Drug-grapefruit juice interactions: two mechanisms are clear but individual responses vary.

来自 dx.doi.org

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作者：

Munir，Pirmohamed

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摘要：

Grapefruit juice, a beverage consumed in large quantities by the general population, is an inhibitor of the intestinal cytochrome P-450 3A4 system, which is responsible for the first-pass metabolism of many medications. Through the inhibition of this enzyme system, grapefruit juice interacts with a variety of medications, leading to elevation of their serum concentrations. Most notable are its effects on cyclosporine, some 1,4-dihydropyridine calcium antagonists, and some 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. In the case of some drugs, these increased drug concentrations have been associated with an increased frequency of dose-dependent adverse effects. The P-glycoprotein pump, located in the brush border of the intestinal wall, also transports many cytochrome P-450 3A4 substrates, and this transporter also may be affected by grapefruit juice. This review discusses the proposed mechanisms of action and the medications involved in drug-grapefruit juice interactions and addresses the clinical implications of these interactions.

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关键词：

AUC area under the plasma concentration–time curve area under the plasma concentration–time curve CYP cytochrome P-450 cytochrome P-450 HMG-CoA 3-hydroxy-3-methyl glutaryl coenzyme A 3-hydroxy-3-methyl glutaryl coenzyme A Pgp P-glycoprotein P-glycoprotein