Grapefruit Drug Interaction List. MayoClinic.com lists several statins that interact with grapefruit. Grapefruit juice shouldn't. Grapefruit juice can interact with drugs. Grapefruit Juice and Medication Interactions. The following is a list of medications and medication classes with. Grapefruit and Some Medications. If you are not taking any drugs that can interact with grapefruit.
These active materials inhibit a key enzyme (cytochrome P4. CYP3. A4) which is responsible (among other activities) for drug metabolism. The effect happens in two ways. One is that grapefruit can block the hepatic CYP3. A4 thereby affecting the medication metabolism. The other effect is that grapefruit can block the enterocyte CYP3. A4 thereby affecting the medication absorption in the intestine. Organic compounds that are furanocoumarin derivatives interfere with the hepatic and intestinalenzymecytochrome P4. CYP3. A4 and are believed to be primarily responsible for the effects of grapefruit on the enzyme. Thus, they are present in all forms of the fruit, including freshly squeezed juice, frozen concentrate, and whole fruit. All these forms of the grapefruit juice have the potential to limit the metabolizing activity of CYP3. A4. One whole grapefruit, or a glass of 2. L (6. 8 US fl oz) of grapefruit juice can cause drug overdose toxicity. Grapefruit relatives and other pomelo descendants have variable amounts of furanocoumarins. Many oral drugs undergo first- pass (presystemic) metabolism by the enzyme. Several organic compounds found in grapefruit and specifically in grapefruit juice exert inhibitory action on drug metabolism by the enzyme. It has been established that a group of compounds called furanocoumarins are responsible for this interaction, and not flavonoids as was previously reported. Another inhibitor of cytochrome P4. This interaction is particularly dangerous when the drug in question has a low therapeutic index, so that a small increase in blood concentration can be the difference between therapeutic effect and toxicity. Grapefruit juice inhibits the enzyme only within the intestines if consumed in small amounts. Intestinal enzyme inhibition will only affect the potency of orally administrated drugs. When larger amounts of grapefruit are consumed it may also inhibit the enzyme in the liver. The hepatic enzyme inhibition may cause an additional increase in potency and a prolonged metabolic half- life (prolonged metabolic half- life for all ways of drug administration). Pgp transports lipophilic molecules out of the enterocyte back into the intestinal lumen. Drugs that possess lipophilic properties are either metabolised by CYP3. A4 or removed into the intestine by the Pgp transporter. Both the Pgp and CYP3. A4 may act synergistically as a barrier to many orally administered drugs. Therefore, their inhibition (both or alone) can markedly increase the bioavailability of a drug. The interaction caused by grapefruit compounds lasts for up to 7. CYP3. A4 is a metabolizing enzyme for almost 5. When the metabolizing enzyme is inhibited, less of the drug will be metabolized by it in the epithelial cells. A decrease in drug metabolism means more of the original form of the drug could pass unchanged to systemic blood circulation. In order for drugs to be absorbed, they must pass through the epithelial cells that line the lumen wall before they can enter the hepatic portal circulation to be distributed systemically in blood circulation. Drugs are metabolized by drug- specific metabolizing enzymes in the epithelial cells. Metabolizing enzymes transform these drugs into metabolites. The primary purpose for drug metabolism is to detoxify, inactivate, solubilize and eliminate these drugs. It takes around 2. For this reason, simply separating grapefruit consumption and medication taken daily does not avoid the interaction. A 4- hour interval between grapefruit consumption and the medication should suffice. Drugs that interact with grapefruit juice share 3 common features: they are taken orally, normally only a small amount enters systemic blood circulation, and they are metabolized by CYP3. A4. Researchers have identified 8. From 2. 00. 8 to 2. Examples of such known CYP3. A4 inhibitors include cisapride (Propulsid). This suggests that repeated intake of grapefruit juice reduces the efficacy and bioavailability of acetaminophen/paracetamol in comparison to a single dose of grapefruit juice which conversely increases the efficacy and bioavailability of acetaminophen/paracetamol. A plausible mechanism involves the combined inhibition of enteric CYP3. A4 and P- glycoprotein, which potentially leads to serious adverse events (e. Blood levels of tacrolimus (Prograf) can also be equally affected for the same reason as ciclosporin, as both drugs are calcineurin inhibitors. 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 CYP3. A 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 CYP3. A enzymes without affecting P- glycoprotein when taken concomitantly with ciclosporin. And a randomized, controlled trial 1. L of either grapefruit juice or water three times daily for five days. On the fourth day 1. Analgesic and behavioral effects were reported for 1. Grapefruit juice and increased the mean area under the oxycodone concentration- time curve (AUC(0- . The metabolite- to- parent ratios of noroxycodone and noroxymorphone decreased by 4. Grapefruit juice may potentially reduce the effectiveness of tamoxifen. The first published report on grapefruit drug interactions was in 1. Lancet entitled . However, the effect only became well- publicized after being responsible for a number of bad interactions with medication. This is problematic as a 4 oz portion of grapefruit contains enough naringin to inhibit the metabolism of substrates of CYP3. A4. Juice of limes and Seville oranges can also inhibit drug metabolism, however, as can apple juice with some drugs. Clinical Pharmacology & Therapeutics, 7. G.; Dresser, G.; Arnold, J. Canadian Medical Association Journal. Journal of Clinical Pharmacology. PMID 1. 29. 53. 34. He K, Iyer KR, Hayes RN, Sinz MW, Woolf TF, Hollenberg PF (April 1. Chemical Research in Toxicology. British Journal of Clinical Pharmacology. Clinical Pharmacology and Therapeutics. American Journal of Cardiovascular Drugs. Exploring mechanisms of this interaction and potential toxicity for certain drugs. Fruits of warm climates. Canadian Medical Association Journal (Canadian Medical Association). The American Journal of Clinical Nutrition. Journal of Clinical Pharmacology. European Journal of Clinical Pharmacology. Clinical Pharmacology and Therapeutics. J Clin Psychopharmacol. Archives of Biochemistry and Biophysics. European Journal of Clinical Pharmacology. Biochemical Pharmacology. Clinical Therapeutics. Nucleic Acids Research. Database issue): D2. Cell Death & Disease. Molecular Pharmacology. National Library of Medicine. Clinical Pharmacology and Therapeutics. American Journal of Cardiovascular Drugs. American Journal of Cardiovascular Drugs. Clinical Pharmacology and Therapeutics. Journal of Medicinal Food. European Journal of Drug Metabolism and Pharmacokinetics. Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft F. Retrieved 3 April 2. Clinical Pharmacokinetics. Clinical Pharmacology and Therapeutics. Mayo Clinic Proceedings. The American Journal of Clinical Nutrition. Clinical Pharmacology and Therapeutics. Medscape Medical News. Journal of Clinical Psychopharmacology. Archived from the original on 2. January 2. 01. 1. Retrieved 3. 1 December 2. British Journal of Clinical Pharmacology. Clinical Pharmacology and Therapeutics. British Journal of Clinical Pharmacology. Basic & Clinical Pharmacology & Toxicology. Journal of Pharmaceutical Sciences. Harvard Medical School Family Health Guide. Pharmacist's Letter/Prescriber's Letter of Natural Medicines Comprehensive Database. Stockton, CA: Therapeutic Research Faculty. Bakalar, Nicholas (2. Clinical Pharmacology and Therapeutics.
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