Interaction of grapefruit juice and calcium channel blockers.
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.
Sica
Domenic A
DA
Department of Clinical Pharmacology and Hypertension, Division of Nephrology, Medical College of Virginia of Virginia Commonwealth University, Richmond, Virginia, USA. dsica@hsc.vcu.edu
D001628:Beverages / Q000009:adverse effects*; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000493:pharmacokinetics* / Q000627:therapeutic use; D032083:Citrus paradisi / Q000009:adverse effects*; D065692:Cytochrome P-450 CYP3A Inhibitors; D018565:Food-Drug Interactions; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D007422:Intestines / Q000201:enzymology
D002121:Calcium Channel Blockers; D065692:Cytochrome P-450 CYP3A Inhibitors