Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new cetirizine research articles will be listed here shortly after becoming available to us.
Related Sponsors
Medical research on cetirizine
Methods Find Exp Clin Pharmacol. 2008 Apr; 30(3): 225-30
Izumi N, Mizuguchi H, Umehara H, Ogino S, Fukui H
Sedation is the most frequent side effect of H(1)-antihistamines, and, sometimes, it may be life-threatening for patients. Evaluation of the sedative properties of H(1)-antihistamines is important to improve the patients' quality of life (QOL). Therefore, we carried out a large-scale surveillance quantified through a questionnaire using visual analog scale (VAS) from 1,742 patients. The results showed that the degree of sleepiness caused by some nonsedative second-generation antihistamines, including fexofenadine, olopatadine and cetirizine, was disease dependent. In atopic dermatitis, an unexpectedly low VAS score of sleepiness was obtained for the first-generation antihistamine d-chlorpheniramine, which is similar to those obtained for bepotastine and epinastine. d-Chlorpheniramine also showed a high VAS score in efficacy. Meanwhile, fexofenadine showed a higher VAS score of sleepiness in atopic dermatitis than those obtained in the other allergic diseases including allergic rhinitis, urticaria and asthma. In asthma, a higher VAS score of sleepiness was found for olopatadine, ebastine and cetirizine, when compared with d-chlorpheniramine. On the other hand, bepotastine showed the lowest VAS score for sleepiness. Our findings suggest the existence of unknown factors influencing the sedative properties of H(1)-antihistamines. Therefore, appropriate H(1)-antihistamines may need to be selected, depending on allergic diseases, to improve patients' QOL.
Allergy. 2008 Jul; 63(7): 924-31
Fantin S, Maspero J, Bisbal C, Agache I, Donado E, Borja J, Mola O, Izquierdo I,
BACKGROUND: With the current increasing incidence of allergies worldwide, new treatments showing efficacy and long term safety are needed for chronic conditions such as persistent allergic rhinitis (PER). New generation H1-antihistamines have demonstrated anti-allergic properties, which could possibly enhance their effectiveness in long-term periods of treatment. OBJECTIVE: To investigate the efficacy of rupatadine, in controlling symptoms of PER over a 12-week period. METHODS: A randomized, double blind, parallel-group, placebo-controlled study was carried out in patients aged older than 12 years with PER. Main inclusion criteria were: instantaneous total symptom score (i6TSS) >or=45, nasal obstruction score or=2 as moderate during the first visit. The primary efficacy endpoint was the 12-week average change from baseline of the patients' i6TSS. RESULTS: In all, 736 patients were selected. Of them, 543 (73.8%) were randomized in three different groups: placebo (n = 185), cetirizine (n = 175) and rupatadine (n = 183). Rupatadine (P = 0.008) but not cetirizine (P = 0.07) statistically reduced the baseline i6TSS vs placebo (47.8%, 44.7% and 38.8%, respectively), after 12 weeks. Onset of action was observed at the first 24 h for both treatments (rupatadine vs placebo, P = 0.013; cetirizine vs placebo, P = 0.015). Furthermore, instantaneous total nasal symptoms score (iTNSS) (including nasal blockage) mean change from baseline showed a significant reduction with rupatadine 10 mg in comparison with placebo, along all treatment duration of 12 weeks. Study treatments were well tolerated. CONCLUSION: Rupatadine significantly relieves symptoms of PER, providing a rapid onset of action and maintains its effects over a long period of 12-weeks.
The safety of cetirizine during pregnancy A prospective observational cohort study.
Reprod Toxicol. 2008 May 13;
Weber-Schoendorfer C, Schaefer C
OBJECTIVE: To assess the safety of cetirizine during pregnancy. STUDY DESIGN: A prospective observational cohort study with data of the Berlin teratology information center from 1992 until 2006. Pregnancy outcome was compared between a cohort of pregnant women exposed to cetirizine during the first trimester (n=196) and a control group not exposed to potential teratogens (n=1686). RESULTS: Major birth defects were not more common in the study group than in the control group (OR 1.07; CI 0.21-3.59). We also compared the crude rate of spontaneous abortions (OR 0.97; CI 0.54-1.65), of preterm deliveries (OR 0.76; CI 0.35-1.5), and the birth weight of term newborns (p=0.13). CONCLUSIONS: This prospective observational study on cetirizine in pregnancy suggests that the use of cetirizine is relatively safe during the first trimester.
[Does new antihistamines characterize tachyphylaxis phenomenon?]
Otolaryngol Pol. 2007; 61(5): 898-901
Kłos K, Kruszewski J
THE AIM OF THE STUDY: was to estimate the skin microcirculation reactivity after histamine administration in patients treated with 10 mg daily dose of cetirizine for 180 days. MATERIAL AND METHODS: Thirty seven young men age 27+12 year, patients suffering from persistent rhinitis were randomized into three groups which received 10 mg/day of cetirizine, 5 mg/day of levocetirizine or placebo respectively. Twenty eight completed the study. The skin microcirculation reaction after 10 mg/ml histamine administration was estimated visually on the forearm (diameter of wheal and flare) and by laser Doppler flowmetry before and after study drug or placebo administration 24 hours and every 30 days during the time of the study. The blood flow was measured by Periflux PF3, using a skin probe 5 mm away from the histamine-induced point. RESULTS: Statistically significant inhibition of skin reaction (over 92%) and blood flow (over 85%) in relation to the start values in cetirizine group as well as between the groups which received cetirizine or placebo (p
Int Immunopharmacol. 2008 Aug; 8(8): 1083-8
Yokota E, Kuyama S, Ogawa M, Kamei C
The aim of this study was to clarify the mechanisms of the inhibitory effect of a histamine H(3) receptor agonist, Sch 50971, on nasal signs in an allergic rhinitis model in mice. The severity of allergic rhinitis was assessed by determining the extent of two markers of allergic symptoms (sneezing and nasal rubbing). The topical application of a histamine H(3) receptor antagonist, clobenpropit, into the nasal cavities resulted in a dose-dependent increase in sneezing and nasal rubbing, and both Sch 50971 and a tachykinin NK(1) receptor antagonist, L-733,060, inhibited these reactions in non-sensitized mice. Sch 50971 caused no inhibition of histamine- and substance P-induced nasal symptoms; however, the reactions induced by capsaicin were significantly decreased by Sch 50971 in non-sensitized mice. Sch 50971 and cetirizine inhibited antigen-induced sneezing and nasal rubbing in sensitized mice. On the other hand, cetirizine inhibited nasal symptoms induced by antigen in capsaicin-pretreated mice, whereas no effect was observed in Sch 50971. From these results, we concluded that Sch 50971 blocked nasal symptoms by the inhibition of substance P release via histamine H(3) receptors located on peri]pheral sensory nerve endings.
Comparative bioavailability of two cetirizine tablet formulations in Indonesian healthy volunteers.
Int J Clin Pharmacol Ther. 2008 May; 46(5): 268-72
Harahap Y, Prasaja B, Indriati E, Lusthom W, Lipin
AIM: To compare the bioavailability of two cetirizine tablet (10 mg) formulations (ZyrtecA from UCB Pharma, Spain as a reference formulation and RyvelA from Novell Pharmaceutical Laboratories, Indonesia as a test formulation). MATERIAL AND METHODS: The study was conducted according to an open, randomized, two-period crossover design with a 1-week washout period. Eighteen volunteers participated and all completed the study successfully. Blood samples were obtained prior to dosing and at 0.25, 0.5, 1, 2, 3, 5, 8, 12, 24 and 30 hours after drug administration. Plasma concentrations of cetirizine were monitored using high-performance liquid chromatography over a period of 30 hours after administration. The pharmacokinetics parameter AUC(0-30h), AUC(0-infinity) and C(max) were tested for bioequivalence after log-transformation of data and ratios of t(max) were evaluated non-parametrically. RESULT: The point estimates and 90% confidence intervals for AUC(0-30h), AUC(0-infinity) and C(max) were 108.23% (101.90 â 114.95%), 108.11% (101.91 â 114.68%) and 99.71% (90.18 â 110.25%), respectively, satisfying the bioequivalence criteria of the European Committee for Proprietary Medicinal Products an the US Food and Drug Administration guidelines. CONCLUSION: These results indicate that two medications of cetirizine are bioequivalent and, thus, may be prescribed interchangeably.
Int Immunopharmacol. 2008 Jul; 8(7): 1049-55
Youssouf MS, Kaiser P, Singh GD, Singh S, Bani S, Gupta VK, Satti NK, Suri KA, Johri RK
An immunopharmacological profile of 2, 7-dimethyl-3-nitro-4H pyrido [1,2-a] pyrimidine-4-one (P-I) has been investigated using in vitro and in vivo models representing various features of Type I allergy. P-I prevented compound 48/80-mediated histamine release from rat peritoneal mast cells. A promising anti-inflammatory activity of P-I was evident in active paw anaphylaxis (mice) and carragenan-induced paw edema (rat). P-I inhibited eosonophil accumulation and eosinophil peroxidase activity in bronchoalveolar lavage fluid from ovalbumin challenged balb/c mice: in these animals blood levels of IL-5, and CD4+ T cells also remained attenuated. A promising bronchorelaxant effect of P-I was observed in histamine-contracted guinea pig tracheal chain via its antagonism to H1 receptor. These findings were compared with some known compounds (ketotifen, cetirizine and promethazine). The anti-histaminic, anti-inflammatory and bronchorelaxant activities of P-I has been discussed in context with its potential profile as an anti-allergic and anti-asthmatic agent.
Pharmacokinetics of cetirizine in healthy cats.
Am J Vet Res. 2008 May; 69(5): 670-4
Papich MG, Schooley EK, Reinero CR
OBJECTIVE: To develop a high-performance liquid chromatography (HPLC) assay for cetirizine in feline plasma and determine the pharmacokinetics of cetirizine in healthy cats after oral administration of a single dose (5 mg) of cetirizine dihydrochloride. ANIMALS: 9 healthy cats. PROCEDURES: Heparinized blood samples were collected prior to and 0.5, 1, 2, 4, 6, 8, 10, and 24 hours after oral administration of 5 mg of cetirizine dihydrochloride to each cat (dosage range, 0.6 to 1.4 mg/kg). Plasma was harvested and analyzed by reverse-phase HPLC. Plasma concentrations of cetirizine were analyzed with a compartmental pharmacokinetic model. Protein binding was measured by ultrafiltration with a microcentrifugation system. RESULTS: No adverse effects were detected after drug administration in the cats. Mean +/- SD terminal half-life was 10.06 +/- 4.05 hours, and mean peak plasma concentration was 3.30 +/- 1.55 microg/mL. Mean volume of distribution and clearance (per fraction absorbed) were 0.24 +/- 0.09 L/kg and 0.30 +/- 0.09 mL/kg/min, respectively. Mean plasma concentrations were approximately 2.0 microg/mL or higher for 10 hours and were maintained at > 0.72 microg/mL for 24 hours. Protein binding was approximately 88%. CONCLUSIONS AND CLINICAL RELEVANCE: A single dose of cetirizine dihydrochloride (approx 1 mg/kg, which corresponded to approximately 0.87 mg of cetirizine base/kg) was administered orally to cats. It was tolerated well and maintained plasma concentrations higher than those considered effective in humans for 24 hours after dosing. The half-life of cetirizine in cats is compatible with once-daily dosing, and the extent of protein binding is high.
Anti-histamines for prolonged non-specific cough in children.
Cochrane Database Syst Rev. 2008; CD005604
Chang AB, Peake J, McElrea MS
BACKGROUND: Non-specific cough is defined as non-productive cough in the absence of identifiable respiratory disease or known aetiology. It is commonly seen in paediatric practice. These children are treated with a variety of therapies including anti-histamines. Also, anti-histamines are advocated as an empirical treatment in adults with chronic cough. OBJECTIVES: To evaluate the effectiveness of anti-histamines in treating children with prolonged non-specific cough. SEARCH STRATEGY: We searched the Cochrane Register of Controlled Trials (CENTRAL), MEDLINE, OLDMEDLINE and EMBASE databases. The latest searches were performed in November 2007. SELECTION CRITERIA: All randomised controlled trials comparing anti-histamines with a placebo or placebo-like medication with cough as an outcome, where cough is not primarily related to an underlying respiratory disorder such as cystic fibrosis, asthma, or suppurative lung disease. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed study quality and extracted data. MAIN RESULTS: Three included therapeutic studies had 182 randomised participants with 162 completing the trials although in one study, children with recurrent wheeze were also included. The two included safety evaluation studies randomised 963 participants with 793 completing the trials. Clinical heterogeneity was evident and limited data prevented combining data for meta-analysis. The two larger therapeutic studies described significant improvement in both the intervention and the placebo/placebo-like arms with no significant difference between the two groups. In the study with the smallest sample size, cetirizine (a second generation anti-histamine) was significantly more efficacious than placebo in reducing chronic cough in children associated with seasonal allergic rhinitis, and the effect was seen within two weeks of therapy. Combined data from the safety evaluation studies revealed a non-significant difference between groups (OR 1.6, 95% CI 0.7 to 3.82) for cough as an adverse event but the trend favoured the placebo arm. AUTHORS' CONCLUSIONS: This review has significant limitations. However, our finding of uncertain efficacy of anti-histamines for chronic cough are similar to that for acute cough in children. In contrast to recommendations in adults with chronic cough, anti-histamines cannot be recommended as empirical therapy for children with chronic cough. If anti-histamines were to be trialled in these children, current data suggest a clinical response (time to response) occurs within two weeks of therapy. However the use of anti-histamines in children with non-specific cough has to be balanced against the well known risk of adverse events especially in very young children.
Zhongguo Zhen Jiu. 2008 Feb; 28(2): 114-6
Yang SR, Chen H, Xie Q
OBJECTIVE: To compare therapeutic effects of moxibustion at "heat sensitive points" and western medicine on perennial allergic rhinitis. METHODS: One hundred and twenty cases were randomly divided into a moxibustion group and a western medicine group, 60 cases in each group. The moxibustion group were treated with moxibustion at "heat sensitive points" on the head-face, abdomen, waist and back, once a day; and the western medicine group with oral administration of Cetirizine Hydrochloride, 10 mg each session, once daily, 10 days constituting one course. RESULTS: The total effective rate and the total effective rate for the cases of over effectiveness 3 months later were 85.0% and 86.3% in the moxibustion group and 63.3% and 50.0% in the western medicine group, respec tively, with significant or very significant difference (P < 0.05, P < 0.01). CONCLUSION: Moxibustion at "heat sensitive points" is an ideal therapy for perennial allergic rhinitis with low recurrence rate.