![]() This process normally lowers the amount of statins. Increased plasma concentrations may cause increased side effects such as headache, fatigue, insomnia, and anxiety. Normally, when a person consumes statins without grapefruit juice, the enzyme CYP3A breaks them down within the intestines and liver. ![]() Increased drug exposure without effects on peak concentration may cause increased adverse events or toxicity evidenced by renal toxicity, hepatic toxicity, and increased immunosuppression. 21 – 24įluvastatin (Lescol), pravastatin (Pravachol), rosuvastatin (Crestor)įibric acids, nicotinic acid, or bile acid sequestrantsĬyclosporine (Sandimmune, Neoral), tacrolimus (Prograf) Increased plasma concentration may cause headaches, gastrointestinal complaints, hepatic inflammation, and myopathies (e.g., rhabdomyolysis). ![]() 9Īmlodipine (Norvasc), diltiazem (Cardizem), verapamil (Calan)Ītorvastatin (Lipitor), lovastatin (Mevacor), simvastatin (Zocor) Increased plasma concentration may lead to flushing, peripheral edema, headaches, tachycardia, symptomatic hypotension, and myocardial infarction in rare cases. 9, 20įelodipine (Plendil), nicardipine (Cardene), nifedipine (Procardia), nimodipine (Nimotop), nisoldipine (Sular) This interaction enhances systemic drug concentration through impaired drug metabolism. 1 3 Currently, more than 85 drugs, most of which are available in Canada, are known or predicted to interact with grapefruit. Increased plasma concentration of quinidine and disopyramide may be cardiotoxic causing torsades de pointes. Grapefruit juice inhibits the CYP3A4 enzyme of the cytochrome P450 system in the intestinal mucosa, increasing the bioavailability of drugs with a high. Our research group discovered the interaction between grapefruit and certain medications more than 20 years ago. 19ĭigoxin (Lanoxin), diltiazem (Cardizem), verapamil (Calan) The probable mechanism of this interaction was inhibition of CYP3A4-mediated first-pass metabolism of simvastatin by grapefruit juice in the small intestine. The most significant of these characteristics is metabolism by the intestinal. ![]() Increased plasma concentrations of amiodarone may cause thyroid or pulmonary toxicity, liver injury, QTc prolongation, proarrhythmic disorders, and bradycardia. MECHANISM OF INTERACTION The characteristics of medications that interact with grapefruit are well defined. Amiodarone (Cordarone), disopyramide (Norpace), quinidine ![]()
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