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Fexofenadine Hydrochloride (fexofenadine + hydrochloride)

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Medical Sciences	100%

Selected Abstracts

Fexofenadine hydrochloride enhances the efficacy of contact immunotherapy for extensive alopecia areata: Retrospective analysis of 121 cases

THE JOURNAL OF DERMATOLOGY, Issue 6 2009
Shigeki INUI
ABSTRACT To study the effect of fexofenadine on extensive alopecia areata (AA), we evaluated retrospectively 121 patients with AA having alopecia in more than 50% of the scalp and followed them for at least 6 months. Patients were treated by immunotherapy using diphenylcyclopropenone or squaric acid dibutylester with or without oral fexofenadine. The regrowth score was estimated as decrease of Severity of Alopecia Tool (SALT) score. In AA with atopic background (atopic AA), the mean regrowth score of the fexofenadine group was 1.333 (n = 33) and that of the control 0.471 (n = 34). The fexofenadine group showed significantly better regrowth than control by Mann,Whitney's U -test (P = 0.00213). In non-atopic AA, the mean regrowth score of the fexofenadine group was 1.303 (n = 33) and that of the control 1.048 (n = 21). There was no significant difference by Mann,Whitney's U -test (P = 0.872). Together, fexofenadine is a helpful reagent in the treatment extensive atopic AA with contact immunotherapy. [source]

The utility of mixed-effects covariate analysis in rapid selection of doses in pediatric subjects: A case study with fexofenadine hydrochloride

BIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 9 2004
Rajesh Krishna
Abstract Fexofenadine hydrochloride is a non-sedating antihistamine that is used in the treatment of symptoms associated with seasonal allergic rhinitis and chronic idiopathic urticaria. A pooled analysis of pharmacokinetic data from children 6 months to 12 years of age and adults was conducted to identify the dose(s) in children that produce exposures comparable to those in adults for the treatment of seasonal allergic rhinitis. The pharmacokinetic parameter database included peak and overall exposure data from 269 treatment exposures from 136 adult subjects, and 90 treatment exposures from 77 pediatric allergic rhinitis patients. The data were pooled and analysed using NONMEM software, version 5.0. A covariate model based on body weight and age and a power function model based on body weight were identified as appropriate models to describe the variability in fexofenadine oral clearance and peak concentration, respectively. Individual oral clearance estimates were on average 44%, 36% and 61% lower in children 6 to 12 years (n = 14), 2 to 5 years (n = 21), and 6 months to 2 years (n = 42), respectively, compared with adults. Trial simulations (n = 100) were carried out based on the final pharmacostatistical models and parameter estimates to identify the appropriate dose(s) in children relative to the marketed dose of 60 mg fexofenadine hydrochloride in adults. The trials were designed as crossover studies in 18 subjects comprising various potential dosing regimens with and without weight stratification. Pharmacokinetic parameter variability was assumed to have a log-normal distribution. Individual weights and ages were simulated using mean (SD) estimates derived from the studies used in this analysis and proportional measurement/model mis-specification errors derived from the analysis were incorporated into the simulation. The results indicated that a 30 mg dose of fexofenadine hydrochloride administered to children 1 to 12 years of age and weighing >10.5 kg and a 15 mg dose administered to children 6 months and older and weighing ,10.5 kg produces exposures similar to those seen with the 60 mg dose in adults. Copyright © 2004 John Wiley & Sons, Ltd. [source]

Suppressive activity of fexofenadine hydrochloride on metalloproteinase production from nasal fibroblasts in vitro

CLINICAL & EXPERIMENTAL ALLERGY, Issue 12 2004
K. Asano
Summary Background Allergic rhinitis (AR) is an inflammatory disease characterized by nasal wall remodelling with intense infiltration of eosinophils and mast cells/basophils. Matrix metalloproteinases (MMPs), MMP-2 and MMP-9, are the major proteolytic enzymes that induce airway remodelling. These enzymes are also important in the migration of inflammatory cells through basement membrane components. Objective We evaluated whether fexofenadine hydrochloride (FEX), the carboxylic acid metabolite of terfenadine with selective H1 -receptor antagonist activity, could inhibit MMP production from nasal fibroblasts (NFs) in response to TNF-, stimulation in vitro. Methods NFs were established from nasal polyp-derived fibroblasts (PFs) taken from patients with AR. Nasal mucosal fibroblasts (MFs) were also induced from nasal mucosal tissues from septal deformity patients without allergy. PF and MF (2 × 105 cells/mL, each) were stimulated with TNF-, in the presence of various concentrations of FEX. After 24 h, culture supernatants were obtained and assayed for MMP-2, MMP-9, tissue inhibitor of metalloproteinase (TIMP)-1 and TIMP-2 levels by ELISA. The influence of FEX on mRNA expression of MMPs and TIMPs in 4 h-cultured cells was also evaluated by real-time RT-PCR. Furthermore, nuclear factor-,B (NF-,B) activation in fibroblasts treated with FEX for 4 h was examined by ELISA. Results FEX at more than 350 ng/mL inhibited the production of MMP-2 and MMP-9 from both PF and MF in response to TNF-, stimulation, whereas TIMP-1 and TIMP-2 production was scarcely affected by FEX. FEX also inhibited MMP mRNA expression and NF-,B activation in PF and MF after TNF-, stimulation. Conclusion The present data suggest that the attenuating effect of FEX on MMP-2 and -9 production from NFs induced by inflammatory stimulation may underlie the therapeutic mode of action of the agent on allergic diseases, including AR. [source]