ebastine ebastine ebastine is a h1 antihistamine with low potential for causing drowsiness. ebastineclinical dataahfs/drugs.cominternational drug namesroutes ofadministrationoralatc coder06ax22 (who) pharmacokinetic dataprotein bindinggreater than 95%metabolismhepatic (cyp3a4-mediated), to carebastineelimination half-life15 to 19 hours (carebastine)identifiers iupac name 4-(4-benzhydryloxy-1-piperidyl)-1-(4-tert-butylphenyl)butan-1-one cas number90729-43-4 ypubchem cid3191chemspider3079 yuniitqd7q784p1chemblchembl305660 ycomptox dashboard (epa)dtxsid6046472 echa infocard100.106.831 chemical and physical dataformulac32h39no2molar mass469.669 g·mol−13d model (jsmol)interactive image smiles o=c(c1ccc(cc1)c(c)(c)c)cccn4ccc(oc(c2ccccc2)c3ccccc3)cc4 inchi inchi=1s/c32h39no2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31h,10,15,20-24h2,1-3h3 ykey:mjjalkddgikvbe-uhfffaoysa-n y (verify) it does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the h1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness. it was patented in 1983 by almirall s.a and came into medical use in 1990. the substance is often provided in micronised form due to poor water solubility. uses ebastine is a second-generation h1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria. it is available in 10 and 20 mg tablets and as fast-dissolving tablets, as well as in pediatric syrup. it has a recommended flexible daily dose of 10 or 20 mg, depending on disease severity. data from over 8,000 patients in more than 40 clinical trials and studies suggest efficacy of ebastine in the treatment of intermittent allergic rhinitis, persistent allergic rhinitis and other indications. safety ebastine has shown overall safety and tolerability profile with no cognitive/psychomotor impairment and no sedation worse than placebo, and cardiac safety, that is, no qt prolongation. the incidence of most commonly reported adverse events was comparable between the ebastine and placebo groups, which confirms that ebastine has a favourable safety profile. while experiments in pregnant animals showed no risk for the unborn, no such data are available in humans. it is not known whether ebastine passes into the breast milk. pharmacokinetic profile after oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome p450 3a4 into its active carboxylic acid metabolite, carebastine. this conversion is practically complete. carebastine, the active metabolite brand names ebastine is available in different formulations (tablets, fast dissolving tablets and syrup) and commercialized under different brand names around the world, ebast, ebatin, ebatin fast, ebatrol, atmos, ebet, ebastel flas, kestine, kestinelio, kestinlyo, estivanlyo, evastel z,tebast (square), ebasten (aci), etc.