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Eur J Clin Pharmacol. 1996;50(1-2):83-9.

Influence of renal failure on cytochrome P450 activity in hypertensive patients using a "cocktail" of antipyrine and nifedipine.

Author information

1
Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Brazil.

Abstract

OBJECTIVE:

Two substrates were coadministered in a "cocktail" approach to evaluate the contribution of renal failure to drug oxidation.

PATIENTS:

Nineteen hypertensive patients, nine of them with chronic renal failure (CLCR 38.9 vs 102.3 ml.min-1 1.73 m-2), were investigated after peroral administration of a combination of antipyrine (500 mg, in capsules) and nifedipine (10 mg, in Oxcord capsules) in the morning after an overnight fast.

RESULTS:

This "cocktail" approach made it possible to characterize in vivo the activities of different forms of cytochrome P450 in a single-study protocol using the total clearance of nifedipine and clearance for production of 3-hydroxymethylantipyrine (HMA), 4-hydroxyantipyrine (OHA) and norantipyrine (NORA). With this "cocktail" approach (antipyrine plus nifedipine), we can suggest a selective effect on the activities of cytochrome P450 forms associated with the formation of dehydronifedipine (P450 III A4) and of NORA in patients with mild renal failure under long-term antihypertensive therapy.

PMID:
8739816
DOI:
10.1007/s002280050073
[Indexed for MEDLINE]

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