evaluated the effect of steady-state 240 mg faldaprevir on the pharmacokinetics (PK) of an oral contraceptive containing ethinylestradiol (EE) and levonorgestrel (LNG) in healthy premenopausal women. In period 1, subjects received EE/LNG once daily (QD) for 14 days. Blood samples were taken on days 1, 11, and 12, with intensive PK blood sampling for EE and LNG on day 13. In period 2, subjects received EE-LNG QD and 240 mg faldaprevir QD on days 14 to 21 (240 mg faldaprevir twice daily on day 14). Blood samples were taken on days 14, 19, and 20, with PK profiling samples obtained for EE and LNG on day 21. A total of 15/16 subjects completed the study. Overall, EE and LNG exposure (assessed by the area under the curve) was approximately 1.4-fold higher when EE and LNG were coadministered with faldaprevir than when administered alone. Median t1/2 (terminal half-life in plasma at steady state) values were prolonged for both EE (2.4 h longer) and LNG (4.7 h longer) when EE and LNG were coadministered with faldaprevir. The mean oral clearance and apparent volume of distribution of both EE and LNG were lower (∼ 30%) when EE and LNG were coadministered with faldaprevir. Coadministration of faldaprevir and an oral contraceptive resulted in a moderate increase in exposure to both EE and LNG. However, this increase was not considered clinically meaningful, and no dose adjustment of oral contraceptives was deemed necessary. (This study has been registered at ClinicalTrials.gov under registration number NCT01570244.). PMID:25385099

  15. Obesity and hormonal contraceptive efficacy

    PubMed Central

    Robinson, Jennifer A; Burke, Anne E

    2014-01-01

    Obesity is a major public health concern affecting an increasing proportion of reproductive-aged women. Avoiding unintended pregnancy is of major importance, given the increased risks associated with pregnancy, but obesity may affect the efficacy of hormonal contraceptives by altering how these drugs are absorbed, distributed, metabolized or eliminated. Limited data suggest that long-acting, reversible contraceptives maintain excellent efficacy in obese women. Some studies demonstrating altered pharmacokinetic parameters and increased failure rates with combined oral contraceptives, the contraceptive patch and emergency contraceptive pills suggest decreased efficacy of these methods. It is unclear whether bariatric surgery affects hormonal contraceptive efficacy. Obese women should be offered the full range of contraceptive options, with counseling that balances the risks and benefits of each method, including the risk of unintended pregnancy. PMID:24007251

  16. Aesthetic and incentive salience of cute infant faces: studies of observer sex, oral contraception and menstrual cycle.

    PubMed

    Sprengelmeyer, Reiner; Lewis, Jennifer; Hahn, Amanda; Perrett, David I

    2013-01-01

    Infant cuteness can influence adult-infant interaction and has been shown to activate reward centres in the brain. In a previous study, we found men and women to be differentially sensitive to small differences in infant facial cuteness, with reproductive hormone status as the potential underlying cause. It is unclear, however, whether reproductive hormone status impacts on the aesthetic and incentive salience of infant faces. To address this question, we conducted two interlinked studies. We used static images of the same smiling and neutral-looking infant faces in both a rating task, in which participants had to rate the cuteness of infant faces (aesthetic salience - 'liking'), and a key-press task, in which participants could prolong or shorten viewing time of infant faces by rapid alternating key-presses (incentive salience - 'wanting'). In a first study, we compared the performance of men, women who are taking oral contraceptives, and regularly cycling women. In this study, we found a significant correlation between cuteness ratings within and between groups, which implies that participants had the same concept of cuteness. Cuteness ratings and effort to look at faces was linked regardless of sex and reproductive hormone status, in that cute faces were looked at for longer than less cute faces. A happy facial expression contributed only marginally to the incentive salience of the face. To explore the potential impact of reproductive hormone status in more detail, we followed a subset of regularly cycling women during the menstrual, follicular and luteal phases of their cycle. The aesthetic and incentive salience of infant faces did not change across the menstrual cycle. Our findings suggest that reproductive hormone status does not modulate the aesthetic and incentive value of infant faces. PMID:23734262

  17. The Effect of Combination Oral Contraceptives on Smoking-Related Symptomatology during Short-Term Smoking Abstinence

    PubMed Central

    Hinderaker, Katie; Tosun, Nicole; al'Absi, Mustafa; Hatsukami, Dorothy; Allen, Sharon S.

    2014-01-01

    Although an estimated 25% of premenopausal smokers report using oral contraceptives (OC), little is known about how OC use may influence smoking cessation. The purpose of this study was to examine the difference in smoking-related symptomatology during acute smoking abstinence between women on a standardized combination OC (Tri-Sprintec ™) compared to women not on OCs (no-OC). Participants were women aged 18-40 who smoked ≥5 cigarettes/day and reported regular menstrual cycles. Using a controlled cross-over design, participants completed two six-day testing weeks: Low Progesterone Week (LPW; Follicular (F) phase in no-OC or 1st week of pills in OC) and High Progesterone Week (HPW; Luteal (L) phase in no-OC or 3rd week of pills in OC). Each testing week included daily assessment of symptomatology and biochemical confirmation of smoking status. During smoking abstinence, the OC group (n=14) reported significantly lower levels of positive affect (21.56±7.12 vs. 24.57±6.46; β=3.63, p=0.0323) than the no-OC group (n=28). Further significant interactions between group and testing week were observed as follows: Smoking satisfaction was higher during LPW in the OC group (LPW: 4.29±1.30 vs. HPW: 4.10±1.37) but higher during HPW in the no-OC group (LPW: 3.91 ± 1.30 vs. HPW: 4.23 ± 1.30; β=-0.5499, p<0.0001). Similar interactions were noted in negative affect and psychological reward of smoking. These results suggest that women on OCs may have different patterns of smoking-related symptomatology during short-term smoking abstinence as compared to women not on OCs. Additional work is needed to examine how this may affect smoking cessation efforts. PMID:25452059

  18. The effect of combination oral contraceptives on smoking-related symptomatology during short-term smoking abstinence.

    PubMed

    Hinderaker, Katie; Allen, Alicia M; Tosun, Nicole; al'Absi, Mustafa; Hatsukami, Dorothy; Allen, Sharon S

    2015-02-01

    Although an estimated 25% of premenopausal smokers report using oral contraceptives (OC), little is known about how OC use may influence smoking cessation. The purpose of this study was to examine the difference in smoking-related symptomatology during acute smoking abstinence between women on a standardized combination OC (Tri-Sprintec(™)) compared to women not on OCs (no-OC). Participants were women aged 18-40 who smoked ≥5 cigarettes/day and reported regular menstrual cycles. Using a controlled cross-over design, participants completed two six-day testing weeks: Low Progesterone Week (LPW; Follicular (F) phase in no-OC or 1st week of pills in OC) and High Progesterone Week (HPW; Luteal (L) phase in no-OC or 3rd week of pills in OC). Each testing week included daily assessment of symptomatology and biochemical confirmation of smoking status. During smoking abstinence, the OC group (n=14) reported significantly lower levels of positive affect (21.56±7.12 vs. 24.57±6.46; β=3.63, p=0.0323) than the no-OC group (n=28). Further significant interactions between group and testing week were observed as follows: Smoking satisfaction was higher during LPW in the OC group (LPW: 4.29±1.30 vs. HPW: 4.10±1.37) but higher during HPW in the no-OC group (LPW: 3.91±1.30 vs. HPW: 4.23±1.30; β=-0.5499, p<0.0001). Similar interactions were noted in negative affect and psychological reward of smoking. These results suggest that women on OCs may have different patterns of smoking-related symptomatology during short-term smoking abstinence as compared to women not on OCs. Additional work is needed to examine how this may affect smoking cessation efforts. PMID:25452059

  19. Risk factors for venous thromboembolism in women under combined oral contraceptive. The PILl Genetic RIsk Monitoring (PILGRIM) Study.

    PubMed

    Suchon, Pierre; Al Frouh, Fadi; Henneuse, Agathe; Ibrahim, Manal; Brunet, Dominique; Barthet, Marie-Christine; Aillaud, Marie-Françoise; Venton, Geoffroy; Alessi, Marie-Christine; Trégouët, David-Alexandre; Morange, Pierre-Emmanuel

    2016-01-01

    Identifying women at risk of venous thromboembolism (VTE) is a major public health issue. The objective of this study was to identify environmental and genetic determinants of VTE risk in a large sample of women under combined oral contraceptives (COC). A total of 968 women who had had one event of VTE during COC use were compared to 874 women under COC but with no personal history of VTE. Clinical data were collected and a systematic thrombophilia screening was performed together with ABO blood group assessment. After adjusting for age, family history, and type and duration of COC use, main environmental determinants of VTE were smoking (odds ratio [OR] =1.65, 95% confidence interval [1.30-2.10]) and a body mass index higher than 35 kg.m⁻² (OR=3.46 [1.81-7.03]). In addition, severe inherited thrombophilia (OR=2.13 [1.32-3.51]) and non-O blood groups (OR=1.98 [1.57-2.49]) were strong genetic risk factors for VTE. Family history poorly predicted thrombophilia as its prevalence was similar in patients with or without first degree family history of VTE (29.3% vs 23.9%, p=0.09). In conclusion, this study confirms the influence of smoking and obesity and shows for the first time the impact of ABO blood group on the risk of VTE in women under COC. It also confirms the inaccuracy of the family history of VTE to detect inherited thrombophilia. PMID:26290123

  20. Effect of administration of oral contraceptives in vivo on collagen synthesis in tendon and muscle connective tissue in young women.

    PubMed

    Hansen, M; Miller, B F; Holm, L; Doessing, S; Petersen, S G; Skovgaard, D; Frystyk, J; Flyvbjerg, A; Koskinen, S; Pingel, J; Kjaer, M; Langberg, H

    2009-04-01

    Women are at greater risk than men for certain kinds of diseases and injuries, which may at least partly be caused by sex hormonal differences. We aimed to test the influence of estradiol in vivo on collagen synthesis in tendon, bone, and muscle. Two groups of young, healthy women similar in age, body composition, and exercise-training status were included. The two groups were either habitual users of oral contraceptives exposed to a high concentration of synthetic estradiol and progestogens (OC, n = 11), or non-OC-users tested in the follicular phase of the menstrual cycle characterized by low concentrations of estradiol and progesterone (control, n = 12). Subjects performed 1 h of one-legged kicking exercise. The next day collagen fractional synthesis rates (FSR) in tendon and muscle connective tissue were measured after a flooding dose of [(13)C]proline followed by biopsies from the patellar tendon and vastus lateralis in both legs. Simultaneously, microdialysis catheters were inserted in vastus lateralis and in front of the patellar tendon for measurement of insulin-like growth factor I (IGF-I) and its binding proteins. Serum NH(2)-terminal propeptide of type I collagen (PINP) and urine COOH-terminal telopeptides of type-I collagen (CTX-I) were measured as markers for bone synthesis and breakdown, respectively. Tendon FSR and PINP were lower in OC compared with control. An increase in muscle collagen FSR postexercise was only observed in control (P < 0.05). Furthermore, the results indicate a lower bioavailability of IGF-I in OC. In conclusion, synthetic female sex hormones administered as OC had an inhibiting effect on collagen synthesis in tendon, bone, and muscle connective tissue, which may be related to a lower bioavailability of IGF-I. PMID:18845777

  1. Effect of the ethinylestradiol/levonorgestrel combined oral contraceptive on the activity of cytochrome P4503A in obese women

    PubMed Central

    Edelman, Alison; Munar, Myrna; Elman, Miriam R; Koop, Dennis; Cherala, Ganesh

    2012-01-01

    AIM(S) While it is known that CYP3A4/5 activity is decreased with combined oral contraceptive (COC) use and obesity suppresses CYP expression, the combined effects of obesity and COC use on CYP3A4/5 activity are unclear. Therefore, our aim was to examine the effect of COC usage on CYP3A4/5 activity in obese women. METHODS Thirty-four, obese (body mass index, BMI > 30 kg m−2) women of reproductive age (18–35 years old) were placed on a COC pill containing 20 µg ethinylestradiol/100 µg levonorgestrel for 21 days starting at the onset of menses. A midazolam pharmacokinetic study was conducted prior to initiation and after 21 days of COC treatment. Serial blood samples were collected and plasma concentrations of midazolam were measured using liquid chromatography tandem mass spectrometry. Pharmacokinetic parameters were estimated using a non-compartmental method. RESULTS Midazolam clearance, a surrogate measure of CYP3A4/5 activity, was significantly decreased upon COC use (63.3 l h−1vs. 53.9 l h−1, P < 0.05). A median decrease of 5.6 l h−1 (95% CI −4.1, 13.3 l h−1) was observed. However, the magnitude of change was similar to that reported in women with normal BMI. CONCLUSIONS Although we hypothesized that obesity might amplify the impact on CYP3A4/5 activity in COC users, we found that this was not the case. This finding is reassuring regarding potential additional drug−drug interactions in obese COC users as CYP3A4/5 is a major enzyme in the metabolism of many marketed drugs. PMID:22299599

  2. Development and characterisation of sustained release solid dispersion oral tablets containing the poorly water soluble drug disulfiram.

    PubMed

    Shergill, Mandip; Patel, Mina; Khan, Siraj; Bashir, Ayesha; McConville, Christopher

    2016-01-30

    Administration of drugs via the oral route is the most common and preferred route due to its ease of administration, cost-effectiveness and flexibility in design. However, if the drug being administered has limited aqueous solubility it can result in poor bioavailability. Furthermore, the low pH of the stomach as well as enzymatic activity can result in drugs delivered via the oral route being rapidly metabolised and degraded. Here we demonstrate the development and characterisation of sustained release solid dispersion oral tablets, containing the poorly water-soluble drug disulfiram (DSF). The tablets, which are manufactured from two different polymers (Kolliphor(®) P 188 and P 237) specifically designed for the manufacture of solid dispersions and two different polymers (Kollidon(®) SR and HPMC) specifically designed to provide sustained release, can enhance the solubility of DSF, sustain its release, while protecting it from degradation in simulated gastric fluid (SGF). The paper demonstrates that when using the hot melt method at 80°C the DSF loading capacity of the Kolliphor(®) P 188 and P 237 polymers is approximately 43 and 46% respectively, with the DSF completely in an amorphous state. The addition of 80% Kollidon(®) SR to the formulation completely protected the DSF in SGF for up to 70 min with 16% degradation after 120 min, while 75% degradation occurred after 120 min with the addition of 80% HPMC. The release rate of DSF can be manipulated by both the loading and type of sustained release polymer used, with HPMC providing for a much faster release rate compared to Kollidon(®) SR. PMID:26608620

  3. In vitro effect of fluoride oral hygiene tablets on artificial caries lesion formation and remineralization in human enamel

    PubMed Central

    Gängler, Peter; Kremniczky, Thomas; Arnold, Wolfgang H

    2009-01-01

    Background Aim of this in-vitro-study was to assess the remineralization potential of a tooth cleaning tablet with different fluoride content. Methods Twenty three caries free impacted third molars were examined, enamel surfaces were wax coated leaving two 3 × 4 mm windows for exposure to demineralization/remineralization cycles. The teeth were randomly assigned to 4 groups of 5 control and 6 experimental teeth. Demineralization by standardised HEC-gel, pH 4.7 at 37°C for 72 h, was alternated by rinsing in remineralization solution, pH 7.0 at 37°C for 72 h, total challenge time 432 h. The negative control group N was treated during remineralization cycles with saline; positive control group P was treated with remineralization solution; experimental group D1 was exposed to remineralization solution containing Denttabs®-tablets with 1450 ppm F; experimental group D2 was exposed to remineralization solution and Denttabs®-tablets with 4350 ppm F. Each tooth was cut into serial sections and analyzed by polarized light microscopy for assessment of the different zones of white-spot lesions in 3 representative sections. Statistical analysis was based on the Mann-Whitney-Test. Results Both control groups N(-) and P(+) exhibited characteristic white-spot lesions. The remineralization and the demineralization inhibition of the lesions increased considerably from N

    oral hygiene product and the remineralization is correlated to the fluoride content. PMID:19799785

  4. Changes in weight, total fat, percent body fat, and central-to-peripheral fat ratio associated with injectable and oral contraceptive use

    PubMed Central

    BERENSON, Abbey B.; RAHMAN, Mahbubur

    2010-01-01

    Objective To determine changes in body weight and composition resulting from hormonal contraception. Study design Dual-energy X-ray absorptiometry was performed at baseline and every 6 months for 3 years on 703 women (200 Black, 247 White, 256 Hispanic) initiating use of oral contraception (OC, n = 245), depot medroxyprogesterone acetate (DMPA, n = 240), or nonhormonal contraception (NH, n = 218). DMPA discontinuers were followed for up to 2 years to examine the reversibility of observed changes. Results Over 36 months, DMPA users increased their weight (+5.1 kg), body fat (+4.1 kg), percent body fat (+3.4%), and central-to-peripheral fat ratio (+0.1) more than OC and NH users (P<.01). OC use did not cause weight gain. After DMPA discontinuation, NH users lost 0.42 kg/6 months while OC users gained 0.43 kg/6 months. Conclusions Body weight and fat significantly increase while using DMPA. After discontinuation, some decrease occurs when NH is used. PMID:19254592

  5. Effect of information on the perception of users and prospective users of combined oral contraceptives regarding the risk of venous thromboembolism.

    PubMed

    Machado, Rogério Bonassi; Morimoto, Mariana; Santana, Narayana; Arruda, Lívia Fernandes; Bernardes, Carine Rejane; de Souza, Isadora Matias

    2015-01-01

    This study evaluated patients' knowledge on the risk of venous thromboembolism (VTE) associated with combined oral contraceptives (COCs) and their perception of this risk when it is presented as a relative risk (RR), absolute risk (AbR) or attributable risk (AR). This was a cross-sectional study involving 159 users or potential users of COCs. The participants answered a self-administered questionnaire in which the risk of VTE associated with COCs was presented as RR, AbR and AR. The degree of concern expressed regarding this risk and the women's changes of opinion when the information was communicated through a different risk model were evaluated. Most of the women (67.9%) expressed concern when the risk was presented as an RR. Conversely, they showed no concern when the risk was presented as an AbR (14.5%) or AR (10.7%). A significant number of women changed their opinion regarding their level of concern when the risk was presented as an AbR or AR (p < 0.001). In conclusion, concerns about thrombotic complications from the use of combined hormonal contraception is reduced when incidence rather than relative risk is presented. Presentation of thrombosis complications in terms of incidence rather than RR may improve communication of side effects during counseling for combined hormonal contraception initiation. PMID:25095700

  6. A clinical evaluation of amlexanox oral adhesive pellicles in the treatment of recurrent aphthous stomatitis and comparison with amlexanox oral tablets: a randomized, placebo controlled, blinded, multicenter clinical trial

    PubMed Central

    Meng, Wenxia; Dong, Yi; Liu, Jie; Wang, Zhi; Zhong, Xiaobo; Chen, Ruiyang; Zhou, Hongmei; Lin, Mei; Jiang, Lu; Gao, Feng; Xu, Tao; Chen, Qianming; Zeng, Xin

    2009-01-01

    Background Amlexanox has been developed as a 5 percent topical oral paste for the treatment of patients with recurrent aphthous stomatitis (RAS) in most European countries. However, it is not yet available in China and has not been generally accepted in clinical treatment. The aim of this study was to explore the effectiveness of amlexanox oral adhesive pellicles in the treatment of minor recurrent aphthous ulcers, and compare the results with those of amlexanox oral adhesive tablets in order to analyse the difference between the two dosage forms of amlexanox. Methods We performed a randomized, blinded, placebo-controlled, parallel, multicenter clinical study. A total of 216 patients with minor recurrent aphthous ulcers (MiRAU) were recruited and randomized to amlexanox pellicles or placebo pellicles. Pellicles were consecutively applied four times per day, for five days. The size and pain level of ulcers were measured and recorded on treatment days 0, 4 and 6. Finally, the results were compared with those of our previous 104 cases treated with amlexanox tablets. Results Amlexanox oral adhesive pellicles significantly reduced ulcer size (P= 0.017 for day 4, P=0.038 for day 6) and alleviated ulcer pain (P=0.021 for day 4, P=0.036 for day 6). No significant difference was observed in the treatment effectiveness between the pellicle and tablet form of amlexanox. Conclusions Amlexanox oral adhesive pellicles are as effective and safe as amlexanox oral adhesive tablets in the treatment of MiRAU for this Chinese cohort. However, pellicles seem to be more comfortable to use when compared with the dosage form of tablets. Therefore, in clinical practice, amlexanox oral adhesive pellicles may be a better choice for RAS patients. Trials registration Nederlands Trial Register NTR1727. PMID:19419555

  7. Preparation and evaluation of orally disintegrating tablets of taste masked phencynonate HCl using ion-exchange resin.

    PubMed

    Ge, Zhenzhong; Yang, Meiyan; Wang, Yuli; Shan, Li; Gao, Chunsheng

    2015-06-01

    This study was intended to design an orally disintegrating tablet (ODT) formulation that can mask the extremely bitter and metallic taste of phencynonate HCl by novel ion-exchange resins. The drug-resin complexes (DRCs) were prepared and characterized by scanning electron microscopy, X-ray powder diffraction and differential scanning calorimetry. In vitro properties (dissolution, wetting time and disintegration time) and in vivo behavior (disintegration time and taste-masking effect) in healthy volunteers of the prepared ODTs were also investigated. The drug was changed from the crystal structure to the amorphous form in the DRC. Compared with commercial tablets, the in vitro and in vivo disintegration of optimized DRC-loaded ODTs with a drug-resin ratio of 1:1 was greatly improved and better palatability with a low bitterness index (0.33) was obtained. The current DRC-loaded ODT could promise a good way to mask the unpleasant taste of certain drugs and accordingly improve the patient compliance. PMID:24785576

  8. Comparative effects of Lunelle monthly contraceptive injection (medroxyprogesterone acetate and estradiol cypionate injectable suspension) and ortho-Novum 7/7/7 oral contraceptive (norethindrone/ethinyl estradiol triphasic) on lipid profiles. Investigators from the Lunelle Study Group.

    PubMed

    Cromie, M A; Maile, M H; Wajszczuk, C P

    2000-01-01

    As part of a 60-week, open-label, nonrandomized, parallel, controlled study comparing a monthly contraceptive injection containing medroxyprogesterone acetate (MPA) 25 mg and estradiol cypionate (E(2)C) 5 mg (Lunelle Monthly Contraceptive Injection) and a norethindrone 0.5, 0.75, 1.0 mg/0.035 mg ethinyl estradiol (NET/EE) triphasic oral contraceptive (Ortho-Novum(R) 7/7/7), a longitudinal examination of lipid profiles was conducted. Lipid parameters were assessed at screening and at weeks 20, 40, and 60 (or the final visit) in 114 women using MPA/E(2)C and 93 using NET/EE (lipid analysis population). Extra blood samples were obtained at weeks 21, 22, and 23 in 61 MPA/E(2)C users and 51 NET/EE users (index-cycle analysis population) to investigate lipid changes during one cycle of use. In the index-cycle population, median changes from screening to week 60 showed a decrease in apolipoprotein (apo) A-I and apo A-II in both groups. MPA/E(2)C users had a decrease in total cholesterol (C), total triglycerides, low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C), with maintenance of the total C/HDL-C ratio. NET/EE users showed an increase in total C and LDL-C, with no change in HDL-C or the total C/HDL-C ratio. Within the index cycle (weeks 20 to 23), median changes in lipid values in both MPA/E(2)C and NET/EE users were generally greatest during the first week after the injection or the start of the pill pack. The results of this first longitudinal examination of serum lipids in US women using MPA/E(2)C confirm earlier findings in women in other countries. However, a direct comparison of the effects of MPA/E(2)C and NET/EE on lipid profiles was not possible in this study because of its design and because of the baseline and pharmacokinetic/pharmacodynamic differences between the two contraceptive groups. The results of this analysis showed that, although overall lipid values decreased, including a significant decrease in HDL

  9. Contraceptive use in acne.

    PubMed

    Lam, Charlene; Zaenglein, Andrea L

    2014-01-01

    Acne vulgaris is an inflammatory disorder of the pilosebaceous follicle. It is well established that androgen hormones play a major role in sebum production and excretion, and are vital in the pathogenesis of acne. Isotretinoin notwithstanding, hormonal therapies such as combined oral contraceptives (COCs) and spironolactone are the only treatments that can affect sebum production and the androgen component of acne. Contraceptives are also used during isotretinoin therapy for pregnancy prevention. It is important for a dermatologist to be familiar with all the available methods of contraception to provide essential counseling to patients. The aim of this paper is to review the role of hormones in acne pathogenesis, discuss the use of hormonal therapies for acne, and detail various alternative contraceptive methods in relation to isotretinoin treatment and pregnancy prevention. PMID:25017461

  10. Oral L-thyroxine liquid versus tablet in patients with hypothyroidism without malabsorption: a prospective study.

    PubMed

    Fallahi, Poupak; Ferrari, Silvia Martina; Antonelli, Alessandro

    2016-06-01

    No consistent data are present in literature about the effectiveness of levothyroxine (L-T4) liquid formulation in patients without malabsorption. The aim of this study is to compare the effectiveness of L-T4 liquid formulation, with L-T4 tablets, in hypothyroid patients without malabsorption or drug interference. One hundred and fifty two patients were recruited. Patients were switched from the L-T4 therapy in tablets, to liquid L-T4 at the same dosage, 30 min before breakfast. Serum thyrotropic hormone (TSH), free thyroxine (FT4), and free triiodothyronine (FT3) were re-evaluated after 1-3 months (first control) and 5-7 months (second control) from the switch. TSH values significantly declined with respect to the basal value after the switch to liquid L-T4 both at the first control (P < 0.05) and at the second control (P < 0.01); FT4 and FT3 levels were not significantly changed. We show that liquid L-T4 is more effective than L-T4 tablet in controlling TSH levels in hypothyroid patients without malabsorption, gastric disorders, or drug interference. PMID:26721663

  11. Emergency contraception in Nairobi, Kenya: knowledge, attitudes and practices among policymakers, family planning providers and clients, and university students.

    PubMed

    Muia, E; Ellertson, C; Lukhando, M; Flul, B; Clark, S; Olenja, J

    1999-10-01

    To gauge knowledge, attitudes, and practices about emergency contraception in Nairobi, Kenya, we conducted a five-part study. We searched government and professional association policy documents, and clinic guidelines and service records for references to emergency contraception. We conducted in-depth interviews with five key policymakers, and with 93 family planning providers randomly selected to represent both the public and private sectors. We also surveyed 282 family planning clients attending 10 clinics, again representing both sectors. Finally, we conducted four focus groups with university students. Although one specially packaged emergency contraceptive (Postinor levonorgestrel tablets) is registered in Kenya, the method is scarcely known or used. No extant policy or service guidelines address the method specifically, although revisions to several documents were planned. Yet policymakers felt that expanding access to emergency contraception would require few overt policy changes, as much of the guidance for oral contraception is already broad enough to cover this alternative use of those same commodities. Participants in all parts of the study generally supported expanded access to emergency contraception in Kenya. They did, however, want additional, detailed information, particularly about health effects. They also differed over exactly who should have access to emergency contraception and how it should be provided. PMID:10640169

  12. A 13-month multicenter clinical experience of a low-dose monophasic oral contraceptive containing 20 microg ethinylestradiol and 75 microg gestodene in Latin American women.

    PubMed

    Bassol, Susana; Alvarado, Gloria; Arreola, Ranferi Gaona; Celis-Gonzalez, Cuauhtemoc; Peña, Efrain Perez; Flores, Josue Garza; Ahued, Jose R; Ricalde, Roger Lara; Lopez, Carlos R; Prieto, Gustavo; Gurucharri, Carlos; Heredia, Monica G; Ortiz, Oscar Contreras; Percossi, Gabriela; Figueroa Casas, Pedro R; Botto, Elida; Tozzini, Roberto Italo; Botti, Gustavo; Nuñez de Pierro, Anibal; Fernandez, Mirta; Lastreto, Enrique; Nañez, Monica; Carneiro de Oliveira, Hildoberto; Diogenes Holanda Yazlle, Martha E; Silva, Jaime; Salazar, German; Gomez, Jorge; Penagos, Gloria; Cifuentes, Rodrigo; Torres, Luz A; Reyes-Marquez, Roberto; Albrecht, Gerhard

    2003-05-01

    This prospective, multicenter study was conducted to evaluate the contraceptive reliability, cycle control and tolerability of a 21-day oral contraceptive regimen containing 20 microg ethinylestradiol and 75 microg gestodene in four Latin American countries (Mexico, Argentina, Brazil and Colombia). Participants took trial medication daily for 21 days. Contraceptive efficacy, cycle control and tolerability were evaluated over a period of 13 cycles. Efficacy data gathered from 5,109 treatment cycles were obtained from 393 participants. The trial medication proved to be an effective contraceptive and provided good cycle control. One pregnancy because of poor compliance was recorded. This resulted in a study Pearl index of 0.25. Forty-six percent of Latin American women reported one intracyclic spotting bleeding episode and 37.6% reported one intracyclic breakthrough bleeding (medium/excessive bleeding) episode during cycles 2-4 (primary target). Overall, intracyclic bleeding was reported in 41%. Overall, there was a trend towards a lower incidence of spotting in all the countries and this difference had statistical significance between Argentina and the others three countries (p < 0.05) during cycles 2-4. This trend was also apparent with respect to breakthrough bleeding, but again the difference did not achieve statistical significance. The discontinuation rate because of adverse events was low (3%); no serious adverse events were reported. More than 78% of the women in the four countries maintained constant body weight or lost weight (2 kg) during the study. The treatment effect on blood pressure was negligible. There were no appreciable changes in mean laboratory values over the course of the study. PMID:12742559

  13. [Contraceptive pill amenorrhea--does it exist?].

    PubMed

    Fries, H; Nillius, S J

    1975-11-01

    The possibility of amenorrhea as a direct result of discontinuing oral contraceptives is discussed and its etiology is explored. In a study of 1860 women in Uppsala county in Sweden, 16% of the amenorrhea cases among these women could be temporally related to the discontinuation of oral contraceptive use. Earlier irregularities of menstruation and psychological stress are discussed as indications that "contraceptive pill amenorrhea" could occur. Loss of weight, often combined with symptoms of anorexia nervosa, is also a frequent indication of susceptibility to "contraceptive pill amenorrhea." The possibility of "contraceptive pill amenorrhea" as an iatrogenic syndrome is discussed. PMID:1186384

  14. Emergency contraception

    MedlinePlus

    Morning-after pill; Postcoital contraception; Birth control - emergency; Plan B ... Emergency contraception most likely prevents pregnancy in the same way as regular birth control pills: By preventing or delaying ...

  15. Association of Combined Tobacco Smoking and Oral Contraceptive Use With Cervical Intraepithelial Neoplasia 2 or 3 in Korean Women

    PubMed Central

    Oh, Hea Young; Kim, Mi Kyung; Seo, Sang-Soo; Lee, Jae-Kwan

    2016-01-01

    Background Cigarette smoking and oral contraceptive (OC) use have been associated with cervical neoplasia, and the combination of smoking and OC use could influence cervical carcinogenesis. We aimed to assess the joint effect of smoking and OC use on the risk of cervical intraepithelial neoplasia (CIN). Methods From a cohort of human papillomavirus-positive subjects recruited from 6 hospitals in Korea from March 2006 to November 2012, a total of 678 subjects (411 control, 133 CIN 1, and 134 CIN 2 or 3 cases) were selected for this study (mean age, 43 years). The risk of CIN associated with smoking and OC use on additive and multiplicative scales was estimated via multinomial logistic regression after adjustment for potential confounding factors. The relative excess risk due to interaction (RERI) and the synergy index (S) were used to evaluate the additive interaction. Results OC users (odds ratio [OR] 1.98; 95% confidence interval [CI], 1.07–3.69) and long-term OC use (≥20 months; OR 2.71; 95% CI, 1.11–6.59) had a higher risk of CIN 2/3, but had no association with CIN 1, compared to non-OC users. Smokers and heavy smoking (≥8 cigarettes/day) were not associated with any CIN grade. Combined smoking and OC use (OR 4.91; 95% CI, 1.68–14.4; RERI/S, 3.77/27.4; P for multiplicative interaction = 0.003) and combined heavy smoking and long-term OC use (OR 11.5; 95% CI, 1.88–70.4; RERI/S, 9.93/18.8; P for multiplicative interaction = 0.009) had a higher risk of CIN 2/3 but had no association with CIN 1 compared to combined non-smoking and non-OC use. Conclusions OC use and smoking acted synergistically to increase the risk of CIN 2 or 3 in Korean women. PMID:26441210

  16. Effect of emergency oral contraceptive use on condom utilization and sexual risk taking behaviours among university students, Northwest Ethiopia: a cross-sectional study

    PubMed Central

    2012-01-01

    Background Young people between the ages of 15 and 24 years are both the most at risk of HIV and the greatest hope for turning the tide against HIV/AIDS. Although various surveys have been done on sexual behaviour of youth in Ethiopia, studies assessing the effect of emergency oral contraceptives on condom utilization of university students are lacking. Methods A cross-sectional study was conducted in two major universities of Ethiopia from January to May 2011 using structured self administered questionnaire with the aim to assess the effect of introducing oral emergency contraceptive pills on condom utilization and sexual risk taking behaviours among female university students. Study participants were selected by simple random sampling using the list from the associate registrars of each University. Data were entered, cleaned and analyzed using SPSS version 17.0. Bivariate and multiple logistic regression analyses were used to determine factors associated with condom utilization. Results a total of 623 students out of 660 were included giving response rate of 94.4%. A total of 103(16.5%) had history of sexual intercourse and nearly half (45.6%) of them had sex before the age of 20 years. Forty (6.4%) students had history of sexually transmitted infections (STI). Sixty seven percent of students had heard about emergency oral contraceptives. One hundred and ninety one (45.7%) of students believe that EOC is effective in preventing pregnancy. Believing that EOC is effective in preventing pregnancy (adjusted Odds ratio, AOR = 0.22 95% CI 0.06, 0.87), condom prevents STI (AOR = 10.37, 95% CI 1.73, 62.24) and younger age below 20 years (AOR = 11.68 95% CI 1.25, 109.19) were statistically significantly associated with condom use. Conclusion a significant number of students had history of sexual intercourse and used emergency contraception. The belief in the effectiveness of EOC negatively affects condom use. The preference for the pill may make

  17. Enteric-coated tablet of risedronate sodium in combination with phytic acid, a natural chelating agent, for improved oral bioavailability.

    PubMed

    Kim, Jeong S; Jang, Sun W; Son, Miwon; Kim, Byoung M; Kang, Myung J

    2016-01-20

    The oral bioavailability (BA) of risedronate sodium (RS), an antiresorptive agent, is less than 1% due to its low membrane permeability as well as the formation of non-absorbable complexes with multivalent cations such as calcium ion (Ca(2+)) in the gastrointestinal tract. In the present study, to increase oral BA of the bisphosphonate, a novel enteric-coated tablet (ECT) dosage form of RS in combination with phytic acid (IP6), a natural chelating agent recognized as safe, was formulated. The chelating behavior of IP6 against Ca(2+), including a stability constant for complex formulation was characterized using the continuous variation method. Subsequently, in vitro dissolution profile and in vivo pharmacokinetic profile of the novel ECT were evaluated comparatively with that of the marketed product (Altevia, Sanofi, US), an ECT containing ethylenediaminetetraacetic acid (EDTA) as a chelating agent, in beagle dogs. The logarithm of stability constant for Ca(2+)-IP6 complex, an equilibrium constant approximating the strength of the interaction between two chemicals to form complex, was 19.05, which was 3.9-fold (p<0.05) and 1.7-fold (p<0.05) higher than those of Ca(2+)-RS and Ca(2+)-EDTA complexes. The release profile of RS from both enteric-coated dosage forms was equivalent, regardless of the type of chelating agent. An in vivo absorption study in beagle dogs revealed that the maximum plasma concentration and area under the curve of RS after oral administration of IP6-containing ECT were approximately 7.9- (p<0.05) and 5.0-fold (p<0.05) higher than those of the marketed product at the same dose (35mg as RS). Therefore, our study demonstrates the potential usefulness of the ECT system in combination with IP6 for an oral therapy with the bisphosphonate for improved BA. PMID:26594027

  18. Contraception in Sweden.

    PubMed

    Riphagen, F E; von Schoultz, B

    1989-06-01

    In 1987, a survey of contraceptive use, knowledge and attitudes was conducted in Sweden by the International Health Foundation (IHF) as part of a multi-country study that has so far involved six other countries in Europe. The women involved, who were aged 15-44, completed a standard questionnaire. The overall percentage use of contraceptive methods, especially the reliable ones, was found to be high (95%). Oral contraception was the most frequently used method, followed by barrier methods and the intrauterine device (IUD). Contraceptive methods were chosen or abandoned mainly because of health reasons and better reliability. Knowledge of fertility proved to be generally good. Medical methods such as oral contraceptives and IUDs were associated with health hazards. In the case of the pill, fears of cardiovascular risks, thrombosis and cancer were widespread, while infection risk and menorrhagia were the most frequently quoted perceived disadvantages of the IUD. Indeed, these two methods suffer from a very negative image among Swedish users. PMID:2752752

  19. Safety of fluralaner chewable tablets (BravectoTM), a novel systemic antiparasitic drug, in dogs after oral administration

    PubMed Central

    2014-01-01

    Background Fluralaner is a novel systemic insecticide and acaricide that provides long acting efficacy in dogs after a single oral treatment. This study investigated the safety of oral administration of fluralaner in chewable tablets to dogs at the highest recommended treatment dose and at multiples of this dose. Methods Thirty-two (16 male and 16 female) healthy 8-week old Beagle dogs weighing 2.0 - 3.6 kg at first administration were included in the study. Fluralaner was administered on three occasions at 8-week intervals at doses of up to 56, 168, and 280 mg fluralaner/kg body weight, equivalent to 1, 3, and 5 times the highest recommended treatment dose of fluralaner; sham dosed dogs served as controls. During the study, all dogs were clinically observed, and their health was carefully monitored including body weight development, food consumption and measurement of hematology, coagulation, clinical chemistry (including measurement of levels of ACTH and C-reactive protein) and urinalysis. Following euthanasia of the dogs, complete gross post mortem examination, including organ weight determination, and histopathological examination of multiple tissues were conducted. Results There were no clinical findings related to fluralaner treatment. Statistically significant differences between the treated groups and the control group were observed for some clinical pathology parameters and organ weights; none of these findings were considered to be of clinical relevance. Conclusions Oral administration of fluralaner at the highest recommended treatment dose (56 mg/kg) at 8-week intervals is well tolerated and has a safety margin of more than five in healthy dogs eight weeks of age or older and weighing at least 2 kg. PMID:24606886

  20. Formulation Optimization of Hydrodynamically Balanced Oral Controlled Release Bioadhesive Tablets of Tramadol Hydrochloride

    PubMed Central

    Singh, Bhupinder; Rani, Ashu; Babita; Ahuja, Naveen; Kapil, Rishi

    2010-01-01

    The directly compressible floating-bioadhesive tablets of tramadol were formulated using varying amounts Carbopol 971P (CP) and hydroxy-propylmethyl cellulose (HPMC), along with other requisite excipients. In vitro drug release profile, floatational characteristics and ex vivo bioadhesive strength using texture analyzer were determined, and systematically optimized using a 32 central composite design (CCD). The studies indicated successful formulation of gastroretentive compressed matrices with excellent controlled release, mucoadhesion and hydrodynamic balance. Comparison of the dissolution profiles of the optimized formulation, with optimal composition of CP:HPMC :: 80.0:125.0, with that of the marketed controlled release formulation other indicated analogy of drug release performance with each other. Validation of optimization study using eight confirmatory experimental runs indicated very high degree of prognostic ability of CCD with mean ± SEM of −0.06% ± 0.37. Further, the study successfully unravels the effect of the polymers on the selected response variables. PMID:21179349

  1. The effect of combined oral contraception on testosterone levels in healthy women: a systematic review and meta-analysis

    PubMed Central

    Zimmerman, Y.; Eijkemans, M.J.C.; Coelingh Bennink, H.J.T.; Blankenstein, M.A.; Fauser, B.C.J.M.

    2014-01-01

    BACKGROUND Combined oral contraceptives (COCs) reduce levels of androgen, especially testosterone (T), by inhibiting ovarian and adrenal androgen synthesis and by increasing levels of sex hormone-binding globulin (SHBG). Although this suppressive effect has been investigated by numerous studies over many years, to our knowledge no systematic review concerning this issue had been performed. This systematic review and meta-analysis was performed to evaluate the effect of COCs on concentrations of total T, free T and SHBG in healthy women and to evaluate differences between the various types of COCs (e.g. estrogen dose, type of progestin) and the assays used to assess total T and free T. METHODS A review of the literature was performed using database searches (MEDLINE, EMBASE and the Cochrane Central Register of Clinical Trials) and all publications (from inception date until July 2012) investigating the effect of COCs on androgen levels in healthy women were considered eligible for selection. Three reviewers were involved in study selection, data extraction and critical appraisal. For the meta-analysis, data on total T, free T and SHBG were extracted and combined using random effects analysis. Additional subgroup analyses were performed to evaluate differences between the various types of COCs (e.g. estrogen dose, type of progestin) and the assays used to assess total T or free T. RESULTS A total of 151 records were identified by systematic review and 42 studies with a total of 1495 healthy young women (age range: 18–40 years) were included in the meta-analysis. All included studies were experimental studies and 21 were non-comparative. Pooling of the results derived from all the included papers showed that total T levels significantly decreased during COC use [mean difference (MD) (95% confidence interval, CI) −0.49 nmol/l (−0.55, −0.42); P < 0.001]. Significantly lower levels of free T were also found [relative change (95% CI) 0.39 (0.35, 0.43); P < 0

  2. Practice Bulletin Summary No. 152: Emergency Contraception.

    PubMed

    2015-09-01

    Emergency contraception, also known as postcoital contraception, is therapy used to prevent pregnancy after an unprotected or inadequately protected act of sexual intercourse. Common indications for emergency contraception include contraceptive failure (eg, condom breakage or missed doses of oral contraceptives) and failure to use any form of contraception (1-3). Although oral emergency contraception was first described in the medical literature in the 1960s, the U.S. Food and Drug Administration (FDA) approved the first dedicated product for emergency contraception in 1998. Since then, several new products have been introduced. Methods of emergency contraception include oral administration of combined estrogen-progestin, progestin only, or selective progesterone receptor modulators and insertion of a copper intrauterine device (IUD). Many women are unaware of the existence of emergency contraception, misunderstand its use and safety, or do not use it when a need arises (4-6). The purpose of this Practice Bulletin is to review the evidence for the efficacy and safety of available methods of emergency contraception and to increase awareness of these methods among obstetrician-gynecologists and other gynecologic providers. PMID:26287780

  3. Practice Bulletin No. 152: Emergency Contraception.

    PubMed

    2015-09-01

    Emergency contraception, also known as postcoital contraception, is therapy used to prevent pregnancy after an unprotected or inadequately protected act of sexual intercourse. Common indications for emergency contraception include contraceptive failure (eg, condom breakage or missed doses of oral contraceptives) and failure to use any form of contraception (). Although oral emergency contraception was first described in the medical literature in the 1960s, the U.S. Food and Drug Administration (FDA) approved the first dedicated product for emergency contraception in 1998. Since then, several new products have been introduced. Methods of emergency contraception include oral administration of combined estrogen-progestin, progestin only, or selective progesterone receptor modulators and insertion of a copper intrauterine device (IUD). Many women are unaware of the existence of emergency contraception, misunderstand its use and safety, or do not use it when a need arises (). The purpose of this Practice Bulletin is to review the evidence for the efficacy and safety of available methods of emergency contraception and to increase awareness of these methods among obstetrician-gynecologists and other gynecologic providers. PMID:26287787

  4. Low dose oestrogen combined oral contraception and risk of pulmonary embolism, stroke, and myocardial infarction in five million French women: cohort study

    PubMed Central

    Dalichampt, Marie; Raguideau, Fanny; Ricordeau, Philippe; Blotière, Pierre-Olivier; Rudant, Jérémie; Alla, François; Zureik, Mahmoud

    2016-01-01

    Objective To assess the risk of pulmonary embolism, ischaemic stroke, and myocardial infarction associated with combined oral contraceptives according to dose of oestrogen (ethinylestradiol) and progestogen. Design Observational cohort study. Setting Data from the French national health insurance database linked with data from the French national hospital discharge database. Participants 4 945 088 women aged 15-49 years, living in France, with at least one reimbursement for oral contraceptives and no previous hospital admission for cancer, pulmonary embolism, ischaemic stroke, or myocardial infarction, between July 2010 and September 2012. Main outcome measures Relative and absolute risks of first pulmonary embolism, ischaemic stroke, and myocardial infarction. Results The cohort generated 5 443 916 women years of oral contraceptive use, and 3253 events were observed: 1800 pulmonary embolisms (33 per 100 000 women years), 1046 ischaemic strokes (19 per 100 000 women years), and 407 myocardial infarctions (7 per 100 000 women years). After adjustment for progestogen and risk factors, the relative risks for women using low dose oestrogen (20 µg v 30-40 µg) were 0.75 (95% confidence interval 0.67 to 0.85) for pulmonary embolism, 0.82 (0.70 to 0.96) for ischaemic stroke, and 0.56 (0.39 to 0.79) for myocardial infarction. After adjustment for oestrogen dose and risk factors, desogestrel and gestodene were associated with statistically significantly higher relative risks for pulmonary embolism (2.16, 1.93 to 2.41 and 1.63, 1.34 to 1.97, respectively) compared with levonorgestrel. Levonorgestrel combined with 20 µg oestrogen was associated with a statistically significantly lower risk than levonorgestrel with 30-40 µg oestrogen for each of the three serious adverse events. Conclusions For the same dose of oestrogen, desogestrel and gestodene were associated with statistically significantly higher risks of pulmonary embolism but not arterial

  5. [Test your knowledge: contraceptives].

    PubMed

    1998-06-01

    A brief self-administered quiz on contraceptive knowledge is presented. The 7 questions ask the reader to explain the mechanism of action of combined oral contraceptives, and why estrogens are used with progestins, and to indicate the main secondary effects of Depo-Provera and implants and the dosage of the "morning-after pill." A multiple-choice question concerns absolute contraindications to combined OC use. One clinical case involves selection of OCs for a woman with a family history of breast cancer and the other requires development of a strategy for reducing high-risk pregnancies and risk of AIDS. PMID:12321847

  6. Relationship between contraceptive method and vaginal flora.

    PubMed

    Peddie, B A; Bishop, V; Bailey, R R; McGill, H

    1984-08-01

    This study was undertaken to assess whether the vaginal flora was affected by the method of contraception, and in particular as to whether the incidence of vaginal candidiasis increased when oral contraceptives were used. One thousand and two consecutive vaginal or cervical swabs from women attending a family planning centre were cultured. Candida albicans was isolated from 13% of women using no contraception, 16% using oral contraceptives, and from 9%, 19% and 18% of those using diaphragms, intrauterine contraceptive devices (IUCD) and condoms respectively. These differences were not statistically significant. Women using an IUCD had significantly more Gram-positive cocci cultured than women in any other group, while those using diaphragms had significantly more Gram-negative bacilli. Our clinical impression that the use of oral contraceptives led to an increase in vaginal candidiasis, was not confirmed by this study. PMID:6596089

  7. [Historical survey of modern reversible contraceptive methods].

    PubMed

    Mbabajende, V

    1986-04-01

    Because of contraception, pregnancy need not be viewed by women as punishment for sexual activity but as a planned and desired event. Most of the contraceptive methods used in developing countries at present were introduced during the 1960s, but use of contraception has a long history and some methods date back to antiquity. Contraceptive pills were already used around 2000 BC in the form of mercury and arsenic tablets. Their effectiveness was questionable. The role of hormones in human reproduction began to be understood only in the early 1900s. The discovery of progesterone in a Mexican iguana in the 1940s permitted production of progesterone on a large scale. Estrogens had been identified around 1930. Human trials of a contraceptive pill beginning in 1956 in Puerto Rico demonstrated that progestins could prevent pregnancy by suppressing ovulation. Later on, estrogen was added to reduce menstrual irregularities. The 1st generation of combined oral contraceptives contained very high levels of hormones associated with high rates of side effects. Numerous formulations with lower hormonal contents became available beginning around 1970 and constitute the principal formulations in use today. A number of long acting hormonal methods based on progestins have been developed, including injectables, some IUDs and vaginal rings, and implants. The 1st commercially available injectable, norethisterone enanthate, did not acquire the wide distribution of medroxyprogesterone acetate, sold as Depo Provera and used to treat various pathological conditions as well as for contraception. The 1st true IUDs were small stones placed within the uteri of camels by nomads to prevent pregnancy during long caravans. An IUD was developed in 1909 by Richter, and the 2 most widely used models before 1960 were the Grafenberg and Ota silver rings. Use of the 2 rings became rare for medical reasons after 1935 despite their efficacy. Safe plastic IUDs which appeared beginning in the early 1960s

  8. [Method for the evaluation of the stability and usability after opening packages of orally disintegrating tablets: case of amlodipine besilate products].

    PubMed

    Hori, Katsuhito; Yoshida, Naoko; Okumura, Tomonori; Okamura, Yasufumi; Kawakami, Junichi

    2010-08-01

    Orally disintegrating (OD) tablets are widely used in clinical practice. However, drug information on the choice and dispensing based on their stability after opening packages and usability in patients and dispensaries is not sufficient. The aim of this study was to investigate possible evaluation methods of the stability and usability of amlodipine OD tablets. Additives of the brand were changed in April 2009, and therefore the previous and current forms and two generics, current and newly marketed (in November 2009) products of different firms, were used. OD tablets were stored at 25 degrees C and 75% relative humidity for 3 months after opening the packages, and their physicochemical properties were evaluated. Their weight, diameter, thickness, and color difference increased slightly from the initial state. The extent of the change in their hardness, disintegration time, and friability was different among products. These physicochemical changes were acceptable in dispensary practice. Storage after opening the packages did not affect their dissolution rate. The dissolution rate at the initial state of the current brand was slower than that of the previous one. All products used were able to be dispensed by an automatic tablet-packing machine and applied to the so-called simple suspension method for intubational administration. Sensory evaluation tests revealed no major difference in the oral disintegration time, taste, impression, and preference among products. In conclusion, the stability and usability of amlodipine OD tablets used in this study were examined using several methods, and they can be used equivalently from the stability and usability viewpoints. PMID:20686207

  9. Comparison of the effect of a single oral L-thyroxine dose (150 micrograms) in tablet and in solution on serum thyroxine and TSH concentrations.

    PubMed

    Carpi, A; De Gaudio, C; Cirigliano, G; Toni, M G

    1993-04-01

    150 micrograms of L-thyroxine were administered to each of 14 euthyroid goitrous patients orally between 7:30 and 8:30 a.m. after fasting overnight. The L-T4 dose given was one and half tablets of the drug "Eutirox" (L-T4 tablet of 100 micrograms distributed by Bracco, Milan, Italy) or one and half ml of the solution "Tiroxen" (solution containing 100 micrograms/ml of L-T4 distributed by Laboratori Baldacci, Pisa, Italy). Two studies (one with tablet and one with solution) were performed on each patient. The tablet or the liquid form of L-T4 were administered in random order. In each study a blood sample for serum hormone determination was drawn immediately before L-T4 administration, then 30 minutes later and every hour up to the fifth hour after. The second study was performed in similar fashion later. The mean serum TT4 concentration value at any time was very similar in the two studies, thus showing the same time course after the administration of solution and the tablet formulation. The mean basal TT4 value (9.07 +/- 0.56 and 8.90 +/- 0.73 micrograms/dl respectively) increased significantly at the first and second hours. The highest value was reached at the second and at the third hour after the solution (11.15 +/- 0.58 micrograms/dl) and the tablet (11.81 +/- 0.78 micrograms/dl) respectively. Subsequently, the mean TT4 values remained significantly higher than basally over the entire 5 hours. The FT4 mean serum concentration at all times were very similar in the two studies and showed the same time course.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:7508742

  10. Bioequivalence study of two oral tablet formulations containing tenofovir disoproxil fumarate in healthy volunteers.

    PubMed

    Yerino, Gustavo A; Halabe, Emilia K; Zini, Elvira; Feleder, Ethel C

    2011-01-01

    Tenofovir disoproxil fumarate (TDF, CAS 147127-20-6) is a nucleotide reverse transcriptase inhibitor which is indicated in combination with other antiretroviral agents for the management of HIV-1 infection. The objective of this study was to compare the rate and extent of absorption and to assess the bioequivalence between a new pharmaceutical equivalent tablet formulation containing 300 mg of TDF and the innovator product. A randomized, single-center, open-label, single-dose, two-way crossover bioequivalence study in 40 healthy adult subjects was conducted. Dosing was separated by a wash-out period of 14 days. Blood samples were collected over 48 h and plasma levels of tenofovir (TFV) were determined by a validated HPLC assay. Rate and extent of absorption were similar between products. The 90% confidence interval (CI) of the ratio of the geometric means for log-transformed C(max), AUC(last) and AUC(inf) values were used to assess bioequivalence between the two formulations using the equivalence interval of 80 and 125%. In healthy subjects, the point estimate and 90% CI of the ratios of C(max), AUC(last) and AUC(inf) values were 0.99 (0.92-1.02), 0.99 (0.95-1.03) and 0.93 (0.85-1.02), respectively. Both treatments exhibited similar tolerability and safety. It was concluded that the new pharmaceutical product was bioequivalent to the innovator. PMID:21355446

  11. Comparison of Rates of and Charges from Pregnancy Complications in Users of Extended and Cyclic Combined Oral Contraceptive (COC) Regimens: A Brief Report

    PubMed Central

    Howard, Brandon; Trussell, James; Grubb, ElizaBeth; Lage, Maureen J.

    2014-01-01

    Objective Evaluate pregnancy complication rates and related charges in users of 84/7, 21/7, and 24/4 combined oral contraceptives (COCs). Study Design Data were obtained from the i3 InVision Data Mart™ retrospective claims database. Subjects were aged 15–40 years; first prescribed a COC between 1/1/2006 and 4/1/2011; and continuously insured for ≥1 year. 84/7 users were matched 1:1 to 21/7 and 24/4 users. Results Pregnancy-related complication rates and associated charges were significantly lower with 84/7 vs. 21/7 and 24/4 regimens. Conclusion Preliminary data suggest 84/7 regimens may be associated with fewer pregnancy complications and lower related charges. PMID:24457060

  12. The practical approach to the evaluation of methods used to determine the disintegration time of orally disintegrating tablets (ODTs).

    PubMed

    Brniak, Witold; Jachowicz, Renata; Pelka, Przemyslaw

    2015-09-01

    Even that orodispersible tablets (ODTs) have been successfully used in therapy for more than 20 years, there is still no compendial method of their disintegration time evaluation other than the pharmacopoeial disintegration test conducted in 800-900 mL of distilled water. Therefore, several alternative tests more relevant to in vivo conditions were described by different researchers. The aim of this study was to compare these methods and correlate them with in vivo results. Six series of ODTs were prepared by direct compression. Their mechanical properties and disintegration times were measured with pharmacopoeial and alternative methods and compared with the in vivo results. The highest correlation with oral disintegration time was found in the case of own-construction apparatus with additional weight and the employment of the method proposed by Narazaki et al. The correlation coefficients were 0.9994 (p < 0.001), and 0.9907 (p < 0.001) respectively. The pharmacopoeial method correlated with the in vivo data much worse (r = 0.8925, p < 0.05). These results have shown that development of novel biorelevant methods of ODT's disintegration time determination is eligible and scientifically justified. PMID:27134547

  13. Formulation, preparation, and evaluation of novel orally disintegrating tablets containing taste-masked naproxen sodium granules and naratriptan hydrochloride.

    PubMed

    Stange, Ulrike; Führling, Christian; Gieseler, Henning

    2014-04-01

    The purpose of this study was to develop and manufacture novel freeze-dried orally disintegrating tablets (ODTs) for migraine therapy containing taste-masked naproxen sodium and naratriptan hydrochloride. The formulation was optimized based on freeze-drying of sucrose solutions with different binders (hydroxyethylstarch, sodium alginate, methylcellulose, and gelatin) and varying amounts of Eudragit® E-coated naproxen sodium granules. Excellent product performance of the ODTs in terms of hardness and disintegration time (<10 s) independent of the mass of particles embedded was found for the solution consisting of sucrose and hydroxyethylstarch. Poloxamer 188, menthol flavor, naratriptan hydrochloride, and taste-masked naproxen sodium granules corresponding to 200 mg of naproxen were then added, and the final batches of ODTs for migraine therapy were produced. The ODTs were fully characterized, and subsequently stored for 1 month at room temperature and at 40°C. The amount of free naproxen sodium after freeze-drying and storage was below the threshold bitterness value, and the coating remained intact. Additionally, the particle size distribution of taste-masked granules was preserved, and more than 90 % naproxen sodium was released after 30 min. Naratriptan hydrochloride was dissolved immediately after disintegration, hence facilitating buccal absorption of the active pharmaceutical ingredient. PMID:24532095

  14. Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology

    PubMed Central

    Alshehri, Sultan M.; Park, Jun-Bom; Alsulays, Bader B.; Tiwari, Roshan V.; Almutairy, Bjad; Alshetaili, Abdullah S.; Morott, Joseph; Shah, Sejal; Kulkarni, Vijay; Majumdar, Soumyajit; Martin, Scott T.; Mishra, Sanjay; Wang, Lijia; Repka, Michael A.

    2015-01-01

    The objective of this study was to enhance the solubility as well as to mask the intensely bitter taste of the poorly soluble drug, Mefenamic acid (MA). The taste masking and solubility of the drug was improved by using Eudragit® E PO in different ratios via hot melt extrusion (HME), solid dispersion technology. Differential scanning calorimetry (DSC) studies demonstrated that MA and E PO were completely miscible up to 40% drug loads. Powder X-ray diffraction analysis indicated that MA was converted to its amorphous phase in all of the formulations. Additionally, FT-IR analysis indicated hydrogen bonding between the drug and the carrier up to 25% of drug loading. SEM images indicated aggregation of MA at over 30% of drug loading. Based on the FT-IR, SEM and dissolution results for the extrudates, two optimized formulations (20% and 25% drug loads) were selected to formulate the orally disintegrating tablets (ODTs). ODTs were successfully prepared with excellent friability and rapid disintegration time in addition to having the desired taste-masking effect. All of the extruded formulations and the ODTs were found to be physically and chemically stable over a period of 6 months at 40°C/75% RH and 12 months at 25°C/60% RH, respectively. PMID:25914727

  15. Comparative Studies on the Dissolution Profiles of Oral Ibuprofen Suspension and Commercial Tablets using Biopharmaceutical Classification System Criteria

    PubMed Central

    Rivera-Leyva, J. C.; García-Flores, M.; Valladares-Méndez, A.; Orozco-Castellanos, L. M.; Martínez-Alfaro, M.

    2012-01-01

    In vitro dissolution studies for solid oral dosage forms have recently widened the scope to a variety of special dosage forms such as suspensions. For class II drugs, like Ibuprofen, it is very important to have discriminative methods for different formulations in physiological conditions of the gastrointestinal tract, which will identify different problems that compromise the drug bioavailability. In the present work, two agitation speeds have been performed in order to study ibuprofen suspension dissolution. The suspensions have been characterised relatively to particle size, density and solubility. The dissolution study was conducted using the following media: buffer pH 7.2, pH 6.8, 4.5 and 0.1 M HCl. For quantitative analysis, the UV/Vis spectrophotometry was used because this methodology had been adequately validated. The results show that 50 rpm was the adequate condition to discriminate the dissolution profile. The suspension kinetic release was found to be dependent on pH and was different compared to tablet release profile at the same experimental conditions. The ibuprofen release at pH 1.0 was the slowest. PMID:23626386

  16. Pharmaceutical development of an oral tablet formulation containing a spray dried amorphous solid dispersion of docetaxel or paclitaxel.

    PubMed

    Sawicki, Emilia; Beijnen, Jos H; Schellens, Jan H M; Nuijen, Bastiaan

    2016-09-25

    Previously, it was shown in Phase I clinical trials that solubility-limited oral absorption of docetaxel and paclitaxel can be drastically improved with a freeze dried solid dispersion (fdSD). These formulations, however, are unfavorable for further clinical research because of limitations in amorphicity of SD and scalability of the production process. To resolve this, a spray drying method for an SD (spSD) containing docetaxel or paclitaxel and subsequently drug products were developed. Highest saturation solubility (Smax), precipitation onset time (Tprecip), amorphicity, purity, residual solvents, yield/efficiency and powder flow of spSDs were studied. Drug products were monitored for purity/content and dissolution during 24 months at +15-25°C. Docetaxel spSD Smax was equal to that of fdSD but Tprecip was 3 times longer. Paclitaxel spSD Smax was 30% increased but Tprecip was equal to fdSD. spSDs were fully amorphous, >99% pure, <5% residual solvents, mean batch yield was 100g and 84%. spSDs had poor powder flow characteristics, which could not be resolved by changing settings, but by using 75% lactose as diluent. The drug product was a tablet with docetaxel or paclitaxel spSD and was stable for at least 24 months. Spray drying is feasible for the production of SD of docetaxel or paclitaxel for upcoming clinical trials. PMID:27480397

  17. Enhancement of Solubility of Lamotrigine by Solid Dispersion and Development of Orally Disintegrating Tablets Using 32 Full Factorial Design

    PubMed Central

    Singh, Jatinderpal; Garg, Rajeev; Gupta, Ghanshyam Das

    2015-01-01

    Present investigation deals with the preparation and evaluation of orally disintegrating tablets (ODTs) of lamotrigine using β-cyclodextrin and PVP-K30 as polymers for the preparation of solid dispersion which help in enhancement of aqueous solubility of this BCS CLASS-II drug and sodium starch glycolate (SSG) and crospovidone as a superdisintegrating agent, to reduce disintegration time. The ODTs were prepared by direct compression method. Nine formulations were developed with different ratios of superdisintegrating agents. All the formulations were evaluated for disintegration time, weight variation, hardness, friability, drug content uniformity, wetting time, and in vitro drug release study. In vitro drug release study was performed using United States Pharmacopoeia (USP) type 2 dissolution test apparatus employing paddle stirrer at 50 rpm using 900 mL of 0.1 N HCl maintained at 37°C ± 0.5°C as the dissolution medium. On the basis of evaluation parameters formulations were prepared using β-CD 1 : 1 solid dispersion. Then 32 full factorial design was applied using SSG and crospovidone in different ratios suggested by using design expert 8.0.7.1 and optimized formulation was prepared using amount of SSG and crospovidone as suggested by the software. The optimized formulation prepared had disintegrating time of 15 s, wetting time of 24 s, and % friability of 0.55. PMID:26634173

  18. The practical approach to the evaluation of methods used to determine the disintegration time of orally disintegrating tablets (ODTs)

    PubMed Central

    Brniak, Witold; Jachowicz, Renata; Pelka, Przemyslaw

    2015-01-01

    Even that orodispersible tablets (ODTs) have been successfully used in therapy for more than 20 years, there is still no compendial method of their disintegration time evaluation other than the pharmacopoeial disintegration test conducted in 800–900 mL of distilled water. Therefore, several alternative tests more relevant to in vivo conditions were described by different researchers. The aim of this study was to compare these methods and correlate them with in vivo results. Six series of ODTs were prepared by direct compression. Their mechanical properties and disintegration times were measured with pharmacopoeial and alternative methods and compared with the in vivo results. The highest correlation with oral disintegration time was found in the case of own-construction apparatus with additional weight and the employment of the method proposed by Narazaki et al. The correlation coefficients were 0.9994 (p < 0.001), and 0.9907 (p < 0.001) respectively. The pharmacopoeial method correlated with the in vivo data much worse (r = 0.8925, p < 0.05). These results have shown that development of novel biorelevant methods of ODT’s disintegration time determination is eligible and scientifically justified. PMID:27134547

  19. Preliminary buprenorphine sublingual tablet pharmacokinetic data in plasma, oral fluid and sweat during treatment of opioid-dependent pregnant women

    PubMed Central

    Concheiro, Marta; Jones, Hendreé E.; Johnson, Rolley E.; Choo, Robin; Huestis, Marilyn A.

    2011-01-01

    Background Buprenorphine is currently under investigation as a pharmacotherapy to treat pregnant women for opioid dependence. This research evaluates buprenorphine (BUP), norbuprenophine (NBUP), buprenorphine-glucuronide (BUP-Gluc) and norbuprenorphine-glucuronide (NBUP-Gluc) pharmacokinetics after high dose (14–20 mg) BUP sublingual tablet administration in three opioid-dependent pregnant women. Methods Oral fluid and sweat specimens were collected in addition to plasma specimens for 24 h during gestation weeks 28 or 29 and 34, and 2 months after delivery. Tmax was not affected by pregnancy; however, BUP and NBUP Cmax and AUC0–24h tended to be lower during pregnancy compared to postpartum levels. Results Statistically significant but weak positive correlations were found for BUP plasma and OF concentrations, and BUP/NBUP ratios in plasma and OF. Conclusion Statistically significant negative correlations were observed for times of specimen collection and BUP and NBUP OF/plasma ratios. BUP-Gluc and NBUP-Gluc were detected in only 5% of OF specimens. In sweat, BUP and NBUP were detected in only 4 of 25 (12 or 24 h) specimens in low concentrations (<2.4 ng/patch). These preliminary data describe BUP and metabolite pharmacokinetics in pregnant women and suggest that, like methadone, upward dose adjustments may be needed with advancing gestation. PMID:21860340

  20. Frovatriptan vs. other triptans for the acute treatment of oral contraceptive-induced menstrual migraine: pooled analysis of three double-blind, randomized, crossover, multicenter studies.

    PubMed

    Allais, G; Tullo, V; Omboni, S; Pezzola, D; Zava, D; Benedetto, C; Bussone, G

    2013-05-01

    Oral contraceptive-induced menstrual migraine (OCMM) is a particularly severe form of migraine triggered by the cyclic hormone withdrawal. To review the efficacy of frovatriptan vs. other triptans, in the acute treatment of OCMM through a pooled analysis of three individual randomized Italian studies. With or without aura migraineurs were randomized to frovatriptan 2.5 mg or rizatriptan 10 mg (study 1), frovatriptan 2.5 mg or zolmitriptan 2.5 mg (study 2), frovatriptan 2.5 mg or almotriptan 12.5 mg (study 3). All studies had a multicenter, randomized, double-blind, crossover design. After treating 1-3 episodes of migraine in 3 months with the first treatment, patients switched to the other treatment for the next 3 months. In this analysis, the subset of 35 of the 280 women of the intention-to-treat population taking combined oral contraceptives and experiencing a migraine attack during the withdrawal phase, were analyzed. The proportion of pain free and pain relief at 2 h were 25 and 51 % with frovatriptan and 28 and 48 % with comparators (p = NS). At 24 h, 71 and 83 % of frovatriptan-treated patients and 60 and 76 % of comparator-treated patients were pain free (p < 0.05 between treatments) and had pain relief (p = NS), respectively. Relapse at 24 and 48 h was significantly (p < 0.05) lower with frovatriptan (17 and 21 %) than with the comparators (27 and 31 %). Our results suggest that, due to its sustained antimigraine effect, frovatriptan may be particularly suitable for the management of OCMM than other triptans. PMID:23695052

  1. Bioequivalence assessment of ambroxol tablet after a single oral dose administration to healthy male volunteers.

    PubMed

    Lee, Hee Joo; Joung, Sun Koung; Kim, Yoon Gyoon; Yoo, Jeong-Yeon; Han, Sang Beom

    2004-01-01

    A bioequivalence study of the ambroxol hydrochloride tablets was conducted. Twenty-four healthy male Korean volunteers received each medicine at the ambroxol hydrochloride dose of 30 mg in a 2 x 2 cross-over study. There was a 1-week washout period between the doses. Plasma concentrations of ambroxol were monitored by a high-performance liquid chromatography (HPLC) for over a period of 24h after the administration. AUC(t) (the area under the plasma concentration-time curve from time 0 to last sampling time, 24h) was calculated by the linear-log trapezoidal rule method. C(max) (maximum plasma drug concentration) and T(max) (time to reach C(max)) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed AUC(t) and C(max), and untransformed T(max). The geometric mean of AUC(t) was 495.8 ng ml(-1)h(-1) (test medication) and 468.3 ng ml(-1)h(-1) (reference medication). C(max) of 61.5 and 57.3 ng ml(-1) were achieved for the test and the reference medication, respectively. The point estimates and 90% confidence intervals for AUC(t) (parametric) and C(max) (parametric) were, in point estimate (90% confidence interval), 1.058 (0.989-1.134) and 1.073 (1.007-1.142), respectively, satisfying the bioequivalence criteria of the European Committee for Proprietary Medicinal Products and the US Food and Drug Administration Guidelines. The corresponding value of T(max) was 0.229 (0.015-0.444). These results indicate that the two medications of ambroxol hydrochloride are bioequivalent and, thus, may be prescribed interchangeably. PMID:14597158

  2. Contraceptive Evaluation.

    ERIC Educational Resources Information Center

    Hulka, Barbara S.; And Others

    The objective of research in contraceptive evaluation is to improve the ability of individuals to choose contraceptive methods best suited to their needs and circumstances and to provide information that will lead to the development of safer and more effective methods. There are usually three considerations in judging the importance of a method of…

  3. 21 CFR 520.2150a - Stanozolol tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ...) Administered orally to cats and small breeds of dogs, 1/2 to 1 tablet twice daily for several weeks; to large breeds of dogs, 1 to 2 tablets twice daily for several weeks. The tablets may be crushed and...

  4. Contraceptive Equity

    PubMed Central

    Temkin, Elizabeth

    2007-01-01

    The Equity in Prescription Insurance and Contraceptive Coverage Act, introduced in Congress in 1997 and still unpassed, seeks to redress health insurers’ failure to pay for birth control as they pay for other prescription drugs, most paradoxically Viagra. In 1936 the International Workers Order (IWO), a fraternal society, became the first insurer to include contraception in its benefits package. A forerunner in the movement for prepaid medical care, the IWO offered its members primary care and contraceptive services for annual flat fees. Founded at a time when the legal status of contraception was in flux, the IWO’s Birth Control Center was the only such clinic to operate on an insurance system. Recent state laws and judicial actions have revived the IWO’s groundbreaking view of contraception as a basic preventive service deserving of insurance coverage. PMID:17761562

  5. [Contraception and pregnancy in adolescence

    PubMed

    Herter, L D; Accetta, S G

    2001-11-01

    OBJECTIVE: To review and discuss different contraceptive methods currently used by adolescents, and also discuss adolescent pregnancy, including the associated risks and the importance of prenatal care. METHODS: Review of literature and clinical experience with different contraceptive methods and with adolescent pregnancy. RESULTS: The oral contraceptive pill is the most common method used by teenagers due to its low failure rate and other non-contraceptive effects. Emergency contraception is a good option in cases of rape, unplanned sexual intercourse, condom rupture, nonuse of oral contraceptives during short intervals. In this case, the pill should be taken within 72 hours after the intercourse (preferably before 24 hours for best effect). Most problems related to adolescent pregnancy have a social or economic origin; however, some medical complications such as preterm labor and anemia are frequently reported. CONCLUSIONS: The use of male and female condoms combined with other contraceptive methods should be encouraged to prevent sexually transmitted diseases. If pregnancy is confirmed, prenatal care must be implemented as soon as possible in order to minimize the risks of complication and to allow for an effective multidisciplinary approach. PMID:14676880

  6. [Chronic illness and contraception].

    PubMed

    Saarikoski, S

    1987-01-01

    In recent years sterilization that can cause problems of the psyche and marital life has been recommended much less frequently with respect to chronic diseases. As regards heart and hypertensive diseases pregnancy is always contraindicated in case of 3rd and 4th disease categories and sterilization is recommended according to the New York Heart Association. As far as 1st and 2nd category patients are concerned if the load carrying capacity is normal pregnancy could be undertaken. Combination pills are not recommended for contraception because they can cause fluid retention or increase the risk of thrombosis. If the patient has a higher-than-normal risk of developing thrombosis or infection, for instance, those who wear pacemakers only tablets containing progesterone or subdermal capsule implants can be used. In those with blood pressure problems the additional use of the IUD is also advised. Among diseases of neurological and psychic origin the effect of hormonal contraceptives is weakened by antiepileptics, but even in such cases older combination pills of larger doses of active ingredients can be employed. Migraine is exacerbated in 1/3 of patients; here IUDs can be used. Even the contraceptive tablets themselves can induce depression. In psychosis methods requiring regular attention can be easily forgotten, therefore the IUD is the most suitable device. In diabetes progesterone and other progestogens reduce insulin response, harm carbohydrate metabolism; therefore in young people the IUD is preferred an in older women with children even sterilization can be employed. Hormonal tablets must not be used in hyperlipidemia and liver diseases. Caution must be exercised in hyperthyroidism and in endocrine disorders (e.g., Cushing's syndrome); if it is accompanied by blood pressure disorders appropriate treatment is required. In kidney diseases pregnancy is contraindicated if it is accompanied by blood pressure increase or a higher level of creatine. On the other hand

  7. Clinical investigation of the biological effects of a new combination low-dose oral contraceptive ('Ovostat E').

    PubMed

    Tarkkila, T; Hulkko, S; Alapiessa, U; Kauraniemi, T

    1977-01-01

    A low-dose contraceptive containing 1 mg of lynestrenol and .05 mg of ethinyl estradiol was studied over 12 cycles in 11 healthy fertile women volunteers. The subjects were aged 20-30 years. Measurements were taken of urinary luteinizing hormone (LH), pregnanediol, and estrogen, and serum progesterone and estradiol values; in addition, on a fixed schedule during treatment, the 3rd, 5th, 7th, and 12th months, vaginal smears and endometrial biopsies were taken, along with SGOT and SGPT determinations. According to determinations, ovulation was inhibited during every cycle tested. A clear estrogenic effect was evident in the karyopyknotic index, during cycle 3, at the beginning of the cycle which became a progestational effect around Day 13 (biphasic). In cycle 6, the indexes of cytology decreased, but during Cycle 12, they rose a bit again. Basal body temperature during treatment was monophasic. Cervical mucus assessed by spinnbarket during treatment was low and arborization absent. The SGOT and SGPT liver function tests were within normal values in all cycles in 7 women; 4 showed clearly higher levels in Cycles 3 and 12. None of the cycles showed the high midcycle urinary excretion of LH. No significant side effects were reported. Examination of the endometrial biopsies showed a drug effect in all cases and there was no secretory activity in any of the samples. These findings confirm clinical results that show this low-dose combination to be an effective contraceptive agent. PMID:162661

  8. Massive pulmonary embolism associated with Factor V Leiden, prothrombin, and methylenetetrahydrofolate reductase gene mutations in a young patient on oral contraceptive pills: a case report.

    PubMed

    Charafeddine, Khalil M; Mahfouz, Rami A; Ibrahim, Georges Y; Taher, Ali T; Hoballah, Jamal J; Taha, Assad M

    2010-10-01

    Factor V Leiden (Factor V G1691A), prothrombin gene mutation G20210A, and homozygous C677T mutation in the methylenetetrahydrofolate reductase (MTHFR) gene are known to predispose venous thromboembolism (VTE). We present herein a rare case of a young woman heterozygous for these mutations and taking oral contraceptive pills for less than 2 months, diagnosed to have massive deep venous thrombosis and bilateral pulmonary embolism. The patient was managed for 10 days in the hospital and discharged home on oral anticoagulants. This case suggests that screening for these factors in people with family history of thrombosis and in relatives of patients with these mutations is highly recommended to prevent fatal consequences. In addition, a new guideline for treatment and prophylaxis with anticoagulant for these patients and others who are at risk of developing VTE (American College of Chest Physicians [ACCP] guidelines-Chest 2008) has been published recently. Our recommendation is to promote for the internationally published algorithms through their application, where necessary, to prevent any future thrombotic morbidity or mortality incidents. PMID:19520679

  9. Effect of food on the oral bioavailability of amlodipine/valsartan and amlodipine/valsartan/hydrochlorothiazide fixed dose combination tablets in healthy subjects.

    PubMed

    Sunkara, Gangadhar; Jiang, Xuemin; Reynolds, Christine; Serra, Denise; Zhang, Yiming; Ligueros-Saylan, Monica; Ayalasomayajula, Surya; Winter, Serge; Jarugula, Venkateswar

    2014-11-01

    A double fixed dose combination of amlodipine/valsartan and triple fixed dose combination of amlodipine/valsartan/HCTZ tablets have been developed to treat patients with moderate-to-severe hypertension. Here, we present the effect of food on the oral bioavailability of these two fixed dose combination tablets from two separate clinical studies in healthy subjects. Single oral doses of amlodipine/valsartan (10/160 mg) and amlodipine/valsartan/HCTZ (10/320/25 mg were administered under fasted or fed conditions. Blood samples were collected in both studies to determine the pharmacokinetic parameters of amlodipine, valsartan, and/or HCTZ using non-compartmental analysis. Following amlodipine/valsartan administration, the geometric mean ratios (GMRs, 90% CI) of AUC0-∞ and Cmax were 1.09 (1.05-1.13) and 1.03 (0.97-1.09) for amlodipine, and 0.94 (0.81-1.10) and 0.86 (0.73-1.02) for valsartan, respectively. Following amlodipine/valsartan/HCTZ administration, the GMRs (90%CI) of AUC0-∞ and Cmax were 1.09 (1.04-1.15) and 1.11 (1.05-1.08) for amlodipine, 1.14 (0.99-1.31) and 1.12 (0.98-1.29) for valsartan, and 1.09 (1.02-1.16) and 0.86 (0.79-0.93) for HCTZ, respectively. Considering the sample size and pharmacokinetic variability associated with analytes, these study results indicate that food effect is minimal or none when fixed dose combination tablets are administered with food. In conclusion, both fixed dose combination tablets can be administered without regards to meals. PMID:27129123

  10. 21 CFR 520.1284 - Sodium liothyronine tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Sodium liothyronine tablets. 520.1284 Section 520... liothyronine tablets. (a) Specifications. Sodium liothyronine tablets consist of tablets intended for oral administration which contain liothyronine at 60 or 120 micrograms per tablet, as the sodium salt. (b)...

  11. 21 CFR 520.1284 - Sodium liothyronine tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Sodium liothyronine tablets. 520.1284 Section 520... liothyronine tablets. (a) Specifications. Sodium liothyronine tablets consist of tablets intended for oral administration which contain liothyronine at 60 or 120 micrograms per tablet, as the sodium salt. (b)...

  12. 21 CFR 520.1284 - Sodium liothyronine tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Sodium liothyronine tablets. 520.1284 Section 520... liothyronine tablets. (a) Specifications. Sodium liothyronine tablets consist of tablets intended for oral administration which contain liothyronine at 60 or 120 micrograms per tablet, as the sodium salt. (b)...

  13. Is oral contraceptive-induced headache dependent on patent foramen ovale? Clinical dynamics, evidence-based hypothesis and possible patient-oriented management.

    PubMed

    Chiofalo, Benito; Laganà, Antonio Simone; Imbesi, Giovanna; Vitale, Salvatore Giovanni; Catena, Ursula; Campolo, Federica; Lanzo, Gabriele; Centini, Gabriele; Triolo, Onofrio

    2016-09-01

    Secondary headache is one of the most common side effect during oral contraceptive (OC) treatment and it leads many patients to stop the therapy. Patent foramen ovale (PFO) is an interatrial communication that spontaneously closes at birth in about 75% of the population. However, in the rest of adults PFO maintains a direct communication between the right and left side of circulation. In these patients PFO is a tunnel-like structure that could allow a blood clot to pass from the right to the left side of circulation, thus can cause paradoxical embolization. Although an increased frequency of PFO in patients with migraine was already reported, the relationship between PFO and migraine remains uncertain. In patients with migraine, the prevalence of moderate or large PFO is 35% and seems not associated with the presence of aura or the frequency of headache. Basing on these assumptions, we hypothesize that asymptomatic PFO could play a role in secondary headache due to OC. The procoagulant effect of OC improves the production of microemboli that through the POF could pass from the right to the left atrium and than to the brain, where they could be responsible of secondary headache. If our hypothesis would be confirmed in future studies, it would be possible to identify high-risk patients for developing OC-induced headache and other cerebrovascular major diseases through transcranial Doppler and transesophageal echocardiography. This scenario may radically change the management of reproductive-age woman who have to undergo OC therapy for contraception or other medical conditions. PMID:27515209

  14. Increased risk of stroke in oral contraceptive users carried replicated genetic variants: a population-based case-control study in China.

    PubMed

    Wang, Chun; Li, Ying; Li, Huiqiao; Sun, Tao; Jin, Guangfu; Sun, Zhiming; Zhou, Jian; Ba, Lei; Huang, Zhizheng; Bai, Jianling

    2012-08-01

    Combined oral contraceptives (COC) use is a unique risk factor for stroke in women, and may modify the associations between genetic polymorphisms and stroke. To investigate whether the genetic variants identified in a recent genome-wide association study (GWAS) could be replicated in Chinese women, as well as, whether related risk was different in COC users, 451 stroke cases and 831 age- and region-matched controls were recruited from our cohort. Genotyping of 3 SNPs (rs700651, rs10958409, and rs1333040) was performed by the polymerase chain reaction assay with TaqMan probes. The history of contraceptive use and relevant information were obtained from a face-to-face interview. Odds ratios (OR) with 95 % confidence interval (CI) were estimated under conditional logistic regression model after adjustment for cardiovascular covariates. Our study replicated the associations of rs10958409 and rs1333040, with the risk of stroke, especially hemorrhagic subtype, but failed to confirm association of rs700651. COC use was associated with a 1.56-fold (OR 1.56, 95 % CI 1.21-2.01) increased risk of stroke. COC users with rs10958409 GA/AA or rs1333040 CT/TT genotypes had an increased risk of overall stroke by 1.59-fold (OR 2.59, 95 % CI 1.59-4.19) and 3.24-fold (OR 4.24, 95 % CI 1.71-10.49), respectively, compared with the non-users with wild-type genotypes. Moreover, the risk of hemorrhagic stroke increased by 4.81- and 15.06-fold when risk allele carriers of rs10958409 or rs1333040 who took COC. Our results confirmed the associations of two GWAS SNPs, also suggested combination effects of these genetic variants and COC use on stroke risk. PMID:22476622

  15. [Involvement of zinc in taste disturbance occurring during treatment for malignant tumor in the chest and the effects of polaprezinc oral disintegrating tablets (a retrospective study)].

    PubMed

    Nakata, Yoko; Hirashima, Tomonori; Kondou, Yoko; Tokuoka, Yoshie; Imazato, Hitomi; Iwata, Kaori; Oomori, Yukari; Yamato, Akihiro; Shimizu, Saburou; Nagao, Sadako; Matsui, Kaoru; Abe, Noriko

    2008-06-01

    We analyzed the correlation between serum zinc levels and taste disturbance, and between patient backgrounds and serum zinc levels or taste disturbance, and evaluated the effects of polaprezinc oral disintegrating tablets on taste disturbance in 29 patients with lung cancer and one patient with malignant pleural mesothelioma who were receiving chemotherapy. Taste disturbance developed in 11 (36.7%) out of 30 patients. Serum zinc levels significantly correlated with taste disturbance (p=0.0227). Serum zinc levels were significantly lower (p=0.0235) and taste disturbance tended to be more frequent (p=0.0625) in males. Polaprezinc improved taste disturbance in 5 of 8 patients. PMID:18633224

  16. Ambulatory blood pressure monitoring (ABPM) in the normal menstrual cycle and in women using oral contraceptives. Comparison with conventional blood pressure measurement.

    PubMed

    Williamson, P M; Buddle, M L; Brown, M A; Whitworth, J A

    1996-10-01

    This study was undertaken to determine if blood pressures (BP) assessed by routine sphygmomanometry and 24 h ambulatory monitoring (ABPM) alter throughout the normal menstrual cycle or in the cycle of women using oral contraceptive pills (OCP), and the interrelationships between urinary sodium (Na) and potassium (K) excretion and ABPM throughout the menstrual cycle. Eleven women with a normal ovulatory cycle (ovulatory) and ten age-matched women taking an oral contraceptive pill (OCP) were studied three times in random order during their menstrual cycle, within days 1 to 5, 13 to 16, and 25 to 28. Twenty-four hour urine Na, K, and creatinine (Cr) excretion and serum Na, K, Cr, cortisol, estradiol, progesterone and plasma renin, angiotensinogen, and aldosterone concentrations were measured. BP was measured by a mercury sphygmomanometer and by 24 h BP (Accutracker II). On days 1 to 5, daytime systolic BP was higher in OCP [mean: 123 mm Hg, 95% confidence interval: 117, 128] than ovulatory women [114 mm Hg (109, 118); P = .011] though daytime diastolic BPs were similar [OCP: 71 (68, 75), ovulatory: 69 (66, 72)]. This difference in daytime systolic BP between groups was also apparent at both of the other stages of the menstrual cycle. Nighttime systolic BPs were significantly higher in OCP users on days 13 to 16 (P < .05) and days 25 to 28 (P < .01). In women taking OCPs, daytime ABPM for days 1 to 5 were higher than their office readings by 15 (7,23)/11 (7,15) mm Hg (P = .001), whereas office and ABPM readings were similar in ovulatory women. This pattern was evident at all three stages. There was no significant change in BP throughout the menstrual cycle within either group, and no correlation between urine Na or K and BP. Systolic BPs are higher throughout the menstrual cycle in women who take OCPs than in ovulatory women but this difference is only detected when ambulatory blood pressure is assessed. Blood pressure does not change subsequently in either ovulatory

  17. The effects of screw configuration and polymeric carriers on hot-melt extruded taste-masked formulations incorporated into orally disintegrating tablets.

    PubMed

    Morott, Joseph T; Pimparade, Manjeet; Park, Jun-Bom; Worley, Chelsea P; Majumdar, Soumyajit; Lian, Zhuoyang; Pinto, Elanor; Bi, Yunxia; Durig, Thomas; Repka, Michael A

    2015-01-01

    The primary aim of this research was to produce successfully taste masked formulations of Sildenafil Citrate (SC) using hot-melt extrusion (HME) technology. Multiple screw configurations and polymeric carriers were evaluated for their effects on taste masking efficiency, which was assessed by both E-tongue analysis and in vitro dissolution in simulated salivary fluid (SSF, pH 6.8 artificial saliva). The screw configurations were further assessed for their effects on the morphology of the API using PXRD, FT-IR and mid-infrared chemical imaging. It was determined that the screw configuration had a profound effect on the taste masking efficiency of the formulations as a result of altering the physical state of the API. Selected extruded formulations using ethylcellulose (EC) with a pore former were further formulated into orally disintegrating tablets (ODTs), which were optimized by varying the grade and percentage of the superdisintegrant used. An optimized disintegration time of approximately 8 seconds was achieved. The final ODT formulation exhibited excellent taste masking properties with over 85% drug release in gastric media as well as physical tablet properties. Interestingly, friability, which tends to be a common concern when formulating ODTs, was well within the acceptable limits (<1%) for common tablets. PMID:25410968

  18. The Effects of Screw Configuration and Polymeric Carriers on Hot-Melt Extruded Taste-Masked Formulations Incorporated into Orally Disintegrating Tablets

    PubMed Central

    Morott, Joseph T.; Pimparade, Manjeet; Park, Jun-Bom; Worley, Chelsea P.; Majumdar, Soumyajit; Lian, Zhuoyang; Pinto, Elanor; Bi, Yunxia; Durig, Thomas; Repka, Michael A.

    2015-01-01

    The primary aim of this research was to produce successfully taste masked formulations of Sildenafil Citrate (SC) using hot-melt extrusion (HME) technology. Multiple screw configurations and polymeric carriers were evaluated for their effects on taste masking efficiency, which was assessed by both E-tongue analysis and in vitro dissolution in simulated salivary fluid (SSF, pH 6.8 artificial saliva). The screw configurations were further assessed for their effects on the morphology of the API using PXRD, FT-IR and mid-infrared chemical imaging. It was determined that the screw configuration had a profound effect on the taste masking efficiency of the formulations as a result of altering the physical state of the API. Selected extruded formulations using ethylcellulose (EC) with a pore former were further formulated into orally disintegrating tablets (ODTs), which were optimized by varying the grade and percentage of the superdisintegrant used. An optimized disintegration time of approximately 8 seconds was achieved. The final ODT formulation exhibited excellent taste masking properties with over 85% drug release in gastric media as well as physical tablet properties. Interestingly, friability, which tends to be a common concern when formulating ODTs, was well within the acceptable limits (<1%) for common tablets. PMID:25410968

  19. Drospirenone/ethinylestradiol 3mg/20microg (24/4 day regimen): a review of its use in contraception, premenstrual dysphoric disorder and moderate acne vulgaris.

    PubMed

    Fenton, Caroline; Wellington, Keri; Moen, Marit D; Robinson, Dean M

    2007-01-01

    Drospirenone 3mg with ethinylestradiol 20microg (Yaz) is a low-dose combined oral contraceptive (COC) administered in a regimen of 24 days of active tablets followed by a short hormone-free interval (4 days; 24/4 regimen). Drospirenone, unlike other synthetic progestogens used in COCs, is a 17alpha-spirolactone derivative and a 17alpha-spironolactone analogue with antimineralocorticoid and antiandrogenic properties. Drospirenone/ethinylestradiol 3mg/20microg (24/4) is approved in the US for the prevention of pregnancy in women, for the treatment of the symptoms of premenstrual dysphoric disorder (PMDD) and for the treatment of moderate acne vulgaris in women who wish to use an oral contraceptive for contraception.Drospirenone/ethinylestradiol 3mg/20microg (24/4) provided 99% contraceptive protection over 1 year of treatment in two large studies. The same treatment regimen over three treatment cycles also significantly improved the emotional and physical symptoms associated with PMDD, and improved moderate acne vulgaris over six treatment cycles in double-blind trials. It was generally well tolerated, with adverse events generally typical of those experienced with other COCs and which were most likely to occur in the first few cycles. Clinical trials indicate that drospirenone/ethinylestradiol 3mg/20microg (24/4) is a good long-term contraceptive option, and additionally offers relief of symptoms that characterise PMDD and has a favourable effect on moderate acne vulgaris. PMID:17683173

  20. Emerging Options for Emergency Contraception

    PubMed Central

    Koyama, Atsuko; Hagopian, Laura; Linden, Judith

    2013-01-01

    Emergency post-coital contraception (EC) is an effective method of preventing pregnancy when used appropriately. EC has been available since the 1970s, and its availability and use have become widespread. Options for EC are broad and include the copper intrauterine device (IUD) and emergency contraceptive pills such as levonorgestrel, ulipristal acetate, combined oral contraceptive pills (Yuzpe method), and less commonly, mifepristone. Some options are available over-the-counter, while others require provider prescription or placement. There are no absolute contraindications to the use of emergency contraceptive pills, with the exception of ulipristal acetate and mifepristone. This article reviews the mechanisms of action, efficacy, safety, side effects, clinical considerations, and patient preferences with respect to EC usage. The decision of which regimen to use is influenced by local availability, cost, and patient preference. PMID:24453516

  1. New regulations for oral contraceptive prescription in France in 2013: what is the impact on adult female acne?

    PubMed

    Leclerc-Mercier, Stéphanie; Buisson, Virginie; Dreno, Brigitte

    2016-08-01

    In 2012, a young French woman lodged a complaint against a pharmaceutical company having suffered a cerebral stroke. The French health authority recommended all prescribers of hormonal contraception (HCP) to favour second-generation HCP. To evaluate the consequences of these recommendations on female acne. A prospective multicentre study using a standardised questionnaire completed by 1,724 women. The mean age was 26.57 years; 58.7% of the women had changed their HCP during the last 12 months. The initial ratio of first or second/third or fourth-generation drugs was 5.5%/82.9% which changed after the recommendations to 70.6%/29.4%. Among the patients who switched from third or fourth to first or second-generation drugs, 83.9% considered that their acne had worsened (p<0.0001). In those patients who received a local acne treatment, 72.1% had additional systemic treatment. This study confirms the important rise in prescriptions of first or second-generation HCP. This switch has resulted in a significant increase in acne, requiring treatment for the large majority of patients, thus confirming the role of a hormonal factor in female acne. PMID:27312707

  2. Emergency contraception.

    PubMed

    Gold, M A

    2000-01-01

    High rates of adolescent pregnancy remain a challenge for health care providers. For most sexually active adolescents, pregnancy is unintended. Emergency contraception, also called the "morning-after-pill" or postcoital contraception, is a way to prevent pregnancy after unprotected intercourse. In the United States, three forms of emergency contraception currently are available: high-dose combination estrogen and progestin pills, high-dose progestin-only pills, and postcoital insertion of a copper intrauterine device. The postcoital intrauterine device is used infrequently. When emergency contraceptive pills (ECPs) are taken within 72 hours of unprotected intercourse, they reduce the risk of pregnancy by at least 75%. However, they are most effective if taken within 24 hours of coitus. Eleven brands of pills currently are marketed in the United States that conform to the regimens approved by the Food and Drug Administration (FDA) for this indication. Recently, two prepackaged ECPs were approved by the FDA. The only medical contraindication to prescribing ECPs is pregnancy. The most common side effects are nausea and vomiting, followed by menstrual disturbances, breast tenderness, abdominal cramping, dizziness, headache, and mood changes. Because vomiting can compromise the efficacy of ECPs, routine pretreatment with an antiemetic is recommended. Primary care providers can reduce unintended adolescent pregnancy by routinely counseling adolescents at all office visits about the existence of emergency contraception and by prescribing it in advance and over the telephone. PMID:10959448

  3. Pharmacokinetic Comparative Study of Gastrodin and Rhynchophylline after Oral Administration of Different Prescriptions of Yizhi Tablets in Rats by an HPLC-ESI/MS Method

    PubMed Central

    Ge, Zhaohui; Liang, Qionglin; Wang, Yiming; Luo, Guoan

    2014-01-01

    Pharmacokinetic characters of rhynchophylline (RIN), gastrodin (GAS), and gastrodigenin (p-hydroxybenzyl alcohol, HBA) were investigated after oral administration of different prescriptions of Yizhi: Yizhi tablets or effective parts of tianma (total saponins from Gastrodiae, EPT) and gouteng (rhynchophylla alkaloids, EPG). At different predetermined time points after administration, the concentrations of GAS, HBA, and RIN in rat plasma were determined by an HPLC-ESI/MS method, and the main pharmacokinetic parameters were investigated. The results showed that the pharmacokinetic parameters Cmax and AUC0–∞ (P < 0.05) were dramatically different after oral administration of different prescriptions of Yizhi. The data indicated that the pharmacokinetic processes of GAS, HBA, and RIN in rats would interact with each other or be affected by other components in Yizhi. The rationality of the compatibility of Uncaria and Gastrodia elata as a classic “herb pair” has been verified from the pharmacokinetic viewpoint. PMID:25610474

  4. Pharmacokinetic Comparative Study of Gastrodin and Rhynchophylline after Oral Administration of Different Prescriptions of Yizhi Tablets in Rats by an HPLC-ESI/MS Method.

    PubMed

    Ge, Zhaohui; Xie, Yuanyuan; Liang, Qionglin; Wang, Yiming; Luo, Guoan

    2014-01-01

    Pharmacokinetic characters of rhynchophylline (RIN), gastrodin (GAS), and gastrodigenin (p-hydroxybenzyl alcohol, HBA) were investigated after oral administration of different prescriptions of Yizhi: Yizhi tablets or effective parts of tianma (total saponins from Gastrodiae, EPT) and gouteng (rhynchophylla alkaloids, EPG). At different predetermined time points after administration, the concentrations of GAS, HBA, and RIN in rat plasma were determined by an HPLC-ESI/MS method, and the main pharmacokinetic parameters were investigated. The results showed that the pharmacokinetic parameters C max and AUC0-∞ (P < 0.05) were dramatically different after oral administration of different prescriptions of Yizhi. The data indicated that the pharmacokinetic processes of GAS, HBA, and RIN in rats would interact with each other or be affected by other components in Yizhi. The rationality of the compatibility of Uncaria and Gastrodia elata as a classic "herb pair" has been verified from the pharmacokinetic viewpoint. PMID:25610474

  5. Effects of oral contraceptive use on the salivary testosterone and cortisol responses to training sessions and competitions in elite women athletes.

    PubMed

    Crewther, Blair T; Hamilton, Dave; Casto, Kathleen; Kilduff, Liam P; Cook, Christian J

    2015-08-01

    This study examined the salivary testosterone (T) and cortisol (C) responses of elite women hockey players across 4 activities (light and heavy training, club and International competitions). The players formed an oral contraceptive (OC) group (n=10) and a Non-OC (n=19) group for analysis. The Non-OC group had higher T levels (by 31-52%) across all activities, whilst the OC group showed signs of reduced T and C reactivity when data were pooled. As a squad, positive T and C changes occurred with heavy training (45%, 46%), club competitions (62%, 80%) and International competitions (40%, 27%), respectively. Our results confirm that OC use lowers T levels in women athletes whilst reducing the T and C responses to training and competition activities within the sporting environment. Differences in the physical and/or psychological demands of the sporting activity could be contributing factors to the observed hormone responses. These factors require consideration when applying theoretical models in sport, with broader implications for women around exercising behaviours and stress physiology. PMID:25866255

  6. Prospective multicenter randomized intermediate biomarker study of oral contraceptive versus depo-provera for prevention of endometrial cancer in women with Lynch syndrome.

    PubMed

    Lu, Karen H; Loose, David S; Yates, Melinda S; Nogueras-Gonzalez, Graciela M; Munsell, Mark F; Chen, Lee-May; Lynch, Henry; Cornelison, Terri; Boyd-Rogers, Stephanie; Rubin, Mary; Daniels, Molly S; Conrad, Peggy; Milbourne, Andrea; Gershenson, David M; Broaddus, Russell R

    2013-08-01

    Women with Lynch syndrome have a 40% to 60% lifetime risk for developing endometrial cancer, a cancer associated with estrogen imbalance. The molecular basis for endometrial-specific tumorigenesis is unclear. Progestins inhibit estrogen-driven proliferation, and epidemiologic studies have shown that progestin-containing oral contraceptives (OCP) reduce the risk of endometrial cancer by 50% in women at general population risk. It is unknown whether they are effective in women with Lynch syndrome. Asymptomatic women ages 25 to 50 with Lynch syndrome were randomized to receive the progestin compounds Depo-Provera (depo-MPA) or OCP for three months. An endometrial biopsy and transvaginal ultrasound were conducted before and after treatment. Endometrial proliferation was evaluated as the primary endpoint. Histology and a panel of surrogate endpoint biomarkers were evaluated for each endometrial biopsy as secondary endpoints. A total of 51 women were enrolled, and 46 completed treatment. Two of the 51 women had complex hyperplasia with atypia at the baseline endometrial biopsy and were excluded from the study. Overall, both depo-MPA and OCP induced a dramatic decrease in endometrial epithelial proliferation and microscopic changes in the endometrium characteristic of progestin action. Transvaginal ultrasound measurement of endometrial stripe was not a useful measure of endometrial response or baseline hyperplasia. These results show that women with Lynch syndrome do show an endometrial response to short-term exogenous progestins, suggesting that OCP and depo-MPA may be reasonable chemopreventive agents in this high-risk patient population. PMID:23639481

  7. Prospective, Multi-center Randomized Intermediate Biomarker Study of Oral Contraceptive vs. Depo-Provera for Prevention of Endometrial Cancer in Women with Lynch Syndrome

    PubMed Central

    Lu, Karen H.; Loose, David S.; Yates, Melinda S.; Nogueras-Gonzalez, Graciela M.; Munsell, Mark F.; Chen, Lee-may; Lynch, Henry; Cornelison, Terri; Boyd-Rogers, Stephanie; Rubin, Mary; Daniels, Molly S.; Conrad, Peggy; Milbourne, Andrea; Gershenson, David M.; Broaddus, Russell R.

    2013-01-01

    Women with Lynch syndrome have a 40–60% lifetime risk for developing endometrial cancer, a cancer associated with estrogen imbalance. The molecular basis for endometrial-specific tumorigenesis is unclear. Progestins inhibit estrogen-driven proliferation, and epidemiologic studies have demonstrated that progestin-containing oral contraceptives (OCP) reduce the risk of endometrial cancer by 50% in women at general population risk. It is unknown if they are effective in women with Lynch syndrome. Asymptomatic women age 25–50 with Lynch syndrome were randomized to receive the progestin compounds depo-Provera (depoMPA) or OCP for three months. An endometrial biopsy and transvaginal ultrasound were performed before and after treatment. Endometrial proliferation was evaluated as the primary endpoint. Histology and a panel of surrogate endpoint biomarkers were evaluated for each endometrial biopsy as secondary endpoints. A total of 51 women were enrolled, and 46 completed treatment. Two of the 51 women had complex hyperplasia with atypia at the baseline endometrial biopsy and were excluded from the study. Overall, both depoMPA and OCP induced a dramatic decrease in endometrial epithelial proliferation and microscopic changes in the endometrium characteristic of progestin action. Transvaginal ultrasound measurement of endometrial stripe was not a useful measure of endometrial response or baseline hyperplasia. These results demonstrate that women with Lynch syndrome do show an endometrial response to short term exogenous progestins, suggesting that OCP and depoMPA may be reasonable chemopreventive agents in this high-risk patient population. PMID:23639481

  8. WWOX CNV-67048 Functions as a Risk Factor for Epithelial Ovarian Cancer in Chinese Women by Negatively Interacting with Oral Contraceptive Use

    PubMed Central

    Chen, Yongxiu; Tan, Xiaochang; Ding, Yongli; Mai, Bi; Huang, Xiaowen; Hu, Guiying

    2016-01-01

    Copy number variations (CNVs) have attracted increasing evidences to represent their roles as cancer susceptibility regulators. However, little is known about the role of CNV in epithelia ovarian cancer (EOC). Recently, the CNV-67048 of WW domain-containing oxidoreductase (WWOX) was reported to alter cancer risks. Considering that WWOX also plays a role in EOC, we hypothesized that the CNV-67048 was associated with EOC risk. In a case-control study of 549 EOC patients and 571 age (±5 years) matched cancer-free controls, we found that the low copy number of CNV-67048 (1-copy and 0-copy) conferred a significantly increased risk of EOC (OR = 1.346, 95% CI = 1.037–1.747) and it determined the risk by means of copy number-dependent dosage effect (P = 0.009). Data from TCGA also confirmed the abovementioned association as the frequency of low copies in EOC group was 3.68 times more than that in healthy group (P = 0.023). The CNV also negatively interacted with oral contraceptive use on EOC risk (P = 0.042). Functional analyses further showed a lower mRNA level of WWOX in tissues with the 0-copy or 1-copy than that in those with the 2-copy (P = 0.045). Our data suggested the CNV-67048 to be a risk factor of EOC in Chinese women. PMID:27190995

  9. Effects of a monophasic combined oral contraceptive containing nomegestrol acetate and 17β-oestradiol in comparison to one containing levonorgestrel and ethinylestradiol on markers of endocrine function

    PubMed Central

    Ågren, Ulla M; Anttilat, Marjatta; Mäenpää-Liukko, Kristiina; Rantala, Maija-Liisa; Rautiainen, Hilkka; Sommer, Werner F; Mommers, Ellen

    2011-01-01

    Objectives To compare the effects of two monophasic combined oral contraceptives, containing either nomegestrol acetate/17β-oestradiol (NOMAC/E2) or levonorgestrel/ ethinylestradiol (LNG/EE) on endocrine function, androgens, and sex hormone-binding globulin (SHBG). Methods Randomised, open-label, multi-centre trial involving 121 healthy women, aged 18-50 years old. Participants received NOMAC/E2 (2.5 mg/1.5 mg) in a 24/4-day regimen (n = 60) or LNG/EE (150 μg/30 μg) in a 21/7-day regimen (n = 61) for six cycles. The primary outcome was the change from baseline to cycle 6 in markers of adrenal and thyroid function, androgens, and SHBG. Results Total cortisol, corticosteroid-binding globulin (CBG), and thyroxine-binding globulin (TBG) increased from baseline in both groups, with significantly greater increases in the LNG/EE group. No relevant changes from baseline or differences between the groups were observed for thyroid-stimulating hormone (TSH) and free thyroxine (T4). Androgens and androgen precursors decreased from baseline in both groups, with significantly greater decreases in the LNG/EE group (except for free testosterone). A greater increase in SHBG was observed with NOMAC/E2 than with LNG/EE. Conclusions NOMAC/E2 has significantly less influence on markers of adrenal and thyroid function and androgens than LNG/EE. The clinical relevance of these findings requires further study. PMID:21942708

  10. Effect of oral contraceptive use on the incidence of dry socket in females following impacted mandibular third molar extraction: a meta-analysis.

    PubMed

    Xu, J-L; Sun, L; Liu, C; Sun, Z-H; Min, X; Xia, R

    2015-09-01

    The aim of this comprehensive meta-analysis was to provide evidence-based data to test whether oral contraceptive (OC) use can promote the incidence of dry socket (DS) in females following impacted mandibular third molar extraction. PubMed, the Cochrane Library, and Elsevier Science Direct databases were searched. The pooled risk ratio (RR) with 95% confidence interval (CI) was calculated using fixed-effects or random-effects model analysis. Heterogeneity among studies was evaluated with the Cochran test and I(2) statistic. Study quality was assessed with the Newcastle-Ottawa scale. Of 70 articles identified in the search, 12 reporting 16 clinical controlled trials were included in this study. The incidence of DS was significantly greater in the OC groups than in the control groups (RR 1.80, 95% CI 1.33-2.43). Subgroup analyses showed that the unit assessed (tooth or patient), the region in which the study was conducted, and the intervention were not related to the incidence of DS in females taking OC after impacted mandibular third molar extraction. The sensitivity analysis showed no significant change when any one study was excluded. Publication bias was also not detected. This study suggests that OC use may promote the incidence of DS in females following impacted mandibular third molar extraction. PMID:26116066

  11. The 'nonmenstrual woman' in the new millennium? Discourses on menstrual suppression in the first decade of extended cycle oral contraception use in Canada.

    PubMed

    Granzow, Kara

    2014-06-01

    In the early-twenty-first century, extended cycle oral contraception (ECOC) became available by physician prescription in North America. Researchers speculate that this drug, with its capacity to reduce or eliminate menstrual bleeding, may shift not only women's biological processes but also their experiences of menstruation. In this paper, I discuss women's experiences of menstrual suppression drawing on findings from a qualitative study conducted before ECOC was available, and examine these findings against recently published research on menstrual suppression in an ECOC era. Findings suggest that the body as a natural entity figures strongly in women's discourses on suppression. They further suggest that suppression is a contingent, paradoxical and practical achievement, not a securely or fully realised embodied state. This paper reads women's accounts of menstrual suppression prior to ECOC as a challenge to the modern artifice of a mind/body split, and questions whether this challenge is perhaps made less discernible in an ECOC era, where attention may no longer be paid to the daily practices of menstrual suppression. Hence, a case is made for the varied political effects of ongoing non-menstruation versus event-specific practices of non-menstruation. PMID:24735380

  12. Co-existence of a giant splenic hemangioma and multiple hepatic hemangiomas and the potential association with the use of oral contraceptives: a case report

    PubMed Central

    Chatzoulis, George; Kaltsas, Andreas; Daliakopoulos, Stauros; Sallam, Osama; Maria, Kaltsa; Chatzoulis, Kostas; Pachiadakis, Ioannis

    2008-01-01

    Introduction Hepatic and splenic hemangiomas are common benign tumors that mainly affect female patients. Giant splenic hemangiomas are extremely rare, especially when correlated with multiple hepatic hemangiomas. Pathogenetic mechanisms between hemangiomas and oral contraceptives, as well as therapeutic approaches, are analyzed in this case report, in particular for the management of synchronous splenic and hepatic hemangiomas. Case presentation We report here a 42-year-old woman with a giant splenic hemangioma, multiple hepatic hemangiomas and a history of oral estrogen intake for many years. At first it was difficult to determine the organ from which the giant hemangioma originated. Angiography proved extremely helpful in tracing its origin in the spleen. Hematomas in the giant hemangioma posed a significant threat of rupture and catastrophic hemorrhage. We left the small hepatic hemangiomas in place, and removed the spleen along with the giant splenic hemangioma. Conclusion Diagnostic pitfalls in the determination of the origin of this giant hemangioma, attribution of its origin to the spleen angiographically, the unusual co-existence of the giant splenic hemangioma with multiple hepatic ones, and the potential threat of rupture of the giant hemangioma are some of the highlights of this case report. Estrogen administration represents a pathogenic factor that has been associated with hemangiomas in solid organs of the abdominal cavity. The therapeutic dilemma between resection and embolization of giant hemangiomas is another point of discussion in this case report. Splenectomy for the giant splenic hemangioma eliminates the risk of rupture and malignant degeneration, whereas observation for the small hepatic ones (<4 cm) was the preferable therapeutic strategy in our patient. PMID:18462497

  13. Oral contraceptives alter circadian rhythm parameters of cortisol, melatonin, blood pressure, heart rate, skin blood flow, transepidermal water loss, and skin amino acids of healthy young women.

    PubMed

    Reinberg, A E; Touitou, Y; Soudant, E; Bernard, D; Bazin, R; Mechkouri, M

    1996-08-01

    Sixteen healthy women users and nonusers of oral contraceptives (OC) volunteered to document a set of circadian rhythms. Nine were taking OC providing ethynyl estradiol (0.03-0.05 mg/24h, 21 days/month) combined with DL- or L-norgestrel or norethisterone. There was no group difference (p > 0.05) in median age (22 years), weight (57 kg), and height (162) cm). Data were obtained at fixed hours, 5 times/24h, during a 48-h span, in November. (Day activity from approximately 08:00 to approximately 23:00 h and night rest). Environmental conditions were controlled, using air-conditioned rooms of constant temperature (26 degrees +/- 0.5) and relative humidity 45% +/- 1. Both cosinor and ANOVA were used for statistical analyses. All circadian rhythms were validated with one exception: that of salivary melatonin was not detected in OC users. The 24h mean (M) exhibited group differences for certain variables: M was greater in OC than non-OC users for systolic blood pressure (p < 0.0001), heart rate (p < 0.01), skin blood flow (p < 0.04), and transepidermal water loss (p < 0.02). M was lower in OC than non-OC users in salivary cortisol (p < 0.04) and skin amino acids (p < 0.003). No group difference was detected in any other documented rhythms: diastolic blood pressure, grip strength of both hands, oral temperature, self-rated fatigue, and the skin variables of urea, lactate, triglycerides, and acid phosphatase activity. PMID:8874983

  14. Reversible contraception for the woman over 35 years of age.

    PubMed

    Archer, D F

    1992-12-01

    Methods of reversible contraception, oral contraceptives, intrauterine devices, and Norplant (systemic progestin-only contraceptive; Wyeth-Ayerst, Radnor, PA), can be used for women over 35 years of age. Oral contraceptive formulations are safe and effective for healthy women up to the age of menopause. Oral contraceptives in women who do not smoke cigarettes do not result in a significant increased risk for cardiovascular disease. The incidence of breast cancer is not increased in women who have used oral contraceptives. A slight increase was found in younger women who had been on oral contraceptives based on a reanalysis of the contraceptive and steroid hormone study of the Centers for Disease Control. A reduction in the incidence of ovarian epithelial neoplasia by 40% was found in three European case-control studies. Two intrauterine devices are currently available on the US market: Paragard (GynoPharma, Somerville, NJ) and Progestasert (Alza Corp., Palo Alto, CA). Both of these provide highly effective contraception. A World Health Organization prospective randomized study found that there was an increase in pelvic inflammatory disease rates in the first 20 days after intrauterine device insertion. The intrauterine device itself did not increase the pelvic inflammatory disease incidence rates. The Norplant system exerts its contraceptive action through ovulation inhibition and alteration of cervical mucus. The major consumer complaint is irregular or prolonged uterine bleeding, which can be controlled by oral estrogen. PMID:1450355

  15. Simultaneous LC-MS/MS determination of five tripterygium pyridine alkaloids in dog plasma and its application to their pharmacokinetic study after oral administration of tripterygium glycosides tablets.

    PubMed

    Su, Meng-xiang; Song, Min; Yang, Da-song; Shi, Jin-fang; Di, Bin; Hang, Tai-jun

    2015-05-15

    A sensitive and selective liquid chromatography tandem mass spectrometric method was developed and validated for the simultaneous determination of five pyridine alkaloids contained in tripterygium glycosides tablets (triptolide, wilforine, wilforgine, wilfording and wilfortrine) in dog plasma. The analysis was carried out on a Sepax GP-Phenyl column using a mixture of methanol and 10mmol/L ammonium formate buffer solution containing 0.1% formic acid (75:25, v/v) as the mobile phase pumped at a flow-rate of 1.0mL/min. All MS data were obtained in the positive ESI mode with selective multiple reaction monitoring of ion transitions. The method was fully validated to be accurate and precise with a linear range of 0.2-1000ng/mL for triptolide and 0.05-1000ng/mL for the other four pyridine alkaloids. The intra-day and inter-day precisions (relative standard deviation, RSD, %) were within 10.6% and 14.0%, respectively, and the relative error (RE, %) were all less than 13.1%. The method was successfully applied to multi-components pharmacokinetic study of the five pyridine alkaloids in beagle dogs after a single oral administration of 3mg/kg and 30mg/kg tripterygium glycosides tablets, respectively, and a multiple oral administration of 30mg/kg for 6 consecutive days. PMID:25855315

  16. Male contraception.

    PubMed

    Chao, Jing; Page, Stephanie T; Anderson, Richard A

    2014-08-01

    Clear evidence shows that many men and women would welcome new male methods of contraception, but none have become available. The hormonal approach is based on suppression of gonadotropins and thus of testicular function and spermatogenesis, and has been investigated for several decades. This approach can achieve sufficient suppression of spermatogenesis for effective contraception in most men, but not all; the basis for these men responding insufficiently is unclear. Alternatively, the non-hormonal approach is based on identifying specific processes in sperm development, maturation and function. A range of targets has been identified in animal models, and targeted effectively. This approach, however, remains in the pre-clinical domain at present. There are, therefore, grounds for considering that safe, effective and reversible methods of contraception for men can be developed. PMID:24947599

  17. Male contraception

    PubMed Central

    Chao, Jing; Page, Stephanie T.; Anderson, Richard A.

    2015-01-01

    Clear evidence shows that many men and women would welcome new male methods of contraception, but none have become available. The hormonal approach is based on suppression of gonadotropins and thus of testicular function and spermatogenesis, and has been investigated for several decades. This approach can achieve sufficient suppression of spermatogenesis for effective contraception in most men, but not all; the basis for these men responding insufficiently is unclear. Alternatively, the nonhormonal approach is based on identifying specific processes in sperm development, maturation and function. A range of targets has been identified in animal models, and targeted effectively. This approach, however, remains in the pre-clinical domain at present. There are, therefore, grounds for considering that safe, effective and reversible methods of contraception for men can be developed. PMID:24947599

  18. Intrauterine Contraception.

    PubMed

    Hsia, Jennifer K; Creinin, Mitchell D

    2016-05-01

    Currently, there are only two basic types of intrauterine devices (IUDs): copper and hormonal. However, other types of IUDs are under development, some of which are in clinical trials around the world. Continued development has focused on increasing efficacy, longer duration of use, and noncontraceptive benefits. This review discusses currently available intrauterine contraceptives, such as the Cu380A IUD and levonorgestrel-releasing intrauterine systems; novel intrauterine contraceptives that are available in select parts of the world including the intrauterine ball, low-dose copper products, frameless devices, and intrauterine delivery systems impregnated with noncontraceptive medication; and novel products currently in development. PMID:26947701

  19. Emergency contraception - Potential for women's health

    PubMed Central

    Mittal, Suneeta

    2014-01-01

    Emergency contraception (EC) is a safe and effective method which is used to prevent unwanted pregnancy after unprotected sexual intercourse. Many of the unwanted pregnancies end in unsafe abortions. The search for an ideal contraceptive, which does not interfere with spontaneity or pleasure of the sexual act, yet effectively controls the fertility, is still continuing. Numerous contraceptive techniques are available, yet contraceptive coverage continues to be poor in India. Thus, even when not planning for a pregnancy, exposure to unprotected sex takes place often, necessitating the use of emergency contraception. This need may also arise due to failure of contraceptive method being used (condom rupture, diaphragm slippage, forgotten oral pills) or following sexual assault. Emergency contraception is an intervention that can prevent a large number of unwanted pregnancies resulting from failure of regular contraception or unplanned sexual activity, which in turn helps in reducing the maternal mortality and morbidity due to unsafe abortions. However, a concern has been expressed regarding repeated and indiscriminate usage of e-pill, currently the rational use of emergency contraception is being promoted as it is expected to make a significant dent in reducing the number of unwanted pregnancies and unsafe abortions. In fact, since the introduction of emergency contraception, the contribution of unsafe abortion towards maternal mortality has declined from 13 to 8 per cent. PMID:25673542

  20. Development and potential application of an oral ColoPulse infliximab tablet with colon specific release: A feasibility study.

    PubMed

    Maurer, Jacoba M; Hofman, Susan; Schellekens, Reinout C A; Tonnis, Wouter F; Dubois, Annelien O T; Woerdenbag, Herman J; Hinrichs, Wouter L J; Kosterink, Jos G W; Frijlink, Henderik W

    2016-05-30

    The monoclonal antibody infliximab is one of the cornerstones in the treatment of Crohn's disease. Local delivery of infliximab would be an alternative to overcome the inherent disadvantages of intravenous therapy. For this purpose 5mg infliximab tablets were developed. To stabilize the antibody during production and storage it was incorporated in a sugar glass containing the oligosaccharide inulin. To obtain colon-specific release a ColoPulse coating was applied. The tablets were stored for 16 months under different conditions based on ICH climatic zone I. PMID:26997425

  1. [Post-abortion contraception: effects of contraception services and reproductive intention].

    PubMed

    Borges, Ana Luiza Vilela

    2016-02-01

    Contraceptive counseling and the supply of contraceptive methods are part of post-abortion care and positively influence the subsequent use of contraceptive methods. Studies showing such evidence have been conducted predominantly in countries with no legal restrictions on abortion and with adequate care for women that terminate a pregnancy. However, little is known about contraceptive practices in contexts where abortion is illegal, as in Brazil, in which post-abortion contraceptive care is inadequate. The objective of this study was to analyze the effect of contraceptive care on male condom use and oral and injectable contraceptives in the six months post-abortion, considering reproductive intention. The results showed that contraceptive care only has a positive effect on the use of oral contraceptives in the first six months post-abortion, as long as the woman had a medical consultation in the same month in which she received information on contraception. One or the other intervention alone had no significant impact. PMID:26910252

  2. 21 CFR 520.1451 - Moxidectin tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Moxidectin tablets. 520.1451 Section 520.1451 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1451 Moxidectin tablets. (a) Specifications. Each tablet contains 30,...

  3. 21 CFR 520.1310 - Marbofloxacin tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Marbofloxacin tablets. 520.1310 Section 520.1310... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications. Each tablet contains 25, 50, 100, or 200 milligrams (mg) marbofloxacin....

  4. 21 CFR 520.1310 - Marbofloxacin tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Marbofloxacin tablets. 520.1310 Section 520.1310... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications. Each tablet contains 25, 50, 100, or 200 milligrams (mg) marbofloxacin....

  5. 21 CFR 520.1310 - Marbofloxacin tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Marbofloxacin tablets. 520.1310 Section 520.1310... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications. Each tablet contains 25, 50, 100, or 200 milligrams (mg) marbofloxacin....

  6. 21 CFR 520.1310 - Marbofloxacin tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Marbofloxacin tablets. 520.1310 Section 520.1310... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications. Each tablet contains 25, 50, 100, or 200 milligrams (mg) marbofloxacin....

  7. 21 CFR 520.1310 - Marbofloxacin tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Marbofloxacin tablets. 520.1310 Section 520.1310... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications. Each tablet contains 25, 50, 100, or 200 milligrams (mg) marbofloxacin....

  8. 21 CFR 520.370 - Cefpodoxime tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Cefpodoxime tablets. 520.370 Section 520.370 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.370 Cefpodoxime tablets. (a) Specifications. Each tablet...

  9. 21 CFR 520.804 - Enalapril tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Enalapril tablets. 520.804 Section 520.804 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.804 Enalapril tablets. (a) Specifications. Each tablet contains either...

  10. 21 CFR 520.370 - Cefpodoxime tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Cefpodoxime tablets. 520.370 Section 520.370 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.370 Cefpodoxime tablets. (a) Specifications. Each tablet...

  11. 21 CFR 520.1880 - Prednisolone tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Prednisolone tablets. 520.1880 Section 520.1880... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1880 Prednisolone tablets. (a) Specifications. Each tablet contains 5 or 20 milligrams prednisolone. (b) Sponsor. See No. 061690 in §...

  12. 21 CFR 520.1880 - Prednisolone tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Prednisolone tablets. 520.1880 Section 520.1880... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1880 Prednisolone tablets. (a) Specifications. Each tablet contains 5 or 20 milligrams prednisolone. (b) Sponsor. See No. 061690 in §...

  13. 21 CFR 520.1880 - Prednisolone tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Prednisolone tablets. 520.1880 Section 520.1880... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1880 Prednisolone tablets. (a) Specifications. Each tablet contains 5 or 20 milligrams prednisolone. (b) Sponsor. See No. 061690 in §...

  14. 21 CFR 520.1880 - Prednisolone tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Prednisolone tablets. 520.1880 Section 520.1880... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1880 Prednisolone tablets. (a) Specifications. Each tablet contains 5 or 20 milligrams prednisolone. (b) Sponsor. See No. 061690 in §...

  15. 21 CFR 520.370 - Cefpodoxime tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Cefpodoxime tablets. 520.370 Section 520.370 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.370 Cefpodoxime tablets. (a) Specifications. Each tablet...

  16. 21 CFR 520.370 - Cefpodoxime tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Cefpodoxime tablets. 520.370 Section 520.370 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.370 Cefpodoxime tablets. (a) Specifications. Each tablet...

  17. 21 CFR 520.312 - Carnidazole tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Carnidazole tablets. 520.312 Section 520.312 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.312 Carnidazole tablets. (a) Specifications. Each tablet contains 10 milligrams of carnidazole. (b) Sponsor. See 053923 in § 510.600(c)...

  18. 21 CFR 520.816 - Epsiprantel tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Epsiprantel tablets. 520.816 Section 520.816 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.816 Epsiprantel tablets. (a) Specifications. Each tablet contains either 12.5, 25, 50, or 100 milligrams of epsiprantel. (b) Sponsor. See...

  19. 21 CFR 520.812 - Enrofloxacin tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Enrofloxacin tablets. 520.812 Section 520.812 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.812 Enrofloxacin tablets. (a) Specifications. Each tablet contains either 22.7, 68.0, or 136.0 milligrams of enrofloxacin. (b) Sponsor. See...

  20. 21 CFR 520.312 - Carnidazole tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Carnidazole tablets. 520.312 Section 520.312 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.312 Carnidazole tablets. (a) Specifications. Each tablet contains 10 milligrams of carnidazole. (b) Sponsor. See 053923 in § 510.600(c)...

  1. 21 CFR 520.1616 - Orbifloxacin tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Orbifloxacin tablets. 520.1616 Section 520.1616... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1616 Orbifloxacin tablets. (a) Specifications. Each tablet contains 5.7, 22.7, or 68 milligrams (mg) orbifloxacin. (b) Sponsor. See No....

  2. 21 CFR 520.581 - Dichlorophene tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Dichlorophene tablets. 520.581 Section 520.581... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.581 Dichlorophene tablets. (a) Specifications. Each tablet contains 1 gram of dichlorophene. (b) Sponsor. See 023851 in § 510.600(c) of...

  3. 21 CFR 520.1900 - Primidone tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Primidone tablets. 520.1900 Section 520.1900 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1900 Primidone tablets. (a) Specifications. Each tablet contains 50 or 250 milligrams of primidone. (b) Sponsor. See No. 000010 in §...

  4. 21 CFR 520.812 - Enrofloxacin tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Enrofloxacin tablets. 520.812 Section 520.812 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.812 Enrofloxacin tablets. (a) Specifications. Each tablet contains either 22.7, 68.0, or 136.0 milligrams of enrofloxacin. (b) Sponsor. See...

  5. 21 CFR 520.816 - Epsiprantel tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Epsiprantel tablets. 520.816 Section 520.816 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.816 Epsiprantel tablets. (a) Specifications. Each tablet contains either 12.5, 25, 50, or 100 milligrams of epsiprantel. (b) Sponsor. See...

  6. 21 CFR 520.1870 - Praziquantel tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Praziquantel tablets. 520.1870 Section 520.1870... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1870 Praziquantel tablets. (a) Specifications. Each tablet contains: (1) 34 milligrams (mg) praziquantel. (2) 11.5 or 23 mg praziquantel....

  7. 21 CFR 520.1510 - Nitenpyram tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Nitenpyram tablets. 520.1510 Section 520.1510 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1510 Nitenpyram tablets. (a) Specifications. Each tablet contains 11.4 or 57 milligrams (mg) nitenpyram. (b) Sponsor. See No. 058198 in §...

  8. 21 CFR 520.455 - Clomipramine tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Clomipramine tablets. 520.455 Section 520.455 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.455 Clomipramine tablets. (a) Specifications. Each tablet contains 5, 20, 40, or 80 milligrams (mg) clomipramine hydrochloride. (b)...

  9. 21 CFR 520.1510 - Nitenpyram tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Nitenpyram tablets. 520.1510 Section 520.1510 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1510 Nitenpyram tablets. (a) Specifications. Each tablet contains 11.4 or 57 milligrams (mg) nitenpyram. (b) Sponsor. See No. 058198 in §...

  10. 21 CFR 520.455 - Clomipramine tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Clomipramine tablets. 520.455 Section 520.455 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.455 Clomipramine tablets. (a) Specifications. Each tablet contains 5, 20, 40, or 80 milligrams (mg) clomipramine hydrochloride. (b)...

  11. 21 CFR 520.312 - Carnidazole tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Carnidazole tablets. 520.312 Section 520.312 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.312 Carnidazole tablets. (a) Specifications. Each tablet contains 10 milligrams of carnidazole. (b) Sponsor. See 053923 in § 510.600(c)...

  12. 21 CFR 520.1870 - Praziquantel tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Praziquantel tablets. 520.1870 Section 520.1870... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1870 Praziquantel tablets. (a) Specifications. Each tablet contains: (1) 34 milligrams (mg) praziquantel. (2) 11.5 or 23 mg praziquantel....

  13. 21 CFR 520.1870 - Praziquantel tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Praziquantel tablets. 520.1870 Section 520.1870... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1870 Praziquantel tablets. (a) Specifications. Each tablet contains: (1) 34 milligrams (mg) praziquantel. (2) 11.5 or 23 mg praziquantel....

  14. 21 CFR 520.816 - Epsiprantel tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Epsiprantel tablets. 520.816 Section 520.816 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.816 Epsiprantel tablets. (a) Specifications. Each tablet contains either 12.5, 25, 50, or 100 milligrams of epsiprantel. (b) Sponsor. See...

  15. 21 CFR 520.1510 - Nitenpyram tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Nitenpyram tablets. 520.1510 Section 520.1510 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1510 Nitenpyram tablets. (a) Specifications. Each tablet contains 11.4 or 57 milligrams (mg) nitenpyram. (b) Sponsor. See No. 058198 in §...

  16. 21 CFR 520.1900 - Primidone tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Primidone tablets. 520.1900 Section 520.1900 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1900 Primidone tablets. (a) Specifications. Each tablet contains 50 or 250 milligrams of primidone. (b) Sponsor. See No. 054628 in §...

  17. 21 CFR 520.1870 - Praziquantel tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Praziquantel tablets. 520.1870 Section 520.1870... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1870 Praziquantel tablets. (a) Specifications. Each tablet contains: (1) 34 milligrams (mg) praziquantel. (2) 11.5 or 23 mg praziquantel....

  18. 21 CFR 520.1616 - Orbifloxacin tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Orbifloxacin tablets. 520.1616 Section 520.1616... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1616 Orbifloxacin tablets. (a) Specifications. Each tablet contains 5.7, 22.7, or 68 milligrams (mg) orbifloxacin. (b) Sponsor. See No....

  19. 21 CFR 520.816 - Epsiprantel tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Epsiprantel tablets. 520.816 Section 520.816 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.816 Epsiprantel tablets. (a) Specifications. Each tablet contains either 12.5, 25, 50, or 100 milligrams of epsiprantel. (b) Sponsor. See...

  20. 21 CFR 520.455 - Clomipramine tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Clomipramine tablets. 520.455 Section 520.455 Food... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.455 Clomipramine tablets. (a) Specifications. Each tablet contains 5, 20, 40, or 80 milligrams (mg) clomipramine hydrochloride. (b)...