The drug-drug interaction mediated by efflux transporters and CYP450 enzymes / 药学学报
Acta Pharmaceutica Sinica
; (12): 590-595, 2014.
Article
em Zh
| WPRIM
| ID: wpr-245042
Biblioteca responsável:
WPRO
ABSTRACT
Multidrug regimens and corresponding drug interactions cause many adverse reactions and treatment failures. Drug efflux transporters: P-glycoprotein (P-gp), multidrug resistance associated protein (MRP) and breast cancer resistance protein (BCRP) in conjunction with metabolizing enzymes (cytochrome P450, CYP450) are major factors in such interaction. In recent years, a large number of studies have shown that P-gp plays a role in the oxidative metabolism of its substrates that are also substrates of CYP3A4. Combined actions of P-gp and CYP3A could account in some part for the low oral bioavailability determined for many of these dual substrates. P-gp along with efflux transporters (MRP and BCRP) having overlapping substrate specificity plays critical role in drug disposition. The relationship between MRP or BCRP and CYP3A is similar to that between P-gp and CYP3A. In this paper, we summarize the classification of efflux transporters, the main metabolizing enzymes CYP3A, clinical significance interactions mediated by efflux transporters and CYP450 enzymes and in vitro studies.
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Especificidade por Substrato
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Disponibilidade Biológica
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Membro 1 da Subfamília B de Cassetes de Ligação de ATP
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Transportadores de Cassetes de Ligação de ATP
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Sistema Enzimático do Citocromo P-450
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Proteínas Associadas à Resistência a Múltiplos Medicamentos
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Interações Medicamentosas
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Citocromo P-450 CYP3A
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Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP
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Metabolismo
Limite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2014
Tipo de documento:
Article