Methapyrilene kinetics and dynamics

A study was undertaken to characterize the H1 receptor blockade, central nervous system depressant properties, and kinetic parameters of methapyrilene in man. Eight healthy subjects received, in random order at weekly intervals, placebo and methapyrilene 20 mg intravenously and 50 mg and 25 mg orall...

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Bibliographic Details
Published inClinical pharmacology and therapeutics Vol. 29; no. 4; p. 527
Main Authors Calandre, E P, Alferez, N, Hassanein, K, Azarnoff, D L
Format Journal Article
LanguageEnglish
Published United States 01.04.1981
Subjects
Adult
Aminopyridines - metabolism
Female
Humans
Kinetics
Male
Methapyrilene - blood
Methapyrilene - metabolism
Methapyrilene - pharmacology
Receptors, Histamine - drug effects
Receptors, Histamine H1 - drug effects
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Summary:A study was undertaken to characterize the H1 receptor blockade, central nervous system depressant properties, and kinetic parameters of methapyrilene in man. Eight healthy subjects received, in random order at weekly intervals, placebo and methapyrilene 20 mg intravenously and 50 mg and 25 mg orally. Methapyrilene exhibited a moderate antihistaminic effect as measured by the reduction of histamine-provoked skin wheals. Sedation and drowsiness were detected only at the first sampling time (0.75 hr) after intravenous doses. The terminal plasma half-life ranged from 1.1 to 2.1 hr, apparent volume of distribution from 2.14 to 6.61 1/kg, and plasma clearance from 0.013 to 0.048 1/min/kg. Systemic bioavailability was low and showed large interindividual differences, ranging from 4% to 46%. Recovery of unchanged drug from the 24-hr urine was under 2% of the doses.
ISSN:0009-9236
1532-6535
DOI:10.1038/clpt.1981.74