Pharmacological modulation of cutaneous reactivity to histamine: a double-blind acute comparative study between cetirizine, terfenadine and astemizole.
In a double-blind study performed in 81 healthy volunteers, 10 mg cetirizine and 60 mg terfenadine given orally in a single administration significantly inhibited skin reactivity to histamine. Astemizole (10 mg) was completely ineffective. The inhibitory effect of cetirizine was potent and regular whereas 6/28 (21%) volunteers did not respond to terfenadine. The difference observed between cetirizine and terfenadine might be due to differences in the metabolism of the two drugs after administration: terfenadine is rapidly and extensively metabolized whereas cetirizine is directly active without the need for biotransformation and, indeed is poorly metabolized.
Ghys
L
L
UCB sa, Chemin du Foriest, Braine l'Alleud, Belgium.
Rihoux
J P
JP
D000328:Adult; D016589:Astemizole; D001559:Benzhydryl Compounds / Q000494:pharmacology*; D001562:Benzimidazoles / Q000494:pharmacology*; D017332:Cetirizine; D004311:Double-Blind Method; D006632:Histamine / Q000494:pharmacology*; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006801:Humans; D006919:Hydroxyzine / Q000031:analogs & derivatives* / Q000494:pharmacology; D012867:Skin / Q000187:drug effects / Q000276:immunology*; D016593:Terfenadine
D001559:Benzhydryl Compounds; D001562:Benzimidazoles; D006634:Histamine H1 Antagonists; D006919:Hydroxyzine; D016593:Terfenadine; D016589:Astemizole; D006632:Histamine; D017332:Cetirizine