Literature DB >> 16029222

Effect of atorvastatin and fluvastatin on the metabolism of midazolam by cytochrome P450 in vitro.

C G Mc Donnell1, G Shorten, F N A M Van Pelt.   

Abstract

We have investigated the effects of the statins atorvastatin and fluvastatin on the cytochrome P450 3A4 enzyme (CYP 3A4)-mediated metabolism of midazolam in vitro, using pooled human liver microsomes. Midazolam was metabolised by human hepatic microsomes with a Michaelis-Menten constant (K(m)) of 5.25 (SD 1.2) micromol.l(-1). Atorvastatin was a moderate competitive inhibitor of CYP 3A4 with an inhibitory constant (K(i)) of 12.4 (95% CI 4.65-20.06) micromol.l(-1). Fluvastatin was a weak non-competitive inhibitor of CYP 3A4 with a K(i) of 94.3 (95% CI 55.01-133.5) micromol.l(-1). Both atorvastatin and fluvastatin inhibit the CYP 3A4-mediated metabolism of midazolam in vitro.

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Year:  2005        PMID： 16029222     DOI： 10.1111/j.1365-2044.2005.04110.x

Source DB:  PubMed          Journal:  Anaesthesia        ISSN： 0003-2409            Impact factor:   6.955


  9 in total

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