Evidence of an interaction between nifedipine and nafcillin in humans.

Article Details

Citation

Lang CC, Jamal SK, Mohamed Z, Mustafa MR, Mustafa AM, Lee TC

Evidence of an interaction between nifedipine and nafcillin in humans.

Br J Clin Pharmacol. 2003 Jun;55(6):588-90.

PubMed ID
12814453 [ View in PubMed
]
Abstract

AIMS: Nafcillin (Wyeth Laboratories, Philadelphia, PA, USA) has been reported to induce the metabolism of cyclosporin and warfarin, which are known substrates of cytochrome P-450 (CYP). However, there has not been any report to date on its possible interaction with nifedipine, an index substrate of the enzyme, CYP3A4. METHODS: Nine healthy normotensive subjects participated in this randomized placebo-controlled two-way crossover study examining the effects of 5 days' pretreatment of nafcillin 500 mg or placebo four times daily on the pharmacokinetics of an oral dose of nifedipine 10 mg. Plasma nifedipine concentrations were measured by gas chromatography-mass spectro. RESULTS: The area under the plasma nifedipine concentration-time curve (AUC0-alpha) in nafcillin-pretreated subjects (80.9 +/- 32.9 micro g l-1 h-1) was significantly decreased compared with subjects who received only nifedipine (216.4 +/- 93.2 micro g l-1 h-1) (P < 0.001). Total plasma clearance of nifedipine (CL/F) was significantly increased with nafcillin pretreatment (138.5 +/- 42.0 l h-1 vs 56.5 +/- 32.0 l h-1) (P < 0.002). CONCLUSIONS: The results show that nafcillin pretreatment markedly increased the clearance of nifedipine and suggest that nafcillin is a potent inducer of CYP enzyme.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
NafcillinCytochrome P450 3A4ProteinHumans
Unknown
Inducer
Details
Drug Interactions
DrugsInteraction
Cyclosporine
Nafcillin
The metabolism of Cyclosporine can be increased when combined with Nafcillin.