title: The inhibition by levocetirizine and fexofenadine of the histamine-induced wheal and flare response in healthy Caucasian and Japanese volunteers.
abstract: This randomized, double-blind, placebo-controlled crossover study compared inhibition by one 5 mg dose of levocetirizine with two 60 mg doses of fexofenadine separated by 12 h of histamine-induced wheal and flare responses in 9 Caucasian and 9 Japanese healthy male volunteers. Levocetirizine was more inhibitory than fexofenadine on wheal, flare and pruritus (p < 0.005). Variability, evaluated from the standard deviation of inhibition, ranged from 14% to 23.2% for levocetirizine and 65.4% to 112.4% for fexofenadine. Levocetirizine had a faster onset of action (30-90 min versus 2 h), shorter time to maximum effect (3-4 versus 3-6 h) and longer duration of action (at least 24 h versus ~12 h) than fexofenadine. The plasma levels of levocetirizine rose more quickly, reached higher levels, were more consistent and decreased slower than those of fexofenadine. There were no clinically significant ethnic differences in responsiveness to the drugs.
authors.affiliation: Department of Dermatology and Allergy, Allergie-Centrum-Charité, Charité - Universitätsmedizin Berlin, Berlin, Germany.
authors.forename: Nicole
authors.initials: N
authors.lastname: Schoepke
authors.forename: Martin K
authors.initials: MK
authors.lastname: Church
authors.forename: Marcus
authors.initials: M
authors.lastname: Maurer
mesh_terms: D000328:Adult; D044466:Asian People; D017332:Cetirizine / Q000097:blood / Q000627:therapeutic use*; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005858:Germany / Q000453:epidemiology; D006632:Histamine / Q000008:administration & dosage*; D039563:Histamine H1 Antagonists, Non-Sedating / Q000097:blood / Q000627:therapeutic use*; D006801:Humans; D007564:Japan / Q000208:ethnology; D008297:Male; D011537:Pruritus / Q000139:chemically induced / Q000208:ethnology / Q000473:pathology / Q000517:prevention & control*; D012867:Skin / Q000187:drug effects* / Q000473:pathology; D016593:Terfenadine / Q000031:analogs & derivatives* / Q000097:blood / Q000627:therapeutic use; D013997:Time Factors; D016896:Treatment Outcome; D014581:Urticaria / Q000139:chemically induced / Q000208:ethnology / Q000473:pathology / Q000517:prevention & control*; D044465:White People; D055815:Young Adult
chemical_list: D039563:Histamine H1 Antagonists, Non-Sedating; C472067:levocetirizine; D016593:Terfenadine; D006632:Histamine; C093230:fexofenadine; D017332:Cetirizine