In vivo effect of diallyl sulfide and cimetidine on phenacetin metabolism and bioavailability in rat

• Autorzy: Szutowski M. M. , Zalewska K. , Jadczak M. , Marek M.
• Języki publikacji: EN

Abstrakty

EN

Numerous cytochrome P450 inhibitors have been described as effective modulators of cytochrome P450 isoforms activity in vitro. Their inhibitory efficiency may be con­siderably modified after in vivo application. The aim of this study was to examine the effect of oral administration of diallyl sulfide — a cytochrome P450 2E1 inhibitor and cimetidine — a cytochrome P450 2C6 and 2C11 inhibitor on rat serum concentration of phenacetin and its metabolite acetaminophen. Both inhibitors increased area un­der the curve (AUC0-4h) for phenacetin by 50%. Only cimetidine reduced AUC0-4 h for acetaminophen indicating inhibition of O-deethylation activity. Quinidine — a cyto­chrome P450 2D subfamily and P-glycoprotein inhibitor did not change significantly phenacetin bioavailability. These results suggest that diallyl sulfide inhibits the deacetylation pathway catalysed by arylamine N-acetyl transferase. Beside cyto­chrome P450 1A2 other cytochrome P450 isoforms (2A6 and/or 2C11) are involved in phenacetin O-deethylation in rat.

Słowa kluczowe

EN

cimetidine; diallyl sulphide; in vivo; phenacetin; cytochrome P450; rat

• Wydawca: -
• Czasopismo: Acta Biochimica Polonica
• Rocznik: 2002
• Tom: 49
• Numer: 1
• Opis fizyczny: p.249-256,fig.

Twórcy

autor

Szutowski M. M.

• Medical University of Warsaw, S.Banacha 1, 02-097 Warsaw, Poland

autor

Zalewska K.

autor

Jadczak M.

autor

Marek M.

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