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Titolo:
INHIBITION OF METHADONE AND BUPRENORPHINE N-DEALKYLATIONS BY 3 HIV-1 PROTEASE INHIBITORS
Autore:
IRIBARNE C; BERTHOU F; CARLHANT D; DREANO Y; PICART D; LOHEZIC F; RICHE C;
Indirizzi:
FAC MED,EA948,LABS BIOCHIM,BP 815 F-29285 BREST FRANCE FAC MED,EA948,LABS BIOCHIM NUTR F-29285 BREST FRANCE FAC MED,PHARMACOL LAB F-29285 BREST FRANCE
Titolo Testata:
Drug metabolism and disposition
fascicolo: 3, volume: 26, anno: 1998,
pagine: 257 - 260
SICI:
0090-9556(1998)26:3<257:IOMABN>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN LIVER-MICROSOMES; CYTOCHROME-P450 3A4; IN-VITRO; INVOLVEMENT; METABOLISM; DEMETHYLATION; RITONAVIR; ENZYME; FAMILY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
27
Recensione:
Indirizzi per estratti:
Citazione:
C. Iribarne et al., "INHIBITION OF METHADONE AND BUPRENORPHINE N-DEALKYLATIONS BY 3 HIV-1 PROTEASE INHIBITORS", Drug metabolism and disposition, 26(3), 1998, pp. 257-260

Abstract

Ritonavir, indinavir, and saquinavir, all human immunodeficiency virus-1 protease inhibitors with a potent antiviral effect during triple therapy, are extensively metabolized by liver cytochrome P450 3A4. As this P450 isoform is involved in the metabolism of about 50% of drugs, coadministration of protease inhibitors with other drugs may lead to serious effects due to enzyme inhibition. Among these drugs, methadone and buprenorphine, both metabolized by P450 3A4, are potential candidates to drug interactions. In this study, metabolic interactions between these protease inhibitors and methadone or buprenorphine were studied in vitro in a panel of 13 human liver microsomes. Ritonavir was the most potent competitive inhibitor with K-i about 50 and 20 nM for methadone and buprenorphine metabolisms, respectively. Indinavir and saquinavir also inhibited methadone N-demethylation (K-i about 3 and 15 mu M, respectively) and buprenorphine N-dealkylation (K-i about 0.8 and 7mu M, respectively), The rank order of inhibition potency against metabolism of methadone and buprenorphine was ritonavir > indinavir > saquinavir. There is obvious potential for clinically significant drug interactions, particularly with ritonavir. In brief, caution should be advised if human immunodeficiency virus-1 protease inhibitors are coadministered with methadone and buprenorphine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 07:06:34