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Titolo:
Inhibition of drug metabolism in human liver microsomes by nizatidine, cimetidine and omeprazole
Autore:
Furuta, S; Kamada, E; Suzuki, T; Sugimoto, T; Kawabata, Y; Shinozaki, Y; Sano, H;
Indirizzi:
Zeria Pharmaceut Co Ltd, Cent Res Labs, Kohnan, Saitama 3600111, Japan Zeria Pharmaceut Co Ltd Kohnan Saitama Japan 3600111 itama 3600111, Japan
Titolo Testata:
XENOBIOTICA
fascicolo: 1, volume: 31, anno: 2001,
pagine: 1 - 10
SICI:
0049-8254(200101)31:1<1:IODMIH>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
S-MEPHENYTOIN 4'-HYDROXYLATION; PROTON PUMP INHIBITORS; IN-VITRO METABOLISM; CYTOCHROME-P450 ENZYMES; CAFFEINE METABOLISM; POOR METABOLIZERS; PHARMACOKINETICS; LANSOPRAZOLE; ANTAGONISTS; CYP2C19;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
30
Recensione:
Indirizzi per estratti:
Indirizzo: Furuta, S Zeria Pharmaceut Co Ltd, Cent Res Labs, 2512-1 Oshikiri, Kohnan,Saitama 3600111, Japan Zeria Pharmaceut Co Ltd 2512-1 Oshikiri Kohnan Saitama Japan 3600111
Citazione:
S. Furuta et al., "Inhibition of drug metabolism in human liver microsomes by nizatidine, cimetidine and omeprazole", XENOBIOTICA, 31(1), 2001, pp. 1-10

Abstract

1. The inhibitory effects of cimetidine, nizatidine and omeprazole on the metabolic activity of CYP2C9, 2C19, 2D6 and 3A were investigated in human liver microsomes. Both cimetidine and omeprazole inhibited each of the CYP subfamily enzymes; in particular, omeprazole extensively inhibited the hydroxylation of S-mephenytoin (CYP2C19, K-i = 7.1 muM). Nizatidine exhibited noinhibition of any of the CYP isoforms examined.2. Cimetidine inhibited the hydroxylation of tolbutamide but nor of diclofenac, whereas omeprazole inhibited the hydroxylation of diclofenac but not that of tolbutamide. The ability to inhibit CYP2C9 varied with incubation time, as measured by the metabolic rate constant for the substrates. Therefore, suitable substrates and incubation times must be selected in inhibitionstudies examining metabolic clearance and the mechanism of inhibition of these drugs.3. Nizatidine did not inhibit the metabolism of cisapride, glibenclamide, benidipine and simvastatin. Omeprazole inhibited the metabolism of cisapride (K-i = 0.4 muM), glibenclamide (11.7 muM) and benidipine (6.5 muM), whereas cimetidine inhibited the metabolism of glibenclamide (11.6 muM). To avoid drug-drug interactions, cure needs to be taken to select suitable medicines for co-administration with anti-ulcer drugs.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 13:21:17