Grapefruit - the bad - drug interactions
In the 90s grapefruit was discovered to increase plasma concentrations of FELODIPINE a calcium channel blocker used in heart disease. How does it do this?
Grapefruit contains two chemicals, naringin and bergamottin that inhibit CYP3A4 which is an enzyme present in the liver and the small bowel. Many drugs are absorbed through the small bowel and metabolised partly in the small bowel with the liver finishing the process. This enzyme is involved in the metabolising of many drugs. Grapefruit increased drug levels by inhibiting the metabolism of that drug.
The more grapefruit you eat, the longer the inhibition.
This is like overdosing on the drug.
Hypertension drugs affected: CCBs: Felodipine Nisoldipine Nicardipine Nimodipine Verapamil. Effects: lowers BP too much causing low blood pressure:may cause rapid heart beats Psychiatric drugs including schizophrenia drugs, tranqilisers, mood altering drugs:Diazepam,Triazolam,Midazolam, Carbamazepine, Buspirone, Sertraline. Effects:increases the normal effect of the drug, e.g., increased sedation. Cholesterol meds: Statins: Simvastatin,Lovastatin,Atorvastatin: may increase the danger of side effects, some of which are fatal Cancer and auto-immune drugs: Immunosuppressants: Cyclosporin, Sirolimus,Tacrolimus : Increased side effects some life threatening.
HIV Saquinavir,Indinavir Erectile dysfunction Sildenafil, Tadalafil,Vardenafil Cardiovascular: Amiodarone, Warfarin
Check all prescriptions with the pharmacist to see if your drug is affected by grapefruit.
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