Palumbo G, Bacchi S, Palumbo P, Primavera L G, Sponta A M
Farmacologia Medica, Dipartimento di Medicina Interna e Sanità Pubblica, Università degli Studi di L'Aquila, Italia.
Clin Ter. 2005 May-Jun;156(3):97-103.
More than a decade has passed since it was unintentionally discovered that grapefruit juice interacts with certain drugs. The coadministration of these drugs with grapefruit juice can markedly elevate drug bioavailability, and can alter pharmacokinetic and pharmacodynamic parameters of the drug. The predominant mechanism for this interaction is the inhibition of cytochrome P-450 3A4 in the small intestine, resulting in a significant reduction of drug presystemic metabolism. An additional mechanism is the inhibition of P-glycoprotein, a transporter that carries drug from the enterocyte back to the gut lumen, resulting in a further increase in the fraction of drug absorbed. Some calcium channel antagonists, benzodiazepines, HMG-CoA reductase inhibitors and cyclosporine are the most affected drugs. A single exposure to one glass of the grapefruit juice can usually produce the maximal magnitude of the interaction. The data available so far, concerning this interaction and its clinical implications, are reviewed in this article. It is likely that more information regarding this interaction will accumulate in the future, and awareness of such is necessary for achieving optimal drug therapy.
自无意间发现葡萄柚汁与某些药物相互作用以来，已经过去了十多年。这些药物与葡萄柚汁共同服用可显著提高药物生物利用度，并可改变药物的药代动力学和药效学参数。这种相互作用的主要机制是小肠中细胞色素P - 450 3A4受到抑制，导致药物的首过代谢显著减少。另一种机制是P - 糖蛋白受到抑制，P - 糖蛋白是一种将药物从肠细胞转运回肠腔的转运蛋白，导致吸收的药物分数进一步增加。一些钙通道拮抗剂、苯二氮䓬类药物、HMG - CoA还原酶抑制剂和环孢素是受影响最大的药物。单次饮用一杯葡萄柚汁通常就能产生最大程度的相互作用。本文综述了目前关于这种相互作用及其临床意义的可用数据。未来可能会积累更多关于这种相互作用的信息，了解这一点对于实现最佳药物治疗很有必要。
