As a result, the amount of the drug in its original form that reaches systemic circulation is reduced due to this first-pass metabolism. The primary purpose for drug metabolism is to detoxify, inactivate, solubilize and eliminate these drugs. Metabolizing enzymes transform these drugs into metabolites. ![]() Drugs are metabolized by drug-specific metabolizing enzymes in the epithelial cells. 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. When drugs are taken orally, they enter the gut lumen to be absorbed in the small intestine and sometimes, in the stomach. Drugs metabolized by these enzymes may have interactions with citrus chemicals. Cytochrome isoforms affected by grapefruit components also include CYP1A2, CYP2C9, and CYP2D6. Organic derivatives of furanocoumarin interfere with liver and intestinal enzyme CYP3A4 and may be responsible for the effects of grapefruit on the enzyme. ( August 2017) ( Learn how and when to remove this template message) Please help improve this section if you can. The specific problem is: lack of coherent overview. This section may require cleanup to meet Wikipedia's quality standards. Furanocoumarins may have a stronger effect than naringin. Grapefruit, Seville oranges, and bergamot contain naringin. Polyphenols Ĭitrus fruits may contain various polyphenols, including naringin and furanocoumarins, such as bergamottin, dihydroxybergamottin, and bergapten. Their first published clinical report on grapefruit drug interactions was in 1991. The effect of grapefruit juice with regard to drug absorption was originally discovered in 1989 by a group led by pharmacologist David Bailey. Low drug concentrations can also be caused when the fruit suppresses drug absorption from the intestine. Compromising its metabolism lowers concentrations of the active drug, reducing its therapeutic effect, and risking therapeutic failure. Conversely, if the medication is a prodrug, it needs to be metabolised to be converted to the active drug. In the first instance, inhibition of drug-metabolizing enzymes results in elevated concentrations of an active drug in the body, which may cause adverse effects.
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