葡萄柚汁与钙通道阻滞剂的相互作用。

Interaction of grapefruit juice and calcium channel blockers.

作者信息

Sica Domenic A

机构信息

Department of Clinical Pharmacology and Hypertension, Division of Nephrology, Medical College of Virginia of Virginia Commonwealth University, Richmond, Virginia, USA.

出版信息

Am J Hypertens. 2006 Jul;19(7):768-73. doi: 10.1016/j.amjhyper.2005.11.003.

DOI:10.1016/j.amjhyper.2005.11.003

PMID:16814135

Abstract

Drug-drug interactions are commonly recognized occurrences in the hypertensive population. Drug-nutrient interactions, however, are less well appreciated. The grapefruit juice-calcium channel blocker interaction is one that has been known since 1989. The basis for this interaction has been diligently explored and appears to relate to both flavanoid and nonflavanoid components of grapefruit juice interfering with enterocyte CYP3A4 activity. In the process, presystemic clearance of susceptible drugs decreases and bioavailability increases. A number of calcium channel blockers are prone to this interaction, with the most prominent interaction occurring with felodipine. The calcium channel blocker and grapefruit juice interaction should be incorporated into the knowledge base of rational therapeutics for the prescribing physician.

摘要

药物相互作用在高血压人群中是常见的现象。然而，药物与营养素之间的相互作用却鲜为人知。自1989年以来，人们就已经知道葡萄柚汁与钙通道阻滞剂之间的相互作用。这种相互作用的机制已得到深入研究，似乎与葡萄柚汁中的类黄酮和非类黄酮成分干扰肠细胞CYP3A4活性有关。在此过程中，易感药物的首过清除率降低，生物利用度增加。许多钙通道阻滞剂都容易发生这种相互作用，其中与非洛地平的相互作用最为显著。对于开处方的医生来说，钙通道阻滞剂与葡萄柚汁之间的相互作用应纳入合理治疗的知识体系中。