Antiallergic effect of ZCR-2060: antihistaminic action.

PubMed

Abe, T; Omata, T; Yoshida, K; Matsumura, T; Ikeda, Y; Segawa, Y; Matsuda, K; Nagai, H

1994-09-01

The antihistaminic effect of 2-[2-[4-(diphenylmethyl)-1-piperadinyl]ethoxy] benzoic acid maleate (ZCR-2060), a newly synthesized antiallergic agent, was investigated in both in vitro and in vivo studies. ZCR-2060 clearly antagonized histamine-induced contraction of isolated guinea pig ileum and trachea. In contrast, carbachol-, BaCl2- and 5-hydroxytryptamine-induced contractions of isolated guinea pig ileum were slightly inhibited by higher concentrations of ZCR-2060. 3H-Mepyramine specific binding to membranes from guinea pig lung and brain were markedly inhibited by ZCR-2060 in a concentration-dependent fashion. In the in vitro studies, the antihistaminic effect of ZCR-2060 was greater than those of cetirizine and terfenadine, but was less than that of ketotifen. In the in vivo studies, ZCR-2060 significantly inhibited the histamine-induced cutaneous reaction in rats, when administered orally 1 hr before the histamine injection. Moreover, ZCR-2060 has a long-lasting antihistaminic effect. In the in vivo studies, the antihistaminic effect of ZCR-2060 was found to be greater than that of cetirizine and terfenadine, and it was the same as that of ketotifen. Thiopental-induced sleep and spontaneous ambulatory activity in mice, however, were unaffected by ZCR-2060 at higher doses. These results indicate that ZCR-2060 has a potent, selective and long acting histamine H1-receptor antagonistic action without causing any unwanted CNS side effect.

[Antihistaminic and antiserotonin properties of new complex tropine esters].

PubMed

Mashkovskiĭ, M D; Shvarts, G Ia

1979-01-01

The antihistaminic and antiserotonin properties of 16 new tropine esters, analogues of atropine, tropacin and tropaphen, were studied. All of them were found to lessen the spasmogenic effects of histamine and serotonin. The intensity of the antihistaminic and antiserotonin action of the drugs varied depending upon the structure of the radical at the alpha-carbon atom in the acidic part of the molecule. Both types of the activity are most marked in the desoxymethyl propyl and butyl analogues of atropine. The absence of the oxymethyl group at alpha-carbon in the series of atropine analogues is shown to facilitate the manifestation of the antihistaminic activity.

Use of Antihistamine Medications During Early Pregnancy and Isolated Major Malformations

PubMed Central

Gilboa, Suzanne M.; Strickland, Matthew J.; Olshan, Andrew F.; Werler, Martha M.; Correa, Adolfo

2013-01-01

BACKGROUND Antihistamines are commonly used during pregnancy. There is little evidence that they have teratogenic effects, but there are knowledge gaps with respect to newer products, as well as the relationship between specific antihistamines and specific birth defects. METHODS Using the National Birth Defects Prevention Study (1997-2003), the authors examined associations between maternal use of 14 antihistamines during early pregnancy and 26 isolated major birth defects. A Bayesian analysis incorporating prior knowledge about the relationships between the antihistamines, birth defects, and measured covariates was conducted. RESULTS Of the 364 associations investigated, 24 had 95% posterior intervals excluding 1.0. All 24 associations were positive; 23 associations were of weak to moderate magnitude (posterior odds ratio [OR] < 3.0) and one was strong (OR > 6.0) but very imprecise. Of the 24 associations, 20 were with non-cardiac defects. Eight associations involved the antihistamine diphenhydramine. CONCLUSIONS The results of this study generally were consistent with no association between birth defects and antihistamine use during early pregnancy. Several of the findings might warrant further investigation, although the observed elevated associations should be interpreted in the context of the number of associations investigated and the analysis of retrospective, self-reported data. PMID:19161158

First-trimester antihistamine exposure and risk of spontaneous abortion or preterm birth.

PubMed

Aldridge, Tiara D; Hartmann, Katherine E; Michels, Kara A; Velez Edwards, Digna R

2014-10-01

We tested whether antihistamine exposure during early pregnancy is associated with spontaneous abortion (SAB) or preterm birth (PTB). Women were enrolled in Right from the Start (2004-2010), a prospective pregnancy cohort. Data about first-trimester antihistamine use were obtained from screening and first-trimester interviews. Self-reported outcomes included SAB and PTB and were verified by medical records. Cox proportional hazards models were used to test for an association between antihistamine use and each outcome, both performed adjusting for confounders. Among the 2685 pregnancies analyzed, 14% (n = 377) reported use of antihistamines. Among antihistamine users, 12% (n = 44) experienced SABs, and 6% (n = 21) had PTBs. Antihistamine exposure was not associated with SAB (adjusted hazard ratio [aHR] = 0.88, 95% confidence interval [CI] 0.64, 1.21) or PTB, which was modified by maternal race (aHR = 1.03, 95%CI 0.61, 1.72 among White women and aHR = 0.43, 95%CI 0.14, 1.34 among Black women). Despite the biologic plausibility that antihistamine use may influence pregnancy outcomes, we did not detect evidence of an association with SAB or PTB. These data demonstrate the utility of large prospective cohorts for evaluating drug safety in pregnancy when concerns are raised from animal models. Copyright © 2014 John Wiley & Sons, Ltd.

Effects of two antihistamine-containing compounds upon performance at three altitudes.

DOT National Transportation Integrated Search

1968-06-01

In a study of 45 human subjects it was determined that a compound drug containing the antihistamine phenindamine did not statistically impair performance on a modified Mashburn coordinator. Another compound containing the antihistamine chlorphenirami...

Antihistamine Use in Early Pregnancy and Risk of Birth Defects

PubMed Central

Li, Qian; Mitchell, Allen A.; Werler, Martha M.; Yau, Wai-Ping; Hernández-Díaz, Sonia

2014-01-01

Background Several studies have reported an association between use of specific antihistamines in early pregnancy and certain specific birth defects. Objective To test 16 previously-hypothesized associations between specific antihistamines and specific birth defects, and identify possible new associations. Methods We used 1998-2010 data from the Slone Epidemiology Center Birth Defects Study, a multicenter case-control surveillance program of birth defects in North America. Mothers were interviewed within six months of delivery about demographic, reproductive, medical, and behavioral factors, and details on use of prescription and non-prescription medications. We compared 1st trimester exposure to specific antihistamines between 13,213 infants with specific malformations and 6,982 non-malformed controls, using conditional logistic regression to estimate odds ratios (ORs) and 95% confidence intervals (CIs), with adjustment for potential confounders, including indication for use. Results Overall, 13.7% of controls were exposed to antihistamines during the 1st trimester. The most commonly-used medications were diphenhydramine (4.2%), loratadine (3.1%), doxylamine (1.9%), and chlorpheniramine (1.7%). Where estimates were stable, none supported the previously-hypothesized associations. Among over 100 exploratory comparisons of other specific antihistamine/defect pairs, 14 had ORs ≥1.5 of which 6 had 95% CI bounds excluding 1.0 before but not after adjustment for multiple comparisons. Conclusion Our findings do not provide meaningful support for previously-posited associations between antihistamines and major congenital anomalies; at the same time, we identified associations that had not been previously suggested. We suspect that previous associations may be chance findings in the context of multiple comparisons, a situation which may also apply to our new findings. PMID:24565715

Risk of ventricular arrhythmias associated with nonsedating antihistamine drugs

PubMed Central

José de Abajo, Francisco; Rodríguez, Luis Alberto García

1999-01-01

Aims To quantify and compare the incidence of ventricular arrhythmias associated with the use of five nonsedating antihistamines: acrivastine, astemizole, cetirizine, loratadine and terfenadine. The effects of age, sex, dose, duration of treatment, and the interaction with P450 inhibitor drugs were also examined. Methods We carried out a cohort study with a nested case-control analysis using the UK-based General Practice Research Database (GPRD). The study cohort included persons aged less than 80 years old who received their first prescription for any of the five study drugs between January 1, 1992 and September 30, 1996. We estimated relative risks and 95% confidence intervals of idiopathic ventricular arrhythmias with current use of antihistamines as compared with non use. Results The study cohort included 197 425 persons who received 513 012 prescriptions. Over the study period 18 valid cases of idiopathic ventricular arrhythmias were detected. Nine occurred during the current use of any antihistamine, resulting in a crude incidence of 1.9 per 10 000 person-years (95%CI: 1.0–3.6) and a relative risk of 4.2 (95%CI: 1.5–11.8) as compared with non use. Astemizole presented the highest relative risk (RR = 19.0; 95%CI: 4.8–76.0) of all study drugs, while terfenadine (RR = 2.1; 95%CI:0.5–8.5) was in the range of other nonsedating antihistamines. Older age was associated with a greater risk of ventricular arrhythmias (RR = 7.4; 95%CI: 2.6–21.4) and seemed to increase the effect of antihistamines (RR = 6.4; 95%CI: 1.7–24.8). The proportions of high dose terfenadine and the concomitant use with P450 inhibitors among current users of terfenadine were 2.7% and 3.4%, respectively over the study period with no single case of ventricular arrhythmias occurring in the presence of these two risk factors. Conclusions The use of nonsedating antihistamines increases the risk of ventricular arrhythmias by a factor of four in the general population. Yet, the absolute

Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

PubMed

Coon, Timothy; Moree, Wilna J; Li, Binfeng; Yu, Jinghua; Zamani-Kord, Said; Malany, Siobhan; Santos, Mark A; Hernandez, Lisa M; Petroski, Robert E; Sun, Aixia; Wen, Jenny; Sullivan, Sue; Haelewyn, Jason; Hedrick, Michael; Hoare, Samuel J; Bradbury, Margaret J; Crowe, Paul D; Beaton, Graham

2009-08-01

The benzimidazole core of the selective non-brain-penetrating H(1)-antihistamine mizolastine was used to identify a series of brain-penetrating H(1)-antihistamines for the potential treatment of insomnia. Using cassette PK studies, brain-penetrating H(1)-antihistamines were identified and in vivo efficacy was demonstrated in a rat EEG/EMG model. Further optimization focused on strategies to attenuate an identified hERG liability, leading to the discovery of 4i with a promising in vitro profile.

[Efficacy of intranasal antihistamine in the treatment of allergic rhinitis: a meta-analysis].

PubMed

Feng, Shaoyan; Deng, Chuntao; Li, Lei; Liao, Wei; Fan, Yunping; Xu, Geng; Li, Huabin

2014-10-01

To systematically evaluate the efficacy of intranasal antihistamine in the treatment of allergic rhinitis. The randomized controlled trials (RCT) about intranasal antihistamines for the treatment of allergic rhinitis between January 1985 and January 2014 were searched in OVID, PubMed, EMBASE, CNKI, WanFang Data and Cochrane Library. Two reviewers independently screened the literatures, extracted the data, and evaluated the methodological quality, then meta-analysis was performed by using RevMan 5.1 software. A total of thirteen RCTs were included. The results of meta-analysis showed that the efficacy of intranasal antihistamine group was superior to the placebo group in total nasal symptom scores (TNSS), the difference was significant[WMD = -1.96, 95%CI (-2.06;-1.85), P < 0.01], and individual nasal symptom scores (blocked nose, rhinorrhea, and sneezing) [WMD = -0.18, 95%CI (-0.28;-0.08); WMD = -0.45, 95%CI (-0.52;-0.38); WMD = -0.41, 95%CI (-0.58;-0.24), all P < 0.01], with significant differences. There was no significant difference between the intranasal antihistamine group and the corticosteroid group in TNSS [WMD = -1.51, 95%CI (-3.51;0.49), P = 0.14], but the intranasal antihistamines group was superior to the corticosteroid group in individual nasal symptom scores (blocked nose, rhinorrhea, and sneezing) [WMD = -0.23, 95%CI (-0.40;-0.06); WMD = -0.35, 95%CI (-0.65;-0.05); WMD = -0.25, 95%CI (-0.42;-0.08), all P < 0.05], with significant differences. The intranasal antihistamine group was superior to the oral antihistamines group in TNSS [WMD = -0.88, 95%CI (-1.51;-0.25), P < 0.01]. Intranasal antihistamine is effective in the control of nasal symptoms in AR patients.

The Use of a Poisson Regression to Evaluate Antihistamines and Fatal Aircraft Mishaps in Instrument Meteorological Conditions.

PubMed

Gildea, Kevin M; Hileman, Christy R; Rogers, Paul; Salazar, Guillermo J; Paskoff, Lawrence N

2018-04-01

Research indicates that first-generation antihistamine usage may impair pilot performance by increasing the likelihood of vestibular illusions, spatial disorientation, and/or cognitive impairment. Second- and third-generation antihistamines generally have fewer impairing side effects and are approved for pilot use. We hypothesized that toxicological findings positive for second- and third-generation antihistamines are less likely to be associated with pilots involved in fatal mishaps than first-generation antihistamines. The evaluated population consisted of 1475 U.S. civil pilots fatally injured between September 30, 2008, and October 1, 2014. Mishap factors evaluated included year, weather conditions, airman rating, recent airman flight time, quarter of year, and time of day. Due to the low prevalence of positive antihistamine findings, a count-based model was selected, which can account for rare outcomes. The means and variances were close for both regression models supporting the assumption that the data follow a Poisson distribution; first-generation antihistamine mishap airmen (N = 582, M = 0.17, S2 = 0.17) with second- and third-generation antihistamine mishap airmen (N = 116, M = 0.20, S2 = 0.18). The data indicate fewer airmen with second- and third-generation antihistamines than first-generation antihistamines in their system are fatally injured while flying in IMC conditions. Whether the lower incidence is a factor of greater usage of first-generation antihistamines versus second- and third-generation antihistamines by the pilot population or fewer deleterious side effects with second- and third-generation antihistamines is unclear. These results engender cautious optimism, but additional research is necessary to determine why these differences exist.Gildea KM, Hileman CR, Rogers P, Salazar GJ, Paskoff LN. The use of a Poisson regression to evaluate antihistamines and fatal aircraft mishaps in instrument meteorological conditions. Aerosp Med Hum Perform

Antihistamines in drivers, aircrew and occupations of risk.

PubMed

Jáuregui, I; Ferrer, M; Montoro, J; Dávila, I; Bartra, J; del Cuvillo, A; Mullol, J; Sastre, J; Valero, A

2013-01-01

The most commonly occurring allergic diseases can involve a daytime drowsiness associated with the condition itself. The antihistamines used in their treatment can also have central effects and affect certain occupations concerned with risk, road safety and maritime and air navigation. Cognitive tests, experimental studies and epidemiological data recommend avoiding 1st generation antihistamines for people who must drive regularly and/or professions concerned with safety. Although there are no comparative studies on real driving between 1st and 2nd generation antihistamines, in this type of patients there should be a preference for prescribing those with least possible central effect, especially those which are a good substrate for transmembrane transporter pumps such as P-glycoprotein and therefore have a low capacity for crossing the hematoencephalic barrier, thus allowing a broader window for therapy. In this sense, bilastine is a good P-glycoprotein substrate and shows good tolerance at CNS level, in both psychometric trials and real driving test protocols, even at double the dose recommended in the technical file.

An overview of the novel H1-antihistamine bilastine in allergic rhinitis and urticaria.

PubMed

Jáuregui, Ignacio; García-Lirio, Eduardo; Soriano, Ana María; Gamboa, Pedro M; Antépara, Ignacio

2012-01-01

Currently available second-generation H1-antihistamines include a wide group of drugs with a better therapeutic index (or risk-benefit ratio) than the classic antihistamines, although their properties and safety profiles may differ. Bilastine is a newly registered H1-antihistamine for the oral treatment of allergic rhinitis and urticaria, with established antihistaminic and antiallergic properties. Clinical studies in allergic rhinitis and chronic urticaria show that once-daily treatment with bilastine 20 mg is effective in managing symptoms and improving patient's quality of life, with at least comparable efficacy to other nonsedative H1-antihistamines. As far as studies in healthy volunteers, clinical assays and clinical experience can establish, bilastine's safety profile is satisfactory, since it lacks anticholinergic effects, does not impair psychomotor performance or actual driving, and appears to be entirely free from cardiovascular effects.

Antihistamine Pretreatment to Reduce Incidence of Withdrawal Movement After Rocuronium Injection

PubMed Central

Lee, Ho Jun; Han, Sung Jin; Kim, Heezoo; Lee, Il Ok; Kong, Myoung Hoon; Kim, Nan Suk; Lim, Sang Ho

2009-01-01

The purpose of this study was to determine the effectiveness of antihistamine therapy for withdrawal movements caused by rocuronium injection. One hundred seventy one ASA I-II adults undergoing elective surgery were randomly assigned to one of two groups. Patients in the control group (Group C) were premedicated with 2 mL normal saline, and those in the antihistamine group (Group A) were pre-medicated with 2 mL (45.5 mg) pheniramine maleate. After the administration of thiopental sodium 5 mg/kg, rocuronium 0.6 mg/kg was injected. Withdrawal movements were assessed using a four-grade scale. The administration of antihistamine reveals lower grade of withdrawal movement after rocuronium injection. PMID:19794987

Aeroallergens, allergic rhinitis, and sedating antihistamines: risk factors for traumatic occupational injury and economic impact.

PubMed

Hanrahan, L P; Paramore, L C

2003-10-01

The U.S. workplace injury burden is significant. Our objective was to assess the particular impact of aeroallergen, allergic rhinitis, and antihistamine exposures and side effects on the risk of traumatic work-related injuries, and the associated economic impact. This is an observational case-control study with 1,223 acute traumatic injury cases that are compared to 1,202 chronic back injury controls. Structured telephone interviews were conducted in 1998 and 1999 on Workers' Compensation applicants injured in 1997. Antihistamine use and pollen levels were measured 2 weeks prior to the injury date. Sedating antihistamine exposures elevated acute injury risk (main effect OR: 2.93). A significant increase in traumatic injury risk was observed for combined sedating antihistamine and high pollen exposures among subjects with physician and self-diagnosed allergic rhinitis (OR: 2.41). Direct medical costs associated with this increased risk were estimated at $143 million in 2001. Workers with physician-diagnosed allergic rhinitis have as high a reliance on sedating antihistamines as do self-diagnosed and self-medicating nasal allergy sufferers. High pollen exposures along with sedating antihistamine use may confer significant additional injury risks among allergic rhinitis sufferers. Medical management "best practices" of diagnosed allergic rhinitis should include avoidance of sedating antihistamines to minimize acute, traumatic injury risks. Copyright 2003 Wiley-Liss, Inc.

Bilastine: a new antihistamine with an optimal benefit-to-risk ratio for safety during driving.

PubMed

Jáuregui, Ignacio; Ramaekers, Johannes G; Yanai, Kazuhiko; Farré, Magí; Redondo, Esther; Valiente, Román; Labeaga, Luis

2016-01-01

Rational selection of a second-generation H1-antihistamine requires efficacy and safety considerations, particularly regarding central nervous system (CNS) effects (cognitive and psychomotor function), potential for driving impairment, minimal sedative effects and a lack of interactions. This review evaluates the key safety features of the non-sedating antihistamine, bilastine, during driving and in preventing road traffic accidents. Among the second-generation H1-antihistamines, sedative effects which can affect cognitive and psychomotor performance, and possibly driving ability, may not be similar. Bilastine is absorbed rapidly, undergoes no hepatic metabolism or cytochrome P450 interaction (minimal drug-drug interaction potential), and is a substrate for P-glycoprotein (limiting CNS entry). Positron emission tomography showed that, compared with other second-generation H1-antihistamines, bilastine has the lowest cerebral histamine H1-receptor occupancy. Bilastine 20 mg once daily (therapeutic dose) is non-sedating, does not enhance the effects of alcohol or CNS sedatives, does not impair driving performance and has at least similar efficacy as other second-generation H1-antihistamines in the treatment of allergic rhinoconjunctivitis and urticaria. Current evidence shows that bilastine has an optimal benefit-to-risk ratio, meeting all conditions for contributing to safety in drivers who need antihistamines, and hence for being considered as an antihistamine of choice for drivers.

Anti-inflammatory and Antihistaminic Study of a Unani Eye Drop Formulation.

PubMed

Abdul, Latif; Abdul, Razique; Sukul, R R; Nazish, Siddiqui

2010-01-01

The Unani eye drop is an ophthalmic formulation prepared for its beneficial effects in the inflammatory and allergic conditions of the eyes. In the present study, the Unani eye drop formulation was prepared and investigated for its anti-inflammatory and antihistaminic activity, using in vivo and in vitro experimental models respectively. The Unani eye drop formulation exhibited significant anti-inflammatory activity in turpentine liniment-induced ocular inflammation in rabbits. The preparation also showed antihistaminic activity in isolated guinea-pig ileum. The anti-inflammatory and antihistaminic activity of eye drop may be due to presence of active ingredients in the formulation. Although there are many drugs in Unani repository which are mentioned in classical books or used in Unani clinical practice effectively in treatment of eye diseases by various Unani physicians. Inspite of the availability of vast literature, there is a dearth of commercial Unani ocular preparations. So, keeping this in mind, the eye drop formulation was prepared and its anti-inflammatory and antihistaminic activity was carried out in animal models. Thus, in view of the importance of alternative anti-inflammatory and antiallergic drugs, it becomes imperative to bring these indigenous drugs to the front foot and evaluate their activities.

Antihistamines modulate the integrin signaling pathway in h9c2 rat cardiomyocytes: Possible association with cardiotoxicity.

PubMed

Yun, J S; Kim, S Y

2015-08-01

The identification of biomarkers for toxicity prediction is crucial for drug development and safety evaluation. The selective and specific biomarkers for antihistamines-induced cardiotoxicity is not well identified yet. In order to evaluate the mechanism of the life-threatening effects caused by antihistamines, we used DNA microarrays to analyze genomic profiles in H9C2 rat cardiomyocytes that were treated with antihistamines. The gene expression profiles from drug-treated cells revealed changes in the integrin signaling pathway, suggesting that cardiac arrhythmias induced by antihistamine treatment may be mediated by changes in integrin-mediated signaling. It has been reported that integrin plays a role in QT prolongation that may induce cardiac arrhythmia. These results indicate that the integrin-mediated signaling pathway induced by antihistamines is involved in various biological mechanisms that lead to cardiac QT prolongation. Therefore, we suggest that genomic profiling of antihistamine-treated cardiomyocytes has the potential to reveal the mechanism of adverse drug reactions, and this signal pathway is applicable to prediction of in vitro cardiotoxicity induced by antihistamines as a biomarker candidate. © The Author(s) 2014.

21 CFR 341.12 - Antihistamine active ingredients.

Code of Federal Regulations, 2010 CFR

2010-04-01

... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Antihistamine active ingredients. 341.12 Section 341.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE COLD, COUGH, ALLERGY, BRONCHODILATOR, AND ANTIASTHMATIC DRUG PRODUCTS FOR OVER-THE...

Early pregnancy exposure to antihistamines and risk of congenital heart defects: results of two case-control studies.

PubMed

Smedts, Huberdina P M; de Jonge, Linda; Bandola, Sarah J G; Baardman, Marlies E; Bakker, Marian K; Stricker, Bruno H C; Steegers-Theunissen, Régine P M

2014-09-01

We aimed to study the association between use of antihistamines in early pregnancy and congenital heart defects (CHD) in the offspring. Two case-control studies. HAVEN study, Erasmus MC, University Medical Centre, Rotterdam, and Eurocat Northern Netherlands (NNL), University Medical Center Groningen, Groningen, the Netherlands. We studied 361 children with CHD and 410 controls without congenital malformations from the HAVEN study and replicated the analyses in 445 children with CHD and 530 controls from the Eurocat NNL registry. Information about antihistamine use in early pregnancy and potential confounders was obtained from questionnaires postpartum. We calculated the association between antihistamines and CHD risk by multivariable logistic regression analysis. Odds ratios (OR) with 95% confidence intervals (CI). In the HAVEN study, 25 of 771 mothers used antihistamines that were associated with an increased CHD risk (OR 3.0, 95% CI 1.2-7.3), particularly atrioventricular septal defects (AVSD) (OR 5.1, 95 % CI 1.3-20.5) and perimembranous ventricular septal defects (pVSD) (OR 5.1, 95% CI 1.8-14.4). Mothers with severe nausea who did not use antihistamines had a reduced risk (OR 0.7, 95% CI 0.5-0.98), whereas nauseous mothers using antihistamines showed an almost fivefold increased risk of pVSD (OR 4.8, 95% CI 1.1-21.8). The association between antihistamines and AVSD was confirmed in the Eurocat cohort (OR 3.5, 95% CI 1.4-8.7), but we could not replicate the association with overall CHD risk. We found a positive association between antihistamine use in early pregnancy and CHD risk, particularly AVSD, which seemed to be independent of nausea/vomiting.

High-dose anti-histamine use and risk factors in children with urticaria

PubMed Central

Uysal, Pınar; Avcil, Sibelnur; Erge, Duygu

2016-01-01

Aim The drugs of choice in the treatment of urticaria in children are H1-antihistamines. The aim of the study was to evaluate children with urticaria and define risk factors for requirement of high-dose H1-antihistamines in children with urticaria. Material and Methods The medical data of children who were diagnosed as having urticaria admitted to our outpatient clinic between January 2014 and January 2016 were searched. The medical histories, concomitant atopic diseases, parental atopy histories, medications, treatment responses, blood eosinophil and basophil counts, and serum total IgE levels were recorded. In addition, the urticaria activity score for seven days, autoimmune antibody tests, and skin prick test results were evaluated in children with chronic urticaria. Results The numbers of the children with acute and chronic urticaria were 138 and 92, respectively. The age of the children with chronic urticaria was higher than that of those with acute urticaria (p<0.0001). There was no difference between the two groups in terms of blood eosinophil and basophil counts, and serum total IgE levels (p>0.05). There was a negative correlation between blood eosinophil count and the UAS7 score in children with chronic urticaria (r=−0.276, p=0.011). Chronic urticaria and requirement of high dose H1-antihistamines were significant in children aged ≥10 years (p<0.001, p=0.015). High UAS7 score (OR: 1.09; CI 95%: [1.03–1.15]) and basopenia (OR: 6.77; CI 95%: [2.01–22.75]) were associated with the requirement of high-dose H1-AH in children with chronic urticaria. Conclusion The requirement of high-dose H1-antihistamines was higher with children’s increasing age. Disease severity and basopenia were risk factors for the requirement of high-dose H1-antihistamines. PMID:28123332

High-dose anti-histamine use and risk factors in children with urticaria.

PubMed

Uysal, Pınar; Avcil, Sibelnur; Erge, Duygu

2016-12-01

The drugs of choice in the treatment of urticaria in children are H1-antihistamines. The aim of the study was to evaluate children with urticaria and define risk factors for requirement of high-dose H1-antihistamines in children with urticaria. The medical data of children who were diagnosed as having urticaria admitted to our outpatient clinic between January 2014 and January 2016 were searched. The medical histories, concomitant atopic diseases, parental atopy histories, medications, treatment responses, blood eosinophil and basophil counts, and serum total IgE levels were recorded. In addition, the urticaria activity score for seven days, autoimmune antibody tests, and skin prick test results were evaluated in children with chronic urticaria. The numbers of the children with acute and chronic urticaria were 138 and 92, respectively. The age of the children with chronic urticaria was higher than that of those with acute urticaria (p<0.0001). There was no difference between the two groups in terms of blood eosinophil and basophil counts, and serum total IgE levels (p>0.05). There was a negative correlation between blood eosinophil count and the UAS7 score in children with chronic urticaria (r=-0.276, p=0.011). Chronic urticaria and requirement of high dose H1-antihistamines were significant in children aged ≥10 years (p<0.001, p=0.015). High UAS7 score (OR: 1.09; CI 95%: [1.03-1.15]) and basopenia (OR: 6.77; CI 95%: [2.01-22.75]) were associated with the requirement of high-dose H1-AH in children with chronic urticaria. The requirement of high-dose H1-antihistamines was higher with children's increasing age. Disease severity and basopenia were risk factors for the requirement of high-dose H1-antihistamines.

Characterization of anti-inflammatory properties and evidence for no sedation liability for the novel antihistamine SUN-1334H.

PubMed

Mandhane, Sanjay N; Shah, Jigar H; Bahekar, Prashant C; Mehetre, Sameer V; Pawar, Chandrashekhar A; Bagad, Ashish S; Chidrewar, Gajanan U; Rao, Chitturi Trinadha; Rajamannar, Thennati

2010-01-01

The anti-inflammatory potential of antihistamines has significant clinical utility. Long-term pharmacotherapy of so-called 'safe' antihistamines may be hampered by side effects in the central nervous system. In the present study, the new potential antihistamine SUN-1334H was compared with different antihistamines for anti-inflammatory effects, sedation potential and interaction with alcohol. Nasal and skin allergy were induced in guinea pig and mice by ovalbumin sensitization and challenge. Neurogenic nasal inflammation was induced by capsaicin. Sedation potential and interaction with alcohol were assessed by i.v. and intracerebroventricular pentobarbital-induced sedation and alcohol-induced ataxia models. Ovalbumin sensitization and challenge caused rhinitis pathology including inflammatory cell infiltration, IL-4, and protein leakage in the nasal lavage fluid (NLF) and presence of inflammatory cells in nasal epithelium. A 5-day treatment of antihistamines reduced these markers of inflammation. SUN-1334H, cetirizine and hydroxyzine caused comparable inhibition of NLF leukocytes, IL-4 and total protein concentrations. Fexofenadine and desloratadine showed moderate inhibition of NLF leukocytes and had no significant effect on IL-4 concentration. While fexofenadine had no effect on total protein concentration, the effect of desloratadine was comparable with the other antihistamines. In neurogenic nasal inflammation induced by capsaicin, SUN-1334H and fexofenadine caused better inhibition at lower and middle dose levels than the other antihistamines. In skin allergy models, SUN-1334H showed potent reduction of passive and active cutaneous anaphylactic reactions. In central nervous system side effects models, SUN-1334H, desloratadine and fexofenadine were devoid of any significant effects. The results are suggestive of a high anti-inflammatory to sedation index of SUN-1334H among leading antihistamines.

Prediction of the Efficacy of Antihistamines in Chronic Spontaneous Urticaria Based on Initial Suppression of the Histamine- Induced Wheal.

PubMed

Sánchez, J; Zakzuk, J; Cardona, R

2016-01-01

Antihistamines are the first line of treatment for chronic spontaneous urticaria. However, there is no effective method to predict whether an antihistamine will have a beneficial clinical effect or not. To assess whether the change in histamine-induced wheal and flare measurements 24 hours after administration of antihistamine can predict the efficacy of treatment. We performed a multicenter, triple-blind, randomized study. Patients received a daily oral dose of cetirizine, fexofenadine, bilastine, desloratadine, or ebastine over 8 weeks. After 4 weeks, a higher dose of antihistamine was administered to patients who did not experience a clinical response. A histamine skin prick test was carried out at baseline and 24 hours after the first dose of antihistamine. Disease severity (Urticaria Activity Score [UAS]), response to the histamine skin prick test, and impact on the patient's quality of life (Dermatology Life Quality Index [DLQI]) were determined every 2 weeks. The study population comprised 150 patients (30 per group) and 30 controls. Twenty-four hours after administration of antihistamine, inhibition of the histamine wheal by >75% was significantly associated with better UAS and DLQI scores. The safety and efficacy of the 5 antihistamines were similar. After updosing, rates of disease control (DLQI score <5) increased from 58.7% to 76.7%. Measurement of the histamine-induced wheal can predict which patients will have a strong clinical response to antihistamines but has limited utility for identifying nonresponders. The clinical significance of these data could be relevant in the search for new urticaria treatment regimens.

Antihistamine effect on synaptosomal uptake of serotonin, norepinephrine and dopamine

NASA Technical Reports Server (NTRS)

Brown, P. A.; Vernikos, J.

1980-01-01

A study on the effects of five H1 and H2 antihistamines on the synaptosomal uptake of serotonin (5HT), norepinephrine (NE), and dopamine (DA) is presented. Brain homogenates from female rats were incubated in Krebs-Ringer phosphate buffer solution in the presence of one of three radioactive neurotransmitters, and one of the five antihistamines. Low concentrations of pyrilamine competitively inhibited 5HT uptake, had little effect on NE uptake, and no effect on DA uptake. Promethazine, diphenhydramine, metiamide, and cimetidine had no effect on 5HT or DA uptake at the same concentration. Diphenhydramine had a small inhibitory effect on NE uptake. It is concluded that pyrilamine is a selective and potent competitive inhibitor of 5HT uptake at concentrations between .05 and .5 micromolars.

First-Generation H1 Antihistamines Found in Pilot Fatalities of Civil Aviation Accidents, 1990-2005

DTIC Science & Technology

2007-05-01

ephedrine, paroxetine, phenylpropanolamine, pseudoephedrine , quinine, and/or tetrahydrocannabinol carboxylic acid—were also present in the fatalities...antihistamine (Table II). Chlorpheniramine, ephedrine, phenylpropanolamine, and pseudoephedrine were also detected in one case and pheniramine and...detected in both cases and pseudoephedrine in 1. Blood was not available in either case. Pheniramine: This antihistamine was found in just 1 fatality

Antihistamines and other prognostic factors for adverse outcome in hyperemesis gravidarum

PubMed Central

Fejzo, Marlena S.; Magtira, Aromalyn; Schoenberg, Frederic Paik; MacGibbon, Kimber; Mullin, Patrick; Romero, Roberto; Tabsh, Khalil

2014-01-01

Objective The purpose of this study is to determine the frequency of adverse perinatal outcome in women with hyperemesis gravidarum and identify prognostic factors. Study design This is a case-control study in which outcomes of first pregnancies were compared between 254 women with hyperemesis gravidarum treated with intravenous fluids and 308 controls. Prognostic factors were identified by comparing the clinical profile of patients with hyperemesis gravidarum with a normal and an adverse pregnancy outcome. Binary responses were analyzed using either a Chi-square or Fisher exact test and continuous responses were analyzed using a t-test. Results Women with hyperemesis gravidarum have over a 4-fold increased risk of poor outcome including preterm birth and lower birth weight (p < 0.0001). Among maternal characteristics, only gestational hypertension had an influence on outcome (p < 0.0001). Treatment as an outpatient and/or by alternative medicine (acupuncture/acupressure/Bowen massage) was associated with a positive outcome (p < 0.0089). Poor outcomes were associated with early start of symptoms (p < 0.019), and treatment with methylprednisolone (p < 0.0217), promethazine (p < 0.0386), and other antihistamines [diphenhy- dramine (Benadryl), dimenhydrinate (Gravol), doxylamine (Unisom), hydroxyzine (Vistaril/Atarax), doxylamine and pyridoxine (Diclectin/Bendectin)] (p < 0.0151) independent of effectiveness. Among these medications, only the other antihistamines were prescribed independent of severity: they were effective in less than 20% of cases and were taken by almost 50% of patients with an adverse outcome. Conclusion Poor outcomes are significantly greater in women with HG and are associated with gestational hypertension, early symptoms, and antihistamine use. Given these results, there is an urgent need to address the safety and effectiveness of medications containing antihistamines in women with severe nausea of pregnancy. PMID:23751910

Comparative Effects of Antihistamines on Aircrew Performance of Simple and Complex Tasks Under Sustained Operations

DTIC Science & Technology

1991-12-01

personnel by identifying the potential symptoms and side effects of each antihistamine and a lactose intolerance reaction. These "symptoms" were then...bachelors degree. All subjects were screened for current prescription medication use, history of antihistamine use, and known lactose sensitivity. Study...assigned drug condition (Seldane, Benadryl, or lactose placebo; see Table 1). Drug group assignment was double-blind. Neither the investigators nor the

Second generation H1 - antihistamines interaction with food and alcohol-A systematic review.

PubMed

Paśko, Paweł; Rodacki, Tomasz; Domagała-Rodacka, Renata; Palimonka, Krzysztof; Marcinkowska, Monika; Owczarek, Danuta

2017-09-01

Histamine is a mediator of many physiological processes. It plays an important role in modulating allergy reactions and immune system responses. H1 receptor is a therapeutic target for drugs applied in allergic diseases such as allergic rhinoconjunctivitis, urticarial, or atopic dermatitis. H1-antihistamines display different chemical structures, pharmacokinetics and a potential for drug-drug and drug-food interactions. Drug-food interactions are known to reduce therapeutic effects of the medicine, as well as to induce a potent adverse drug reactions. Considering it all, a systematic review was conducted to investigate the importance of drug-food interaction for H1-antihistamine drugs. As non-sedating second generation H1-antihistamines remain to be drugs of choice in treating allergic conditions, the review has been focused on this particular class of medicines. The aim of this paper is to examine the evidence of food-drug and food-alcohol interactions for second generation H1-antihistamine drugs. A systematic literature queries were performed in the following databases: Medline (via PubMed), Cochrane Library, Embase and Web of Science (all from their inception date till October 2016). The queries covered nine specific names of second generation anthistamine drugs, namely bilastine, cetirizine, desloratadine, ebastine, fexofenadine, levocetirizine, loratadine, mizolastine, and rupatadine, in combinations with such terms as "food", "juice", "grapefruit", "fruits", "alcohol", "pharmacokinetics", and "meal". Additional publications were found by checking all the reference lists. Where none data on drug-food interaction could be found within the investigated databases, a specific drug prescribing information was used. 2326 publications were identified with the database queries. Articles were subjected to analysis by reviewing their title, abstract and full text; duplicated papers were removed. Having collected a complete set of data, a critical review was undertaken

[Analysis of the Cochrane Review: Antihistamines for the Common Cold. Cochrane Database Syst Rev. 2015;11:CD009345].

PubMed

Sterrantino, Carmel; Duarte, Gonçalo; Costa, João; Vaz-Carneiro, António

2016-03-01

The common cold is an acute, self-limiting inflammation of the mucosa of the upper airways, which may involve one or all the sinuses, nasopharynx, oropharynx and larynx. It is common to have at least one episode per year. Common cold symptoms, which may include sore throat, sneezing, nasal congestion, runny nose, headache, malaise and mild fever usually disappear within a few days without treatment. The causative agent of most colds is rhinovirus. Although not associated with mortality, common cold is associated with significant morbidity. There is no vaccine or cure for common cold and, therefore, their treatment is centered on relieving the symptoms. This Cochrane review aimed to synthesize the existing evidence about the clinical benefit of antihistamines, used as monotherapy, compared with placebo or no treatment in children and adult patients with common cold. A total of 18 randomized clinical trials with 4342 participants were included. Main results were: 1) Antihistamines have a small (days one and two) beneficial effect in the short term on the severity of overall symptoms in adult patients, although this effect is not present in the medium to long term; 2) antihistamines were not associated with a clinically significant beneficial effect on the individual symptoms (nasal congestion, rhinorrhea, and sneezing); 3) Antihistamines are not associated with an increased risk of adverse effects; 4) No conclusion can be made about the effectiveness of antihistamines in pediatric populations. Our interpretation of the results is that the available evidence is insufficient to support the prescription or buying OTC antihistamines to relieve the symptoms of common cold without allergic component.

Selecting optimal second-generation antihistamines for allergic rhinitis and urticaria in Asia.

PubMed

Recto, Marysia Tiongco; Gabriel, Ma Teresita; Kulthanan, Kanokvalai; Tantilipikorn, Pongsakorn; Aw, Derrick Chen-Wee; Lee, Tak Hong; Chwen, Ch'ng Chin; Mutusamy, Somasundran; Hao, Nguyen Trong; Quang, Vo Thanh; Canonica, Giorgio Walter

2017-01-01

Allergic diseases are on the rise in many parts of the world, including the Asia-Pacific (APAC) region. Second-generation antihistamines are the first-line treatment option in the management of allergic rhinitis and urticaria. International guidelines describe the management of these conditions; however, clinicians perceive the additional need to tailor treatment according to patient profiles. This study serves as a consensus of experts from several countries in APAC (Hong Kong, Malaysia, the Philippines, Singapore, Thailand, Vietnam), which aims to describe the unmet needs, practical considerations, challenges, and key decision factors when determining optimal second-generation antihistamines for patients with allergic rhinitis and/or urticaria. Specialists from allergology, dermatology, and otorhinolaryngology were surveyed on practical considerations and key decision points when treating patients with allergic rhinitis and/or urticaria. Clinicians felt the need for additional tools for diagnosis of these diseases and a single drug with all preferred features of an antihistamine. Challenges in treatment include lack of clinician and patient awareness and compliance, financial constraints, and treatment for special patient populations such as those with concomitant disease. Selection of optimal second-generation antihistamines depends on many factors, particularly drug safety and efficacy, impact on psychomotor abilities, and sedation. Country-specific considerations include drug availability and cost-effectiveness. Survey results reveal bilastine as a preferred choice due to its high efficacy and safety, suitability for special patient populations, and the lack of sedative effects. Compliance to the international guidelines is present among allergists, dermatologists and otorhinolaryngologists; however, this is lower amongst general practitioners (GPs). To increase awareness, allergy education programs targeted at GPs and patients may be beneficial. Updates to

Potential negative effects of anti-histamines on male reproductive function.

PubMed

Mondillo, Carolina; Varela, María Luisa; Abiuso, Adriana María Belén; Vázquez, Ramiro

2018-05-01

Histamine (HA) is a pleiotropic biogenic amine synthesized exclusively by histidine decarboxylase (HDC) in most mammalian tissues. The literature on the role of HA within the male gonad has expanded over the last years, attracting attention to potential unexpected side-effects of anti-histamines on testicular function. In this regard, HA receptors (HRH1, HRH2 and HRH4) have been described in Leydig cells of different species, including human. Via these receptors, HA has been reported to trigger positive or negative interactions with the LH/hCG signaling pathway depending upon its concentration, thereby contributing to the local control of testicular androgen levels. It should then be considered that anti-histamines may affect testicular homeostasis by increasing or decreasing steroid production. Additionally, HRH1 and HRH2 receptors are present in peritubular and germ cells, and HRH2 antagonists have been found to negatively affect peritubular cells and reduce sperm viability. The potential negative impact of anti-histamines on male reproduction becomes even more dramatic if we consider that HA has also been associated with human sexual behavior and penile erection. What is more, although testicular mast cells are the major source of locally produced HA, recent studies have described HDC expression in macrophages, Leydig cells and germ cells, revealing the existence of multiple sources of HA within the testis. Undoubtedly, the more we learn about the testicular histaminergic system, the more opportunities there will be for rational design of drugs aimed at treating HA-related pathologies, with minimum or nule negative impact on fertility. © 2018 Society for Reproduction and Fertility.

Bilastine: a new H1 -antihistamine with an optimal profile for updosing in urticaria.

PubMed

Church, M K; Labeaga, L

2017-09-01

This review set out to examine published papers detailing the efficacy of bilastine in skin models and urticaria to assess whether it meets the optimal profile for updosing in urticaria, that is, strong clinical efficacy and freedom from unwanted side effects, particularly sedation. Bilastine is a highly effective H 1 -antihistamine even when used at the basic dose of 20 mg daily. Its facilitated uptake after oral dosage gives it a rapid onset and long duration of action. In both wheal and flare studies and in urticaria updosing fourfold showed increased effectiveness. With respect to somnolence, bilastine is a substrate for P-glycoprotein, a membrane pump which prevents it crossing the blood-brain barrier. Consequently, bilastine is a practically 'non-sedating' H 1 -antihistamine. In conclusion, the excellent profile of bilastine in both efficacy and safety make it the ideal H 1 -antihistamine for updosing the daily dose fourfold in difficult-to-treat urticaria as recommended by the EAACI/GA 2 LEN/EDF/WAO guideline for the management of urticaria. © 2017 European Academy of Dermatology and Venereology.

Quantitative electrophysiological monitoring of anti-histamine drug effects on live cells via reusable sensor platforms.

PubMed

Pham Ba, Viet Anh; Cho, Dong-Guk; Kim, Daesan; Yoo, Haneul; Ta, Van-Thao; Hong, Seunghun

2017-08-15

We demonstrated the quantitative electrophysiological monitoring of histamine and anti-histamine drug effects on live cells via reusable sensor platforms based on carbon nanotube transistors. This method enabled us to monitor the real-time electrophysiological responses of a single HeLa cell to histamine with different concentrations. The measured electrophysiological responses were attributed to the activity of histamine type 1 receptors on a HeLa cell membrane by histamine. Furthermore, the effects of anti-histamine drugs such as cetirizine or chlorphenamine on the electrophysiological activities of HeLa cells were also evaluated quantitatively. Significantly, we utilized only a single device to monitor the responses of multiple HeLa cells to each drug, which allowed us to quantitatively analyze the antihistamine drug effects on live cells without errors from the device-to-device variation in device characteristics. Such quantitative evaluation capability of our method would promise versatile applications such as drug screening and nanoscale bio sensor researches. Copyright © 2017 Elsevier B.V. All rights reserved.

Analysis of pharmaceutical preparations containing antihistamine drugs by micellar liquid chromatography.

PubMed

Martínez-Algaba, C; Bermúdez-Saldaña, J M; Villanueva-Camañas, R M; Sagrado, S; Medina-Hernández, M J

2006-02-13

Rapid chromatographic procedures for analytical quality control of pharmaceutical preparations containing antihistamine drugs, alone or together with other kind of compounds are proposed. The method uses C18 stationary phases and micellar mobile phases of cetyltrimethylammonium bromide (CTAB) with either 1-propanol or 1-butanol as organic modifier. The proposed procedures allow the determination of the antihistamines: brompheniramine, chlorcyclizine, chlorpheniramine, diphenhydramine, doxylamine, flunarizine, hydroxyzine, promethazine, terfenadine, tripelennamine and triprolidine, in addition to caffeine, dextromethorphan, guaifenesin, paracetamol and pyridoxine in different pharmaceutical presentations (tablets, capsules, suppositories, syrups and ointments). The methods require minimum handling sample and are rapid (between 3 and 12 min at 1 mLmin(-1) flow rate) and reproducible (R.S.D. values<5%). Limits of detection are lower than 1 microgmL(-1) and the recoveries of the analytes in the pharmaceutical preparations are in the range 100+/-10%.

Selecting the optimal oral antihistamine for patients with allergic rhinitis.

PubMed

Lehman, Jeffrey M; Blaiss, Michael S

2006-01-01

Allergic rhinitis (AR) is now recognised as a global health problem that affects 10-30% of adults and up to 40% of children. Each year, millions of patients seek treatment from their healthcare provider. However, the prevalence of AR maybe significantly underestimated because of misdiagnosis, under diagnosis and failure of patients to seek medical attention. In addition to the classical symptoms such as sneezing, nasal pruritus, congestion and rhinorrhoea, it is now recognised that AR has a significant impact on quality of life (QOL). This condition can lead to sleep disturbance as a result of nasal congestion, which leads to significant impairment in daily activities such as work and school. Traditionally, AR has been subdivided into seasonal AR (SAR) or perennial AR (PAR). SAR symptoms usually appear during a specific season in which aeroallergens are present in the outdoor air such as tree and grass pollen in the spring and summer and weed pollens in the autumn (fall); and PAR symptoms are present year-round and are triggered by dust mite, animal dander, indoor molds and cockroaches. Oral histamine H(1)-receptor antagonists (H(1) antihistamines) are one of the most commonly prescribed medications for the treatment of AR. There are several oral H(1) antihistamines available and it is important to know the pharmacology, such as administration interval, onset of action, metabolism and conditions that require administration adjustments. When prescribing oral H(1) antihistamines, the healthcare provider must take into account the clinical efficacy and weigh this against the risk of adverse effects from the agent. In addition to the clinical efficacy, potential for improvement in QOL with a particular treatment should also be considered.

Cardiorespiratory assessment of decongestant-antihistamine effects of altitude, +Gz, and fatigue tolerances.

DOT National Transportation Integrated Search

1978-04-01

Decongestants and antihistamines are known to produce effects capable of adversely modifying physiological function and psychomotor task performance. Because of relevance to safe pilot performance, the effects of single doses of two decongestant-anti...

Antihistamines and driving-related behavior : a review of the evidence for impairment

DOT National Transportation Integrated Search

2004-05-01

A review of the scientific literature concerning the effects of antihistamines on driving-related skills was conducted. After reviewing all pertinent publications from 1998 and earlier, a total of 130 publications were found to meet criteria for incl...

No high level evidence to support the use of oral H1 antihistamines as monotherapy for eczema: a summary of a Cochrane systematic review

PubMed Central

2014-01-01

Background The most important symptom as well as one of the major diagnostic criteria for eczema is itch. Although oral antihistamines continue to be prescribed for people with eczema, it is unclear if they are effective and safe in relieving itch and skin lesions. We sought to evaluate the available evidence on effectiveness of oral antihistamines (H1 antagonists) as monotherapy in children and adults with eczema. Methods Searches included 10 databases and trial registers as well as conference proceedings (January 2014). Randomised controlled trials that assessed the effects of oral H1 antihistamines as monotherapy in children and adults with eczema were included. Results Our searches retrieved 757 references, but no randomised controlled trial met our inclusion criteria. Most studies allowed concomitant treatments, making the assessment of the individual effects of oral H1 antihistamines impossible. Conclusions There is currently no high-level evidence to support or refute the efficacy or safety of oral H1 antihistamines used as monotherapy for eczema. A further review of studies that assesses the effects of oral H1 antihistamines as ‘add-on’ therapy together with concomitant treatments is warranted to determine the beneficial effects of this group of medications in the treatment of eczema. PMID:24625301

Safety and efficacy of bilastine: a new H(1)-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria.

PubMed

Church, Martin K

2011-09-01

New H(1)-antihistamines should be effective in relieving the symptoms of allergic disease, should have a rapid onset and long duration of action and should neither cause sedation nor interact with cytochrome P450. A review of bilastine was undertaken to determine whether this newer H(1)-antihistamine meets these requirements. A Medline search was conducted to identify preclinical and clinical studies of bilastine. This was supplemented with additional articles or abstracts cited in reference lists and/or obtained from online sources and internal reports supplied by Faes Farma. Review of these data indicated that bilastine has high selectivity for H(1)-receptors, is rapidly and effectively absorbed, undergoes negligible metabolism and is a substrate for P-glycoprotein, which limits its passage across the blood-brain barrier. At the recommended dose of 20 mg, bilastine is non-sedative, does not enhance the effects of alcohol or CNS sedatives, does not impair actual driving tests, shows no cardiotoxicity and has a similar efficacy to other second-generation H(1)-antihistamines in the treatment of allergic rhinoconjunctivitis and urticaria. In view of its favorable pharmacological and clinical characteristics, bilastine is likely to have particular benefit in urticaria for which guidelines recommend increasing the dosage of H(1)-antihistamines up to fourfold if standard dosing is ineffective.

Bilastine: A New Nonsedating Oral H1 Antihistamine for Treatment of Allergic Rhinoconjunctivitis and Urticaria

PubMed Central

2013-01-01

Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine. In the fasting state bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice. Therefore, it is recommended that bilastine is taken at least one hour before and no sooner than two hours after a meal. Clinical studies sponsored by the manufacturer have shown that bilastine 20 mg once daily is as efficacious as other nonsedating antihistamines in allergic rhinoconjunctivitis and chronic urticaria in individuals from 12 and 18 years of age, respectively. Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms. The observations indicate that non-sedating antihistamines, as opposed to what has been thought previously, may be helpful in patients with allergic rhinitis in whom nasal obstruction is a major concern. Current international guidelines need to be revised in the light of the recent evidence. Research into aspects of pharmacokinetics and efficacy and adverse effect profiles of bilastine in children under 12 years of age is needed as are dose-response assessments and studies planned rigorously with the aim of assessing quality of life effects. PMID:23956994

Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria.

PubMed

Wolthers, Ole D

2013-01-01

Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine. In the fasting state bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice. Therefore, it is recommended that bilastine is taken at least one hour before and no sooner than two hours after a meal. Clinical studies sponsored by the manufacturer have shown that bilastine 20 mg once daily is as efficacious as other nonsedating antihistamines in allergic rhinoconjunctivitis and chronic urticaria in individuals from 12 and 18 years of age, respectively. Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms. The observations indicate that non-sedating antihistamines, as opposed to what has been thought previously, may be helpful in patients with allergic rhinitis in whom nasal obstruction is a major concern. Current international guidelines need to be revised in the light of the recent evidence. Research into aspects of pharmacokinetics and efficacy and adverse effect profiles of bilastine in children under 12 years of age is needed as are dose-response assessments and studies planned rigorously with the aim of assessing quality of life effects.

Considerations in pharmaceutical conversion: focus on antihistamines.

PubMed

Garbus, S B; Moulton, B W; Meltzer, E O; Reich, P R; Weinreb, L F; Friedman, J A; Orland, B I

1997-04-01

The practice of pharmaceutical conversion, which encompasses three types of drug interchange (generic, brand, and therapeutic substitution), is increasing in managed care settings. Pharmaceutical conversion has numerous implications for managed care organizations, their healthcare providers, and their customers. Although drug cost may be a driving consideration in pharmaceutical conversion, a number of other considerations are of equal or greater importance in the decision-making process may affect the overall cost of patient care. Among these considerations are clinical, psychosocial, and safety issues; patient adherence; patient satisfaction; and legal implications of pharmaceutical conversion. Patient-centered care must always remain central to decisions about pharmaceutical conversion. This article discusses the issues related to, and implications of, pharmaceutical conversion utilizing the antihistamines class of drugs as the case situation.

The changing face of antihistamines and cardiac adverse drug reactions: a clinical perspective.

PubMed

Shaikh, W A

2000-07-01

Recent times have witnessed a qualitative shift in the recognition and management of adverse drug effects. Many of them occur in organs that are unconnected to the primary target of pharmacological action. Out of these, cardiac side-effects have drawn particular attention because of their potential to cause death. Starting with the early observations on antibiotics such as macrolides, followed by fluoroquinolones and others, the focus has now shifted to the antihistamine class of drugs which are used extensively by patients all over the world, thanks to the ever increasing levels of environmental pollution. The occurrence of prolonged QTc interval following treatment with terfenadine leading to ventricular tachycardia of torsades de points variety with a potentially fatal outcome has forced many regulatory authorities of the world to clamp a ban the use of this drug. Alerted by these developments, studies on a new member, followed by fluoroquinolones and others, the focus has now shifted to the antihistamine class of drugs which are used extensively by patients all over the world, thanks to the ever incresing levels of envrionmental pollution. The occurrence of prolonged QTc interval following treatment with terfenadine leading to ventricular tachycardia of torsades de points variety with a potentially fatal outcome has forced many regulatory authorities of the world to clamp a ban use of this drug. Alerted by these developments, studies on a new member of non-sedating antihistamine class viz, fexofenadine, have been reviewed especially because of the structural similarity between terfenadine and fexofenadine. It is now clear that despite the closeness of its chemical structure to terfenadine fexofenadine behaves in a different manner and does not affect the electrophysiology of the heart muscle tissue, as proved by data from extensive clinical trials as well as membrane models in vitro. Interestingly, the solitary false alarm that was sounded on the drug by a

Allergic rhinitis: continuous or on demand antihistamine therapy?

PubMed

Montoro, J; Sastre, J; Jáuregui, I; Bartra, J; Dávila, I; del Cuvillo, A; Ferrer, M; Mullol, J; Valero, A

2007-01-01

Allergic rhinitis is an inflammatory disease of the nasal mucosa, caused by an IgE-mediated reaction after exposure to the allergen to which the patient is sensitized. Histamine is the most important preformed mediator released in the early stage of the allergic reaction, and also contributes to the late phase of the latter, exhibiting proinflammatory effects. Minimal persistent inflammation is a physiopathological phenomenon induced by the presence of an inflammatory cell infiltrate, together with ICAM-1 expression in the epithelial cells of the mucosa exposed to the allergen to which they are sensitized, in the absence of clinical symptoms. This molecule is considered to be an allergic inflammatory marker. The priming effect first described by Connell in 1968 consists of the reduction in the allergen concentration required to elicit a nasal hyper-response when performing a daily nasal exposure test. This implies that with natural exposure to inhaled allergens, small amounts of environmental allergen will maintain the patient symptoms, and thus of course minimal persistent inflammation. Considering the above, it is questionable whether antihistamines should be administered on a continuous basis or upon demand. The antihistamines, and fundamentally the second-generation drugs, have been shown to exert an antiinflammatory effect, and this effect is greater when the drug is administered continuously than when administered upon demand. Likewise, a reduction in treatment cost and an improvement in quality of life among patients treated on a continuous basis has been documented. However, no studies have been specifically designed to clarify the indication of treatment on a continuous basis or upon demand, as occurs in the GINA. As a result, the individualization of treatment according to the concrete characteristics of each patient seems to be the best approach, at least for the time being.

Antihistamine medication may alleviate negative effects of prenatal exposure to polycyclic aromatic hydrocarbons (PAH) on lung function in children. Birth cohort prospective study.

PubMed

Jedrychowski, Wieslaw A; Perera, Frederica P; Maugeri, Umberto; Majewska, Renata; Spengler, Jack; Mroz, Elzbieta; Flak, Elzbieta; Klimaszewska-Rembiasz, Maria; Camman, David

2015-05-01

The main purpose of the present study was to test the hypothesis that the depressed lung growth attributable to prenatal exposure to polycyclic aromatic hydrocarbons (PAH) may be modified by the intake of antihistamine medications. Individual prenatal PAH exposure was assessed by personal air monitoring in 176 children who were followed over nine years, in the course of which outdoor residential air monitoring, allergic skin tests for indoor allergens, lung function tests (FVC, FEV(1), FEV(05), and FEF(25-75)) were performed. The analysis with the General Estimated Equation (GEE) showed no association between prenatal PAH exposure and lung function in the group of children who were reported to be antihistamine users. However, in the group of antihistamine non-users all lung function tests except for FEF(25-75) were significantly and inversely associated with prenatal airborne PAH exposure. The results of the study suggest that the intake of antihistamine medications in early childhood may inhibit the negative effect of fetal PAH exposure on lung growth and provides additional indirect evidence for the hypothesis that lung alterations in young children resulting from PAH exposure may be caused by the allergic inflammation within lung. © 2014 Wiley Periodicals, Inc.

Is there a role for nonsedating antihistamines in motion sickness? Fallout from space research may soon benefit your patients

NASA Technical Reports Server (NTRS)

Kohl, R. L.

1991-01-01

The rotating chair test, a novel research technique for simulating motion sickness, is used to study the effect of nonsedating oral antihistamines in preventing or forestalling motion sickness. After receiving terfenadine, astemizole, doxepin, or placebo, four groups of male volunteers were rotated at accelerating speed, and they made head movements out of the axis of rotation until they perceived that vomiting would occur if additional head movements were made. Those pretreated with doxepin or terfenadine experienced a statistically significant prophylactic effect, as measured by increased tolerance to Coriolis stimulation. This suggests that selective peripheral H1 antihistamine action may protect against motion sickness.

The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

PubMed Central

Bosma, Reggie; Witt, Gesa; Vaas, Lea A. I.; Josimovic, Ivana; Gribbon, Philip; Vischer, Henry F.; Gul, Sheraz; Leurs, Rob

2017-01-01

The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (Kd or Ki value) or target modulation (IC50). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and modulation is lost. Drug-target residence time is a measure for the lifetime of the drug-target complex, which has recently been receiving considerable interest, as target residence time is shown to have prognostic value for the in vivo efficacy of several drugs. In this study, we have investigated the relation between the increased residence time of antihistamines at the histamine H1 receptor (H1R) and the duration of effective target-inhibition by these antagonists. Hela cells, endogenously expressing low levels of the H1R, were incubated with a series of antihistamines and dissociation was initiated by washing away the unbound antihistamines. Using a calcium-sensitive fluorescent dye and a label free, dynamic mass redistribution based assay, functional recovery of the H1R responsiveness was measured by stimulating the cells with histamine over time, and the recovery was quantified as the receptor recovery time. Using these assays, we determined that the receptor recovery time for a set of antihistamines differed more than 40-fold and was highly correlated to their H1R residence times, as determined with competitive radioligand binding experiments to the H1R in a cell homogenate. Thus, the receptor recovery time is proposed as a cell-based and physiologically relevant metric for the lead optimization of G protein-coupled receptor antagonists, like the H1R antagonists. Both, label-free or real-time, classical signaling assays allow an efficient and physiologically relevant determination of kinetic properties of drug molecules. PMID:29033838

Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity.

PubMed

Corcóstegui, Reyes; Labeaga, Luis; Innerárity, Ana; Berisa, Agustin; Orjales, Aurelio

2005-01-01

This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist. In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using H1 receptor binding studies and in vitro H1 antagonism studies conducted in guinea-pig tissues and human cell lines. Receptor selectivity was established using a receptor binding screening panel and a receptor antagonism screening conducted in guinea-pig, rat and rabbit tissues. Inhibition of inflammatory mediators was determined through the Schultz-Dale reaction in sensitised guinea-pig ileum. Bilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments conducted on guinea-pig and rat tissues. The results of these studies confirmed the lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, alpha1-adrenoceptors, beta2-adrenoceptors, and H2- and H3-receptors. The results of the in vitro Schultz-Dale reaction demonstrated that bilastine also has anti-inflammatory activity. These preclinical studies provide evidence that bilastine has H1- antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.

Enantioseparation of Six Antihistamines with Immobilized Cellulose Chiral Stationary Phase by HPLC

PubMed Central

Zhou, Jie; Luo, Pei; Chen, Shanshan; Meng, Lingchang; Sun, Chong; Du, Qiuzheng; Sun, Fang

2016-01-01

A stereoselective high performance liquid chromatography method has been developed for the chiral separation of the enantiomers of six antihistamines, doxylamine, carbinoxamine, dioxopromethazine, oxomemazine, cetirizine and hydroxyzine. The effects of mobile phase additive, column temperature and flow rate on the retention time and resolution were studied. Enantiomeric separation of cetirizine, doxylamine and hydroxyzine were achieved on cellulose tris-(3,5-dichlorophenylcarbamate) immobilized on silica gel chiral stationary phase known as Chiralpak IC (RS = 3.74, RS = 1.85 and RS = 1.74, respectively). PMID:26657408

Night-time sedating H1 -antihistamine increases daytime somnolence but not treatment efficacy in chronic spontaneous urticaria: a randomized controlled trial.

PubMed

Staevska, M; Gugutkova, M; Lazarova, C; Kralimarkova, T; Dimitrov, V; Zuberbier, T; Church, M K; Popov, T A

2014-07-01

Many physicians believe that the most effective way to treat chronic urticaria is to take a nonsedating second-generation H1 -antihistamine in the morning and a sedating first-generation H1 -antihistamine, usually hydroxyzine, at night to enhance sleep. But is this belief well founded? To test this belief by comparing the effectiveness and prevalence of unwanted sedative effects when treating patients with chronic spontaneous urticaria (CSU) with levocetirizine 15 mg daily plus hydroxyzine 50 mg at night (levocetirizine plus hydroxyzine) vs. levocetirizine 20 mg daily (levocetirizine monotherapy). In this randomized, double-blind, cross-over study, 24 patients with difficult-to-treat CSU took levocetirizine plus hydroxyzine or levocetirizine monotherapy for periods of 5 days each. At the end of each treatment period, assessments were made of quality of life (Chronic Urticaria Quality of Life Questionnaire, CU-Q2 oL), severity of urticaria symptoms (Urticaria Activity Score, UAS), sleep disturbance during the night and daytime somnolence. Both treatments significantly decreased UAS, night-time sleep disturbances and CU-Q2 oL scores (P < 0·001) without significant differences between the two. Compared with baseline, daytime somnolence was significantly reduced by levocetirizine monotherapy (P = 0·006) but not by levocetirizine plus hydroxyzine (P = 0·218). Direct comparison of the two treatment modalities in terms of daytime somnolence favoured levocetirizine monotherapy (P = 0·026). The widespread belief that sleep is aided by the addition of a sedating first-generation H1 -antihistamine, usually hydroxyzine, at night is not supported. These results are in line with the urticaria guidelines, which state that first-line treatment for urticaria should be new-generation, nonsedating H1 -antihistamines only. © 2014 The Authors. British Association of Dermatology published by John Wiley & Sons Ltd on behalf of British Association of Dermatologists.

Night-time sedating H1-antihistamine increases daytime somnolence but not treatment efficacy in chronic spontaneous urticaria: a randomized controlled trial

PubMed Central

Staevska, M; Gugutkova, M; Lazarova, C; Kralimarkova, T; Dimitrov, V; Zuberbier, T; Church, MK; Popov, TA

2014-01-01

Background Many physicians believe that the most effective way to treat chronic urticaria is to take a nonsedating second-generation H1-antihistamine in the morning and a sedating first-generation H1-antihistamine, usually hydroxyzine, at night to enhance sleep. But is this belief well founded? Objectives To test this belief by comparing the effectiveness and prevalence of unwanted sedative effects when treating patients with chronic spontaneous urticaria (CSU) with levocetirizine 15 mg daily plus hydroxyzine 50 mg at night (levocetirizine plus hydroxyzine) vs. levocetirizine 20 mg daily (levocetirizine monotherapy). Methods In this randomized, double-blind, cross-over study, 24 patients with difficult-to-treat CSU took levocetirizine plus hydroxyzine or levocetirizine monotherapy for periods of 5 days each. At the end of each treatment period, assessments were made of quality of life (Chronic Urticaria Quality of Life Questionnaire, CU-Q2oL), severity of urticaria symptoms (Urticaria Activity Score, UAS), sleep disturbance during the night and daytime somnolence. Results Both treatments significantly decreased UAS, night-time sleep disturbances and CU-Q2oL scores (P < 0·001) without significant differences between the two. Compared with baseline, daytime somnolence was significantly reduced by levocetirizine monotherapy (P = 0·006) but not by levocetirizine plus hydroxyzine (P = 0·218). Direct comparison of the two treatment modalities in terms of daytime somnolence favoured levocetirizine monotherapy (P = 0·026). Conclusions The widespread belief that sleep is aided by the addition of a sedating first-generation H1-antihistamine, usually hydroxyzine, at night is not supported. These results are in line with the urticaria guidelines, which state that first-line treatment for urticaria should be new-generation, nonsedating H1-antihistamines only. PMID:24472058

The effect on social welfare of a switch of second-generation antihistamines from prescription to over-the-counter status: a microeconomic analysis.

PubMed

Shih, Ya-Chen Tina; Prasad, Manishi; Luce, Bryan R

2002-04-01

The US Food and Drug Administration (FDA) recently held a meeting to determine whether the status of second-generation antihistamines (SGAs) should be switched from prescription (Rx) to over-the-counter (OTC) status. This article provides a conceptual microeconomic framework for addressing issues regarding the impact of such a switch on social welfare. A review of the economic literature on Rx-to-OTC switches was conducted. Relevant articles published in English between 1990 and 2001 were identified through searches of ABI Info, EconLit, PsychInfo, MEDLINE, CANCERLIT, AIDSLINE, and HealthStar, as well as a general Internet search for statements in the press or on the FDA Web site. The search terms used were Rx, prescription, OTC, over-the-counter, second-generation antihistamines, nonsedating antihistamines, first-generation antihistamines, and sedating antihistamines. Microeconomic models focusing on consumer surplus were employed to determine the potential price response and social-welfare implications of a switch of SGAs to OTC status. Unlike the agents involved in previous Rx-to-OTC switches, SGAs are still under patent protection. Economic theory suggests that a firm that is protected by a patent will price aggressively. The market for OTC SGAs is likely to be more elastic due to a lack of insurance coverage for OTC products; hence, drug manufacturers would be likely to charge a lower price if SGAs were sold OTC. However, a lower price does not necessarily guarantee an improvement in social welfare; the net impact is determined by whether the increase in consumer surplus outweighs the deadweight loss (losses of consumer and producer surplus not transferred to other parties). Additionally, the assumption of a price reduction would be called into question if there were inequalities in marginal costs between the Rx and OTC markets. In this situation, the postswitch price might increase or not be reduced significantly. It is uncertain whether granting OTC status

Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells.

PubMed

Kim, Jiwon; Song, Jin-Ho

2017-03-05

Microglial NADPH oxidase is a major source of toxic reactive oxygen species produced during chronic neuroinflammation. Voltage-gated proton channel (H V 1) functions to maintain the intense activity of NADPH oxidase, and channel inhibition alleviates the pathology of neurodegenerative diseases such as ischemic stroke and multiple sclerosis associated with oxidative neuroinflammation. Antagonists of histamine H 1 receptors have beneficial effects against microglia-mediated oxidative stress and neurotoxicity. We examined the effects of the H 1 antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells recorded using the whole-cell patch clamp technique. Diphenhydramine and chlorpheniramine reduced the proton currents with almost the same potency, yielding IC 50 values of 42 and 43μM, respectively. Histamine did not affect proton currents, excluding the involvement of histamine receptors in their action. Neither drug shifted the voltage-dependence of activation or the reversal potential of the proton currents, even though diphenhydramine slowed the activation and deactivation kinetics. The inhibitory effects of the two antihistamines on proton currents could be utilized to develop therapeutic agents for neurodegenerative diseases and other diseases associated with H V 1 proton channel abnormalities. Copyright © 2017 Elsevier B.V. All rights reserved.

Identification of a coumarin-based antihistamine-like small molecule as an anti-filoviral entry inhibitor.

PubMed

Cheng, Han; Schafer, Adam; Soloveva, Veronica; Gharaibeh, Dima; Kenny, Tara; Retterer, Cary; Zamani, Rouzbeh; Bavari, Sina; Peet, Norton P; Rong, Lijun

2017-09-01

Filoviruses, consisting of Ebola virus, Marburg virus and Cuevavirus, cause severe hemorrhagic fevers in humans with high mortality rates up to 90%. Currently, there is no approved vaccine or therapy available for the prevention and treatment of filovirus infection in humans. The recent 2013-2015 West African Ebola epidemic underscores the urgency to develop antiviral therapeutics against these infectious diseases. Our previous study showed that GPCR antagonists, particularly histamine receptor antagonists (antihistamines) inhibit Ebola and Marburg virus entry. In this study, we screened a library of 1220 small molecules with predicted antihistamine activity, identified multiple compounds with potent inhibitory activity against entry of both Ebola and Marburg viruses in human cancer cell lines, and confirmed their anti-Ebola activity in human primary cells. These small molecules target a late-stage of Ebola virus entry. Further structure-activity relationship studies around one compound (cp19) reveal the importance of the coumarin fused ring structure, especially the hydrophobic substituents at positions 3 and/or 4, for its antiviral activity, and this identified scaffold represents a favorable starting point for the rapid development of anti-filovirus therapeutic agents. Copyright © 2017 Elsevier B.V. All rights reserved.

Identification of histamine receptors and reduction of squalene levels by an antihistamine in sebocytes.

PubMed

Pelle, Edward; McCarthy, James; Seltmann, Holger; Huang, Xi; Mammone, Thomas; Zouboulis, Christos C; Maes, Daniel

2008-05-01

Overproduction of sebum, especially during adolescence, is causally related to acne and inflammation. As a way to reduce sebum and its interference with the process of follicular keratinization in the pilosebaceous unit leading to inflammatory acne lesions, antihistamines were investigated for their effect on sebocytes, the major cell of the sebaceous gland responsible for producing sebum. Reverse transcriptase-PCR analysis and immunofluorescence of an immortalized sebocyte cell line (SZ95) revealed the presence of histamine-1 receptor (H-1 receptor), and thus indicated that histamines and, conversely, antihistamines could potentially modulate sebocyte function directly. When sebocytes were incubated with an H-1 receptor antagonist, diphenhydramine (DPH), at non-cytotoxic doses, a significant decrease in squalene levels, a biomarker for sebum, was observed. As determined by high-performance liquid chromatography, untreated sebocytes contained 6.27 (+/-0.73) nmol squalene per 10(6) cells, whereas for DPH-treated cells, the levels were 2.37 (+/-0.24) and 2.03 (+/-0.97) nmol squalene per 10(6) cells at 50 and 100 microM, respectively. These data were further substantiated by the identification of histamine receptors in human sebaceous glands. In conclusion, our data show the presence of histamine receptors on sebocytes, demonstrate how an antagonist to these receptors modulated cellular function, and may indicate a new paradigm for acne therapy involving an H-1 receptor-mediated pathway.

Effects of antihistamine on up-regulation of histamine H1 receptor mRNA in the nasal mucosa of patients with pollinosis induced by controlled cedar pollen challenge in an environmental exposure unit.

PubMed

Kitamura, Yoshiaki; Nakagawa, Hideyuki; Fujii, Tatsuya; Sakoda, Takema; Enomoto, Tadao; Mizuguchi, Hiroyuki; Fukui, Hiroyuki; Takeda, Noriaki

2015-11-01

In the present study, we examined the effects of antihistamine on the up-regulation of H1R mRNA in the nasal mucosa of patients with pollinosis induced by controlled exposure to pollen using an environmental exposure unit. Out of 20 patients, we designated 14 responders, whose levels of H1R mRNA in the nasal mucosa were increased after the first pollen exposure and excluded 6 non-responders. Accordingly, the first exposure to pollen without treatment significantly induced both nasal symptoms and the up-regulation of H1R mRNA in the nasal mucosa of the responders. Subsequently, prophylactic administration of antihistamine prior to the second pollen exposure significantly inhibited both of the above effects in the responders. Moreover, the nasal expression of H1R mRNA before the second pollen exposure in the responders pretreated with antihistamine was significantly decreased, as compared with that before the first pollen exposure without treatment. These findings suggest that antihistamines suppressed histamine-induced transcriptional activation of H1R gene in the nasal mucosa, in addition to their blocking effect against histamine on H1R, resulting in a decrease of nasal symptoms. These findings further suggest that by their inverse agonistic activity, antihistamines suppress the basal transcription of nasal H1R in the absence of histamine in responders. Copyright © 2015 Japanese Pharmacological Society. Production and hosting by Elsevier B.V. All rights reserved.

Ranitidine-Associated Sleep Disturbance: Case Report and Review of H2 Antihistamine-Related Central Nervous System Adverse Effects.

PubMed

Werbel, Tyler; Cohen, Philip R

2018-04-03

Ranitidine is an H2 antihistamine used as an off-label therapy for recalcitrant verruca vulgaris. We describe a man who developed a sleep disturbance after initiating therapy with ranitidine and review similar adverse effects associated with other drugs in this class. The patient was a 40-year-old man with an eight-year history of a wart on his right plantar foot that was recalcitrant to several topical therapies. Adjunctive treatment with ranitidine 150 mg twice daily was initiated. He developed sleep disturbance with bizarre dreams and gastrointestinal symptoms. All symptoms resolved after discontinuation of the medication and recurred when he restarted the drug. PubMed was searched for the following terms: disturbance, dream, ranitidine, verruca, wart, and Zantac. The papers containing these terms and their references were reviewed. Sleep disturbance caused by ranitidine is an uncommon adverse event in patients receiving the drug. However, similar reactions have been observed with other H2 antihistamines such as cimetidine and famotidine. Clinicians should be aware that sleep disturbance secondary to ranitidine is a potential side effect of this medication.

Efficacy of amoxicillin with and without decongestant-antihistamine for otitis media with effusion in children. Results of a double-blind, randomized trial.

PubMed

Mandel, E M; Rockette, H E; Bluestone, C D; Paradise, J L; Nozza, R J

1987-02-19

In a randomized, double-blind, placebo-controlled trial involving 518 infants and children who had otitis media with effusion ("secretory" otitis media), we evaluated the efficacy of a two-week course of amoxicillin (40 mg per kilogram of body weight per day) with and without a four-week course of an oral decongestant-antihistamine combination. Among the 474 subjects who were evaluated at the four-week end point, the rate of resolution of middle-ear effusion was twice as high in those treated with amoxicillin, either with or without the decongestant-antihistamine, as in those who received placebo (P less than 0.001), but 69.8 percent of the amoxicillin-treated subjects still had effusion. Among both the amoxicillin-treated subjects and the placebo-treated subjects, resolution was more likely in those with initially unilateral effusion, in those who had had effusion for eight weeks or less, and in those without an upper respiratory tract infection at the four-week end point. Side effects were reported more often in subjects who received decongestant-antihistamine than in those who did not. Among the subjects without effusion at the four-week end point, recurrent effusion developed in approximately half those in both the amoxicillin and placebo groups during the subsequent three months. We conclude that in infants and children with otitis media with effusion, amoxicillin treatment increases to some extent the likelihood of resolution.

Photodegradation of the antihistamine cetirizine in natural waters.

PubMed

Mead, Ralph N; Barefoot, Seth; Helms, John R; Morgan, Jeremy B; Kieber, Robert J

2014-10-01

The photodegradation rate of the anti-histamine cetirizine (Zyrtec®) was investigated in various water matrices. The average observed first-order photodegradation rate coefficient (kobs ), obtained by linear regression of the logarithmic-transformed cetirizine concentrations versus irradiation time in simulated sunlight, was 0.024 h(-1) (n = 6; standard deviation ± 0.004) in deionized water corresponding to a half-life of approximately 30 h. There was no statistical difference in the kobs of cetirizine photodegradation in coastal seawater compared with deionized water or deionized water amended with dissolved chromophoric organic matter. The quantum yield of cetirizine photodegradation decreased dramatically with increasing wavelength and decreasing energy of incoming radiation, with the average value ranging from 5.28 × 10(-4) to 6.40 × 10(-3) in the ultraviolet wavelength range (280-366 nm). The activation energy of cetirizine photodegradation was 10.3 kJ mol(-1) with an observed increase in cetirizine photodegradation as temperature increased. This is a significant environmental factor influencing half-life and an important consideration, given that cetirizine has been detected in wastewater and receiving waters from different locations globally. © 2014 SETAC.

H1-antihistamines in pregnancy and lactation.

PubMed

Schatz, Michael

2002-01-01

Antihistamines may be used for the treatment of allergic rhinitis, upper respiratory infections, urticaria/angioedema, atopic dermatitis, and, rarely, as adjunctive treatment for anaphylaxis, during pregnancy. Because these illnesses may affect maternal comfort and safety as well as threaten the fetus directly (anaphylaxis) or indirectly, they often require therapy during pregnancy. Based on the information available to date, in this chapter we have attempted to provide rational guidelines for the gestational use of H1-receptor antagonists in a manner that will lead to the optimal well-being of both the mother and her infant. As more information becomes available, the recommendations herein may require modification. Although this chapter has dealt specifically with gestational management, a case can be made for considering this information when making therapeutic decisions in all women of childbearing potential. First, most pregnancies are unplanned, and the peak period of fetal vulnerability to drug-induced teratogenesis begins the day a woman's period is due. Second, during gestation, substantial alterations in a previously successful but not optimal-for-pregnancy chronic therapeutic regimen may be psychologically threatening to the patient and may lead to either uncontrolled disease or unanticipated side effects. Thus, pregnancy-appropriate regimens should ideally be discussed with all women of childbearing age as part of the informed therapeutic decision-making process.

Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine

PubMed Central

Wang, Xue Yan; Lim-Jurado, Margaret; Prepageran, Narayanan; Tantilipikorn, Pongsakorn; Wang, De Yun

2016-01-01

Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients’ quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug–drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug’s safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily). The fourfold higher than standard dose is specified as an acceptable second-line treatment option for urticaria in international guidelines. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity. Based on its pharmacokinetic properties, efficacy, and tolerability profile, bilastine will be valuable in the management of allergic rhinitis and urticaria. PMID:27110120

Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine.

PubMed

Wang, Xue Yan; Lim-Jurado, Margaret; Prepageran, Narayanan; Tantilipikorn, Pongsakorn; Wang, De Yun

2016-01-01

Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug's safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily). The fourfold higher than standard dose is specified as an acceptable second-line treatment option for urticaria in international guidelines. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity. Based on its pharmacokinetic properties, efficacy, and tolerability profile, bilastine will be valuable in the management of allergic rhinitis and urticaria.

Bitterness prediction of H1-antihistamines and prediction of masking effects of artificial sweeteners using an electronic tongue.

PubMed

Ito, Masanori; Ikehama, Kiyoharu; Yoshida, Koichi; Haraguchi, Tamami; Yoshida, Miyako; Wada, Koichi; Uchida, Takahiro

2013-01-30

The study objective was to quantitatively predict a drug's bitterness and estimate bitterness masking efficiency using an electronic tongue (e-Tongue). To verify the predicted bitterness by e-Tongue, actual bitterness scores were determined by human sensory testing. In the first study, bitterness intensities of eight H(1)-antihistamines were assessed by comparing the Euclidean distances between the drug and water. The distances seemed not to represent the drug's bitterness, but to be greatly affected by acidic taste. Two sensors were ultimately selected as best suited to bitterness evaluation, and the data obtained from the two sensors depicted the actual taste map of the eight drugs. A bitterness prediction model was established with actual bitterness scores from human sensory testing. Concerning basic bitter substances, such as H(1)-antihistamines, the predictability of bitterness intensity using e-Tongue was considered to be sufficiently promising. In another study, the bitterness masking efficiency when adding an artificial sweetener was estimated using e-Tongue. Epinastine hydrochloride aqueous solutions containing different levels of acesulfame potassium and aspartame were well discriminated by e-Tongue. The bitterness masking efficiency of epinastine hydrochloride with acesulfame potassium was successfully predicted using e-Tongue by several prediction models employed in the study. Copyright © 2012 Elsevier B.V. All rights reserved.

Transitioning the second-generation antihistamines to over-the-counter status: a cost-effectiveness analysis.

PubMed

Sullivan, Patrick W; Follin, Sheryl L; Nichol, Michael B

2003-12-01

A U.S. Food and Drug Administration advisory committee deemed the second-generation antihistamines (SGA) safe for over-the-counter use against the preliminary opposition of the manufacturers. As a result, loratadine is now available over-the-counter. First-generation antihistamines (FGA) are associated with an increased risk of unintentional injuries, fatalities, and reduced productivity. Access to SGA over-the-counter could result in decreased use of FGA, thereby reducing deleterious outcomes. The societal impact of transitioning this class of medications from prescription to over-the-counter status has important policy implications. To examine the cost-effectiveness of transitioning SGA to over-the-counter status from a societal perspective. A simulation model of the decision to transition SGA to over-the-counter status was compared with retaining prescription-only status for a hypothetical cohort of individuals with allergic rhinitis in the United States. Estimates of costs and effectiveness were obtained from the medical literature and national surveys. Sensitivity analysis was performed using a second-order Monte Carlo simulation. Discounted, quality-adjusted life-years saved as a result of amelioration of allergic rhinitis symptoms and avoidance of motor vehicle, occupational, public and home injuries and fatalities; discounted direct and indirect costs. Availability of SGA over-the-counter was associated with annual savings of 4 billion dollars (2.4-5.3 billion dollars) or 100 dollars (64-137 dollars) per allergic rhinitis sufferer and 135,061 time-discounted quality-adjusted life years (84,913-191,802). The sensitivity analysis provides evidence in support of these results. Making SGA available over-the-counter is both cost-saving and more effective for society, largely as a result of reduced adverse outcomes associated with FGA-induced sedation. Further study is needed to determine the differential impact on specific vulnerable populations.

Lack of efficacy of a decongestant-antihistamine combination for otitis media with effusion ("secretory" otitis media) in children. Results of a double-blind, randomized trial.

PubMed

Cantekin, E I; Mandel, E M; Bluestone, C D; Rockette, H E; Paradise, J L; Stool, S E; Fria, T J; Rogers, K D

1983-02-10

In a double-blind, randomized trial of 553 infants and children who had otitis media with effusion ("secretory" otitis media), we compared the efficacy of a four-week course of an oral decongestant-antihistamine combination (pseudoephedrine hydrochloride, 4 mg per kilogram of body weight per day, and chlorpheniramine maleate, 0.35 mg per kilogram per day) with that of placebo. Among patients with initially unilateral disease, resolution of middle-ear effusion occurred at four weeks in 38 per cent of those treated with placebo and 34 per cent of those treated with drug (P = 0.74). Among patients with initially bilateral disease the corresponding proportions were 19 and 21 per cent, respectively (P = 0.67). Side effects were reported more often among drug-treated than placebo-treated patients. Decongestant-antihistamine combinations do not appear to be indicated for the treatment of otitis media with effusion in infants and children.

FT-IR and FT-Raman spectra, molecular structure and first-order molecular hyperpolarizabilities of a potential antihistaminic drug, cyproheptadine HCl

NASA Astrophysics Data System (ADS)

Sagdinc, Seda G.; Erdas, Dilek; Gunduz, Ilknur; Sahinturk, Ayse Erbay

2015-01-01

Cyproheptadine hydrochloride (CYP HCl) {4-(5H-dibenzo[a,d]-cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride} is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local-anesthetic properties. The geometry optimization, Mulliken atomic charges and wavenumber and intensity of the vibrational bands of all of the possible modes of CYP HCl have been calculated using ab initio Hartree-Fock (HF) and density functional theory (DFT) employing the B3LYP functional with the 6-311G(d,p) basis set. We have compared the calculated IR and Raman wavenumbers with experimental data. Quantum-chemical calculations of the geometrical structure, energies, and molecular electrostatic potential and NBO analysis of CYP HCl have been performed using the B3LYP/6-311G(d,p) method. The electric dipole moment (μ), static polarizability (α) and the first hyperpolarizability (β) values of the title compound have been computed using HF and DFT methods. The study reveals that the antihistaminic pharmacological property of CYP HCl has a large β value and, hence, may in general have potential applications in the development of non-linear optical materials. The experimental and calculated results for CYP HCl have also been compared with those for mianserin HCl.

Can Twitter Be a Source of Information on Allergy? Correlation of Pollen Counts with Tweets Reporting Symptoms of Allergic Rhinoconjunctivitis and Names of Antihistamine Drugs.

PubMed

Gesualdo, Francesco; Stilo, Giovanni; D'Ambrosio, Angelo; Carloni, Emanuela; Pandolfi, Elisabetta; Velardi, Paola; Fiocchi, Alessandro; Tozzi, Alberto E

2015-01-01

Pollen forecasts are in use everywhere to inform therapeutic decisions for patients with allergic rhinoconjunctivitis (ARC). We exploited data derived from Twitter in order to identify tweets reporting a combination of symptoms consistent with a case definition of ARC and those reporting the name of an antihistamine drug. In order to increase the sensitivity of the system, we applied an algorithm aimed at automatically identifying jargon expressions related to medical terms. We compared weekly Twitter trends with National Allergy Bureau weekly pollen counts derived from US stations, and found a high correlation of the sum of the total pollen counts from each stations with tweets reporting ARC symptoms (Pearson's correlation coefficient: 0.95) and with tweets reporting antihistamine drug names (Pearson's correlation coefficient: 0.93). Longitude and latitude of the pollen stations affected the strength of the correlation. Twitter and other social networks may play a role in allergic disease surveillance and in signaling drug consumptions trends.

Global scanning of antihistamines in the environment: Analysis of occurrence and hazards in aquatic systems.

PubMed

Kristofco, Lauren A; Brooks, Bryan W

2017-08-15

Concentration of the global population is increasingly occurring in megacities and other developing regions, where access to medicines is increasing more rapidly than waste management systems are implemented. Because freshwater and coastal systems are influenced by wastewater effluent discharges of differential quality, exposures in aquatic systems must be considered. Here, we performed a global scanning assessment of antihistamines (AHs), a common class of medicines, in surface waters and effluents. Antihistamines were identified, literature occurrence and ecotoxicology data on AHs collated, therapeutic hazard values (THVs) calculated, and environmental exposure distributions (EEDs) of AHs compared to ecotoxicity thresholds and drug specific THVs to estimate hazards in surface waters and effluents. Literature searches of 62 different AHs in environmental matrices identified 111 unique occurrence publications of 24 specific AHs, largely from Asia-Pacific, Europe, and North America. However, the majority of surface water (63%) and effluent (85%) observations were from Europe and North America, which highlights relatively limited information from many regions, including developing countries and rapidly urbanizing areas in Africa, Latin America and Asia. Less than 10% of all observations were for estuarine or marine systems, though the majority of human populations reside close to coastal habitats. EED 5 th and 95 th centiles for all AHs were 2 and 212ng/L in surface water, 5 and 1308ng/L in effluent and 6 and 4287ng/L in influent, respectively. Unfortunately, global hazards and risks of AHs to non-target species remain poorly understood. However, loratadine observations in surface waters exceeded a THV without an uncertainty factor 40% of the time, indicating future research is needed to understand aquatic toxicology, hazards and risks associated with this AH. This unique global scanning study further illustrates the utility of global assessments of pharmaceuticals

Ultraviolet A photosensitivity profile of dexchlorpheniramine maleate and promethazine-based creams: Anti-inflammatory, antihistaminic, and skin barrier protection properties.

PubMed

Facchini, Gustavo; Eberlin, Samara; Clerici, Stefano Piatto; Alves Pinheiro, Ana Lucia Tabarini; Costa, Adilson

2017-12-01

Unwanted side effects such as dryness, hypersensitivity, and cutaneous photosensitivity are challenge for adherence and therapeutical success for patients using treatments for inflammatory and allergic skin response. In this study, we compared the effects of two dermatological formulations, which are used in inflammatory and/or allergic skin conditions: dexchlorpheniramine maleate (DCP; 10 mg/g) and promethazine (PTZ; 20 mg/g). We evaluated both formulations for phototoxicity potential, skin irritation, anti-inflammatory and antihistaminic abilities, and skin barrier repair in vitro and ex vivo using the standard OECD test guideline n° 432, the ECVAM protocol n° 78, and cultured skin explants from a healthy patient. Ultraviolet A was chosen as exogenous agent to induce allergic and inflammatory response. Both PTZ and DCP promoted increases in interleukin-1 (IL-1) synthesis in response to ultraviolet A (UVA) radiation compared to control. However, the increase observed with PTZ was significantly greater than the DCP, indicating that the latter has a lower irritant potential. DCP also demonstrated a protective effect on UVA-induced leukotriene B4 and nuclear factor kappa B (NF-κB) synthesis. Conversely, PTZ demonstrates more robust UVA antihistaminic activity. Likewise, PTZ promoted a significantly greater increase in the production of involucrin and keratin 14, both associated with protective skin barrier property. In conclusion, these data suggest possible diverging UVA response mechanisms of DCP and PTZ, which gives greater insight into the contrasting photosensitizing potential between DCP and PTZ observed in the patients. © 2017 Wiley Periodicals, Inc.

New model for prediction binary mixture of antihistamine decongestant using artificial neural networks and least squares support vector machine by spectrophotometry method

NASA Astrophysics Data System (ADS)

Mofavvaz, Shirin; Sohrabi, Mahmoud Reza; Nezamzadeh-Ejhieh, Alireza

2017-07-01

In the present study, artificial neural networks (ANNs) and least squares support vector machines (LS-SVM) as intelligent methods based on absorption spectra in the range of 230-300 nm have been used for determination of antihistamine decongestant contents. In the first step, one type of network (feed-forward back-propagation) from the artificial neural network with two different training algorithms, Levenberg-Marquardt (LM) and gradient descent with momentum and adaptive learning rate back-propagation (GDX) algorithm, were employed and their performance was evaluated. The performance of the LM algorithm was better than the GDX algorithm. In the second one, the radial basis network was utilized and results compared with the previous network. In the last one, the other intelligent method named least squares support vector machine was proposed to construct the antihistamine decongestant prediction model and the results were compared with two of the aforementioned networks. The values of the statistical parameters mean square error (MSE), Regression coefficient (R2), correlation coefficient (r) and also mean recovery (%), relative standard deviation (RSD) used for selecting the best model between these methods. Moreover, the proposed methods were compared to the high- performance liquid chromatography (HPLC) as a reference method. One way analysis of variance (ANOVA) test at the 95% confidence level applied to the comparison results of suggested and reference methods that there were no significant differences between them.

The antihistamine olopatadine regulates T cell activation in palladium allergy.

PubMed

Iguchi, Naohiko; Takeda, Yuri; Sato, Naoki; Ukichi, Kenichirou; Katakura, Akira; Ueda, Kyosuke; Narushima, Takayuki; Higuchi, Shigehito; Ogasawara, Kouetsu

2016-06-01

Because of its corrosion resistance palladium (Pd) has been widely used in many consumer products ranging from fashion accessories to dental materials. Recently, however, an increase in Pd allergy cases has been reported. Metal allergy is categorized as a Type IV allergy, which is characterized as a delayed-type hypersensitivity reaction in which T cells are known to play an important role; however, the precise mechanism of their action remains unclear. Here we defined the relationship between histamine and the Pd allergic reaction specifically with respect to T cell responses. To verify the effects of histamine on T cells, we examined whether there is a change in IFN-γ production following stimulation of histamine or the antihistamine, olopatadine hydrochloride (OLP), in vitro. In addition, we assessed whether OLP administration affected the degree of footpad swelling or IFN-γ production during the Pd allergy response in mice. We found that histamine stimulation increased IFN-γ production in T cells, specifically enhancing IFN-γ production in CD8(+) T cells compared with CD4(+) T cells. Interestingly, OLP suppressed the production of IFN-γ in CD8(+) T cells, and this compound inhibited footpad swelling and IFN-γ production in mice with Pd allergy. These results suggest that histamine promotes the Type IV allergic reaction and thus, the histamine 1 receptor (H1R) might be useful therapeutic target for treatment of metal allergy. Copyright © 2016 Elsevier B.V. All rights reserved.

Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract of Zanthoxylum alatum seeds on isolated tissue preparations: An ex vivo study.

PubMed

Saikia, Beenita; Barua, Chandana Choudhury; Haloi, Prakash; Patowary, Pompy

2017-01-01

The aim of this study was to evaluate anticholinergic, antihistaminic, and antiserotonergic activity of the n-hexane extract of the seeds of Zanthoxylum alatum (ZAHE) on isolated ileum of rat and guinea pig and fundus of rat. ZAHE was prepared using soxhlet extraction and cumulative concentration response curves were constructed using various doses on the tissues for acetylcholine (ACh), 5-hydroxytryptamine (5-HT), and histamine with or without n-hexane extract. Atropine, ketanserin, and pheniramine maleate were used as antagonists for ACh, serotonin, and histamine, respectively. ZAHE-induced concentration-dependent inhibition of isolated ileum and fundus in rat and ileum of guinea pig. The half maximal effective concentration (EC 50 ) of ACh in the presence of atropine (10 -6 M; P < 0.05) and ZAHE (1000 μg/ml; P < 0.01) was significantly higher than EC 50 of ACh alone. The EC 50 of 5-HT in the presence of ketanserin (10 -5 M; P < 0.01) and ZAHE (1000 μg/ml; P < 0.05) was higher than EC 50 of 5-HT alone. Similarly, the EC 50 of histamine in the presence of pheniramine maleate (10 -6 M; P < 0.01) and ZAHE (300 μg/ml; P < 0.01 and 1000 μg/ml; P < 0.05) was also significantly higher than EC 50 of histamine alone. From the study, it was observed that ZAHE shows significant anticholinergic, antiserotonergic, and antihistaminic activity. The study provides sufficient evidence that the seeds can be used in gastric disorders, cough, chest infection, etc., as per folklore claims.

Toxic effects of the antihistamine cetirizine in mussel Mytilus galloprovincialis.

PubMed

Teixeira, Miguel; Almeida, Ângela; Calisto, Vânia; Esteves, Valdemar I; Schneider, Rudolf J; Wrona, Frederick J; Soares, Amadeu M V M; Figueira, Etelvina; Freitas, Rosa

2017-05-01

Recent studies have become increasingly focused on the assessment of pharmaceuticals occurrence in aquatic ecosystems, however the potential toxicity to non-target organisms is still largely unknown. The antihistamine cetirizine is a commonly used pharmaceutical, already detected in surface waters of marine aquatic systems worldwide. In the present study Mytilus galloprovincialis mussels were exposed to a range of cetirizine concentrations (0.3, 3.0, 6.0 and 12.0 μg/L), resembling moderate to highly contaminated areas, over 28 days. The responses of different biochemical markers were evaluated in mussels whole soft tissue, and included energy-related parameters (glycogen content, GLY; protein content, PROT; electron transport system activity, ETS), and oxidative stress markers (superoxide dismutase activity, SOD; catalase activity, CAT; glutathione S-transferases activity, GSTs; lipid peroxidation levels, LPO; reduced (GSH) and oxidized (GSSG) glutathione content). The results obtained demonstrated that with the increase of exposure concentrations mussels tended to increase their energy reserves and maintain their metabolic potential, which was significantly higher only at the highest concentration. Our findings clearly revealed that cetirizine inhibited the activity of GSTs and although induced the activity of antioxidant enzymes (SOD and CAT) mussels were not able to prevent cellular damages observed through the increase of LPO associated to the increase of exposure concentrations. Thus, this study confirmed that cetirizine induces toxic effects in Mytilus galloprovincialis, which, considering their trophic relevance, wide use as bioindicator and wide spatial distribution of this species, can result in ecological and economic negative impacts at a large scale. Copyright © 2017 Elsevier Ltd. All rights reserved.

Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract of Zanthoxylum alatum seeds on isolated tissue preparations: An ex vivo study

PubMed Central

Saikia, Beenita; Barua, Chandana Choudhury; Haloi, Prakash; Patowary, Pompy

2017-01-01

Objectives: The aim of this study was to evaluate anticholinergic, antihistaminic, and antiserotonergic activity of the n-hexane extract of the seeds of Zanthoxylum alatum (ZAHE) on isolated ileum of rat and guinea pig and fundus of rat. Materials and Methods: ZAHE was prepared using soxhlet extraction and cumulative concentration response curves were constructed using various doses on the tissues for acetylcholine (ACh), 5-hydroxytryptamine (5-HT), and histamine with or without n-hexane extract. Atropine, ketanserin, and pheniramine maleate were used as antagonists for ACh, serotonin, and histamine, respectively. Results: ZAHE-induced concentration-dependent inhibition of isolated ileum and fundus in rat and ileum of guinea pig. The half maximal effective concentration (EC50) of ACh in the presence of atropine (10−6 M; P < 0.05) and ZAHE (1000 μg/ml; P < 0.01) was significantly higher than EC50of ACh alone. The EC50of 5-HT in the presence of ketanserin (10−5 M; P < 0.01) and ZAHE (1000 μg/ml; P < 0.05) was higher than EC50of 5-HT alone. Similarly, the EC50of histamine in the presence of pheniramine maleate (10−6 M; P < 0.01) and ZAHE (300 μg/ml; P < 0.01 and 1000 μg/ml; P < 0.05) was also significantly higher than EC50of histamine alone. Conclusion: From the study, it was observed that ZAHE shows significant anticholinergic, antiserotonergic, and antihistaminic activity. The study provides sufficient evidence that the seeds can be used in gastric disorders, cough, chest infection, etc., as per folklore claims. PMID:28458421

Seasonal changes in antibiotics, antidepressants/psychiatric drugs, antihistamines and lipid regulators in a wastewater treatment plant.

PubMed

Golovko, Oksana; Kumar, Vimal; Fedorova, Ganna; Randak, Tomas; Grabic, Roman

2014-09-01

Seasonal changes in the concentration of 21 pharmaceuticals in a wastewater treatment plant (WWTP) in České Budějovice were investigated over 12months. The target compounds were 10 antibiotics, 4 antidepressants, 3 psychiatric drugs, 2 antihistamines and 2 lipid regulators. 272 Wastewater samples (136 influents and 136 effluents) were collected from March 2011 to February 2012 and analyzed using two-dimensional liquid chromatography coupled with tandem mass spectrometry. All studied pharmaceuticals were frequently detected in both the influent and the effluent wastewater samples, except for meclozine, which was only found in the influent. The mean concentration of pharmaceuticals varied from 0.006μgL(-1) to 1.48μgL(-1) in the influent and from 0.003μgL(-1) to 0.93μgL(-1) in the effluent. The concentration of most pharmaceuticals was higher during winter. Copyright © 2014 Elsevier Ltd. All rights reserved.

The role and choice criteria of antihistamines in allergy management - expert opinion.

PubMed

Kuna, Piotr; Jurkiewicz, Dariusz; Czarnecka-Operacz, Magdalena M; Pawliczak, Rafał; Woroń, Jarosław; Moniuszko, Marcin; Emeryk, Andrzej

2016-12-01

Allergic diseases are the most common chronic conditions lasting throughout the patient's life. They not only cause significant deterioration in the quality of life of patients but also lead to significant absenteeism and reduced productivity, resulting in very high costs for society. Effective and safe treatment of allergic diseases is therefore one of the main challenges for public health and should be carried out by all the specialists in family medicine, internists and paediatricians in collaboration with allergists, otorhinolaryngologists and dermatologists. Antihistamines are most commonly used in the treatment of allergies. Several dozen drugs are available on the pharmaceutical market, and their generic forms are advertised widely as very effective drugs for the treatment of allergic diseases. What is the truth? What are the data from clinical trials and observational studies? Are all drugs equally effective and safe for the patient? According to a panel of experts representing various fields of medicine, inappropriate treatment of allergies can be very risky for patients, and seemingly equally acting medications may differ greatly. Therefore, a panel of experts gathered the latest data from the entire scientific literature and analysed the latest standards and recommendations prepared by scientific societies. This paper provides a summary of these studies and highlights the importance for the patient of the proper choice of drug to treat his allergies.

Cost-Effectiveness of Second-Generation Antihistamines and Montelukast in Relieving Allergic Rhinitis Nasal Symptoms

PubMed Central

Goodman, Michael J.; Jhaveri, Mehul; Saverno, Kim; Meyer, Kellie; Nightengale, Brian

2008-01-01

Objective Allergic rhinitis imposes a significant health and economic burden both on individuals and the healthcare system. Second-generation prescription antihistamines, levocetirizine, fexofenadine, and desloratadine, and the leukotriene receptor antagonist, montelukast, differ in their ability to relieve common rhinitis symptoms. The purpose of this study was to compare the cost-effectiveness of prescription agents based on their effectiveness in relieving nasal symptoms. Methods Effectiveness was measured as the composite of nasal symptoms, including congestion, rhinorrhea, and sneezing, from clinical studies that compared each of the 4 comparators to placebo. Direct costs included prescription therapy and rhinitis-related physician office visits. Physician office visit costs were collected from an analysis of the PharMetrics insurance claims database. Sensitivity analyses were conducted using a Monte Carlo simulation to assess the robustness of the average and incremental cost-effectiveness ratios. Results The cost per clinically significant improvement of nasal symptoms for levocetirizine was less than for the other model comparator agents. The incremental cost-effectiveness ratio for levocetirizine dominated montelukast and desloratadine and was lower than either branded or generic fexofenadine. Conclusion Levocetirizine is a cost-effective therapy for the relief of nasal symptoms of allergic rhinitis. PMID:25126257

Evidence for the hERG Liability of Antihistamines, Antipsychotics, and Anti-Infective Agents: A Systematic Literature Review From the ARITMO Project.

PubMed

Hazell, Lorna; Raschi, Emanuel; De Ponti, Fabrizio; Thomas, Simon H L; Salvo, Francesco; Ahlberg Helgee, Ernst; Boyer, Scott; Sturkenboom, Miriam; Shakir, Saad

2017-05-01

A systematic review was performed to categorize the hERG (human ether-a-go-go-related gene) liability of antihistamines, antipsychotics, and anti-infectives and to compare it with current clinical risk of torsade de pointes (TdP). Eligible studies were hERG assays reporting half-minimal inhibitory concentrations (IC50). A "hERG safety margin" was calculated from the IC50 divided by the peak human plasma concentration (free C max ). A margin below 30 defined hERG liability. Each drug was assigned an "uncertainty score" based on volume, consistency, precision, and internal and external validity of evidence. The hERG liability was compared to existing knowledge on TdP risk (www.credibledrugs.org). Of 1828 studies, 82 were eligible, allowing calculation of safety margins for 61 drugs. Thirty-one drugs (51%) had evidence of hERG liability including 6 with no previous mention of TdP risk (eg, desloratadine, lopinavir). Conversely, 16 drugs (26%) had no evidence of hERG liability including 6 with known, or at least conditional or possible, TdP risk (eg, chlorpromazine, sulpiride). The main sources of uncertainty were the validity of the experimental conditions used (antihistamines and antipsychotics) and nonuse of reference compounds (anti-infectives). In summary, hERG liability was categorized for 3 widely used drug classes, incorporating a qualitative assessment of the strength of available evidence. Some concordance with TdP risk was observed, although several drugs had hERG liability without evidence of clinical risk and vice versa. This may be due to gaps in clinical evidence, limitations of hERG/C max data, or other patient/drug-specific factors that contribute to real-life TdP risk. © 2016, The American College of Clinical Pharmacology.

Misuse and dependence on non-prescription codeine analgesics or sedative H1 antihistamines by adults: a cross-sectional investigation in France.

PubMed

Roussin, Anne; Bouyssi, Annabelle; Pouché, Lucie; Pourcel, Laure; Lapeyre-Mestre, Maryse

2013-01-01

Given the growing worldwide market of non-prescription drugs, monitoring their misuse in the context of self-medication represents a particular challenge in Public Health. The aim of this study was to investigate the prevalence of misuse, abuse, and dependence on non-prescription psychoactive drugs. During one month, in randomly solicited community pharmacies, an anonymous questionnaire was offered to adults requesting paracetamol (control group), codeine combined with paracetamol in analgesics, or sedative H1 antihistamines. Responses about misuse (drug use not in agreement with the Patient Information Leaflet) abuse (excessive drug use having detrimental consequences), and dependence (established according to questions adapted from the Diagnostic and Statistical Manual of Mental Disorders, 4th Edition criteria) on psychoactive drugs were compared to those of the paracetamol control group. 295 patients (mean age 48.5 years, 68.5% of women) having used one of the studied drugs during the previous month were included. Misuse and dependence to codeine analgesics concerned 6.8% and 17.8% of the patients exposed to these drugs, respectively, (n = 118), which was significantly higher than for paracetamol. 19.5% had used codeine analgesics daily for more than six months. Headache was the most frequent reason for persistent daily use. A high prevalence of persistent daily users of sedative H1 antihistamines was also observed. Whereas these drugs are recommended only for short treatment courses of occasional insomnia, 72.2% of the participants having taken doxylamine (n = 36) were daily users, predominantly for more than six months. Results on misuse and dependence on non-prescription codeine analgesics suggest that chronic pain, in particular chronic cephalalgia, requires better medical care. In addition, as for hypnotics on prescription, persistent use of doxylamine for self-medication is not justified until an acceptable benefit-risk ratio for chronic sleep

Utility of NBD-Cl for the spectrophotometric determination of some skeletal muscle relaxant and antihistaminic drugs

NASA Astrophysics Data System (ADS)

Saleh, Hanaa M.; EL-Henawee, Magda M.; Ragab, Gamal H.; El-Hay, Soad S. Abd

2007-08-01

A simple, accurate, precise and sensitive colorimetric method for the determination of some skeletal muscle relaxant drugs, namely orphenadrine citrate ( I), baclofen ( II), antihistaminic drugs as acrivastine ( III) and fexofenadine hydrochloride ( IV) is described. This method is based on the formation of charge transfer complex with 4-chloro-7-nitro-2,1,3-benzoxadiazole (NBD-Cl) in non-aqueous medium. The orange color products were measured at 472, 465, 475 and 469 nm for drugs I, II, III and IV, respectively. The optimization of various experimental conditions was described. Beer's Law was obeyed in the range (2.5-17.5), (5-70), (2.5-25) and (10-50) μg/ml for drugs I, II, III and IV, respectively. The molar absorptivity ( ɛ), sandell sensitivity, detection (LOD) and quantitation limits (LOQ) are calculated. The procedure was favorably applied for determination of certain pharmaceutical dosage forms containing the studied drugs. The obtained results were compared with the official and reported methods. There were no significant differences between proposed, reported and the official methods.

The relationship between birch pollen, air pollution and weather types and their effect on antihistamine purchase in two Swedish cities.

PubMed

Grundström, Maria; Dahl, Åslög; Ou, Tinghai; Chen, Deliang; Pleijel, Håkan

2017-01-01

Exposure to elevated air pollution levels can aggravate pollen allergy symptoms. The aim of this study was to investigate the relationships between airborne birch ( Betula ) pollen, urban air pollutants NO 2 , O 3 and PM 10 and their effects on antihistamine demand in Gothenburg and Malmö, Sweden, 2006-2012. Further, the influence of large-scale weather pattern on pollen-/pollution-related risk, using Lamb weather types (LWTs), was analysed. Daily LWTs were obtained by comparing the atmospheric pressure over a 16-point grid system over southern Sweden (scale ~3000 km). They include two non-directional types, cyclonic (C) and anticyclonic (A) and eight directional types depending on the wind direction (N, NE, E…). Birch pollen levels were exceptionally high under LWTs E and SE in both cities. Furthermore, LWTs with dry and moderately calm meteorological character (A, NE, E, SE) were associated with strongly elevated air pollution (NO 2 and PM 10 ) in Gothenburg. For most weather situations in both cities, simultaneously high birch pollen together with high air pollution had larger over-the-counter (OTC) sales of antihistamines than situations with high birch pollen alone. LWTs NE, E, SE and S had the highest OTC sales in both cities. In Gothenburg, the city with a higher load of both birch pollen and air pollution, the higher OTC sales were especially obvious and indicate an increased effect on allergic symptoms from air pollution. Furthermore, Gothenburg LWTs A, NE, E and SE were associated with high pollen and air pollution levels and thus classified as high-risk weather types. In Malmö, corresponding high-risk LWTs were NE, E, SE and S. Furthermore, occurrence of high pollen and air pollutants as well as OTC sales correlated strongly with vapour pressure deficit and temperature in Gothenburg (much less so in Malmö). This provides evidence that the combination of meteorological properties associated with LWTs can explain high levels of birch pollen and air

The role and choice criteria of antihistamines in allergy management – expert opinion

PubMed Central

Jurkiewicz, Dariusz; Czarnecka-Operacz, Magdalena M.; Pawliczak, Rafał; Woroń, Jarosław; Moniuszko, Marcin; Emeryk, Andrzej

2016-01-01

Allergic diseases are the most common chronic conditions lasting throughout the patient’s life. They not only cause significant deterioration in the quality of life of patients but also lead to significant absenteeism and reduced productivity, resulting in very high costs for society. Effective and safe treatment of allergic diseases is therefore one of the main challenges for public health and should be carried out by all the specialists in family medicine, internists and paediatricians in collaboration with allergists, otorhinolaryngologists and dermatologists. Antihistamines are most commonly used in the treatment of allergies. Several dozen drugs are available on the pharmaceutical market, and their generic forms are advertised widely as very effective drugs for the treatment of allergic diseases. What is the truth? What are the data from clinical trials and observational studies? Are all drugs equally effective and safe for the patient? According to a panel of experts representing various fields of medicine, inappropriate treatment of allergies can be very risky for patients, and seemingly equally acting medications may differ greatly. Therefore, a panel of experts gathered the latest data from the entire scientific literature and analysed the latest standards and recommendations prepared by scientific societies. This paper provides a summary of these studies and highlights the importance for the patient of the proper choice of drug to treat his allergies. PMID:28035215

Quantitation of antihistamines in pharmaceutical preparations by liquid chromatography with a micellar mobile phase of sodium dodecyl sulfate and pentanol.

PubMed

Gil-Agustí, M; Monferrer-Pons, L; Esteve-Romero, J; García-Alvarez-Coque, M C

2001-01-01

A reversed-phase liquid chromatographic procedure with a micellar mobile phase of sodium dodecyl sulfate (SDS), containing a small amount of pentanol, was developed for the control of 7 antihistamines of diverse action in pharmaceutical preparations (tablets, capsules, powders, solutions, and syrups): azatadine, carbinoxamine, cyclizine, cyproheptadine, diphenhydramine, doxylamine, and tripelennamine. The retention times of the drugs were <9 min with a mobile phase of 0.15M SDS-6% (v/v) pentanol. The recoveries with respect to the declared compositions were in the range of 93-110%, and the intra- and interday repeatabilities and interday reproducibility were <1.2%. The results were similar to those obtained with a conventional 60 + 40 (v/v) methanol-water mixture, with the advantage of reduced toxicity, flammability, environmental impact, and cost of the micellar-pentanol solutions. The lower risk of evaporation of the organic solvent dissolved in the micellar solutions also increased the stability of the mobile phase.

Interactions of bilastine, a new oral H₁ antihistamine, with human transporter systems.

PubMed

Lucero, Maria Luisa; Gonzalo, Ana; Ganza, Alvaro; Leal, Nerea; Soengas, Itziar; Ioja, Eniko; Gedey, Szilvia; Jahic, Mirza; Bednarczyk, Dallas

2012-06-01

Membrane transporters play a significant role in facilitating transmembrane drug movement. For new pharmacological agents, it is important to evaluate potential interactions (e.g., substrate specificity and/or inhibition) with human transporters that may affect their pharmacokinetics, efficacy, or toxicity. Bilastine is a new nonsedating H₁ antihistamine indicated for the treatment of allergic rhinoconjunctivitis and urticaria. The in vitro inhibitory effects of bilastine were assessed on 12 human transporters: four efflux [multidrug resistance protein 1 (MDR1) or P-glycoprotein, breast cancer resistance protein (BCRP), multidrug resistance associated protein 2 (MRP2), and bile salt export pump) and eight uptake transporters (sodium taurocholate cotransporting polypeptide, organic cation transporter (OCT)1, organic anion transporter (OAT)1, OAT3, OCT2, OATP2B1, OATP1B1, and OATP1B3). Only mild inhibition was found for MDR1-, OCT1-, and OATP2B1-mediated transport of probe substrates at the highest bilastine concentration assayed (300 μM; half-maximal inhibitory concentration: ≥300 μM). Bilastine transport by MDR1, BCRP, OAT1, OAT3, and OCT2 was also investigated in vitro. Only MDR1 active transport of bilastine was relevant, whereas it did not appear to be a substrate of OCT2, OAT1, or OAT3, nor was it transported substantially by BCRP. Drug-drug interactions resulting from bilastine inhibition of drug transporters that would be generally regarded as clinically relevant are unlikely. Additionally, bilastine did not appear to be a substrate of human BCRP, OAT1, OAT3, or OCT2 and thus is not a potential victim of inhibitors of these transporters. On the other hand, based on in vitro evaluation, clinically relevant interactions with MDR1 inhibitors are anticipated.

Simultaneous detection and quantification of select nitromusks, antimicrobial agent, and antihistamine in fish of grocery stores by gas chromatography-mass spectrometry.

PubMed

Foltz, James; Abdul Mottaleb, M; Meziani, Mohammed J; Rafiq Islam, M

2014-07-01

Continually detected biologically persistent nitromusks; galaxolide (HHCB), tonalide (AHTN) and musk ketone (MK), antimicrobial triclosan (TCS), and antihistamine diphenhydramine (DPH) were examined for the first time in edible fillets originating from eight fish species grown in salt- and fresh-water. The sampled fish collected from local grocery stores were homogenized, extracted, pre-concentrated and analyzed by gas chromatography-mass spectrometry (GC-MS) using selected ion monitoring (SIM). The presence of the target compounds in fish extracts was confirmed based on similar mass spectral features and retention behavior with standards. Internal standard based calibration plots were used for quantification. The HHCB, AHTN, TCS and DPH were consistently observed with concentration of 0.163-0.892, 0.068-0.904, 0.189-1.182, and 0.942-7.472 ng g(-1), respectively. These values are at least 1-3 orders of magnitude lower than those obtained in environmental fish specimens. The MK was not detected in any fish. Copyright © 2013 Elsevier Ltd. All rights reserved.

Seasonal patterns of oral antihistamine and intranasal corticosteroid purchases from Australian community pharmacies: a retrospective observational study.

PubMed

Carney, A Simon; Price, David B; Smith, Pete K; Harvey, Richard; Kritikos, Vicky; Bosnic-Anticevich, Sinthia Z; Christian, Louise; Skinner, Derek A; Carter, Victoria; Durieux, Alice Ms

2017-01-01

To explore patterns in the purchase of prescription and over-the-counter (OTC) oral antihistamines (OAHs) and intranasal corticosteroids (INCSs) by patients, from pharmacies in different geographical regions of Australia. Retrospective observational study using a database containing anonymous pharmacy transaction data from 20.0% of the pharmacies in Australia that link doctor prescriptions and OTC information. Pharmacy purchases of at least one prescription or OTC rhinitis treatment during 2013 and 2014 were assessed. In total, 4,247,193 prescription and OTC rhinitis treatments were purchased from 909 pharmacies over 12 months. Of treatments purchased, 75.9% were OAHs and 16.6% were INCSs. OTC purchases of both treatments exceeded purchases through prescription. OTC OAHs purchasing patterns were seasonal and almost identical in the Australian Capital Territory, Victoria, Western Australia, South Australia, and New South Wales, and similar seasonal patterns for OTC INCSs were noted in most regions except for South Australia and Tasmania. Prescription purchasing patterns of both OAHs and INCSs remained unchanged throughout the year in most regions. This large-scale retrospective observational study identified seasonal purchasing patterns of OTC and prescription OAHs and INCSs in a real-world setting. It highlighted that seasonality only affects OTC purchasing patterns of OAHs and INCSs across Australia and that practitioner prescribing remains unchanged, suggesting that it is only for persistent disease.

Seasonal patterns of oral antihistamine and intranasal corticosteroid purchases from Australian community pharmacies: a retrospective observational study

PubMed Central

Carney, A Simon; Price, David B; Smith, Pete K; Harvey, Richard; Kritikos, Vicky; Bosnic-Anticevich, Sinthia Z; Christian, Louise; Skinner, Derek A; Carter, Victoria; Durieux, Alice MS

2017-01-01

Purpose To explore patterns in the purchase of prescription and over-the-counter (OTC) oral antihistamines (OAHs) and intranasal corticosteroids (INCSs) by patients, from pharmacies in different geographical regions of Australia. Patients and methods Retrospective observational study using a database containing anonymous pharmacy transaction data from 20.0% of the pharmacies in Australia that link doctor prescriptions and OTC information. Pharmacy purchases of at least one prescription or OTC rhinitis treatment during 2013 and 2014 were assessed. Results In total, 4,247,193 prescription and OTC rhinitis treatments were purchased from 909 pharmacies over 12 months. Of treatments purchased, 75.9% were OAHs and 16.6% were INCSs. OTC purchases of both treatments exceeded purchases through prescription. OTC OAHs purchasing patterns were seasonal and almost identical in the Australian Capital Territory, Victoria, Western Australia, South Australia, and New South Wales, and similar seasonal patterns for OTC INCSs were noted in most regions except for South Australia and Tasmania. Prescription purchasing patterns of both OAHs and INCSs remained unchanged throughout the year in most regions. Conclusion This large-scale retrospective observational study identified seasonal purchasing patterns of OTC and prescription OAHs and INCSs in a real-world setting. It highlighted that seasonality only affects OTC purchasing patterns of OAHs and INCSs across Australia and that practitioner prescribing remains unchanged, suggesting that it is only for persistent disease. PMID:28919832

Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects.

PubMed

Togawa, Michinori; Yamaya, Hidetoshi; Rodríguez, Mónica; Nagashima, Hirotaka

2016-12-01

Bilastine is a novel second-generation antihistamine for the symptomatic treatment of allergic rhinitis and urticaria. The objective of this study was to evaluate the pharmacokinetics, pharmacodynamics, and tolerability of bilastine following single and multiple oral doses in healthy Japanese subjects. The pharmacokinetic and pharmacodynamic profiles were compared with those reported in Caucasian subjects. In a single-blind, randomized, placebo-controlled, parallel-group, single- and multiple-ascending dose study, bilastine tablets were administered at single doses of 10, 20, and 50 mg (Part I), and once daily for 14 days at 20 and 50 mg (Part II). After single oral doses, maximum plasma concentrations (C max ) were reached at 1.0-1.5 h postdose. Plasma exposure [C max and area under the plasma concentration-time curve (AUC)] increased dose-proportionally at single doses of 10-50 mg. In repeated-dose administration, no remarkable differences were observed between Day 1 and Day 14 for C max or AUC. For inhibitory effects on wheal and flare response, bilastine 20 and 50 mg showed significant inhibition from 1.5 h after administration as compared with placebo, and the significant effect persisted for 24 h after administration. The rates of adverse events (AEs) were comparable between bilastine and placebo in both Part I and Part II. In addition, no dose- or administration period-dependent tendency of increase in rate of AEs or worsening of severity was observed. Bilastine exhibits similar single- and multiple-dose pharmacokinetic and pharmacodynamic characteristics in healthy Japanese subjects compared with those observed in Caucasian subjects in previous studies.

Reasons for prescribing second generation antihistamines to treat allergic rhinitis in real-life conditions and patient response

PubMed Central

2014-01-01

Background Second generation H1 antihistamines (H1A) are currently recommended as first choice medications for allergic rhinitis and rhinoconjunctivitis. However, little is known about what influences the choice of prescription of one second generation (H1A) as opposed to another in real-life conditions. Objective The aim of the study was to identify the main criteria determining the choice of a second generation H1A by allergy specialists in mainland France. Methods Consecutive patients suffering from allergic rhinitis or rhinoconjunctivitis were included and followed prospectively for 30 days from the prescription of a second generation H1A in monotherapy. Patients were asked to fill in auto-questionnaires at baseline, daily during the first 10 days of the new treatment, and at the end of follow-up. Data on efficacy, tolerance, safety, rate and type of response to treatment, as well as patient satisfaction were recorded and analyzed. Results 1,080 patients were included between March 2011 and October 2012, mostly suffering from moderate to severe rhinitis (82.0%). The most frequently cited reason for choosing a specific H1A was the expected efficacy (85.3%). The mean time to nasal and ocular recovery was 6 days and 78.2% of patients responded to treatment within this interval. The presence of conjunctivitis was significantly associated with a more rapid response. At the end of follow-up, the satisfaction rate was higher for patients who were switched from a previous treatment (87.5%), compared to those receiving their first treatment (78.8%). Conclusion and clinical relevance The main reason for choosing a specific second generation H1A was its expected efficacy. Concomitant conjunctivitis is associated with a more rapid response to treatment. Symptom recovery necessitates a mean of 6 days. PMID:24944561

Lack of interaction between a new antihistamine, mizolastine, and lorazepam on psychomotor performance and memory in healthy volunteers.

PubMed

Patat, A; Perault, M C; Vandel, B; Ulliac, N; Zieleniuk, I; Rosenzweig, P

1995-01-01

1. The possible interaction between a new H1 antihistamine, mizolastine, and lorazepam was assessed in a randomised, double-blind, cross-over, placebo-controlled study involving 16 healthy young male volunteers who received mizolastine 10 mg or placebo once daily for 8 days with a 1 week wash-out interval. The interaction of mizolastine, at steady-state, with a single oral dose of lorazepam or placebo was assessed on days 6 or 8 of each treatment period. 2. Psychomotor performance and cognitive function were evaluated using objective tests (critical flicker fusion threshold, choice reaction time, tapping, arithmetic calculation, body sway) and self-ratings (visual analogue scale, ARCI) before and at 2, 4, 6 and 8 h after dosing. Short-term memory (Sternberg memory scanning immediate free recall of a word list) and long-term memory (delayed free recall and recognition of words and pictures) were assessed before and at 3 h after dosing. Pharmacodynamic interactions were evaluated by repeated measures ANOVA in a 2 x 2 factorial interaction model. 3. Mizolastine, 10 mg once daily, at steady-state, was devoid of sedation and detrimental effect on skilled performance and memory. 4. In contrast, a single 2 mg dose of lorazepam produced marked impairment of psychomotor performance, cognitive functions (significant reduction in flicker fusion threshold, tapping and arithmetic calculation and increase in reaction times and body sway) and subjective sedation from 2 to 8 h after dosing. In addition, lorazepam induced an anterograde amnesia, characterised by a decrease in delayed free recall and recognition, and a deficit in short term memory.(ABSTRACT TRUNCATED AT 250 WORDS)

Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients.

PubMed

Demonte, A; Guanti, M B; Liberati, S; Biffi, A; Fernando, F; Fainello, M; Pepe, P

2018-02-01

Bilastine is a highly selective, non-sedating antihistamine, indicated for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. Available data suggest that bilastine interferes neither with driving ability nor with flying-related performance. However, no data are available on the effect of bilastine on the driving ability in extreme conditions. Here we analyzed the effect of 7 days treatment with 20 mg bilastine in patients with allergic rhinitis and/or chronic urticaria, on psychophysical performance assessed by the Formula One (F1) high-speed simulator-driving test. This study is a phase IV, interventional, prospective, mono-centric, single arm, open-label trial. Eighteen outpatients affected by allergic rhinitis and/or chronic urticaria, able to perform a preliminary driving test on F1 simulator were considered (V-1). First, the patients had a screening visit to assess their eligibility (V0). Visit 1 (V1), at the end of placebo before bilastine treatment and Visit 2 (V2), at the end of bilastine treatment. The primary variable parameter was the ability to maintain the vehicle in a central position at different speeds (50, 150, and 250 km/h). Bilastine had a good safety profile and was well tolerated in terms of adverse events, laboratory parameters and vital signs. Bilastine did not have any negative effect on the ability to maintain the requested path, a constant speed as well as on attention and reactivity levels, even in extreme driving conditions. This study is the first done in patients with allergic rhinitis and/or chronic urticaria using a F1-high speed simulator-driving test evaluating subjects' performance under bilastine treatment.

Mast cell stabilization, lipoxygenase inhibition, hyaluronidase inhibition, antihistaminic and antispasmodic activities of Aller-7, a novel botanical formulation for allergic rhinitis.

PubMed

Amit, A; Saxena, V S; Pratibha, N; D'Souza, P; Bagchi, M; Bagchi, D; Stohs, S J

2003-01-01

Allergic rhinitis, also known as hay fever, rose fever or summer catarrh, is a major challenge to health professionals. A large number of the world's population, including approximately 40 million Americans, suffers from allergic rhinitis. A novel, botanical formulation (Aller-7) has been developed for the treatment of allergic rhinitis using a combination of extracts from seven medicinal plants, including Phyllanthus emblica, Terminalia chebula, T. bellerica, Albizia lebbeck, Piper nigrum, Zingiber officinale and P. longum, which have a proven history of efficacy and health benefits. The clinical manifestations of allergy are due to a number of mediators that are released from mast cells. The effect of Aller-7 on rat mesenteric mast cell degranulation was studied by incubating different concentrations of Aller-7 and challenging them with a degranulating agent, compound 48/80. The inhibitory activity of Aller-7 was determined against lipoxygenase and hyaluronidase, the key enzymes involved in the initiation and maintenance of inflammatory responses. Furthermore, most of these manifestations are due to histamine, which causes vasodilatation, increasing capillary permeability and leading to bronchoconstriction. Hence, the antihistaminic activity of Aller-7 was determined is isolated guinea pig ileum substrate using cetirizine as a positive control. The antispasmodic effect of Aller-7 on contractions of guinea pig tracheal chain was determined using papaverine and cetirizine as controls. Aller-7 exhibited potent activity in all these in vitro models tested, thus demonstrating the novel anti-allergic potential of Aller-7.

Thin layer chromatography-densitometric determination of some non-sedating antihistamines in combination with pseudoephedrine or acetaminophen in synthetic mixtures and in pharmaceutical formulations.

PubMed

El-Kommos, Michael E; El-Gizawy, Samia M; Atia, Noha N; Hosny, Noha M

2014-03-01

The combination of certain non-sedating antihistamines (NSA) such as fexofenadine (FXD), ketotifen (KET) and loratadine (LOR) with pseudoephedrine (PSE) or acetaminophen (ACE) is widely used in the treatment of allergic rhinitis, conjunctivitis and chronic urticaria. A rapid, simple, selective and precise densitometric method was developed and validated for simultaneous estimation of six synthetic binary mixtures and their pharmaceutical dosage forms. The method employed thin layer chromatography aluminum plates precoated with silica gel G 60 F254 as the stationary phase. The mobile phases chosen for development gave compact bands for the mixtures FXD-PSE (I), KET-PSE (II), LOR-PSE (III), FXD-ACE (IV), KET-ACE (V) and LOR-ACE (VI) [Retardation factor (Rf ) values were (0.20, 0.32), (0.69, 0.34), (0.79, 0.13), (0.36, 0.70), (0.51, 0.30) and (0.76, 0.26), respectively]. Spectrodensitometric scanning integration was performed at 217, 218, 218, 233, 272 and 251 nm for the mixtures I-VI, respectively. The linear regression data for the calibration plots showed an excellent linear relationship. The method was validated for precision, accuracy, robustness and recovery. Limits of detection and quantitation were calculated. Statistical analysis proved that the method is reproducible and selective for the simultaneous estimation of these binary mixtures. Copyright © 2013 John Wiley & Sons, Ltd.

Validated spectroscopic methods for determination of anti-histaminic drug azelastine in pure form: Analytical application for quality control of its pharmaceutical preparations.

PubMed

El-Masry, Amal A; Hammouda, Mohammed E A; El-Wasseef, Dalia R; El-Ashry, Saadia M

2018-02-15

Two simple, sensitive, rapid, validated and cost effective spectroscopic methods were established for quantification of antihistaminic drug azelastine (AZL) in bulk powder as well as in pharmaceutical dosage forms. In the first method (A) the absorbance difference between acidic and basic solutions was measured at 228nm, whereas in the second investigated method (B) the binary complex formed between AZL and Eosin Y in acetate buffer solution (pH3) was measured at 550nm. Different criteria that have critical influence on the intensity of absorption were deeply studied and optimized so as to achieve the highest absorption. The proposed methods obeyed Beer ' s low in the concentration range of (2.0-20.0μg·mL -1 ) and (0.5-15.0μg·mL -1 ) with % recovery±S.D. of (99.84±0.87), (100.02±0.78) for methods (A) and (B), respectively. Furthermore, the proposed methods were easily applied for quality control of pharmaceutical preparations without any conflict with its co-formulated additives, and the analytical results were compatible with those obtained by the comparison one with no significant difference as insured by student's t-test and the variance ratio F-test. Validation of the proposed methods was performed according the ICH guidelines in terms of linearity, limit of quantification, limit of detection, accuracy, precision and specificity, where the analytical results were persuasive. Copyright © 2017 Elsevier B.V. All rights reserved.

Cost-benefit analysis of first-generation antihistamines in the treatment of allergic rhinitis.

PubMed

Sullivan, Patrick W; Follin, Sheryl L; Nichol, Michael B

2004-01-01

The majority of individuals with allergic rhinitis in the US take first-generation antihistamines (FGAs). Although FGAs have been proven effective in alleviating allergic rhinitis symptoms, they have been associated with an increased risk of motor vehicle, aviation and occupational injuries and deaths, reduced productivity and impaired learning. The objective of this analysis was to quantify the total costs and benefits of FGA use in the US from the societal perspective. We used a decision-analytic model to quantify the annual societal costs and benefits of treatment with FGAs compared with the hypothetical alternative of no treatment for the population of individuals with allergic rhinitis and taking FGAs in the US in 2001. The benefit associated with FGA use was estimated using the willingness-to-pay framework and projected to the US population using published estimates of the prevalence of allergic rhinitis. The costs of FGA-associated sedation included lost productivity and the direct and indirect cost of unintentional injuries (including motor vehicle, occupational, public and home injuries and fatalities). The incidence of injuries and fatalities associated with FGA use was estimated using the risk of injury attributable to the sedentary effects of FGAs in the allergic rhinitis population. To evaluate uncertainty in the model assumptions, a probabilistic sensitivity analysis was conducted using Bayesian second-order Monte Carlo simulation. Costs and benefits are expressed in 2001 US dollars, using a 3% discount rate. Based on current utilisation, the total societal benefit (95% credible interval) associated with the use of FGAs for the treatment of allergic rhinitis was US 7.7 billion dollars (US 1.3 billion dollars to US 21 billion dollars). The societal cost of purchasing FGAs was only US 697 million dollars. However, the societal cost of FGA-associated sedation was US 11.3 billion dollars (US 2.4 billion dollars to US 50.8 billion dollars). The annual

Pyrilamine-induced prolonged QT interval in adolescent with drug overdose.

PubMed

Paudel, Govinda; Syed, Muhammad; Kalantre, Sarika; Sharma, Jayendra

2011-10-01

The widespread availability of antihistamines in many over-the-counter preparations can lead to significant hazard to the public because of their possible link to potential ventricular arrhythmias secondary to prolongation of QT interval. The effect can be further compounded by the use of other commonly used medications such as macrolides, antifungal agents, antipsychotics, and other antihistamine-containing preparations. The effect of antihistamines on QT interval is not a class effect but is unique to certain medications. Pyrilamine, a first-generation antihistaminic agent, is considered safe as there are no reports regarding its cardiac toxicity available in literature. We report a case of an adolescent with prolonged QT interval after an overdose of pyrilamine.

Over-the-counter medicines

MedlinePlus

... throat lozenges can be soothing. Be careful in young children because of the choking risk. ALLERGIES Antihistamine pills and liquids work well for treating allergy symptoms . Antihistamines that may ...

Chronic Spontaneous Urticaria: Pathogenesis and Treatment Considerations.

PubMed

Kaplan, Allen P

2017-11-01

The treatment of chronic spontaneous urticaria begins with antihistamines; however, the dose required typically exceeds that recommended for allergic rhinitis. Second-generation, relatively non-sedating H₁-receptor blockers are typically employed up to 4 times a day. First-generation antihistamines, such as hydroxyzine or diphenhydramine (Atarax or Benadryl), were employed similarly in the past. Should high-dose antihistamines fail to control symptoms (at least 50%), omalizumab at 300 mg/month is the next step. This is effective in 70% of antihistamine-refractory patients. H₂-receptor blockers and leukotriene antagonists are no longer recommended; they add little and the literature does not support significant efficacy. For those patients who are unresponsive to both antihistamines and omalizumab, cyclosporine is recommended next. This is similarly effective in 65%-70% of patients; however, care is needed regarding possible side-effects on blood pressure and renal function. Corticosteroids should not be employed chronically due to cumulative toxicity that is dose and time dependent. Brief courses of steroid e.g., 3-10 days can be employed for severe exacerbations, but should be an infrequent occurrence. Finally, other agents, such as dapsone or sulfasalazine, can be tried for those patients unresponsive to antihistamines, omalizumab, and cyclosporine. Copyright © 2017 The Korean Academy of Asthma, Allergy and Clinical Immunology · The Korean Academy of Pediatric Allergy and Respiratory Disease.

Controlled-release formulation of antihistamine based on cetirizine zinc-layered hydroxide nanocomposites and its effect on histamine release from basophilic leukemia (RBL-2H3) cells

PubMed Central

Hasan, Samer; Ali, Hussein Al; Al-Qubaisi, Mothanna; Hussein, Mohd Zobir; Ismail, Maznah; Zainal, Zulkarnain; Hakim, Muhammad Nazrul

2012-01-01

A controlled-release formulation of an antihistamine, cetirizine, was synthesized using zinc-layered hydroxide as the host and cetirizine as the guest. The resulting well-ordered nanolayered structure, a cetirizine nanocomposite “CETN,” had a basal spacing of 33.9 Å, averaged from six harmonics observed from X-ray diffraction. The guest, cetirizine, was arranged in a horizontal bilayer between the zinc-layered hydroxide (ZLH) inorganic interlayers. Fourier transform infrared spectroscopy studies indicated that the intercalation takes place without major change in the structure of the guest and that the thermal stability of the guest in the nanocomposites is markedly enhanced. The loading of the guest in the nanocomposites was estimated to be about 49.4% (w/w). The release study showed that about 96% of the guest could be released in 80 hours by phosphate buffer solution at pH 7.4 compared with about 97% in 73 hours at pH 4.8. It was found that release was governed by pseudo-second order kinetics. Release of histamine from rat basophilic leukemia cells was found to be more sensitive to the intercalated cetirizine in the CETN compared with its free counterpart, with inhibition of 56% and 29%, respectively, at 62.5 ng/mL. The cytotoxicity assay toward Chang liver cells line show the IC50 for CETN and ZLH are 617 and 670 μg/mL, respectively. PMID:22848164

IC Treatment: Antihistamines

MedlinePlus

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Bilastine as a potential treatment in allergic rhinitis.

PubMed

Kowal, Krzysztof; DuBuske, Lawrence

2014-01-01

Allergic rhinitis is a very frequent disease. H1 antihistamines have been used for treatment of allergic rhinitis for more than 5 decades. They differ in chemical structure, pharmacokinetics, pharmacodynamics, clinical efficacy and adverse effects. We performed a detailed analysis of all available publications concerning the new H1-antihistamine bilasitine. Bilastine, a piperidine derivative, is a novel potent H1 antihistamine. It is at least as potent as cetirizine or fexofenadine in in vitro studies. In animal studies it demonstrates dose-dependent antihistaminic and antiallergic effects. In humans its metabolism is not affected by age, gender or renal function but may be affected by coadministration of P glycoprotein inhibitors. Efficacy of bilastine in therapy of allergic rhinitis patients has been documented in several large controlled clinical trials showing bilastine being at least as effective as cetirizine or desloratadine. No significant suppressive effect on central nervous system could be demonstrated when bilastine was used in the recommended doses. Bilastine is a novel H1 antihistamine with anti-allergic properties which is highly effective in the treatment of symptoms of allergic rhinitis. It has a favorable pharmacokinetic and pharmacodynamic profile and is generally well tolerated.

Effect of bilastine upon nasal obstruction.

PubMed

Dávila, I; Sastre, J; Mullol, J; Montoro, J; Jáuregui, I; Ferrer, M; del Cuvillo, A; Bartra, J; Valero, A

2011-01-01

H1 antihistamines constitute one of the main references for the treatment of allergic rhinitis. Classically, these drugs have been considered effective in controlling sneezing, rhinorrhea and itching, though they have not been regarded as particularly effective in application to nasal obstruction. The most recent studies, involving second-generation H1 antihistamines (desloratadine, fexofenadine, levocetirizine, rupatadine), have shown these drugs to offer effects upon nasal obstruction significantly superior to those of placebo. The present review examines the effect of bilastine, a new, potent and highly specific H1 antihistamine without sedative effects or cardiac toxicity, upon nasal obstruction. The analysis of the data from the different clinical trials indicates that in patients with allergic rhinitis, the effect of bilastine upon nasal obstruction is superior to that of placebo and similar to that of other second-generation H1 antihistamines, manifesting within 24 hours after the start of treatment.

Validated spectroscopic methods for determination of anti-histaminic drug azelastine in pure form: Analytical application for quality control of its pharmaceutical preparations

NASA Astrophysics Data System (ADS)

El-Masry, Amal A.; Hammouda, Mohammed E. A.; El-Wasseef, Dalia R.; El-Ashry, Saadia M.

2018-02-01

Two simple, sensitive, rapid, validated and cost effective spectroscopic methods were established for quantification of antihistaminic drug azelastine (AZL) in bulk powder as well as in pharmaceutical dosage forms. In the first method (A) the absorbance difference between acidic and basic solutions was measured at 228 nm, whereas in the second investigated method (B) the binary complex formed between AZL and Eosin Y in acetate buffer solution (pH 3) was measured at 550 nm. Different criteria that have critical influence on the intensity of absorption were deeply studied and optimized so as to achieve the highest absorption. The proposed methods obeyed Beer's low in the concentration range of (2.0-20.0 μg·mL- 1) and (0.5-15.0 μg·mL- 1) with % recovery ± S.D. of (99.84 ± 0.87), (100.02 ± 0.78) for methods (A) and (B), respectively. Furthermore, the proposed methods were easily applied for quality control of pharmaceutical preparations without any conflict with its co-formulated additives, and the analytical results were compatible with those obtained by the comparison one with no significant difference as insured by student's t-test and the variance ratio F-test. Validation of the proposed methods was performed according the ICH guidelines in terms of linearity, limit of quantification, limit of detection, accuracy, precision and specificity, where the analytical results were persuasive. The absorption spectrum of AZL (16 μg·mL- 1) in 0.1 M HCl. The absorption spectrum of AZL (16 μg·mL- 1) in 0.1 M NaOH. The difference absorption spectrum of AZL (16 μg·mL- 1) in 0.1 M NaOH vs 0.1 M HCl. The absorption spectrum of eosin binary complex with AZL (10 μg·mL- 1).

Pharmacy Use and Costs in Employer-Provided Health Plans. Insights for TRICARE Benefit Design from the Private Sector

DTIC Science & Technology

2005-01-01

non - steroidal anti - inflammatory drugs ( NSAIDs ), oral antihistamines, gastrointestinal agents, and oral...National Defense Authorization Act NSAID non - steroidal anti - inflammatory drug OLS ordinary least squares p-value probability value P&T Pharmacy...antihypertensives, non - steroidal anti - inflammatory drugs ( NSAIDs ), oral antihistamines, gastrointestinal agents, and oral hy-

Allergy Medications During Pregnancy.

PubMed

Gonzalez-Estrada, Alexei; Geraci, Stephen A

2016-09-01

Allergic diseases are common in women of childbearing age. Both asthma and atopic conditions may worsen, improve or remain the same during pregnancy. Primary care physicians commonly encounter women receiving multiple medications for pre-existing atopic conditions, who then become pregnant and require medication changes to avoid potential fetal injury or congenital malformations. Each medication should be evaluated; intranasal and inhaled steroids are relatively safe to continue during pregnancy (budesonide is the drug of choice), second-generation antihistamines of choice are cetirizine and loratadine, leukotriene receptor antagonists are safe, sparing use of oral decongestants during the first trimester and omalizumab may be used for both uncontrolled asthma and for antihistamine-resistant urticaria. Medications to avoid during pregnancy include intranasal antihistamines, first-generation antihistamines, mycophenolate mofetil, methotrexate, cyclosporine, azathioprine and zilueton. Common allergic diseases may develop de novo during pregnancy, such as anaphylaxis. Copyright © 2016 Southern Society for Clinical Investigation. Published by Elsevier Inc. All rights reserved.

Antiemetics With Concomitant Sedative Use in Civil Aviation Pilot Fatalities: From 2000 to 2006

DTIC Science & Technology

2007-10-01

Unclassified Unclassified 13 Form DOT F 1700.7 (8-72) Reproduction of completed page authorized iii CONTENTS INTRODUCTION...sedative hypnotics , and ethanol. Antiemetics and drugs with antiemetic properties such as metoclopramide, diphenhydramine (a sedating...antihistamines, ethanol, barbiturates, serotonin modulators, and/or sedative- hypnotics . Antihistamines such as diphenhydramine are commonly used. The

Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view.

PubMed

Sharma, A; Hamelin, B A

2003-04-01

The so-called "classic" histamine H(1) receptor antagonists are highly lipophilic compounds associated with significant biotransformation and tissue distribution. They are categorized according to their chemical structure into ethanolamines, alkylamines, ethylenediamines, piperazines, phenothiazines and piperidines, all of which have characteristic metabolic fates. The former four categories undergo primarily cytochrome P450-mediated oxidative N-desalkylations and deamination whereas the aromatic rings of the latter two undergo P450-mediated oxidative hydroxylation and/or epoxide formation. The common tertiary amino group is susceptible to oxidative metabolism by flavin containing monooxygenases forming N-oxides, and the alicyclic tertiary amines produce small amounts (up to 7%) of N-glucuronides in humans. Species, sex and racial differences in the metabolism and pharmacokinetics of antihistamines are known. Specific P450-isozymes implicated in the metabolism were identified in a few cases, such as CYP2D6 that contributes to the metabolism of promethazine, diphenhydramine and chlorpheniramine. Low circulating plasma concentrations of antihistamines are in part explained by significant first-pass effect and tissue distribution. Antihistaminic effects last up to 6 hours though some compounds exhibit a longer duration of action due to circulating active metabolites. Importantly, diphenhydramine inhibited CYP2D6 leading to a clinically significant drug-drug interaction with metoprolol. Other classic antihistamines were shown to be potent in vitro inhibitors of CYP2D6 and CYP3A4. The prescription-free access to most classic antihistamines can easily lead to their co-administration with other drugs metabolized by the same enzyme system thereby leading to drug accumulation and adverse effects. In depth knowledge of the metabolic pathways of classic antihistamines and the enzymes involved is crucial to prevent the high incidence of drug interactions in humans, which are

Effect of bilastine upon the ocular symptoms of allergic rhinoconjunctivitis.

PubMed

Bartra, J; Mullol, J; Montoro, J; Jáuregui, I; del Cuvillos, A; Dávila, I; Ferrer, M; Sastre, J; Valero, A

2011-01-01

Ocular symptoms often accompany allergic rhinitis and can be as or even more bothersome for the patient than the actual nasal symptoms. Ocular manifestations of allergic rhinoconjunctivitis may result from both direct allergen-mediated mast cell stimulation on the surface of the eye and naso-ocular reflexes--histamine being one of the mediators of symptoms onset. An H1 antihistamine would be the first line treatment for allergic conjunctivitis. Since allergic conjunctivitis is always (or almost always) accompanied by nasal symptoms, a second-generation H1 antihistamine administered via oral route is the drug of choice for jointly managing both the nasal and the ocular symptoms--minimizing the impact of the effects inherent to first-generation H, antihistamine, including particularly drowsiness. Bilastine is a new H1 antihistamine with an excellent safety profile, developed for the treatment of allergic rhinoconjunctivitis and urticaria, with potency similar to that of cetirizine and desloratadine, and superior to that of fexofenadine. This new drug has been shown to be effective in controlling the ocular symptoms of allergic rhinoconjunctivitis.

Loss of work productivity due to illness and medical treatment.

PubMed

Cockburn, I M; Bailit, H L; Berndt, E R; Finkelstein, S N

1999-11-01

We examined the effects on work productivity of treatment with antihistamines in a retrospective study using linked health claims data and daily work output records for a sample of nearly 6000 claims processors at a large insurance company, between 1993 and 1995. We explained the variation in work output depending on the subjects' demographic characteristics, their jobs, and whether they were treated with "sedating" versus "nonsedating" antihistamines for nasal allergies. Differences of up to 13% in productivity were found after the subjects took sedating or nonsedating antihistamines. The observed effect suggests substantial indirect economic costs, which up to now have been largely overlooked because work productivity has proved difficult to measure objectively.

Psychiatric co-morbidity associated with pheniramine abuse and dependence

PubMed Central

Pal, Hemraj; Kumar, Rajesh; Bhushan, Shashi; Berry, Neeraj

2005-01-01

The abuse of cough syrups containing antihistamines and codeine is being increasingly noted. The abuse of antihistamines alone has also been reported. The use of antihistamines alone or in combination with other substances of abuse may predispose individuals to develop psychiatric symptoms or syndromes as a part of intoxication, withdrawal or as co-morbid conditions. We present two case reports to highlight the occurrence of co-morbid psychopathology in association with antihistamine abuse and dependence. Case I used high doses of pheniramine for about 2 years and became suspicious of his wife; he even doubted the paternity of his yet-to-be-born child. The associated behavioural abnormalities suggested that he was acting out on the delusion. He also had seizures associated with the intake of a high dose of pheniramine. Case II had multiple substance use, and dependence on alcohol and pheniramine. He demonstrated abnormal behaviour suggestive of psychosis and organic brain syndrome that persisted for a few days and remitted on discontinuation of the substances. These two cases demonstrate the occurrence of psychotic syndromes associated with heavy pheniramine use. The psychopathology can vary from an independent psychotic syndrome to an organic brain syndrome-like disorder.

Development and validation of a rapid stability indicating HPLC-method using monolithic stationary phase and two spectrophotometric methods for determination of antihistaminic acrivastine in capsules

NASA Astrophysics Data System (ADS)

Gouda, Ayman A.; Hashem, Hisham; Jira, Thomas

2014-09-01

Simple, rapid and accurate high performance liquid chromatographic (HPLC) and spectrophotometric methods are described for determination of antihistaminic acrivastine in capsules. The first method (method A) is based on accurate, sensitive and stability indicating chromatographic separation method. Chromolith® Performance RP-18e column, a relatively new packing material consisting of monolithic rods of highly porous silica, was used as stationary phase applying isocratic binary mobile phase of ACN and 25 mM NaH2PO4 pH 4.0 in the ratio of 22.5:77.5 at flow rate of 5.0 mL/min and 40 °C. A diode array detector was used at 254 nm for detection. The elution time of acrivastine was found to be 2.080 ± 0.032. The second and third methods (methods B and C) are based on the oxidation of acrivastine with excess N-bromosuccinimide (NBS) and determination of the unconsumed NBS with, metol-sulphanilic acid (λmax: 520 nm) or amaranth dye (λmax: 530 nm). The reacted oxidant corresponds to the drug content. Beer’s law is obeyed over the concentration range 1.563-50, 2.0-20 and 1.0-10 μg mL-1 for methods A, B and C, respectively. The limits of detection and quantitation were 0.40, 0.292 and 0.113 μg mL-1 and 0.782, 0.973 and 0.376 μg mL-1 for methods A, B and C, respectively. The HPLC method was validated for system suitability, linearity, precision, limits of detection and quantitation, specificity, stability and robustness. Stability tests were done through exposure of the analyte solution for four different stress conditions and the results indicate no interference of degradants with HPLC-method. The proposed methods was favorably applied for determination of acrivastine in capsules formulation. Statistical comparison of the obtained results from the analysis of the studied drug to those of the reported method using t- and F-tests showed no significant difference between them.

Can human allergy drug fexofenadine, an antagonist of histamine (H1) receptor, be used to treat dog and cat? Homology modeling, docking and molecular dynamic Simulation of three H1 receptors in complex with fexofenadine.

PubMed

Sader, Safaa; Cai, Jun; Muller, Anna C G; Wu, Chun

2017-08-01

Fexofenadine, a potent antagonist to human histamine 1 (H 1 ) receptor, is a non-sedative third generation antihistamine that is widely used to treat various human allergic conditions such as allergic rhinitis, conjunctivitis and atopic dermatitis. Encouragingly, it's been successfully used to treat canine atopic dermatitis, this supports the notion that it might have a great potential for treating other canine allergic conditions and other mammal pets such as dog. Regrettably, while there is a myriad of studies conducted on the interactions of antihistamines with human H 1 receptor, the similar studies on non-human pet H 1 are considerably scarce. The published studies using the first and second generation antihistamines drugs have shown that the antihistamine response is varied and unpredictable. Thus, to probe its efficacy on pet, the homology models of dog and cat H 1 receptors were built based on the crystal structure of human H 1 receptor bound to antagonist doxepin (PDB 3RZE) and fexofenadine was subsequently docked to human, dog and cat H 1 receptors. The docked complexes are then subjected to 1000ns molecular dynamics (MD) simulations with explicit membrane. Our calculated MM/GBSA binding energies indicated that fexofenadine binds comparably to the three receptors; and our MD data also showed the binding poses, structural and dynamic features among three receptors are very similar. Therefore, our data supported the application of fexofenadine to the H 1 related allergic conditions of dog and cat. Nonetheless, subtle systemic differences among human, dog and cat H 1 receptors were also identified. Clearly, there is still a space to develop a more selective, potent and safe antihistamine alternatives such as Fexofenadine for dog or cat based on these differences. Our computation approach might provide a fast and economic way to predict if human antihistamine drugs can also be safely and efficaciously administered to animals. Copyright © 2017 Elsevier Inc

Bilastine and the central nervous system.

PubMed

Montoro, J; Mullol, J; Dávila, I; Ferrer, M; Sastre, J; Bartra, J; Jáuregui, I; del Cuvillo, A; Valero, A

2011-01-01

Antihistamines have been classifed as first or second generation drugs, according to their pharmacokinetic properties, chemical structure and adverse effects. The adverse effects of antihistamines upon the central nervous system (CNS) depend upon their capacity to cross the blood-brain barrier (BBB) and bind to the central H1 receptors (RH1). This in turn depends on the lipophilicity of the drug molecule, its molecular weight (MW), and affinity for P-glycoprotein (P-gp) (CNS xenobiotic substances extractor protein). First generation antihistamines show scant affinity for P-gp, unlike the second generation molecules which are regarded as P-gp substrates. Histamine in the brain is implicated in many functions (waking-sleep cycle, attention, memory and learning, and the regulation of appetite), with numerous and complex interactions with different types of receptors in different brain areas. Bilastine is a new H1 antihistamine that proves to be effective in treating allergic rhinoconjunctivitis (seasonal and perennial) and urticaria. The imaging studies made, as well as the objective psychomotor tests and subjective assessment of drowsiness, indicate the absence of bilastine action upon the CNS. This fact, and the lack of interaction with benzodiazepines and alcohol, define bilastine as a clinically promising drug with a good safety profile as regards adverse effects upon the CNS.

Establishing the place in therapy of bilastine in the treatment of allergic rhinitis according to ARIA: evidence review.

PubMed

Bousquet, Jean; Ansótegui, Ignacio; Canonica, G Walter; Zuberbier, Torsten; Baena-Cagnani, Carlos E; Bachert, Claus; Cruz, Alvaro A; González, Sandra N; Kuna, Piotr; Morais-Almeida, Mario; Mullol, Joaquim; Ryan, Dermot P; Sánchez-Borges, Mario; Valiente, Román; Church, Martin K

2012-01-01

The ARIA (Allergic Rhinitis and its Impact on Asthma) guidelines development group examined the properties of oral H(1)-antihistamines and made proposals about an 'optimal' drug. Several criteria should be met by oral H(1)-antihistamines in terms of their pharmacological, and clinical efficacy and safety profiles. Bilastine, a new H(1)-antihistamine, has been approved in 28 European countries for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria in adults and children older than 12 years. To determine its potential place in therapy in the treatment of allergic rhinitis, this manuscript examines whether bilastine meets the criteria defined in the European Academy of Allergy and Clinical Immunology (EAACI)/ARIA proposals for oral H(1)-antihistamines. The optimal properties of oral H(1)-antihistamines and current ARIA recommendations for their use in allergic rhinitis are presented, as well as relevant pharmacological and clinical data for bilastine obtained from the published literature that specifically address the defined criteria. Bilastine is a potent inhibitor of the histamine H(1) receptor. Data from preclinical studies have confirmed its selectivity for the histamine H(1) receptor over other receptors, and demonstrated antihistaminic properties in vitro and in vivo. Bilastine does not interfere with the cytochrome P450 system and is devoid of cardiac side effects. Studies in healthy volunteers and patients have shown that bilastine does not affect driving ability, cardiac conduction or alertness. In large pivotal randomized, placebo-controlled trials (RCTs), bilastine had a favourable safety profile. Bilastine 20 mg once daily improved all nasal and ocular symptoms of allergic rhinitis with greater efficacy than placebo and comparable to that of cetirizine and desloratadine. Moreover, bilastine was shown to improve quality of life, an important outcome of RCTs in allergic diseases. There were no significant changes in laboratory tests

Management for the children with otitis media with effusion in the tertiary hospital.

PubMed

Choung, Yun-Hoon; Shin, You Ree; Choi, Seong Jun; Park, Keehyun; Park, Hun Yi; Lee, Jong Bin; Han, Dong Hee; Kahng, Hison

2008-12-01

Recently, new evidence-based recommendations have been introduced for diagnosing and managing otitis media with effusion (OME) in children. However, there are some difficulties to follow the general guidelines in the tertiary hospitals. The purpose is to evaluate the efficiency of antibiotics or antihistamines for treatment of children with OME in the tertiary hospital with a randomized prospective clinical study. Eighty-four children with OME who had been diagnosed in the tertiary hospital were randomized to receive 5 different medications for 2 weeks. We prescribed antibiotics (amoxicillin-clavulanate syrup) in Group I (n=16), antibiotics/steroids (prednisolone) in Group II (n=18), antibiotics/antihistamines (ebastine) in Group III (n=15), antibiotics/steroids/antihistamines in Group IV (n=17), and mucolytics (ivy leaf extract) in Group V (n=17) for control. We followed-up children every 2 weeks and evaluated the state of OME at 3 months. Thirty six (42.9%) of 84 children were resolved within average 6.9 weeks after the treatments. Thirty-six (42.9%) were treated with ventilation tube insertion and 12 patients (14.3%) were observed. There was no difference in the resolution rates of OME among the five different protocols (P>0.05). There was no difference in the resolution rates among groups who used steroids, antihistamines, steroids and antihistamines, or other medications to manage 42 children with allergies (P>0.05). In the tertiary hospital, the cure rate of children with OME was not as high as well-known, and antibiotics or anti-allergic medications were not more effective than control. We may, therefore, need any other guidelines which are different from the previous evidence-based recommendations, including early operation in the tertiary hospitals.

In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist.

PubMed

Corcóstegui, Reyes; Labeaga, Luis; Innerárity, Ana; Berisa, Agustín; Orjales, Aurelio

2006-01-01

We set out to establish the in vivo histamine H(1) receptor antagonistic (antihistaminic) and antiallergic properties of bilastine. In vivo antihistaminic activity experiments consisted of measurement of: inhibition of increase in capillary permeability and reduction in microvascular extravasation and bronchospasm in rats and guinea pigs induced by histamine and other inflammatory mediators; and protection against lethality induced by histamine and other inflammatory mediators in rats. In vivo antiallergic activity experiments consisted of measurement of passive and active cutaneous anaphylactic reactions as well as type III and type IV allergic reactions in sensitised rodents. In the in vivo antihistaminic activity experiments, bilastine was shown to have a positive effect, similar to that of cetirizine and more potent than that of fexofenadine. The results of the in vivo antiallergic activity experiments showed that the properties of bilastine in this setting are similar to those observed for cetirizine and superior to fexofenadine in the model of passive cutaneous anaphylactic reaction. When active cutaneous anaphylactic reaction experiments were conducted, bilastine showed significant activity, less potent than that observed with cetirizine but superior to that of fexofenadine. Evaluation of the type III allergic reaction showed that of the antihistamines only bilastine was able to inhibit oedema in sensitised mice, although its effect in this respect was much less potent than that observed with dexamethasone. In terms of the type IV allergic reaction, neither bilastine, cetirizine nor fexofenadine significantly modified the effect caused by oxazolone. The results of our in vivo preclinical studies corroborate those obtained from previously conducted in vitro experiments of bilastine, and provide evidence that bilastine possesses antihistaminic as well as antiallergic properties, with similar potency to cetirizine and superior potency to fexofenadine.

Diagnosis, pathogenesis, and treatment of chronic spontaneous urticaria.

PubMed

Kaplan, Allen P

2018-05-01

Chronic Spontaneous Urticaria (CSU) is an endogenous disorder that is strongly associated with autoimmunity, particularly with immunoglobulin G (IgG) antibody to the alpha subunit of the IgE receptor seen in 35-40% of patients. Basophils and cutaneous mast cells can be activated and lead to a late-phase-like perivascular infiltration about small venules and hive formation. Review of current literature. Antibody to thyroid antigens are seen in 25% of patients; a small fraction of these may be clinically hypothyroid (Hashimoto's Thyroiditis). Forty percent of patients have angioedema, but not laryngeal edema. Therapy typically begins with second-generation antihistamines (H1 receptor blockers) up to four times a day. The failure rate is substantial, and estimates vary from 25% to 50%. The drug of choice for antihistamine resistant cases is omalizumab, at 300 mg/month, which is effective in 70% of patients. H-2-antagonists and leucotriene antagonists are no longer recommended because the literature does not support additional efficacy beyond blockage of H-1 receptors. For patients unresponsive to antihistamines and omalizumab, cyclosporine is recommended next. This is similarly effective in 65-70% of patients; however, assessment of blood pressure and renal function need to be followed every 4-6 weeks. Corticosteroid should not be employed chronically; however, a brief course of 3-10 days can be used acutely for severe exacerbations. Other agents, such as dapsone, sulfasalazine, or hydroxychloroquin, can be tried when the aforementioned medications fail, but the results are unpredictable because they have not been shown to have efficacy beyond the placebo effect (25-30%), and have not been studied in patients for whom the aforementioned approach i.e. antihistamines, omalizumab, and cyclosporine has failed. High dose antihistamines, omalizumab and cyclosporine (in that order) are effective and recommended for therapy of CUS, an inflammatory skin disorder associated

Antihistamines, Decongestants, and Cold Remedies

MedlinePlus

... Humanitarian Efforts International Outreach Advocacy Board of Governors Industry Programs Professional Development Home AcademyU Home Study Course Maintenance of Certification Conferences & Events Practice Management Home Resources ...

Antihistamines: Understanding Your OTC Options

MedlinePlus

... you can buy over the counter include: Brompheniramine (brand names include Children’s Dimetapp Cold) Chlorpheniramine (brand names include Chlor-Trimeton, Actifed Cold) Dimenhydrinate (brand ...

Antihistamines, Decongestants, and Cold Remedies

MedlinePlus

... Programs Professional Development Home AcademyU Home Study Course Maintenance of Certification Conferences & Events Practice Management Home Resources Quality Clinical Data Registry Research Reimbursement ...

Impact of fexofenadine, osthole and histamine on peripheral blood mononuclear cell proliferation and cytokine secretion.

PubMed

Karolina Kordulewska, Natalia; Kostyra, Elżbieta; Matysiewicz, Michał; Cieślińska, Anna; Jarmołowska, Beata

2015-08-15

This paper compares results of peripheral blood mononuclear cell (PBMC) incubation with fexofenadine (FXF) and osthole. FXF is a third-generation antihistamine drug and osthole is assumed a natural antihistamine alternative. To our best knowledge, this is the first comparative study on FXF, osthole and histamine cytokine secretion and cytotoxicity in PBMC in vitro cultures using cell proliferation ELISA BrdU. The cultures were treated 12, 42, 48 and 72h with FXF and osthole at 150, 300 and 450ng/ml concentrations and histamine at 50, 100 and 200ng/ml. Our study results confirm that FXF, osthole and histamine exert no cytotoxic effect on PBMCs and that IL-6, IL-10 and TNF-α cytokine secretion following osthole cell stimulation was similar to that by FXF stimulation.This confirms our hypothesis that osthole is a natural histamine antagonist, and can therefore be beneficially applied in antihistamine treatment. Copyright © 2015 Elsevier B.V. All rights reserved.

Critical appraisal of the unmet needs in the treatment of chronic spontaneous urticaria with omalizumab: an Italian perspective.

PubMed

Asero, Riccardo; Canonica, Giorgio W; Cristaudo, Antonio; Fierro, Maria T; Girolomoni, Giampiero; Marzano, Angelo V; Nettis, Eustachio; Pepe, Patrizia; Pigatto, Paolo; Rossi, Oliviero

2017-12-01

The humanized anti-IgE antibody omalizumab has been available for patients with chronic spontaneous urticaria (CSU) in Italy since 2015. This review summarizes the unresolved issues and unmet therapeutic needs associated with omalizumab and discusses practical recommendations for its use in the management of CSU. Although modern second-generation H1-antihistamines are the standard of care for patients with CSU, adjunctive treatments (including omalizumab) may be required for effective control of symptoms in many patients. Evidence from clinical trials and experience from daily clinical practice suggest that the use of omalizumab in patients with CSU who have inadequate response to H1-antihistamines remains challenging. Based on current international guidelines, omalizumab labelling information and our experience in clinical practice, we provide treatment recommendations regarding the use of omalizumab in patients with CSU. These include: optimal treatment duration, the use of concomitant antihistamine therapy, the definition and management of disease relapse after treatment, and the management of patients with late or no response to treatment.

The Effectiveness of Automatic Recommending System for Premedication in Reducing Recurrent Radiocontrast Media Hypersensitivity Reactions

PubMed Central

Bae, Yun-Jeong; Hwang, Ye Won; Yoon, Sun-young; Kim, Sujeong; Lee, Taehoon; Lee, Yoon Su; Kwon, Hyouk-Soo; Cho, You Sook; Shin, Myung Jin; Moon, Hee-Bom; Kim, Tae-Bum

2013-01-01

Background Non-ionic radiocontrast media (RCM) is rarely associated with hypersensitivity reactions. Premedication of patients who reacted previously to RCM with systemic corticosteroids and/or antihistamines can help reduce recurrent hypersensitivity reactions. However, premedication is still not prescribed in many cases for various reasons. This study aimed to determine the effectiveness of our novel RCM hypersensitivity surveillance and automatic recommending system for premedication. Methods and Results Hospitalized patients with a history of RCM hypersensitivity were identified in an electronic medical record system that included a mandatory reporting system for past adverse drug reactions. In 2009, a novel automatic prescription system was added that classified index RCM reactions by severity and dispensed appropriate corticosteroid and/or antihistamine pretreatment prior to new RCM exposures. The data from 12 months under the previous system and 12 months under the current system were compared. The two systems had similar overall premedication rates (91% and 95%) but the current system was associated with a significantly higher corticosteroid premedication rate (65% vs. 14%), which significantly reduced the breakthrough reaction rate (6.7% vs. 15.2%). The current system was also associated with increased corticosteroid and antihistamine premedication of patients with a mild index reaction (61% vs. 7%) and a reduction in their breakthrough reaction rate (6% vs. 15%). Conclusions Premedication with corticosteroid and/or antihistamine, which was increased by our novel automatic prescription system, significantly reduced breakthrough reactions in patients with a history of RCM hypersensitivity. PMID:23840391

Nonprescription medications for respiratory symptoms: Facts and marketing fictions.

PubMed

Weinberger, Miles; Hendeles, Leslie

2018-05-01

There are many nonprescription (over-the-counter [OTC]) medications available on pharmacy shelves marketed for relief of respiratory symptoms. The number of such medications has been increasing. This review provides an evidence-based examination of OTC products used for respiratory symptoms. Antihistamines, decongestants, mucolytics, antitussives, and intranasal steroids were selected as the most common OTC medications taken by adults and children for various respiratory symptoms. Controlled clinical trials of efficacy were identified by searching a medical literature data base. Those trials and key publications related to the pharmacokinetics and pharmacodynamics of the products were reviewed. Comparisons of the various OTC antihistamines' ability to suppress the effects of histamine were related to their clinical benefit. Intranasal corticosteroids are the preferred agents for maintenance therapy of persistent nasal congestion and are highly effective for symptoms of inhalant allergy other than allergic conjunctivitis. The disconnect between marketing claims and evidence was demonstrated for antihistamines and oral alpha-1 adrenergic agonist decongestants. Data for OTC mucolytics and antitussives were insufficient to justify their use based on the evidence. There was little relationship between marketing claims and evidence regarding OTC medications used for respiratory symptoms. Analysis of data supported cetirizine, levocetirizine, and fexofenadine as the most effective of the OTC antihistamines. There were no data that supported the use of oral phenylephrine as a decongestant. Neither OTC mucolytics or antitussives provided sufficient evidence to justify their use.

Advertisements impact the physiological efficacy of a branded drug

PubMed Central

Kamenica, Emir; Naclerio, Robert; Malani, Anup

2013-01-01

We conducted randomized clinical trials to examine the impact of direct-to-consumer advertisements on the efficacy of a branded drug. We compared the objectively measured, physiological effect of Claritin (Merck & Co.), a leading antihistamine medication, across subjects randomized to watch a movie spliced with advertisements for Claritin or advertisements for Zyrtec (McNeil), a competitor antihistamine. Among subjects who test negative for common allergies, exposure to Claritin advertisements rather than Zyrtec advertisements increases the efficacy of Claritin. We conclude that branded drugs can interact with exposure to television advertisements. PMID:23878212

Advertisements impact the physiological efficacy of a branded drug.

PubMed

Kamenica, Emir; Naclerio, Robert; Malani, Anup

2013-08-06

We conducted randomized clinical trials to examine the impact of direct-to-consumer advertisements on the efficacy of a branded drug. We compared the objectively measured, physiological effect of Claritin (Merck & Co.), a leading antihistamine medication, across subjects randomized to watch a movie spliced with advertisements for Claritin or advertisements for Zyrtec (McNeil), a competitor antihistamine. Among subjects who test negative for common allergies, exposure to Claritin advertisements rather than Zyrtec advertisements increases the efficacy of Claritin. We conclude that branded drugs can interact with exposure to television advertisements.

[Management of side effects of targeted therapies in renal cancer: iatrogenic side effects].

PubMed

Massard, Christophe; Patard, Jean-Jacques; Hermine, Olivier; Ravaud, Alain

2011-01-01

Since premedication of patients with an H1 antihistamine is recommended before the start of the intravenous infusion of temsirolimus, temsirolimus is to be used with caution in cases where there is a history of hypersensitivity to this class of antihistamines, or medical contra-indication for treatment with antihistamines. Comorbidities and co-medications must be taken into account in the prescription of targeted therapies. For sunitinib, sorafenib, and pazopanib: potential drug interactions are possible with inducers/inhibitors of CYP3A4, anti-hypertensive drugs, antidiabetic drugs, thyroid hormones, and anticoagulant treatments. The combination of bevacizumab and sunitinib is very toxic (microangiopathic haemolytic anaemia), and is contra-indicated unless part of a clinical trial. Screening, equilibration or treatment of hypothyroidism, anaemia, undernutrition, hypophosphatemia, hypomagnesaemia, sleep disorders, depression or other comorbidities, which may contribute to asthenia is recommended. In patients treated with sunitinib or pazopanib, a thyroid function test is recommended at the treatment centre as well as regular TSH assays. Copyright © 2011 Société Française du Cancer. Published by Elsevier Masson SAS. All rights reserved.

A dose-ranging study of the effects of mequitazine on actual driving, memory and psychomotor performance as compared to dexchlorpheniramine, cetirizine and placebo.

PubMed

Theunissen, E L; Vermeeren, A; van Oers, A C M; van Maris, I; Ramaekers, J G

2004-02-01

Mequitazine is a so-called 'non-sedative' second-generation antihistamine even though it has never been firmly established that this drug's sedative potential actually differs from that of the 'sedative' first-generation antihistamines. The present study compares the sedative effects of three doses of mequitazine on actual driving, psychomotor performance and memory with those of a first- and a second-generation antihistamine. Eighteen healthy volunteers received on separate days a single dose of 5, 10 and 15 mg mequitazine, 10 mg cetirizine, 6 mg dexchlorpheniramine and placebo. Drug effects were assessed using two actual driving tests (highway-driving test and car-following test), cognitive and psychometric tests (tracking, divided attention, memory, reasoning and critical flicker fusion), pupil size and questionnaires. Highway-driving data revealed an overall effect of Treatment on the standard deviation of lateral position (SDLP). Dexchlorpheniramine impaired driving performance as indicated by a significant rise in SDLP. Mequitazine significantly increased SDLP in a dose-related manner, but the separate dose effects failed to reach statistical significance. Divided attention performance was also affected by Treatment. Reaction time (RT) during mequitazine treatments increased in a dose-related manner and significantly differed from placebo at the highest dose. Subjects reported to be less alert after treatment with dexchlorpheniramine. Cetirizine did not affect performance in any of the tasks. It was concluded that mequitazine is mildly sedating. The effects of mequitazine are comparable to those of other second-generation antihistamines, in that it causes mild driving impairment, particularly at higher doses.

Prolonged anticholinergic delirium following antihistamine overdose.

PubMed

Scott, James; Pache, David; Keane, Greg; Buckle, Helen; O'Brien, Natalie

2007-06-01

A case of anticholinergic delirium in a female adolescent is described, exploring the pharmacokinetic reasons for the prolonged time course and reviewing the management provided. A 14 year old female hospitalised for depression ingested large quantities of promethazine and cyproheptadine. A severe anticholinergic delirium ensued which resolved after six days, much longer than the expected duration. The likely cause of the prolonged delirium was the interaction of promethazine and fluvoxamine through the inhibition of the CYP2D6 enzyme. The patient's young age, the severity of the poisoning and the use of drugs with anticholinergic properties to manage the delirium may also have contributed. The delirium may have been reversed had a cholinesterase inhibitor been provided soon after the overdose.

Evaluating approved medications to treat allergic rhinitis in the United States: an evidence-based review of efficacy for nasal symptoms by class.

PubMed

Benninger, Michael; Farrar, Judith R; Blaiss, Michael; Chipps, Bradley; Ferguson, Berrylin; Krouse, John; Marple, Bradley; Storms, William; Kaliner, Michael

2010-01-01

To evaluate how well the medications currently approved in the United States for allergic rhinitis (AR) treat nasal symptoms when examined according to Food and Drug Administration-indicated uses and dosages. MEDLINE (1966 onward), EMBASE (1974 onward), and the Cochrane Library (2007) were systematically searched according to the following criteria defined at a roundtable meeting of the authors: randomized controlled trial, at least a 2-week duration, and approved indication and dosage in the United States. Data from studies that met the inclusion criteria were extracted into evidence tables, which were reviewed twice by the full panel of authors. Individual panel members also were asked to comment on abstracts, articles, and summary tables based on their known expertise. The entire faculty approved the selection of studies included in this review. Fifty-four randomized, placebo-controlled studies involving more than 14,000 adults and 1,580 children with AR met the criteria for review: 38 studies of seasonal allergic rhinitis (SAR; n = 11,980 adults and 946 children) and 12 studies of perennial allergic rhinitis (PAR; n = 3,800 adults and 366 children). The median percentage changes from baseline for total nasal symptom score for SAR were as follows: nasal antihistamines, -22.2%; oral antihistamines, -23.5%; intranasal steroids (INSs), -40.7%; and placebo, -15.0%. For PAR, the changes were as follows: oral antihistamines, -51.4%; INSs, -37.3%; and placebo, -24.8%. Data for mediator antagonists were limited. The data, although limited, confirm that INSs produce the greatest improvements in nasal symptoms in patients with SAR. In addition, INSs are effective for PAR, but the data were of variable quality, and oral antihistamines may be equally effective for some patients. The reporting of published data should be standardized to permit better comparisons in future studies.

The Allergic Rhinitis Control Test questionnaire is valuable in guiding step-down pharmacotherapy treatment of allergic rhinitis.

PubMed

Zhu, Rongfei; Wang, Jingru; Wu, Yuying; Yang, Yongshi; Huang, Nan; Yang, Yaqi; Zhang, Rui; Ma, Dongxia; Yang, Lin; Demoly, Pascal

2018-06-07

Allergic Rhinitis Control Test(ARCT) has been validated in allergic rhinitis(AR) step-up pharmacotherapy management approach. The aim of our study was to evaluate the potential of ARCT in AR step-down pharmacotherapy. In an open-labelled randomized controlled study, AR patients controlled with intranasal corticosteroid(INS) plus antihistamine(step 4) were included and randomized into an ARCT or a control group. In ARCT group, the patients were followed up every 15 days; if ARCT score was ≥20(controlled AR), the patient would step down to step 3(INS), step 2(daily antihistamine), step 1(antihistamine as needed) and step 0(no medication) consecutively; if ARCT score was strictly <20, the treatment would not be adjusted. In the control group, patients would be treated with step 4 medications during the whole study. Rhinitis Quality-of-Life Questionnaire(RQLQ), Morisky Questionnaire and Brief Illness-Perception-Questionnaire(B-IPQ) were completed at baseline and the end of the study. Medication use and side effects were recorded. A total of 255 AR patients were enrolled into the study, 27 patients dropped out. The control rates at D45 were 77.8% in ARCT group and 85.8% in control group(P>0.05). ARCT group had less mean medication use than control group(INS 1.27 vs. 2.22 bottle, antihistamines 35.9 vs. 61.4 tablets)(P<0.05). RQLQ, Morisky and B-IPQ score were significantly improved in both groups after treatment(P<0.05). Stepping down AR medications in controlled patients led to similar clinical outcomes at reduced cost compared with those who maintained their current treatment level. ARCT is an optimal tool for evaluating the step-down eligibility. Copyright © 2018. Published by Elsevier Inc.

Management of Allergic Rhinitis

PubMed Central

Sausen, Verra O.; Marks, Katherine E.; Sausen, Kenneth P.; Self, Timothy H.

2005-01-01

Allergic rhinitis is the most common chronic childhood disease. Reduced quality of life is frequently caused by this IgE-mediated disease, including sleep disturbance with subsequent decreased school performance. Asthma and exercise-induced bronchospasm are commonly seen concurrently with allergic rhinitis, and poorly controlled allergic rhinitis negatively affects asthma outcomes. Nonsedating antihistamines or intranasal azelastine are effective agents to manage allergic rhinitis, often in combination with oral decongestants. For moderate to severe persistent disease, intranasal corticosteroids are the most effiective agents. Some patients require concomitant intranasal corticosteroids and nonsedating antihistamines for optimal management. Other available agents include leukotriene receptor antagonists, intranasal cromolyn, intranasal ipratropium, specific immunotherapy, and anti-IgE therapy. PMID:23118635

Medicines for sleep

MedlinePlus

Benzodiazepines; Sedatives; Hypnotics; Sleeping pills; Insomnia - medicines; Sleep disorder - medicines ... the-counter (OTC) sleeping pills contain antihistamines. These medicines are commonly used to treat allergies. While these ...

Cytokine production by PBMC and serum from allergic and non-allergic subjects following in vitro histamine stimulation to test fexofenadine and osthole anti-allergic properties.

PubMed

Kordulewska, Natalia Karolina; Kostyra, Elżbieta; Cieślińska, Anna; Fiedorowicz, Ewa; Jarmołowska, Beata

2016-11-15

FXF is a third-generation antihistamine drug and osthole is assumed a natural antihistamine alternative. This paper compares peripheral blood mononuclear cell (PBMC) incubation with FXF and osthole, by studying FXF, osthole and histamine cytokine secretion in PBMC in vitro cultures. Mabtech kits determined the interleukins IL-1β, IL-4, IL-10, IL-13 and TNF-α. The influence of the above active substances on cytokine secretion in PBMC's and serum was assessed: cytokines were IL-1β, IL-4, IL-10, IL-13 and TNF-α; and cytokine levels secreted by untreated PBMCs in pure culture medium formed the absolute control (ctrl). We determined that osthole affects PBMC cytokine secretion to almost precisely the same extent as FXF (IL-1β, IL-4, IL-10 and TNF). In addition osthole had greater IL-13 blocking ability than FXF. Moreover, we observed significantly decreased IL-4 level in histamine/osthole theatment compared to histamine alone. Meanwhile, FXF not significantly decrease the level of IL-4 increased by histamine. This data indicates osthole's strong role in allergic inflamation. All results confirm our hypothesis that osthole is a natural histamine antagonist and therefore can be beneficially used in antihistamine treatment of conditions such as allergies. Copyright © 2016 Elsevier B.V. All rights reserved.

Effects of fexofenadine and hydroxyzine on brake reaction time during car-driving with cellular phone use.

PubMed

Tashiro, Manabu; Horikawa, Etsuo; Mochizuki, Hideki; Sakurada, Yumiko; Kato, Motohisa; Inokuchi, Takatoshi; Ridout, Fran; Hindmarch, Ian; Yanai, Kazuhiko

2005-10-01

Antihistamines are a mainstay treatment for allergic rhinitis; however, many older agents cause adverse events, including sedation and central nervous system (CNS) impairment. Research has shown sedating effects of antihistamines on driving; currently, no known study has examined whether cellular phone usage while driving further compounds impairment in individuals administered antihistamines. The aim of this study was to examine this endpoint. In a randomized, double-blind, placebo-controlled, three-way crossover study, healthy volunteers received fexofenadine HCl 120 mg, hydroxyzine HCl 30 mg and placebo. Brake reaction time (BRT) was used to examine driving performance across four conditions: driving only; driving while completing simple calculations; complex calculations; and conversing on a cellular phone. Subjective sedation assessments were also conducted. Brake reaction time with and without cellular phone usage in fexofenadine-treated subjects did not differ significantly from placebo in any condition. In contrast, hydroxyzine-treated subjects were significantly more sedated and had slower BRTs, suggesting slower hazard recognition and brake application, compared with the fexofenadine and placebo groups in all conditions. Importantly, cellular phone operation was an additive factor, increasing BRTs in hydroxyzine-treated volunteers. Fexofenadine did not impair CNS function in subjects involved in a divided attention task of driving and cellular phone operation. Copyright (c) 2005 John Wiley & Sons, Ltd.

Bilastine for the treatment of urticaria.

PubMed

Jáuregui, Ignacio; Ferrer, Marta; Bartra, Joan; del Cuvillo, Alfonso; Dávila, Ignacio; Montoro, Javier; Mullol, Joaquim; Sastre, Joaquín; Valero, Antonio

2013-08-01

Urticaria is a highly prevalent disease among people. First-choice treatment continues to be centred on the second-generation H1 antihistamines, including a wide group of drugs with a better therapeutic index (or risk:benefit ratio) than the classic ones, even in the high, off-label dosage occasionally required in chronic urticaria. Bilastine is a newly registered H1-antihistamine for treatment of allergic rhinoconjunctivitis and urticaria. With established antihistaminic and antiallergic properties, it is widely reviewed in the medical literature; however, to our knowledge, a specific review of bilastine's role in the treatment of urticaria was lacking. This article reviews the medical literature on the effectiveness and safety of bilastine in urticarial syndromes, either spontaneous or inducible, by means of a Medline search from 1990 to present, completed with some nonpublished data provided by the manufacturer. Once-daily treatment with bilastine 20 mg is effective in managing symptoms and improving patient's quality of life in chronic urticaria, with at least comparable efficacy to levocetirizine. As far as studies in healthy volunteers, clinical assays, and recent clinical experience can establish, bilastine's safety profile is adequate, appearing to be entirely free from cardiovascular effects, and not impairing psychomotor performance or actual driving, even at twice the therapeutic dose.

Desloratadine and pseudoephedrine combination therapy as a comprehensive treatment for allergic rhinitis and nasal congestion.

PubMed

Anolik, Robert

2009-06-01

Allergic rhinitis (AR) is rapidly increasing in global prevalence. Symptoms of AR, particularly nasal congestion, can cause quality of life (QoL) impairment. Second-generation antihistamines are a recommended first-line therapy for AR but are not viewed as very effective for the treatment of congestion. Therefore, an antihistamine plus a decongestant, such as the combination of desloratadine and pseudoephedrine, is a convenient and efficacious treatment. To review the clinical evidence on the efficacy and safety of combination desloratadine/pseudoephedrine for the treatment of AR symptoms, particularly nasal congestion. Four large studies found that improvement in nasal congestion is enhanced when patients are treated with combination desloratadine/pseudoephedrine. The combination drug significantly improved mean reflective nasal congestion scores in these studies compared with either component as monotherapy (p antihistamine desloratadine in combination with the decongestant pseudoephedrine may be regarded as an efficacious and convenient option for patients with AR who are particularly troubled by nasal congestion.

Indomethacin-antihistamine combination for gastric ulceration control

NASA Technical Reports Server (NTRS)

Brown, P. A.; Danellis, J. V. (Inventor)

1981-01-01

An anti-inflammatory and analgesic composition containing indomethacin and an H sub 1 or an H sub 2 histamine receptor antagonist in an amount sufficient to reduce gastric distress caused by the indomethacin is described. Usable antagonists include pyrilamine, promethazine, metiamide and cimetidine.

Dimenhydrinate overdose

MedlinePlus

... this page: //medlineplus.gov/ency/article/002634.htm Dimenhydrinate overdose To use the sharing features on this page, please enable JavaScript. Dimenhydrinate is a type of medicine called an antihistamine. ...

Treatment of the Hyperactive Child

ERIC Educational Resources Information Center

Wunderlich, Ray C.

1973-01-01

Described individually are the following forms of medical treatment for the hyperactive child: stimulants, tranquilizers, megavitamins, corticosteroids, antihistamines, anticonvulsants, food elimination, air filtration, allergic desensitization, perceptual motor training, and behavioral counseling. (DB)

21 CFR 522.2063 - Pyrilamine maleate injection.

Code of Federal Regulations, 2010 CFR

2010-04-01

...) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522... treating horses in conditions in which antihistaminic therapy may be expected to lead to alleviation of...

[Argentine guidelines for urticaria and angioedema].

PubMed

Máspero, Jorge; Cabrera, Hugo; Ardusso, Ledit; De Gennaro, Mónica; Fernández Bussy, Ramón; Galimany, José; Galimberti, Daniel; Label, Marcelo; La Forgia, Marta; Medina, Iris; Neffen, Hugo; Troielli, Patricia

2014-01-01

This interdisciplinary paper summarizes the news in the diagnosis and treatment of chronic urticaria (CU), and provides concepts, definitions and evidence-based suggestions for its management. Urticaria occurs in at least 20% of the population at some point in their lives. Acute urticaria (less than 6 weeks' duration), differs from CU in its etiology, but the onset of this disease is always acute. CU may occur as spontaneous (SCU) or induced (ICU). The diagnosis is simple, although a careful evaluation is necessary for differential diagnosis. ICU's diagnosis is mainly clinical, even if provocation tests can be useful. Supplementary studies should be limited and based on the clinical suspicion. Treatment may be divided into three approaches: avoidance, elimination or treatment of the cause, and pharmacological treatment. Recently treatment has been modified with the use of second-generation antihistamines as first-line and increased doses of nonsedating H1 antihistamines, up to 4 times, as second line. Antihistamines are essential to treat CU; however, 40% of patients do not achieve good control despite increased doses and require additional treatment. The most recent evidence indicates a group of drugs to be used as third line in these cases, to improve quality of life and to limit toxicity from frequent or chronic use of systemic steroids. Only 3 drugs are recommended as third line: omalizumab, cyclosporin A or anti-leukotrienes.

The Effect of Schinus terebinthifolius Raddi (Anacardiaceae) Bark Extract on Histamine-Induced Paw Edema and Ileum Smooth Muscle Contraction.

PubMed

Nunes-Neto, Paulo Alexandre; Peixoto-Sobrinho, Tadeu José da Silva; da Silva Júnior, Edilson Dantas; Leopoldina da Silva, Jamilka; Rodrigo da Silva Oliveira, Alisson; Pupo, André Sampaio; Araújo, Alice Valença; da Costa-Silva, João Henrique; Wanderley, Almir Gonçalves

2017-01-01

Schinus terebinthifolius Raddi (Anacardiaceae), popularly known as red aroeira, is used in traditional medicine to treat inflammatory, gastric, and respiratory disorders. The aim of this study was to evaluate the antihistaminic activity of S. terebinthifolius (St) bark extract by using in vivo and in vitro experimental models. The effects of St were investigated on contractions induced by histamine, carbachol, and potassium chloride in isolated guinea pig ileum. St was also studied in response to hind paw edema induced by histamine in rats. Experiments revealed that although St (250, 500, and 1,000  µ g/mL) reduced the histamine-induced contractions by 9.1 ± 1.8, 50.2 ± 2.0, and 68.9 ± 2.0%, respectively, it did not inhibit contractions induced by carbachol or KCl. The association of St (250 and 500  µ g/mL) with hydroxyzine, an H 1 -antihistamine (0.125 and 0.250  µ M), increased the inhibitory effect to 67.0 ± 3.2 and 85.1 ± 2.1%, respectively. Moreover, St (100, 200, and 400 mg/kg) decreased paw edema from its peak by 33.9, 48.4, and 54.8%, respectively, whereas hydroxyzine (70 mg/kg) inhibited the peak edema by 56.5%. Altogether, the results suggest that the bark extract of S. terebinthifolius has an antihistaminic effect (H 1 ).

The Effect of Schinus terebinthifolius Raddi (Anacardiaceae) Bark Extract on Histamine-Induced Paw Edema and Ileum Smooth Muscle Contraction

PubMed Central

Nunes-Neto, Paulo Alexandre; da Silva Júnior, Edilson Dantas; Leopoldina da Silva, Jamilka; Rodrigo da Silva Oliveira, Alisson; Pupo, André Sampaio; Araújo, Alice Valença

2017-01-01

Schinus terebinthifolius Raddi (Anacardiaceae), popularly known as red aroeira, is used in traditional medicine to treat inflammatory, gastric, and respiratory disorders. The aim of this study was to evaluate the antihistaminic activity of S. terebinthifolius (St) bark extract by using in vivo and in vitro experimental models. The effects of St were investigated on contractions induced by histamine, carbachol, and potassium chloride in isolated guinea pig ileum. St was also studied in response to hind paw edema induced by histamine in rats. Experiments revealed that although St (250, 500, and 1,000 µg/mL) reduced the histamine-induced contractions by 9.1 ± 1.8, 50.2 ± 2.0, and 68.9 ± 2.0%, respectively, it did not inhibit contractions induced by carbachol or KCl. The association of St (250 and 500 µg/mL) with hydroxyzine, an H1-antihistamine (0.125 and 0.250 µM), increased the inhibitory effect to 67.0 ± 3.2 and 85.1 ± 2.1%, respectively. Moreover, St (100, 200, and 400 mg/kg) decreased paw edema from its peak by 33.9, 48.4, and 54.8%, respectively, whereas hydroxyzine (70 mg/kg) inhibited the peak edema by 56.5%. Altogether, the results suggest that the bark extract of S. terebinthifolius has an antihistaminic effect (H1). PMID:28928787

Sedative Effects of Levocetirizine: A Systematic Review and Meta-Analysis of Randomized Controlled Studies.

PubMed

Snidvongs, Kornkiat; Seresirikachorn, Kachorn; Khattiyawittayakun, Likhit; Chitsuthipakorn, Wirach

2017-02-01

As a substrate of P-glycoprotein, levocetirizine should not cause sedative effects. However, while cetirizine, a mixture of levocetirizine and dextrocetirizine, can slightly penetrate the blood brain barrier, the sedative effects of levocetirizine are still under study. The aim of this study was to investigate the sedative effects of levocetirizine. An electronic literature search was performed using Medline and EMBASE from January 01, 2001 through August 6, 2015. Randomized controlled trials (RCTs) comparing levocetirizine with other antihistamines or placebo for patients with allergy and healthy subjects were selected. Primary outcome was risk ratio between levocetirizine and comparators. Secondary outcome was change in psychomotor speed. Data were pooled for meta-analysis using a fixed-effect model. Forty-eight studies of 18,014 patients met the inclusion criteria. When compared to placebo, levocetirizine produced modest sedative effects (RR: 1.67; 95% CI 1.17, 2.38). However, when compared to other second-generation antihistamines, sedative effects of levocetirizine did not differ (RR: 1.23; 95% CI 0.96, 1.58). In subgroup analysis, there was no difference between the sedative effects of levocetirizine and fexofenadine (RR: 1.7; 95% CI 0.59, 4.88), desloratadine (RR: 1.58; 95% CI 0.9, 2.77), loratadine (RR: 1.56; 95% CI 0.28, 8.56), bilastine (RR: 1.17; 95% CI 0.48, 2.84), olopatadine (RR: 1.09; 95% CI 0.81, 1.47), azelastine (RR: 0.19; 95% CI 0.01, 3.68) and rupatadine (RR: 1.47; 95% CI 0.14, 15.72). When compared to first-generation antihistamines, levocetirizine had less sedative effects and less change of reaction time (mean difference: -250.76 s; 95% CI -338.53, -162.98). Levocetirizine has modest sedative effects with a risk ratio of 1.67 when compared with placebo. The sedative effects observed for levocetirizine are not different from other second-generation antihistamines.

Don't Sweat the Small Stuff: Food Allergy Sufferer Lives a Cautious but Normal Life

MedlinePlus

... normal life Follow us Don’t Sweat the Small Stuff Food allergy sufferer lives a cautious but ... stings. The show recommended giving your child a small dose of antihistamine if you feared an allergic ...

Seasonal Allergies: Symptoms, Diagnosis, and Treatment | NIH MedlinePlus the Magazine

MedlinePlus

... for example, 6 weeks for ragweed or grass pollen seasons) Treatment Antihistamines Decongestants Nonsteroidal anti-inflammatory medicines ... things that you are allergic to, such as pollen, house dust mites, mold, pet dander, cockroaches Complications ...

Allergy Diagnosis and Treatment | NIH MedlinePlus the Magazine

MedlinePlus

... breathe is loaded with allergens, such as ragweed pollen. Various over-the-counter or prescription medications can ... for example, 6 weeks for ragweed or grass pollen seasons) Treatment Cold Airborne Allergy Antihistamines Decongestants Nonsteroidal ...

Olopatadine Nasal Spray

MedlinePlus

... medications called antihistamines. It works by blocking the effects of histamine, a substance in the body that ... to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in ...

Fexofenadine

MedlinePlus

... medications called antihistamines. It works by blocking the effects of histamine, a substance in the body that ... to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in ...

Lack of effects of astemizole on vestibular ocular reflex, motion sickness, and cognitive performance in man

NASA Technical Reports Server (NTRS)

Kohl, Randall L.; Homick, Jerry L.; Cintron, Nitza; Calkins, Dick S.

1987-01-01

Astemizole was orally administered to 20 subjects in a randomized, double-blind design to assess the efficacy of this peripherally active antihistamine as an antimotion sickness drug possessing no central side-effects. Measures of vestibular ocular reflex (VOR) were made to evaluate the agent as a selective vestibular depressant. Following one week of orally administered astemizole (30 mg daily), a Staircase Profile Test, a VOR test, and a variety of tests of cognitive performance were administered. These tests revealed no statistically significant effects of astemizole. This leads to the conclusion that, although the drug probably reaches the peripheral vestibular apparatus in man by crossing the blood-vestibular barrier, a selective peripheral antihistamine (H1) action is inadequate to control motion sickness induced through cross-coupled accelerative semicircular canal stimulation in a rotating chair.

Allergies and Hay Fever

MedlinePlus

... discomfort. Symptom control is most successful when multiple approaches are used together to manage the allergy. They may include reducing exposure to allergens, medications, and allergy shots or drops. If used properly, medications, including antihistamines, ...

Hey! A Brown Recluse Spider Bit Me!

MedlinePlus

... like antibiotics, antihistamines, or pain medicines. Rarely, a skin graft might be needed if the skin is really damaged at the area of the bite. (A skin graft is when a small amount of skin is ...

29 CFR Appendix A to Subpart T to... - Examples of Conditions Which May Restrict or Limit Exposure to Hyperbaric Conditions

Code of Federal Regulations, 2012 CFR

2012-07-01

... duration of isolation. History of seizure disorder other than early febrile convulsions. Malignancies... or drug use. Conditions requiring continuous medication for control (e.g., antihistamines, steroids, barbiturates, moodaltering drugs, or insulin). Meniere's disease. Hemoglobinopathies. Obstructive or...

29 CFR Appendix A to Subpart T of... - Examples of Conditions Which May Restrict or Limit Exposure to Hyperbaric Conditions

Code of Federal Regulations, 2013 CFR

2013-07-01

... duration of isolation. History of seizure disorder other than early febrile convulsions. Malignancies... or drug use. Conditions requiring continuous medication for control (e.g., antihistamines, steroids, barbiturates, moodaltering drugs, or insulin). Meniere's disease. Hemoglobinopathies. Obstructive or...

29 CFR Appendix A to Subpart T to... - Examples of Conditions Which May Restrict or Limit Exposure to Hyperbaric Conditions

Code of Federal Regulations, 2011 CFR

2011-07-01

... duration of isolation. History of seizure disorder other than early febrile convulsions. Malignancies... or drug use. Conditions requiring continuous medication for control (e.g., antihistamines, steroids, barbiturates, moodaltering drugs, or insulin). Meniere's disease. Hemoglobinopathies. Obstructive or...

29 CFR Appendix A to Subpart T of... - Examples of Conditions Which May Restrict or Limit Exposure to Hyperbaric Conditions

Code of Federal Regulations, 2014 CFR

2014-07-01

... duration of isolation. History of seizure disorder other than early febrile convulsions. Malignancies... or drug use. Conditions requiring continuous medication for control (e.g., antihistamines, steroids, barbiturates, moodaltering drugs, or insulin). Meniere's disease. Hemoglobinopathies. Obstructive or...

Multiple Myeloma: Patient Handbook

MedlinePlus

... incidence of deep vein thrombosis and pulmonar y embolism. • Patients must be pre-medicated with dexamethasone, antihistamine, ... foods that include processed sugars and artificial trans fats. Caution should be used in two areas: • Vitamin ...

29 CFR Appendix A to Subpart T to... - Examples of Conditions Which May Restrict or Limit Exposure to Hyperbaric Conditions

Code of Federal Regulations, 2010 CFR

2010-07-01

... duration of isolation. History of seizure disorder other than early febrile convulsions. Malignancies... or drug use. Conditions requiring continuous medication for control (e.g., antihistamines, steroids, barbiturates, moodaltering drugs, or insulin). Meniere's disease. Hemoglobinopathies. Obstructive or...

Dry Mouth Treatment: Tips for Controlling Dry Mouth

MedlinePlus

... Dry Mouth Mouthwash, which also offer protection against tooth decay. Avoid using over-the-counter antihistamines and decongestants ... and drinks because they increase your risk of tooth decay. Brush with a fluoride toothpaste — ask your dentist ...

Bronchiolitis - discharge

MedlinePlus

... bronchiolitis. Your health care provider may prescribe such medicine for your child. DO NOT give your child decongestant nose drops, antihistamines, or any other cold medicines unless your child's doctor tells you to. When to Call the ...

Role of bilastine in the management of allergic rhinitis and urticaria: an Asia-Pacific consensus statement

PubMed Central

Lee, Dennis Lip Yen; Abong, Jovilia; Siasoco, Bella; Chow, Steven KW; Leong, Jern-Lin; Singh, Harvinder; Kuljit, S; Campomanes, Benjamin

2016-01-01

The prevalence of allergic diseases is increasing globally, most particularly in middle- to low-income countries. This article examines the burden of allergic rhinitis and chronic urticaria in the Asia-Pacific region, unmet clinical needs, and the potential role of bilastine in the management of these conditions. An International Advisory Group meeting was convened in association with the Asian Pacific Society of Respirology Annual Congress in November 2014, followed by a literature review, and consensus-based outcomes from the meeting and literature review are described. Regional estimates of the prevalence of allergic rhinitis range from 10% to 50%, while little is known regarding the burden of urticaria in the Asia-Pacific region. A survey of allergy patients in the region identified fast, complete, and long-lasting symptom relief as the medication attributes most important to patients. International treatment guidelines for allergic rhinitis and urticaria advocate the first-line use of second-generation, no-sedating H1-antihistamines, such as bilastine, over their first-generation counterparts and a range of these agents are available to Asia-Pacific patients. The newer agents possess many of the properties of an "ideal" antihistamine (once daily administration, rapid and complete symptom relief, limited potential for drug-drug interactions, minimal side effects). The burgeoning prevalence of allergic diseases in the Asia-Pacific region and the uncontrolled symptoms that these patients experience demand a new antihistamine that offers the highest number of positive features according to the international guidelines. PMID:26844221

Role of bilastine in the management of allergic rhinitis and urticaria: an Asia-Pacific consensus statement.

PubMed

Mösges, Ralph; Lee, Dennis Lip Yen; Abong, Jovilia; Siasoco, Bella; Chow, Steven Kw; Leong, Jern-Lin; Singh, Harvinder; Kuljit, S; Campomanes, Benjamin

2016-01-01

The prevalence of allergic diseases is increasing globally, most particularly in middle- to low-income countries. This article examines the burden of allergic rhinitis and chronic urticaria in the Asia-Pacific region, unmet clinical needs, and the potential role of bilastine in the management of these conditions. An International Advisory Group meeting was convened in association with the Asian Pacific Society of Respirology Annual Congress in November 2014, followed by a literature review, and consensus-based outcomes from the meeting and literature review are described. Regional estimates of the prevalence of allergic rhinitis range from 10% to 50%, while little is known regarding the burden of urticaria in the Asia-Pacific region. A survey of allergy patients in the region identified fast, complete, and long-lasting symptom relief as the medication attributes most important to patients. International treatment guidelines for allergic rhinitis and urticaria advocate the first-line use of second-generation, no-sedating H1-antihistamines, such as bilastine, over their first-generation counterparts and a range of these agents are available to Asia-Pacific patients. The newer agents possess many of the properties of an "ideal" antihistamine (once daily administration, rapid and complete symptom relief, limited potential for drug-drug interactions, minimal side effects). The burgeoning prevalence of allergic diseases in the Asia-Pacific region and the uncontrolled symptoms that these patients experience demand a new antihistamine that offers the highest number of positive features according to the international guidelines.

Inappropriate prescription of cough remedies among children hospitalised with respiratory illness over the period 2002-2015 in Kenya.

PubMed

Maina, Michuki; Akech, Samuel; Mwaniki, Paul; Gachau, Susan; Ogero, Morris; Julius, Thomas; Ayieko, Phillip; Irimu, Grace; English, Mike

2017-03-01

To examine trends in prescription of cough medicines over the period 2002-2015 in children aged 1 month to 12 years admitted to Kenyan hospitals with cough, difficulty breathing or diagnosed with a respiratory tract infection. We reviewed hospitalisation records of children included in four studies providing cross-sectional prevalence estimates from government hospitals for six time periods between 2002 and 2015. Children with an atopic illness were excluded. Amongst eligible children, we determined the proportion prescribed any adjuvant medication for cough. Active ingredients in these medicines were often multiple and were classified into five categories: antihistamines, antitussives, mucolytics/expectorants, decongestants and bronchodilators. From late 2006, guidelines discouraging cough medicine use have been widely disseminated and in 2009 national directives to decrease cough medicine use were issued. Across the studies, 17 963 children were eligible. Their median age and length of hospital stay were comparable. The proportion of children who received cough medicines shrank across the surveys: approximately 6% [95% CI: 5.4, 6.6] of children had a prescription in 2015 vs. 40% [95% CI: 35.5, 45.6] in 2002. The most common active ingredients were antihistamines and bronchodilators. The relative proportion that included antihistamines has increased over time. There has been an overall decline in the use of cough medicines among hospitalised children over time. This decline has been associated with educational, policy and mass media interventions. © 2016 The Authors. Tropical Medicine & International Health Published by John Wiley & Sons Ltd.

The history and progression of treatments for allergic rhinitis.

PubMed

Ostrom, Nancy K

2014-01-01

This article intends to place new treatments in the context of allergic rhinitis (AR) treatment history. The medical literature was searched for significant advances and changes in AR treatment. Historical data on AR treatment options and management were selected. Reviews of AR management published throughout the 20th century were included to provide context for treatment advances. Modern AR treatment began in the early 20th century with immunotherapy and was soon followed by the emergence of antihistamine therapy in the 1930s. Numerous treatments for AR have been used over the ensuing decades, including decongestants, mast cell stabilizers, and leukotriene receptor antagonists. Topical corticosteroid options were developed the 1950s, and, added to baseline antihistamine therapy, became the foundation of AR treatment. Treatment options were significantly impacted after the 1987 Montreal Protocol, which phased out the use of chlorofluorocarbon propellant aerosols because of environmental concerns. From the mid-1990s until recently, this left only aqueous solution options for intranasal corticosteroids (INSs). The approval of the first hydrofluoroalkane propellant aerosol INSs for AR in 2012 restored a "dry" aerosol treatment option. The first combination intranasal antihistamine/INSs was also approved in 2012, providing a novel treatment option for AR. Treatment of AR has progressed with new therapeutic options now available. This should continue to move forward with agents to alter the allergic mechanism itself and impact the disease burden that has a significant impact on patient outcomes.

21 CFR 522.2615 - Tripelennamine hydrochloride injection.

Code of Federal Regulations, 2013 CFR

2013-04-01

... use—(1) Amount—(i) Dogs, cats, and horses. For intramuscular use only at a dose of 0.5 milligram per... antihistaminic therapy may be expected to lead to alleviation of some signs of disease. (3) Limitations. Do not...

21 CFR 522.2615 - Tripelennamine hydrochloride injection.

Code of Federal Regulations, 2012 CFR

2012-04-01

... use—(1) Amount—(i) Dogs, cats, and horses. For intramuscular use only at a dose of 0.5 milligram per... antihistaminic therapy may be expected to lead to alleviation of some signs of disease. (3) Limitations. Do not...

Snoring and Nasal Congestion

MedlinePlus

... treat the various causes of nasal congestion include: Topical nasal steroid spray Topical nasal antihistamine spray Oral antibiotic (in case of ... include more than just the decrease in oxygen levels at night during the apnea episodes. They also ...

Suppression of reactions to certain cosmetics.

PubMed

Fisher, A A

1977-08-01

Reactions to hair dyes and bleaches may be "suppressed" with corticosteroids and antihistamines. Reactions to nail polish may be prevented by a "drying" or "polymerizing" technique. Sensitization to certain perfume ingredients may be inhibited by a "quenching" phenomenon.

Cholinergic urticaria with anaphylaxis: hazardous duty of a deployed US marine.

PubMed

Handfield, Kent S; Dolan, Christopher K; Kaplan, Michael

2015-04-01

Cholinergic urticaria (CU) is triggered by a rise in body temperature and can be complicated by bronchial hyperresponsiveness and anaphylaxis. It primarily affects young adults who actively engage in strenuous exercise, such as servicemen and servicewomen. If the patient reports a history of wheezing or difficulty breathing with urticaria, a water challenge test in a warm bath can be performed to confirm the presence of anaphylaxis. The test should be conducted in an environment in which the patient's airway can be secured and epinephrine can be administered if necessary. Nonsedating antihistamines commonly are used to treat CU, but few other treatments have been thoroughly evaluated for cases that are refractory to antihistamines. We present the case of a 27-year-old US Marine with CU and anaphylaxis confirmed by a water challenge test in a warm bath.

Physiological recording from pilots operating an aircraft simulator.

DOT National Transportation Integrated Search

1964-09-01

The questions to be answered were reduced to the following : (1) to determine whether or not theraputic doses of two common drugs, a tranquilizer and an antihistamine, cause decrements in the operating proficiency of pilots, and (2) do those drugs wh...

A Forehead-Mounted Measure of O2 Saturation: The Potential for in Cockpit Hypoxia Early Detection and Warning

DTIC Science & Technology

2010-07-09

past 24 hours. (circle all that apply) a. None b. Sedatives/Tranquilizers c. Aspirin/ Tylenol /any analgesic d. Antihistamines...e. Decongestants f. Other (please specify) 6. Do you take any over the counter medications (e.g., antacids, Benadryl, Tylenol , etc

Indometh acin-antihistamine combination for gastric ulceration control

NASA Technical Reports Server (NTRS)

Brown, P. A.; Vernikos, J. (Inventor)

1980-01-01

An anti-inflammatory and analgesic composition containing indomethacin and an H2 histamine receptor antagonist in an amount sufficient to reduce gastric distress caused by the indomethacin was developed. Usable antagonists are metiamide and cimetidine.

Efficacy and safety of desloratadine/pseudoephedrine combination vs its components in seasonal allergic rhinitis.

PubMed

Grubbe, R E; Lumry, W R; Anolik, R

2009-01-01

Antihistamines are first-line therapy for the treatment of seasonal allergic rhinitis (AR); however, an oral decongestant is often added to improve control of nasal congestion. To examine whether a tablet combining the nonsedating antihistamine desloratadine and the decongestant pseudoephedrine was more effective than either drug administered alone in reducing the symptoms of seasonal AR, including nasal congestion. In this multicenter, double-blind study, participants (N = 598) with symptomatic seasonal AR were administered either a combination tablet of desloratadine 2.5 mg/pseudoephedrine 120 mg (DL/PSE) bid, a desloratadine 5.0 mg qd and a placebo tablet, or pseudoephedrine 120 mg bid. Participants assessed their symptom severity twice daily over the 2-week treatment period. The primary variable to assess the effects of the antihistamine component--mean change from baseline in average AM/PM reflective total symptom score (TSS), excluding nasal congestion--was significantly greater (-6.54) for DL/PSE than for desloratadine (-5.09) or pseudoephedrine (-5.07) monotherapy (P < .001 for both). The primary variable to assess the effects of the decongestant component--mean change from baseline in average AM/PM reflective nasal congestion score--was also significantly greater (-0.93) for DL/PSE than for desloratadine (-0.66) or pseudoephedrine (-0.75) (P < .001 vs desloratadine; P = .006 vs pseudoephedrine). This study demonstrated that DL/PSE therapy was more effective in reducing symptoms of seasonal AR, including nasal congestion, than the individual components when administered alone, thus supporting use of this combination in participants with symptomatic seasonal AR and prominent nasal congestion.

Evidence-based guidelines for anti-allergic drug withdrawal times before allergen-specific intradermal and IgE serological tests in dogs.

PubMed

Olivry, Thierry; Saridomichelakis, Manolis

2013-04-01

Anti-allergic drugs (e.g. antihistamines, glucocorticoids and ciclosporin) are often administered to dogs with atopic dermatitis to relieve pruritus and skin lesions. Allergen-specific intradermal tests (IDT) and allergen-specific IgE serological (ASIS) tests are used to characterize the allergens to which dogs are hypersensitive. Anti-allergic drugs have the potential to influence the results or interpretation of these tests. To provide evidence-based recommendations for anti-allergic drug withdrawal times before IDT and ASIS tests. Three citation databases and abstracts from international meetings were searched for relevant studies. Studies were grouped based on similar interventions and types of tests. Withdrawal times for each type of drug and test were then extrapolated from the study results. Before the assessment of immediate reactions to IDT, proposed optimal withdrawal times for antihistamines, oral glucocorticoids, topical/otic glucocorticoids and ciclosporin are 7, 14, 14 and 0 days, respectively. Studies have provided no evidence for drug withdrawal prior to ASIS tests for oral ciclosporin or prednisone/prednisolone. Owing to a lack of studies, recommendations for withdrawal times before ASIS tests cannot be made for topical glucocorticoids and antihistamines. These proposed withdrawal times are based on the existing evidence at the end of 2011. Care must be taken before extrapolating the suggested withdrawal times to other species, higher dosages, different formulations and/or durations of administration of tested drugs, as well as to other medications from the same category. © 2013 The Authors. Veterinary Dermatology © 2013 ESVD and ACVD.

Efficacy of Armodafinil for Maintaining Vigilance Among Navy Air Traffic Controllers Eight to Twelve Hours Post-Dose

DTIC Science & Technology

2009-04-12

circle all that apply) a. None b. Sedatives/Tranquilizers c. Aspirin/ Tylenol /any analgesic 31 d. Antihistamines e. Decongestants f. Other (please specify...4. Do you take any over the counter medications (e.g., antacids, Benadryl, Tylenol , etc.) two (2) or more times a month

77 FR 4758 - Foreign-Trade Zone 59-Lincoln, Nebraska, Application for Temporary/Interim Manufacturing...

Federal Register 2010, 2011, 2012, 2013, 2014

2012-01-31

... authority to produce over-the-counter (OTC) pharmaceutical products, such as analgesics, cough/cold medicine, antihistamines/decongestants, and penicillin-based antibiotics (HTSUS 3004.10, 3004.40, 3004.90--duty free). Foreign ingredients that would be used in production (representing 25% of the value of the finished...

Lesson of the month 2: The limitations of steroid therapy in bradykinin-mediated angioedema attacks.

PubMed

Ismail, Sharif; Cheng, Leo; Grigoriadou, Sofia; Laffan, James; Menon, Manoj

2015-02-01

Acute angioedema attacks are conventionally treated with antihistamines and steroids, in line with a presumed mechanism of disease involving overwhelming mast-cell degranulation. This approach overlooks a small but important minority of cases in which attacks are bradykinin driven and exhibit poor responsiveness to steroid or anti-histamine therapy. These patients may have a family history of angioedema (hereditary angioedema), or a past medical history including B-cell lymphoproliferative disorders or autoimmune disease (acquired angioedema). Rather than steroid therapy, they respond to administration of a bradykinin inhibitor, or more commonly, a C1 esterase inhibitor substitute, to control acute symptoms and reduce the probability of invasive airway insertion. In the long-term, they require C1 esterase inhibitor sparing therapy and a treat-the-cause approach to reduce the risk of recurrent attacks. We present here a case of a middle-aged woman who presented with recurrent angioedema of initially uncertain aetiology. © 2015 Royal College of Physicians.

Eye itching in ophthalmology and its treatment.

PubMed

Mikuni, I

1984-12-01

Itching in the field of ophthalmology is detailed in its physiopathology and a few other aspects were described. The therapeutic modalities which have been practiced are explained. In addition to steroids and antihistaminics which are commonly used, INTAL and others, suppressors of chemical transmitter substance release, are described.

Academic Functioning and Quality of Life of Children and Adolescents with Allergic Rhinitis--Part II

ERIC Educational Resources Information Center

McCabe, Paul C.

2008-01-01

This article is the second of a two-part series on allergic rhinitis (AR). Treatments for AR are now widely available in both prescription and over-the-counter form. The medication therapies include antihistamines, decongestants, leukotriene receptor antagonists, cromolyn sodium, and immunotherapy. Corticosteroids are also used via nasal…

Use of cough and cold preparations during breastfeeding.

PubMed

Mitchell, J L

1999-12-01

Adverse reactions in infants from maternal drug ingestion depend largely on the amount of milk consumed by the infant, timing of breastfeeding in relation to dosing, dose of the medication, dosing interval, and duration of therapy. When taking medications, breastfeeding mothers should be instructed to take their medication after breastfeeding, at the lowest effective dose and for the shortest duration. Overall, there are few data from human studies on the use of antihistamines, decongestants, and cough products during breastfeeding. Studies of pseudoephedrine, triprolidine, and loratadine in humans conclude that low levels of each drug would reach a breastfed infant. Since triprolidine and pseudoephedrine are also considered compatible with breastfeeding by the AAP, these 2 drugs should be the first-line choices. Codeine is considered compatible with breastfeeding by the AAP, and would be an acceptable choice for short-term use as a cough suppressant. It is important to note that many of the liquid cough and cold products contain alcohol. In addition, many of the combination products are a mixture of an antihistamine and a decongestant and may also contain aspirin, acetaminophen, ibuprofen, or caffeine. It is preferable for nursing mothers to only take medications that are necessary and to avoid such combination products. The AAP considers alcohol, acetaminophen, ibuprofen, and caffeine compatible with breastfeeding. Aspirin has been associated with significant negative effects on some nursing infants, and the AAP recommends giving aspirin to nursing mothers with caution. Mothers taking cough and cold products should watch for adverse events in their breastfed infants. Infants may experience paradoxical central nervous stimulation from antihistamines and irritability and insomnia from decongestants.

In vivo antimuscarinic actions of the third generation antihistaminergic agent, desloratadine.

PubMed

Howell, G; West, L; Jenkins, C; Lineberry, B; Yokum, D; Rockhold, R

2005-08-18

Muscarinic receptor mediated adverse effects, such as sedation and xerostomia, significantly hinder the therapeutic usefulness of first generation antihistamines. Therefore, second and third generation antihistamines which effectively antagonize the H1 receptor without significant affinity for muscarinic receptors have been developed. However, both in vitro and in vivo experimentation indicates that the third generation antihistamine, desloratadine, antagonizes muscarinic receptors. To fully examine the in vivo antimuscarinic efficacy of desloratadine, two murine and two rat models were utilized. The murine models sought to determine the efficacy of desloratadine to antagonize muscarinic agonist induced salivation, lacrimation, and tremor. Desloratadine's effect on the cardiovascular system was explored in both rodent models. In the pithed rat, both desloratadine (1.0 mg/kg, i.v.) and the muscarinic M2 selective antagonist, methoctramine (0.5 mg/kg, i.v.), inhibited negative inotropic (left ventricular dP/dt) effects caused by oxotremorine, a nonselective muscarinic agonist (p < 0.05). Negative chronotropic effects caused by oxotremorine were inhibited by desloratadine, methoctramine, and the muscarinic M3 selective antagonist, 4-DAMP (1.0 mg/kg, i.v.). A late positive inotropic event observed after the initial decrease was inhibited by all three test compounds with desloratadine and 4-DAMP being the most efficacious. In the conscious animal, inhibition of baroreflex-mediated bradycardia was evaluated. Unlike atropine (0.5 mg/kg, i.v.), desloratadine did not alter this bradycardia. The antimuscarinic action of desloratadine on salivation, lacrimation, and tremor was also explored. In urethane-anesthetized (1.5 g/kg, i.p.) male ICR mice (25-35 g) desloratadine (1.0, 5.0 mg/kg) did not inhibit oxotremorine-induced (0.5 mg/kg, s.c.) salivation, unlike atropine (0.5 mg/kg) and 4-DAMP (1.0 mg/kg). In conscious mice, desloratadine failed to inhibit oxotremorine

21 CFR 341.72 - Labeling of antihistamine drug products.

Code of Federal Regulations, 2010 CFR

2010-04-01

... of the following: “relieves,” “alleviates,” “decreases,” “reduces,” or “dries”) “runny nose and... the nose or throat, and itchy, watery eyes due to hay fever” (which may be followed by one or both of... temporary relief of runny nose, sneezing, itching of the nose or throat, and itchy, watery eyes due to hay...

21 CFR 341.72 - Labeling of antihistamine drug products.

Code of Federal Regulations, 2011 CFR

2011-04-01

... of the following: “relieves,” “alleviates,” “decreases,” “reduces,” or “dries”) “runny nose and... the nose or throat, and itchy, watery eyes due to hay fever” (which may be followed by one or both of... temporary relief of runny nose, sneezing, itching of the nose or throat, and itchy, watery eyes due to hay...

21 CFR 341.72 - Labeling of antihistamine drug products.

Code of Federal Regulations, 2013 CFR

2013-04-01

... of the following: “relieves,” “alleviates,” “decreases,” “reduces,” or “dries”) “runny nose and... the nose or throat, and itchy, watery eyes due to hay fever” (which may be followed by one or both of... temporary relief of runny nose, sneezing, itching of the nose or throat, and itchy, watery eyes due to hay...

21 CFR 341.72 - Labeling of antihistamine drug products.

Code of Federal Regulations, 2012 CFR

2012-04-01

... of the following: “relieves,” “alleviates,” “decreases,” “reduces,” or “dries”) “runny nose and... the nose or throat, and itchy, watery eyes due to hay fever” (which may be followed by one or both of... temporary relief of runny nose, sneezing, itching of the nose or throat, and itchy, watery eyes due to hay...

21 CFR 341.72 - Labeling of antihistamine drug products.

Code of Federal Regulations, 2014 CFR

2014-04-01

... of the following: “relieves,” “alleviates,” “decreases,” “reduces,” or “dries”) “runny nose and... the nose or throat, and itchy, watery eyes due to hay fever” (which may be followed by one or both of... temporary relief of runny nose, sneezing, itching of the nose or throat, and itchy, watery eyes due to hay...

The antihistamine diphenhydramine is demethylated by anaerobic wastewater microorganisms.

PubMed

Wolfson, Sarah J; Porter, Abigail W; Villani, Thomas S; Simon, James E; Young, Lily Y

2018-07-01

While emerging pharmaceutical contaminants are monitored in wastewater treatment and the environment, there is little information concerning their microbial metabolites. The transformation of diphenhydramine by microorganisms in anaerobic digester sludge was investigated using anaerobic cultures amended with 1 mM diphenhydramine as the sole carbon source. Complete transformation of the parent compound to a persistent metabolite occurred within 191 days. Using GC/MS analysis, the metabolite was identified as N-desmethyl diphenhydramine. Loss of the parent compound diphenhydramine followed a first order rate constant of 0.013 day -1 . There was no observed decrease in metabolite concentration even after a further 12 months of incubation, suggesting that the metabolite resists further degradation during wastewater treatment. Bacterial community diversity in the diphenhydramine transforming assay cultures showed enrichment in Comamonadaceae, Symbiobacteriaceae, Anaerolineaceae, and Prevotellaceae relative to unamended background controls. An anaerobic toxicity assay demonstrated that diphenhydramine has an inhibitory effect on both fermentative bacteria and methanogenic archaea in the wastewater community. In contrast, the metabolite N-desmethyl diphenhydramine partially suppressed methanogens but did not impact the fermenting community. To our knowledge, this is the first report of diphenhydramine metabolism by a bacterial community. The limited transformation of diphenhydramine by wastewater microorganisms indicates that N-desmethyl diphenhydramine will enter the environment along with unmetabolized diphenhydramine. Copyright © 2018 Elsevier Ltd. All rights reserved.

New H1/H3 antagonists for treating allergic rhinitis: WO2010094643.

PubMed

Norman, Peter

2011-03-01

This application claims dual receptor specificity antihistamines, active as H(1) and H(3) antagonists, which additionally have a long duration of action that renders them suitable for once daily administration via inhalation for the treatment of allergic rhinitis. The compounds lack CNS penetration and have a high affinity for both histamine receptors.

Palonosetron and Hydroxyzine Pre-treatment Reduces the Objective Signs of Experimentally-Induced Acute Opioid Withdrawal in Humans: A Double-Blinded, Randomized, Placebo-Controlled Crossover Study

PubMed Central

Erlendson, Matthew; D'Arcy, Nicole; Encisco, Ellen; Yu, Jeff; Rincon-Cruz, Lorena; Peltz, Gary; Clark, J. David

2017-01-01

Background Treatments for reducing opioid withdrawal are limited and prone to problematic side effects. Laboratory studies, clinical observations, and limited human trial data suggest 5-HT3-receptor antagonists and antihistamines may be effective. Objectives This double-blind, crossover, placebo-controlled study employing an acute physical dependence model evaluated whether (i) treatment with a 5-HT3-receptor antagonist (palonosetron) would reduce opioid withdrawal symptoms, and (ii) co-administration of an antihistamine (hydroxyzine) would enhance any treatment effect. Methods At timepoint T=0, healthy (non-opioid dependent, non-substance abuser) male volunteers (N=10) were pre-treated with either a) placebo, b) palonosetron IV (0.75 mg), or c) palonosetron IV (0.75 mg) and hydroxyzine PO (100 mg) in a crossover study design. This was followed at T=30 by intravenous morphine (10mg/70kg). At T=165, 10mg/70kg naloxone IV was given to precipitate opioid withdrawal. The objective opioid withdrawal score (OOWS) and subjective opioid withdrawal score (SOWS) were determined 5 and 15 minutes after naloxone administration (T=170, 180, respectively). Baseline measurements were recorded at T=-30 and T=-15. Results Comparison of average baseline OOWS scores with OOWS scores obtained fifteen minutes after naloxone was significant (p=0.0001). Scores from fifteen minutes post-naloxone infusion showed significant differences in OOWS scores between treatment groups: placebo, 3.7 ± 2.4; palonosetron, 1.5± 0.97; and palonosetron with hydroxyzine, 0.2 ± .1333. Conclusions Pretreatment with palonosetron significantly reduced many signs of experimental-induced opioid withdrawal. Co-administration with hydroxyzine further reduced opioid withdrawal severity. These results suggest that 5-HT3 receptor antagonists, alone or in combination with an antihistamine, may be useful in the treatment of opioid withdrawal. PMID:27712113

Randomised controlled trial of butterbur and cetirizine for treating seasonal allergic rhinitis

PubMed Central

Schapowal, Andreas

2002-01-01

Objectives To compare the efficacy and tolerability of butterbur (Petasites hybridus) with cetirizine in patients with seasonal allergic rhinitis (hay fever). Design Randomised, double blind, parallel group comparison. Setting Four outpatient general medicine and allergy clinics in Switzerland and Germany. Participants 131 patients were screened for seasonal allergic rhinitis and 125 patients were randomised (butterbur 61; cetirizine 64). Interventions Butterbur (carbon dioxide extract tablets, ZE 339) one tablet, four times daily, or cetirizine, one tablet in the evening, both given for two consecutive weeks. Main outcome measures Scores on SF-36 questionnaire and clinical global impression scale. Results Improvement in SF-36 score was similar in the two treatment groups for all items tested hierarchically. Butterbur and cetirizine were also similarly effective with regard to global improvement scores on the clinical global impression scale (median score 3 in both groups). Both treatments were well tolerated. In the cetirizine group, two thirds (8/12) of reported adverse events were associated with sedative effects (drowsiness and fatigue) despite the drug being considered a non-sedating antihistamine. Conclusions The effects of butterbur are similar to those of cetirizine in patients with seasonal allergic rhinitis when evaluated blindly by patients and doctors. Butterbur should be considered for treating seasonal allergic rhinitis when the sedative effects of antihistamines need to be avoided. What is already known on this topicSeasonal allergic rhinitis (hay fever) is common in countries with temperate climates.Most patients have their symptoms treated for short periods, particularly during peaks in atmospheric pollen countWhat this study addsAfter two weeks, the effects of butterbur and cetirizine were comparable in patients with hay feverButterbur produced fewer sedating effects than cetirizineButterbur should be considered when the sedating effects of

Prevalence and Clinical Characteristics of Chronic Spontaneous Urticaria in Pediatric Patients.

PubMed

Balp, Maria-Magdalena; Weller, Karsten; Carboni, Veruska; Chirilov, Alexandra; Papavassilis, Charis; Severin, Thomas; Tian, Haijun; Zuberbier, Torsten; Maurer, Marcus

2018-04-21

Data on the prevalence and disease management of chronic urticaria (CU) and chronic spontaneous urticaria (CSU) in the pediatric population are scarce. The present study assessed the prevalence of CU and CSU, and disease management among pediatric patients (0-17 years). A physician-based online survey was conducted in 5 European countries (United Kingdom, Germany, Italy, France, and Spain) assessing the annual diagnosed prevalence, disease characteristics and treatment patterns in the target population. Results are based on physician responses and analyzed using descriptive statistics. Prevalence estimates were calculated based on the number of CU/CSU pediatric patients seen, treated and referred by the respondents and extrapolated to the total pediatric population from each country. Across 5 European countries, the one-year diagnosed prevalence of CU and CSU in pediatric patients was 1.38% (95% CI, 0.94-1.86) and 0.75% (95% CI, 0.44-1.08), respectively. Angioedema was reported in 6%-14% of patients. A large proportion of CSU pediatric patients (40%-60%) were treated with H1-antihistamines at approved dose and 16% to 51% received H1-antihistamines at higher doses. Approximately 1/3 of pediatric CSU patients remained uncontrolled with H1- antihistamines at approved/higher doses. Other prescribed treatments were oral corticosteroids (10% to 28%) and topical creams (15% to 26%). This study revealed a prevalence of CSU among pediatric population comparable to adults and also suggested an unmet need for approved treatments for inadequately-controlled pediatric CSU patients. It is truly of concern that harmful (oral steroids) or insufficient (topical creams) treatments were frequently used despite of better and guideline recommended alternatives. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

A new class of nitric oxide-releasing derivatives of cetirizine; pharmacological profile in vascular and airway smooth muscle preparations

PubMed Central

Larsson, A-K; Fumagalli, F; DiGennaro, A; Andersson, M; Lundberg, J; Edenius, C; Govoni, M; Monopoli, A; Sala, A; Dahlén, S-E; Folco, G C

2007-01-01

Background and purpose: The pharmacological properties of compounds NCX 1512 and NCX 1514, synthesized by linking the histamine H1-receptor antagonist cetirizine to NO-releasing spacer groups, are reported. The aim was to establish if the compounds retained the antihistamine action of the parent compound, to assess their efficacy as NO donors and to test if they had broader antiallergic activity than cetirizine in the lung. Experimental approach: Antihistamine activity of NCX 1512 and NCX 1514 was investigated in vitro in the guinea pig ileum, in tracheal rings (GPTR) and lung parenchymal strips (GPLP) of the guinea-pig. The NO-releasing capacity was investigated in vascular preparations; the isolated rabbit and guinea-pig aorta and guinea-pig pulmonary artery. Kinetics of NO release were assessed in a rat whole blood assay. Key results: Both NCX 1512 and NCX 1514 retained activity as H1-receptor antagonists in the guinea pig ileum and airway preparations. The NO-releasing NCX compounds relaxed the rabbit aorta, an action prevented by the guanylyl cyclase inhibitor ODQ (10 μM). NCX 1512 and NCX 1514 did not relax the antigen (ovalbumin) pre-contracted GPTR, whereas the NO donors NCX 2057 and DEA-NONOate relaxed guinea-pig pre-contracted vascular and tracheal preparations. Cetirizine (1–100 μM) and NCX 1512 (1–100 μM) reduced the cumulative (0.01–100 μg ml−1) ovalbumin-induced constriction in GPTR, but had no significant effect in GPLP. Conclusions and implications: NCX 1512 and NCX 1514 act as antihistamines and NO donors. However, there was no improved effect compared to cetirizine on antigen-induced constriction of the central and peripheral lung. PMID:17351654

Pilots using selective serotonin reuptake inhibitors compared to other fatally injured pilots.

PubMed

Rogers, Paul; Hileman, Christy; Salazar, Guillermo; Cliburn, Kacey; Paskoff, Lawrence; Hathaway, William; Gildea, Kevin; Tejera Villalaz, Victor Hugo

2017-10-01

Selective Serotonin Reuptake Inhibitors (SSRI) were a disqualifying medication for U.S. civil pilots before April 5, 2010. After this date, a Federal Aviation Administration policy was created that allowed airmen, on select SSRIs, a pathway to hold a valid medical certificate. The purpose of this study was to provide a detailed look at SSRIs in the U.S. pilot population since the inception of this new policy. We examined the toxicology results from fatally injured airmen in addition to outcomes concerning pilots who are participating in the program. This study examined data from the Civil Aerospace Medical Institute's Bioaeronautical Sciences Research Laboratory in conjunction with the Medical Analysis Tracking Registry and the Document Imaging and Workflow System. A count-based regression model quantified the relationships between positive SSRI findings with additional factors of interest. These factors included pilot rating, ethanol, and first generation antihistamines. There were 1484 fatally injured airmen over the six year study period, of which 44-tested positive for an SSRI. First-generation antihistamines were statistically associated with positive findings of SSRIs. Published by Elsevier Ltd.

Histamine H1 receptor antagonist cetirizine impairs working memory processing speed, but not episodic memory.

PubMed

van Ruitenbeek, P; Vermeeren, A; Riedel, W J

2010-09-01

The histaminergic neurotransmitter system is currently under investigation as a target for drug treatment of cognitive deficits in clinical disorders. The therapeutic potential of new drugs may initially be screened using a model of histaminergic dysfunction, for example, as associated with the use of centrally active antihistamines. Of the selective second generation antihistamines, cetirizine has been found to have central nervous system effects. The aim of the present study was to determine whether cetirizine can be used as a tool to model cognitive deficits associated with histaminergic hypofunction. The study was conducted according to a three-way, double-blind, cross-over design. Treatments were single oral doses of cetirizine 10 and 20 mg and placebo. Effects on cognition were assessed using tests of word learning, memory scanning, vigilance, divided attention, tracking and visual information processing speed. Cetirizine 10 mg impaired tracking performance and both doses impaired memory scanning speed. None of the other measures indicated impaired performance. Cetirizine affects information processing speed, but these effects were not sufficient to serve as a model for cognitive deficits in clinical disorders.

Fatal overdose from Bendectin.

PubMed

Bayley, M; Walsh, F M; Valaske, M J

1975-05-01

A three-year old male ingested approximately 100 tablets of Bendectin. He developed tonic-clonic seizures followed by cardiac arrest. Toxicologic analysis yielded high levels of doxylamine, dicyclomine, and pyridoxine in blood, peritoneal fluid, and tissue homogenates. The antihistamine, doxylamine succinate appears to be the toxic constituent. Analytical methods used to document the case are herein described.

A Comparison of Health Care Resource Utilization and Costs for Patients with Allergic Rhinitis on Single-Product or Free-Combination Therapy of Intranasal Steroids and Intranasal Antihistamines.

PubMed

Harrow, Brooke; Sedaghat, Ahmad R; Caldwell-Tarr, Amanda; Dufour, Robert

2016-12-01

Allergic rhinitis (AR) is a common condition that can be treated with a number of different therapies. Treatments such as intranasal antihistamines (INAs) and intranasal steroids (INSs) are widely used by AR patients. For some allergy sufferers, a combination of therapies, specifically an INA and an INS, is required to address their symptoms. A new treatment, the formulation of azelastine hydrochloride and fluticasone pro-pionate used as a single spray (MP-AzeFlu), has become available for AR patients who need both types of treatment. In this regard, the comparison with the alternative concomitant use of INAs and INSs is of interest. The current study examines the health care resource utilization and costs for each cohort. To examine the resource utilization and costs associated with AR for patients treated with MP-AzeFlu or concurrent therapy with single-ingredient INA and INS sprays (free-combination therapy). A retrospective administrative claims study for commercially insured patients from a large U.S. health plan was performed. Patients with an AR diagnosis and a prescription claim for MP-AzeFlu or free-combination therapy between September 1, 2012, and September 30, 2013, were identified. Patients were aged at least 12 years at index date (first prescription fill for intranasal therapy) and were required to have 12 months pre-index and 6 months post-index of continuous enrollment. Health care resource utilization and costs were assessed for the post-index period. The cohorts were adjusted on baseline demographic and clinical characteristics using inverse propensity treatment weights. Other covariates, prescriber specialty, product switching during the post-index period, and pre-index total costs were included in the regression models measuring outcomes. One clinical characteristic of interest was the presence of asthma as comorbidity. A subset analysis of AR patients with asthma was also performed. All-cause-related pharmacy fills as well as pharmacy, medical

In vivo antimuscarinic actions of the third generation antihistaminergic agent, desloratadine

PubMed Central

Howell, G; West, L; Jenkins, C; Lineberry, B; Yokum, D; Rockhold, R

2005-01-01

Background Muscarinic receptor mediated adverse effects, such as sedation and xerostomia, significantly hinder the therapeutic usefulness of first generation antihistamines. Therefore, second and third generation antihistamines which effectively antagonize the H1 receptor without significant affinity for muscarinic receptors have been developed. However, both in vitro and in vivo experimentation indicates that the third generation antihistamine, desloratadine, antagonizes muscarinic receptors. To fully examine the in vivo antimuscarinic efficacy of desloratadine, two murine and two rat models were utilized. The murine models sought to determine the efficacy of desloratadine to antagonize muscarinic agonist induced salivation, lacrimation, and tremor. Desloratadine's effect on the cardiovascular system was explored in both rodent models. Results In the pithed rat, both desloratadine (1.0 mg/kg, i.v.) and the muscarinic M2 selective antagonist, methoctramine (0.5 mg/kg, i.v.), inhibited negative inotropic (left ventricular dP/dt) effects caused by oxotremorine, a nonselective muscarinic agonist (p < 0.05). Negative chronotropic effects caused by oxotremorine were inhibited by desloratadine, methoctramine, and the muscarinic M3 selective antagonist, 4-DAMP (1.0 mg/kg, i.v.). A late positive inotropic event observed after the initial decrease was inhibited by all three test compounds with desloratadine and 4-DAMP being the most efficacious. In the conscious animal, inhibition of baroreflex-mediated bradycardia was evaluated. Unlike atropine (0.5 mg/kg, i.v.), desloratadine did not alter this bradycardia. The antimuscarinic action of desloratadine on salivation, lacrimation, and tremor was also explored. In urethane-anesthetized (1.5 g/kg, i.p.) male ICR mice (25–35 g) desloratadine (1.0, 5.0 mg/kg) did not inhibit oxotremorine-induced (0.5 mg/kg, s.c.) salivation, unlike atropine (0.5 mg/kg) and 4-DAMP (1.0 mg/kg). In conscious mice, desloratadine failed to inhibit

Safety profile of bilastine: 2nd generation H1-antihistamines.

PubMed

Scaglione, F

2012-12-01

Bilastine is a new H1 antagonist with no sedative side effects, no cardiotoxic effects, and no hepatic metabolism. In addition, bilastine has proved to be effective for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. Pharmacological studies have shown that bilastine is highly selective for the H1 receptor in both in vivo and in vitro studies, and with no apparent affinity for other receptors. The absorption of bilastine is fast, linear and dose-proportional; it appears to be safe and well tolerated at all doses levels in healthy population. Multiple administration of bilastine has confirmed the linearity of the kinetic parameters. The distribution in the brain is undetectable. The safety profile in terms of adverse effects is very similar to placebo in all Phase I, II and III clinical trials. Bilastine (20 mg), unlike cetirizine, does not increase alcohol effects on the CNS. Bilastine 20 mg does not increase the CNS depressant effect of lorazepam. Bilastine 20 mg is similar to placebo in the driving test. Therefore, it meets the current criteria for medication used in the treatment of allergic rhinitis and urticaria.

Allergy to dexchlorpheniramine. Study of a case.

PubMed

Cáceres Calle, O; Fernández-Benítez, M

2004-01-01

Dexchlorpheniramine (DH) is a classical or first generation antihistamine belonging to the ethanolamine group. Adverse effects related to these antihistamines are frequent, but the hypersensitivity reactions described in the literature since 1940 are exceptional. We report the case of a 32-year-old woman who experienced two episodes of akathisia secondary to intravenous (i.v.) dexchlorpheniramine administration for a possible hypersensitivity reaction to local anesthetics. Allergological study consisted of the following tests: skin prick tests with routine allergens, with a negative result; skin prick and intradermal tests with local anesthetics and DH, with a positive result to DH in the intradermal skin test (+ +); serum specific IgE, which was within normal levels; histamine release test with DH with a negative result, and the basophil activation test (BAT) with local anesthetics and DH, which was positive for DH and weakly positive to Lidocaine. BAT is proving to be a highly useful tool in the field of drug allergy, with a higher sensitivity and specificity than other in vitro tests. Because it avoids the need for provocation tests, this is especially important in drug-induced allergic reactions in which in vivo tests are repeatedly negative despite a clear clinical history.

Efficacy of dimetinden and hydroxyzine/chlorpheniramine in atopic dogs: a randomised, controlled, double-blinded trial

PubMed Central

Eichenseer, M.; Johansen, C.; Mueller, R. S.

2013-01-01

Antihistaminic drugs are commonly used as symptomatic therapy of atopic dermatitis in dogs. Unfortunately, their clinical benefit is largely unsubstantiated. In a double-blinded, placebo-controlled, cross-over trial, the influence of dimetinden and of a combination of chlorpheniramine and hydroxyzine on pruritus and lesions was evaluated in 19 dogs. They were treated with either product or a placebo orally for 14 days, each time followed by a 14-day washout period. Before and after each period, the dogs were examined and the Canine Atopic Dermatitis Extent and Severity Index (CADESI) determined by a clinician, and the pruritus and general condition by the owner. Dimetinden improved the pruritus significantly (P=0.014) but not the CADESI (P=0.087), the combination of hydroxyzine and chlorpheniramine improved the CADESI (P=0.049) and pruritus (P=0.05) significantly. Ten of 17 dogs improved by more than 25 per cent in pruritus with the combination of hydroxyzine and chlorpheniramine, 12 of 18 with dimetindenmaleate and only 2 of 19 with placebo. Antihistamines can help to reduce pruritus in atopic dogs, but in most cases, the improvement is limited and additional treatment may be needed. PMID:24114734

An overview of bilastine metabolism during preclinical investigations.

PubMed

Lucero, María Luisa; Gonzalo, Ana; Mumford, Rory; Betanzos, Mónica; Alejandro, Ana

2012-06-01

Knowledge of the biotransformation of oral H₁ antihistamines is clinically important because it can define their pharmacokinetic profile through possible effects on absorption (i.e., first-pass metabolism) and elimination. Further, clinically significant interactions with inhibitors of cytochrome P450 (CYP) have previously been reported for drugs of this therapeutic group, such as terfenadine and astemizole, indicating the possibility of drug-drug interactions involving agents that share the same metabolic pathway. The aim of this article was to review the preclinical testing of a new antihistamine (i.e., bilastine) in terms of its biotransformation in various animal species, including humans, and to evaluate its potential for possible drug-drug interactions involving the CYP system. A wide array of preclinical experiments were reviewed, all of which demonstrated that bilastine undergoes minimal metabolism in all species tested to date, including humans. Further, bilastine did not interact significantly, either as an inhibitor or inducer, with the CYP enzyme system, suggesting a low propensity for involvement in drug-drug interactions. These characteristics demonstrate the potential for bilastine to be a good choice for allergic patients receiving treatment for other concomitant diseases, including those with renal or hepatic dysfunction.

[Allergic transfusion reactions in a patient with multiple food allergies].

PubMed

Strobel, E; Schöniger, M; Münz, M; Hiefinger-Schindlbeck, R

2012-07-01

A 13-year-old girl with an osteosarcoma was treated by surgery and chemotherapy. During three transfusions of apheresis platelet concentrates allergic reactions occurred, partly in spite of premedication with an antihistamine and a corticoid. As the patient declared to be allergic to some foods, in-vitro tests for allergen-specific IgE antibodies were performed and showed markedly positive results for specific IgE to carrot and celery, less so to hazelnut, peanut and a lot of other food antigens. The donor of one of the unsuitable platelet concentrates remembered when questioned, that he had eaten carrots and chocolate with hazelnuts during the evening before platelet donation. Two washed platelet concentrates were transfused without any problem. Furthermore, transfusions of nine red blood cell concentrates and one unit of virus-inactivated frozen pooled plasma were well tolerated. Patients should be asked for allergies previous to transfusions to be alert to allergic reactions in patients with a positive history of food or drug allergies. If premedication with antihistamines does not prevent severe allergic transfusion reactions, transfusion of washed platelet concentrates and of virus-inactivated frozen pooled plasma can be considered. © Georg Thieme Verlag KG Stuttgart · New York.

The burden of allergies--and the capacity of medications to reduce this burden-in a heavy manufacturing environment.

PubMed

Bunn, William B; Pikelny, Dan B; Paralkar, Sadhna; Slavin, Thomas; Borden, Spencer; Allen, Harris M

2003-09-01

This article addresses the observational findings of the first systematic study undertaken by a manufacturer to address the impact of allergies and use of allergy medications on health, safety, and productivity. It provides background for 3 other papers from the same project, including an evaluation of an intervention to promote appropriate medication use among affected employees, which appear in this issue. The observational data are developed on 10,714 employees from: 1) 2 employee surveys; 2) administrative databases monitoring employee absenteeism, workers compensation, short-term disability, and group health. The results show that health, productivity, absenteeism, workplace injury, and workers compensation measures register consistent declines as allergy severity levels increase. This pattern is present but less pronounced for the short-term disability and group health measures. In addition, among the 16 measures registering a significant allergy burden, 6 posted significant advantages for the use of nonsedating antihistamines relative to other medication regimens that included sedative antihistamines. These results document the burden of allergies and the capacity of medications to reduce this burden. Effective intervention programs that target this condition can achieve improved health, productivity, and related outcomes.

[ENT inflammation and importance of fenspiride].

PubMed

Jankowski, R

2002-09-01

PERSISTENT INFLAMMATION: Inflammation may persist despite the eviction of the aggressive agent because of the disruption of the regulator mechanisms. In such patients, drugs such as fenspiride can be effective at several levels, from onset of inflammation, in an attempt to control its progression. INHIBITION OF NEUROPHIL MIGRATION: Could be a very interesting propriety for controlling inflammation of the human respiratory mucosa. CONTROL OF FREE RADICALS: In certain cases, clearance of free oxygen radicals by cells implicated in the inflammatory process may be overrun. Fenespiride can limit the production of free radicals, probably at the level of the producing cells. ACTION ON THE ARACHIDONIC ACID CASCADE: The mechanism and site of action of fenspiride remains to be clarified. It does not act like conventional antiinflammatory drugs by inhibiting cyclo-oxygenase. ANTIHISTAMINE ACTIVITY: Fenspiride has a certain antihistamine activity, basically by blocking H1 receptors. This action should be tested in subjects with nonspecific nasal hyperreactivity. OTHER PROPERTIES: Fenspiride also has an alpha-1-adrenolytic activity and an inhibitor effect on cyclic AMP, two properties which could have an impact on inflammatory diseases of the upper airways.

Antagonism of the effects of tremorine by tropine derivatives

PubMed Central

Farquharson, Muriel E.; Johnston, R. G.

1959-01-01

Methods of testing new drugs for anti-Parkinson activity are briefly reviewed. The production in animals of Parkinson-like effects by Tremorine (1,4-dipyrrolidin-1'-ylbut-2-yne), and the inhibition of these effects in mice by a number of tropine derivatives, are described. No correlation was found between the activity against tremor and the anticholinergic, antihistaminic or local anaesthetic properties of the compounds. PMID:13821613

Antagonism of the effects of tremorine by tropine derivatives.

PubMed

FARQUHARSON, M E; JOHNSTON, R G

1959-12-01

Methods of testing new drugs for anti-Parkinson activity are briefly reviewed. The production in animals of Parkinson-like effects by Tremorine (1,4-dipyrrolidin-1'-ylbut-2-yne), and the inhibition of these effects in mice by a number of tropine derivatives, are described. No correlation was found between the activity against tremor and the anticholinergic, antihistaminic or local anaesthetic properties of the compounds.

EAACI/GA(2)LEN/EDF/WAO guideline: management of urticaria.

PubMed

Zuberbier, T; Asero, R; Bindslev-Jensen, C; Walter Canonica, G; Church, M K; Giménez-Arnau, A M; Grattan, C E H; Kapp, A; Maurer, M; Merk, H F; Rogala, B; Saini, S; Sánchez-Borges, M; Schmid-Grendelmeier, P; Schünemann, H; Staubach, P; Vena, G A; Wedi, B

2009-10-01

This guideline, together with its sister guideline on the classification of urticaria (Zuberbier T, Asero R, Bindslev-Jensen C, Canonica GW, Church MK, Giménez-Arnau AM et al. EAACI/GA(2)LEN/EDF/WAO Guideline: definition, classification and diagnosis of urticaria. Allergy 2009;64: 1417-1426), is the result of a consensus reached during a panel discussion at the Third International Consensus Meeting on Urticaria, Urticaria 2008, a joint initiative of the Dermatology Section of the European Academy of Allergology and Clinical Immunology (EAACI), the EU-funded network of excellence, the Global Allergy and Asthma European Network (GA(2)LEN), the European Dermatology Forum (EDF) and the World Allergy Organization (WAO). As members of the panel, the authors had prepared their suggestions regarding management of urticaria before the meeting. The draft of the guideline took into account all available evidence in the literature (including Medline and Embase searches and hand searches of abstracts at international allergy congresses in 2004-2008) and was based on the existing consensus reports of the first and the second symposia in 2000 and 2004. These suggestions were then discussed in detail among the panel members and with the over 200 international specialists of the meeting to achieve a consensus using a simple voting system where appropriate. Urticaria has a profound impact on the quality of life and effective treatment is, therefore, required. The recommended first line treatment is new generation, nonsedating H(1)-antihistamines. If standard dosing is not effective, increasing the dosage up to four-fold is recommended. For patients who do not respond to a four-fold increase in dosage of nonsedating H(1)-antihistamines, it is recommended that second-line therapies should be added to the antihistamine treatment. In the choice of second-line treatment, both their costs and risk/benefit profiles are most important to consider. Corticosteroids are not recommended for

Evolving paradigm in the management of allergic rhinitis-associated ocular symptoms: role of intranasal corticosteroids.

PubMed

Blaiss, Michael S

2008-03-01

Along with nasal symptoms, ocular symptoms such as itching, tearing, and redness are common, bothersome components of the allergic rhinitis (AR) profile. Treatment of the patient with ocular allergy symptoms should take into account a variety of factors, including severity of symptoms, convenience/compliance issues, and patient preferences. To review from the primary care perspective the epidemiology, pathophysiology, and management of ocular symptoms associated with AR, and to evaluate the emerging role of intranasal corticosteroids (INSs). A search of the PubMed database identified clinical trials that assessed efficacy of agents in reducing ocular allergy symptoms. Internet searches identified further information including data on over-the-counter agents for treatment of ocular symptoms. Searches were conducted using search terms such as pathophysiology, epidemiology, ocular allergy, quality of life, drug class, and drug names. Primary care physicians are often the first point of contact for patients with seasonal AR (SAR) or perennial AR (PAR) symptoms. Ocular allergy associated with SAR and PAR (seasonal and perennial allergic conjunctivitis, respectively) is characterized by both early- and late-phase reactions, with symptoms often persisting long after allergen exposure. Non-pharmacologic measures such as allergen avoidance, use of artificial tears, and cool compresses are pertinent for all ocular allergy sufferers, but may not afford adequate symptom control. Pharmacotherapy options have traditionally included topical ophthalmic products for cases of isolated ocular symptoms, and oral antihistamines for patients with both nasal and ocular symptoms. However, this paradigm is changing with new evidence regarding the efficacy of INSs in reducing ocular symptoms. A number of meta-analyses and individual studies, most of which studied ocular symptoms as secondary variables, have demonstrated the ocular effects of INSs versus topical and oral antihistamines

[Efficacy and safety of astemizole in the treatment of allergic rhinitis and urticaria: a systematic review with meta-analysis].

PubMed

Gutiérrez Castrellón, Pedro; Ramírez Mayans, Jaime; López Pérez, Gerardo

2005-01-01

To compare astemizole with other first or second generation antihistaminics in the treatment of allergic rhinitis or urticaria. Systematic revision of clinical, controlled and randomized tests. 36 controlled, randomized, clinical, double or simple blind tests were made in 6,446 patients; 4,513 of them were assigned to astemizole and 1,933 to other first or second generation antihistaminics. Analyzed outcomes: Rate of global success; global scoring improvement of rhinitis; ocular, nasal or pharingeal pruritus; watering; nasal obstruction; sneeze; urticaria; cutaneous response to histamine; time to get a satisfactory improvent; frequency of sedation and headache. In connection to global success there were significant differences in favor of astemizole (OR 6.72, CI95% 5.36 to 8.41, p 0.0001); alike global scoring improvement of rhinitis (SMD -0.82, CI95% -1.70 to 0.06, p 0.04); rhinorrhea (SMD of -0.70, CI95% -1.47 to -0.03, p 0.02); nasal, pharingeal or ocular pruritus (SMD -0.64, CI95% -1.63 to 0.35, p 0.03); urticaria (SMD of -3.53, CI95% -4.11 to -2.94, p 0.0001), and reduction of cutaneous response to histamine (SMD -2.02, CI95% -2.47 to -1.57, p 0.0001). Differences for watering, nasal obstruction or sneeze were not observed. Finally, the safety area was analyzed considering the existence of sedation and headache; it was demonstrated less sedation (OR 0.23, CI95% 0.18 to 0.30, p 0.0001) and less headache (OR 0.58, CI95% 0.40 to 0.85, p 0.005) in the group treated with astemizole. The available evidence shows a therapeutic superiority of astemizole versus other antihistaminics in relation to the percentage of global success and the global scoring improvement of rhinitis, rhinorrhea, pruritus in general, urticaria symptoms and of the reduction of response to histamine, with a smaller frequency of headache or sedation.

Bilastine vs. hydroxyzine: occupation of brain histamine H1-receptors evaluated by positron emission tomography in healthy volunteers

PubMed Central

Farré, Magí; Pérez-Mañá, Clara; Papaseit, Esther; Menoyo, Esther; Pérez, Marta; Martin, Soraya; Bullich, Santiago; Rojas, Santiago; Herance, José-Raúl; Trampal, Carlos; Labeaga, Luis; Valiente, Román

2014-01-01

Aim A close correlation exists between positron emission tomography (PET)-determined histamine H1-receptor occupancy (H1RO) and the incidence of sedation. Antihistamines with H1RO <20% are classified as non-sedating. The objective was to compare the H1RO of bilastine, a second generation antihistamine, with that of hydroxyzine. Methods This randomized, double-blind, crossover study used PET imaging with [11C]-doxepin to evaluate H1RO in 12 healthy males (mean age 26.2 years), after single oral administration of bilastine (20 mg), hydroxyzine (25 mg) or placebo. Binding potentials and H1ROs were calculated in five cerebral cortex regions of interest: frontal, occipital, parietal, temporal, insula. Plasma bilastine concentrations, subjective sedation (visual analogue scale), objective psychomotor performance (digital symbol substitution test), physiological variables and safety (adverse events, AEs), were also evaluated. Results The mean binding potential of all five regions of interest (total binding potential) was significantly greater with bilastine than hydroxyzine (mean value 0.26 vs. 0.13, P < 0.01; mean difference and 95% CI −0.130 [−0.155, 0.105]). There was no significant difference between bilastine and placebo. Overall H1RO by bilastine was significantly lower than that by hydroxyzine (mean value −3.92% vs. 53.95%, P < 0.01; mean difference and 95% CI 57.870% [42.664%, 73.075%]). There was no significant linear relationship between individual bilastine plasma concentrations and total binding potential values. No significant between-treatment differences were observed for sedation and psychomotor performance. Twenty-six non-serious AEs were reported. Sleepiness or sedation was not reported with bilastine but appeared in some subjects with hydroxyzine. Conclusions A single oral dose of bilastine 20 mg had minimal H1RO, was not associated with subjective sedation or objective impairment of psychomotor performance and was devoid of

Bilastine vs. hydroxyzine: occupation of brain histamine H1 -receptors evaluated by positron emission tomography in healthy volunteers.

PubMed

Farré, Magí; Pérez-Mañá, Clara; Papaseit, Esther; Menoyo, Esther; Pérez, Marta; Martin, Soraya; Bullich, Santiago; Rojas, Santiago; Herance, José-Raúl; Trampal, Carlos; Labeaga, Luis; Valiente, Román

2014-11-01

A close correlation exists between positron emission tomography (PET)-determined histamine H1 -receptor occupancy (H1 RO) and the incidence of sedation. Antihistamines with H1 RO <20% are classified as non-sedating. The objective was to compare the H1 RO of bilastine, a second generation antihistamine, with that of hydroxyzine. This randomized, double-blind, crossover study used PET imaging with [(11) C]-doxepin to evaluate H1 RO in 12 healthy males (mean age 26.2 years), after single oral administration of bilastine (20 mg), hydroxyzine (25 mg) or placebo. Binding potentials and H1 ROs were calculated in five cerebral cortex regions of interest: frontal, occipital, parietal, temporal, insula. Plasma bilastine concentrations, subjective sedation (visual analogue scale), objective psychomotor performance (digital symbol substitution test), physiological variables and safety (adverse events, AEs), were also evaluated. The mean binding potential of all five regions of interest (total binding potential) was significantly greater with bilastine than hydroxyzine (mean value 0.26 vs. 0.13, P < 0.01; mean difference and 95% CI -0.130 [-0.155, 0.105]). There was no significant difference between bilastine and placebo. Overall H1 RO by bilastine was significantly lower than that by hydroxyzine (mean value -3.92% vs. 53.95%, P < 0.01; mean difference and 95% CI 57.870% [42.664%, 73.075%]). There was no significant linear relationship between individual bilastine plasma concentrations and total binding potential values. No significant between-treatment differences were observed for sedation and psychomotor performance. Twenty-six non-serious AEs were reported. Sleepiness or sedation was not reported with bilastine but appeared in some subjects with hydroxyzine. A single oral dose of bilastine 20 mg had minimal H1 RO, was not associated with subjective sedation or objective impairment of psychomotor performance and was devoid of treatment-related sedative AEs

Not in My Navy. A Legal Guide to Drug Abuse.

DTIC Science & Technology

1984-06-01

opiates produces drowsiness, sleep, and a reduction in physical activity. Side effects can include nausea and vomiting, constipation, itching, flushing...diarrhea, pallor, and dilation of the pupils. Such effects are generally seen only with high doses or as occasional side effects with therapeutic doses...that will produce low-level side effects . or, a person might be drowsy from ingesting a nonprescription product - such as an antihistamine. A clue to

Scombroid poisoning.

PubMed

Lange, W R

1988-04-01

The symptoms of scombroid poisoning resemble an acute allergic reaction. Tuna, albacore, mackerel and bonito are implicated, as are nonscombroid fish such as mahi-mahi and bluefish. The histamine content of affected fish is high, but the pathophysiology is more complex than the mere ingestion of histamine. Antihistamines and cimetidine appear to be effective in controlling symptoms. Prevention consists of prompt and adequate refrigeration of dark-meated fish.

Management of a black leopard (Panthera pardus) with seasonal atopy and cutaneous adverse food reaction by using transmucosal immunotherapy.

PubMed

Newton, Heather P; Gamble, Kathryn C; Friberg, Cecilia

2013-03-01

An 11-yr-old female black leopard (Panthera pardus) was presented with pruritus and intermittent gastrointestinal distress for a duration of 18 mo. Dietary elimination trial and challenge confirmed food hypersensitivity. Milder and persistent pruritus, while consuming a strict elimination diet, confirmed atopic dermatitis also was related to airborne environmental triggers identified by intradermal allergy testing. Ultimately, atopy was controlled successfully by antihistamines and transmucosal immunotherapy for 7 yr after diagnosis.

Role of neurotensin in radiation-induced hypothermia in rats

DOE Office of Scientific and Technical Information (OSTI.GOV)

Kandasamy, S.B.; Hunt, W.A.; Harris, A.H.

1991-05-01

The role of neurotensin in radiation-induced hypothermia was examined. Intracerebroventricular (ICV) administration of neurotensin produced dose-dependent hypothermia. Histamine appears to mediate neurotensin-induced hypothermia because the mast cell stabilizer disodium cromoglycate and antihistamines blocked the hypothermic effects of neurotensin. An ICV pretreatment with neurotensin antibody attenuated neurotensin-induced hypothermia, but did not attenuate radiation-induced hypothermia, suggesting that radiation-induced hypothermia was not mediated by neurotensin.

Treatment of systemic mast cell disorders.

PubMed

Worobec, A S

2000-06-01

The heterogeneous nature of disease manifestations in mastocytosis requires the individualization of therapy to each patient's clinical presentation and prognosis. The mainstay of treatment for most categories of mastocytosis are H1 and H2 antihistamines with the addition of corticosteroids for more severe symptoms. This article presents a summary of treatment strategies for indolent and aggressive forms of mastocytosis along with a discussion of future therapeutic directions.

Section V: Conclusions

DTIC Science & Technology

2001-06-01

aeromedical issues. The section concludes with a sample review of a candidate medication, in this case losartan potassium, with a possible approach to...as losartan , Allergic rhinitis is a very common condition appear to hold promise for use in aircrew and generally compatible with military aircrew...evaluating the aeromedical suitability of HI antihistamines for this condition in aircrew losartan led our group to designate losartan as a because of

Anaphylactic deaths in asthmatic patients.

PubMed

Settipane, G A

1989-01-01

We reviewed seven documented deaths to peanuts and two near deaths. We excluded hearsay undocumented deaths to peanuts. Peanut allergy is one of the most common food allergies and probably the most common cause of death by food anaphylaxis in the United States. About one-third of peanut-sensitive patients have severe reactions to peanuts. Asthmatics with peanut sensitivity appear more likely to develop fatal reactions probably because of the exquisite sensitivity that asthamatics have to chemical mediators of anaphylaxis. Severe reactions occur within a few minutes of ingestion and these patients must carry preloaded epinephrine syringes, antihistamines, and medic-alert bracelets. Treatment should include repeated doses of epinephrine, antihistamines and corticosteroids as well as availability of oxygen, mechanical methods to open airways, vasopressors, and intravenous fluids. Hidden sources of peanuts such as chili, egg rolls, cookies, candy, and pastry should be recognized and identified. Scratch/prick test to peanuts are highly diagnostic. Peanut is one of the most sensitive food allergens known requiring only a few milligrams to cause a reaction. In some individuals, even contact of peanut with unbroken skin can cause an immediate local reaction. Unfortunately, peanut reaction is not outgrown and remains a life-long threat.

A Nanoporous Alumina Membrane Based Electrochemical Biosensor for Histamine Determination with Biofunctionalized Magnetic Nanoparticles Concentration and Signal Amplification

PubMed Central

Ye, Weiwei; Xu, Yifan; Zheng, Lihao; Zhang, Yu; Yang, Mo; Sun, Peilong

2016-01-01

Histamine is an indicator of food quality and indispensable in the efficient functioning of various physiological systems. Rapid and sensitive determination of histamine is urgently needed in food analysis and clinical diagnostics. Traditional histamine detection methods require qualified personnel, need complex operation processes, and are time-consuming. In this study, a biofunctionalized nanoporous alumina membrane based electrochemical biosensor with magnetic nanoparticles (MNPs) concentration and signal amplification was developed for histamine determination. Nanoporous alumina membranes were modified by anti-histamine antibody and integrated into polydimethylsiloxane (PDMS) chambers. The specific antibody modified MNPs were used to concentrate histamine from samples and transferred to the antibody modified nanoporous membrane. The MNPs conjugated to histamine were captured in the nanopores via specific reaction between histamine and anti-histamine antibody, resulting in a blocking effect that was amplified by MNPs in the nanopores. The blockage signals could be measured by electrochemical impedance spectroscopy across the nanoporous alumina membrane. The sensing platform had great sensitivity and the limit of detection (LOD) reached as low as 3 nM. This biosensor could be successfully applied for histamine determination in saury that was stored in frozen conditions for different hours, presenting a potentially novel, sensitive, and specific sensing system for food quality assessment and safety support. PMID:27782087

The drug-use patterns of helping-profession students in Brisbane, Australia.

PubMed

Engs, R C

1980-10-01

A survey of 1691 first-and final-year students in the helping professions (medicine, law, nursing, pharmacy, police science, seminary, social work/ psychology, and teaching) as to their use of drugs was carried out during February to April, 1980, in Brisbane, Australia. The results indicated that about 86% drank coffee or tea, 85% drank alcohol, 85% used non-prescription analgesics, 31% used tobacco, 25% antihistamines, 9% marijuana, 9% sedatives, 6% tranquilizers, 2% hallucinogens, 2% stimulants, 1% cocaine and 1% used opiates at least once a year. Of these students, females used analgesics and antihistamines significantly more frequently than males and consumed more caffeine, tobacco and analgesics than males, while males drank significantly more alcohol than females. Final-year students used more alcohol, coffee or tea and tobacco, and used marijuana, coffee and tea and tobacco significantly more frequently than first-year students. Individuals who did not consider religion important used more alcohol and tobacco and used marijuana, tobacco and hallucinogens more frequently compared to individuals who considered religion to be important. There was also a significant difference in drug usage between the different courses of study for most of the substances, with law students using the majority of substances the most frequently and seminarians the least frequently.

Treatment of Sleep Disturbance in Alcohol Recovery: A National Survey of Addiction Medicine Physicians

PubMed Central

Friedmann, Peter D.; Herman, Debra S.; Freedman, Shelby; Lemon, Stephenie C.; Ramsey, Susan; Stein, Michael D.

2009-01-01

Sleep disturbance is common among patients in recovery from alcoholism and can precipitate relapse. Though sleep complaints are commonly managed with medication, little is known about their management among recovering alcoholic patients. We performed a postal survey of a self-weighted, random systematic sample of 503 members of the American Society of Addiction Medicine (ASAM) to examine addiction medicine physicians’ medical management of sleep disturbance among patients in early recovery from alcoholism. After 3 mailings, 311 (62%) responded. Of responents, 64% have offered pharmacological treatment to an insomniac, alcoholic patient in the first 3 months after detoxification, but only 22% offered medication to more than half of such patients. Trazodone was the preferred therapy, chosen first by 38% of respondents, followed by other sedating antidepressants (12%), and antihistamines (12%). The mean duration of therapy for trazodone and other sedating antidepressants exceeded one month. Experts in addiction medicine appear reluctant to prescribe medication to sleep-disturbed patients in early recovery from alcoholism. When they do prescribe, trazodone, other sedating antidepressants and antihistamines are favored, despite limited evidence for or against this indication. Although the treatment of disordered sleep among alcoholic patients in early recovery may have merit to prevent relapse, controlled studies of these sleep agents are needed. PMID:12703672

Tannate complexes of antihistaminic drug: sustained release and taste masking approaches.

PubMed

Rahman, Ziyaur; Zidan, Ahmed S; Berendt, Robert T; Khan, Mansoor A

2012-01-17

The aim of this investigation was to evaluate the complexation potential of brompheniramine maleate (BPM) and tannic acid (TA) for sustained release and taste masking effects. The complexes (1:1-1:7 TA to BPM ratio) were prepared by the solvent evaporation method using methanol, phosphate buffer pH 6.8 or 0.1N HCl as common solvents. The complexes were characterized microscopically by scanning electron microscopy (SEM), chemically by Fourier transform infrared (FTIR) and solid-state NMR (SSNMR), thermally by differential scanning calorimetry (DSC), for crystallinity by powder X-ray powder diffraction (PXRD), for organoleptic evaluation by electronic tongue (e-tongue), and for solubility in 0.1N HCl and phosphate buffer pH 6.8. The dissolution studies were carried out using the USP II method at 50 rpm in 500 ml of dissolution media (0.1N HCl or phosphate buffer pH 6.8). SEM images revealed that the morphology of complexes were completely different from the individual components, and all complexes had the same morphological characteristics, irrespective of the solvent used for their preparation, pH or ratio of BPM and TA. The FTIR spectra showed the presence of chemical interactions between the TA and BPM. DSC, PXRD and SSNMR indicated that the drug lost its crystalline nature by formation of the complex. Complexation has significantly reduced the solubility of BPM and sustained the drug release up to 24h in phosphate buffer pH 6.8 media. The bitter taste of the BPM was completely masked which was indicated by Euclidean distance values which was far from the drug but near to its placebo in the complexes in all ratios studied. The taste masked complexes can be potentially developed as suitable dosage forms for pediatric use. In summary, complexation of BPM and TA effectively sustained the dissolution and masked the bitter taste of drug for the development of suitable dosage forms for pediatric use. Published by Elsevier B.V.

Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.

PubMed

Jauregizar, Nerea; de la Fuente, Leire; Lucero, Maria Luisa; Sologuren, Ander; Leal, Nerea; Rodríguez, Mónica

2009-01-01

To model the pharmacokinetic and pharmacodynamic relationship of bilastine, a new histamine H(1) receptor antagonist, from single- and multiple-dose studies in healthy adult subjects. The pharmacokinetic model was developed from different single-dose and multiple-dose studies. In the single-dose studies, a total of 183 subjects received oral doses of bilastine 2.5, 5, 10, 20, 50, 100, 120, 160, 200 and 220 mg. In the multiple-dose studies, 127 healthy subjects received bilastine 10, 20, 40, 50, 80, 100, 140 or 200 mg/day as multiple doses during a 4-, 7- or 14-day period. The pharmacokinetic profile of bilastine was investigated using a simultaneous analysis of all concentration-time data by means of nonlinear mixed-effects modelling population pharmacokinetic software NONMEM version 6.1. Plasma concentrations were modelled according to a two-compartment open model with first-order absorption and elimination. For the pharmacodynamic analysis, the inhibitory effect of bilastine (inhibition of histamine-induced wheal and flare) was assessed on a preselected time schedule, and the predicted typical pharmacokinetic profile (based on the pharmacokinetic model previously developed) was used. An indirect response model was developed to describe the pharmacodynamic relationships between flare or wheal areas and bilastine plasma concentrations. Finally, once values of the concentration that produced 50% inhibition (IC(50)) had been estimated for wheal and flare effects, simulations were carried out to predict plasma concentrations for the doses of bilastine 5, 10 and 20 mg at steady state (72-96 hours). A non-compartmental analysis resulted in linear kinetics of bilastine in the dose range studied. Bilastine was characterized by two-compartmental kinetics with a rapid-absorption phase (first-order absorption rate constant = 1.50 h(-1)), plasma peak concentrations were observed at 1 hour following administration and the maximal response was observed at approximately 4 hours or later. Concerning the selected pharmacodynamic model to fit the data (type I indirect response model), this selection is attributable to the presence of inhibitory bilastine plasma concentrations that decrease the input response function, i.e. the production of the skin reaction. This model resulted in the best fit of wheal and flare data. The estimates (with relative standard errors expressed in percentages in parentheses) of the apparent zero-order rate constant for flare or wheal spontaneous appearance (k(in)), the first-order rate constant for flare or wheal disappearance (k(out)) and bilastine IC(50) values were 0.44 ng/mL/h (14.60%), 1.09 h(-1) (15.14%) and 5.15 ng/mL (16.16%), respectively, for wheal inhibition, and 11.10 ng/mL/h (8.48%), 1.03 h(-1) (8.35%) and 1.25 ng/mL (14.56%), respectively, for flare inhibition. The simulation results revealed that bilastine plasma concentrations do not remain over the IC(50) value throughout the inter-dose period for doses of 5 and 10 mg. However, with a dose of 20 mg of bilastine administered every 24 hours, plasma concentrations remained over the IC(50) value during the considered period for the flare effect, and up to 20 hours for the wheal effect. Pharmacokinetic and pharmacodynamic relationships of bilastine were reliably described with the use of an indirect response pharmacodynamic model; this led to an accurate prediction of the pharmacodynamic activity of bilastine.

Comparative Effects of Antihistamines on Aircrew Mission Effectiveness under Sustained Operations

DTIC Science & Technology

1992-06-01

measures consist mainly of process measures. Process measures are measures of activities used to accomplish the mission and produce the final results...They include task completion times and response variability, and information processing rates as they relate to unique task assignment. Performance...contains process measures that assess the Individual contributions of hardware/software and human components to overall system performance. Measures

[Socio-economic impact of allergic rhinitis and perspectives of appropriate therapy].

PubMed

May, Uwe

2014-07-24

Allergic rhinitis is a very common disease that causes high economic costs. Furthermore inadequate treatment can lead to bronchial asthma. Against this background, drugs for the treatment of allergic rhinitis should be evaluated from a comprehensive medical-economic perspective. The new combination of an antihistamine and a corticosteroid, introduced in the market in 2013, emerges as useful pharmaceutical alternative, both with regard to the medical outcome parameters as well as cost-effectiveness.

Scombroid fish poisoning illness and coronary artery vasospasm.

PubMed

Anastasius, Malcolm; Yiannikas, John

2015-01-01

We present an interesting case of a young man with coronary artery vasospasm complicating scombroid fish poisoning illness. The initial presentation included tachycardia and significant hypotension. A 12-lead ECG showed sinus tachycardia with marked widespread ST segment depression and ST elevation in aVR. Symptoms subsequently improved with intravenous fluid rehydration, antihistamines, and glyceral trinitrate. The underlying pathogenesis and treatment of this rarely described manifestation of the fish poisoning illness is discussed.

GUIDELINES OF CARE FOR THE MANAGEMENT OF ATOPIC DERMATITIS

PubMed Central

Sidbury, Robert; Davis, Dawn M.; Cohen, David E.; Cordoro, Kelly M.; Berger, Timothy G.; Bergman, James N.; Chamlin, Sarah L.; Cooper, Kevin D.; Feldman, Steven R.; Hanifin, Jon M.; Krol, Alfons; Margolis, David J.; Paller, Amy S.; Schwarzenberger, Kathryn; Silverman, Robert A.; Simpson, Eric L.; Tom, Wynnis L.; Williams, Hywel C.; Elmets, Craig A.; Block, Julie; Harrod, Christopher G.; Begolka, Wendy Smith; Eichenfield, Lawrence F.

2014-01-01

Atopic dermatitis (AD) is a chronic, pruritic inflammatory dermatosis that affects up to 25% of children and 2-3% of adults. This guideline addresses important clinical questions that arise in AD management and care, providing recommendations based on the available evidence. In this third of four sections, treatment of AD with phototherapy and systemic immunomodulators, antimicrobials, and antihistamines is reviewed, including indications for use and the risk-benefit profile of each treatment option. PMID:24813298

[Ketotifen treatment of chronic urticaria. An open study of therapeutically difficult courses].

PubMed

Taube, K M; Wozniak, K D; Lässig, W

1985-12-01

21 patients suffering from chronic urticaria were treated with Ketotifen (2 X 1 mg/d) for 4 weeks. The suppression of weals and pruritus, the side effects in comparison with antihistamines, as well as the effect after finishing therapy have been studied. Ketotifen has a good suppressing effect on weals and pruritus. The general tolerance of the preparation is good, as well. Thus Ketotifen may be regarded as an additional possibility concerning treatment of chronic urticaria.

Ciguatera poisoning in the Cook Islands

PubMed Central

Bailey, Stephanie; Withers, Tristan

2014-01-01

This case report presents two British medical students who contracted ciguatera poisoning while on elective in the Cook Islands. Thirty-six hours after consuming two reef fish they developed paraesthesia of the mouth, hands and feet, myalgia, pruritis and cold allodynia. Neurological examination was normal. Diagnosis of ciguatera poisoning was made on history of reef fish consumption and classical clinical presentation. Management was symptomatic (antihistamines) and both students made a full recovery within 10 weeks. PMID:24966268

Prevention for Pediatric and Adolescent Migraine.

PubMed

Hickman, Carolyn; Lewis, Kara Stuart; Little, Robert; Rastogi, Reena Gogia; Yonker, Marcy

2015-01-01

Children and adolescents can experience significant disability from frequent migraine. A number of tools have been developed to help quantify the impact of migraine in this population. Many preventative medications used in adults are routinely used to prevent migraines in children, although there has been less rigorous study. This article reviews the indications and evidence for the use of migraine preventatives, such as antidepressants, antihypertensives, anticonvulsants, antihistamines, and botulinum toxin, in this population. © 2015 American Headache Society.

Evaluation of a New Equation for Calculating the Maximum Wait Time for Pilots That Have Used an Impairing Medication

DTIC Science & Technology

2013-08-01

were treating pre-existing medical conditions using over-the-counter (OTC) medications ( Aspirin ™, Tylenol™, antihistamines, etc.), provided blood...time would decrease to 45 hours for a 150-lb person taking the same dose; a 300 -lb individual taking a 25-mg dose would only need to wait 31 hours...If the 300 -lb person mentioned above had taken a 50- mg dose, the wait time would have been 45 hours, which is approximately the same as the 49

Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-κB, CCR1, chemokine CCL5/RANTES and interleukin-1β in PBMC allergic and non-allergic patients.

PubMed

Kordulewska, Natalia Karolina; Kostyra, Elżbieta; Cieślińska, Anna; Matysiewicz, Michał; Fiedorowicz, Ewa; Sienkiewicz-Szłapka, Edyta

2017-03-01

Fexofenadine (FXF) is a third-generation antihistamine drug and osthole is assumed as a natural antihistamine alternative. This paper compares results of histamine, FXF and osthole impact on HRH-1, COX-2, NF-κB-p50, CCR1 mRNA expression. We also measured mRNA expression of IL-1β and CCL5/RANTES in incubated peripheral blood mononuclear cells (PBMC) to compared how histamine, FXF and osthole had influence on expression level and interacts on product secretion. The purpose was to investigate expression pattern in asthma PBMC. The cultures were treated 72h with FXF and osthole. We measured mRNA expression of histamine HRH-1, COX-2, NF-κB-p50, CCR1, IL-1β and CCL5/RANTES with Real-Time PCR (RT-PCR). The present study suggest that osthole may be a potential inhibitor of histamine H 1 receptor activity. We also demonstrated that cells cultured with histamine increase COX-2 mRNA expression and osthole reduce it. Allergy remains one of the most common chronic diseases in Europe and it is rapidly approaching epidemic proportions; with current predictions estimating that the number of allergy-afflicted will equal the healthy population by 2020. It is therefore paramount to find new pharmaceuticals which successfully combat allergic disease. Copyright © 2016 Elsevier GmbH. All rights reserved.

Allergic reactions to antithyroid drugs are associated with autoimmunity a retrospective case-control study.

PubMed

Chivu, R D; Chivu, Laura Ioana; Ion, Daniela Adriana; Barbu, Carmen; Fica, Simona

2006-01-01

Thiamazole is the most used antithyroid drug for thyrotoxicosis in Basedow-Graves' (BG) (autoimmune) disease and in toxic multinodular goitre (TMG) (non-autoimmune). This study aims to find whether allergic reactions to thiamazole occur more frequently during the treatment of BG than of TMG. Retrospective study, of 128 patients newly diagnosed and treated for thyrotoxicosis in the first 6 months of 2006, in the Endocrinology Department of "Elias" Hospital, Bucharest. Cases were all patients treated with thiamazole who developed allergic reactions. Controls were all patients treated with thiamazole without allergic reactions. Risk factor was considered to be the presence of BG. Cases group consisted of 6 patients. All 6 started treatment with thiamazole for BG, and developed allergic reactions after 2-4 weeks of treatment. When thiamazole was withdrawn, allergic symptoms ceased under antihistamines and steroids. In order to control the thyrotoxicosis, antihistamines and oral steroids was administered, together with thiamazole in slow increasing doses. After about 4 weeks under this combination, a tolerance to thiamazole seems to appear. Control group consisted of 122 patients who started thiamazole: 66 for BG and 56 for TMG (without allergic reactions). Allergy to thiamazole was significantly associated with the autoimmune BG, and not with TMG (p = 0.03, OR = 11.04). None of the patients with TMG developed allergic reactions to the drug. Tolerance to this drug may occur.

Effect of terfenadine on nasal, eustachian tube, and pulmonary function after provocative intranasal histamine challenge.

PubMed

Skoner, D P; Doyle, W J; Boehm, S; Fireman, P

1991-12-01

Previous studies have documented that intranasal histamine challenge results in nasal and eustachian tube obstruction (ETO) in human volunteers. The purpose of the present study was to assess the effect of pretreatment with terfenadine, a nonsedating antihistamine on the pathophysiologic consequences of intranasal histamine challenge. Fifteen subjects with allergic rhinitis were challenged intranasally with saline and increasing histamine doses (0.01, 0.1, 0.5, 1.0, 5.0, and 10.0 mg) before pretreatment (baseline) and after 1 week of pretreatment with terfenadine, 60 mg b.i.d., terfenadine, 120 mg b.i.d., and placebo. Nasal conductance as measured by posterior rhinomanometry showed a dose-dependent, monotonic decrease following sequential administration of the histamine solutions, but there were no apparent differences in the average responses among the four challenge sessions. The frequency of ETO after histamine challenge was decreased by pretreatment with both doses of terfenadine, although this was not significant. Histamine-induced sneezing and rhinorrhea, but not congestion, were significantly reduced by terfenadine pretreatment. There was no evidence of extension of the histamine effects to the lower airway. The results of the present study suggest that terfenadine, a nonsedating antihistamine, had a favorable effect on sneezing and rhinorrhea after provocative intranasal histamine challenge, but did not significantly attenuate the subjective or objective nasal and ET obstructive responses.

Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria

PubMed Central

Sadaba, Belen; Azanza, Jose Ramon; Gomez-Guiu, Almundena; Rodil, Raquel

2013-01-01

Bilastine is a second generation antihistamine indicated for the treatment of seasonal or perennial allergic rhinoconjunctivitis and chronic urticaria with a daily dose of 20 mg, in adults and children over 12 years of age. The efficacy of bilastine has been shown to be similar to that of the comparator drugs for the control of the nasal and nonnasal symptoms of allergic rhinoconjunctivitis, while also showing a subjective improvement in the quality of life and in overall clinical impression. For chronic urticaria the symptoms (itching and the development of papules) lessens from the second day of treatment onwards, in a similar way to other antihistamines used as comparators. Bilastine should not be administered at meal times to avoid interference with the absorption process. It is not distributed to the central nervous system, is scarcely metabolized, and elimination is through the kidneys and feces, with a 14-hour elimination half-life. It has no effect on cytochrome P450. During clinical development, bilastine was shown to be a drug that is adequately tolerated, with a similar effect to placebo with regard to drowsiness and changes in heart rate. In relation to its use, headaches were the most frequent adverse effect to be reported. No cardiotoxic effects have been observed, and the therapeutic dose does not alter the state of alertness. PMID:23667312

Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria.

PubMed

Sadaba, Belen; Azanza, Jose Ramon; Gomez-Guiu, Almundena; Rodil, Raquel

2013-01-01

Bilastine is a second generation antihistamine indicated for the treatment of seasonal or perennial allergic rhinoconjunctivitis and chronic urticaria with a daily dose of 20 mg, in adults and children over 12 years of age. The efficacy of bilastine has been shown to be similar to that of the comparator drugs for the control of the nasal and nonnasal symptoms of allergic rhinoconjunctivitis, while also showing a subjective improvement in the quality of life and in overall clinical impression. For chronic urticaria the symptoms (itching and the development of papules) lessens from the second day of treatment onwards, in a similar way to other antihistamines used as comparators. Bilastine should not be administered at meal times to avoid interference with the absorption process. It is not distributed to the central nervous system, is scarcely metabolized, and elimination is through the kidneys and feces, with a 14-hour elimination half-life. It has no effect on cytochrome P450. During clinical development, bilastine was shown to be a drug that is adequately tolerated, with a similar effect to placebo with regard to drowsiness and changes in heart rate. In relation to its use, headaches were the most frequent adverse effect to be reported. No cardiotoxic effects have been observed, and the therapeutic dose does not alter the state of alertness.

Promethazine affects autonomic cardiovascular mechanisms minimally

NASA Technical Reports Server (NTRS)

Brown, T. E.; Eckberg, D. L.

1997-01-01

Promethazine hydrochloride, Phenergan, is a phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. These properties have made promethazine a candidate for use in environments such as microgravity, which provoke emesis and motion sickness. Recently, we evaluated carotid baroreceptor-cardiac reflex responses during two Space Shuttle missions 18 to 20 hr after the 50 mg intramuscular administration of promethazine. Because the effects of promethazine on autonomic cardiovascular mechanisms in general and baroreflex function in particular were not known, we were unable to exclude a possible influence of promethazine on our results. Our purpose was to determine the ground-based effects of promethazine on autonomic cardiovascular control. Because of promethazine's antihistaminic and anticholinergic properties, we expected that a 50-mg intramuscular injection of promethazine would affect sympathetically and vagally mediated cardiovascular mechanisms. Eight healthy young subjects, five men and three women, were studied at rest in recumbency. All reported drowsiness as a result of the promethazine injection; most also reported nervous excitation, dry mouth, and fatigue. Three subjects had significant reactions: two reported excessive anxiety and one reported dizziness. Measurements were performed immediately prior to injection and 3.1 +/- 0.1 and 19.5 +/- 0.4 hr postinjection. We found no significant effect of promethazine on resting mean R-R interval, arterial pressure, R-R interval power spectra, carotid baroreflex function, and venous plasma catecholamine levels.

Safety and efficacy of cetirizine versus cetirizine plus ranitidine in chronic urticaria: Double-blind randomized placebo-controlled study.

PubMed

Guevara-Gutierrez, Elizabeth; Bonilla-Lopez, Sonia; Hernández-Arana, Socorro; Tlacuilo-Parra, Alberto

2015-01-01

First-line treatment for chronic urticaria is H1 non-sedating antihistamines. When these fail, guidelines recommend combination with H2 antihistamines. We conducted a randomized, double-blind, placebo-controlled trial. Thirty-two patients with chronic urticaria were included. Group A (16 subjects) treated with cetirizine plus ranitidine and Group B (16 subjects) with cetirizine plus placebo, both for 30 days. Efficacy measures were Urticaria Activity Score (UAS), Chronic Urticaria Quality of Life Questionnaire (CU-Q2oL) and time of symptom remission, safety measures were clinical and laboratory effects. Complete remission was obtained in ten patients (62.5%) from Group A and seven patients (44%) from Group B (p = 0.28). The UAS in Group A was 1.53 ± 2.09 versus Group B 2.06 ± 1.34 (p = 0.20). The CU-Q2oL in Group A was 12.93 ± 19.20 versus Group B 12.68 ± 10.30 (p = 0.20). At the end of treatment, 13 patients (81%) from Group A and 14 patients (87.5%) from Group B had some type of adverse effect (p = 1.0). Combination of cetirizine with ranitidine was not more effective than cetirizine alone in chronic urticaria. Both treatments resulted equally safe; however, our main limitation is the small sample size.

Actual therapeutic management of allergic and hyperreactive nasal disorders

PubMed Central

Rudack, Claudia

2004-01-01

Allergic rhinitis (AR) and hyperractive disorders of the upper airways, depending upon the type of releasing stimuli, are defined as nasal hyperreactivity, for example in the case of AR, or as non-specific nasal hyperreactivity and as idiopathic rhinitis (IR) (synonyms frequently used in the past: non-specific nasal hyperreactivity; vasomotor rhinitis) in the case of non-characterised stimuli. An early and professional therapy of allergic disorders of the upper airways is of immense importance as allergic rhinitis is detected in comorbidities such as asthma and rhino sinusitis. The therapeutic concept is influenced by new and further developments in pharmacological substance classes such as antihistamines and glucocorticosteroids. Specific immune therapy, the only causal therapy for AR, has been reviewed over the past few years in respect of the type and pattern of application. However, to date no firm recommendations on oral, sublingual and /or nasal immune therapy have yet been drawn up based on investigations of these modifications. Therapeutic management of IR is aimed at a symptom-oriented therapy of nasal hyperactivity as etiological factors relating to this form of rhinitis are not yet sufficiently known. Drug groups such as mast cell stabilizers, systemic and topic antihistamines, topic and systemic glucocorticosteroids, ipatroium bromide and alpha symphatomimetics belong to the spectrum of the therapeutics employed. PMID:22073046

[The marketing analysis of assortment of market of pharmaceuticals applied in treatment of psoriasis in Ukraine].

PubMed

Kotvitskaya, A A; Karlo, V V

2013-01-01

The analysis of assortment of pharmaceuticals for treatment of psoriasis recommended by Minzdrav of Ukraine and present at the national pharmaceutical market is made. The characteristics of distribution of national and foreign producers of antihistamine and anti-psoriatic pharmaceuticals are established The availability of particular medicinal forms of various producers is analyzed too. The characteristics and tendencies in consumption of these groups of pharmaceuticals in natural and monetary units are analyzed including dynamics of changes of mean wholesale prices during the analyzed period.

Performance assessment in complex individual and team tasks

NASA Technical Reports Server (NTRS)

Eddy, Douglas R.

1992-01-01

Described here is an eclectic, performance based approach to assessing cognitive performance from multiple perspectives. The experience gained from assessing the effects of antihistamines and scenario difficulty on C (exp 2) decision making performance in Airborne Warning and Control Systems (AWACS) weapons director (WD) teams can serve as a model for realistic simulations in space operations. Emphasis is placed on the flexibility of measurement, hierarchical organization of measurement levels, data collection from multiple perspectives, and the difficulty of managing large amounts of data.

Ciguatera poisoning in the Cook Islands.

PubMed

Bailey, Stephanie; Withers, Tristan

2014-06-25

This case report presents two British medical students who contracted ciguatera poisoning while on elective in the Cook Islands. Thirty-six hours after consuming two reef fish they developed paraesthesia of the mouth, hands and feet, myalgia, pruritis and cold allodynia. Neurological examination was normal. Diagnosis of ciguatera poisoning was made on history of reef fish consumption and classical clinical presentation. Management was symptomatic (antihistamines) and both students made a full recovery within 10 weeks. 2014 BMJ Publishing Group Ltd.

Cardiorespiratory Assessment of Decongestant-Antihistamine Effects on Altitude, +Gz, and Fatigue Tolerances

DTIC Science & Technology

1978-04-01

tolerated. Two subjec~ts were cle~rly incapacitated during the first +2Gz test under Comyon A at1A50fI ,’titude. Ic ’.s fe~lt that the +Gz intolerance ...I intolerance to altitude, LBNP, or ergometry disqualified the candidate from subsequent participation in the study. Some of the vital...altitude with a single dose of Compound A, Compound B, or lactose placebo. All three ingesta were prepared in identical-appearing cap- sules. Each

Identification of a coumarin based antihistamine as an anti filoviral entry inhibitor

DTIC Science & Technology

2017-06-20

Gharaibeh2, Tara Kenny2, Cary Retterer2, Rouzbeh Zamani2, Sina Bavari2, Norton P. Peet3 and Lijun Rong1 1. Department of Microbiology and Immunology...authors: Han Cheng, Department of Microbiology and Immunology, University of Illinois at Chicago, 8040 COMRB, 909 S. Wolcott Avenue, Chicago, IL 60612...Phone: (312)-996-0110 Fax: (312)- 996-6415 Email: hancheng@uic.edu Lijun Rong, Department of Microbiology and Immunology, University of Illinois at

ANTI-ULCER ACTIVITY OF THE ALKALI PREPARATION OF THE ROOT AND FRESH LEAF JUICE OF MORINGA OLEIFERA LAM

PubMed Central

Ruckmani, K.; Kavimani, S.; Jayakar, B.; Anandan, R.

1998-01-01

The alkali preparation of the root and fresh leaf juice of Moringa oleifera possessed significant dose –depen-dent anti-ulcer activity in experimentally induced acute gastric ulcers with aspirin, the anti-ulcer effect of the alkali preparation of the root seems to be more pronounced than that of the fresh leaf juice. Te anti-ulcer activity of the alkali preparation of the root could be due to its content of alkaloids or its anticholinergic and antihistaminic activities, or a combination of these factors. PMID:22556845

Poison ivy, oak, and sumac dermatitis identification, treatment, and prevention.

PubMed

Garner, L A

1999-05-01

Allergic contact dermatitis from poison ivy, oak, or sumac is common among people who work or exercise outdoors. The plants, classified in the genus Rhus or Toxicodendron, contain allergens that can cause reactions ranging from mild pruritus to severe urticaria or generalized maculopapular eruptions. Initial management includes cleansing, cold compresses, and, possibly, oral antihistamines for symptomatic relief. Topical corticosteroids are given for localized nonfacial eruptions; systemic corticosteroids are used for severe eruptions. Prevention involves avoiding contact with the plants and washing exposed skin within 2 hours.

Pruritus: an overview. What drives people to scratch an itch?

PubMed Central

Lavery, Michael Joseph; Kinney, Michael Owen; Mochizuki, Hideki; Craig, John

2016-01-01

Pruritus is a common complaint associated with many conditions. It negatively impacts sleep, quality of life, and mortality. Itch is transmitted along both histaminergic and non-histaminergic pathways with a complex interplay between keratinocytes, immune cells and cutaneous neurons. Individuals who present with pruritus should undergo a thorough assessment, especially those over 65 years old, to exclude underlying malignancy. Treatment no longer consists of antihistamines alone. Physicians now have an array of therapies in their armamentarium, to help alleviate this distressing symptom. PMID:27698518

Mechanisms of Radiation-Induced Conditioned Taste Aversion Learning

DTIC Science & Technology

1986-01-01

to Walter A. Hunt. 86 4 21 144 . J Jr -.W U *’ = 7 . 7 .: M: W. ,WLW;i , .-, -’ .’P. %k T .- - ’ .: ’W ; .a --,.-" -. t .:-. , 56 RABIN AND HUNT can...8217. 7m. U RADIATION-INDUCED TASTE AVERSIONS 57 induced CTA 11021. Alternatively, when the antihistamine is [ 21 . A radiation-induced CTA can be...in rats. Pharmmad psychioactive drugs. J (omp Phvsiod Pvchld .;’: 21 -26. 1972. Biochem Behav 17: 305-311. 1982. 4. Berger. B. D.. C. D. Wise and L

[Kounis syndrome: a paradoxal non-ST elevation myocardial infarction case after triamcinolone treatment for dermatitis].

PubMed

Yılmaz, Mücahid; Korkmaz, Hasan

2018-04-01

Kounis syndrome is defined as the clinical development of acute coronary syndrome caused by the activation of inflammatory cells due to an allergy, hypersensitivity, anaphylaxis, or anaphylactic reaction. Corticosteroids that are used in the treatment of many inflammatory conditions may paradoxically cause allergic reactions and even anaphylaxis. This article is a description of the case of a 52-yearold female patient who had a non-ST elevation myocardial infarction after the administration of triamcinolone that was relieved with antihistaminic treatment. The patient had been diagnosed with dermatitis at another medical center and injected with 40 mg/mL (intramuscular [IM]) of triamcinolone acetonide and developed chest pain 15 minutes after the first dose. Despite a normal physical examination and echocardiogram, laboratory tests revealed troponin positivity and an inferolateral ST depression was present on an electrocardiogram (ECG). The ECG findings and clinical symptoms resolved completely after conservative anti-ischemic treatment and antihistaminic therapy (pheniramine maleate 45.5 mg/2 mL, Avil ampoule, IV; Sanofi-Aventis, Paris, France) and coronary angiography evaluation of the arteries was normal. The heart, and in particular the coronary arteries, are among the organs that are most damaged during hypersensitivity reactions and anaphylaxis. Although Kounis syndrome is not a rare condition, few cases have been reported in clinical practice. The failure to recognize Kounis syndrome due to inadequately defined cases may lead to unwanted medical results. Kounis syndrome should be kept in mind in order to make a rapid and accurate diagnosis.

The use of a responder analysis to identify clinically meaningful differences in chronic urticaria patients following placebo- controlled treatment with rupatadine 10 and 20 mg.

PubMed

Giménez-Arnau, A; Izquierdo, I; Maurer, M

2009-09-01

According to the EAACI/GA(2)LEN/EDF guidelines for urticaria management, modern non-sedating H1-antihistamines are the first-line symptomatic treatment for chronic urticaria. Two previous randomized clinical trials demonstrated rupatadine efficacy and safety in chronic urticaria treatment. However, a responder analysis to identify clinically meaningful differences in patients with chronic urticaria has not yet been performed. This analysis includes the pooled data from two randomized, double-blind, placebo-controlled, multicentre studies in which chronic urticaria patients were treated with rupatadine at different doses. Responder rates were defined as the percentage of patients after 4 weeks of treatment who exhibited a reduction of symptoms by at least 50% or 75% as compared to baseline. The variables analysed were as follows: Mean Pruritus Score (MPS), Mean Number of Wheals (MNW), and Mean Urticaria Activity Score (UAS). A total of 538 patients were included. This responder analysis, using different response levels, shows that the efficacy of rupatadine 10 mg and 20 mg is significantly better as compared to placebo in the treatment of chronic urticaria patients. Notably, treatment with rupatadine 20 mg daily resulted in a higher percentage of patients with response of 75% symptom reduction or better than rupatadine 10 mg. Our results support the use of higher than standard doses of non sedating antihistamines in chronic urticaria. We strongly recommend performing and reporting responder analyses for established and new drugs used by patients with chronic urticaria.

Bilastine: in allergic rhinitis and urticaria.

PubMed

Carter, Natalie J

2012-06-18

Bilastine is an orally administered, second-generation antihistamine used in the symptomatic treatment of seasonal or perennial allergic rhinoconjunctivitis and urticaria. In two well designed phase III trials, 14 days' treatment with bilastine was associated with a significantly lower area under the effect curve (AUEC) for the reflective total symptom score (TSS) than placebo in patients with symptomatic seasonal allergic rhinitis. Additionally, reflective nasal symptom scores were significantly lower in bilastine than placebo recipients in patients with a history of seasonal allergic rhinitis who were challenged with grass pollen allergen in a single-centre, phase II study. Neither bilastine nor cetirizine was effective in the treatment of perennial allergic rhinitis with regard to the mean AUEC for reflective TSS in another well designed phase III trial. However, results may have been altered by differences in some baseline characteristics and placebo responses between study countries. In another well designed phase III trial, compared with placebo, bilastine was associated with a significantly greater change from baseline to day 28 in the mean reflective daily urticaria symptom score in patients with chronic urticaria. There were no significant differences in primary endpoint results between bilastine and any of the active comparators used in these trials (i.e. cetirizine, levocetirizine and desloratadine). Bilastine was generally well tolerated, with a tolerability profile that was generally similar to that of the other second-generation antihistamines included in phase III clinical trials.

The safety issues and hardware-related complications of deep brain stimulation therapy: a single-center retrospective analysis of 478 patients with Parkinson’s disease

PubMed Central

Zhang, Jing; Wang, Tao; Zhang, Chen-cheng; Zeljic, Kristina; Zhan, Shikun; Sun, Bo-min; Li, Dian-you

2017-01-01

Introduction Deep brain stimulation (DBS) is a well-established therapy for the treatment of advanced Parkinson’s disease (PD) in patients experiencing motor fluctuations and medication-refractory tremor. Despite the relative tolerability and safety of this procedure, associated complications and unnatural deaths are still unavoidable. Methods In this study, hardware-related complications and the causes of unnatural death were retrospectively analyzed in 478 patients with PD who were treated with DBS. Results The results showed a 3-year survival rate of 98.6% and a 5-year survival rate of 96.4% for patients with PD who underwent DBS treatment at the study center. Pneumonia was the cause of death with the highest frequency. Prophylactic antibiotics and steroids or antihistamine drugs were adopted to reduce the risk of infection. Twenty-two patients (4.6%) experienced hardware-related complications. Conclusion Deaths of PD patients who receive DBS are typically unrelated to the disease itself or complications associated with the surgery. Pneumonia, malignant tumors, asphyxia, and multiple-organ failure are the common causes of death. Swallowing-related problems may be the most important clinical symptom in late-stage PD, as they cannot be stabilized or improved by DBS alone, and are potentially lethal. Although prophylactic antibiotics and steroids or antihistamine drugs may reduce the risk of infection, it is imperative to identify high-risk patients for whom a therapeutic approach not requiring an implantable device is more suitable, for example, pallidotomy and potentially transcranial ultrasound. PMID:28652714

Systemic Contact Dermatitis.

PubMed

Aquino, Marcella; Rosner, Greg

2018-05-15

Systemic contact dermatitis (SCD) traditionally refers to a skin condition where an individual who is cutaneously sensitized to an allergen will subsequently react to that same allergen or a cross reacting allergen via a different route. It occurs to allergens including metals, medications, and foods. The exact pathophysiology underlying this disease remains unknown, although it appears to be mediated by type 4 hypersensitivity reactions and possibly type 3 hypersensitivity reactions. The p-I concept (pharmacologic interaction with immunoreceptors) hypothesized that drugs are able to bind directly to a T cell receptor without first being presented by MHC (major histocompatibility complex) molecules and without prior metabolism, which would help explain why SCD can be seen on first exposure to medications. Nomenclature remains a challenge as SCD can be subcategorized using terms such as ACDS (allergic contact dermatitis syndrome) and its four clinical stages, Baboon syndrome, and SDRIFE (symmetrical drug-related intertriginous and flexural exanthema), which share many overlapping features. Food allergens may be responsible for uncontrolled or persistent symptoms in patients with contact dermatitis who do not respond to topical avoidance. With medications, symptoms may be induced by topical application versus systemic administration. Patch testing (PT) may be beneficial in diagnosing SCD caused by metals and many topical medications including corticosteroids, antimicrobials (ampicillin, bacitracin, erythromycin, neomycin, nystatin), NSAIDs (diclofenac, ibuprofen), anesthetics, and antihistamines (chlorphenamine, piperazine). Current treatment options include topical steroids and oral antihistamines for symptom relief and dietary avoidance to causative foods or metals.

[The effect of a new antiparkinson agent, Selegilin, on psychomotor performance in humans].

PubMed

Müller-Limmroth, W

1985-01-01

A combination of tests consisting of a compensation task with differential value indication, a tachystoscopic arrangement with verbal identification of characteristic features and an arrangement for a visually induced motor reaction was carried out on 12 healthy volunteers aged from 20-30 to determine psychomotor efficiency under the influence of the new antiparkinson drug selegiline (Eldepryl). The results were compared with the effects of the psychostimulant fenetylline and the depressant-antihistamine chlorphenoxamine, and with a placebo. While fenetylline and chlorphenoxamine produced the anticipated effects with regard to an improvement or deterioration in performance in all parameters, selegiline resulted in a slightly longer motor reaction time and an increase in control errors, and in a significantly longer mental processing time. In comparison with the placebo, selegiline increased the motor reaction time by 0.8 +/- 1.95% and mental processing time by 4.1 +/- 1.7%. This depressant effect of selegiline, however, only attained 1/8 and 2/3, resp., of the sedative effect of the normal dose of the antihistamine chlorophenoxamine. Under the influence of chlorphenoxamine, performance becomes less regular and under fenetylline more regular. Selegiline does not differ significantly from the placebo. In spite of selegiline metabolites 1-metamphetamine and 1-amphetamine, which act as mild stimulants, the slightly depressant effect of selegiline detected can be explained by the increased effect of dopamine inhibitory neurons, particularly in the inhibitory system of the formatio reticularis and the cortex frontalis as a result of a concentration of dopamine.

Triprotic acid-base microequilibria and pharmacokinetic sequelae of cetirizine.

PubMed

Marosi, Attila; Kovács, Zsuzsanna; Béni, Szabolcs; Kökösi, József; Noszál, Béla

2009-06-28

(1)H NMR-pH titrations of cetirizine, the widely used antihistamine and four related compounds were carried out and the related 11 macroscopic protonation constants were determined. The interactivity parameter between the two piperazine amine groups was obtained from two symmetric piperazine derivatives. Combining these two types of datasets, all the 12 microconstants and derived tautomeric constants of cetirizine were calculated. Upon this basis, the conflicting literature data of cetirizine microspeciation were clarified, and the pharmacokinetic absorption-distribution properties could be interpreted. The pH-dependent distribution of the microspecies is provided.

Urticarial Reactions: Vascular Erythema, Urticaria, Vasculitis

PubMed Central

Sibbald, R. Gary

1987-01-01

Vascular erythemas, including urticaria and vasculitis, represent diagnostic and therapeutic challenges. A careful systemic approach to history and physical examination should be followed by appropriate investigations to rule out systemic disease. Chronic urticaria patients should be physically tested to identify cholinergic, dermagraphic, and cold-induced responses. Food diaries and careful drug history may be important to identify exacerbating factors in chronic urticaria. A skin biopsy is necessary to diagnose vasculitis. Therapy of any underlying cause is supplemented with H1 antihistamines in urticaria patients, while vasculitis requires a different anti-inflammatory approach. PMID:21263956

Antihistaminic and antieicosanoid effects of oleanolic and ursolic acid fraction from Helichrysum picardii.

PubMed

Santos Rosa, C; García Gimenez, M D; Saenz Rodriguez, M T; De la Puerta Vazquez, R

2007-06-01

Helichrysum picardii Boiss. & Reuter is a Mediterranean vegetal species from the Asteraceae family. From the methanolic extract of the aerial flowering parts of this plant, a fraction of two pentacyclic triterpenes has been isolated. Gas chromatography revealed that the triterpene isomers ursolic and oleanolic acids comprised 69% and 29% respectively of the composition of this fraction. The triterpene isomeric fraction was tested in two phagocyte cell systems. It inhibited compound 48/80-induced histamine release from rat peritoneal mast cells in an approximately percentage of 45% at 100 microM and myeloperoxidase secretion from A23187-ionophore-stimulated rat peritoneal leukocytes in a significant manner at doses of 50 and 100 miroM. Furthermore, the triterpene isomers very significantly and dose-dependently inhibited generation of the cyclo-oxygenase metabolite prostaglandin E2 (41% inhibition at 50 miroM) and the 5-lipoxygenase metabolite leukotriene B4 (79% inhibition at 50 microM) from activated rat leukocytes. This anti-eicosanoid activity of the triterpene fraction was more potent than that produced by the pure triterpene oleanolic acid used for comparision, indicating a stronger action of the ursolic acid, the major compound of the isolated triterpene fraction. From these data, it can be suggested that the triterpene isomers oleanolic and ursolic acids present in the medicinal plant Helichrysum picardii contribute to the anti-inflammatory profile of this vegetal species.

Over-the-Counter Agents for the Treatment of Occasional Disturbed Sleep or Transient Insomnia: A Systematic Review of Efficacy and Safety

PubMed Central

Culpepper, Larry; Wingertzahn, Mark A.

2015-01-01

Objective: To investigate the level of evidence supporting the use of common over-the-counter (OTC) agents (diphenhydramine, doxylamine, melatonin, and valerian) for occasional disturbed sleep or insomnia. Data sources: A systematic review of the literature was conducted on July 31, 2014, using MEDLINE (PubMed) and the search terms (insomnia OR sleep) AND (over*the*counter OR OTC OR non*prescription OR antihistamine OR doxylamine OR diphenhydramine OR melatonin OR valerian) with the filters English, human, and clinical trials. Study selection: Identified publications (from 2003 to July 31, 2014, following previous published literature reviews) that met the inclusion criteria were selected. The criteria included randomized placebo-controlled clinical studies that utilized overnight objective (polysomnography) or next-day participant-reported sleep-related endpoints and that were conducted in healthy participants with or without occasional disturbed sleep or diagnosed insomnia. Results: Measures of efficacy and tolerability were summarized for each study individually and grouped according to OTC agent: H1 antagonists or antihistamines (3 studies, diphenhydramine), melatonin (8), and valerian or valerian/hops (7). Of the 3 sleep agents, studies conducted with melatonin, especially prolonged-release formulations in older individuals with diagnosed insomnia, demonstrated the most consistent beneficial effects (vs placebo) on sleep measures, specifically sleep onset and sleep quality, with favorable tolerability. In contrast, the clinical trial data for diphenhydramine, immediate-release melatonin, and valerian suggested limited beneficial effects. Conclusions: A review of randomized controlled studies over the past 12 years suggests commonly used OTC sleep-aid agents, especially diphenhydamine and valerian, lack robust clinical evidence supporting efficacy and safety. PMID:27057416

Repeated-dose effects of mequitazine, cetirizine and dexchlorpheniramine on driving and psychomotor performance.

PubMed

Theunissen, Eef L; Vermeeren, Annemiek; Ramaekers, Johannes G

2006-01-01

Previous studies have demonstrated that the antihistamines mequitazine, cetirizine and dexchlorpheniramine produce mild sedation after single doses. It is unknown, however, whether acute sedation persists after repeated dosing. Therefore, this study assessed the effects of repeated dosing of these antihistamines on driving and psychomotor performance. Sixteen healthy volunteers were treated with mequitazine 10 mg q.a.m., cetirizine 10 mg q.a.m., dexchlorpheniramine Repetab 6 mg b.i.d. and placebo for four separate 8-day periods. Drug effects were assessed on days 1 and 8 using on-the-road driving tests (highway driving and car following), psychomotor tests (tracking and divided attention) and subjective questionnaires. Dexchlorpheniramine and mequitazine significantly impaired driving performance on the highway driving test on the first day; dexchlorpheniramine increased Standard Deviation of Lateral Position by 2 cm [95% confidence interval (CI) 0.5, 3.8] and mequitazine by 2.5 cm (CI 1.0, 4.3). These effects on driving performance disappeared after 8 days of treatment. No effect of treatment was found on car following, tracking and divided attention. Although subjective ratings confirmed that subjects knew their driving had been impaired in the mequitazine and dexchlorpheniramine condition after completion of the highway driving test on day 1, they did not expect their driving to be affected before the start of the test. Cetirizine did not impair performance on any of the tests. Single doses of mequitazine 10 mg and dexchlorpheniramine Repetab 6 mg cause mild driving impairment. However, when taken over several days, the impairing effect wears off, possibly as a result of tolerance.

Allergies are associated with arterial changes in young children.

PubMed

Evelein, Annemieke M V; Visseren, Frank L J; van der Ent, Cornelis K; Grobbee, Diederick E; Uiterwaal, Cuno S P M

2015-11-01

Inflammation is important in atherosclerosis development. Whether common causes of inflammation, such as allergies and infections, already exert this influence in early childhood is unknown. The objective of this study was to investigate the association between both allergies and infections with children's vasculature. This was a longitudinal study in a general population cohort. In 390 five-year-olds of the WHISTLER (Wheezing-Illnesses-Study-LEidsche-Rijn) birth cohort, carotid intima-media thickness (CIMT) and arterial stiffness were obtained ultrasonographically. Physician-diagnosed allergies and infections and recent prescriptions of systemic antihistamines and antibiotics were obtained, as well as parental history of allergies. General linear regression was performed with vascular characteristics as dependent variables and measures of inflammation as independent variables. Having both a positive parental history of allergy and an allergy diagnosis showed 15.0 µm (95% confidence interval (CI): 2.3-27.8, p = 0.02) larger CIMT than not having such history and diagnosis. Having a positive parental history of allergy only showed 11.9 µm (0.87-23.0, p = 0.04) larger CIMT. Recent use of antihistamines and antibiotics showed 18.8 µm (1.6-35.9, p = 0.03) and 16.1 µm (4.5-27.7, p = 0.01) larger CIMT, respectively. Childhood infections were not clearly related to vascular parameters. Neither allergy nor infections were associated with arterial stiffness. An allergic predisposition is already associated with thicker arterial walls in early childhood. © The European Society of Cardiology 2014.

[Pharmacotherapy of urticaria--an analysis of the discrepancies between guidelines of expert bodies, registration documents and evidence for the effectiveness of drugs].

PubMed

Plichta, Danuta; Spiewak, Radosław

2013-01-01

The year 2012 has seen relevant changes in Polish pharmaceutical legislation and drug reimbursement, among others limiting the reimbursement solely to indications stated in the Summaries of Product Characteristics (SPCs). A discrepancy with expert recommendations became apparent. The aim of this study was to analyze discordances between up-to-date expert recommendations, the SPCs in force, and the evidence for the effectiveness of recommended drugs in urticaria. Guidelines for the treatment of urticaria issued by Polish and international expert bodies were analyzed, along with the SPCs. A systematic review of clinical trials of recommended drugs was carried out. Of drugs recommended by the experts, 203 were authorized in Poland for urticaria treatment, including 167 oral preparations of second-generation antihistamines (SGAH, 8 active substances), 29 oral preparations of first-generation antihistamines (6 substances), 4 preparations of systemic glucocorticosteroids (2), 2 topical glucocorticosteroid preparations (2) and one combined preparation of human immunoglobulin with histamine. Among products both recommended by experts and licensed for the treatment of urticaria in Poland, high or moderate-level of evidence of effectiveness was available for 7 active substances (bilastine, cetirizine, desloratadine, fexofenadine, loratadine, levocetirizine, rupatadine). Nevertheless, 39% of SGAH available in Poland (66 preparations of cetirizine, emedastine, levocetirizine, loratadine or fexofenadine) were registered exclusively for "chronic idiopathic urticaria" - a diagnosis inconsistent with the current state of medical knowledge. We conclude that there exist considerable discrepancies between expert recommendations for the pharmacotherapy of urticaria, the licensed use of drugs as defined in Summaries of Product Characteristics and scientific evidence for their effectiveness.

Management of chronic spontaneous urticaria in the elderly.

PubMed

Ventura, Maria Teresa; Cassano, Nicoletta; Romita, Paolo; Vestita, Michelangelo; Foti, Caterina; Vena, Gino Antonio

2015-04-01

The guidelines for the management of urticaria in adults and children have been revised and updated recently. However, there are few data in the literature concerning several aspects of this disease in the elderly (e.g., epidemiology, etiopathogenesis, clinical aspects, association with co-morbidities, efficacy and safety profiles of treatments, and management strategies). This is an obvious deficiency in the data, as this disease causes a deterioration in quality of life, affecting the quality of sleep, everyday life habits and activities, and inducing severe disability. Chronic spontaneous urticaria (CSU) can also be associated with internal, infectious, autoimmune, or neoplastic diseases. It is therefore necessary to pay particular attention to these clinical issues through appropriate clinical examinations. At the same time, the specific features of medications used to treat CSU in the elderly should be carefully evaluated, as its pharmacological treatment raises a number of problems related both to the clinical condition of the patient and to concomitant diseases, as well as to the polypharmacotherapy, which is common in older subjects and may cause safety problems because of the drug interactions. Non-sedating new-generation antihistamines are the mainstay treatment of CSU for the elderly. The efficacy and safety of alternative treatment options have not been assessed in the geriatric population with CSU; corticosteroids and cyclosporine (ciclosporin) should be used by this population with extreme caution. Similarly, there are no data regarding the actual safety profile of the new-generation antihistamines at higher doses than those recommended in elderly patients.

Chapter 5: Allergic rhinitis.

PubMed

Uzzaman, Ashraf; Story, Rachel

2012-01-01

Rhinitis is a symptomatic inflammatory disorder of the nose with different causes such as allergic, nonallergic, infectious, hormonal, drug induced, and occupational and from conditions such as sarcoidosis and necrotizing antineutrophil cytoplasmic antibodies positive (Wegener's) granulomatosis. Allergic rhinitis affects up to 40% of the population and results in nasal (ocular, soft palate, and inner ear) itching, congestion, sneezing, and clear rhinorrhea. Allergic rhinitis causes extranasal untoward effects including decreased quality of life, decreased sleep quality, obstructive sleep apnea, absenteeism from work and school, and impaired performance at work and school termed "presenteeism." The nasal mucosa is extremely vascular and changes in blood supply can lead to obstruction. Parasympathetic stimulation promotes an increase in nasal cavity resistance and nasal gland secretion. Sympathetic stimulation leads to vasoconstriction and consequent decrease in nasal cavity resistance. The nasal mucosa also contains noradrenergic noncholinergic system, but the contribution to clinical symptoms of neuropeptides such as substance P remains unclear. Management of allergic rhinitis combines allergen avoidance measures with pharmacotherapy, allergen immunotherapy, and education. Medications used for the treatment of allergic rhinitis can be administered intranasally or orally and include oral and intranasal H(1)-receptor antagonists (antihistamines), intranasal and systemic corticosteroids, intranasal anticholinergic agents, and leukotriene receptor antagonists. For intermittent mild allergic rhinitis, an oral or intranasal antihistamine is recommended. In individuals with persistent moderate/severe allergic rhinitis, an intranasal corticosteroid is preferred. When used in combination, an intranasal H(1)-receptor antagonist and a nasal steroid provide greater symptomatic relief than monotherapy. Allergen immunotherapy is the only disease-modifying intervention available.

Comparison of efficacy, safety, and cost-effectiveness of montelukast-levocetirizine and montelukast-fexofenadine in patients of allergic rhinitis: A randomized, double-blind clinical trial.

PubMed

Mahatme, Mohini Sachin; Dakhale, Ganesh Natthuji; Tadke, Kanchan; Hiware, Sachin Keshaorao; Dudhgaonkar, S D; Wankhede, Sumit

2016-01-01

Allergic rhinitis (AR) is a global health problem. Almost 10%-25% of population worldwide is affected by AR. Oral/intranasal H1-antihistamine, decongestants, leukotriene receptor antagonists, and intranasal corticosteroids are the pillars in the management of AR. The combination therapy of montelukast with antihistaminic provides enhancing and complimentary effects, thereby reducing the symptoms effectively, but there are scanty data regarding the comparisons of combinations. Therefore, we aimed to compare the efficacy, safety, and cost-effectiveness of montelukast-levocetirizine and montelukast-fexofenadine combination in patients of AR. Seventy patients with AR participated in a prospective, randomized, double-blind, parallel, active-controlled, comparative 4-week trial. The patients between the age group of 18-65 years of either gender having moderate-severe intermittent or mild persistent AR were included in the study. The study inclusion criteria required the patients with total nasal symptom score (TNSS) of 5 or higher. The patients were randomly divided into two treatment groups with montelukast-levocetirizine (10 mg and 5 mg) in one group and montelukast-fexofenadine (10 mg and 120 mg) in another group. TNSS parameter was the main effectiveness parameter. Evaluation of TNSS revealed significant difference ( P < 0.05) when compared from baseline to 4 th week in both groups. The mean change of TNSS, i.e., 9.46 was significant ( P < 0.05) in montelukast-fexofenadine group. The cost-effectiveness ratio was less in montelukast-levocetirizine group than in montelukast-fexofenadine group. The decrease in TNSS was more in montelukast-fexofenadine group, but the cost-effectiveness is more with montelukast-levocetirizine combination.

Patient assessment of onset of action and overall satisfaction with ebastine fast-dissolving tablets in allergic rhinitis.

PubMed

Roger, Albert; Fortea, Josep; Mora, Sheila; Artés, Maite

2008-08-01

To evaluate patient perception of the onset of action and overall satisfaction with a fast-dissolving tablet (FDT) formulation of ebastine in patients with intermittent or persistent allergic rhinitis. This was a cross-sectional, multicenter, pharmacy-based survey involving adult patients (>18 years) with allergic rhinitis who presented with a prescription for ebastine FDT. Via a telephone interview, patients were asked to evaluate the characteristics of ebastine FDT in comparison with their previous experience with other antihistamines. 100 patients with allergic rhinitis were included in the study (41 had intermittent disease, 57 persistent disease and two with unknown disease states). Patients rated ebastine FDT very highly (mean scores: 4.5-4.7 out of a possible 5) for all characteristics related to convenience, such as easy to take, easy to carry around in a bag or pocket, suitable for taking anytime/anywhere, and convenient to use. A total of 85% of patients perceived ebastine FDTs onset of action to be fast or very fast, and 77% indicated that it acted faster than their usual antihistamine. A total of 96% were satisfied or very satisfied with ebastine FDT and 98% were interested in using the drug again. Patients with rhinitis rate ebastine FDT very highly in terms of its formulation, convenience of use and its rapid onset of action. These characteristics resulted in a high level of individual satisfaction with the new formulation and a clear preference by the majority of patients to use ebastine FDT in the future.

[Pseudoallergies].

PubMed

Bernardini, R; Novembre, E; Lombardi, E; Monaco, M G; Monte, M T; Pucci, N; Rossi, M E; Vierucci, A

2001-01-01

Pseudo-allergic-reactions (PAR) are clinical manifestations including urticaria, angioedema, conjunctivitis, rhinitis, asthma, and anaphylaxis. The prevalence of PAR ranges from 0.1% to 75% according to various studies. The pathogenetic mechanism of these diseases is not immunologically mediated. Food, additives, and drugs are the main responsibilities for PAR. The diagnosis of PAR is characterized by the absence of specific IgE for the suspected products. The absence of immunological mechanisms is confirmed by in vitro and in vivo tests. The treatment of PAR is similar to that of allergic diseases (antihistamine drugs, steroids, B2 agonists, epinephrine).

[Intrasal corticosteriods prescription to allergic rhinoconjunctivitis and rhinosinusitis during pediatric ages].

PubMed

Sacre Hazouri, José Antonio; de la Torre González, Carlos; López González, Ana Luisa; Alvarez Vega, Ricardo

2007-01-01

The different diseases that affect the upper respiratory tract, like allergic rhinitis, rhinoconjunctivitis, and rhinosinusitis have inflammation as their main pathophysiological component. Affects approximately 25% of the adults and 40% of the children. Intranasal corticosteroids (INSs) are considered the most effective treatment for the management of allergic rhinoconjunctivitis. Unlike antihistamines or antileukotrienes, INSs have a more profound effect on nasal congestion and the related sleep disturbance and daytime somnolence resulting from nasal congestion that affect their everyday quality of life. We review INSs mechanism of action, pharmacological properties of the different INSs, their therapeutic use and give our suggestions for their proper use.

Antinauseants in Pregnancy: Teratogens or Not?

PubMed Central

Biringer, Anne

1984-01-01

Nausea and/or vomiting affect 50% of all pregnant women. For most women, this is a self-limited problem which responds well to conservative management. However, there are some situations where the risk to the mother and fetus posed by the illness are greater than the possible risks of teratogenicity of antinauseant drugs. Antihistamines have had the widest testing, and to date, there has been no evidence linking doxylamine, dimenhydrinate or promethazine to congenital malformations. Since no available drugs have official approval for use in nausea and vomiting of pregnancy the physician is left alone to make this difficult decision. PMID:21279128

Keratoconjunctivitis and Periorbital Edema due to Ecballium elaterium.

PubMed

Brouzas, Dimitrios; Oanta, Mariana; Loukianou, Eleni; Moschos, Marillita

2012-01-01

To report on a case of keratoconjunctivitis with periorbital edema after accidental exposure to undiluted juice of Ecballium elaterium fruit during the ripening season of this plant. Case report. Keratoconjunctivitis with Descemet's membrane folds and superficial upper corneal well-defined edematous areas were noted after an Ecballium elaterium fruit burst and its juice splashed into the patient's left eye. Prompt administration of antibiotic and steroid eye drops along with per os antihistamine therapy, resulted in quick regression of symptoms. This report demonstrates the toxic effects of this herb to the eye and also that prompt therapy is effective.

Intoxications from the seas: ciguatera, scombroid, and paralytic shellfish poisoning.

PubMed

Sanders, W E

1987-09-01

Sporadic cases and outbreaks of intoxications borne by fish and shellfish have increased in frequency during recent years. Ciguatera, scombroid, and paralytic shellfish poisoning account for nearly 16 per cent of all reported foodborne outbreaks of disease in the United States. Fishborne ciguatera and paralytic shellfish poisoning are characterized by gastrointestinal and neuromuscular manifestations attributable to toxins of dinoflagellates. These toxins impair sodium transport in cell membranes. Treatment is primarily supportive. Scombroid fish intoxication resembles histamine poisoning and may be treated effectively with antihistamines or cimetidine. Prevention of these intoxications at present depends upon avoidance of potential vectors.

Flushing syndrome due to mahimahi (scombroid fish) poisoning.

PubMed

Kim, R

1979-08-01

Scombroid fish poisoning, one of the most common adverse reactions to fish, is also probably one of the most common causes of a flushing syndrome. The reaction usually involves fishes of the Scombridae family but, in Hawaii, the reaction is most often due to mahimahi (Coryphaena hippurus). Onset of the reaction is usually abrupt and commonly associated with a prominent flush resembling a sunburn. Headache, tachye to a toxin with histamine-like properties, which is formed because improper refrigeration enables endogenous bacteria to decarboxylate histidine normally present in dark-meat fishes. Symptoms are usually promptly relieved by parenteral antihistamine therapy.

Phytochemicals and bioactivities of Anemone raddeana Regel: a review.

PubMed

Sun, Yong-Xu; Liu, Ji-Cheng; Liu, Da-You

2011-11-01

Anemone raddeana, usually called as'"Toujian Liang" in China, is an Anemone herb belonging to the Ranunculaceae family. Until now there are in total 67 of chemical components identified including triterpenoids, steroids, lactones, fats and oils, saccharide and alkaloids. A broad spectrum of pharmacological activity of A. raddeana compounds have been reported, such as antitumor, antimicrobial, anti-inflammatory, sedative and analgesic activites, as well as anti-convulsant and anti-histamine effects. In view of this, we initiated this short review to present the phytochemical and pharmacological profile of A. raddeana to support future studies in this discipline.

Orexin receptor antagonist-induced sleep does not impair the ability to wake in response to emotionally salient acoustic stimuli in dogs

PubMed Central

Tannenbaum, Pamela L.; Stevens, Joanne; Binns, Jacquelyn; Savitz, Alan T.; Garson, Susan L.; Fox, Steven V.; Coleman, Paul; Kuduk, Scott D.; Gotter, Anthony L.; Marino, Michael; Tye, Spencer J.; Uslaner, Jason M.; Winrow, Christopher J.; Renger, John J.

2014-01-01

The ability to awaken from sleep in response to important stimuli is a critical feature of normal sleep, as is maintaining sleep continuity in the presence of irrelevant background noise. Dual orexin receptor antagonists (DORAs) effectively promote sleep across species by targeting the evolutionarily conserved wake-promoting orexin signaling pathway. This study in dogs investigated whether DORA-induced sleep preserved the ability to awaken appropriately to salient acoustic stimuli but remain asleep when exposed to irrelevant stimuli. Sleep and wake in response to DORAs, vehicle, GABA-A receptor modulators (diazepam, eszopiclone and zolpidem) and antihistamine (diphenhydramine) administration were evaluated in telemetry-implanted adult dogs with continuous electrocorticogram, electromyogram (EMG), electrooculogram (EOG), and activity recordings. DORAs induced sleep, but GABA-A modulators and antihistamine induced paradoxical hyperarousal. Thus, salience gating studies were conducted during DORA-22 (0.3, 1, and 5 mg/kg; day and night) and vehicle nighttime sleep. The acoustic stimuli were either classically conditioned using food reward and positive attention (salient stimulus) or presented randomly (neutral stimulus). Once conditioned, the tones were presented at sleep times corresponding to maximal DORA-22 exposure. In response to the salient stimuli, dogs woke completely from vehicle and orexin-antagonized sleep across all sleep stages but rarely awoke to neutral stimuli. Notably, acute pharmacological antagonism of orexin receptors paired with emotionally salient anticipation produced wake, not cataplexy, in a species where genetic (chronic) loss of orexin receptor signaling leads to narcolepsy/cataplexy. DORA-induced sleep in the dog thereby retains the desired capacity to awaken to emotionally salient acoustic stimuli while preserving uninterrupted sleep in response to irrelevant stimuli. PMID:24904334

Management of chronic spontaneous urticaria in routine clinical practice: A Delphi-method questionnaire among specialists to test agreement with current European guidelines statements.

PubMed

Giménez-Arnau, A; Ferrer, M; Bartra, J; Jáuregui, I; Labrador-Horrillo, M; Frutos, J Ortiz de; Silvestre, J F; Sastre, J; Velasco, M; Valero, A

Chronic spontaneous urticaria (CSU) is a frequent clinical entity that often presents a diagnostic and therapeutic challenge. To explore the degree of agreement that exists among the experts caring for patients with CSU diagnosis, evaluation, and management. An online survey was conducted to explore the opinions of experts in CSU, address controversial issues, and provide recommendations regarding its definition, natural history, diagnosis, and treatment. A modified Delphi method was used for the consensus. The questionnaire was answered by 68 experts (dermatologists, allergologists, and primary care physicians). A consensus was reached on 54 of the 65 items posed (96.4%). The experts concluded that CSU is a difficult-to-control disease of unpredictable evolution. Diagnostic tests should be limited and based on clinical history and should not be indiscriminate. Autoinflammatory syndromes and urticarial vasculitis must be ruled out in the differential diagnosis. A cutaneous biopsy is only recommended when wheals last more than 24h, to rule out urticarial vasculitis. The use of specific scales to assess the severity of the disease and the quality of life is recommended. In patients with severe and resistant CSU, second-generation H1-antihistamines could be used at doses up to four times the standard dose before giving second-line treatments. Omalizumab is a safe and effective treatment for CSU that is refractory to H1-antihistamines treatment. In general, diagnosis and treatment recommendations given for adults could be extrapolated to children. This work offers consensus recommendations that may be useful in the management of CSU. Copyright © 2016 SEICAP. Published by Elsevier España, S.L.U. All rights reserved.

[Diagnostic and Therapeutic Approach of Chronic Spontaneous Urticaria: Recommendations in Portugal].

PubMed

Costa, Célia; Gonçalo, Margarida

2016-11-01

Chronic spontaneous urticaria is a complex disorder, of unclear etiology, easily diagnosed although often difficult to treat. It has a significant impact on the patients' quality of life and results in high direct and indirect costs. The diagnosis of chronic spontaneous urticaria is mainly clinical and a limited number of tests is recommended for differential diagnosis and/or for the investigation/exclusion of possible causes. In addition to the complete blood count and C-reactive protein, and/or erythrocyte sedimentation rate, additional tests must be selected according to clinical criteria. The aim of therapy is the complete clinical control of chronic spontaneous urticaria. Evolution should be documented by weekly symptom scoring - Weekly Urticaria Activity Score (UAS7) -, as well as the assessment of quality of life. The therapeutic approach is based on second-generation H1 antihistamines (anti-H1) administered continuously in the approved doses (first line), and, in the absence of a clinical response, up to four times the daily-approved dose (second line). First generation H1 antihistamines are not recommended. Approximately 30% of patients are not controlled with second line therapy, and it is recommended to add a third line therapy. Of the two options, omalizumab and cyclosporine, only omalizumab is approved for chronic spontaneous urticaria and has a better safety profile, thus being preferably recommended. In Portugal there are no national-based recommendations applicable to clinical practice. The elaboration of these recommendations is justified by the need to standardize both the diagnosis and the treatment approach of patients with chronic spontaneous urticaria in Portugal, and for the referral of patients to specialized centers, in the most severe cases.

Wastewater treatment plants as a pathway for aquatic contamination by pharmaceuticals in the ebro river basin (northeast Spain).

PubMed

Gros, Meritxell; Petrović, Mira; Barceló, Damià

2007-08-01

The occurrence of 28 pharmaceuticals of major human consumption in Spain, including analgesics and anti-inflammatories, lipid regulators, psychiatric drugs, antibiotics, antihistamines, and beta-blockers, was assessed along the Ebro river basin, one of the biggest irrigated lands in that country. Target compounds were simultaneously analyzed by off-line solid-phase extraction, followed by liquid chromatography-tandem mass spectrometry. The loads of detected pharmaceuticals and their removal rates were studied in seven wastewater treatment plants (WWTPs) located in the main cities along the basin. Total loads ranged from 2 to 5 and from 0.5 to 1.5 g/d/1,000 inhabitants in influent and effluent wastewaters, respectively. High removal rates (60-90%) were achieved mainly for analgesics and anti-inflammatories. The other groups showed lower rates, ranging from 20 to 60%, and in most cases, the antiepileptic carbamazepine, macrolide antibiotics, and trimethoprim were not eliminated at all. Finally, the contribution of WWTP effluents to the presence of pharmaceuticals in receiving river waters was surveyed. In receiving surface water, the most ubiquitous compounds were the analgesics and anti-inflammatories ibuprofen, diclofenac, and naproxen; the lipid regulators bezafibrate and gemfibrozil; the antibiotics erythromycin, azithromycin, sulfamethoxazole, trimethoprim, and less frequently, ofloxacin; the antiepileptic carbamazepine; the antihistamine ranitidine; and the beta-blockers atenolol and sotalol. Although levels found in WWTP effluents ranged from low microg/L to high ng/L, pharmaceuticals in river waters occurred at levels at least one order of magnitude lower (low ng/L range) because of dilution effect. From the results obtained, it was proved that WWTP are hot spots of aquatic contamination concerning pharmaceuticals of human consumption.

Cultured smooth muscle cells of the human vesical sphincter are more sensitive to histamine than are detrusor smooth muscle cells.

PubMed

Neuhaus, Jochen; Oberbach, Andreas; Schwalenberg, Thilo; Stolzenburg, Jens-Uwe

2006-05-01

To compare histamine receptor expression in cultured smooth muscle cells from the human detrusor and internal sphincter using receptor-specific agonists. Smooth muscle cells from the bladder dome and internal sphincter were cultured from 5 male patients undergoing cystectomy for bladder cancer therapy. Calcium transients in cells stimulated with carbachol, histamine, histamine receptor 1 (H1R)-specific heptanecarboxamide (HTMT), dimaprit (H2R), and R-(alpha)-methylhistamine (H3R) were measured by calcium imaging. Histamine receptor proteins were detected by Western blot analysis and immunocytochemistry. H1R, H2R, and H3R expression was found in tissue and cultured cells. Carbachol stimulated equal numbers of detrusor and sphincter cells (60% and 51%, respectively). Histamine stimulated significantly more cells than carbachol in detrusor (100%) and sphincter (99.34%) cells. Calcium responses to carbachol in detrusor and sphincter cells were comparable and did not differ from those to histamine in detrusor cells. However, histamine and specific agonists stimulated more sphincter cells than did carbachol (P <0.001), and the calcium increase was greater in sphincter cells than in detrusor cells. Single cell analysis revealed comparable H2R responses in detrusor and sphincter cells, but H1R and H3R-mediated calcium reactions were significantly greater in sphincter cells. Histamine very effectively induces calcium release in smooth muscle cells. In sphincter cells, histamine is even more effective than carbachol regarding the number of reacting cells and the intracellular calcium increase. Some of the variability in the outcome of antihistaminic interstitial cystitis therapies might be caused by the ineffectiveness of the chosen antihistaminic or unintentional weakening of sphincteric function.

Distilled water nasal provocation in hyperreactive patients.

PubMed

Baudoin, T; Anzic, S A; Kalogjera, L

1999-01-01

Nonisotonic aerosol may act as a provocation agent in the upper and lower airways of hyperreactive individuals. The purpose of the study was to compare the results of nasal challenge with distilled water in patients with allergic rhinitis to those with noninfective nonallergic rhinitis (NINAR), with respect to the potential clinical use of the obtained data. A group of 68 ambulatory patients with allergic rhinitis or NINAR (39 perennial allergic, 6 seasonal, 23 NINAR) were challenged with 10 mL of distilled water aerosol after the baseline active anterior rhinomanometry. Patients with nasal polyposis at endoscopy, significant unilateral septal deviation, positive bacteriologic swab, recent nasal surgery, and uncertain anamnestic data about the medication taken 6 weeks before the provocation were excluded from the study. After 10 minutes of nasal provocation, rhinomanometry was repeated to assess the response. In 15 patients of the perennial allergic group, the same measurements were performed after a 2-week oral antihistamine and topical steroid therapy. Nasal resistance was significantly increased on the more patent side of the nose after nasal provocation with distilled water aerosol in allergic patients in comparison to the nasal resistance before provocation. In the patients with NINAR, the provocation resulted in a significant rise on the more patent side, but the total nasal airway resistance (NAR) levels were also significantly increased. The systemic antihistamine and topical steroid 2-week therapy in patients with perennial allergic rhinitis significantly reduced the response to nasal distilled water provocation. Nasal provocation with distilled water aerosol is a cheap, simple, and acceptable method that provides useful clinical data on the level of nonspecific nasal hyperreactivity and the therapy success.

Histamine H1-receptor antagonists against Leishmania (L.) infantum: an in vitro and in vivo evaluation using phosphatidylserine-liposomes.

PubMed

Pinto, Erika G; da Costa-Silva, Thais A; Tempone, Andre Gustavo

2014-09-01

Considering the limited and toxic therapeutic arsenal available for visceral leishmaniasis (VL), the drug repositioning approach could represent a promising tool to the introduction of alternative therapies. Histamine H1-receptor antagonists are drugs belonging to different therapeutic classes, including antiallergics and anxyolitics. In this work, we described for the first time the activity of H1-antagonists against L. (L.) infantum and their potential effectiveness in an experimental hamster model. The evaluation against promastigotes demonstrated that chlorpheniramine, cinnarizine, hydroxyzine, ketotifen, loratadine, quetiapine and risperidone exerted a leishmanicidal effect against promastigotes, with IC50 values in the range of 13-84μM. The antihistaminic drug cinnarizine demonstrated effectiveness against the intracellular amastigotes, with an IC50 value of 21μM. The mammalian cytotoxicity was investigated in NCTC cells, resulting in IC50 values in the range of 57-229μM. Cinnarizine was in vivo studied as a free formulation and entrapped into phosphatidylserine-liposomes. The free drug was administered for eight consecutive days at 50mg/kg by intraperitoneal route (i.p.) and at 100mg/kg by oral route to L. infantum-infected hamsters, but showed lack of effectiveness in both regimens, as detected by real time PCR. The liposomal formulation was administered by i.p. route at 3mg/kg for eight days and reduced the parasite burden to 54% in liver when compared to untreated group; no improvement was observed in the spleen of infected hamsters. Cinnarizine is the first antihistaminic drug with antileishmanial activity and could be used as scaffold for drug design studies for VL. Copyright © 2014 Elsevier B.V. All rights reserved.

Adrenaline in anaphylaxis treatment and self-administration: experience from an inner city emergency department.

PubMed

Mostmans, Y; Grosber, M; Blykers, M; Mols, P; Naeije, N; Gutermuth, J

2017-03-01

Anaphylaxis is a life-threatening emergency of which reliable epidemiological data are lacking. This study aimed to analyze how quickly patients presenting with anaphylaxis were treated in emergency and whether treatment followed the European Academy of Allergy and Clinical Immunology (EAACI) guidelines. Patient data were collected between April 2009 and April 2013. Emergency doctors completed a questionnaire for adult patients presenting at the emergency department (ED) of the St. Pierre hospital in Brussels with anaphylaxis. Inclusion criteria were based on the Sampson criteria of anaphylaxis. Data were analyzed using a Microsoft Excel database. About 0.04% (100/230878) of all emergency visits in adults presented with anaphylaxis. 64% of patients received their first medical help later than 30 min after symptom onset. 67% of patients received adrenaline, 85% oral antihistamines, and 89% received IV glucocorticosteroids. 46/100 patients were discharged directly from the ED, of which 87% received further medical prescriptions for self-administration: 67% corticosteroids, 83% antihistamines, and 9% intramuscular adrenaline. 74% were instructed to consult an allergologist for adequate diagnosis. 54/100 patients were hospitalized. The majority of patients were treated according to the EAACI guidelines for management of anaphylaxis, but only a minority received the recommended adrenaline auto-injector for self-administration at discharge. Because the majority of patients received medical help later than 30 min after symptom onset, adrenaline auto-injector prescription is a necessity. The low rate of doctors prescribing adrenaline auto-injectors in the ED setting underlines the need to train doctors of various backgrounds in prevention and treatment of anaphylaxis and the close collaboration with allergologists. © 2016 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

Grapefruit juice reduces the oral bioavailability of fexofenadine but not desloratadine.

PubMed

Banfield, Christopher; Gupta, Samir; Marino, Mark; Lim, Josephine; Affrime, Melton

2002-01-01

Certain foods, such as grapefruit juice, are known to substantially alter the bioavailability of some drugs. These effects may be mediated by interactions with enzyme systems, such as cytochrome P450, or with active transporter systems, such as P-glycoprotein and organic anion transporting polypeptides. To assess the effect of consumption of grapefruit juice on the oral bioavailability of two nonsedating antihistamines, fexofenadine and desloratadine. Non-blinded, randomised, single-dose, four-way crossover study. Twenty-four healthy adult volunteers. Single oral doses of desloratadine 5mg and fexofenadine 60mg taken without and with grapefruit juice (pretreatment with 240ml of double-strength juice three times daily for 2 days prior to administration of study drug, plus the same amount simultaneously with, and 2 hours after, the drug dose). Each treatment was separated by at least 10 days. Log-transformed pharmacokinetic parameters [peak plasma concentration (C(max)) and area under the curve (AUC)], time to maximum concentration, elimination half-life and electrocardiographic (ECG) parameters. Comparing the ratio of the pharmacokinetic parameter means (C(max) and AUC) with and without grapefruit juice (expressed as a percentage), the rate (C(max)) and extent (AUC) of absorption of fexofenadine were reduced by 30% by consumption of grapefruit juice. In contrast, the bioavailability of desloratadine was unaffected by grapefruit juice. No clinically significant changes in ECG parameters were observed following coadministration of grapefruit juice with desloratadine or fexofenadine compared with either antihistamine given alone. The bioavailability of drugs that do not undergo significant intestinal or hepatic metabolism, such as fexofenadine, may be altered when administered with agents that influence drug transport mechanisms.

The effects of altitude and two decongestant-antihistamine preparations on physiological functions and performance.

DOT National Transportation Integrated Search

1978-04-01

Fourteen men were studied to determine the combined effects of two altitudes (ground level (1,274 ft) and 12,500 ft), and three preparations (lactose placebo, Compound A (Actifed - Registered Trade Name), and Compound B (Dristan - Registered Trade Na...

Urticaria.

PubMed

Amar, Sheila M; Dreskin, Stephen C

2008-03-01

Urticaria with or without angioedema is frequently encountered in primary care medicine. Although many patients and physicians think that urticaria is evidence of an IgE-mediated allergic reaction, often the etiology of urticaria is unknown. This uncertainty frequently results in patients enduring unnecessary lifestyle changes or extensive testing. In more persistent cases, patients achieve control of their disease only with the use of more toxic medications, such as corticosteroids, and this can lead to a range of systemic complications. Acute urticaria is typically due to a hypersensitivity reaction while chronic urticaria has a more complex pathogenesis. Antihistamines remain the mainstay of symptomatic treatment for both.

Idiopathic anaphylaxis.

PubMed

Fenny, Nana; Grammer, Leslie C

2015-05-01

Idiopathic anaphylaxis is a diagnosis of exclusion after other causes have been thoroughly evaluated and excluded. The pathogenesis of idiopathic anaphylaxis remains uncertain, although increased numbers of activated lymphocytes and circulating histamine-releasing factors have been implicated. Signs and symptoms of patients diagnosed with idiopathic anaphylaxis are indistinguishable from the manifestations of other forms of anaphylaxis. Treatment regimens are implemented based on the frequency and severity of patient symptoms and generally include the use of epinephrine autoinjectors, antihistamines, and steroids. The prognosis of idiopathic anaphylaxis is generally favorable with well-established treatment regimens and effective patient education. Copyright © 2015 Elsevier Inc. All rights reserved.

Treatment of hay fever.

PubMed Central

Wood, S F

1989-01-01

The range of treatments for hay fever available to the general practitioner has changed considerably in recent years. New antihistamines have addressed the problem of sedation and moved towards one daily dose; nasally applied corticosteroids avoid the need for systemic steroid therapy and its potential adverse effect; and regulatory decisions have set a trend away from immunotherapy in general practice. However, knowledge about the mechanism of action of immunotherapy is increasing and new developments with improved safety profiles include allergen polymers, allergoids, oral immunotherapy and nasal immunotherapy. Choice of treatment depends, as always, on the individual circumstances of the patient and his or her disease. PMID:2556545

Keratoconjunctivitis and Periorbital Edema due to Ecballium elaterium

PubMed Central

Brouzas, Dimitrios; Oanta, Mariana; Loukianou, Eleni; Moschos1st, Marillita

2012-01-01

Purpose To report on a case of keratoconjunctivitis with periorbital edema after accidental exposure to undiluted juice of Ecballium elaterium fruit during the ripening season of this plant. Methods Case report. Results Keratoconjunctivitis with Descemet's membrane folds and superficial upper corneal well-defined edematous areas were noted after an Ecballium elaterium fruit burst and its juice splashed into the patient's left eye. Prompt administration of antibiotic and steroid eye drops along with per os antihistamine therapy, resulted in quick regression of symptoms. Conclusions This report demonstrates the toxic effects of this herb to the eye and also that prompt therapy is effective. PMID:22529808

Medication for Behavior Modification in Birds.

PubMed

van Zeeland, Yvonne

2018-01-01

The use of behavior modifying drugs may be considered in birds with behavior problems, especially those refractory to behavior modification therapy and environmental management. To accomplish behavior change, a variety of drugs can be used, including psychoactive drugs, hormones, antihistamines, analgesics, and anticonvulsants. Because their prescription to birds is off-label, these drugs are considered appropriate only when a sound rationale can be provided for their use. This requires a (correct) behavioral diagnosis to be established. In addition, regular monitoring and follow-up are warranted to determine the efficacy of the treatment and evaluate the occurrence of potential adverse side effects. Copyright © 2017 Elsevier Inc. All rights reserved.

Chronic toxicity of diphenhydramine hydrochloride and erythromycin thiocyanate to Daphnia, Daphnia magna, in a continuous exposure test system

USGS Publications Warehouse

Meinertz, Jeffery R.; Schreier, Theresa M.; Bernardy, Jeffry A.; Franz, Jeanne L.

2011-01-01

Diphenhydramine hydrochloride (DH; Benadryl(TM), an over-the-counter antihistamine) and erythromycin thiocyanate (ET; a commonly used macrolide antibiotic) are pharmaceutical compounds whose chronic toxicity to Daphnia magna had not been characterized. Continuous exposure to DH concentrations about 5 times greater than the maximum reported environmental concentration of 0.023 μg/L for 21 days or to ET concentrations about 40 times the maximum reported environmental concentration of 6 μg/L for 21 days did not significantly impact D. magna survival and production. In this study the no observable effect concentration for DH was 0.12 μg/L and for ET was 248 μg/L.

Chloroquine-induced pruritus in Nigerian medical and nursing students.

PubMed

Harries, A D; Chugh, K S

1986-10-01

Two hundred and fifty-one Nigerian medical and nursing students from the University of Maiduguri Teaching Hospital completed a questionnaire on chloroquine-induced pruritus. One hundred and thirty (51.8) students experienced itching, and in 71 the symptoms were so distressing that chloroquine was no longer used for treating febrile malarial episodes. Antihistamines taken before chloroquine or a change in the route of administration were helpful in preventing or a ameliorating symptoms in some of the students. Significantly more students with chloroquine-induced pruritus had parents or siblings similarly affected compared with students who did not get pruritus, and this supports the concept of a pharmacogenetic basis to the disorder.

Projected 24-hour post-dose ocular itching scores post-treatment with olopatadine 0.7% versus 0.2.

PubMed

Fidler, Matthew L; Ogundele, Abayomi; Covert, David; Sarangapani, Ramesh

2018-04-21

Olopatadine is an antihistamine and mast cell stabilizer used for treating allergic conjunctivitis. Olopatadine 0.7% has been recently approved for daily dosing in the US, which supersedes the previously approved 0.2% strength. The objective of this analysis was to characterize patients who have better itching relief at 24 h when taking olopatadine 0.7% treatment instead of olopatadine 0.2% (in terms of proportions of responses) and relate this to the severity of baseline itching as an indirect metric of a patient's sensitivity to antihistamines. A differential odds model was developed using data from two conjunctival allergen challenge (CAC) studies to characterize individual-level and population-level response to ocular itching following olopatadine treatment and the data was analyzed retrospectively. This modeling analysis was designed to predict 24 h ocular itching scores and to quantify the differences in 24 h itching relief following treatment with olopatadine 0.2% versus 0.7% in patients with moderate-to-high baseline itching. A one-compartment kinetic-pharmacodynamic E max model was used to determine the effect of olopatadine. Impact of baseline itching severity, vehicle effect and the drug effect on the overall itching scores post-treatment were explicitly incorporated in the model. The model quantified trends observed in the clinical data with regards to both mean scores and the proportions of patients responding to olopatadine treatment. The model predicts a higher proportion of patients in the olopatadine 0.7% versus 0.2% group will experience relief within 24 h. This prediction was confirmed with retrospective clinical data analysis. The number of allergy patients relieved with olopatadine 0.7% increased with higher baseline itching severity scores, when compared to olopatadine 0.2%.

Prescription medicine use by pedestrians and the risk of injurious road traffic crashes: A case-crossover study.

PubMed

Née, Mélanie; Avalos, Marta; Luxcey, Audrey; Contrand, Benjamin; Salmi, Louis-Rachid; Fourrier-Réglat, Annie; Gadegbeku, Blandine; Lagarde, Emmanuel; Orriols, Ludivine

2017-07-01

While some medicinal drugs have been found to affect driving ability, no study has investigated whether a relationship exists between these medicines and crashes involving pedestrians. The aim of this study was to explore the association between the use of medicinal drugs and the risk of being involved in a road traffic crash as a pedestrian. Data from 3 French nationwide databases were matched. We used the case-crossover design to control for time-invariant factors by using each case as its own control. To perform multivariable analysis and limit false-positive results, we implemented a bootstrap version of Lasso. To avoid the effect of unmeasured time-varying factors, we varied the length of the washout period from 30 to 119 days before the crash. The matching procedure led to the inclusion of 16,458 pedestrians involved in an injurious road traffic crash from 1 July 2005 to 31 December 2011. We found 48 medicine classes with a positive association with the risk of crash, with median odds ratios ranging from 1.12 to 2.98. Among these, benzodiazepines and benzodiazepine-related drugs, antihistamines, and anti-inflammatory and antirheumatic drugs were among the 10 medicines most consumed by the 16,458 pedestrians. Study limitations included slight overrepresentation of pedestrians injured in more severe crashes, lack of information about self-medication and the use of over-the-counter drugs, and lack of data on amount of walking. Therapeutic classes already identified as impacting the ability to drive, such as benzodiazepines and antihistamines, are also associated with an increased risk of pedestrians being involved in a road traffic crash. This study on pedestrians highlights the necessity of improving awareness of the effect of these medicines on this category of road user.

Cognitive Performance Effects of Bilastine 20 mg During 6 Hours at 8000 ft Cabin Altitude.

PubMed

Valk, Pierre J L; Simons, Ries; Jetten, Andrea M; Valiente, Román; Labeaga, Luis

2016-07-01

Bilastine is a new oral, second generation antihistamine used in the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. It is considered a nonsedating antihistamine and might be recommended for use in pilots, pending research on the effects on flying-related performance under hypobaric conditions that prevail in an airliner. We assessed the effects of a single dose of bilastine 20 mg on alertness and complex task performance of healthy volunteers in a hypobaric chamber at 75.2 kPa (8000 ft/2438 m cabin altitude). In a randomized, double-blind, crossover study, 24 volunteers received a single dose of bilastine 20 mg, hydroxyzine 50 mg (active control), and placebo. Using the Vigilance and Tracking Task, Multi-Attribute Task Battery, and Stanford Sleepiness Scale, assessments were made before and up to 6 h after intake of the study medication. Bilastine 20 mg had no impairing effects on sleepiness levels, vigilance, or complex task performance for up to 6 h post-dose. Hydroxyzine 50 mg (active control) was associated with significant sleepiness and impaired performance across this time period, confirming the sensitivity of the tests. Bilastine 20 mg did not cause sleepiness or impaired performance on tasks related to flying. It is anticipated that a single dose of bilastine 20 mg will not affect flying performance. Bilastine may provide a safe therapeutic alternative for pilots suffering from allergic rhinitis or urticaria. Our findings might also have implications for the treatment of allergic disorders of personnel involved in other safety-sensitive jobs. Valk PJL, Simons R, Jetten AM, Valiente R, Labeaga L. Cognitive performance effects of bilastine 20 mg during 6 hours at 8000 ft cabin altitude. Aerosp Med Hum Perform. 2016; 87(7):622-627.

One-year safety and efficacy study of bilastine treatment in Japanese patients with chronic spontaneous urticaria or pruritus associated with skin diseases.

PubMed

Yagami, Akiko; Furue, Masutaka; Togawa, Michinori; Saito, Akihiro; Hide, Michihiro

2017-04-01

A number of second-generation non-sedating antihistamines are used in clinical practices over the world. However, long-term safety and efficacy have not been proved high level evidence based medicine. We have performed an open-label, multicenter, phase III study to evaluate the long-term safety and efficacy of bilastine, a novel non-sedating H 1 -antihistamine for patients with chronic spontaneous urticaria (CSU) or pruritus associated with skin diseases (trial registration no. JapicCTI-142528). Patients aged 18-74 years were treated with bilastine 20 mg once daily for up to 52 weeks. Safety and tolerability were assessed on the basis of adverse events (AE), bilastine-related AE, laboratory tests and vital signs. Efficacy was assessed based on rash score, itch score, overall improvement and quality of life. One hundred and ninety-eight patients enrolled, 122 of whom (61.6%) completed the 52-week treatment period. AE were reported in 64.5% and bilastine-related AE in 2.5% of patients throughout the 52-week treatment period. All AE were mild to moderate in severity. AE associated with the nervous system occurred in 10 patients (5.1%) including seven patients (3.6%) with headache. Somnolence reported in two of these patients (1.0%) was related to bilastine. All efficacy variables improved during treatment with bilastine. In conclusion, long-term treatment with bilastine 20 mg once daily for 52 weeks is safe and well tolerated in Japanese patients with CSU or pruritus associated with skin diseases. Bilastine improved disease symptoms of both conditions early in treatment, and the efficacy was maintained throughout the treatment. © 2016 The Authors. The Journal of Dermatology published by John Wiley & Sons Australia, Ltd on behalf of Japanese Dermatological Association.

Computational fluid dynamics: a suitable assessment tool for demonstrating the antiobstructive effect of drugs in the therapy of allergic rhinitis.

PubMed

Achilles, N; Pasch, N; Lintermann, A; Schröder, W; Mösges, R

2013-02-01

This systematic review aims first to summarize the previous areas of application of computational fluid dynamics (CFD) and then to demonstrate that CFD is also a suitable instrument for generating three-dimensional images that depict drug effects on nasal mucosa. Special emphasis is placed on the three-dimensional visualization of the antiobstructive effect of nasal steroids and antihistamines in the treatment of allergic rhinitis. In the beginning, CFD technology was only used to demonstrate physiological and pathophysiological airflow conditions in the nose and to aid in preoperative planning and postoperative monitoring of surgical outcome in the field of rhinosurgery. The first studies using CFD examined nasal respiratory physiology, important functions of the nose, such as conditioning and warming of inspired air, and the influence of pathophysiological changes on nasal breathing. Also, postoperative outcome of surgical procedures could be "predicted" using the nasal airflow model. Later studies focused on the three-dimensional visualization of the effect of nasal sprays in healthy subjects and postoperative patients. A completely new approach, however, was the use of CFD in the area of allergic rhinitis and the treatment of its cardinal symptom of nasal obstruction. In two clinical trials, a suitable patient with a positive history of allergic rhinitis was enrolled during a symptom-free period after the pollen season. The patient developed typical allergic rhinitis symptoms after provocation with birch pollen. The 3-D visualization showed that the antiallergic treatment successfully counteracted the effects of nasal allergen provocation on nasal airflow. These observations were attributed to the antiobstructive effect of a nasal steroid (mometasone furoate) and a systemic antihistamine (levocetirizine), respectively. CFD therefore constitutes a non-invasive, precise, reliable and objective examination procedure for generating three-dimensional images that

The effect of levocabastine and furosemide pretreatment on hyperreactive response after nasal provocation with hypotonic aerosol in subjects with allergic rhinitis.

PubMed

Anzic, Srdjan Ante; Dzepina, Davor; Kalogjera, Livije

2007-11-01

Patients with allergic rhinitis demonstrate hyperreactive response in distilled water nasal provocation, shown by significant increase in nasal airway resistance (NAR). Antihistamines, including topical antihistamine, levocabastine, reduce response in non-specific nasal provocation tests. Furosemide is a diuretic which reduces hyperreactivity in lower airways, but the mode of its action is not yet fully understood. In this study, we hypothesized that either levocabastine or furosemide pre-treatment in allergic rhinitis patients reduced response to nasal challenge with non-isotonic aerosol. To test the hypothesis, we measured the effect of pre-treatment with levocabastine and furosemide in topical application on suppression of hyperreactive response to distilled water nasal inhalation. Nasal resistance was measured, prior to and after the provocation, by active anterior rhinomanometry in two randomized groups of patients, according to pre-treatment, either by levocabastine or furosemide, 20 patients in each group, respectively. Nasal airflow resistance and level of hyperreactive response considering nasal eosinophilia were tested. Significant increase in nasal resistance following provocation was found at baseline conditions (without pre-medication); pre-treatment with levocabastine and furosemide has suppressed such response. Patients with positive nasal eosinophilia showed a significantly higher increase in nasal resistance compared to those with negative smears. Furosemide has shown significantly better protective effect on nasal resistance increase in patients with positive eosinophils nasal smears. Levocabastine and furosemide pre-treatment suppress hyperreactive response to distilled water nasal provocation. Comparison of resistances (pre-treatment vs. without) showed more protective effect of furosemide, measured on both better and worse patent side of nose, in contrast to levocabastine group for which it was shown only on better patent side prior to

A role for Waldeyer's ring in immunological response to allergens.

PubMed

Masieri, Simonetta; Trabattoni, Daria; Incorvaia, Cristoforo; De Luca, Maria Cristina; Dell'Albani, Ilaria; Leo, Gualtiero; Frati, Franco

2014-02-01

Adenoids, tubal tonsil, palatine tonsil, and lingual tonsil are immunological organs included in the Waldeyer's ring, the basic function of which is the antibody production to common environmental antigens. Adenoidal hypertrophy (AH) is a major medical issue in children, and adenoidectomy is still the most used treatment worldwide. The response of adenoids to allergens is a good model to evaluate their immunological function. This report assessed the immunological changes in adenoid tissues from children with allergic rhinitis (AR) undergoing sublingual immunotherapy (SLIT). Adenoid samples from 16 children (seven males, nine females, mean age 7.12 years) with AH and clinical indication to adenoidectomy were collected. Of them, five children were not allergic and 11 had house dust mite and grass pollen-induced AR. Among allergic children, in four AR was treated by antihistamines while in seven AR was treated by high-dose SLIT during 4-6 months. The evaluation addressed the T helper 1 (Th1), Th2, and Th3 cells by performing a PCR array on mRNA extracted from adenoid samples. In non-allergic children, a typical Th1 pattern was found. SLIT induced a strong down-regulation of genes involved in Th2 and Th1 activation and function. In particular, in SLIT-treated allergic children IL-4, CCR2, CCR3, and PTGDR2 (Th2 related genes) and CD28, IL-2, and INHA (Th1 related genes) expression was reduced, compared with children treated with antihistamines. These preliminary findings warrant investigation in trials including larger numbers of patients, but indicate that hypertrophic adenoids of allergic children have the typical response to the specific allergen administered by SLIT. This should suggest that one should reconsider the immunological role of adenoids.

Genetic Variation along the Histamine Pathway in Children with Allergic versus Nonallergic Asthma

PubMed Central

Anvari, Sara; Vyhlidal, Carrie A.; Dai, Hongying

2015-01-01

Histamine is an important mediator in the pathogenesis of asthma. Variation in genes along the histamine production, response, and degradation pathway may be important in predicting response to antihistamines. We hypothesize that differences exist among single-nucleotide polymorphisms (SNPs) in genes of the histamine pathway between children with allergic versus nonallergic asthma. Children (7–18 yr of age; n = 202) with asthma were classified as allergic or nonallergic based on allergy skin testing. Genotyping was performed to detect known SNPs (n = 10) among genes (HDC, HNMT, ABP1, HRH1, and HRH4) within the histamine pathway. Chi square tests and Cochran-Armitage Trend were used to identify associations between genetic variants and allergic or nonallergic asthma. Significance was determined by P < 0.05 and false-positive report probability. After correction for race differences in genotype were observed, HRH1-17 TT (6% allergic versus 0% nonallergic; P = 0.04), HNMT-464 TT (41% allergic versus 29% nonallergic; P = 0.04), and HNMT-1639 TT (30% allergic versus 20% nonallergic; P = 0.04) were overrepresented among children with allergic asthma. Genotype differences specifically among the African-American children were also observed: HRH1-17 TT (13% allergic versus 0% nonallergic; P = 0.04) and HNMT-1639 TT (23% allergic versus 3% nonallergic; P = 0.03) genotypes were overrepresented among African-American children with allergic asthma. Our study suggests that genetic variation within the histamine pathway may be associated with an allergic versus nonallergic asthma phenotype. Further studies are needed to determine the functional significance of identified SNPs and their impact on antihistamine response in patients with asthma and allergic disease. PMID:25909280

International consensus on (ICON) anaphylaxis

PubMed Central

2014-01-01

ICON: Anaphylaxis provides a unique perspective on the principal evidence-based anaphylaxis guidelines developed and published independently from 2010 through 2014 by four allergy/immunology organizations. These guidelines concur with regard to the clinical features that indicate a likely diagnosis of anaphylaxis -- a life-threatening generalized or systemic allergic or hypersensitivity reaction. They also concur about prompt initial treatment with intramuscular injection of epinephrine (adrenaline) in the mid-outer thigh, positioning the patient supine (semi-reclining if dyspneic or vomiting), calling for help, and when indicated, providing supplemental oxygen, intravenous fluid resuscitation and cardiopulmonary resuscitation, along with concomitant monitoring of vital signs and oxygenation. Additionally, they concur that H1-antihistamines, H2-antihistamines, and glucocorticoids are not initial medications of choice. For self-management of patients at risk of anaphylaxis in community settings, they recommend carrying epinephrine auto-injectors and personalized emergency action plans, as well as follow-up with a physician (ideally an allergy/immunology specialist) to help prevent anaphylaxis recurrences. ICON: Anaphylaxis describes unmet needs in anaphylaxis, noting that although epinephrine in 1 mg/mL ampules is available worldwide, other essentials, including supplemental oxygen, intravenous fluid resuscitation, and epinephrine auto-injectors are not universally available. ICON: Anaphylaxis proposes a comprehensive international research agenda that calls for additional prospective studies of anaphylaxis epidemiology, patient risk factors and co-factors, triggers, clinical criteria for diagnosis, randomized controlled trials of therapeutic interventions, and measures to prevent anaphylaxis recurrences. It also calls for facilitation of global collaborations in anaphylaxis research. In addition to confirming the alignment of major anaphylaxis guidelines, ICON

A Survey of Korean Physicians' Prescription Patterns for Allergic Rhinitis.

PubMed

Seo, Min Young; Kim, Dong-Kyu; Jee, Hye Mi; Ahn, Young Min; Kim, Yong Min; Hong, Sang Duk

2017-12-01

The aim of this study was to compare the prescription patterns according to characteristics of physicians using a survey distributed amongst physicians in Korea. We surveyed the prescription patterns for allergic rhinitis (AR) of the members of the Korean Academy of Asthma, Allergy and Clinical Immunology (KAAACI) and the Korean Association of Otorhinolaryngologists (KAO). Questionnaire contained 4 categories with 28 queries. 448 physicians including 98 internal medicine (IM), 113 pediatrics (PED), and 237 otorhinolaryngology (ENT) were responded. Although the Allergic Rhinitis and its Impact on Asthma (ARIA) guidelines are most frequently used in all specialties, seasonal or perennial AR is the most frequent classification system. For the definitive diagnosis of AR, ENT physicians reported using multiple allergen simultaneous test (MAST)/radio allergy sorbent test (RAST) more than others (IM, 10.9%; PED, 20.6%; ENT, 44.2%; P<0.001). In treatment, most physicians reported that antihistamine medication is the initial treatment for AR. PED physicians prescribed fewer intranasal steroid to combinations with an antihistamine than other specialists (IM, 65.3%; PED, 42.5%; ENT, 63.3%), but preferred leukotriene antagonists (IM, 4.1%; PED, 23.0%; ENT, 3.9%; P=0.041). Overall, 53% (235/448) of the physicians performed allergen immunotherapy (AIT), and IM administers the most AIT (IM, 71.6%; PED, 42.0%; ENT, 39.5%; P=0.019). Furthermore, university and general hospital physicians prescribed more AIT than doctors at other hospital types (university hospital, 76.4%; general hospital, 64.3%; local hospital, 21.4%; private clinic, 20.2%; P<0.001). The prescription patterns for AR were different according to the physicians' characteristics and general rate of prescribing AIT is just about 53% in Korea. Thus, the development of complementary Korean-specific guidelines is needed and proper clinical instruction of AIT would be necessary.

Nasal budesonide offers superior symptom relief in perennial allergic rhinitis in comparison to nasal azelastine.

PubMed

Stern, M A; Wade, A G; Ridout, S M; Cambell, L M

1998-10-01

Allergic rhinitis is usually treated with oral antihistamines or nasal steroids. Topically active nasal antihistamine is a new treatment modality for allergic rhinitis. The efficacy in comparison to well established topical treatment alternatives is not fully known. To compare the efficacy of intranasally administered azelastine to budesonide, at their respectively recommended dosage, on the symptoms of perennial rhinitis patients. A placebo-controlled, randomized, parallel group study was conducted to compare the efficacy and tolerability of intranasal budesonide aqueous suspension (256 microg once daily) with azelastine hydrochloride nasal spray (280 microg twice daily (560 microg/day)) and with placebo in the treatment of perennial allergic rhinitis. The 195 patients (with at least a 2-year history of perennial allergic rhinitis) recorded individual nasal symptom scores, the degree of symptom control achieved and any adverse events experienced over a 2-week baseline period and a 6-week treatment period. Following treatment, the reductions in mean combined and individual nasal symptom scores from baseline values were significantly greater in the budesonide group compared with the placebo group (P < .0001 for all variables except runny nose P = .01). In patients treated with budesonide, there were also significantly larger reductions from baseline values in combined nasal symptom scores (P < .01) and in scores for all individual nasal symptoms (P < or = .05) compared with those treated with azelastine. The reductions from baseline in both combined and individual nasal symptom scores did not differ between azelastine and placebo. The study medications were well tolerated, producing no unexpected or serious treatment-related adverse events. A once-daily dose of 256 microg of intranasal budesonide aqueous suspension is significantly more effective at relieving the symptoms of perennial allergic rhinitis compared with a twice daily dose of 280 microg of azelastine

PubMed Central

ACHILLES, N.; PASCH, N.; LINTERMANN, A.; SCHRÖDER, W.; MÖSGES, R.

2013-01-01

SUMMARY This systematic review aims first to summarize the previous areas of application of computational fluid dynamics (CFD) and then to demonstrate that CFD is also a suitable instrument for generating three-dimensional images that depict drug effects on nasal mucosa. Special emphasis is placed on the three-dimensional visualization of the antiobstructive effect of nasal steroids and antihistamines in the treatment of allergic rhinitis. In the beginning, CFD technology was only used to demonstrate physiological and pathophysiological airflow conditions in the nose and to aid in preoperative planning and postoperative monitoring of surgical outcome in the field of rhinosurgery. The first studies using CFD examined nasal respiratory physiology, important functions of the nose, such as conditioning and warming of inspired air, and the influence of pathophysiological changes on nasal breathing. Also, postoperative outcome of surgical procedures could be "predicted" using the nasal airflow model. Later studies focused on the three-dimensional visualization of the effect of nasal sprays in healthy subjects and postoperative patients. A completely new approach, however, was the use of CFD in the area of allergic rhinitis and the treatment of its cardinal symptom of nasal obstruction. In two clinical trials, a suitable patient with a positive history of allergic rhinitis was enrolled during a symptom-free period after the pollen season. The patient developed typical allergic rhinitis symptoms after provocation with birch pollen. The 3-D visualization showed that the antiallergic treatment successfully counteracted the effects of nasal allergen provocation on nasal airflow. These observations were attributed to the antiobstructive effect of a nasal steroid (mometasone furoate) and a systemic antihistamine (levocetirizine), respectively. CFD therefore constitutes a non-invasive, precise, reliable and objective examination procedure for generating three-dimensional images

Allergic rhinitis

PubMed Central

2011-01-01

Allergic rhinitis is a common disorder that is strongly linked to asthma and conjunctivitis. It is usually a long-standing condition that often goes undetected in the primary-care setting. The classic symptoms of the disorder are nasal congestion, nasal itch, rhinorrhea and sneezing. A thorough history, physical examination and allergen skin testing are important for establishing the diagnosis of allergic rhinitis. Second-generation oral antihistamines and intranasal corticosteroids are the mainstay of treatment. Allergen immunotherapy is an effective immune-modulating treatment that should be recommended if pharmacologic therapy for allergic rhinitis is not effective or is not tolerated. This article provides an overview of the pathophysiology, diagnosis, and appropriate management of this disorder. PMID:22166009

An open-label pilot trial of alpha-lipoic acid for weight loss in patients with schizophrenia without diabetes.

PubMed

Ratliff, Joseph C; Palmese, Laura B; Reutenauer, Erin L; Tek, Cenk

2015-01-01

A possible mechanism of antipsychotic-induced weight gain is activation of hypothalamic monophosphate-dependent kinase (AMPK) mediated by histamine 1 receptors. Alpha-lipoic acid (ALA), a potent antioxidant, counteracts this effect and may be helpful in reducing weight for patients taking antipsychotics. The objective of this open-label study was to assess the efficacy of ALA (1,200 mg) on twelve non-diabetic schizophrenia patients over ten weeks. Participants lost significant weight during the intervention (-2.2 kg±2.5 kg). ALA was well tolerated and was particularly effective for individuals taking strongly antihistaminic antipsychotics (-2.9 kg±2.6 kg vs. -0.5 kg±1.0 kg). NCT01355952.

Meclizine-induced enhanced glycolysis is neuroprotective in Parkinson disease cell models.

PubMed

Hong, Chien Tai; Chau, Kai-Yin; Schapira, Anthony H V

2016-05-05

Meclizine is a well-tolerated drug routinely used as an anti-histamine agent in the management of disequilibrium. Recently, meclizine has been assessed for its neuroprotective properties in ischemic stroke and Huntington disease models. We found that meclizine protected against 6-hydroxydopamine-induced apoptosis and cell death in both SH-SY5Y cells and rat primary cortical cultures. Meclizine increases the level of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which activates phosphofructokinase, a rate-determining enzyme of glycolysis. This protection is therefore mediated by meclizine's ability to enhance glycolysis and increase mitochondrial hyperpolarization. Meclizine represents an interesting candidate for further investigation to re-purpose for its potential to be neuroprotective in Parkinson disease.

Hydroxychloroquine-induced erythroderma.

PubMed

Pai, Sunil B; Sudershan, Bhuvaneshwari; Kuruvilla, Maria; Kamath, Ashwin; Suresh, Pooja K

2017-01-01

Erythroderma is characterized by diffuse erythema and scaling of the skin involving more than 90% of the total body skin surface area. Drug-induced erythroderma has rarely been reported with hydroxychloroquine. We report a case of a 50-year-old female patient, with systemic lupus erythematosus, who developed itchy lesions all over the body 1 month after starting treatment with hydroxychloroquine. Drug-induced erythroderma was suspected. Hydroxychloroquine was withdrawn and the patient was treated with emollients, mid-potency corticosteroids, and oral antihistamines. A biopsy was done which confirmed the diagnosis of erythroderma. She recovered with treatment and was discharged. A careful history and clinical examination to search for potential causative factors will help prevent disabling sequelae in erythroderma.

Scombroid-type poisoning induced by the ingestion of smoked kahawai.

PubMed

Foo, L Y

1975-05-28

Three incidents of presumptive scombroid poisoning were reported in the Wellington area in 1973. Two of these cases were attributed to canned mackerel and the third to smoked kahawai. The marked similarity of the symptoms of the kahawai poisoning to those of the other two outbreaks of scombroid fish poisoning and the relief following anti-histamine therapy suggests that the poisoning arose from a similar source. Analysis of the extracts from the smoked kahawai revealed an abnormally high level of histamine and the presence of an unknown toxin. The unknown substance resembled saurine, the toxin that has been incriminated in scromboid poisoning, thus suggesting that scombroid intoxication may not be confined to fish belonging to the sub-order Scombroidei.

Successful treatment of bullous lichen planus with acitretin monotherapy. Review of treatment options for bullous lichen planus and case report.

PubMed

Rallis, Efstathios; Liakopoulou, Angeliki; Christodoulopoulos, Constantinos; Katoulis, Alexandros

2016-12-31

Bullous lichen planus (BLP) is a rare variant of lichen planus, characterized by the development of vesicular and bullous lesions, of skin, nails, hair and/or mucosa. We present a case of 63-year-old woman with BLP, unresponsive to previous therapies with topical corticosteroids, topical calcipotriol, antihistamines and oral cyclosporine (4 mg/kg/day for 4 months). She was already receiving treatment for arterial hypertension, hyperlipidemia, atrial fibrillation and uncontrolled diabetes mellitus. Acitretin was administered for 5 months with complete remission of BLP lesions and no major side effects. This is probably the first reported case of BLP treated with acitretin monotherapy. In this case acitretin was an efficacious and well-tolerated therapeutic option for BLP.

A pharmacologic continuum in the treatment of rhinorrhea: the clinician as economist.

PubMed

Meltzer, E O; Tyrell, R J; Rich, D; Wood, C C

1995-05-01

The economics of medications are now of great concern to health-care providers. Pharmacoeconomic issues are by no means simple, and yet, ironically, they assume greater importance in prescribing for modest disorders like rhinorrhea than for life-threatening conditions. The therapeutic continuum of quality and cost becomes foreshortened, and safety is an additional concern. Choosing the appropriate medication for rhinorrhea, then, can pose a challenge to the clinician, just as choosing a vital medication. This paper reviews the usage, quality, and cost of major therapies for the rhinorrhea that occurs secondary to various conditions, including nasal steroids, antihistamines and anticholinergics, and discusses the role of the clinician in factoring costs into therapy.

An overview of the pharmacological properties and potential applications of natural monoterpenes.

PubMed

Kozioł, Agata; Stryjewska, Agnieszka; Librowski, Tadeusz; Sałat, Kinga; Gaweł, Magdalena; Moniczewski, Andrzej; Lochyński, Stanisław

2014-01-01

Monoterpenes, the major components of essential oils, belong to the group of isoprenoids containing ten carbon atoms. Being widely distributed in the plant kingdom they are extensively used in cuisine and human health care products. Studies have shown that both natural monoterpenes and their synthetic derivatives are endowed with various pharmacological properties including antifungal, antibacterial, antioxidant, anticancer, antiarrhythmic, anti-aggregating, local anesthetic, antinociceptive, anti-inflammatory, antihistaminic and anti-spasmodic activities. Monoterpenes act also as regulators of growth, heat, transpiration, tumor inhibitors, inhibitors of oxidative phosphorylation, insect repellants, feline and canine attractants and antidiabetics. These interesting activities which might be potentially used not only in pharmaceutical, but also food and cosmetic industries are discussed below.

Chronic urticaria in adults: state-of-the-art in the new millennium*

PubMed Central

Criado, Paulo Ricardo; Criado, Roberta Facchini Jardim; Maruta, Celina Wakisaka; dos Reis, Vitor Manoel Silva

2015-01-01

Chronic urticaria has been explored in several investigative aspects in the new millennium, either as to its pathogenesis, its stand as an autoimmune or auto-reactive disease, the correlation with HLA-linked genetic factors, especially with class II or its interrelation with the coagulation and fibrinolysis systems. New second-generation antihistamines, which act as good symptomatic drugs, emerged and were commercialized over the last decade. Old and new drugs that may interfere with the pathophysiology of the disease, such as cyclosporine and omalizumab have been developed and used as treatments. The purpose of this article is to describe the current state of knowledge on aspects of chronic urticaria such as, pathophysiology, diagnosis and the current therapeutic approach proposed in the literature. PMID:25672302

Synthesis of Structurally Diverse 2,3-Fused Indoles via Microwave-Assisted AgSbF6-Catalysed Intramolecular Difunctionalization of o-Alkynylanilines

PubMed Central

Huang, Yuanqiong; Yang, Yan; Song, Hongjian; Liu, Yuxiu; Wang, Qingmin

2015-01-01

2,3-Fused indoles are found in numerous natural products and drug molecules. Although several elegant methods for the synthesis of this structural motif have been reported, long reaction times and harsh conditions are sometimes required, and the yields tend to be low. Herein, we report a microwave method for straightforward access to various types of 2,3-fused indoles via AgSbF6-catalysed intramolecular difunctionalization of o-alkynylanilines. AgSbF6 played a role in both the hydroamination step and the imine-formation step. This method, which exhibited excellent chemoselectivity (no ring-fused 1,2-dihydroquinolines were formed), was used for formal syntheses of the natural products conolidine and ervaticine and the antihistamine drug latrepirdine. PMID:26310858

Resistant itchy lesions in a young man.

PubMed

Grillo, Emiliano; Jimenez, Natalia; Miguel-Morrondo, Angela; Vano-Galvan, Sergio

2012-12-01

Case study A man, 18 years of age, presented with a 6-month history of a widespread itchy rash, more intense at night, which had appeared 1 month after returning from a holiday to the Dominican Republic. The rash initially appeared as white patches affecting the fingers. The patient reported unprotected heterosexual intercourse while on holiday. There was no previous or family history of atopic dermatitis, however, the patient's sister had recently begun to experience similar symptoms. Clinical examination revealed scattered excoriated papules over the trunk (Figure 1), limbs and hands (Figure 2). Intensely itchy nodules were observed on the scrotum (Figure 3). A prolonged course of oral antihistamine in addition to topical corticosteroids did not improve the symptoms. 

The pharmacologic management of nausea and vomiting of pregnancy.

PubMed

Niebyl, Jennifer R; Briggs, Gerald G

2014-02-01

Nausea and vomiting are common in early pregnancy. Forty percent or more of pregnant women may continue to suffer beyond the first trimester and 10% beyond the second trimester. A focus of the assessment is to confirm that the nausea and vomiting is due to the pregnancy and not some other cause. Nonpharmacologic options, particularly dietary modification, are a mainstay of treatment. For those who continue to experience symptoms, pharmacologic management can be employed. The combination of doxylamine succinate/pyridoxine hydrochloride was reintroduced in the United States following FDA approval in early 2013. The product was given a pregnancy safety rating of A and is recommended as first-line pharmacologic treatment for NVP. Other options include antihistamines, metoclopramide, ondansetron, phenothiazines, and after the first trimester, corticosteroids.

Epidemiological evidence in forensic pharmacovigilance.

PubMed

Persaud, Nav; Healy, David

2012-01-01

Until recently epidemiological evidence was not regarded as helpful in determining cause and effect. It generated associations that then had to be explained in terms of bio-mechanisms and applied to individual patients. A series of legal cases surrounding possible birth defects triggered by doxylamine (Bendectin) and connective tissue disorders linked to breast implants made it clear that in some instances epidemiological evidence might have a more important role, but the pendulum swung too far so that epidemiological evidence has in recent decades been given an unwarranted primacy, partly perhaps because it suits the interests of certain stakeholders. Older and more recent epidemiological studies on doxylamine and other antihistamines are reviewed to bring out the ambiguities and pitfalls of an undue reliance on epidemiological studies.

Hydroxychloroquine-induced erythroderma

PubMed Central

Pai, Sunil B.; Sudershan, Bhuvaneshwari; Kuruvilla, Maria; Kamath, Ashwin; Suresh, Pooja K.

2017-01-01

Erythroderma is characterized by diffuse erythema and scaling of the skin involving more than 90% of the total body skin surface area. Drug-induced erythroderma has rarely been reported with hydroxychloroquine. We report a case of a 50-year-old female patient, with systemic lupus erythematosus, who developed itchy lesions all over the body 1 month after starting treatment with hydroxychloroquine. Drug-induced erythroderma was suspected. Hydroxychloroquine was withdrawn and the patient was treated with emollients, mid-potency corticosteroids, and oral antihistamines. A biopsy was done which confirmed the diagnosis of erythroderma. She recovered with treatment and was discharged. A careful history and clinical examination to search for potential causative factors will help prevent disabling sequelae in erythroderma. PMID:28458440

[Hypersensitivity to mosquito bite manifested as Skeeter síndrome].

PubMed

Pérez-Vanzzini, Rafael; González-Díaz, Sandra Nora; Arias-Cruz, Alfredo; Palma-Gómez, Samuel; Yong-Rodríguez, Adrián; Gutiérrez-Mujica, José Julio; García-Calderín, Diego; Ibarra, Jesús Arturo

2015-01-01

The reactions to mosquito bites are immunological reactions with involvement of IgE, IgG and T cells mediated hypersensitivity. These reactions are common and range from small local reactions, large local reactions to systemic allergic reactions. Skeeter syndrome is defined as a large local induced inflammatory reaction to mosquito bite and sometimes accompanied by systemic symptoms such as fever and vomiting. Diagnosis is based on clinical history and physical examination, supported by the identification of specific IgE by skin testing. Treatment includes prevention, antihistamines and steroids in some cases. Specific immunotherapy still requires further study. This paper reports two cases of patients with hypersensitivity reactions to mosquito bites, which were evaluated in our center presenting positive skin tests.

[Chronic urticaria in childhood : Rational diagnostics and treatment].

PubMed

Ott, H

2017-07-01

Chronic urticaria (CU) is defined by episodes of urticaria with or without angioedema, which recur daily or nearly daily over more than 6 weeks. Sudden manifestations of CU with or without known causes are termed chronic spontaneous urticaria, which is differentiated from chronic inducible urticaria. The differential diagnoses of CU in childhood range from self-limiting dermatoses to severe systemic diseases. Further targeted steps are taken to detect potential trigger factors or underlying illnesses only if suspicion arises on anamnestic grounds and CU is best treated in accordance with international guidelines. First-line therapy consists of non-sedating H 1 -antihistamines at approved or even higher doses. If symptoms persist, additional treatment with omalizumab, cyclosporine or montelukast can be initiated after careful individual consideration.

What's eating you? chiggers.

PubMed

Hohenberger, Megan E; Elston, Dirk M

2017-06-01

Belonging to the Trombiculidae family of mites, chigger specifically refers to the larval stage of the mite's life cycle when it is able to bite its host. Although humans act as an accidental host, chiggers will latch on to the skin and their feeding process leads to localized inflammation and irritation. In most cases, these pruritic erythematous papules and papulovesicles are self-healing within a couple weeks, so only symptomatic relief is required as necessary by means of topical antipruritics, oral antihistamines, topical corticosteroids, or an intralesional triamcinolone acetonide injection in severe instances. The best practice, however, is to take preventative measures by completely covering one's skin and applying products containing DEET to the skin and clothing when traveling in infested areas.

Hypersensitivity reaction to ranitidine: description of a case and review of the literature.

PubMed

Foti, Caterina; Cassano, Nicoletta; Panebianco, Rosanna; Calogiuri, Gian Franco; Vena, Gino A

2009-01-01

Ranitidine is an H2-receptor antagonist which is usually well tolerated. Hypersensitivity reactions to ranitidine, as well as other H2 antihistamines, have been rarely described. We report the case of a 47-year-old woman who developed an anaphylactic reaction to ranitidine used as intravenous premedication before anesthesia induction. The patient's history revealed that previous use of oral ranitidine for a peptic ulcer disease did not cause any adverse reaction. Intradermal test with ranitidine at a dilution of 1:100 gave an intense positive reaction. The protective role of H2-receptor antagonists as premedication is still unclear and should be carefully reconsidered on the basis of the available controversial evidence and the possible risk of hypersensitivity reactions.

Potentiometric determination of antihistaminic diphenhydramine hydrochloride in pharmaceutical preparations and biological fluids using screen-printed electrode.

PubMed

Frag, Eman Y Z; Mohamed, Gehad G; El-Sayed, Wael G

2011-10-01

The performance characteristic of sensitive screen-printed (SPE) and carbon paste (CPE) electrodes was investigated for the determination of diphenhydramine hydrochloride (DPH) drug in pure, pharmaceutical preparations and biological fluids. Different experimental conditions namely types of materials used to prepare the working electrode (plasticizer), titrant, pH, temperature and life time were studied. Under these conditions, the SPE shows the best performance than CPE with respect to total potential change and potential break at the end point. The SPE and CPE exhibit suitable response to DPH in a concentration range of 1.0.10(-2) to 1.0.10(-6) mol/L with a limit of detection 9.70.10(-7) and 9.80.10(-7) mol/L, respectively. The slope of the system was 55.2±1.0 and 54.7±1.0 mV/decade over pH range 3.0-8.0 and 3-7 for SPE and CPE, respectively. Selectivity coefficients for DPH relative to a numbers of potential interfering substances were investigated. The SPE and CPE show a fast response time of 10 and 16s and were used over a period of 2 months with a good reproducibility. The sensors were applied successfully to determine DPH in pharmaceutical preparations and biological fluids. The results are compared with the official method. Copyright © 2011 Elsevier B.V. All rights reserved.

Parental attitudes toward new dosage forms of desloratadine in an online survey: results from four European countries.

PubMed

Valovirta, Erkka; Scadding, Glenis

2009-08-01

Allergic disease affects an estimated 50% of children worldwide and causes considerable impairment in academic performance and daily activities. Pediatric formulations for allergy treatment are often highly sugared or contain ingredients to improve palatability, appearance, and patient acceptance/adherence. These excipients, however, are associated with dental caries, gastrointestinal intolerance, and dermatologic reactions. To assess the appeal of new sugar-free/dye-free syrup and orodispersible formulations of the second-generation antihistamine desloratadine to parents of children with allergy in four European countries. In an online survey of households with children aged < or =12 years with allergies in France, Italy, the Netherlands, and Spain, respondents were asked to consider one of two desloratadine product concepts: a sugar-free, dye-free oral solution or an orodispersible tablet. Eligible households had to have at least one child aged < or =12 years with symptomatic seasonal, pet, or indoor allergies or hives for > or =1 week/year. Respondents had to be the decision makers regarding their child's allergy medication and to be likely to treat symptoms with prescription medication some of the time. There were 627 eligible households. Most (88%) parents in Spain were likely to ask their physician about and to consider trying sugar-free, dye-free desloratadine syrup, followed by 76% of those in France, 68% in Italy, and 56% in the Netherlands. About three-quarters of parents in France, Spain, and Italy and more than half of those in the Netherlands were likely to ask their physician about and to consider trying the orodispersible formulation. There is no control group for comparisons between the study's online responses and those that would have resulted from another survey methodology. Further, response biases do exist across countries based on cultural norms. Survey respondents were generally receptive to the new sugar-free, dye-free syrup and

State of the art of chronic spontaneous urticaria in Italy: a multicentre survey to evaluate physicians’ and patients’ perspectives

PubMed Central

Rimoldi, Marco; Rossi, Oliviero; Rota, Nadia

2016-01-01

Objective To assess the clinical status of chronic spontaneous urticaria (CSU) and understand treatment approaches in Italy through specialists who treat CSU (dermatologists and allergy specialists) and CSU patients' experience. Design Multicentre survey. Setting Online structured questionnaires (one for physicians and one for patients). Participants Physicians and patients with CSU in Italy. Interventions None. Primary/secondary outcomes Physician and patient attitudes/experiences. Results Survey results from 160 allergy and 160 dermatology specialists show that specialists see a median of 40 (IQR 20–80) patients with CSU/year. While most specialists (56%) know the CSU guidelines, only 27% use them regularly (36% of allergy specialists vs 18% of dermatologists). This is reflected in treatment choices with differences between physicians who use guidelines regularly and those who do not: 91.6% vs 71.7% choose standard-dose, non-sedating antihistamines as first-line treatment; 85.9% vs 56.0% select up-dosing for second-line treatment and 65.3% vs 37.2% add leukotriene receptor antagonists or H2-antihistamines as third-line treatment. The diaries from 1385 patients highlight that, regardless of treatment regimen, 29.4% of currently treated patients are refractory to therapy. Specialists aim to resolve symptoms and only 7.8% report improving quality of life (QoL) as a priority. Only 16.6% of specialists are familiar with and use the Urticaria Activity Score while 46.9% do not know it. Overall, 537 patients with CSU were surveyed (median age 37 years, IQR 30–46; 44.3% men; median disease duration 5 years, IQR 3–20). Approximately 62% confirm that CSU negatively impacts their QoL. Patients also complain of difficulties in getting information and support: <5% of medical centres provide patient support services. Conclusions In Italy, the gap between guideline-based care and QoL-related needs in CSU patients affects treatment satisfaction. This information could

Acute and preventive management of anaphylaxis in German primary school and kindergarten children.

PubMed

Kilger, Magdalena; Range, Ursula; Vogelberg, Christian

2015-10-15

Anaphylaxis is a severe, life-threatening situation. However, little is known about real-life anaphylactic management in children, especially in kindergarten and school settings, where a large number of anaphylaxes take place. Parents, school teachers and child-care providers of 86 primary schools and kindergartens in the city of Dresden, Germany, received questionnaires to report their experience with anaphylaxis in children. The main foci of interest were symptoms, allergens, sites of occurrence, acute treatment and emergency sets. Out of 6352 returned questionnaires, 87 cases of anaphylaxis were identified. Prevalence was calculated at 1.5%. Average age of the patients was 7 years, 58% were boys. The majority of reactions occurred at home (67%/58 children). Fourty seven percent (41 children) had recurrent episodes of anaphylaxis. Eighty two percent (71 children) showed cutaneous symptoms, 40% (35 children) respiratory symptoms, 29% (25 children) gastrointestinal symptoms, and 3.4% (3 children) cardiovascular symptoms. Fourty seven percent were classified as mild reactions. Foods were the most common cause (60%/52 cases). Out of these 52, tree-nuts (23%/12 cases) and peanuts (16%/8 cases) were the most frequent triggers. Sixty percent (52 cases) of reactions were treated by a physician, 35% (30 cases) were treated by non-medical professionals only. Fifty one percent (44 children) received antihistamines, 37% (32 children) corticosteroids, 1% (1 child) intramuscular adrenaline. Sixty one percent of children (53 cases) received an emergency kit. Content were corticosteroids (70%/37 cases) and antihistamines (62%/33 cases). Adrenaline auto-injectors were prescribed to 26% (14 cases). Concerning school and kindergarten-staff, 13% of the child-care providers had no knowledge about the emergency kit's content, compared to 34% of teachers. This study might support the impression of severe under-treatment of anaphylactic children in the use of adrenaline and prescription

State of the art of chronic spontaneous urticaria in Italy: a multicentre survey to evaluate physicians' and patients' perspectives.

PubMed

Rimoldi, Marco; Rossi, Oliviero; Rota, Nadia

2016-10-14

To assess the clinical status of chronic spontaneous urticaria (CSU) and understand treatment approaches in Italy through specialists who treat CSU (dermatologists and allergy specialists) and CSU patients' experience. Multicentre survey. Online structured questionnaires (one for physicians and one for patients). Physicians and patients with CSU in Italy. None. Physician and patient attitudes/experiences. Survey results from 160 allergy and 160 dermatology specialists show that specialists see a median of 40 (IQR 20-80) patients with CSU/year. While most specialists (56%) know the CSU guidelines, only 27% use them regularly (36% of allergy specialists vs 18% of dermatologists). This is reflected in treatment choices with differences between physicians who use guidelines regularly and those who do not: 91.6% vs 71.7% choose standard-dose, non-sedating antihistamines as first-line treatment; 85.9% vs 56.0% select up-dosing for second-line treatment and 65.3% vs 37.2% add leukotriene receptor antagonists or H 2 -antihistamines as third-line treatment. The diaries from 1385 patients highlight that, regardless of treatment regimen, 29.4% of currently treated patients are refractory to therapy. Specialists aim to resolve symptoms and only 7.8% report improving quality of life (QoL) as a priority. Only 16.6% of specialists are familiar with and use the Urticaria Activity Score while 46.9% do not know it. Overall, 537 patients with CSU were surveyed (median age 37 years, IQR 30-46; 44.3% men; median disease duration 5 years, IQR 3-20). Approximately 62% confirm that CSU negatively impacts their QoL. Patients also complain of difficulties in getting information and support: <5% of medical centres provide patient support services. In Italy, the gap between guideline-based care and QoL-related needs in CSU patients affects treatment satisfaction. This information could be used to improve the management of CSU in Italy. Published by the BMJ Publishing Group Limited. For

Direct-to-consumer advertising and the patient-physician relationship.

PubMed

Shah, Mansi B; Bentley, John P; McCaffrey, David J; Kolassa, E Mick

2005-06-01

Differences in attitudes of patients and physicians toward direct-to-consumer advertising (DTCA) of prescription medications may influence the patient-physician relationship, which may in turn influence health care outcomes. The objective of this study was to provide empirical evidence to show how the patient-physician relationship may be influenced by DTCA. The study used a cross-sectional research design. Pharmacists at 71 pharmacies were asked to distribute self-report survey instruments to patients who used either a proton-pump inhibitor or a nonsedating antihistamine by prescription. Data were collected between March and June 2003. Hierarchical multiple regression was used to assess the research propositions. A usable response rate of 7.3% (n=326) was obtained. About 95% of the sample had seen an advertisement for either a proton-pump inhibitor or a nonsedating antihistamine. Response to DTCA was significantly related to the patient's satisfaction with the physician and the patient's evaluation of communication, even after controlling for demographic variables and length of the patient-physician relationship. Other outcome variables (trust, relationship commitment, and average visit time) were not significantly related to DTCA response. Post hoc analyses revealed that DTCA responders, who asked their doctor to prescribe a specific product after seeing its advertisement, rated satisfaction and communication lower than the DTCA nonresponders. Additional follow-up analyses showed that these findings were largely attributed to patients in the proton-pump inhibitor group. The findings suggest that response to DTCA may be significantly related to patients' evaluation of communication quality and their satisfaction with the physician. However, these findings may not generalize to all medical conditions or types of patient. Furthermore, DTCA response does not appear to be related to other patient-physician relationship outcome variables. Given these findings, key

Clinical Pharmacology in Sleep Medicine

PubMed Central

Proctor, Ashley; Bianchi, Matt T.

2012-01-01

The basic treatment goals of pharmacological therapies in sleep medicine are to improve waking function by either improving sleep or by increasing energy during wakefulness. Stimulants to improve waking function include amphetamine derivatives, modafinil, and caffeine. Sleep aids encompass several classes, from benzodiazepine hypnotics to over-the-counter antihistamines. Other medications used in sleep medicine include those initially used in other disorders, such as epilepsy, Parkinson's disease, and psychiatric disorders. As these medications are prescribed or encountered by providers in diverse fields of medicine, it is important to recognize the distribution of adverse effects, drug interaction profiles, metabolism, and cytochrome substrate activity. In this paper, we review the pharmacological armamentarium in the field of sleep medicine to provide a framework for risk-benefit considerations in clinical practice. PMID:23213564

Fish allergy causing angioedema and secondary angle-closure glaucoma.

PubMed

Calder, Donovan; Calder, Jennifer

2013-03-06

A 56-year-old woman with a history of primary angle-closure glaucoma presented with acute generalised swelling, and facial angioedema following a fish meal. She complained of nausea, vomiting, headache, pain in both eyes and acute loss of vision. Her visual acuity was reduced and intraocular pressures (IOP) were elevated. Gonioscopy revealed complete angle closure in the left eye and complete to partial closure in the right eye. Through existing peripheral iridotomies the anterior capsules were seen pressed up against the iris of both eyes. A diagnosis of angle-closure glaucoma was made, medications were started to reduce the elevated intraocular pressure and systemic antihistamine to counter the allergic reaction. She was hospitalised for further management. A follow-up at 2 years revealed her visual acuities and IOP had remained normal.

Difficult to control atopic dermatitis

PubMed Central

2013-01-01

Difficult to control atopic dermatitis (AD) presents a therapeutic challenge and often requires combinations of topical and systemic treatment. Anti-inflammatory treatment of severe AD most commonly includes topical glucocorticosteroids and topical calcineurin antagonists used for exacerbation management and more recently for proactive therapy in selected cases. Topical corticosteroids remain the mainstay of therapy, the topical calcineurin inhibitors tacrolimus and pimecrolimus are preferred in certain locations. Systemic anti-inflammatory treatment is an option for severe refractory cases. Microbial colonization and superinfection contribute to disease exacerbation and thus justify additional antimicrobial / antiseptic treatment. Systemic antihistamines (H1) may relieve pruritus but do not have sufficient effect on eczema. Adjuvant therapy includes UV irradiation preferably of UVA1 wavelength. “Eczema school” educational programs have been proven to be helpful. PMID:23663504

Electrochemotherapy-induced radiation recall in a cat.

PubMed

Spugnini, Enrico P; Dotsinsky, Ivan; Mudrov, Nikolay; Citro, Gennaro; Caruso, Giovanni; Cardelli, Pierluigi; Baldi, Alfonso

2008-01-01

Electrochemotherapy is gaining popularity for the treatment of malignancies of companion animals due to its efficacy and low cost. In this paper, we describe the successful treatment of a recurring fibrosarcoma in a cat by using cisplatin selectively driven within the tumor cells by trains of biphasic pulses. The cat's tumor did not recur over the following five months, however the cat did experience severe erythema at the site of previous irradiation, followed by moist desquamation and ulcer that required debridement and prolonged therapy with steroids and antihistaminic drugs. The symptoms and the response to symptomatic therapy were strongly suggestive of radiation recall. Electrochemotherapy (ECT) should be used with caution in previously irradiated areas. Further studies are warranted in this field due to its potential as a rescue for relapsing tumors.

Scombroid Poisoning: A Practical Approach.

PubMed

Guergué-Díaz de Cerio, O; Barrutia-Borque, A; Gardeazabal-García, J

2016-09-01

Scombroid poisoning is a common cause of food poisoning worldwide. It is caused by ingestion of oily fish contaminated with bacteria that trigger the formation of high concentrations of histamine. Scombroid poisoning manifests mainly as a skin complaint (flushing that spreads downward and/or an erythematous urticarial rash affecting the face and upper trunk). Although the clinical course is usually self-limiting and benign, vascular compromise, bronchospasm, and arrhythmias have been described. It is important to establish a differential diagnosis that includes conditions such as fish allergy. Oral antihistamines are the mainstay of treatment. Scombroid poisoning is best prevented by refrigerating fish properly. The practical review of scombroid poisoning provided here is intended for dermatologists. Copyright © 2016 AEDV. Publicado por Elsevier España, S.L.U. All rights reserved.

Serum sickness-like reaction after influenza vaccination.

PubMed

Chiong, Fabian Joon Kiong; Loewenthal, Mark; Boyle, Michael; Attia, John

2015-12-16

Serum sickness (SS) and SS-like reaction (SSLR) are rare immune complex-mediated hypersensitivity illnesses characterised by key features of fever, rash, polyarthralgia or polyarthritis. They are self-limiting with an excellent prognosis, settling as the antigen is cleared. We describe a 30-year-old man who presented with fever, rash, polyarthralgia and subcutaneous soft tissue swelling in his hands and feet at day 5 after influenza vaccination. A thorough investigation for infective and autoimmune causes for the presenting symptoms was negative. Given the temporal relationship between the symptoms and influenza vaccination, clinical evidence and biological plausibility of influenza vaccination causing SSLR, a clinical diagnosis of SSLR was made. The patient was treated with anti-histamines, non-steroidal anti-inflammatories and glucocorticoids with gradual resolution of symptoms over 5 weeks. 2015 BMJ Publishing Group Ltd.

Successful Treatment of Provisional Cutaneous Mastocytosis with Interferon Alpha

PubMed Central

Rosario, Andrea; Bhat, Ramesh M

2016-01-01

Mastocytosis is a disorder characterized by the clonal proliferation of mast cells and their accumulation in skin, bone marrow, liver, and spleen. Cutaneous mastocytosis presents in children in over 90% of the cases and any cutaneous manifestation in an adult is the earliest sign of the systemic disease. A 45-year-old patient presented with itchy dark lesions over the body since childhood and Darier's sign was positive. Skin biopsy showed features of mastocytosis and immunohistochemistry was positive for CD34. Since the patient was refractory to treatment with antihistamines and psoralen-ultraviolet A therapy, injections of interferon alpha were given – 3 million IU twice weekly subcutaneously as they have been proven to improve constitutional symptoms. Very few reports of successful treatment of cutaneous mastocytosis using interferon alpha have been published. PMID:27293273

Treating intermittent allergic rhinitis: a prospective, randomized, placebo and antihistamine-controlled study of Butterbur extract Ze 339.

PubMed

Schapowal, Andreas

2005-06-01

Intermittent allergic rhinitis (IAR) causes patients distress and impairs their work performance and quality of life. A variety of medicines are used by sufferers whose anguish frequently leads to trying new treatments, increasingly from herbal sources. Prospective, randomized, double-blind, parallel group comparison study of Butterbur extract (Ze 339; 8 mg total petasine; one tablet thrice-daily), fexofenadine (Telfast 180, one tablet once-daily) and placebo in 330 patients. Protocol and analysis were according to the latest guidelines on new treatments for allergic rhinitis. The primary efficacy variable was a change in symptoms from baseline to endpoint during daytime. The secondary efficacy variables were: (a) as per primary variable (evening/night); (b) Physician's global assessment; (c) Responder rates. Safety was closely monitored. Both active treatments were individually significantly superior to placebo (p<0.001) in improving symptoms of IAR, while there were no differences between the two active treatments (p=0.37). Superiority to placebo was similarly shown during the evening/night (p<0.001), by physicians' own assessment and by responder rates. Both treatments were well tolerated. Butterbur Ze 339 and Fexofenadine are comparably efficacious relative to placebo. Despite being a herbal drug, Butterbur Ze 339 has now been subject to a series of well controlled trials and should be considered as an alternative treatment for IAR. Copyright (c) 2005 John Wiley & Sons, Ltd.

Treatment of canine atopic dermatitis with cetirizine, a second generation antihistamine: A single-blinded, placebo-controlled study

PubMed Central

2004-01-01

Abstract Cetirizine and placebo were administered orally as individual agents to 23 dogs with atopic dermatitis. The pruritus was satisfactorily reduced in 4/22 (18%) dogs that completed the trial with cetirizine. Two dogs vomited after administration of the active drug. PMID:15206590

Risperidone induced angioedema with concurrent EPS symptoms: a case report and review of literature

PubMed Central

Samra, Gursharan Singh; Kant, Saumitra; Chow, Robert

2018-01-01

ABSTRACT Angioedema has recently been reported as a side effect associated with the antipsychotic risperidone. We report a case of dystonia with concurrent angioedema due to risperidone. A 40-year-old male with a history of schizophrenia was started on 3 mg of risperidone BID and developed perioral and periorbital edema along with increased muscle rigidity and hand tremor within 24 h of initial administration. His symptoms abated after cessation of risperidone and intravenous administration of corticosteroids and antihistamine. This case study adds to the current literature, which has already established angioedema as a dose-dependent side effect of risperidone. Moreover, this case study aims to increase awareness about the potential for the simultaneous occurrence of angioedema and extrapyramidal symptoms, and promotes vigilance among prescribers so that the life-threatening consequences of such effects can be avoided. PMID:29686794

An outbreak of scombroid fish poisoning in a kindergarten.

PubMed

Wu, Shu-Fen; Chen, Walter

2003-01-01

We report an outbreak of scombroid poisoning at one kindergarten on September 25, 1997. There were 94 cases. The onset of symptoms of scombrotoxin after ingestion of fish is rapid (40 to 50 minutes after consumption). Clinical manifestation consisted of hyperemia, particularly on the face and neck (94.7%), nausea and vomiting (17.0%), abdominal pain (17.0%), pruritus (4.3%), headache and dizziness (4.3%) and diarrhea (3.2%). The duration of symptoms was 3 hours on average. Most patients responded to antihistamine very well. The poisoning was caused by the ingestion of spoiled scombroid fish. The tissues of scombroid fish had undergone a number of changes provoked by bacteria and the uncooked fish containing 2,104 ppm of histamine whereas cooked fish containing 1,980 ppm (198 mg/100 gm) of histamine was found in this accident.

Mapping pharmaceuticals in rat brain sections using MALDI imaging mass spectrometry.

PubMed

Hsieh, Yunsheng; Li, Fangbiao; Korfmacher, Walter A

2010-01-01

Matrix-assisted laser desorption/ionization-tandem mass spectrometric method (MALDI-MS/MS) has proven to be a reliable tool for direct measurement of the disposition of small molecules in animal tissue sections. As example, MALDI-MS/MS imaging system was employed for visualizing the spatial distribution of astemizole and its primary metabolite in rat brain tissues. Astemizole is a second-generation antihistamine, a block peripheral H1 receptor, which was introduced to provide comparable therapeutic benefit but was withdrawn in most countries due to toxicity risks. Astemizole was observed to be heterogeneously distributed to most parts of brain tissue slices including cortex, hippocampus, hypothalamic, thalamus, and ventricle regions while its major metabolite, desmethylastemizole, was only found around ventricle sites. We have shown that astemizole alone is likely to be responsible for the central nervous system (CNS) side effects when its exposures became elevated.

Clinical practice

PubMed Central

Mulder, W. M. C.

2010-01-01

Immediate type allergic reactions to medication are potentially life threatening and can hamper drug therapy of several medical conditions. Exact incidence and prevalence data for these reactions in children are lacking. If no alternative drug treatment is available, a desensitization procedure may secure the continuation of necessary therapy. Desensitization is only appropriate in case of a strong suspicion of an IgE-mediated allergic reaction. It should be performed by trained clinicians (allergy specialists) in a hospital setting where treatment of a potential anaphylactic reaction can be done without any delay. In this article, literature describing desensitization procedures for several antibiotics, antineoplastic agents, and vaccines in children is reviewed. In general, desensitization schemes for children differ only in final dose from schemes for adults. Contradictory data were found regarding the protective effects of premedication with antihistamines and glucocorticoids. PMID:20571825

Dermanyssus gallinae infestation: an unusual cause of scalp pruritus treated with permethrin shampoo.

PubMed

Dogramaci, Asena Cigdem; Culha, Gulnaz; Ozçelik, Semra

2010-09-01

Dermanyssus gallinae is a blood parasite of wild birds, but it is also a pest in the poultry industry. It occasionally bites mammals and thus rarely creates skin problems such as itching, papules, vesicles, and dermatitis. A 92-year-old man presented with severe itch on his head, particularly at night. He had been misdiagnosed with senile pruritus and treated with antihistamines and topical corticosteroids with temporary relief of the symptoms. On the basis of clinical and parasitological findings, D. gallinae dermatitis was diagnosed. Decontamination of the patient's immediate environment was not helpful. The patient was successfully treated using a 1% permethrin shampoo once a week for 2 weeks. During 3 months of follow-up he was free of symptoms. The case is of significance because most dermatologists have difficulty identifying ectoparasitoses, such as those that arise within new or atypical conditions.

Chronic Urticaria: Indian Context—Challenges and Treatment Options

PubMed Central

Khan, Sujoy; Maitra, Anirban; Hissaria, Pravin; Roy, Sitesh; Padukudru Anand, Mahesh; Nag, Nalin; Singh, Harpal

2013-01-01

Urticaria is a common condition that occurs in both children and adults. Most cases have no specific allergic trigger and the aetiology of urticaria remains idiopathic and occasionally spontaneous in nature. Inappropriate advice such as avoidance of foods (milk, egg, prawn, and brinjal) is common place in certain sections of India mostly by nonspecialists that should not be routinely recommended. It is important to look for physical urticarias such as pressure urticaria in chronic cases, which may be present either alone or in combination with other causes. Autoimmune causes for chronic urticaria have been found to play an important role in a significant proportion of patients. Long-acting nonsedating antihistamines at higher than the standard doses is safe and effective. Quality of life is affected adversely in patients with chronic symptomatic urticaria and some may require multidisciplinary management. PMID:24223585

[Rhinitis in adults].

PubMed

Kalogjera, Livije

2011-01-01

test, and by proving specific antibody IgE in patient serum. Allergic rhinitis is categorized according to sensitivity to allergens that occur seasonally, like pollens, or to allergens that are present all year round, like house dust mite, molds and animal dander, into seasonal and perennial allergic rhinitis. Allergy to pollens causes the same mechanism of inflammation in response to allergens, which is the result of allergen binding to specific IgE antibody; however, patients with pollen allergy usually complain more of sneezing and runny nose, whereas patients with allergy to perennial allergens more often complain of obstruction, with the episodes of sneezing and runny nose occurring only when exposed to higher concentrations of allergens (house cleaning, around pets). Treatment includes avoidance of allergens, medical treatment and immunotherapy (allergy vaccines, tablets with allergens). Avoidance of allergens means reduction of environmental allergen load to the respiratory system including workplace, which is not easy to accomplish. Medical treatment is usually necessary to control symptoms, and it includes antihistamines, nasal or in tablets, and nasal glucocorticoids (steroids). Antihistamines should be second generation, which do not cause sedation, and such treatment shows more efficacy on runny nose, sneezing and nasal itch than on nasal stuffiness. Nasal steroids are more potent in improving nasal patency than antihistamines, and are at least as potent in the control of all other nasal and ocular symptoms. Nasal patency may be improved by nasal or oral decongestants, but such treatment should be reduced to as short period as possible, since after several days of using nasal decongestants rebound congestion may occur and patients will need nasal decongestants to improve nasal airways even when allergens are not around anymore.

Clinical outcomes and adverse effect monitoring in allergic rhinitis.

PubMed

Juniper, Elizabeth F; Ståhl, Elisabeth; Doty, Richard L; Simons, F Estelle R; Allen, David B; Howarth, Peter H

2005-03-01

The subjective recording in diary cards of symptoms of itch, sneeze, nose running, and blockage, with the use of a rating scale to indicate the level of severity, is usual for clinical trials in allergic rhinitis. The primary outcome measure is usually a composite score that enables a single total symptoms score endpoint. It is appreciated, however, that rhinitis has a greater effect on the individual than is reflected purely by the recording of anterior nasal symptoms. Nasal obstruction is troublesome and may lead to sleep disturbance in addition to impaired daytime concentration and daytime sleepiness. These impairments affect school and work performance. Individuals with rhinitis find it socially embarrassing to be seen sneezing, sniffing, or blowing their nose. To capture these and other aspects of the disease-specific health-related quality of life, questionnaires such as the Rhinoconjunctivitis Quality of Life Questionnaire have been developed and validated for clinical trial use. The adoption of health-related quality of life questionnaires into clinical trials broadens the information obtained regarding the effect of the therapeutic intervention and helps focus on issues relevant to the individual patient. It must be appreciated that it is not only the disease that may adversely affect health-related quality of life; administered therapy, although intended to be beneficial, may also cause health impairment. Adverse-event monitoring is thus essential in clinical trials. The first-generation H 1 -histamines, because of their effect on central H 1 -receptors, are classically associated with central nervous system (CNS) effects such as sedation. Although this is not always perceived by the patient, it is clearly evident with objective performance testing, and positron emission tomography scanning has directly demonstrated the central H 1 -receptor occupancy. The second-generation H 1 -antihistamines have reduced central H 1 -receptor occupancy and considerably

Hydrogen sulfide donors alleviate itch secondary to the activation of type-2 protease activated receptors (PAR-2) in mice.

PubMed

Coavoy-Sánchez, S A; Rodrigues, L; Teixeira, S A; Soares, A G; Torregrossa, R; Wood, M E; Whiteman, M; Costa, S K P; Muscará, M N

2016-11-01

Hydrogen sulfide (H 2 S) has been highlighted as an endogenous signaling molecule and we have previously found that it can inhibit histamine-mediated itching. Pruritus is the most common symptom of cutaneous diseases and anti-histamines are the usual treatment; however, anti-histamine-resistant pruritus is common in some clinical settings. In this way, the involvement of mediators other than histamine in the context of pruritus requires new therapeutic targets. Considering that the activation of proteinase-activated receptor 2 (PAR-2) is involved in pruritus both in rodents and humans, in this study we investigated the effect of H 2 S donors on the acute scratching behavior mediated by PAR-2 activation in mice, as well as some of the possible pharmacological mechanisms involved. The intradermal injection of the PAR-2 peptide agonist SLIGRL-NH 2 (8-80nmol) caused a dose-dependent scratching that was unaffected by intraperitoneal pre-treatment with the histamine H1 antagonist pyrilamine (30mg/kg). Co-injection of SLIGRL-NH 2 (40nmol) with either the slow-release H 2 S donor GYY4137 (1 and 3nmol) or the spontaneous donor NaHS (1 and 0.3nmol) significantly reduced pruritus. Co-treatment with the K ATP channel blocker glibenclamide (200nmol) or the nitric oxide (NO) donor sodium nitroprusside (10nmol) abolished the antipruritic effects of NaHS; however, the specific soluble guanylyl cyclase inhibitor ODQ (30μg) had no significant effects. The transient receptor potential ankyrin type 1 (TRPA1) antagonist HC-030031 (20μg) significantly reduced SLIGRL-NH 2 -induced pruritus; however pruritus induced by the TRPA1 agonist AITC (1000nmol) was unaffected by NaHS. Based on these data, we conclude that pruritus secondary to PAR-2 activation can be reduced by H 2 S, which acts through K ATP channel opening and involves NO in a cyclic guanosine monophosphate (cGMP)-independent manner. Furthermore, TRPA1 receptors mediate the pruritus induced by activation of PAR-2, but H 2 S

Scombroid fish poisoning: an overlooked marine food poisoning.

PubMed

Wu, M L; Yang, C C; Yang, G Y; Ger, J; Deng, J F

1997-08-01

Scombroid fish poisoning is a food-borne chemical intoxication caused by certain spoiled fish that contain a large amount of histamine and some biogenic diamines. It has gradually become a world-wide medical problem and probably is the most common cause of fish poisoning. As the data on the incidents of scombroid fish poisoning in Taiwan remains scarce, we report 2 incidents of scombroid fish poisoning in Northern Taiwan. We collected data of the 2 outbreaks of suspected fish poisoning which were reported to us in 1996. An epidemiological investigation was undertaken. Questionnaire interviews were given to persons who ate lunch in the same cafeteria in outbreak 2. The leftover fish were sent for species identification and toxin analysis. The first incident involving 4 women occurred in March 1996. All cases experienced flush, dizziness, blurred vision and skin rashes after eating lunch. A non-scombroid fish of Makaira with histamine levels as high as 84.13 mg/100 g flesh was implicated in this incident. In August 1996, another incident involving some cases who ate lunch at the same cafeteria were investigated. A total of 146 questionnaires were distributed with a return of 132 questionnaires (90.4%). Fifty-five employees reported positive signs or symptoms; 48 persons who ate fish and 7 women who did not eat fish were ill. Fish was the only food associated with the illness with an attack rate of 73.8% (p < 0.001). The incriminated fish was later identified as a scombroid fish of Euthynnus with a histamine content of 271.9 mg/100 g flesh in 1 leftover piece and 118.5 mg/100 g flesh in another piece. Most cases in these 2 outbreaks received treatment with antihistamines and had rapid and complete recovery. The diagnosis of scombroid fish poisoning could be misdiagnosed as food allergy or bacterial food poisoning if physicians are not aware of such poisoning. The nonspecific but characteristic symptomatology of histamine food poisoning and previous consumption of fish

Atopic Dermatitis in Children: Clinical Features, Pathophysiology and Treatment

PubMed Central

Lyons, Jonathan J.; Milner, Joshua D.; Stone, Kelly D.

2014-01-01

Atopic dermatitis (AD) is a chronic, relapsing, highly pruritic skin condition resulting from disruption of the epithelial barrier and associated immune dysregulation in the skin of genetically predisposed hosts. AD generally develops in early childhood, has a characteristic age-dependent distribution and is commonly associated with elevated IgE, peripheral eosinophilia and other allergic diseases. Staphylococcus aureus colonization is common and may contribute to disease progression and severity. Targeted therapies to restore both impaired skin barrier and control inflammation are required for optimal outcomes for patients with moderate to severe disease. Pruritus is universal among patients with AD and has a dominant impact on diminishing quality of life. Medications such as anti-histamines have demonstrated poor efficacy in controlling AD-associated itch. Education of patients regarding the primary underlying defects and provision of a comprehensive skin care plan is essential for disease maintenance and management of flares. PMID:25459583

Hypersensitivity reactions to etoposide.

PubMed

Hoetelmans, R M; Schornagel, J H; ten Bokkel Huinink, W W; Beijnen, J H

1996-04-01

To report a hypersensitivity reaction to etoposide occurring in a patient after 2 months of drug therapy. A 20-year-old man with a diagnosis of testicular carcinoma was treated with bleomycin, etoposide, and cisplatin (BEP regimen). After dose 20 of etoposide, an exanthema was noted, which was attributed to etoposide. The patient had received 19 doses of etoposide during the previous 2 months without any sign of an allergic reaction. Rechallenging the patient with etoposide from another batch resulted in recurrence of the exanthema. Both etoposide and its excipient (polysorbate 80) are suspected of causing hypersensitivity reactions. Although the exact mechanism of the hypersensitivity reaction is not known, it is believed to be of nonimmunogenic origin. With a lower rate of infusion of etoposide and/or by premedication with antihistamines and/or corticosteroids, hypersensitivity reactions to etoposide might be prevented in patients with a history of hypersensitivity to this drug.

A Complete Profile on Blind-your-eye Mangrove Excoecaria Agallocha L. (Euphorbiaceae): Ethnobotany, Phytochemistry, and Pharmacological Aspects.

PubMed

Mondal, Sumanta; Ghosh, Debjit; Ramakrishna, K

2016-01-01

Traditional system of medicine consists of large number of plants with various medicinal and pharmacological importances. This article provides a comprehensive review of the complete profile of an important mangrove plant Excoecaria agallocha L. ( Euphorbiaceae ) and elaborately describing the ethnobotany, phytochemistry, and pharmacological properties. It is used traditionally in the treatment of various diseases such as epilepsy, ulcers, leprosy, rheumatism, and paralysis. The latex obtained from the bark is poisonous in nature and may cause temporary blindness, thus it is also known as the blind-your-eye mangrove plant. Many phytoconstituents were isolated from the plant, which were mainly diterpenoids, triterpenoids, flavonoids, sterols, and few other compounds. The plant also showed many pharmacological activities such as antioxidant, antimicrobial, anti-inflammatory, analgesic, antiulcer, anticancer, antireverse transcriptase, antihistamine-release, antifilarial, DNA damage protective, antidiabetic, and antitumor protecting activities. Hence, this review could help guide researchers anticipating to undertake further investigations in these directions.

Nasal filters in prevention of seasonal rhinitis induced by allergenic pollen grains. Open clinical study.

PubMed

D'Amato, G; Liccardi, G; Salzillo, A; Russo, M; Narciso, P; Allegra, L

2012-04-01

Nasal filters (Sanispira) might represent a novel approach in preventing exacerbations of symptoms of seasonal allergic rhinitis by reducing pollen access to nasal cavities. Female and male voluntary patients between the ages of 18 and 64 years living in Naples area and affected by allergic rhinitis were recruited in an open clinical study. All were allergic to Parietaria pollen as assessed by skin-prick and/or RAST test with or without associated sensitization to other pollens such as Gramineae and Olea europaea. A pollen count was also carried out from 10th April until 30th of June 2011. The results of our study show positive statistical differences between the scores of common nasal symptoms and the reduced use of antihistaminic drugs in patients using nasal filters in comparison to non users. Nasal filters constitute a useful mean to reduce symptoms of seasonal allergic rhinitis in patients suffering from pollen allergy.

Review of Anemone raddeana Rhizome and its pharmacological effects.

PubMed

Wang, Shu-Ling; Zhao, Zhen-Kun; Sun, Jian-Feng; Sun, Yun-Ting; Pang, Xiao-Qing; Zeng, Zhao-Wu; Xie, Tian

2018-01-01

The chemical compositions of Anemone raddeana Rhizome, a kind of traditional Chinese medicine, were reviewed, along with its bioactivity and pharmacological properties and method improvements of extracting and detecting triterpenoid saponins. A. raddeana Rhizome is used to treat neuralgia and rheumatism, and is rich in triterpenoid saponins, most of which are pentacyclic, with oleanane as the nucleus. So far, 37 triterpenoid saponins have been determined from the herb. Its reported bioactivity and pharmacological properties have been described as anticancerous, antimicrobial, anti-inflammatory, analgesic, antipyretic, anticonvulsive, antihistaminic, and sedative. It has also been used for the induction of the humoral immune response and treatment of liver fibrosis in chronic hepatitis. However, the herb also has hemolytic effects and can be toxic, which limits its clinical application. Further studies are needed on the pharmaceutical functions, mechanisms, and immunological responses to contribute to the herb's clinical applications.

Delayed pressure urticaria: response to treatment with sulfasalazine in a case series of seventeen patients.

PubMed

Swerlick, Robert A; Puar, Neha

2015-01-01

We retrospectively identified 17 patients with delayed pressure urticaria (DPU), diagnosed by history and confirmed with provocative pressure testing. The average age in the cohort was 42.6 years with 10 women and seven men. The mean duration of disease before diagnosis was 19.7 months (range, 1-60 months). The diagnosis of DPU was not included in the differential diagnosis of referring physicians and was not a diagnostic consideration in any of seven biopsies obtained. None of the patients responded adequately to treatment with antihistamines, but all 17 responded transiently when treated with either oral or intramuscular steroids. Eleven patients experienced complete or near complete resolution of DPU with treatment with sulfasalazine (SZ). Four patients had a partial response while two were unable to continue therapy because of drug intolerance. SZ appears to be a low cost and effective treatment for DPU. © 2015 Wiley Periodicals, Inc.

[Clinical symptomps, diagnosis and therapy of feline allergic dermatitis].

PubMed

Favrot, C; Rostaher, A; Fischer, N

2014-07-01

Allergies are often suspected in cats and they are mainly hypersensitivity reactions against insect bites, food- or environmental allergens. Cats, with non flea induced atopic dermatitis, normally present with one oft he following reaction patterns: miliary dermatitis, eosinophilic dermatitis, selfinduced alopecia or head and neck excoriations. None of these reaction patterns is nevertheless pathognomonic for allergic dermatitis, therefore the diagnosis is based on the one hand on the exclusion of similar diseases on the other hand on the successful response on a certain therapy. Recently a study on the clinical presentation of cats with non flea induced atopic dermatitis was published. In this study certain criteria for diagnosing atopy in cats were proposed. For therapy of allergic cats cyclosporin, glucocorticoids, antihistamines, hypoallergenic diets and allergen specific immunotherapy are used. This article should provide a recent overview on the clinical symptoms, diagnosis and therapy of feline allergic dermatitis.

Severe facial swelling in a pregnant woman after using hair dye.

PubMed

van Genderen, Michel E; Carels, Ginette; Lonnee, Edward R; Dees, Adriaan

2014-03-31

A 33-year-old Caucasian pregnant woman (26 weeks' gestation) presented to the emergency department. She had a 2-day history of severe itching of the scalp and steadily worsening swelling of the face over the previous 12 h, which had extended to the neck. She had no difficulty breathing. The itching and swelling had developed 3 days after she had used hair dye. The patient had no history of allergic responses to hair dye or black henna tattoos. A diagnosis of type IV delayed hypersensitivity reaction was made. Permanent hair dyes are the most frequently used professional hair dyes and are most commonly based on paraphenylenediamine (PPD) or related chemicals. PPD is known to be one of the most potent allergens which cause allergic contact dermatitis. After treatment with intravenous antihistamines and steroids, the facial swelling reduced and the patient had completely recovered by the following day.

Dimebon Inhibits Calcium-Induced Swelling of Rat Brain Mitochondria But Does Not Alter Calcium Retention or Cytochrome C Release

PubMed Central

Naga, Kranthi Kumari

2012-01-01

Dimebon was originally introduced as an antihistamine and subsequently investigated as a possible therapeutic for a variety of disorders, including Alzheimer's disease. One putative mechanism underlying the neuroprotective properties of Dimebon is inhibition of mitochondrial permeability transition, based on the observation that Dimebon inhibited the swelling of rat liver mitochondria induced by calcium and other agents that induce permeability transition. Because liver and brain mitochondria differ substantially in their properties and response to conditions associated with opening of the permeability transition pore, we sought to determine whether Dimebon inhibited permeability transition in brain mitochondria. Dimebon reduced calcium-induced mitochondrial swelling but did not enhance the calcium retention capacity or impair calcium-induced cytochrome C release from non-synaptic mitochondria isolated from rat brain cerebral cortex. These findings indicate that Dimebon does not inhibit mitochondrial permeability transition, induced by excessive calcium uptake, in brain mitochondria. PMID:20625939

Dimebon inhibits calcium-induced swelling of rat brain mitochondria but does not alter calcium retention or cytochrome C release.

PubMed

Naga, Kranthi Kumari; Geddes, James W

2011-03-01

Dimebon was originally introduced as an antihistamine and subsequently investigated as a possible therapeutic for a variety of disorders, including Alzheimer's disease. One putative mechanism underlying the neuroprotective properties of Dimebon is inhibition of mitochondrial permeability transition, based on the observation that Dimebon inhibited the swelling of rat liver mitochondria induced by calcium and other agents that induce permeability transition. Because liver and brain mitochondria differ substantially in their properties and response to conditions associated with opening of the permeability transition pore, we sought to determine whether Dimebon inhibited permeability transition in brain mitochondria. Dimebon reduced calcium-induced mitochondrial swelling but did not enhance the calcium retention capacity or impair calcium-induced cytochrome C release from non-synaptic mitochondria isolated from rat brain cerebral cortex. These findings indicate that Dimebon does not inhibit mitochondrial permeability transition, induced by excessive calcium uptake, in brain mitochondria.

Alternative products to treat allergic rhinitis and alternative routes for allergy immunotherapy.

PubMed

Ipci, Kagan; Oktemer, Tugba; Muluk, Nuray Bayar; Şahin, Ethem; Altıntoprak, Niyazi; Bafaqeeh, Sameer Ali; Kurt, Yasemin; Mladina, Ranko; Šubarić, Marin; Cingi, Cemal

2016-09-01

Some alternative products instead of immunotherapy are used in patients with allergic rhinitis (AR). In this paper, alternative products to treat allergic rhinitis and alternative routes for allergy immunotherapy are reviewed. Alternative products and methods used instead of immunotherapy are tea therapy, acupuncture, Nigella sativa, cinnamon bark, Spanish needle, acerola, capsaicin (Capsicum annum), allergen-absorbing ointment, and cellulose powder. N. sativa has been used in AR treatment due to its anti-inflammatory effects. N. sativa oil also inhibits the cyclooxygenase and 5-lipoxygenase pathways of arachidonic acid metabolism. The beneficial effects of N. sativa seed supplementation on the symptoms of AR may be due to its antihistaminic properties. To improve the efficacy of immunotherapy, some measures are taken regarding known immunotherapy applications and alternative routes of intralymphatic immunotherapy and epicutaneous immunotherapy are used. There are alternative routes and products to improve the efficacy of immunotherapy.

Separation of pharmacologically active nitrogen-containing compounds on silica gels modified with 6,10-ionene, dextran sulfate, and gold nanoparticles

NASA Astrophysics Data System (ADS)

Ioutsi, A. N.; Shapovalova, E. N.; Ioutsi, V. A.; Mazhuga, A. G.; Shpigun, O. A.

2017-12-01

New stationary phases for HPLC are obtained via layer-by-layer deposition of polyelectrolytes and studied: (1) silica gel modified layer-by-layer with 6,10-ionene and dextran sulfate (Sorbent 1); (2) silica gel twice subjected to the above modification (Sorbent 2); and (3) silica gel modified with 6,10-ionene, gold nanoparticles, and dextran sulfate (Sorbent 3). The effect the content of the organic solvent in the mobile phase and the concentration and pH of the buffer solution have on the chromatographic behavior of several pharmacologically active nitrogen-containing compounds is studied. The sorbents are stable during the process and allow the effective separation of beta-blockers, calcium channel blockers, alpha-agonists, and antihistamines. A mixture of caffeine, nadolol, tetrahydrozoline, pindolol, orphenadrine, doxylamine, carbinoxamine, and chlorphenamine is separated in 6.5 min on the silica gel modified with 6,10-ionene, gold nanoparticles, and dextran sulfate.

Original research paper. Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying.

PubMed

Amelian, Aleksandra; Szekalska, Marta; Ciosek, Patrycja; Basa, Anna; Winnicka, Katarzyna

2017-03-01

Taste of a pharmaceutical formulation is an important parameter for the effectiveness of pharmacotherapy. Cetirizine dihydrochloride (CET) is a second-generation antihistamine that is commonly administered in allergy treatment. CET is characterized by extremely bitter taste and it is a great challenge to successfully mask its taste; therefore the goal of this work was to formulate and characterize the microparticles obtained by the spray drying method with CET and poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate 1:2:1 copolymer (Eudragit E PO) as a barrier coating. Assessment of taste masking by the electronic tongue has revealed that designed formulations created an effective taste masking barrier. Taste masking effect was also confirmed by the in vivo model and the in vitro release profile of CET. Obtained data have shown that microparticles with a drug/polymer ratio (0.5:1) are promising CET carriers with efficient taste masking potential and might be further used in designing orodispersible dosage forms with CET.

Hospitalisation due to Acute Poisoning in Children – Tabuk Experience

PubMed Central

Al Hifzi, Ibrahim S.; Kumar, Pejaver; Talol, Wafaa

1995-01-01

Background & Method: Acute poisoning in children is still a major problem in our community, taking up a lot of resources from the health care system. We report here the result of’ a three year study (1991-1994) carried out in the Northwest Armed Forces Hospital, Tabuk, Saudi Arabia regarding hospitalisation of children as a result of poisoning. Results: Sixty eight children below twelve years of age were admitted, accounting for a total of approximately 175 inpatient days. The majority of them (n=60, 88.2%) were below the age of five years. house hold products (16.2%), kerosene (10.3%) and antihistamines (19.1%) were the commonest ingested substances. An analysis of various aspects of this problem and the review of relevant literature is included. Conclusions: Health education about safe storage of medicine at home and a knowledge of first aid is very necessary. This may prevent the occurence of such accidents and reduce morbidity. PMID:23012222

Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT.

PubMed

Deane, Karen J; Summers, Robert L; Lehane, Adele M; Martin, Rowena E; Barrow, Russell A

2014-05-08

The emergence and spread of malaria parasites that are resistant to chloroquine (CQ) has been a disaster for world health. The antihistamine chlorpheniramine (CP) partially resensitizes CQ-resistant (CQR) parasites to CQ but possesses little intrinsic antiplasmodial activity. Mutations in the parasite's CQ resistance transporter (PfCRT) confer resistance to CQ by enabling the protein to transport the drug away from its site of action, and it is thought that resistance-reversers such as CP exert their effect by blocking this CQ transport activity. Here, a series of new structural analogues and homologues of CP have been synthesized. We show that these compounds (along with other in vitro CQ resistance-reversers) inhibit the transport of CQ via a resistance-conferring form of PfCRT expressed in Xenopus laevis oocytes. Furthermore, the level of PfCRT-inhibition was found to correlate well with both the restoration of CQ accumulation and the level of CQ resensitization in CQR parasites.

Recent Patents and Emerging Therapeutics in the Treatment of Allergic Conjunctivitis

PubMed Central

Mishra, Gyan P.; Tamboli, Viral; Jwala, Jwala; Mitra, Ashim K.

2011-01-01

Ocular allergy is an inflammatory response of the conjunctival mucosa that also affects the cornea and eyelids. Allergic conjunctivitis includes seasonal allergic conjunctivitis (SAC), perennial allergic conjunctivitis (PAC), vernal keratoconjunctivitis (VKC), atopic keratoconjunctivitis (AKC) and giant papillary conjunctivitis (GPC). In general, allergic conditions involve mast cell degranulation that leads to release of inflammatory mediators and activation of enzymatic cascades generating pro-inflammatory mediators. In chronic ocular inflammatory disorders associated with mast cell activation such as VKC and AKC constant inflammatory response is observed due to predominance of inflammatory mediators such as eosinophils and Th2-generated cytokines. Antihistamines, mast-cell stabilizers, non-steroidal anti-inflammatory agents, corticosteroids and immunomodulatory agents are commonly indicated for the treatment of acute and chronic allergic conjunctivitis. In recent years newer drug molecules have been introduced in the treatment of allergic conjunctivitis. This article reviews recent patents and emerging therapeutics in the treatment of allergic conjunctivitis. PMID:21171952

Urgent consultations at the dermatology department of Basel University Hospital, Switzerland: characterisation of patients and setting - a 12-month study with 2,222 patients data and review of the literature.

PubMed

Ruzza, N; Itin, P H; Beltraminelli, H

2014-01-01

Urgent consultations for skin disorders are commonly done in different settings. Scarce data exist about the characteristics of these patients. The aim of this study was to analyse specific characteristics of patients receiving an urgent consultation at a dermatology department in a university hospital. We prospectively recorded the data of all patients having had an urgent consultation during a period of 12 months. We registered 2,222 urgent consultations. The most frequent diagnoses were eczemas (24.8%), dermatomycoses (5.1%) and dermatitis not otherwise specified (4.8%). The most frequent treatments were topical steroids, emollients, topical antibiotics, systemic antihistamines, antibiotics and virostatics. 2.2% of patients were hospitalized, 78.8% asked for a consultation for a disease lasting less than 4 weeks, and 6.9% presented the same day as the skin disease appeared. This study shows the characteristics of patients receiving an urgent dermatologic consultation. It underlines the need for collaboration between dermatologists, other physicians, general practitioners and nurses. © 2014 S. Karger AG, Basel.

Diagnosis and management of nasal congestion: the role of intranasal corticosteroids.

PubMed

Benninger, Michael

2009-01-01

Nasal congestion is considered the most bothersome of allergic rhinitis (AR) symptoms and can significantly impair ability to function at work, home, and school. Effective management of AR-related nasal congestion depends on accurate diagnosis and appropriate treatment. Many individuals with AR and AR-related congestion remain undiagnosed and do not receive prescription medication. However, new tools intended to improve the diagnosis of nasal congestion have been developed and validated. Intranasal corticosteroids (INSs) are recommended as first-line therapy for patients with moderate-to-severe AR and also when nasal congestion is a prominent symptom. Double blind, randomized clinical trials have demonstrated greater efficacy of INSs versus placebo, antihistamines, or montelukast for relief of all nasal symptoms, especially congestion. Patient adherence to treatment also affects outcomes, and this may be influenced by patient preferences for the sensory attributes of an individual drug. Increased awareness of the effects of AR-related nasal congestion, the efficacy and safety of available pharmacotherapies, and barriers to adherence may improve clinical outcomes.

Simultaneous screening for 238 drugs in blood by liquid chromatography-ion spray tandem mass spectrometry with multiple-reaction monitoring.

PubMed

Gergov, M; Ojanperä, I; Vuori, E

2003-09-25

A liquid chromatography-tandem mass spectrometry (LC-MS-MS) method is presented for the qualitative screening for 238 drugs in blood samples, which is considerably more than in previous methods. After a two-step liquid-liquid extraction and C(18) chromatography, the compounds were introduced into a triple quadrupole mass spectrometer equipped with a turbo ion spray ion source operating in the positive ionization mode. Identification was based on the compound's absolute retention time, protonated molecular ion, and one representative fragment ion obtained by multiple reaction monitoring (MRM) at an individually selected collision energy of 20, 35, or 50 eV. The limit of detection (LOD) for the majority of the compounds (80%) was < or = 0.05 mg/l, ranging from 0.002 mg/l (e.g., antihistamines) to 5 mg/l (acidic compounds), and for malathion it was 10 mg/l. The LOD values were sufficiently low to allow the majority of compounds to be detected at therapeutic concentrations in the blood.

Acute hemorrhagic edema of infancy: a troubling cutaneous presentation with a self-limiting course.

PubMed

Savino, Francesco; Lupica, Maria M; Tarasco, Valentina; Locatelli, Emanuela; Viola, Serena; di Montezemolo, Luca C; Coppo, Paola

2013-01-01

Acute hemorrhagic edema of infancy (AHEI) is an unusual form of leukocytoclastic vasculitis with dramatic distinguishing skin lesions that occurs in infants ages 4 to 24 months old. The disease presents with skin eruptions that usually start with large (1-5 cm), symmetrically distributed, hemorrhagic lesions in a characteristic cockade pattern. The lesions are typically located on the lower extremities, face (in particular the ears, cheeks, and eyelids), and gluteal area. Fever may accompany skin eruptions. Clinical presentation at onset requires clinical and laboratory examination to distinguish it from more serious diseases and other vasculitis. The main differential diagnosis of AHEI is Henoch-Schönlein purpura. AHEI is generally a self-limiting disease, so a conservative approach should be considered. Topical or systemic corticosteroid therapy has been reported to be beneficial, as well as antihistamines and dapsone, although AHEI usually resolves completely with or without treatment. We report two cases of AHEI and an update of the literature. © 2012 Wiley Periodicals, Inc.

Novel usage of fresh frozen plasma in hereditary angioedema.

PubMed

Hanizah, N; Affirul, C A; Farah, N A; Shamila, M A; Ridzuan, M I

2016-01-01

Hereditary angioedema (HAE) is a rare and potentially life threatening autosomal dominant disease characterized by recurrent episodes of cutaneous and mucosal oedema. It results from reduced expression or loss of function of CI-esterase inhibitors (C1-INH). As opposed to the more common histamine-mediated angioedema, HAE does not respond well to conventional treatments with anti-histamines, steroids and adrenaline. Early recognition and timely intervention with the correct treatment are crucial particularly preventing airway obstruction. New disease specific treatment including plasma derived or recombinant C1-INH, ecallantide and icatibant have recently emerged and its appropriate use can reduce HAE-associated mortality and morbidity. However due to its costs, these disease specific treatments have yet to reach Malaysia. Despite that no randomized clinical trial on FFP has been performed, its efficacy in treating acute attacks of HAE is only demonstrated in case studies. This case report illustrates the successful treatment of acute HAE episode with FFP in a Malaysian government hospital setting.

Bromism caused by mix-formulated analgesic injectables.

PubMed

Hsieh, P F; Tsan, Y T; Hung, D Z; Hsu, C L; Lee, Y C; Chang, M H

2007-12-01

Bromism, chronic bromide intoxication, can be caused by a variety of medicines, but bromism due to pain-relieving injectable medications has not been reported. In this study, the methods used were internet searching on bromide-containing injectables available in Taiwan and the first case report of bromism due to mixed-formulated injectable medication. Many analgesic/antipyretic and antihistamine injections containing bromides are still being used in Taiwan. They contain sodium bromide up to 1000 mg/ampoule or calcium bromide up to 800 mg/amp. A 25-year-old female suffered from forgetfulness and unstable gait after long-term frequent injections of a preparation to relieve head and neck pain. Blood tests showed hyperchloremia (171 mEq/L) and a negative anion gap (-48.7 mEq/L). Serum bromide measured 2150 mg/L. She recovered completely in 3 days with saline treatment. Many bromide-containing injections are still being used in Taiwan. Clinicians should keep alert on this issue to avoid iatrogenic bromism or making misdiagnoses.

Successful pregnancy by insemination of spermatozoa in a woman with a human seminal plasma allergy: should in vitro fertilization be considered first?

PubMed

Frapsauce, Cynthia; Berthaut, Isabelle; de Larouziere, Vanina; d'Argent, Emmanuelle Mathieu; Autegarden, Jean-Eric; Elloumi, Hanene; Antoine, Jean-Marie; Mandelbaum, Jacqueline

2010-07-01

To raise the possibility that pregnancy can be obtained by assisted reproductive techniques in patients with human seminal plasma allergy. Case report. University hospital. A woman consulted for a 3-year primary infertility. She reported lack of intercourse because of a seminal plasma allergy. One intrauterine insemination associated with antihistamine treatment was performed with carefully washed spermatozoa. Immediately after the insemination, the patient had an allergic reaction treated by steroids. Fortunately, this single attempt led to a successful pregnancy, and the patient gave birth to a healthy girl. Pregnancies can be obtained in patients with seminal plasma hypersensitivity by means of intrauterine insemination. However, serious complications may occur after performing intrauterine insemination, which is not a totally reliable method to prevent an allergic reaction. Thus a multidisciplinary team should follow such patients carefully and watch for the potential risks and side effects. In vitro fertilization may represent the more cautious option. Copyright 2010 American Society for Reproductive Medicine. Published by Elsevier Inc. All rights reserved.

Parkinson's disease: carbidopa, nausea, and dyskinesia.

PubMed

Hinz, Marty; Stein, Alvin; Cole, Ted

2014-01-01

When l-dopa use began in the early 1960s for the treatment of Parkinson's disease, nausea and reversible dyskinesias were experienced as continuing side effects. Carbidopa or benserazide was added to l-dopa in 1975 solely to control nausea. Subsequent to the increasing use of carbidopa has been the recognition of irreversible dyskinesias, which have automatically been attributed to l-dopa. The research into the etiology of these phenomena has identified the causative agent of the irreversible dyskinesias as carbidopa, not l-dopa. The mechanism of action of the carbidopa and benserazide causes irreversible binding and inactivation of vitamin B6 throughout the body. The consequences of this action are enormous, interfering with over 300 enzyme and protein functions. This has the ability to induce previously undocumented profound antihistamine dyskinesias, which have been wrongly attributed to l-dopa and may be perceived as irreversible if proper corrective action is not taken.

Parkinson’s disease: carbidopa, nausea, and dyskinesia

PubMed Central

Hinz, Marty; Stein, Alvin; Cole, Ted

2014-01-01

When l-dopa use began in the early 1960s for the treatment of Parkinson’s disease, nausea and reversible dyskinesias were experienced as continuing side effects. Carbidopa or benserazide was added to l-dopa in 1975 solely to control nausea. Subsequent to the increasing use of carbidopa has been the recognition of irreversible dyskinesias, which have automatically been attributed to l-dopa. The research into the etiology of these phenomena has identified the causative agent of the irreversible dyskinesias as carbidopa, not l-dopa. The mechanism of action of the carbidopa and benserazide causes irreversible binding and inactivation of vitamin B6 throughout the body. The consequences of this action are enormous, interfering with over 300 enzyme and protein functions. This has the ability to induce previously undocumented profound antihistamine dyskinesias, which have been wrongly attributed to l-dopa and may be perceived as irreversible if proper corrective action is not taken. PMID:25484598

Mast cells and histamine alter intestinal permeability during malaria parasite infection.

PubMed

Potts, Rashaun A; Tiffany, Caitlin M; Pakpour, Nazzy; Lokken, Kristen L; Tiffany, Connor R; Cheung, Kong; Tsolis, Renée M; Luckhart, Shirley

2016-03-01

Co-infections with malaria and non-typhoidal Salmonella serotypes (NTS) can present as life-threatening bacteremia, in contrast to self-resolving NTS diarrhea in healthy individuals. In previous work with our mouse model of malaria/NTS co-infection, we showed increased gut mastocytosis and increased ileal and plasma histamine levels that were temporally associated with increased gut permeability and bacterial translocation. Here, we report that gut mastocytosis and elevated plasma histamine are also associated with malaria in an animal model of falciparum malaria, suggesting a broader host distribution of this biology. In support of mast cell function in this phenotype, malaria/NTS co-infection in mast cell-deficient mice was associated with a reduction in gut permeability and bacteremia. Further, antihistamine treatment reduced bacterial translocation and gut permeability in mice with malaria, suggesting a contribution of mast cell-derived histamine to GI pathology and enhanced risk of bacteremia during malaria/NTS co-infection. Copyright © 2015 Elsevier GmbH. All rights reserved.

Middle Ear Effusion in Children: A Report of Treatment in 500 Cases

PubMed Central

Forquer, Brian D.; Linthicum, Fred H.

1982-01-01

Records were studied of 500 children younger than 9 years of age with middle ear effusion who had received one of three treatment strategies: (1) administration of medication, including decongestants, antihistamines or antibiotics (or a combination), (2) administration of medication for a limited time and then surgical therapy if effusion did not resolve or (3) myringotomy done immediately with insertion of ventilation tubes and, in some cases, removal of adenoids. Early surgical intervention resulted in significantly shorter delay in hearing restoration. It did not result in a lower recurrence rate and it did not reduce the number of occasions when thick fluid, as compared with thin fluid, was found at operation. Four children for whom medical and surgical treatment failed were considered candidates for mild gain, low maximum-power-output hearing aids. All other children had normal hearing after treatment. Medication was successful in achieving this goal in 48 percent of the cases. PMID:6184891

[Acute asthma in children--anaphylaxis].

PubMed

Carlsen, K H

1993-05-30

Acute asthma is a manifestation of chronic inflammation of airways, and may be due to inadequate control. Assessment of acute asthma is based upon respiratory rate and pattern, thoracic respiratory recessions, auscultatory rales and rhonchi, skin colour (cyanosis/pallor) and heart rate. Acute asthma in children is best treated with inhaled nebulised drugs, especially beta 2-agonists and adrenaline. Acute severe asthma should be treated with systemic steroids (by injection or orally), and it is important that this treatment is not started too late. Symptomatic treatment with intravenous theophyllamine may also be relevant. Anaphylactic shock occurs most often after injection of drugs or after bites by a wasp or a bee. Food allergy may be the cause in some patients. Speed is necessary in the treatment of anaphylactic shock, and intramuscular injection of adrenaline is the treatment of choice. Systemic steroids or antihistaminics may be used to stabilize the state of the patient.

Otitis media with effusion: benefits and harms of strategies in use for treatment and prevention.

PubMed

Principi, Nicola; Marchisio, Paola; Esposito, Susanna

2016-01-01

Otitis media with effusion (OME) is a common clinical condition that is associated with hearing loss. It can be diagnosed at least once in approximately 80% of preschool children: 30-40% of them have recurrent episodes, and 5-10% have chronic disease. OME, in recurrent and persistent cases, might significantly delay or impair communication skills, resulting in behavioral and educational difficulties. Several therapeutic approaches have been used to avoid these problems. Most, however, have not been adequately studied, and no definitive conclusions can be drawn. Official guidelines do not recommend the use of decongestants, antihistamines, steroids, or antibiotics. The data are too scanty to assess other interventions, although autoinflation, because it incurs neither cost nor adverse events, deserves attention. Surgical procedures (i.e., tympanostomy tube insertion and adenoidectomy as an adjuvant) can be useful in some cases. This review evaluates all the current OME treatments and preventive measures, including their possible adverse events.

Bilateral ethmoid sinusitis with unilateral proptosis as an initial manifestation of metastatic prostate carcinoma.

PubMed Central

Fortson, J. K.; Bezmalinovic, Z. L.; Moseley, D. L.

1994-01-01

This article presents a case of bilateral ethmoid sinusitis with unilateral proptosis as a presenting sign of an unsuspected prostate carcinoma. A 59-year-old Hispanic male presented to his primary care physician with nasal congestion and rhinitis. He was treated with antibiotics and antihistamine decongestants for 3 weeks without improvement. A trial of steroids resulted in brief improvement followed by a rapid onset of nasal obstruction with proptosis. A computed tomography scan revealed opacification of the ethmoid sinus with right proptosis. The presumptive diagnosis was orbital cellulitis secondary to chronic ethmoid sinusitis. Endoscopic sinusotomy and bilateral ethmoidectomies were performed. Biopsy results returned as metastatic adenocarcinoma, probably of prostate origin. Urological work-up and evaluation with biopsy confirmed the diagnosis of prostatic carcinoma. The patient was treated with chemotherapy and radiation therapy. He died 7 months later with disseminated disease. Images Figure 1 Figure 2 Figure 3 Figure 4A Figure 4B PMID:7861473

Outbreak of tropical rat mite (Ornithonyssus bacoti) dermatitis in a home for disabled persons.

PubMed

Baumstark, J; Beck, W; Hofmann, H

2007-01-01

Five mentally handicapped individuals living in a home for disabled persons in Southern Germany were seen in our outpatient department with pruritic, red papules predominantly located in groups on the upper extremities, neck, upper trunk and face. Over several weeks 40 inhabitants and 5 caretakers were affected by the same rash. Inspection of their home and the sheds nearby disclosed infestation with rat populations and mites. Finally the diagnosis of tropical rat mite dermatitis was made by the identification of the arthropod Ornithonyssus bacoti or so-called tropical rat mite. The patients were treated with topical corticosteroids and antihistamines. After elimination of the rats and disinfection of the rooms by a professional exterminator no new cases of rat mite dermatitis occurred. The tropical rat mite is an external parasite occurring on rats, mice, gerbils, hamsters and various other small mammals. When the principal animal host is not available, human beings can become the victim of mite infestation. 2007 S. Karger AG, Basel

Occupational Risks during a Monkeypox Outbreak, Wisconsin, 2003

PubMed Central

Sotir, Mark J.; Williams, Carl J.; Kazmierczak, James J.; Wegner, Mark V.; Rausch, Darren; Graham, Mary Beth; Foldy, Seth L.; Wolters, Mat; Damon, Inger K.; Karem, Kevin L.; Davis, Jeffrey P.

2007-01-01

We determined factors associated with occupational transmission in Wisconsin during the 2003 outbreak of prairie dog–associated monkeypox virus infections. Our investigation included active contact surveillance, exposure-related interviews, and a veterinary facility cohort study. We identified 19 confirmed, 5 probable, and 3 suspected cases. Rash, headache, sweats, and fever were reported by >80% of patients. Occupationally transmitted infections occurred in 12 veterinary staff, 2 pet store employees, and 2 animal distributors. The following were associated with illness: working directly with animal care (p = 0.002), being involved in prairie dog examination, caring for an animal within 6 feet of an ill prairie dog (p = 0.03), feeding an ill prairie dog (p = 0.002), and using an antihistamine (p = 0.04). Having never handled an ill prairie dog (p = 0.004) was protective. Veterinary staff used personal protective equipment sporadically. Our findings underscore the importance of standard veterinary infection-control guidelines. PMID:17953084

Hypersensitivity reaction to human papillomavirus vaccine due to polysorbate 80.

PubMed

Badiu, Iuliana; Geuna, Massimo; Heffler, Enrico; Rolla, Giovanni

2012-05-08

A 17-year-old girl reported generalised urticaria, eyelid angioedema, rhino-conjunctivitis, dyspnoea and wheezing 1 h after third intramuscular administration of quadrivalent human papilloma virus vaccine (Gardasil). She was treated with antihistamine, and corticosteroids with prompt relief of rhinitis and dyspnoea, while urticaria and angioedema lasted 24 h. Intradermal test with Gardasil, which contains polysorbate 80 (PS80), resulted positive, while skin tests with the bivalent vaccine were negative. Prick test performed with PS80 resulted positive in the patient and negative in ten healthy controls. The CD203 basophil activation test result was negative for PS80 at all the tested dilutions and specific IgE was not found. As flu vaccine was recommended, the authors skin tested two flu vaccine, one containing PS80 (Fluarix, GSK), which resulted positive and another flu vaccine with no adjuvant or preservative (Vaxigrip, Sanofi Pasteur MSD), which gave negative results. The patient then received Vaxigrip without adverse reactions.

[Urinary incontinence].

PubMed

Kuhn, Annette

2010-01-01

Incontinence is a common age-dependent and increasing problem in women that may mainly present as stress incontinence, overactive bladder, mixed incontinence or other forms. A thorough history, gynaecological and neurological examination and urinalysis as initial step will lead to the diagnosis and treatment. If midstream urine is difficult to receive, a catheter urine will be easy to obtain. Further investigations as urodynamics, cystoscopy and ultrasound may be required. As initial step, stress incontinence should be treated with physiotherapy and pelvic floor exercises, if not successful with operations as suburethral slings. Slings have good long-term success rates of approximately 85 % with a low morbidity and can even be inserted under local anaesthetic. The treatment of idiopathic overactive bladder consists of bladder training, a behavioural therapy, and mainly anticholinergics. Anticholinergics may cause side effects particularly in the elderly who are under several medications that may add anticholinergic effects as antidepressants, antibiotics or antihistaminics.

Assessing fitness-for-duty and predicting performance with cognitive neurophysiological measures

NASA Astrophysics Data System (ADS)

Smith, Michael E.; Gevins, Alan

2005-05-01

Progress is described in developing a novel test of neurocognitive status for fitness-for-duty testing. The Sustained Attention & Memory (SAM) test combines neurophysiologic (EEG) measures of brain activation with performance measures during a psychometric test of sustained attention and working memory, and then gauges changes in neurocognitive status relative to an individual"s normative baseline. In studies of the effects of common psychoactive substances that can affect job performance, including sedating antihistamines, caffeine, alcohol, marijuana, and prescription medications, test sensitivity was greater for the combined neurophysiological and performance measures than for task performance measures by themselves. The neurocognitive effects of overnight sleep deprivation were quite evident, and such effects predicted subsequent performance impairment on a flight simulator task. Sensitivity to diurnal circadian variations was also demonstrated. With further refinement and independent validation, the SAM Test may prove useful for assessing readiness-to-perform in high-asset personnel working in demanding, high risk situations.

Beer, Cider, and Wine Allergy.

PubMed

Bansal, Rhea A; Tadros, Susan; Bansal, Amolak S

2017-01-01

Background . Allergy to beer is often due to specific proteins in barley and sometimes to lipid transfer protein. Allergy to wine is frequently due to a sensitivity to grape proteins. We present a rare case of allergy to beer, wine, and cider resulting from IgE reactivity to yeasts and moulds which also explained the patient's additional sensitivity to yeast extracts and blue cheese. Case Presentation . The patient's symptoms included throat and facial itching accompanied by mild wheeze and severe urticaria. Diagnosis of allergy to yeast was confirmed by specific IgE testing as well as that to relevant foods and beverages. The patient's ongoing management included advice to avoid beer, wine, and other food groups containing specific yeasts, in addition to carrying a short acting nonsedating antihistamine as well as an adrenaline autoinjector. Conclusions . Cases of yeast allergy are extremely rare in medical literature but may be underrecognised and should be considered in patients presenting with reactions to alcoholic beverages and other yeast-containing products.

Antisecretory Action of the Extract of the Aerial Parts of Eremomastax speciosa (Acanthaceae) Occurs through Antihistaminic and Anticholinergic Pathways.

PubMed

André Perfusion, Amang; Tan, Paul V; Ernestine, Nkwengoua; Barthélemy, Nyasse

2014-01-01

Objective. The objective of this study was to find out the possible antiulcer mechanism of action of Eremomastax speciosa. Method. Carbachol- and histamine-induced hypersecretion, associated with the pylorus ligation technique, were used in rats. Gastric mucosal ulceration, mucus production, pH, gastric volume, and acidity were measured. Results. Histamine and carbachol raised gastric acidity to 86.50 and 84.80 mEq/L, respectively, in the control rats, and the extracts (200 mg/kg) reduced gastric acidity to 34.60 and 39.00 mEq/L, respectively. Intraduodenal aqueous extract (400 mg/kg) in histamine- and carbachol-treated rats produced significant (P < 0.001) decreases in acid secretion to 28.50 and 28.80 mEq/L, respectively, and 100 percent inhibition of gastric ulceration. Augmented histamine-induced gastric acid secretion (90.20 mEq/L) was significantly reduced to 52.60 and 27.50 mEq/L by the 200 and 400 mg/kg doses of the aqueous extract, respectively. The extract significantly reduced (P < 0.001) the volume of gastric secretion and significantly increased mucus production. The ulcer inhibition potential of the extract significantly dropped to 25-44% (oral extract) and to 29-37% (duodenal extract) in carbachol/indomethacin-treated rats. Conclusion. The aqueous extract of E. speciosa has both cytoprotective and antisecretory effects. The antisecretory effect may involve a mechanism common to both cholinergic and histaminergic pathways.

Overuse of diagnostic tools and medications in acute rhinosinusitis in Spain: a population-based study (the PROSINUS study)

PubMed Central

Jaume, Francesca; Quintó, Llorenç; Alobid, Isam; Mullol, Joaquim

2018-01-01

Objectives Acute rhinosinusitis (ARS) has a high incidence. Diagnosis is clinical, and evolution is mostly self-limited. The aim of this study was to describe the sociodemographic characteristics and use of diagnostic tools and medications in patients with ARS. Design This is a prospective observational study in real-life clinical practice. Setting Patients with clinical diagnosis of ARS (n=2610) were included from ear, nose and throat clinics in Spain. A second visit at resolution was done. Participants Patients were classified according to the duration of symptoms: viral ARS (≤10 days), postviral ARS (>10 days, ≤12 weeks) and chronic rhinosinusitis (>12 weeks). Main outcome measures Sociodemographic characteristics, symptoms, disease severity, quality of life (Sino-Nasal Outcome Test-16), used diagnostic tools and medications, and the management performed by primary care physicians (PCPs) and by otorhinolaryngologists (ORLs) were assessed. Results Of the patients 36% were classified as having viral ARS, 63% postviral ARS and 1% as chronic rhinosinusitis. Working in a poorly air-conditioned environment was a risk factor (OR: 2.26, 95% CI 1.27 to 4.04) in developing postviral ARS. A higher number of diagnostic tools (rhinoscopy/endoscopy: 80% vs 70%; plain X-ray: 70% vs 55%; CT scan: 22% vs 12%; P<0.0001) were performed in postviral than viral cases. PCPs performed more X-rays than ORLs (P<0.0001). Patients, more those with postviral than viral ARS, received a high number of medications (oral antibiotics: 76% vs 62%; intranasal corticosteroids: 54% vs 38%; antihistamines: 46% vs 31%; mucolytic: 48% vs 60%; P<0.0001). PCPs prescribed more antibiotics, antihistamines and mucolytics than ORLs (P<0.0068). More patients with postviral than viral ARS reported symptoms of potential complications (1.5% vs 0.4%; P=0.0603). Independently of prescribed medications, quality of life was more affected in patients with postviral (38.7±14.2 vs 36.0±15.3; P=0

Chronic urticaria: aetiology, management and current and future treatment options.

PubMed

Kozel, Martina M A; Sabroe, Ruth A

2004-01-01

Chronic urticaria is a common condition that can be very disabling when severe. A cause for chronic idiopathic urticaria (CIU) is only infrequently identified. Potential causes include reactions to food and drugs, infections (rarely) and, apart from an increased incidence of thyroid disease, uncomplicated urticaria is not usually associated with underlying systemic disease or malignancy. About one-third of patients with CIU have circulating functional autoantibodies against the high affinity IgE receptor or against IgE, although it is not known why such antibodies are produced, or how the presence of such antibodies alters the course of the disease or response to treatment. There are only a few publications relating to childhood urticaria, but it is probably similar to the adult form, except that adult urticaria is more common. The diagnosis is based on patient history and it is vital to spend time documenting this in detail. Extensive laboratory tests are not required in the vast majority of patients. Chronic urticaria resolves spontaneously in 30-55% of patients within 5 years, but it can persist for many years. Treatment is aimed firstly at avoiding underlying causative or exacerbating factors. Histamine H1 receptor antagonists remain the mainstay of oral treatment for all forms of urticaria. The newer low-sedating antihistamines desloratadine, fexofenadine, levocetirizine and mizolastine should be tried first. Sedating antihistamines have more adverse effects but are useful if symptoms are causing sleep disturbance. Low-dose dopexin is effective and especially suitable for patients with associated depression. There is controversy as to whether the addition of an histamine H2 receptor antagonist or a leukotriene antagonist is helpful. For CIU, second-line agents include ciclosporin (cyclosporine) [which is effective in approximately 75% of patients], short courses of oral corticosteroids, intravenous immunoglobulins and plasmapheresis, although the last two were

Beer, Cider, and Wine Allergy

PubMed Central

Tadros, Susan

2017-01-01

Background. Allergy to beer is often due to specific proteins in barley and sometimes to lipid transfer protein. Allergy to wine is frequently due to a sensitivity to grape proteins. We present a rare case of allergy to beer, wine, and cider resulting from IgE reactivity to yeasts and moulds which also explained the patient's additional sensitivity to yeast extracts and blue cheese. Case Presentation. The patient's symptoms included throat and facial itching accompanied by mild wheeze and severe urticaria. Diagnosis of allergy to yeast was confirmed by specific IgE testing as well as that to relevant foods and beverages. The patient's ongoing management included advice to avoid beer, wine, and other food groups containing specific yeasts, in addition to carrying a short acting nonsedating antihistamine as well as an adrenaline autoinjector. Conclusions. Cases of yeast allergy are extremely rare in medical literature but may be underrecognised and should be considered in patients presenting with reactions to alcoholic beverages and other yeast-containing products. PMID:28396809

Enhancing Effect of Continuous Cobalt-60 Gamma-Radiation on Susceptibility to Anaphylactic Shock in Mice

DOE Office of Scientific and Technical Information (OSTI.GOV)

Hale, William M.; Stoner, Richard D.

1958-05-01

Continuous exposure to gamma -radiation at a dose rate of 4 rep/hr enhanced the severity of anaphylactnic shock ln mice sensitized with tetanus toxoid and challenged 1 hour or 7 days postradiation with fluid tetanus toxoid. A sharp increase in susceptibility to fatal anaphylaxis was observed as the accumulated dose was increased from 192 to 288 rep. Recovery from the enhancing effect of continuous gamma -radiation began during the second week postradiation; complete recovery occurred during the third week after an accumulated dose of 672 rep. Anaphylactic shock was demonstrable in mice sensitized 6 months before challenge with the specificmore » antigen. An enhanced susceptibility to fatal anaphylaxis was obtained when these animals were given an accumulated dose of 288 rep and challenged 1 hour postradiation. Passive anaphylaxis was more severe in irradiated mice sensitized with homopogous antitoxin 1 hour postradiation and challenged the following day with tetanus toxoid. The antihistaminic agent Thephorin afforded complete protection from fatal anaphypaxis in irradiated mice. (auth)« less

[Perception of body weight by pharmacists and pharmaceutical laboratory assistants in Slovakia I].

PubMed

Kolář, Jozef; Zabolyová, Stefánia

2013-10-01

The paper presents the results of a questionnaire poll carried out in the workers in pharmacies in the Slovak Republic in the year 2012. Altogether 1,884 questionnaires were distributed, of which 492 (26.1%) were returned. The poll aimed to find the perception of and attitudes to overweight and obesity in pharmacists and pharmaceutical laboratory assistants. The average BMI values in pharmacists were 25.08, in pharmaceutical laboratory assistants 24.86. Overweight and/or obesity were recorded in 36.6% of respondents, BMI 25 was found in 5.2 % men and 33.7% women. An absence of a chronic disease was reported in 61.8% of respondents, and 38.8% of respondents reported medication - most frequently administration of antihistamines, hormones of the thyroid gland, and antihypertensive drugs. In 220 (44.7%) of respondents, overweight/obesity existed in the family. Physical exercise carried out more than 3 times a week was reported by 9.6% of respondents. Drinking regime was evaluated as good in 52.1% of respondents, and 14.6% of participants compensated stress with food.

Approach to novel functional foods for stress control 4. Regulation of serotonin transporter by food factors.

PubMed

Ito, Mikiko; Haito, Sakiko; Furumoto, Mari; Kawai, Yoshichika; Terao, Junji; Miyamoto, Ken-ichi

2005-11-01

Serotonin transporters (SERTs) are pre-synaptic proteins specialized for the clearance of serotonin following vesicular release at central nervous system (CNS) and enteric nervous system synapses. SERTs are high affinity targets in vivo for antidepressants such as serotonin selective reuptake inhibitors (SSRIs). These include 'medical' psychopharmacological agents such as analgesics and antihistamines, a plant extract called St John's Wort (Hypericum). Osteoclasts are the primary cells responsible for bone resorption. They arise by the differentiation of osteoclast precursors of the monocyte/macrophage lineage. The expression of SERTs was increased in RANKL-induced osteoclast-like cells. Using RANKL stimulation of RAW264.7 cells as a model system for osteoclast differentiation, we studied the direct effects of food factor on serotonin uptake. The SSRIs (fluoxetine and fluvoxamine) inhibited markedly (approximately 95%) in serotonin transport in differentiated osteoclast cells. The major components of St. John's Wort, hyperforin and hypericine were significantly decreased in serotonin transport activity. Thus, a new in vitro model using RANKL-induced osteoclast-like cells may be useful to analyze the regulation of SERT by food factors and SSRIs.

Enzyme therapy in Fabry disease: severe adverse events associated with anti-agalsidase cross-reactive IgG antibodies.

PubMed

Tesmoingt, Chloe; Lidove, Olivier; Reberga, Axele; Thetis, Marguerite; Ackaert, Chloe; Nicaise, Pascale; Arnaud, Philippe; Papo, Thomas

2009-11-01

To report a severe adverse event related to enzyme replacement therapy with agalsidase in an hemizygous male patient treated for Fabry disease. Retrospective analysis of clinical, radiological and biochemical data in a patient who suffered adverse events related to both agalsidase alfa and agalsidase beta treatments. A hemizygous male patient was first treated for Fabry disease with agalsidase alfa. After more than 1 year of therapy, infusion-related symptoms necessitated systemic steroids and antihistaminic therapy. Decline in kidney function prompted a switch for agalsidase beta. Anaphylactoid shock occurred after the second infusion. No serum IgE antibodies were disclosed. Skin-test reactivity to agalsidase beta was negative. Following a published rechallenge infusion protocol, agalsidase beta was reintroduced, leading to a second anaphylactoid shock episode. Enzyme replacement therapy was stopped and the patient was treated with symptomatic therapy only. This case was referred to the pharmacovigilance department. The negativity of immunological tests (specific anti-agalsidase IgE antibodies and skin tests) does not rule out the risk of repeated anaphylactoid shock following agalsidase infusion.

Enzyme therapy in Fabry disease: severe adverse events associated with anti-agalsidase cross-reactive IgG antibodies

PubMed Central

Tesmoingt, Chloe; Lidove, Olivier; Reberga, Axele; Thetis, Marguerite; Ackaert, Chloe; Nicaise, Pascale; Arnaud, Philippe; Papo, Thomas

2009-01-01

AIMS To report a severe adverse event related to enzyme replacement therapy with agalsidase in an hemizygous male patient treated for Fabry disease. METHODS Retrospective analysis of clinical, radiological and biochemical data in a patient who suffered adverse events related to both agalsidase alfa and agalsidase beta treatments. RESULTS A hemizygous male patient was first treated for Fabry disease with agalsidase alfa. After more than 1 year of therapy, infusion-related symptoms necessitated systemic steroids and antihistaminic therapy. Decline in kidney function prompted a switch for agalsidase beta. Anaphylactoid shock occurred after the second infusion. No serum IgE antibodies were disclosed. Skin-test reactivity to agalsidase beta was negative. Following a published rechallenge infusion protocol, agalsidase beta was reintroduced, leading to a second anaphylactoid shock episode. Enzyme replacement therapy was stopped and the patient was treated with symptomatic therapy only. This case was referred to the pharmacovigilance department. CONCLUSION The negativity of immunological tests (specific anti-agalsidase IgE antibodies and skin tests) does not rule out the risk of repeated anaphylactoid shock following agalsidase infusion. PMID:19917001

The action of 5-hydroxytryptamine and some of its antagonists on the umbilical vessels of the human placenta

PubMed Central

Åström, A.; Samelius, U.

1957-01-01

The vasoconstrictor action of 5-hydroxytryptamine (5-HT) in the human placental preparation is about 10 times stronger than that of adrenaline and is antagonized by anti-adrenaline compounds like phentolamine. Both 5-HT and adrenaline are antagonized by yohimbine and chlorpromazine. Specific and strong anti-5-HT action is demonstrated for lysergic acid diethylamide (LSD) and tryptamine. Both LSD and tryptamine in larger doses have a vasoconstrictor action. Mescaline has no certain modifying effect on the action of 5-HT, but itself causes vasoconstriction in large doses. The antihistamine drug phenbenzamine in histamine blocking doses abolishes the action of 5-HT in half the preparations tested. The ganglionic blocking agent trimetaphan in large doses antagonizes the action of 5-HT added subsequently, and also, to a lesser degree, the effect of adrenaline. Hexamethonium and tetraethylammonium bromides are ineffective in this preparation. No certain modifying action of reserpine on subsequently added 5-HT could be demonstrated, and the same was true for heparin even in very high concentrations. PMID:13489166

[Atopic dermatitis and urticaria: for the prevention and cure via disease control and management].

PubMed

Furukawa, Fukumi

2009-11-01

Standard ways of management are introduced through guidelines. The present standard therapies for atopic dermatitis consist of the use of topical steroids and tacrolimus ointment for inflammation as well as emollients for dry and barrier-disrupted skin as the first-line topical application, systemic anti-histamines and anti-allergic drugs for pruritus, avoidance of apparent exacerbating factors and so on. The importance of correct selection of topical steroids according to the severity of the lesion is also emphasized. As for urticaria, the use of oral histamine H1-receptor antagonists is the first line treatment, regardless of the groups, provided that sufficient efforts to eliminate the cause and/or aggravating factors are taken. Several options for the treatment are suggested as the second and/or the third line treatments, but the aim of examinations and treatments should be determined according to the type and severity of the diseases. Standard therapies and elimination of the cause and/or aggravating factors are the best way for the cure and prevention.

Pharmaceuticals in grocery market fish fillets by gas chromatography-mass spectrometry.

PubMed

Mottaleb, Musavvir Arafat; Stowe, Carly; Johnson, Daniel R; Meziani, Mohammed J; Mottaleb, M Abdul

2016-01-01

Occurrences of pharmaceuticals are evident in aquatic organisms. A reproducible gas chromatography-mass spectrometry (GC-MS) method using selected ion monitoring (SIM) has been used to determine the anti-histamine diphenhydramine (DPH), anti-anxiety diazepam (DZP), anti-seizure carbamazepine (CZP) drugs and their metabolites in grocery stores fish that were homogenized, extracted, pre-concentrated, cleaned up, and examined. Identifications of the compounds in extracts were obtained by comparing similar mass spectral features and retention properties with standards. Among nine frequently detected drugs, only DPH and DZP were observed and ranged from 0.61 to 6.21 and 1.99 to 16.57 ng/g, respectively, in fourteen fish species. These concentration values were lower than the environmental fish. Mean spike recoveries of analytes exceeded 75% with relative standard deviations (RSD)<10%. The statistically-derived method detection limits (MDLs) for nine compounds ranged from 0.13 to 5.56 ng/g. Average surrogate recoveries were 80-85% with 4-9% RSD. Copyright © 2015 Elsevier Ltd. All rights reserved.

Active treatment for food allergy.

PubMed

Kobernick, Aaron K; Burks, A Wesley

2016-10-01

Food allergy has grown in rapidly in prevalence, currently affecting 5% of adults and 8% of children. Management strategy is currently limited to 1) food avoidance and 2) carrying and using rescue intramuscular epinephrine/adrenaline and oral antihistamines in the case of accidental ingestion; there is no FDA approved treatment. Recently, oral, sublingual and epicutaneous immunotherapy have been developed as active treatment of food allergy, though none have completed phase 3 study. Efficacy and safety studies of immunotherapy have been variable, though there is clearly signal that immunotherapy will be a viable option to desensitize patients. The use of bacterial adjuvants, anti-IgE monoclonal antibodies, and Chinese herbal formulations either alone or in addition to immunotherapy may hold promise as future options for active treatment. Active prevention of food allergy through early introduction of potentially offending foods in high-risk infants will be an important means to slow the rising incidence of sensitization. Copyright © 2016 Japanese Society of Allergology. Production and hosting by Elsevier B.V. All rights reserved.

Anaphylactic shock following castor bean contact: a case report.

PubMed

Coattrenec, Y; Jaques, D; Jandus, P; Harr, T; Spoerl, D

2017-01-01

The castor bean plant, Ricinus communis , is known to have allergenic and toxic properties. Castor bean allergy has been described mainly as an occupational inhalation allergy in laboratory workers, in persons working in oil processing mills or in agricultural industry. So far, only one case of anaphylactic reaction due to castor bean sensitization confirmed by specific IgE has been described in literature. A 30-year-old woman presented to the emergency room with severe angioedema followed by urticaria, hypotension and tachycardia. She recovered after treatment with antihistamines, corticosteroids, nebulized adrenaline and intravenous fluids. Food induced anaphylaxis was excluded by allergological investigations. After repeated thorough history, the patient mentioned having bitten into a castor bean just before the reaction. Cutaneous test (prick-to-prick) and specific IgE for castor bean were highly positive. We report the second case of a severe anaphylactic reaction to castor beans, confirmed by IgE testing, reported in the literature. It underlines the importance of a meticulous history in allergology and highlights the fact, that castor beans may cause potentially fatal anaphylaxis.

[Cutaneous mastocytosis: A case report].

PubMed

Zegpi-Trueba, María Soledad; Hasbún-Acuña, Paula; Berroeta-Mauriziano, Daniela

2016-01-01

Mastocytosis represents a group of diseases characterised by an excesive accumulation of mastocytes in one or multiple tissues. It can affect only the skin, or have a systemic involvement. It has a low prevalence, and the prognosis is benign in children. To report a case of urticaria pigmentosa as a subtype of cutaneous mastocytosis, and present a literature review focused on clinical findings, diagnosis and initial basic management. A child of six months of age presenting with multiple blemishes and light brown papules located on the trunk, arms and legs. The symptoms were compatible with urticaria pigmentosa, and was confirmed by biopsy. Tests to rule out systemic involvement were requested. The patient was treated with general measures, education, and antihistamines, with favourable results. Cutaneous mastocytosis is a rare disease with a good prognosis. In childhood general measures and education are usually enough to obtain favourable results. Histamine H1 antagonists are the first line drug treatment. Copyright © 2015 Sociedad Chilena de Pediatría. Publicado por Elsevier España, S.L.U. All rights reserved.

[Motion sickness in motion: from carsickness to cybersickness].

PubMed

Bos, J E; van Leeuwen, R B; Bruintjes, T D

2018-01-01

- Motion sickness is not a disorder, but a normal response to a non-normal situation in which movement plays a central role, such as car travel, sailing, flying, or virtual reality.- Almost anyone can suffer from motion sickness, as long as at least one of the organs of balance functions. If neither of the organs of balance functions the individual will not suffer from carsickness, seasickness, airsickness, nor from cybersickness. - 'Cybersickness' is a form of motion sickness that is stimulated by artificial moving images such as in videogames. Because we are now exposed more often and for longer periods of time to increasingly realistic artificial images, doctors will also encounter cases of motion sickness more often. - The basis for motion sickness is the vestibular system, which can be modulated by visual-vestibular conflicts, i.e. when the movements seen by the eyes are not the same as those experienced by the organs of balance.- Antihistamines can be effective against motion sickness in everyday situations such as car travel if taken before departure, but the effectiveness of medication for motion sickness is limited.

A review of sleep disorders and melatonin.

PubMed

Xie, Zizhen; Chen, Fei; Li, William A; Geng, Xiaokun; Li, Changhong; Meng, Xiaomei; Feng, Yan; Liu, Wei; Yu, Fengchun

2017-06-01

Sleep disorders are a group of conditions that affect the ability to sleep well on a regular basis and cause significant impairments in social and occupational functions. Although currently approved medications are efficacious, they are far from satisfactory. Benzodiazepines, antidepressants, antihistamines and anxiolytics have the potential for dependence and addiction. Moreover, some of these medications can gradually impair cognition. Melatonin (N-acetyl-5-methoxytryptamine) is an endogenous hormone produced by the pineal gland and released exclusively at night. Exogenous melatonin supplementation is well tolerated and has no obvious short- or long-term adverse effects. Melatonin has been shown to synchronize the circadian rhythms, and improve the onset, duration and quality of sleep. It is centrally involved in anti-oxidation, circadian rhythmicity maintenance, sleep regulation and neuronal survival. This narrative review aims to provide a comprehensive overview of various therapeutic functions of melatonin in insomnia, sleep-related breathing disorders, hypersomnolence, circadian rhythm sleep-wake disorders and parasomnias. Melatonin offers an alternative treatment to the currently available pharmaceutical therapies for sleep disorders with significantly less side effects.

Report of Allergic Reaction After Application of Botulinum Toxin.

PubMed

Careta, Mariana Figueiroa; Delgado, Livia; Patriota, Régia

2015-07-01

Botulinum toxin is a widely used treatment with satisfactory results, and it is relatively safe in the doses used for cosmetic procedures. The authors report a case of allergic reaction to Chinese botulinum toxin serotype A (CBTX-A). Although this is a rare adverse event, it is nonetheless clinically relevant to healthcare professionals. A 44-year-old woman presented to the authors' hospital complaining of dynamic wrinkles. CBTX-A was used to treat her. Minutes after application, she developed urticarial plaques proximal to the injection site. The patient had an allergic reaction, as documented by a positive skin test, which was controlled by the administration of antihistamines and systemic corticosteroids. This report is intended to guide healthcare professionals faced with this type of adverse event regarding how to proceed without hindering the delivery and effectiveness of the treatment. When performed by a qualified health professional, this treatment brings excellent results in the vast majority of cases. 5 Risk. © 2015 The American Society for Aesthetic Plastic Surgery, Inc. Reprints and permission: journals.permissions@oup.com.

Intramolecular interactions contributing for the conformational preference of bioactive diphenhydramine: Manifestation of the gauche effect

NASA Astrophysics Data System (ADS)

de Rezende, Fátima M. P.; Andrade, Laize A. F.; Freitas, Matheus P.

2015-08-01

Diphenhydramine is an antihistamine used to treat some symptoms of allergies and the common cold. It is usually marketed as the hydrochloride salt, and both the neutral and cation forms have the O-C-C-N fragment. The gauche effect is well known in fluorine-containing chains, because its main origin is hyperconjugative and the σ∗C-F is a low-lying acceptor orbital, allowing electron delocalization in the conformation where F and an adjacent electronegative substituent in an ethane fragment are in the gauche orientation. Our experimental (NMR) and theoretical findings indicate that diphenhydramine exhibits the gauche effect, since the preferential conformations have the O-C-C-N moiety in this orientation due especially to antiperiplanar σC-H → σ∗C-O and σC-H → σ∗C-N interactions. This conformational preference is strengthened in the protonated form due to an incremental electrostatic gauche effect. Because the gauche conformation matches the bioactive structure of diphenhydramine complexed with histamine methyltransferase, it is suggested that intramolecular interactions, and not only induced fit, rule its bioactive form.

Scombroid poisoning. Case series of 10 incidents involving 22 patients.

PubMed

Müller, G J; Lamprecht, J H; Barnes, J M; De Villiers, R V; Honeth, B R; Hoffman, B A

1992-04-18

Scombroid poisoning is a form of ichthyosarcotoxism caused by the consumption of 'spoiled' fish of the dark meat varieties. It can be considered a mild-to-moderate form of 'food poisoning' and it occurs world-wide. Ten incidents, involving 22 patients, were reported to Tygerberg Hospital Pharmacology and Toxicology Consultation Centre in the first quarter of 1990. Cape yellowtail (Seriola lalandii) was involved in all the cases. The presenting symptoms and signs (in order of frequency) were: skin rash, diarrhoea, palpitations, headache, nausea and abdominal cramps, paraesthesia, an unusual taste sensation and breathing difficulties. The patients responded well to anti-histamines and, in most, the condition resolved within 12-24 hours. Although histamine plays an important role in the pathogenesis of scombroid poisoning, the exact mechanism is still unresolved. The condition should be recognised and not confused with a true seafood allergy. Health workers are urged to alert the authorities when outbreaks of suspected cases of scombroid poisoning are encountered in order to establish the possible cause and to prevent further cases.

[Secondary and tertiary prevention of allergic asthma in children].

PubMed

Rancé, F; Deschildre, A; Bidat, E; Just, J; Couderc, L; Wanin, S; Weiss, L

2010-12-01

Asthma is a disease of the lung epithelial barrier, most often associated with allergy in children. Asthma and allergy are two distinct diseases, but the phenotypic expression of asthma depends on atopic status. A better definition of phenotypes of asthma would result in better targeting of prevention and treatment modalities. Secondary prevention aims to prevent the onset of asthma and the acquisition of new sensitizations in sensitized children. Studies concerning allergen avoidance are insufficient to reach a definitive conclusion and antihistamines have not been shown to be effective. The results for specific immunotherapy suggest a benefit to prevent transition from allergic rhinitis to asthma and the onset of new sensitizations. Tertiary prevention aims to reduce symptoms in children with an existing allergic asthma diagnosis. The avoidance of known respiratory allergens will only be effective in combination with management of the whole environment. Specific immunotherapy has a real place, in combination with background therapy. It should be used according to guidelines in appropriately treated patients. Copyright © 2010 SPLF. Published by Elsevier Masson SAS. All rights reserved.

New therapies for allergic rhinitis.

PubMed

Braido, Fulvio; Sclifò, Francesca; Ferrando, Matteo; Canonica, Giorgio Walter

2014-04-01

Because of its burden on patient's lives and its impact on asthma, allergic rhinitis must be treated properly with more effective and safer treatments. According to guidelines by Allergic Rhinitis and Its Impact on Asthma (ARIA), the classification, pathogenesis, and treatment of allergic rhinitis are well defined. Currently, second-generation antihistamines and inhaled steroids are considered the cornerstone of first-line therapy. However, new formulations of available drugs (e.g., loratadine and rupatadine oral solution, ebastine fast-dissolving tablets, and the combination of intranasal fluticasone propionate and azelastine hydrochloride), recently discovered molecules (e.g., ciclesonide, bilastine, and phosphodiesterase-4 inhibitors), immunologic targets (e.g., omalizumab), and unconventional treatments (e.g., homeopathic treatments) are currently under investigation and represent a new frontier in modern medicine and in allergic rhinitis management. The aim of this review is to provide an update on allergic rhinitis treatment, paying particular attention to clinical trials published within the past 20 months that assessed the efficacy and safety of new formulations of available drugs or new molecules.

Bilastine for the relief of allergy symptoms.

PubMed

Sádaba Díaz de Rada, B; Azanza Perea, J R; Gomez-Guiu Hormigos, A

2011-04-01

Bilastine is a potent inhibitor of the histamine H1 receptor. It was recently approved in 28 countries of the European Union for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria in adults and children older than 12 years. Data from preclinical studies confirmed its selectivity for the histamine H1 receptor over other receptors, and demonstrated antihistaminic and antiallergic properties in vivo. Studies in healthy volunteers and patients have shown that bilastine does not affect driving ability, cardiac conduction or alertness. Bilastine has demonstrated a good safety profile, without serious adverse effects or antimuscarinic effects in clinical trials. There were no significant changes in laboratory tests, electrocardiograms or vital signs. In clinical studies, oral treatment with bilastine 20 mg once daily improved allergic rhinitis with greater efficacy than placebo and comparable to cetirizine and desloratadine. Bilastine 20 mg was more effective than placebo and equivalent to levocetirizine in chronic urticaria, relieving symptoms, improving quality of life and controlling sleep disorders. 2011 Prous Science, S.A.U. or its licensors. All rights reserved.

Rhinitis and its impact on work.

PubMed

Vandenplas, Olivier; D'Alpaos, Vinciane; Van Brussel, Philippe

2008-04-01

Health-related work disability has been increasingly recognized as an important component of the economic and societal burden of a disease. The purpose of this review is to summarize recently published data pertaining to the impact of rhinitis on work disability. Recent studies have investigated the impact of rhinitis on both the amount of time missed from work (absenteeism) and the level of work effectiveness while on the job (presenteeism). These studies have shown that rhinitis has a rather modest effect on absenteeism, with estimated productivity losses of approximately 1-4% resulting from missed work time. By contrast, rhinitis is associated with substantial impairment in at-work performance. Estimates of lost productivity attributable to reduced on-the-job effectiveness ranged from 11 to 40%. The impact of rhinitis on work productivity is affected by symptom severity, and allergen exposure, and it can be reduced by second-generation antihistamines. The impact of rhinitis on work productivity should be further characterized and taken into account for establishing cost-effective management strategies.

[Drug rash with eosinophilia and systemic symptoms syndrome induced by carbamazepine: Case report].

PubMed

Marín, Jorge Alonso; Ortega, Mayra Alexandra; Sánchez, Isaura Pilar; Pacheco, José Armando

2017-06-01

Drug rash with eosinophilia and systemic symptoms (DRESS) syndrome is a hypersensitivity reaction associated with a variety of drugs, mainly anticonvulsants, which is characterized by systemic symptoms and erythematous lesions, common to other toxicodermas. It is an uncommon clinical entity that requires a high suspicion by clinical staff given its varied initial presentation, and the fact that symptoms can overlap with those of other adverse cutaneous reactions to drugs. Without early diagnosis and appropriate treatment, mortality increases.We report the case of a 22-year-old patient with impaired neurodevelopment who received treatment with carbamazepine. Two months later he presented with general symptoms and skin erythematous lesions that began on his trunk. The patient received outpatient care with antihistamines and antipyretics without an appropriate response. His case progressed with increased skin lesions and systemic symptoms that met the diagnostic criteria for DRESS syndrome. He was hospitalized and received medical treatment according to recommended guidelines. The patient's condition improved as his symptoms and associated complications resolved. He was discharged with gradual clearing of the steroid therapy.

Emerging Approaches to Food Desensitization in Children.

PubMed

Hamad, Ahmad; Burks, Wesley A

2017-05-01

The purpose of this review is to highlight the recent advances in food desensitization in children with food allergy. Recent advancements in epicutaneous, sublingual, and oral immunotherapy for food allergy in the future may offer children with food allergy and their families a viable option to reduce risk or severity of anaphylaxis with phase III trials ongoing for two of these treatment modalities. Food allergy prevalence in children is estimated to be up to 8%. These children are at risk of significant allergic reactions and anaphylaxis. Food avoidance and use of antihistamines or epinephrine has been the standard of care for these patients. This approach also has a significant socioeconomic effects on patients and their families. Recent advancements in understanding food allergy have allowed for exploring new methods of treatment. There is an increasing interest in oral immunotherapy, epicutaneous immunotherapy, or sublingual immunotherapy for food allergy. There have been also innovative approaches to immunotherapy by modification of food allergens (to make them less allergenic while maintain their immunogenicity) or adding adjunctive treatments (probiotics, anti-IgE, etc.) to increase efficacy or safety.

The cost of productivity losses associated with allergic rhinitis.

PubMed

Crystal-Peters, J; Crown, W H; Goetzel, R Z; Schutt, D C

2000-03-01

To measure the cost of absenteeism and reduced productivity associated with allergic rhinitis. The National Health Interview Survey (NHIS) was used to obtain information on days lost from work and lost productivity due to allergic rhinitis. Wage estimates for occupations obtained from the Bureau of Labor Statistics (BLS) were used to calculate the costs. Productivity losses associated with a diagnosis of allergic rhinitis in the 1995 NHIS were estimated to be $601 million. When additional survey information on the use of sedating over-the-counter (OTC) allergy medications, as well as workers' self-assessments of their reduction in at-work productivity due to allergic rhinitis, were considered, the estimated productivity loss increased dramatically. At-work productivity losses were estimated to range from $2.4 billion to $4.6 billion. Despite the inherent difficulty of measuring productivity losses, our lowest estimate is several times higher than previous estimates of the indirect medical costs associated with allergic rhinitis treatment. The most significant productivity losses resulted not from absenteeism but from reduced at-work productivity associated with the use of sedating OTC antihistamines.

Allergy-induced preterm labor after the ingestion of shellfish

PubMed Central

ROMERO, ROBERTO; KUSANOVIC, JUAN PEDRO; MUÑOZ, HERNAN; GOMEZ, RICARDO; LAMONT, RONALD F.; YEO, LAMI

2012-01-01

Preterm parturition is a syndrome caused by several mechanisms of disease, including intrauterine infection/inflammation, uteroplacental ischemia, uterine overdistension, cervical disease, maternal/fetal stress, abnormal allogeneic responses, allergic reactions, and unknown insults. An allergic-like mechanism was proposed as a potential etiology for the preterm parturition syndrome, based on the observation that eosinophils were present in the amniotic fluid in a fraction of women with preterm labor and a history of allergy, coupled with the observation that conditioned media from degranulated mast cells (the effector cells of type 1 hypersensitivity) induced contractility of human myometrial strips. This communication describes a case of a pregnant woman who had an allergic reaction and regular uterine contractions after the ingestion of lobster meat, to which she was known to be allergic. Preterm labor subsided after the treatment of antihistamines and steroids. The patient subsequently delivered at term. At follow-up, the child was diagnosed with atopy and asthma, and required frequent use of inhaled corticosteroids and beta-2 adrenergic agents. PMID:19900031

Large local reactions to insect envenomation.

PubMed

Carlson, John; Golden, David B K

2016-08-01

Insect stings often induce large local reactions (LLRs) that result in morbidity. These reactions do have an immunologic basis; however, patients presenting with LLRs should be managed differently than those with systemic allergic reactions, as described in this review. Morbidity results from the inflammation itself along with the iatrogenic consequences of treatment. The prescription of antihistamine medications and the use of antibiotics are generally not indicated for patients with LLRs because of the risks/side-effects of these medications and the low probability of benefit. Some patients are also concerned over the possibility that a future sting will evolve into a life-threatening reaction. Although these reactions do involve IgE, patients are not at sufficient risk to warrant prescription of autoinjectable epinephrine. Venom-specific immunotherapy can be considered when LLRs are frequent and associated with significant impairment. Clinicians can reduce morbidity from LLRs by reassuring the patients, avoiding medications that result in side-effects when they are not indicated, and referring to an allergist when there are additional concerns, such as frequent impairment.

Separation of drug stereoisomers by the formation of. beta. -cyclodextrin inclusion complexes

DOE Office of Scientific and Technical Information (OSTI.GOV)

Armstrong, D.W.; Ward, T.J.; Armstrong, R.D.

For many drugs, only racemic mixtures are available for clinical use. Because different stereoisomers of drugs often cause different physiological responses, the use of pure isomers could elicit more exact therapeutic effects. Differential complexation of a variety of drug stereoisomers by immobilized ..beta..-cyclodextrin was investigated. Chiral recognition and racemic resolution were observed with a number of compounds from such clinically useful classes as ..beta..-blockers, calcium-channel blockers, sedative hypnotics, antihistamines, anticonvulsants, diuretics, and synthetic opiates. Separation of the diastereomers of the cardioactive and antimalarial cinchona alkaloids and of two antiestrogens was demonstrated as well. Three dimensional projections of ..beta..-cyclodextrin complexes ofmore » propanol, which is resolved by this technique, and warfarin, which is not, are compared. These studies have improved the understanding and application of the chiral interactions of ..beta..-cyclodextrin, and they have demonstrated a means to measure optical purity and to isolate or produce pure enantiomers of drugs. In addition, this highly specific technique could also be used in the pharmacological evaluation of enantiometric drugs. 27 references, 3 figures, 2 tables.« less

[Cold-induced urticaria].

PubMed

Delorme, N; Drouet, M; Thibaudeau, A; Verret, J L

2002-09-01

Cold urticaria is characterized by the development of urticaria, usually superficial and/or angioedematous reaction after cold contact. It was found predominantly in young women. The diagnosis is based on the history and ice cube test. Patients with a negative ice cube test may have represented systemic cold urticaria (atypical acquired cold urticaria) induced by general body cooling. The pathogenesis is poorly understood. Cold urticaria can be classified into acquired and familial disorders, with an autosomal dominant inheritance. Idiopathic cold urticaria is most common type but the research of a cryopathy is necessary. Therapy is often difficult. It is essential that the patient be warned of the dangers of swimming in cold water because systemic hypotension can occur. H1 antihistamines can be used for treatment of cold urticaria but the clinical responses are highly variable. The combination with an H2 antagonists is more effective. Doxepin may be useful in the treatment. Leukotriene receptor antagonists may be a novel, promising drug entity. In patients who do not respond to previous treatments, induction of cold tolerance may be tried.

[Emergency due to allergy: the therapy--adrenaline for physicians and patients].

PubMed

Fricker, M; Helbling, A

2005-06-01

Emergency due to allergy may proceed within minutes to life-threatening respiratory and circulatory problems. Therefore, after diagnosis prompt and correct therapy might be vital. Because of its effect on alpha-, beta1-, and beta2-receptors, adrenaline is the treatment of choice in emergency due to allergy. For fear of cardiovascular side effects, often adrenaline is withheld even in case of anaphylaxis. If given properly such as an intramuscular injection the danger of undesirable side effects, however, is small. After a systemic, allergic reaction each patient needs to be equipped with rescue medications. If an adrenaline-containing device is prescribed--nowadays with EpiPen and the metered-dose inhaler Primatene Mist 2 systems are available--, the patient must get a correct instruction in its use. In case of a severe allergic reaction, antihistamines and corticosteroids are given in second line. Following any systemic allergy, an allergological work-up should be required. Only through exact diagnosis and profound patient's education, recurrences can be avoided, and in some cases, specific immunotherapy is indicated.

Histopathological effects of intranasal phototherapy and nasal corticosteroids in allergic rhinitis in a rabbit model.

PubMed

Yurttas, Veysel; Şereflican, Murat; Erkoçoğlu, Mustafa; Terzi, Elçin Hakan; Kükner, Aysel; Oral, Mesut

2015-08-01

Allergic rhinitis is one of the most common health problems and has a major effect on quality of life. Although new-generation antihistamines and nasal steroids are the main treatment options, complete resolution cannot be obtained in some patients. Besides common side effects such as nasal irritation and epistaxis, the use of these drugs is controversial in some patients, such as pregnant or breastfeeding women. These findings highlight the need for new treatment options. Although phototherapy has been successfully used in the treatment of atopic dermatitis, which is an IgE-mediated disease and shares several common pathogenic features with allergic rhinitis, there are limited studies about its role in the treatment of allergic rhinitis. In this study, we aimed to evaluate and compare the histopathological effects of intranasal phototherapy (Rhinolight) and nasal corticosteroid treatment on the nasal mucosa in allergic rhinitis in a rabbit model and we found that both treatment options significantly reduced inflammation in the nasal mucosa without increasing apoptosis of mucosal cells. Copyright © 2015 Elsevier B.V. All rights reserved.

Pathogenesis and treatment of skin lesions caused by sulfur mustard.

PubMed

Poursaleh, Zohreh; Ghanei, Mostafa; Babamahmoodi, Farhang; Izadi, Morteza; Harandi, Ali Amini; Emadi, Seyed Emad; Taghavi, Nez'hat-o-Sadat; Sayad-Nouri, Seyede Somaye; Emadi, Seyed Naser

2012-09-01

Sulfur mustard (SM) exposure intensely causes lesions that range in severity from mild erythema to blister formation and necrosis. This review will discuss acute and long-term skin consequences due to exposure to SM and different kinds of medical prophylaxis and therapeutics against SM-induced skin lesions. Literature survey of medical case reports, clinical studies, and original articles was performed using PubMed, Medline, and the Cochrane Database (1917-2011 March). Key words included sulfur mustard, skin, toxicity, pathogenesis, cancer, treatment. SM-induced damage to the skin is characterized by edema, inflammation, and cell death mainly of the basal keratinocyte layer, with varying immunological and pathological changes in the acute phase. Also, xerosis, hypo or hyper pigmentation, scars, and rarely, skin cancers are long-term cutaneous effects. So far,the combination therapy of topical drugs and oral antihistamines, also iodine and antitumor necrosis factor alpha antibodies, are effective remedies in the treatment of skin lesions. The requirement for preparedness in the dermatological community concerning SM exposure is underlined. Novel treatments for prevention and therapeutics against SM toxicity and carcinogenicity are reviewed.

Psychotropic medication patterns among youth in juvenile justice.

PubMed

Lyons, Camilla L; Wasserman, Gail A; Olfson, Mark; McReynolds, Larkin S; Musabegovic, Hana; Keating, Joseph M

2013-03-01

This paper aims to determine the prevalence, patterns, and demographic and diagnostic correlates of psychotropic medication use in a sample of youth in one state's post-adjudicatory secure facilities. The health records database of the facilities was the source of linked demographic, diagnostic and pharmacy information for the 1-year period ending June 30, 2008. Age, gender, race, offense, prior petitions and diagnoses were examined across groups, and concomitant psychotropic pharmacotherapy patterns were identified. Period prevalence was 10.2% for youth ranging in age from 12 through 22 years who had any psychotropic drug prescribed during the first 30 days after intake to the facility. Among medicated youths, almost half received concomitant therapy. Medicated youth were significantly less likely to be Hispanic and more likely to endorse one or more diagnoses. Antidepressants, antipsychotics and antihistamines were the most commonly dispensed agents. Our findings revealed that the rate of psychotropic medication use was low, concomitant medication use was common, and ethnic/race differences in psychopharmacologic treatment were present in this sample of youths in post-adjudicatory secure facilities.

Adjuvant treatment with a symbiotic in patients with inflammatory non-allergic rhinitis.

PubMed

Gelardi, M; De Luca, C; Taliente, S; Fiorella, M L; Quaranta, N; Russo, C; Ciofalo, A; Macchi, A; Mancini, M; Rosso, P; Seccia, V; Guagnini, F; Ciprandi, G

2017-01-01

Inflammatory non-allergic rhinitis (INAR) is characterized by the presence of an inflammatory infiltrate and a non-IgE-mediated pathogenesis. This retrospective, controlled, multicentre study investigated whether a symbiotic, containing Lactobacillus acidophilus NCFM, Bifidobacterium lactis, and fructo-oligosaccharides (Pollagen®, Allergy Therapeutics, Italy), prescribed as adjunctive therapy to a standard pharmacological treatment, was able to reduce symptom severity, endoscopic features, and nasal cytology in 93 patients (49 males and 44 females, mean age 36.3±7.1 years) with INAR. The patients were treated with nasal corticosteroid, oral antihistamine, and isotonic saline. At randomization, 52 patients were treated also with symbiotic as adjunctive therapy, whereas the remaining 41 patients served as controls. Treatment lasted for 4 weeks. Patients were visited at baseline, after treatment, and after 4-week follow-up. Adjunctive symbiotic treatment significantly reduced the percentages of patients with symptoms and endoscopic signs, and diminished inflammatory cells. In conclusion, the present study demonstrates that a symbiotic was able, as adjuvant treatment, to significantly improve symptoms, endoscopic feature, and cytology in patients with INAR, and its effect may be long lasting.

Snake poisoning in rural Zimbabwe--a prospective study.

PubMed

Nhachi, C F; Kasilo, O M

1994-01-01

Over a period of 2 years (January 1991 to December 1992) 274 cases of snake bite were admitted to hospital in the eight provinces of Zimbabwe. Of these patients, 54% were males and 88% belonged to the 6-40-year age group. Five deaths (1.8% of the total cases) were reported. The majority of snake bites (63%) occurred at night (between 6.30 p.m. and midnight) and over 74% took place during the hot rainy season, i.e. between November and April. In over 58% of the cases the victim accidentally stepped on the snake, the snake being cobra in 37%, puff adder in 20% and the black and green mamba in 18% of the cases. Most of the bites occurred on the leg, below the knee. Treatment of snake envenomation consisted mainly of the administration of antibiotics (151 cases), analgesics (144 cases), antivenom tropical snake polyvalent (ATT) (89 cases), antitoxoid tetanus (TT) (61 cases), antihistamines (47 cases) and traditional medicines (43 cases). This study indicates that snake envenomation in rural Zimbabwe is common but fatalities are relatively rare.

Development of modified-release dosage forms containing loratadine and pseudoephedrine sulfate.

PubMed

Sznitowska, Małgorzata; Cal, Krzysztof; Kupiec, Katarzyna

2004-12-01

Pseudoephedrine sulfate (PES) is a short-acting sympathomimetic amine and decongestant. Loratadine (L) is a long-acting antihistamine, H1 blocker. These drugs administered together provide relief from a whole range of rhinitis (hay fever) symptoms. Combination of both drugs is available in the form of sugar-coated modified-release tablets Clarinase (Schering-Plough). In this product, 5 mg of L and 60 mg of PES is present in the sugar-coating layer ready for an immediate release, and the rest of PES (60 mg) is incorporated in the extended-release core of the tablet. This enables fast as well as prolonged release of PES over 6-8 h. Because the sugar coating technologies are troublesome and rarely used nowadays, the aim of this study was to develop alternative oral dosage forms containing L (5 mg) and PES (120 mg). It was assumed that, similarly to the original product, the total dose of L and the half dose of PES should be released during 1 h and the remaining dose of PES ought to be gradually released for up to 8 h.

Treatment of nausea and vomiting in terminally ill cancer patients.

PubMed

Glare, Paul A; Dunwoodie, David; Clark, Katherine; Ward, Alicia; Yates, Patsy; Ryan, Sharon; Hardy, Janet R

2008-01-01

Nausea and vomiting is a common and distressing symptom complex in patients with far-advanced cancer, affecting up to 60% of individuals at some stage of their illness. The current approach to the palliative care of patients with nausea and vomiting is based on identifying the cause, understanding its pathophysiology and knowing the pharmacology of the drugs available for its amelioration. The following six main syndromes are identified: gastric stasis, biochemical, raised intracranial pressure, vestibular, mechanical bowel obstruction and ileus. A careful history, focused physical examination and appropriate investigations are needed to elucidate the syndrome and its cause, so that therapy is rational. Drugs are the mainstay of treatment in terminal cancer, and the main classes of antiemetic agents are prokinetics, dopamine antagonists, antihistamines, anticholinergics and serotonin antagonists. Dexamethasone and octreotide are also used, especially in bowel obstruction. Non-drug measures are important in relieving the associated distress. Patients should be able to die comfortably, without tubes. Despite decades of practice affirming this approach, the evidence base is weak and well designed studies are urgently needed.

Therapeutic Targeting of Eosinophil Adhesion and Accumulation in Allergic Conjunctivitis

PubMed Central

Baiula, Monica; Bedini, Andrea; Carbonari, Gioia; Dattoli, Samantha Deianira; Spampinato, Santi

2012-01-01

Considerable evidence indicates that eosinophils are important effectors of ocular allergy. Increased worldwide prevalence of allergic eye pathologies has stimulated the identification of novel drug targets, including eosinophils and adhesion molecules. Accumulation of eosinophils in the eye is a key event in the onset and maintenance of allergic inflammation and is mediated by different adhesion molecules. Antihistamines with multiple mechanisms of action can be effective during the early and late phases of allergic conjunctivitis by blocking the interaction between β1 integrins and vascular cell adhesion molecule (VCAM)-1. Small molecule antagonists that target key elements in the process of eosinophil recruitment have been identified and reinforce the validity of α4β1 integrin as a therapeutic target. Glucocorticoids are among the most effective drugs for ocular allergy, but their use is limited by adverse effects. Novel dissociated glucocorticoids can prevent eosinophil accumulation and induce apoptosis of eosinophils, making them promising candidates for ophthalmic drugs. This article reviews recent understanding of the role of adhesion molecules in eosinophil recruitment in the inflamed conjunctiva along with effective treatments for allergic conjunctivitis. PMID:23271999

Clinical efficacy of herbal Padmapatradi yoga in bronchial asthma (Tamaka Swasa)

PubMed Central

Panda, Ashok Kumar; Doddanagali, S. R.

2011-01-01

Ayurveda refers to bronchial asthma as Tamaka Swasa and it is well explained in Charaka Samhita. It contributes several modalities of the treatment for Swasa roga(asthma). Among all modalities of treatment, polyherbal combinations are said to be well-accepted, safe and effective in asthma. A study was carried out in 40 patients of either sex in between the age of 15-65 years to assure the clinical response of Padmapatradi yoga in bronchial asthma (Tamaka Swasa) at P.G. department of Kayachikitsa, D.G.M. Ayurvedic Medical College, Gadag, Karnataka. The sum total properties of Padmapatradi yoga is tikta katu rasa, laghu and tikna guna (light and penetrating properties), ushna virya (hot potency) and vatakaphagna (decrease vata and kapha dosa) Padmapatradi yoga is effective in increased peak expiratory flow rate, breath holding time, and reduces the absolute eosinophil count of studied cases and also found statistically highly significant at p<0.001 level. The drug is quite safe and acts as a bronchodilator, antihistaminic and anti-inflammatory. PMID:21760694

If 'atypical' neuroleptics did not exist, it wouldn't be necessary to invent them: perverse incentives in drug development, research, marketing and clinical practice.

PubMed

Charlton, Bruce G

2005-01-01

Perverse incentives in drug development, research, marketing and clinical usage can be illustrated by considering the example of the so-called 'atypical' neuroleptics which have grown to become a standard - indeed expanding - part of psychiatric practice despite their probable inferiority to older sedative agents. There is now ample evidence to suggest that neuroleptics (aka. anti-psychotics and major tranquillizers) are dangerous drugs, and patients' exposure to them should be minimized wherever possible. This clinical imperative applies whether neuroleptics are of the traditional type or atypical variety, albeit for different reasons since the traditional agents are neurotoxic, while atypicals are mainly metabolic poisons. Usage of traditional neuroleptics seems indeed to be declining progressively, but the opposite seems to be happening for 'atypicals', and new indications for these drugs are being promoted. Yet the atypical neuroleptics are a category of pharmaceuticals which are close to being un-necessary since there are safer, cheaper and pleasanter substitutes, such as benzodiazepines and the sedative antihistamines (e.g. promethazine). If 'atypical' neuroleptics did not exist, it would not be necessary to invent them. Analysis of how such expensive, dangerous and inferior drugs as the 'atypicals' have nevertheless come to dominate clinical practice casts light on the perverse incentives which now motivate the pharmaceutical industry in an era of massive state regulation. The lack of positive incentives to deploy off-patent drugs is longstanding, but there is a new disincentive in the widespread but erroneous belief that only randomized controlled trials (RCTs) can provide valid 'evidence' of effectiveness. Consequently, those who control RCTs now control clinical practice. It sometimes makes commercial sense to develop and market new drugs that are inferior to existing agents, since new drugs are patent-protected and can be promoted on the back of a mass

Attitudes and experiences of community pharmacists towards paediatric off-label prescribing: a prospective survey

PubMed Central

Stewart, Derek; Rouf, Abdul; Snaith, Ailsa; Elliott, Kathleen; Helms, Peter J; McLay, James S

2007-01-01

What is already known about this subject There are increasing concerns about the safety and efficacy of paediatric off-label medicines. In the UK, each year 26% of children receive an off-label prescription from their general practitioner. The community pharmacist is the final and key professional in the chain, with the responsibility to ensure that medicines are both prescribed and dispensed appropriately. What this study adds The majority of community pharmacists are aware of off-label prescribing, but through work experience rather than undergraduate or postgraduate training or professional development. Community pharmacists, like UK general practitioners, underestimate the levels of paediatric off-label prescribing, and appear unclear as to the most common reasons for a prescription being off label. Most community pharmacists stated that they should inform the prescriber that a medicine was off label; however, when given specific practical examples, less than half would actually appear to do so. The majority of community pharmacists have been asked by the public to sell over-the-counter medicines for paediatric off-label use. Aim To identify community pharmacist experiences of, and attitudes towards paediatric off-label prescribing. Methods A prospective questionnaire-based study, with a 21-item questionnaire issued to 1500 randomly selected community pharmacies throughout the UK during 2005 on three separate occasions. Results Four hundred and eighty-two (32.1%) completed questionnaires were returned. Over 70% of respondents were familiar with the concept of off-label prescribing, primarily through dispensing experience rather than education, although only 40% were aware of having dispensed a paediatric off-label prescription within the previous month. The reasons given for a prescription being off label were younger age than recommended (84.6%, 297/351), primarily for antihistamines, analgesics and β2-agonists, and higher (73.9%, 229/310) or lower than (41

Sleep complaints: Whenever possible, avoid the use of sleeping pills.

PubMed

2008-10-01

(1) Most sleep complaints involve difficulties in getting to sleep or staying asleep, or not feeling refreshed on awakening. Misconceptions and worrying over the lack of sleep and its consequences can contribute to reinforcing these disorders; (2) How can patients who complain of poor-quality sleep be helped, without resorting to treatments that can have adverse effects? To answer this question, we conducted a systematic review of the literature based on the standard Prescrire procedure; (3) One effective approach is to explain the basic physiology of sleep, to discuss misconceptions, and to adopt a strategy of "stimulus control". This method has a similar efficacy to prescribing a benzodiazepine. and the effect is longer lasting; (4) Moderate, regular physical exercise, especially in the morning, seems to help some patients, but the evidence is weak; (5) Some clinical trials of phytotherapy have shown a positive risk-benefit balance of weak aqueous or hydroalcoholic valerian extracts. Efficacy is limited, however; (6) A meta-analysis of placebo-controlled trials showed that benzodiazepines and related drugs increase the duration of sleep and help patients to fall asleep sooner. However, none of these trials provides comparative data spanning periods of more than two weeks. Efficacy is uncertain in the longer term, as patients quickly develop a tolerance to the hypnotic effects of benzodiazepines; (7) The adverse effects of benzodiazepines include frequent memory disorders, daytime drowsiness, falls, fractures and road accidents, and a withdrawal syndrome after treatment cessation. Related drugs such as zolpidem and zopiclone provoke similar adverse effects; (8) Sedative antihistamines have not been as well-evaluated as benzodiazepines in this setting. Small comparative trials of doxylamine and diphenhydramine showed no major difference in efficacy versus benzodiazepines and related drugs. The main adverse effects of sedative antihistamines are daytime drowsiness

CLINICAL AND TREATMENT FEATURES OF OPEN INFECTED FRACTURES IN THE KNEE JOINT REGION IN CONJUNCTION WITH RADIATION SICKNESS (EXPERIMENTAL STUDY)

DOE Office of Scientific and Technical Information (OSTI.GOV)

Sakharov, B.V.

1963-08-01

Clinical aspects and the course of treatment of open infected fractures in the knee joint region against a background of moderate and severe radiation sickness are discussed. The experiment involved 35 healthy dogs of both sexes. In all, three experiments were involved: on open infected fractures in the knee joint region in conjunction with radiation sickness; open infected fractures in the knee joint region without radiation sickness; radiation sickness without trauma. Infected open injury to the knee joint against a radiation sickness background is a severe affection. The use of delayed surgical and drug treatment (antibiotics, vitamins, antihistamine preparations) affordedmore » survival of at least one-half of the animals. Oral use of phenoxymethyl-penicillin in large doses established in the blood and synovial fluid of the damaged knee joint a therapeutic concentration of antibiotic of long duration (not less than a day). In radiation damage to knee joint accompanied by fracture of the bone fragment, the best method of surgical treatment is osteosynthesis using metal parts. In open infection of a damaged knee joint against a radiation sickness background, even with proper treatment a tendency toward formation of deforming arthrosis was observed. (OTS)« less

Survey of colourings and preservatives in drugs.

PubMed Central

Pollock, I.; Young, E.; Stoneham, M.; Slater, N.; Wilkinson, J. D.; Warner, J. O.

1989-01-01

OBJECTIVE--To assess the prevalence of colourings and preservatives in drug formulations in the United Kingdom. DESIGN--Postal survey. PARTICIPANTS--All pharmaceutical manufacturers in the United Kingdom were requested to supply data on drug formulations with particular regard to the content of colourings and preservatives. MAIN OUTCOME MEASURE--Prevalence in proprietary drugs of colourings or preservatives, or both, that have been implicated in adverse reactions. Computation of a list of formulations of bronchodilators, antihistamines, and antibiotics that are free of such additives. RESULTS--A total of 118 out of 120 pharmaceutical companies supplied the data requested. In all, 2204 drug formulations were analysed and found to contain 419 different additives, of which 52 were colourings and preservatives that have been implicated in adverse reactions; 930 formulations contained such an additive. Tartrazine was the fourth most commonly occurring colouring, being present in 124 drug formulations. CONCLUSION--Many drugs contain additives that help to identify them and prolong their shelf life but are implicated in adverse reactions in some people. Some form of labelling of drug additives would enable these people to avoid drugs containing such additives. PMID:2508849

[Anaphylaxis caused by royal jelly].

PubMed

Roger, A; Rubira, N; Nogueiras, C; Guspi, R; Baltasar, M; Cadahia, A

1995-01-01

Royal jelly is the food on which are fed and which causes them to develop into queen bees. It is claimed to have rejuvenating virtues for human beings. This report describes a 15-year-old atopic woman who presented, 15 minutes after the intake of royal jelly, local angioedema, generalised urticaria, dysphonia and bronchospasm. She was given antihistaminics and corticoesteroids and responded well. The ingested product contains royal jelly, lactose and potassium sorbate. No anaphylactic reactions to lactose and sorbates have been described previously. Prick test to common food allergens hymenoptera venoms and pollens were negative. RAST to meletin was also negative. Blood eosinophils were 600 and total IgE 465. Non-commercial prepared specific IgE to royal jelly was positive (0.8 KU/l). Prick by prick was positive to 1/10 dilution, being negative in controls (undiluted). No oral provocation test was performed due to the risk of anaphylaxis. No reported cases of royal jelly allergy were founded in a review of the medical literature. Concluding, it is the first described case of IgE anaphylactic reaction due to royal jelly.

Recreational use of dextromethorphan, "Robotripping"-A brief review.

PubMed

Stanciu, Cornel N; Penders, Thomas M; Rouse, Eden M

2016-08-01

Dextromethorphan (DXM) in combination with antihistamines and/or pseudoephedrine is widely available as an over-the counter remedy commonly used for relief of colds and cough. In supra-therapeutic amounts, DXM has psychoactive effects. These cough preparations have been adopted by many young users of recreational drugs for these effects. This paper aims to highlight the increasingly prevalent practice of Robotripping, review pharmacokinetic and dynamic data and discuss potential tolerance and withdrawal from the substance as well as treatment modalities. A Medline search (1985-2015) for literature concerning the DXM was conducted. This was supplemented by references gleaned from recent epidemiological surveys and credible online sources to ensure most up to date information is gathered. Use in amounts exceeding those recommended, a practice known as "Robotripping", may result in a toxidrome of psychomotor agitation, hallucinations and paranoia best characterized as Intoxication Delirium. Increasing misuse places greater numbers at risk. Providers should be alert to such presentations and be aware of methods for managing the symptoms. With chronic use, tolerance and withdrawal has been noted along with prolonging psychiatric sequelae. (Am J Addict 2016;25:374-377). © 2016 American Academy of Addiction Psychiatry.

Swift onset of central nervous system depression and asystole followingan overdose of Guaifenesin.

PubMed

Okic, Merisa; Johnson, Tom; Crifasi, Joseph A; Long, Christopher; Mitchell, Erik K

2013-06-01

Guaifenesin is an over-the-counter expectorant used for chest congestion and is available both in single-ingredient formulations and in combination with antihistamines, cough suppressants and decongestants. The documented side-effects of guaifenesin are generally mild. We present the case of a 23-year-old female who committed suicide by ingestion of guaifenesin along with small amounts of cetirizine, ethanol and sertraline. Approximately 2 h after ingestion, the patient experienced central nervous system depression followed by asystole. No anatomic cause of death could be determined at autopsy. The initial toxicology detected only ethanol, which was found at a concentration insufficient to cause death. Upon further analysis, guaifenesin was detected in femoral blood at 25.0 μg/mL, urine at >50.0 μg/mL, vitreous fluid at 9.2 μg/mL, brain at 17.0 μg/g and liver at 25.0 μg/g. This is the first reported human case that can be considered a death to which guaifenesin was the significant pharmacologic contributor. Guaifenesin is not detected by the primary screening methods employed by some labs and may be missed in toxicological analyses of overdoses unless specifically suspected.

Extended suicide using an atypical stud gun.

PubMed

Hagemeier, L; Schyma, C; Madea, B

2009-08-10

Suicides with stud guns are uncommon, but are well documented in the literature. On rare occasions, stud guns are also used as a homicide weapon. This case report describes an extended suicide in which a husband killed his wife and their two dogs, which lived on the property. The husband then committed suicide with a shot from the stud gun into his skull. He was a 70-year-old pensioner, a retired butcher, who was found by his son. He was lying in a supine position on a carpet in the living room, with the stud gun stuck in his skull. During autopsy, high concentrations of an antihistamine were found in the blood of each corpse; this drug is used as a soporific. In contrast to the literature, which mainly describes powder deposits due to the use of conventional stud guns, in this case a stud gun was used in which the expanding gases and powder escaped together with the central bolt at the front of the device; powder drains were not involved. Detailed findings of the autopsy are given with reference to this type of stud gun.

Phytochemicals to prevent inflammation and allergy.

PubMed

Bellik, Yuva; Hammoudi, Si M; Abdellah, Fatiha; Iguer-Ouada, Mokrane; Boukraâ, Laïd

2012-05-01

Recently, much interest has been generated for a wide range of phyto-constituents with reports demonstrating their role in the modulation of inflammatory responses, including phenolics, alkaloids, and terpenoids. Natural products have long been, over the years, contributed to the development of modern therapeutic drugs. At present, steroids, antihistaminic drugs, suppressants or inhibitors of the release of mediators and the like have been used as anti-allergic agents. However, some of them lack immediate effectiveness or have central side effects. Drug discovery from plants involves a multidisciplinary approach combining botanical, ethno-botanical, phytochemical and biological techniques. Several natural product drugs of plant origin are in clinical use and some are undergoing Phase II and Phase III clinical trials. A major effort was directed toward discovery of novel anti-inflammatory and anti-allergic agents, which resulted in the invention of several patented formulations. These formulations concern a variety of pharmaceutical preparations which can be used as solid or liquid dosage forms or encapsulated as a soft or hard gelatin capsule. The present article is a short review of recent patents on the role of phytochemicals in preventing inflammation and allergy.

Cough in children.

PubMed

Lamas, Adelaida; Ruiz de Valbuena, Marta; Máiz, Luis

2014-07-01

Cough during childhood is very common, and is one of the most frequent reasons for consultation in daily pediatric practice. The causes differ from those in adults, and specific pediatric guidelines should be followed for correct diagnosis and treatment. The most common cause of cough in children is viral infection producing "normal cough", but all children with persistent cough, i.e. a cough lasting more than 4-8weeks or "chronic cough", must be carefully evaluated in other to rule out specific causes that may include the entire pediatric pulmonology spectrum. The treatment of cough should be based on the etiology. Around 80% of cases can be diagnosed using an optimal approach, and treatment will be effective in 90% of them. In some cases of "nonspecific chronic cough", in which no underlying condition can be found, empirical treatment based on the cough characteristics may be useful. There is no scientific evidence to justify the use of over-the-counter cough remedies (anti-tussives, mucolytics and/or antihistamines), as they could have potentially serious side effects, and thus should not be prescribed in children. Copyright © 2013 SEPAR. Published by Elsevier Espana. All rights reserved.

Effect of ebastine on mosquito bites.

PubMed

Reunala, T; Brummer-Korvenkontio, H; Petman, L; Palosuo, T; Sarna, S

1997-07-01

Mosquito bites usually cause wealing and delayed bite papules. Cetirizine decreases wealing, bite papules and pruritus but the effect of other antihistamines on mosquito bites is unknown. We studied the effect of ebastine in 30 mosquito bite-sensitive adult subjects. Ebastine 10 mg or 20 mg and placebo were given for 4 days in a cross-over fashion. Aedes aegypti bites were given on forearms. The size of the bite lesions and pruritus (visual analogue score) were measured at 15 min, 2, 6, and 24 h after the bites. Twenty-five subjects were evaluable in the study. At 15 min ebastine decreased significantly the size of the bite lesion (p = 0.0017) and pruritus (p<0.0001). The effects of 10 mg and 20 mg of ebastine were similar. No significant effect was found at 2, 6 or 24 h, but when the measurements at all four time points were compiled the size of the bite lesion and pruritus score decreased significantly. Sedation occurred during ebastine treatment in 6 (21%) and during placebo treatment in 2 (7%) subjects. The present results show that prophylactically given ebastine is effective against immediate mosquito bite symptoms.

[Allergic rhinitis update and its impact on asthma (ARIA 2008). Latin American perspective].

PubMed

Cagnani, Carlos E Baena; Solé, Dirceu; Díaz, Sandra N González; Zernotti, Mario E; Sisul, Juan C; Borges, Mario Sánchez; Guzmán, María Antonieta; Ivancevich, Juan C; Cepeda, Alfonso; Pérez, Noel Rodríguez; Gereda, José; Cruz, Alvaro; Croce, Victor H; Khaltaev, Nikolai; Bousquet, Jean

2009-01-01

Rhinitis is the most frequent respiratory disease in most countries of the world. It is estimated that 600 million people suffer this condition. Allergic rhinitis is a public health problem at global level. Patients who suffer allergic rhinitis have from mild to annoying nasal symptoms which affect quality of life, cause sleep disorders, scholar and workplace absenteeism, and health expenditure. Rhinitis is frequently associated to co-morbidities such as sinusitis, otitis media, and especially asthma. Rhinitis is under-diagnosed and under-treated worldwide and also in Latin American countries. ARIA is the very first evidence-based guideline for the diagnosis and treatment of rhinitis with focus in its co-morbidities (2001), especially asthma published in 2001. In 2008 an update was published. ARIA recommends an integrative approach for management; including anti-histamines (second generation), intra-nasal corticosteroids, anti-leukotrienes and immunotherapy. It also provides a questionnaire to evaluate asthma and its severity in those patients suffering rhinitis. The prevalence of allergic rhinitis is quite high in Latin American countries and in recent years a great insight on the burden of this condition has been gained.

Desensitization to clopidogrel: a tailor-made protocol.

PubMed

Barreira, P; Cadinha, S; Malheiro, D; Moreira da Silva, J P

2014-01-01

Clopidogrel is an antiplatelet drug widely used for treatment and prevention of a variety of cardiovascular diseases. We report a successful desensitization to clopidogrel in a 70-year-old Caucasian man with delayed hypersensitivity (HS) reaction. He developed lip, hand and foot swelling, erythematous papular non-pruritic lesions and arthralgias 2 weeks after starting treatment with clopidogrel 75 mg/d. A 3-hour desensitization protocol was started, achieving a cumulative dose of 154 mg without any reaction, and a daily dose of 75 mg was recommended. On the 4th day, the patient developed skin lesions similar to the previously described. He was treated with topical steroids and oral antihistamines, and the daily dose of clopidogrel was reduced to 20 mg. A new desensitization protocol was established, with a slow dose increment, according to the patient's response. It was only possible to achieve the dose of 75 mg/d after 2 months. Although well tolerated by most patients, HS reactions with clopidogrel may occur and desensitization is rising as a safe alternative in those patients. In delayed reactions with cutaneous lesions, a slower desensitization protocol may be necessary, as in this case.

Eosinophilic cystitis with recurrent urinary retention: case report.

PubMed

Park, Hongzoo

2017-01-01

Eosinophilic cystitis is a rare inflammatory disease of the bladder whose origin, pathogenesis, and treatment are unknown. Frequency, dysuria, and hematuria are frequent symptoms. Here, we report a rare occurrence of recurrent urinary retention and repetitive catheterization. A 67-year-old male presented with acute urinary retention and intermittent gross hematuria of 2 weeks duration. Urethral catheterization followed by a trial without catheter, was successful. Complete blood count showed presence of eosinophils (eosinophilia) and computed tomography of kidneys, ureter and bladder with contrast showed thickened bladder wall and small prostate. Cystoscopy revealed an erythematous lesion over the anterior wall. The rest of the mucosa was normal. Transurethral biopsies of the lesion were performed and histologic examination showed features of eosinophilic cystitis. Despite multiple medication regimens containing corticosteroids and antihistamines, he presented with recurrent urinary retention, approximately once every month. After 6 months, he was started on bethanechol, which led to no catheterization for up to 2 years. To the best of our knowledge, this is the first report on the successful use of bethanechol as a treatment for eosinophilic cystitis with recurrent urinary retention.

Mastocytosis and insect venom allergy.

PubMed

Bonadonna, Patrizia; Zanotti, Roberta; Müller, Ulrich

2010-08-01

To analyse the association of systemic allergic hymenoptera sting reactions with mastocytosis and elevated baseline serum tryptase and to discuss diagnosis and treatment in patients with both diseases. In recent large studies on patients with mastocytosis a much higher incidence of severe anaphylaxis following hymenoptera stings than in the normal population was documented. In patients with hymenoptera venom allergy, elevated baseline tryptase is strongly associated with severe anaphylaxis. Fatal sting reactions were reported in patients with mastocytosis, notably after stopping venom immunotherapy. During venom immunotherapy most patients with mastocytosis are protected from further sting reactions. Based on these observations immunotherapy for life is recommended for patients with mastocytosis and venom allergy. The incidence of allergic side-effects is increased in patients with mastocytosis and elevated baseline tryptase, especially in those allergic to Vespula venom. Premedication with antihistamines, or omalizumab in cases with recurrent severe side-effects, can be helpful. In all patients with anaphylaxis following hymenoptera stings, baseline serum tryptase should be determined. A value above 11.4 microg/l is often due to mastocytosis and indicates a high risk of very severe anaphylaxis following re-stings. Venom immunotherapy is safe and effective in this situation.

A Case of Chromium Contact Dermatitis due to Exposure from a Golf Glove.

PubMed

Lim, Jong Ho; Kim, Hei Sung; Park, Young Min; Lee, Jun Young; Kim, Hyung Ok

2010-02-01

Chromium is a transition metal and has been shown to elicit contact dermatitis. Although leather products have been known to be the most significant source of chromium exposure these days, the majority of reports have been related to exposure from shoe products. We herein report a professional golfer who became allergic to golf gloves made of chromium-tanned leather. A 27-year-old woman golfer presented with recurrent, pruritic, erythematous plaques that had been occurring on both hands for several years. The lesions developed whenever she had worn golf gloves for an extended period of time, especially during tournament season. To identify the causative agent, patch tests were performed and the results demonstrated a strong positive reaction to potassium dichromate 0.5% and to her own glove. The amount of chromium in her golf glove was analyzed to be 308.91 ppm and based on this, a diagnosis of allergic contact dermatitis due to a chromium-tanned leather glove was made. She was treated with oral antihistamines combined with topical steroids and advised to wear chromium-free leather gloves. There has been no evidence of recurrence during a six month follow-up period.

Endonasal phototherapy with Rhinolight for the treatment of allergic rhinitis.

PubMed

Brehmer, Detlef

2010-01-01

Allergic rhinitis, although not life threatening, significantly affects the quality of the patient's daily life. The three major steps in the treatment of the condition are avoidance of allergens, treatment of symptoms (in particular, antihistaminics and topical nasal corticosteroids) and specific immunotherapy. Avoidance of the allergen is usually not possible and symptom relief is often limited, despite the availability of a number of pharmacological options. Specific immunotherapy demands a high level of cooperation on the part of the patient for at least 3 years. Endonasal phototherapy with the Rhinolight device (Rhinolight Ltd, Szeged, Hungary) for the treatment of immunoglobulin E-mediated allergic rhinitis is a new option that utilizes the immunosuppressive effects of UV radiation. The method directs a combination of UV-B (5%), UV-A (25%) and visible light (70%) into the nasal cavity, and its effectiveness has been demonstrated in one double-blind, placebo-controlled study. The results of additional studies have been presented at various medical conferences and in abstracts. Reports in the literature confirm that phototherapy is a well-established and successful treatment of atopic dermatitis and other skin diseases.

Neutralization of the oedematogenic activity of Bothrops jararaca venom on the mouse paw by an antibothropic fraction isolated from opossum (Didelphis marsupialis) serum.

PubMed

Perales, J; Amorim, C Z; Rocha, S L; Domont, G B; Moussatché, H

1992-11-01

The pharmacological modulation of mice paw oedema produced by Bothrops jararaca venom (BJV) has been studied. Intraplantar injection of BJV (1-30 micrograms/paw) produced a dose- and time-related oedema, which was maximal 30 min after injection, reduced gradually thereafter and disappeared over 48 h. BJV heated at 100 degrees C for 5 or 15 min blocked local hemorrhage and caused partial inhibition of its oedematogenic activity. The BJV oedema was not inhibited by the anti-histamine meclizine, the inhibitor of histamine and serotonin, cyproheptadine, PAF-acether antagonist WEB 2170 or by the anti-leukotrienes C4/D4, LY 171883. Dexamethasone, aspirin, indomethacin, and the dual cyclooxygenase and lipoxygenase inhibitor BW 755C inhibited BJV-induced oedema indicating that arachidonic acid metabolism products via the cyclooxygenase pathway participate in its genesis and/or maintenance. The antibothropic fraction (ABF) (25-200 micrograms/paw) isolated from Didelphis marsupialis serum neutralized the oedema induced by the venom with and without heating, the hemorrhage induced by BJV and partially blocked the oedema induced by bradykinin and by cellulose sulphate. The oedema produced by histamine, serotonin, PAF-acether or leukotriene C4 was not inhibited.

Ocular Jellyfish Stings: Report of 2 Cases and Literature Review.

PubMed

Mao, Chen; Hsu, Chien-Chin; Chen, Kuo-Tai

2016-09-01

An ocular jellyfish sting is an ophthalmic emergency and is rarely reported in the medical literature. With the evolution of aquatic activities and entertainment in recent decades, we anticipate that more patients with ocular jellyfish stings may be taken to the emergency department. However, most physicians are unaware of the typical presentations, suitable treatments, prognosis, and possible complications of ocular jellyfish stings. We reported 2 cases with ocular jellyfish stings and collected cases series from literature review. The most common clinical features of ocular jellyfish stings were pain, conjunctival injection, corneal lesion, and photophobia. All patients who sustained ocular stings did so during aquatic activities, and the best management at the scene was proper analgesics and copious irrigation of affected eyes with seawater or saline. The ocular lesions were treated with topical cycloplegics, topical steroids, topical antibiotics, topical antihistamines, and removal of nematocysts. The prognosis was good, and all patients recovered without any permanent sequelae. However, symptoms in some patients may last longer than 1 week. Reported complications included iritis, increased intraocular pressures, mydriasis, decreased accommodation, and peripheral anterior synechiae. Copyright © 2016 Wilderness Medical Society. Published by Elsevier Inc. All rights reserved.

In Vivo and In Vitro Toxicity Evaluation of Hydroethanolic Extract of Kalanchoe brasiliensis (Crassulaceae) Leaves.

PubMed

Fonseca, Aldilane Gonçalves; Ribeiro Dantas, Luzia Leiros Sena Fernandes; Fernandes, Júlia Morais; Zucolotto, Silvana Maria; Lima, Adley Antoninni Neves; Soares, Luiz Alberto Lira; Rocha, Hugo Alexandre Oliveira; Lemos, Telma Maria Araújo Moura

2018-01-01

The species Kalanchoe brasiliensis , known as "Saião , " has anti-inflammatory, antimicrobial, and antihistamine activities. It also has the quercetin and kaempferol flavonoids, which exert their therapeutic activities. With extensive popular use besides the defined therapeutical properties, the study of possible side effects is indispensable. The objective of this study is to evaluate the toxicity in vitro and in vivo from the hydroethanolic extract of the leaves of K. brasiliensis . The action of the extract (concentrations from 0.1 to 1000 uL/100 uL) in normal and tumor cells was evaluated using the MTT method. Acute toxicity and subchronic toxicity were evaluated in mice with doses of 250 to 1000 mg/kg orally, following recognized protocols. The in vitro results indicated cytotoxic activity for 3T3 cell line (normal) and 786-0 (kidney carcinoma), showing the activity to be concentration-dependent, reaching 92.23% cell inhibition. In vivo , the extract showed no significant toxicity; only liver changes related to acute toxicity and some signs of liver damage, combining biochemical and histological data. In general, the extract showed low or no toxicity, introducing itself as safe for use with promising therapeutic potential.

CHRONIC URTICARIA

PubMed Central

Sachdeva, Sandeep; Gupta, Vibhanshu; Amin, Syed Suhail; Tahseen, Mohd

2011-01-01

Chronic urticaria (CU) is a disturbing allergic condition of the skin. Although frequently benign, it may sometimes be a red flag sign of a serious internal disease. A multitude of etiologies have been implicated in the causation of CU, including physical, infective, vasculitic, psychological and idiopathic. An autoimmune basis of most of the ‘idiopathic’ forms is now hypothesized. Histamine released from mast cells is the major effector in pathogenesis and it is clinically characterized by wheals that have a tendency to recur. Laboratory investigations aimed at a specific etiology are not always conclusive, though may be suggestive of an underlying condition. A clinical search for associated systemic disease is strongly advocated under appropriate circumstances. The mainstay of treatment remains H1 antihistaminics. These may be combined with complementary pharmacopeia in the form of H2 blockers, doxepin, nifedipine and leukotriene inhibitors. More radical therapy in the form of immunoglobulins, plasmapheresis and cyclophosphamide may be required for recalcitrant cases. Autologous transfusion and alternative remedies like acupuncture have prospects for future. A stepwise management results in favorable outcomes. An update on CU based on our experience with patients at a tertiary care centre is presented. PMID:22345759

Involvement of Histamine and RhoA/ROCK in Penicillin Immediate Hypersensitivity Reactions.

PubMed

Han, Jiayin; Yi, Yan; Li, Chunying; Zhang, Yushi; Wang, Lianmei; Zhao, Yong; Pan, Chen; Liang, Aihua

2016-09-13

The mechanism of penicillin immediate hypersensitivity reactions has not been completely elucidated. These reactions are generally considered to be mediated by IgE, but penicillin-specific IgE could not be detected in most cases. This study demonstrated that penicillin was able to cause vascular hyperpermeability in a mouse model mimicking clinical symptoms of penicillin immediate hypersensitivity reactions. The first exposure to penicillin also induced immediate edema and exudative reactions in ears and lungs of mice in a dose-dependent manner. Vasodilation was noted in microvessels in ears. These reactions were unlikely to be immune-mediated reactions, because no penicillin-specific IgE was produced. Furthermore, penicillin treatment directly elicited rapid histamine release. Penicillin also led to F-actin reorganization in human umbilical vein endothelial cells and increased the permeability of the endothelial monolayer. Activation of the RhoA/ROCK signaling pathway was observed in ears and lungs of mice and in endothelial cells after treatment with penicillin. Both an anti-histamine agent and a ROCK inhibitor attenuated penicillin immediate hypersensitivity reactions in mice. This study presents a novel mechanism of penicillin immediate hypersensitivity reactions and suggests a potential preventive approach against these reactions.

Involvement of Histamine and RhoA/ROCK in Penicillin Immediate Hypersensitivity Reactions

PubMed Central

Han, Jiayin; Yi, Yan; Li, Chunying; Zhang, Yushi; Wang, Lianmei; Zhao, Yong; Pan, Chen; Liang, Aihua

2016-01-01

The mechanism of penicillin immediate hypersensitivity reactions has not been completely elucidated. These reactions are generally considered to be mediated by IgE, but penicillin-specific IgE could not be detected in most cases. This study demonstrated that penicillin was able to cause vascular hyperpermeability in a mouse model mimicking clinical symptoms of penicillin immediate hypersensitivity reactions. The first exposure to penicillin also induced immediate edema and exudative reactions in ears and lungs of mice in a dose-dependent manner. Vasodilation was noted in microvessels in ears. These reactions were unlikely to be immune-mediated reactions, because no penicillin-specific IgE was produced. Furthermore, penicillin treatment directly elicited rapid histamine release. Penicillin also led to F-actin reorganization in human umbilical vein endothelial cells and increased the permeability of the endothelial monolayer. Activation of the RhoA/ROCK signaling pathway was observed in ears and lungs of mice and in endothelial cells after treatment with penicillin. Both an anti-histamine agent and a ROCK inhibitor attenuated penicillin immediate hypersensitivity reactions in mice. This study presents a novel mechanism of penicillin immediate hypersensitivity reactions and suggests a potential preventive approach against these reactions. PMID:27619816

Perinatal Anxiety: Approach to Diagnosis & Management in the Obstetric Setting.

PubMed

Thorsness, Katie R; Watson, Corey; Larusso, Elizabeth M

2018-05-24

Anxiety is common in women during the perinatal period, manifests with various symptomatology and severity, and is associated with significant maternal morbidity and adverse obstetrical and neonatal outcomes. Given the intimate relationship and frequency of contact, the obstetric provider is optimally positioned to create a therapeutic alliance and manage perinatal anxiety. Time constraints, absence of randomized controlled trials, mixed quality of data, and concern for potential adverse reproductive outcomes all limit clinicians' ability to initiate informed risk-benefit discussions. Clear understanding of the role of the obstetric provider in the identification, stabilization, and initiation of medication and/or referral to psychotherapy for women with perinatal anxiety disorders is critical to maternal and neonatal wellbeing. Informed by our clinical practice as perinatal psychiatric providers, we have provided a concise summary of current research on the approach to treatment of perinatal anxiety disorders in the obstetric setting, including psychotherapy and supportive interventions, primary and adjuvant psychiatric medication, and general prescribing pearls. Medications examined include antidepressants, benzodiazepines, sedative-hypnotics, antihistamines, quetiapine, buspirone, propranolol, and melatonin. Further research into management of perinatal anxiety, particularly psychopharmacological management, is warranted. Copyright © 2018 Elsevier Inc. All rights reserved.

Antivenom potential of ethanolic extract of Cordia macleodii bark against Naja venom.

PubMed

Soni, Pranay; Bodakhe, Surendra H

2014-05-01

To evaluate the antivenom potential of ethanolic extract of bark of Cordia macleodii against Naja venom induced pharmacological effects such as lethality, hemorrhagic lesion, necrotizing lesion, edema, cardiotoxicity and neurotoxicity. Wistar strain rats were challenged with Naja venom and treated with the ethanolic extract of Cordia macleodii bark. The effectiveness of the extract to neutralize the lethalities of Naja venom was investigated as recommended by WHO. At the dose of 400 and 800 mg/kg ethanolic extract of Cordia macleodii bark significantly inhibited the Naja venom induced lethality, hemorrhagic lesion, necrotizing lesion and edema in rats. Ethanolic extract of Cordia macleodii bark was effective in neutralizing the coagulant and defibrinogenating activity of Naja venom. The cardiotoxic effects in isolated frog heart and neurotoxic activity studies on frog rectus abdominus muscle were also antagonized by ethanolic extract of Cordia macleodii bark. It is concluded that the protective effect of extract of Cordia macleodii against Naja venom poisoning may be mediated by the cardiotonic, proteolysin neutralization, anti-inflammatory, antiserotonic and antihistaminic activity. It is possible that the protective effect may also be due to precipitation of active venom constituents.

Antivenom potential of ethanolic extract of Cordia macleodii bark against Naja venom

PubMed Central

Soni, Pranay; Bodakhe, Surendra H.

2014-01-01

Objective To evaluate the antivenom potential of ethanolic extract of bark of Cordia macleodii against Naja venom induced pharmacological effects such as lethality, hemorrhagic lesion, necrotizing lesion, edema, cardiotoxicity and neurotoxicity. Methods Wistar strain rats were challenged with Naja venom and treated with the ethanolic extract of Cordia macleodii bark. The effectiveness of the extract to neutralize the lethalities of Naja venom was investigated as recommended by WHO. Results At the dose of 400 and 800 mg/kg ethanolic extract of Cordia macleodii bark significantly inhibited the Naja venom induced lethality, hemorrhagic lesion, necrotizing lesion and edema in rats. Ethanolic extract of Cordia macleodii bark was effective in neutralizing the coagulant and defibrinogenating activity of Naja venom. The cardiotoxic effects in isolated frog heart and neurotoxic activity studies on frog rectus abdominus muscle were also antagonized by ethanolic extract of Cordia macleodii bark. Conclusions It is concluded that the protective effect of extract of Cordia macleodii against Naja venom poisoning may be mediated by the cardiotonic, proteolysin neutralization, anti-inflammatory, antiserotonic and antihistaminic activity. It is possible that the protective effect may also be due to precipitation of active venom constituents. PMID:25183127

Desensitization of B-adrenergic receptors following repeated injections of 2-substituted-4-phenylquinolines

DOE Office of Scientific and Technical Information (OSTI.GOV)

Alhaider, A.A.

1986-03-05

In a previous work, they synthesized some new 2-substituted-4-phenylquinoline derivatives which demonstrated potent antidepressant activities as revealed by their antagonism to the uptake of /sup 3/(H)-norepinephrine and /sup 3/(H)-serotonin into brain synaptosomal preparation. Also, these compounds have demonstrated less anticholinergic, antihistamine and cardiovascular effects as compared to imipramine in animal models. In this present work, the chronic effects of some of these compounds on the sensitivity of the noradrenergic cyclic-AMP generating system on rat brain cortex has been conducted by the daily injection of 20 mg/kg i.p. for a period of three weeks. Imipramine and trazodone were utilized as standards,more » representing typical and atypical antidepressants, respectively. Acute treatment (single dose 20 mg/kg) and subchronic treatment (20 mg/kg for 10 days) produced no significant desensitization of the B-adrenoceptors. However, chronic treatment with the compounds significantly decreased isoprenaline-induced increase in c-AMP in the cortex which suggests desensitization of B-adrenoceptors. This effect coupled with the previous findings point to a potential rule of these compounds as suitable antidepressant candidates.« less

[Outbreak of dermatitis caused by pine processionary caterpillar (Thaumetopoea pityocampa) in schoolchildren].

PubMed

Artola-Bordás, F; Arnedo-Pena, A; Romeu-García, M A; Bellido-Blasco, J B

2008-01-01

To describe a dermatitis outbreak caused by exposure to pine processionary caterpillar (Thaumetopoea pityocampa ) that took place on March 15th, 2006, in schoolchildren during their stay at a rural farm holiday centre in Villahermosa del Río (Castellón). A cross sectional epidemiological study was carried out on seventy schoolchildren, average age 10 years, and 3 teachers from Castellón. A specific questionnaire was used to be filled in by the schoolchildren. Six cases of dermatitis (attack rate 8.6%: 6/70) took place after children had swum in the heated farm pool and dried themselves with towels that had been left outside the heated pool enclosure, where they had come into contact with Thaumetopoea pityocampa. The cases needed medical attention, with prescription of antihistamine drugs, corticosteroids, and cold showers. The risk of dermatitis from contact with Thaumetopoea pityocampa was very high (Odds Ratio=157.2 Confidence Interval 95% 18.4-inf). Thaumetopoea pityocampa were collected near the swimming pool and Thaumetopoea pityocampa nests were observed on nearby pines. The presence of Thaumetopoea pityocampa near rural centres can cause outbreaks. Health education for schoolchildren and the removal of Thaumetopoea pityocampa nests near these centres are required.

Exposure to heavy charged particles affects thermoregulation in rats

DOE Office of Scientific and Technical Information (OSTI.GOV)

Kandasamy, S.B.; Hunt, W.A.; Dalton, T.K.

1994-09-01

Rats exposed to 0.1-5 Gy of heavy particles ({sup 56}Fe, {sup 40}Ar, {sup 20}Ne or {sup 4}He) showed dose-dependent changes in body temperature. Lower doses of all particles produced hyperthermia, and higher doses of {sup 20}Ne and {sup 56}Fe produced hypothermia. Of the four HZE particles, {sup 56}Fe particles were the most potent and {sup 4}He particles were the least potent in producing changes in thermoregulation. The {sup 20}Ne and {sup 40}Ar particles produced an intermediate level of change in body temperature. Significantly greater hyperthermia was produced by exposure to 1 Gy of {sup 20}Ne, {sup 40}Ar and {sup 56}Femore » particles than by exposure to 1 Gy of {sup 60}Co {gamma} rays. Pretreating rats with the cyclo-oxygenase inhibitor indomethacin attenuated the hyperthermia produced by exposure to 1 Gy of {sup 56}Fe particles, indicating that prostaglandins mediate {sup 56}Fe-particle-induced hyperthermia. The hypothermia produced by exposure to 5 Gy of {sup 56}Fe particles is mediated by histamine and can be attenuated by treatment with the antihistamines mepyramine and cimetidine. 15 refs., 4 figs.« less

Subcutaneous infiltration of doxylamine on cutaneous analgesia in rats.

PubMed

Hung, Ching-Hsia; Shieh, Ja-Ping; Chiu, Chong-Chi; Wang, Jhi-Joung; Chen, Yu-Wen

2018-06-01

We aimed to evaluate the effect of doxylamine, a first generation antihistamine, as a local analgesic agent by comparing its effect to bupivacaine. After blocking the cutaneous trunci muscle reflex (CTMR) by subcutaneous injection of doxylamine, we assessed doxylamine's cutaneous analgesic effect in rats. The dose-related effect and duration of doxylamine on infiltrative cutaneous analgesia were compared with that of bupivacaine. We demonstrated that doxylamine, as well as the local anesthetic bupivacaine produced the cutaneous analgesic effects in a dose-related fashion. At the equipotent dose (50% effective doses (ED 50 )), the relative potency was bupivacaine (0.41 (0.36-0.48) mmol)> doxylamine (7.39 (6.91-7.91)mmol) (p<0.01). On an equipotent basis (ED 25 , ED 50 and ED 75 ), subcutaneous doxylamine resulted in greater duration of action (p<0.01) than bupivacaine at producing cutaneous analgesia. The result of this experiment indicated that doxylamine has the local anesthetic property less potent than bupivacaine, but its nociceptive block duration is longer than that of bupivacaine at an equianalgesic dose. Copyright © 2017 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier B.V. All rights reserved.

Extraction and Determination of Cyproheptadine in Human Urine by DLLME-HPLC Method

PubMed Central

Maham, Mehdi; Kiarostami, Vahid; Waqif-Husain, Syed; Abroomand-Azar, Parviz; Tehrani, Mohammad Saber; Khoeini Sharifabadi, Malihe; Afrouzi, Hossein; Shapouri, MahmoudReza; Karami-Osboo, Rouhollah

2013-01-01

Novel dispersive liquid-liquid microextraction (DLLME), coupled with high performance liquid chromatography with photodiode array detection (HPLC-DAD) has been applied for the extraction and determination of cyproheptadine (CPH), an antihistamine, in human urine samples. In this method, 0.6 mL of acetonitrile (disperser solvent) containing 30 μL of carbon tetrachloride (extraction solvent) was rapidly injected by a syringe into 5 mL urine sample. After centrifugation, the sedimented phase containing enriched analyte was dissolved in acetonitrile and an aliquot of this solution injected into the HPLC system for analysis. Development of DLLME procedure includes optimization of some important parameters such as kind and volume of extraction and disperser solvent, pH and salt addition. The proposed method has good linearity in the range of 0.02-4.5 μg mL-1 and low detection limit (13.1 ng mL-1). The repeatability of the method, expressed as relative standard deviation was 4.9% (n = 3). This method has also been applied to the analysis of real urine samples with satisfactory relative recoveries in the range of 91.6-101.0%. PMID:24250605

Extraction and Determination of Cyproheptadine in Human Urine by DLLME-HPLC Method.

PubMed

Maham, Mehdi; Kiarostami, Vahid; Waqif-Husain, Syed; Abroomand-Azar, Parviz; Tehrani, Mohammad Saber; Khoeini Sharifabadi, Malihe; Afrouzi, Hossein; Shapouri, Mahmoudreza; Karami-Osboo, Rouhollah

2013-01-01

Novel dispersive liquid-liquid microextraction (DLLME), coupled with high performance liquid chromatography with photodiode array detection (HPLC-DAD) has been applied for the extraction and determination of cyproheptadine (CPH), an antihistamine, in human urine samples. In this method, 0.6 mL of acetonitrile (disperser solvent) containing 30 μL of carbon tetrachloride (extraction solvent) was rapidly injected by a syringe into 5 mL urine sample. After centrifugation, the sedimented phase containing enriched analyte was dissolved in acetonitrile and an aliquot of this solution injected into the HPLC system for analysis. Development of DLLME procedure includes optimization of some important parameters such as kind and volume of extraction and disperser solvent, pH and salt addition. The proposed method has good linearity in the range of 0.02-4.5 μg mL(-1) and low detection limit (13.1 ng mL(-1)). The repeatability of the method, expressed as relative standard deviation was 4.9% (n = 3). This method has also been applied to the analysis of real urine samples with satisfactory relative recoveries in the range of 91.6-101.0%.

Development, Validation and Application of RP-HPLC Method: Simultaneous Determination of Antihistamine and Preservatives with Paracetamol in Liquid Formulations and Human Serum.

PubMed

Hasan, Najmul; Chaiharn, Mathurot; Toor, Umair Ali; Mirani, Zulfiqar Ali; Sajjad, Ghulam; Sher, Nawab; Aziz, Mubashir; Siddiqui, Farhan Ahmed

2016-01-01

In this article we describe development and validation of stability indicating, accurate, specific, precise and simple Ion-pairing RP-HPLC method for simultaneous determination of paracetamol and cetirizine HCl along with preservatives i.e. propylparaben, and methylparaben in pharmaceutical dosage forms of oral solution and in serum. Acetonitrile: Buffer: Sulfuric Acid (45:55:0.3 v/v/v) was the mobile phase at flow rate 1.0 mL min(-1) using a Hibar(®) Lichrosorb(®) C18 column and monitored at wavelength of 230nm. The averages of absolute and relative recoveries were found to be 99.3%, 99.5%, 99.8% and 98.7% with correlation coefficient of 0.9977, 0.9998, 0.9984, and 0.9997 for cetirizine HCl, paracetamol, methylparaben and Propylparaben respectively. The limit of quantification and limit of detection were in range of 0.3 to 2.7 ng mL(-1) and 0.1 to 0.8 ng mL(-1) respectively. Under stress conditions of acidic, basic, oxidative, and thermal degradation, maximum degradation was observed in basic and oxidative stress where a significant impact was observed while all drugs were found almost stable in the other conditions. The developed method was validated in accordance with ICH and AOAC guidelines. The proposed method was successfully applied to quantify amount of paracetamol, cetirizine HCl and two most common microbial preservatives in bulk, dosage form and physiological fluid.

Development, Validation and Application of RP-HPLC Method: Simultaneous Determination of Antihistamine and Preservatives with Paracetamol in Liquid Formulations and Human Serum

PubMed Central

Hasan, Najmul; Chaiharn, Mathurot; Toor, Umair Ali; Mirani, Zulfiqar Ali; Sajjad, Ghulam; Sher, Nawab; Aziz, Mubashir; Siddiqui, Farhan Ahmed

2016-01-01

In this article we describe development and validation of stability indicating, accurate, specific, precise and simple Ion-pairing RP-HPLC method for simultaneous determination of paracetamol and cetirizine HCl along with preservatives i.e. propylparaben, and methylparaben in pharmaceutical dosage forms of oral solution and in serum. Acetonitrile: Buffer: Sulfuric Acid (45:55:0.3 v/v/v) was the mobile phase at flow rate 1.0 mL min-1 using a Hibar® Lichrosorb® C18 column and monitored at wavelength of 230nm. The averages of absolute and relative recoveries were found to be 99.3%, 99.5%, 99.8% and 98.7% with correlation coefficient of 0.9977, 0.9998, 0.9984, and 0.9997 for cetirizine HCl, paracetamol, methylparaben and Propylparaben respectively. The limit of quantification and limit of detection were in range of 0.3 to 2.7 ng mL-1 and 0.1 to 0.8 ng mL-1 respectively. Under stress conditions of acidic, basic, oxidative, and thermal degradation, maximum degradation was observed in basic and oxidative stress where a significant impact was observed while all drugs were found almost stable in the other conditions. The developed method was validated in accordance with ICH and AOAC guidelines. The proposed method was successfully applied to quantify amount of paracetamol, cetirizine HCl and two most common microbial preservatives in bulk, dosage form and physiological fluid. PMID:27651840

Validated sensitive spectrofluorimetric method for determination of antihistaminic drug azelastine HCl in pure form and in pharmaceutical dosage forms: application to stability study.

PubMed

El-Masry, Amal A; Hammouda, Mohammed E A; El-Wasseef, Dalia R; El-Ashry, Saadia M

2017-03-01

A highly sensitive, simple and rapid spectrofluorimetric method was developed for the determination of azelastine HCl (AZL) in either its pure state or pharmaceutical dosage form. The proposed method was based on measuring the native fluorescence of the studied drug in 0.2 M H 2 SO 4 at λ em  = 364 nm after excitation at λ ex  = 275 nm. Different experimental parameters were studied and optimized carefully to obtain the highest fluorescence intensity. The proposed method showed a linear dependence of the fluorescence intensity on drug concentration over a concentration range of 10-250 ng/mL, with a limit of detection of 1.52 ng/mL and limit of quantitation of 4.61 ng/mL. Moreover, the method was successfully applied to pharmaceutical preparations, with percent recovery values (± SD) of 99.96 (± 0.4) and 100.1 (± 0.52) for nasal spray and eye drops, respectively. The results were in good agreement with those obtained by the comparison method, as revealed by Student's t-test and the variance ratio F-test. The method was extended to study the stability of AZL under stress conditions, where the drug was exposed to neutral, acidic, alkaline, oxidative and photolytic degradation according to International Conference on Harmonization (ICH) guidelines. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

What's new in atopic eczema? An analysis of systematic reviews published in 2012 and 2013. Part 2. Treatment and prevention.

PubMed

Madhok, V; Futamura, M; Thomas, K S; Barbarot, S

2015-06-01

This review provides a summary of key findings from 22 systematic reviews on atopic eczema (AE) published over the 2-year period from January 2012 to 31 December 2013, focusing on prevention and treatment of AE. For an update of systematic reviews on the epidemiology, mechanisms of disease and methodological issues, see Part 1 of this update. Based on current systematic review evidence, the most promising intervention for the prevention of AE is the use of probiotics (and possibly prebiotics) during the late stages of pregnancy and early life. Exposure to household pets, especially dogs, may also be protective, but exclusive breastfeeding for up to 7 months does not confer benefit. The role of vitamin D in preventing AE is currently unclear. Very few of the systematic reviews provided additional evidence for the use of specific treatments for AE. Further research is required to establish the role of desensitization, Chinese herbal medicines, homeopathy and specialist clothing. Nevertheless, there is now clear evidence that evening primrose oil and borage oil are not effective for the treatment of AE. There have been no randomized controlled trials on the use of H1 anti-histamines as monotherapy for the treatment of AE. © 2015 British Association of Dermatologists.

Proteomic changes in Corbicula fluminea exposed to wastewater from a psychiatric hospital.

PubMed

Bebianno, M J; Sroda, S; Gomes, T; Chan, P; Bonnafe, E; Budzinski, H; Geret, F

2016-03-01

The increase use of pharmaceutical compounds in veterinary practice and human population results in the ubiquitous presence of these compounds in aquatic ecosystems. Because pharmaceuticals are highly bioactive, there is concern about their toxicological effects in aquatic organisms. Therefore, the aim of this study was to assess the effects of an effluent from a psychiatric hospital (containing a complex mixture of 25 pharmaceutical compounds from eleven therapeutic classes) on the freshwater clam Corbicula fluminea using a proteomic approach. The exposure of C. fluminea to this complex effluent containing anxiolytics, analgesics, lipid regulators, beta blockers, antidepressants, antiepileptics, antihistamines, antihypertensives, antiplatelets and antiarrhythmics induced protein changes after 1 day of exposure in clam gills and digestive gland more evident in the digestive gland. These changes included increase in the abundance of proteins associated with structural (actin and tubulin), cellular functions (calreticulin, proliferating cell nuclear antigen (PCNA), T complex protein 1 (TCP1)) and metabolism (aldehyde dehydrogenase (ALDH), alcohol dehydrogenase, 6 phosphogluconate dehydrogenase). Results from this study indicate that calreticulin, PCNA, ALDH and alcohol dehydrogenase in the digestive gland and T complex protein 1 (TCP1)) and 6 phosphogluconate dehydrogenase in the gills represent useful biomarkers for the ecotoxicological characterization of psychiatric hospital effluents in this species.

A comparison of the leaf gel extracts of Aloe ferox and Aloe vera in the topical treatment of atopic dermatitis in Balb/c mice.

PubMed

Finberg, M J; Muntingh, G L; van Rensburg, C E J

2015-12-01

Aloe vera gel is widely used in the treatment of an array of disturbances, especially skin disorders. The wound-healing effects have been attributed to its moisturizing and anti-inflammatory effects as well as its beneficial effect on the maturation of collagen. The aim of the present study is to compare the effects of topically applied extracts of Aloe ferox with that of Aloe vera on the symptoms as well as IgE levels of a mouse model of atopic dermatitis (AD). Mice were sensitized and challenged with 2,4-dinitrochlorobenzene and treated afterwards for 10 consecutive days with the gels of either A. ferox or A. vera applied topically to the affected areas. A placebo gel was used for the control mice. Blood was collected at the beginning and end of the treatment period to measure serum IgE levels. Although the gels of both the Aloe species inhibited the cutaneous inflammatory response as well as serum IgE levels in the rats, the extracts of A. ferox were superior to that of A. vera in reducing IgE levels. The gels of A. ferox and A. vera, applied topically, may be a safe and useful alternative to antihistamines and topical corticosteroids, for the treatment of patients suffering from recurring chronic AD.

The auditory cross-section (AXS) test battery: A new way to study afferent/efferent relations linking body periphery (ear, voice, heart) with brainstem and cortex

NASA Astrophysics Data System (ADS)

Lauter, Judith

2002-05-01

Several noninvasive methods are available for studying the neural bases of human sensory-motor function, but their cost is prohibitive for many researchers and clinicians. The auditory cross section (AXS) test battery utilizes relatively inexpensive methods, yet yields data that are at least equivalent, if not superior in some applications, to those generated by more expensive technologies. The acronym emphasizes access to axes-the battery makes it possible to assess dynamic physiological relations along all three body-brain axes: rostro-caudal (afferent/efferent), dorso-ventral, and right-left, on an individually-specific basis, extending from cortex to the periphery. For auditory studies, a three-level physiological ear-to-cortex profile is generated, utilizing (1) quantitative electroencephalography (qEEG); (2) the repeated evoked potentials version of the auditory brainstem response (REPs/ABR); and (3) otoacoustic emissions (OAEs). Battery procedures will be explained, and sample data presented illustrating correlated multilevel changes in ear, voice, heart, brainstem, and cortex in response to circadian rhythms, and challenges with substances such as antihistamines and Ritalin. Potential applications for the battery include studies of central auditory processing, reading problems, hyperactivity, neural bases of voice and speech motor control, neurocardiology, individually-specific responses to medications, and the physiological bases of tinnitus, hyperacusis, and related treatments.

Combination of LC/TOF-MS and LC/Ion Trap MS/MS for the Identification of Diphenhydramine in Sediment Samples

USGS Publications Warehouse

Ferrer, I.; Heine, C.E.; Thurman, E.M.

2004-01-01

Diphenhydramine (Benadryl) is a popular over-the-counter antihistaminic medication used for the treatment of allergies. After consumption, excretion, and subsequent discharge from wastewater treatment plants, it is possible that diphenhydramine will be found in environmental sediments due to its hydrophobicity (log P = 3.27). This work describes a methodology for the first unequivocal determination of diphenhydramine bound to environmental sediments. The drug is removed from the sediments by accelerated solvent extraction and then analyzed by liquid chromatography with a time-of-flight mass spectrometer and an ion trap mass spectrometer. This combination of techniques provided unequivocal identification and confirmation of diphenhydramine in two sediment samples. The accurate mass measurements of the protonated molecules were m/z 256.1703 and 256.1696 compared to the calculated mass of m/z 256.1701, resulting in errors of 0.8 and 2.3 ppm. This mass accuracy was sufficient to verify the elemental composition of diphenhydramine in each sample. Furthermore, accurate mass measurements of the primary fragment ion were obtained. This work is the first application of time-of-flight mass spectrometry for the identification of diphenhydramine and shows the accumulation of an over-the-counter medication in aquatic sediments at five different locations.

Investigational new drugs for allergic rhinitis.

PubMed

Ricketti, Peter A; Alandijani, Sultan; Lin, Chen Hsing; Casale, Thomas B

2017-03-01

Allergic rhinitis (AR) is a multifactorial disease characterized by paroxysmal symptoms of sneezing, rhinorrhea, postnasal drip and nasal congestion. For over a century, subcutaneous allergen immunotherapy (SCIT) has been recognized as the most effective therapy to date that may modify the underlying disease course and provide long-term benefits for individuals refractory to pharmacotherapy. However, over the past 25 years, there has been substantial growth in developing alternative therapies to traditional SCIT. Areas covered: This article will review the most current literature focusing on advancements of AR therapies. Novel AR therapies that are currently under investigation include: the addition of omalizumab, an anti-immunoglobulin E (IgE) monoclonal antibody (mAb), to SCIT; altering the method of delivery of allergen immunotherapy (AIT) including sublingual (SLIT), epicutaneous (EIT), intralymphatic (ILIT), intranasal (INIT) and oral mucosal immunotherapy (OMIT); use of capsaicin spray; novel H3 and H4 antihistamines; activation of the innate immune system through Toll-like receptor agonists; and the use of chemically altered allergens, allergoids, recombinant allergens and relevant T-cell epitope peptides to improve the efficacy and safety of AIT. Expert opinion: These promising novel therapies may offer more effective and/or safer treatment options for AR patients, and in some instances, induce immunologic tolerance.

A large outbreak of scombroid fish poisoning associated with eating yellowfin tuna (Thunnus albacares) at a military mass catering in Dakar, Senegal.

PubMed

Demoncheaux, J-P; Michel, R; Mazenot, C; Duflos, G; Iacini, C; de Laval, F; Delaval, F; Saware, E M; Renard, J-C

2012-06-01

On 26 November 2010, an outbreak of scombroid fish poisoning occurred in the French Armed Forces in Dakar, Senegal. This chemical intoxication, due to high histamine concentration in fish, is often mistaken for an allergic reaction. A case-control study was undertaken including the 71 cases and 78 randomly selected controls among lunch attendees. The usual symptoms for scombroid fish poisoning were observed in cases, i.e. flushing (85.9%), headache (83.1%), rapid/weak pulse (59.1%) and diarrhoea (47.9%). Symptoms occurred from within a few minutes to up to 3 h following the meal. Most patients quickly recovered with antihistamine and/or symptomatic treatment. Tuna was the only food item positively associated with illness (odds ratio 36.3, 95% confidence interval 6.3-210.0), with the risk of illness increasing with the quantity of fish consumed. No bacterial contamination was found in leftover food, but histamine concentration in tuna was found to be 4900 mg/kg, almost 50-fold higher than the concentration allowed by European regulations. This report is unique because of the large size of the case series - to our knowledge, the largest event of scombroid fish poisoning ever reported - and the chemical and bacteriological analyses results obtained on leftover food.

Evaluation and Management of Patch Test-Negative Patients With Generalized Dermatitis.

PubMed

Spiker, Alison; Mowad, Christen M

Patients with generalized dermatitis are common in dermatology practices. Allergic contact dermatitis is often suspected, and patients frequently undergo patch testing. When the patch testing result is negative, further evaluation and management of these patients are challenging. The purpose of this study was to survey members of the American Contact Dermatitis Society regarding the evaluation and management of patch test-negative patients with generalized dermatitis. Generalized dermatitis was the most common term identified for patch test-negative patients with diffuse dermatitis. After having negative expanded patch testing results, most physicians proceeded with additional testing including skin biopsy, complete blood cell count with differential, and liver and renal function tests. The most commonly used systemic treatment is prednisone, followed by methotrexate. Narrow-band ultraviolet B (UVB) is the most commonly used light source. Antihistamines are frequently prescribed. Food allergy is not felt to be causative. This cohort of patients experiences significant impairment in quality of life, stress on personal relationships, and time off work. The management of patch test-negative patients with generalized dermatitis is challenging. This study provides insight into management of these complex patients. It also demonstrates practice gaps in the management of these patients, indicating a need for further studies to direct the evaluation and management of this patient population.

What we can learn about hereditary dystonia from HSDI of the glottis

NASA Astrophysics Data System (ADS)

Pedersen, Mette; Eeg, Martin

2012-02-01

This study examined efficacy of the innate immune defence via the mannose binding lectin (MBL) in a cohort of 55 dystonic patients prospectively referred to the clinic with laryngeal mucosal complaints, who were placed on local steroids (budesonid inhaler, 400 μg 2 times daily) and antihistamines (fexofenadin 180 mg mostly 3 times daily) with adjuvant lifestyle corrections. Treatment efficacy of the larynx was assessed based on mucosal findings of the vocal folds examined with High speed mucosa studies comprising simultaneous high speed digital imagines (HSDI), kymography, electroglottography (EGG) and voice acoustics combined with a visual score of arytenoids oedema, as these measures are indicative of the magnitude of laryngitis. Lactose and gluten intolerance and immunological analyses of the innate system were made systematically. Results showed that the genetic aspects of immunology did not reveal a role for the innate immune system, represented by the mannose binding lectin (MBL). An unexpected positive effect of the larynx treatment on dystonia symptoms was found evidenced by reduction of dystonic complaints and more normative results of High speed mucosa, and a reduction of oedema of the inter arytenoids region. Symptoms relieve and better quality of life was observed on follow up for the dystonia complaints.

[Management of anaphylaxis in Latin America: current situation].

PubMed

Cardona, Victoria; Álvarez-Perea, Alberto; Ansotegui, Ignacio J; Arias-Cruz, Alfredo; González-Díaz, Sandra Nora; Latour-Staffeld, Patricia; Ivancevich, Juan Carlos; Sánchez-Borges, Mario; Serrano, Carlos; Solé, Dirceu; Tanno, Luciana K

2017-01-01

Anaphylaxis is a systemic and severe allergic reaction, which can be fatal. The first-line treatment of choice, according to international guidelines, is intramuscular adrenaline. However, different studies show that the performance of health professionals managing anaphylaxis is often inadequate. To assess the current resources available in Latin American countries for the diagnosis and treatment of anaphylaxis. Online survey promoted by the Latin American Society of Allergy and Immunology to representatives of the national allergy societies of Latin American countries. Responses were received from 10 countries out of the 14 countries invited to participate. Only five of the countries have clinical practice guidelines in anaphylaxis. Adrenaline autoinjectors are available only in two countries, Argentina and Brazil, but are not subsidized by public health systems. In all countries, adrenaline is available in ampoules, which is the presentation usually prescribed to patients for self-administration. The use of adrenaline was estimated to be less than 50 % of cases in five countries, while antihistamines and corticosteroids are almost always used. The determination of serum tryptase is possible in some health centers, often private, in five of the countries surveyed. It is necessary to improve resources related to the diagnosis and management of anaphylaxis in Latin American countries.

A case of loiasis in Rome.

PubMed

Morrone, A; Franco, G; Toma, L; Tchangmena, O B; Marangi, M

2002-05-01

Owing to the increase of an immigrant population and of Italian citizens travelling for tourism or on business, it is nowadays possible to observe clinical pictures characteristic of tropical regions, often with indistinct symptoms. One of these is Loa loa infestation, or loiasis, a form of filariasis caused by Loa loa and transmitted by the Chrysops fly. We present the case of a male immigrant from Cameroon. Characteristic symptoms were intense xerosis, mostly of the third inferior part of the legs, intensely pruritic, with numerous lesions from scratching. No benefit was obtained by emollient topics, anti-acarus and systemic antihistamines. Serum samples and Giemsa, haematoxylin, haematoxylin + Giemsa concentration-on-membrane stains, have evidenced the presence of Loa loa microfilariae. A diagnosis for L. loa (loiasis) infestation was made. At the beginning of the migration phenomenon, particularly from Africa, Italian physicians, especially dermatologists, were eagerly looking for 'tropical' diseases; this approach can be defined as 'Salgari's syndrome' from the name of the Italian novelist who, though never travelling out of Italy, had perfectly described environments and habits typical of far away countries. Now, conversely, we have to avoid the opposite approach of considering real tropical diseases as related to social or psychological difficult conditions.

Poisoning, envenomation, and trauma from marine creatures.

PubMed

Perkins, R Allen; Morgan, Shannon S

2004-02-15

In the course of their clinical work or during leisure activity, family physicians occasionally may encounter patients with injuries from marine creatures. Poisoning, envenomation, and direct trauma are all possible in the marine environment. Ciguatera poisoning can result from ingestion of predatory fish that have accumulated biotoxins. Symptoms can be gastrointestinal or neurologic, or mixed. Management is mostly symptomatic. Scombroid poisoning results from ingestion of fish in which histamine-like substances have developed because of improper refrigeration. Gastrointestinal and systemic symptoms occur. Treatment is based on antihistamines. Envenomations from jellyfish in U.S. waters and the Caribbean are painful but rarely deadly. Household vinegar deactivates the nematocysts, and manual removal of tentacles is important. Treatment is symptomatic. Heat immersion may help with the pain. Stingrays cause localized damage and a typically severe envenomation. The venom is deactivated by heat. The stingray spine, including the venom gland, typically is difficult to remove from the victim, and radiographs may be necessary to localize the spine or fragment. Surgical débridement occasionally is needed. Direct trauma can result from contact with marine creatures. Hemorrhage and tissue damage occasionally are severe. Infections with organisms unique to the marine environment are possible; antibiotic choices are based on location and type of injury. Shark attacks, although rare, require immediate attention.

Removal of diphenhydramine from water by swelling clay minerals.

PubMed

Li, Zhaohui; Chang, Po-Hsiang; Jiang, Wei-Teh; Jean, Jiin-Shuh; Hong, Hanlie; Liao, Libing

2011-08-01

Frequent detection of pharmaceuticals in surface water and wastewater attracted renewed attention on studying interactions between pharmaceuticals and sludge or biosolids generated from wastewater treatment. Less attention was focused on studying interactions between pharmaceuticals and clay minerals, important soil and sediment components. This research targeted on investigating interactions between diphenhydramine (DPH), an important antihistamine drug, and a montmorillonite, a swelling clay, in aqueous solution. Stoichiometric desorption of exchangeable cations accompanying DPH adsorption confirmed that cation exchange was the most important mechanism of DPH uptake by the swelling clay. When the solution pH was below the pK(a) of DPH, its adsorption on the swelling clay was less affected by pH. Increasing solution pH above the pK(a) value resulted in a decrease in DPH adsorption by the clay. An increase in d(001) spacing at a high DPH loading level suggested interlayer adsorption, thus, intercalation of DPH. The results from this study showed that swelling clays are a good environmental sink for weak acidic drugs like DPH. In addition, the large cation exchange capacity and surface area make the clay a good candidate to remove cationic pharmaceuticals from the effluent of wastewater treatment facilities. Copyright © 2011 Elsevier Inc. All rights reserved.

Immediate and delayed allergic reactions to Crotalidae polyvalent immune Fab (ovine) antivenom.

PubMed

Clark, Richard F; McKinney, Patrick E; Chase, Peter B; Walter, Frank G

2002-06-01

Allergic reactions are the most commonly reported adverse events after administration of antivenoms. Conventional horse serum-based crotalid antivenom used in the United States (Antivenin [Crotalidae] polyvalent) can lead to both immediate and delayed hypersensitivity reactions. Crotalidae polyvalent immune Fab (ovine) (CroFab; FabAV) has recently been approved for use in the United States. Experience from premarketing trials of this product and in the administration of other types of Fab, such as in digoxin poisoning, has demonstrated these fragments to be safe and effective, with a low incidence of sequella; however, allergic reactions can occur when any animal-protein derivatives are administered to human subjects. We report in detail the nature and course of allergic reactions that occurred in 4 patients treated with FabAV. Cases of anaphylaxis, acute urticaria, angioedema, and delayed serum sickness are described. All reactions were easily treated with some combination of antihistamines, epinephrine, and steroids, with prompt resolution of signs and symptoms enabling further dosing of antivenom as required. Several of these cases may have resulted from batches of antivenom contaminated with Fc fragments. The overall incidence of immediate and delayed allergic reactions to this product appears so far to be lower than that reported with conventional whole-immunoglobulin G (IgG) antivenom, but postmarketing surveillance is warranted.

Facial follicular cysts: a case of lichen planus follicularis tumidus?

PubMed

Jiménez-Gallo, David; Albarrán-Planelles, Cristina; Linares-Barrios, Mario; Martínez-Rodríguez, Alberto; Báez-Perea, José María; González-Fernández, Julio Abraham

2013-09-01

Lichen planus follicularis tumidus (LPFT) represents an uncommon variety of lichen planus (LP). Clinically, it presents with prominent purplish lesions or white-pigmented yellowish cysts and comedones. Histopathologically, it is similar to lichen planopilaris, and it is additionally characterized by follicles and cysts surrounded by a lichenoid lymphocytic infiltrate. The most common location is the retroauricular region, and it may be associated with other variants of LP. Herein, we describe the case of a 50-year-old woman with a history of lower limb hypertrophic LP who subsequently presented with multiple pink, tumid, pruritic plaques with white-yellow cysts and comedones extensively affecting the bilateral face. Histopathologic examination revealed a lichenoid infiltrate surrounding the follicles and cysts. We diagnosed LPFT and began treatment with topical corticosteroids, antihistamines, systemic corticosteroids and oral acitretin without improvement. Subsequently, the patient had an acceptable response to cyclosporine at doses of 5 mg/kg/day with remission of itching and tumidity but with residual cysts and comedones remaining. To date, the literature contains only 16 cases of LPFT. To our knowledge, this is the most severe case and is the only one with cessation of disease activity in response to cyclosporine. © 2013 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

[Drug-facilitated crimes: prospective data collection in a forensic unit in Paris].

PubMed

Questel, Franck; Sec, Isabelle; Sicot, Romain; Pourriat, Jean-Louis

2009-01-01

Little is known about the rate of crimes that are facilitated by the administration of psychoactive products without the victim's knowledge. This study analyzes the cases collected over a two-year period in a forensic unit in Paris. The study covers the period from January 1, 2005 and December /31, 2006. It includes crime victims who consulted for toxicological testing in the forensic unit of the Hôtel Dieu in Paris, after filing a criminal complaint describing symptoms suggestive of chemical submission (amnesia, impaired vigilance or behavior) and whose toxicological tests indicated the presence of a psychoactive product that they had not been aware of taking. The tests used chromatographic techniques on blood, urine, hair, and food or drink residue. Toxicological testing identified 52 cases of drug-facilitated crimes, primarily for theft and sexual abuse (including rape). The psychoactive products were most often incorporated in drinks, half of them alcoholic beverages. Benzodiazepines accounted for 77% of the cases. Other substances, found more rarely, included antihistamines, neuroleptics, and GHB. Appropriate samples must be taken from victims rapidly to enable toxicological analysis. Chromatographic analysis must supplement immunological analysis, which is not sufficiently specific or sensitive. The collection of this information must continue in order to quantify the phenomenon and monitor the emergence of new products.

Long-term bradycardia caused by atrioventricular block can remodel the canine heart to detect the histamine H1 blocker terfenadine-induced torsades de pointes arrhythmias.

PubMed

Takahara, Akira; Sugiyama, Atsushi; Ishida, Yuko; Satoh, Yoshioki; Wang, Kai; Nakamura, Yuji; Hashimoto, Keitaro

2006-03-01

Although a second-generation histamine H(1) blocker terfenadine induced torsades de pointes (TdP) arrhythmias in patients via the blockade of a rapid component of delayed rectifier K(+) current (I(Kr)), such action of terfenadine has not been detected in previous animal models. We analysed the potential of the canine persistent atrioventricular block heart, a new in vivo proarrhythmia model, to detect a torsadogenic effect of terfenadine of an oral dose of 3 or 30 mg kg(-1). The doses can provide therapeutic to supra-therapeutic plasma concentrations as an anti-histamine. In 2 weeks of bradycardiac heart model, there were no significant changes in any of the electrocardiogram parameters after the administration of both doses of terfenadine. In 4-6 weeks of bradycardiac heart model, the low dose of terfenadine hardly affected any of the electrocardiogram parameters except that it induced TdP in one out of six animals. The high dose significantly decreased the atrial rate and ventricular rate, prolonged the QT interval, and induced TdP in five out of six animals. Moreover, temporal variability of repolarization increased after the high-dose administration. These results suggest that long-term bradycardia caused by atrioventricular block can remodel the canine heart to detect terfenadine-induced TdP.

Rapid drug desensitization for hypersensitivity reactions to chemotherapy and monoclonal antibodies in the 21st century.

PubMed

Castells Guitart, M C

2014-01-01

The frequency of hypersensitivity reactions (HSR) to drugs has risen in the last 10 years owing to increased exposure to better and more allergenic medications including monoclonal antibodies. HSRs prevent patients from using their first-line therapy, leading to decreased quality of life and life expectancy. Although premedication with antihistamines, leukotriene blockers, and corticosteroids can protect against mild-to-moderate HSR, none of these medications has provided protection against anaphylaxis. Rapid drug desensitization is a treatment option for patients with HSR to their first-line medication that protects against anaphylaxis.Although the mechanisms of drug desensitization are not completely understood, in vitro mast cell models of IgE antigen desensitization have led to the design of safe and effective in vivo protocols aimed at protecting highly sensitized patients from hypersensitivity reactions and anaphylaxis. This review provides an insight into the mechanisms of IgE/mast cell desensitization, the principles and practice of drug desensitization, and an overview of the different desensitization protocols and their safety and efficacy profiles. Drug desensitization should only be performed by allergists, trained nurses, and experienced pharmacists, since this high-risk procedure involves reintroducing allergenic medication to highly sensitized patients, with the consequent potential for severe or fatal HSRs.

Repurposing a Histamine Detection Platform for High-Throughput Screening of Histidine Decarboxylase.

PubMed

Juang, Yu-Chi; Fradera, Xavier; Han, Yongxin; Partridge, Anthony William

2018-06-01

Histidine decarboxylase (HDC) is the primary enzyme that catalyzes the conversion of histidine to histamine. HDC contributes to many physiological responses as histamine plays important roles in allergic reaction, neurological response, gastric acid secretion, and cell proliferation and differentiation. Small-molecule modulation of HDC represents a potential therapeutic strategy for a range of histamine-associated diseases, including inflammatory disease, neurological disorders, gastric ulcers, and select cancers. High-throughput screening (HTS) methods for measuring HDC activity are currently limited. Here, we report the development of a time-resolved fluorescence resonance energy transfer (TR-FRET) assay for monitoring HDC activity. The assay is based on competition between HDC-generated histamine and fluorophore-labeled histamine for binding to a Europium cryptate (EuK)-labeled anti-histamine antibody. We demonstrated that the assay is highly sensitive and simple to develop. Assay validation experiments were performed using low-volume 384-well plates and resulted in good statistical parameters. A pilot HTS screen gave a Z' score > 0.5 and a hit rate of 1.1%, and led to the identification of a validated hit series. Overall, the presented assay should facilitate the discovery of therapeutic HDC inhibitors by acting as a novel tool suitable for large-scale HTS and subsequent interrogation of compound structure-activity relationships.

In Vivo and In Vitro Toxicity Evaluation of Hydroethanolic Extract of Kalanchoe brasiliensis (Crassulaceae) Leaves

PubMed Central

Lima, Adley Antoninni Neves; Soares, Luiz Alberto Lira

2018-01-01

The species Kalanchoe brasiliensis, known as “Saião,” has anti-inflammatory, antimicrobial, and antihistamine activities. It also has the quercetin and kaempferol flavonoids, which exert their therapeutic activities. With extensive popular use besides the defined therapeutical properties, the study of possible side effects is indispensable. The objective of this study is to evaluate the toxicity in vitro and in vivo from the hydroethanolic extract of the leaves of K. brasiliensis. The action of the extract (concentrations from 0.1 to 1000 uL/100 uL) in normal and tumor cells was evaluated using the MTT method. Acute toxicity and subchronic toxicity were evaluated in mice with doses of 250 to 1000 mg/kg orally, following recognized protocols. The in vitro results indicated cytotoxic activity for 3T3 cell line (normal) and 786-0 (kidney carcinoma), showing the activity to be concentration-dependent, reaching 92.23% cell inhibition. In vivo, the extract showed no significant toxicity; only liver changes related to acute toxicity and some signs of liver damage, combining biochemical and histological data. In general, the extract showed low or no toxicity, introducing itself as safe for use with promising therapeutic potential. PMID:29593788

Mastocytosis complicating pregnancy.

PubMed

Worobec, A S; Akin, C; Scott, L M; Metcalfe, D D

2000-03-01

To review the experience of women who conceived after developing mastocytosis and who were observed at the National Institutes of Health. We reviewed our patient database for the years 1984-1998 to identify women with mastocytosis who had conceived. We then reviewed each woman's record, asked each woman to complete a questionnaire, and with permission wrote outside hospitals to obtain records of each labor and delivery. We identified eight women who had become pregnant. These women delivered a total of 11 live infants. In approximately a third of the pregnancies, patients experienced worsening of symptoms. They often used fewer medications during pregnancy because of safety concerns, and no greater incidence of adverse reactions was noted. Antihistamines were used most commonly, followed by oral prednisone. Medications used during delivery were well tolerated and included epidural analgesics. Neonates were generally healthy. None to date have developed urticaria pigmentosa or systemic mastocytosis. A subset of women with mastocytosis might have had exacerbated mastocytosis during and after pregnancy, but labor and delivery progressed normally. Infants were born generally healthy and were without mastocytosis. Thus there appears to be no absolute contraindication to pregnancy for women with mastocytosis, although women should be aware that the choice to have a child is not without some added risk.

THE CASE OF A 14-YEAR-OLD BOY WHO EXPERIENCED ANAPHYLAXIS DUE TO JELLYFISH (MASTIGIAS PAPUA) INGESTION.

PubMed

Kubota, Shohei; Nozawa, Asako; Yanai, Takanori; Ozasa, Koji; Mori, Satomi; Kurihara, Kazuyuki

2017-01-01

We report a case of jellyfish allergy diagnosed via an oral food challenge. A 14-year-old boy had no history of jellyfish stings and had been eating commercially available jellyfish products twice yearly for the past 5-6 years. Five minutes after eating a commercially available boiled jellyfish product (100g), he experienced nausea, wheezing, and erythema and had visited our hospital. We suspected an anaphylactic reaction and treated him with intramuscular adrenaline injection, corticosteroid and antihistamine infusions, volume resuscitation, and salbutamol sulfate inhalation, which resulted in an improvement of the symptoms. One-month later in our hospital, we administered an oral food challenge of the same boiled jellyfish product bought at the same grocery store to the patient. After ingesting 14g of boiled jellyfish, he experienced erythema, wheezing, nausea, and abdominal pain. Several reports have described anaphylaxis caused by the ingestion of jellyfish, but the allergens in jellyfish have not been analyzed. A skin prick test for poly-gamma-glutamic acid (PGA) which is a component of jellyfish stings was negative. This suggests that he was sensitized to some allergen other than PGA via a route different from that of jellyfish sting. Our skin prick test for several kinds of edible jellyfish suggests that allergenicity may be different for different jellyfish.