Influence of nicardipine and nifedipine on plasma carvedilol disposition after oral administration in rats.

Article Details

Citation

Hokama N, Hobara N, Sakai M, Kameya H, Ohshiro S, Sakanashi M

Influence of nicardipine and nifedipine on plasma carvedilol disposition after oral administration in rats.

J Pharm Pharmacol. 2002 Jun;54(6):821-5.

PubMed ID
12078998 [ View in PubMed
]
Abstract

The effect of two kinds of 1,4-dihydropyridine calcium-channel blockers, nicardipine hydrochloride and nifedipine, on the disposition of carvedilol, was studied in rats. Blood samples were assayed for carvedilol levels using solid-phase extraction and high-performance liquid chromatography. The plasma carvedilol concentration was found to be significantly higher, and the area under the concentration-time curve up to 24 h (AUC0-->24) was 6.7 and 3.0 times higher after simultaneous oral administration of 20 mg kg(-1) carvedilol with 40 mg kg(-1) nicardipine hydrochloride, or with 40 mg kg(-1) nifedipine, respectively, than after administration of carvedilol alone. The pharmacokinetic interaction between carvedilol and dihydropyridine calcium-channel blockers is thought to be attributable to vasodilator-induced changes in hepatic first-pass metabolism, inhibition in the absorption barrier by P-glycoprotein and in the metabolism of carvedilol.

DrugBank Data that Cites this Article

Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
CarvedilolP-glycoprotein 1ProteinHumans
Unknown
Inhibitor
Details
Drug Interactions
DrugsInteraction
Carvedilol
Nicardipine
Nicardipine may increase the hypotensive activities of Carvedilol.