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Titolo:
THE TOLERABILITY AND PHARMACOKINETICS OF THE NOVEL ANTIMIGRAINE COMPOUND 311C90 IN HEALTHY MALE-VOLUNTEERS
Autore:
SEABER E; ON N; PHILLIPS S; CHURCHUS R; POSNER J; ROLAN P;
Indirizzi:
GLAXO WELLCOME,DEPT CLIN PHARMACOL,S EDEN PK RD BECKENHAM BR3 3BS KENT ENGLAND
Titolo Testata:
British journal of clinical pharmacology
fascicolo: 2, volume: 41, anno: 1996,
pagine: 141 - 147
SICI:
0306-5251(1996)41:2<141:TTAPOT>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
SUMATRIPTAN; MIGRAINE;
Keywords:
311C90; TOLERABILITY; PHARMACOKINETICS; FIRST ADMINISTRATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
9
Recensione:
Indirizzi per estratti:
Citazione:
E. Seaber et al., "THE TOLERABILITY AND PHARMACOKINETICS OF THE NOVEL ANTIMIGRAINE COMPOUND 311C90 IN HEALTHY MALE-VOLUNTEERS", British journal of clinical pharmacology, 41(2), 1996, pp. 141-147

Abstract

1 311C90 is a novel and selective agonist at 5-HT1D receptors, with central and peripheral actions, currently in development for the acute oral treatment of migraine. 2 The pharmacokinetic and tolerability profiles of single oral doses from 1-50 mg 311C90 were investigated in 12healthy male volunteers in a double-blind, placebo-controlled, dose-escalating study. 3 311C90 was well tolerated with most adverse experiences of mild and transient nature. 4 Absorption was rapid with dose-independent kinetics. Median t(max) was 2-4 h although 50-85% of eventual C-max was attained within 1 h. The t(1/2) was 2.5-3 h with a high apparent plasma clearance (CL/F > 2000 ml min(-1)) and apparent volume of distribution (V-z/F) of 400-500 l. 5 Three metabolites were detectedin plasma and urine, one of which, the N-desmethyl metabolite, has 5-HT1D agonist activity. 6 311C90 showed no clinically significant effects on blood pressure, heart rate, ECG or laboratory variables at any dose and demonstrated a tolerability and pharmacokinetic profile compatible with an acute oral migraine treatment.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 15:32:57