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Affected drugs
This list is incomplete; you can help by expanding it [3]. The following drugs are affected by CYP3A4 inhibition with grapefruit compounds: The benzodiazepines triazolam (Halcion), orally administered midazolam (Versed), orally administered nitrazepam (Mogodon), diazepam (Valium), alprazolam (Xanax) and quazepam (Doral, Dormalin)[4] ritonavir (Norvir): Inhibition of CYP3A4 prevents the metabolism of protease inhibitors such as ritonavir.[5] sertraline (Zoloft and Lustral)[6] Additional drugs found to be affected by grapefruit juice include, but are not limited to: Some statins such as atorvastatin (Lipitor), lovastatin (Mevacor) and simvastatin (Zocor, Simlup, Simcor, Simvacor); however, pravastatin (Pravachol), fluvastatin (Lescol) and rosuvastatin (Crestor) are unaffected by grapefruit.[][7] Dihydropyridines including felodipine (Plendil), nicardipine (Cardene), nifedipine, nisoldipine (Sular) and nitrendipine (Bayotensin)[] losartan (Cozaar)[] The cough suppressant dextromethorphan[citation needed] modafinil (Provigil, Alertec, Modavigil, Modalert, Modiodal, Modafinilo, Carim, Vigia)[citation needed] repaglinide (Prandin)[] verapamil (Calan SR, Covera HS, Isoptin SR, Verelan)[] buspirone (Buspar): Grapefruit juice increased peak and AUC plasma concentrations of buspirone 4.3- and 9.2-fold, respectively, in a randomized, 2-phase, ten-subject crossover study.[8] levothyroxine (Eltroxin, Levoxyl, Synthroid): the absorption of levothyroxine is affected by grapefruit juice.Wikipedia:Please clarify [9]
Grapefruit drug interactions Antiarrhythmics including amiodarone (Cordarone), dronedarone (Multaq), quinidine (Quinidex, Cardioquin, Quinora), disopyramide (Norpace), propafenone (Rhythmol) and carvedilol (Coreg)[] Antihistamines astemizole (Hismanal) and terfenadine (Seldane) - now removed from the US and Canadian markets[citation needed] cisapride (Prepuslid, Propulsid) (which treats GERD) - now removed from the US and Canadian markets[citation
needed]
Erectile dysfunction drugs sildenafil (Viagra), tadalafil (Cialis) and vardenafil (Levitra)[][10] The anti-migraine drugs ergotamine (Cafergot, Ergomar), amitryptiline (Elavil, Endep, Vanatrip) and nimodipine (Nimotop)[] Fluvoxamine (Luvox, Faverin, Fevarin and Dumyrox)[] Codeine:[] Grapefruit juice reduces the amount of codeine converted by CYP3A4 into norcodeine, thus increasing the amount metabolized into morphine.[citation needed] Morphine itself, however, is not affected by grapefruit juice, as it is not metabolized by the cytochrome P450 system. Cyclosporine (Neoral): Blood levels of cyclosporine are increased if taken with grapefruit juice. A plausible mechanism involves the combined inhibition of enteric CYP3A4 and P-glycoprotein, which potentially leads to serious adverse events (e.g., nephrotoxicity). Blood levels of tacrolimus (Prograf) can also be equally affected for the same reason as cyclosporine, as both drugs are calcineurin inhibitors.[11] omeprazole (Losec, Prilosec)[12] zolpidem (Ambien): Little or no interaction with grapefruit juice.[] oxycodone: metabolized by the cytochrome P450 system, specifically CYP3A4, of which the bergamottin flavonoid is a strong inhibitor[13] hydrocodone: The hepatic cytochrome P450 enzyme CYP2D6 converts it into hydromorphone, a more potent opioid.[citation needed] dihydrocodeine[citation needed] quetiapine (Seroquel)[14] methadone: Inhibits the metabolism of methadone and raises serum levels.[15] buprenorphine: Metabolized into norbuprenorphine by cytochrome-P450 isoenzyme 3A4[16] Tyrosine kinase inhibitors, including imatinib (Gleevec) and nilotinib (Tasigna), used to treat chronic myelogenous leukemia and gastrointestinal stromal tumors.[citation needed] trazodone (Desyrel): Little or no interaction with grapefruit juice.[] Anthelmintics: Used for treating certain parasitic infections; includes praziquantel albendazole and mebendazole[citation needed] carbamazepine (Tegretol): Grapefruit or grapefruit juice slows the breakdown of this drug, increasing the level of it in blood[citation needed] imatinib (Gleevec): Although no formal studies with imatinib and grapefruit juice have been conducted, the fact that grapefruit juice is a known inhibitor of the CYP 3A4 suggests that co-administration may lead to increased imatinib plasma concentrations. Likewise, although no formal studies were conducted, co-administration of imatinib with another specific type of citrus juice called Seville orange juice (SOJ) may lead to increased imatinib plasma concentrations via inhibition of the CYP3A isoenzymes. Seville orange juice is not usually consumed as a juice because of its sour taste, but it is found in marmalade and other jams. Seville orange juice has been reported to be a possible inhibitor of CYP3A enzymes without affecting P-glycoprotein when taken concomitantly with cyclosporine.[17] Loperamide (Imodium)[citation needed] colchicine (Colcrys)[citation needed] erlotinib (Tarceva) [18] In a mouse study, blood concentrations of acetaminophen/paracetamol (Tylenol) were found to be increased by white and pink grapefruit juice, with the white juice acting faster.[19]
Antihistamines
Cholesterol-lowering drugs aka simvastatin (Zocor) Statins (HMG-CoA reductase inhibitors) lovastatin (Mevacor) Cough Suppressant/NMDA Antagonist Erectile Dysfunction drugs dextromethorphan
4
saquinavir (Invirase) ritonavir (Norvir) nelfinavir (Viracept) amprenavir (Agenerase) ethinyl estradiol (Ortho-Cept, many others) methylprednisolone (Medrol) cyclosporine (Sandimmune, Neoral) tacrolimus (Prograf) sirolimus (Rapamune) mercaptopurine buspirone (Buspar) triazolam (Halcion) midazolam (Versed) diazepam (Valium) zaleplon (Sonata) alprazolam (Xanax) carbamazepine (Tegretol) trazodone (Desyrel) quetiapine (Seroquel) fluvoxamine (Luvox) nefazodone (Serzone) (off the market) cisapride (Prepulsid, Propulsid) []
Hormones
Immunosuppressants
Other psychotropics
References
[3] http:/ / en. wikipedia. org/ w/ index. php?title=Grapefruit_drug_interactions& action=edit [11] " Further characterization of a furanocoumarin-free grapefruit juice on drug disposition: studies with cyclosporine (http:/ / www. ajcn. org/ cgi/ content/ abstract/ 87/ 4/ 863)", American Journal of Clinical Nutrition, Vol. 87, No. 4, 863-871, April 2008. [12] http:/ / www. ncbi. nlm. nih. gov/ pmc/ articles/ PMC2014525/ Mouly and Paine, Br J Clin Pharmacol. 2001 August; 52(2): 216217. [13] Wikipedia article on oxycodone metabolism; pharmaceutical insert w/ Purdue OxyContin tablets - http:/ / en. wikipedia. org/ wiki/ Oxycodone#Metabolism [17] (http:/ / www. gistsupport. org/ treatments-for-gist/ gleevec/ novartis-answers-about-gleevec. php) [20] Lundahl J, Regardh CG, Edgar B, Johnsson G. Relationship between time of intake of grapefruit juice and its effect on pharmacokinetics and pharmacodynamics of felodipine in healthy subjects. Eur J Clin Pharmacol 1995;49:61-7.
External links
USDA Database of Flavonoid content of food (http://www.nal.usda.gov/fnic/foodcomp/Data/Flav/flav.pdf) Graedon's Guide to Grapefruit Interactions. (http://www.healthcentral.com/peoplespharmacy/pp_guides/PDF/ gfruit02.pdf)PDF(34.6KB) Appendix 1: Grapefruit Interacting Drugs and Associated Oral Bioavailability, Adverse Event(s), Risk Ranking and Potential Alternative Medications (http://www.cmaj.ca/content/suppl/2012/11/26/cmaj.120951.DC1/ grape-bailey-1-at.pdf) Appendix to: Bailey DG, Dresser G, Arnold JMA. Grapefruit and medication interactions: forbidden fruit or avoidable consequences? CMAJ 2012; doi: 10.1503/cmaj.120951 (http://dx.doi.org/10. 1503/cmaj.120951). Copyright 2012 Canadian Medical Association or its licensors
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