Dose-response relationship of the H1-histamine antagonist, ebastine, against histamine and methacholine-induced bronchoconstriction in patients with asthma.
In a double blind, randomised, placebo controlled trial in a group of extrinsic asthmatics, we have evaluated the potency and selectivity of ebastine, a new piperidine-type H1-receptor antagonist, against histamine and methacholine-induced bronchoconstriction. The median histamine PC20FEV1 value following placebo was 3.15 mg/ml (0.24-58.84). When compared with placebo, ebastine produced significant protection at 10 mg (median PC20 = 31.36 mg/ml, p = 0.008) and 30 mg (median PC20 = 42.14 mg/ml, p = 0.001) but there appeared to be no significant dose effect. Ebastine also produced a small shift in the methacholine concentration-response curves to the right. We conclude that ebastine is an effective antagonist of histamine-induced bronchoconstriction in the asthmatic airway with evidence of minor blockade of methacholine-induced bronchoconstriction.
Wood-Baker
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Immunopharmacology Group, Southampton General Hospital, Hampshire, UK.
Holgate
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D000328:Adult; D001249:Asthma / Q000139:chemically induced* / Q000503:physiopathology; D001980:Bronchi / Q000503:physiopathology; D002090:Butyrophenones / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005541:Forced Expiratory Volume; D006632:Histamine; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006801:Humans; D008297:Male; D008688:Methacholine Compounds; D008875:Middle Aged; D010880:Piperidines / Q000494:pharmacology*
D002090:Butyrophenones; D006634:Histamine H1 Antagonists; D008688:Methacholine Compounds; D010880:Piperidines; D006632:Histamine; C058249:ebastine