Title : Pharmacogenetic determinants of human liver microsomal alfentanil metabolism and the role of cytochrome P450 3A5.

Pub. Date : 2005 Mar

PMID : 15731592






5 Functional Relationships(s)
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1 Alfentanil undergoes extensive metabolism by cytochrome P4503A4 (CYP3A4). Alfentanil cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Alfentanil undergoes extensive metabolism by cytochrome P4503A4 (CYP3A4). Alfentanil cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 METHODS: Alfentanil metabolism to noralfentanil and N-phenylpropionamide was determined in microsomes from two groups of human livers, characterized for CYP3A4 and CYP3A5 protein content: low CYP3A5 (2.0-5.2% of total CYP3A, n = 10) and high CYP3A5 (46-76% of total CYP3A, n = 10). Alfentanil cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 The effects of the CYP3A inhibitors troleandomycin and ketoconazole, the latter being more potent toward CYP3A4, on alfentanil metabolism were also determined. Alfentanil cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 Therefore, alfentanil is metabolized by human liver microsomal CYP3A5 in addition to CYP3A4, and pharmacogenetic variability in CYP3A5 expression significantly influences human liver alfentanil metabolism in vitro. Alfentanil cytochrome P450 family 3 subfamily A member 4 Homo sapiens