what drugs are metabolized by cyp2d6

CYP2D6 is a particularly challenging enzyme to understand and study because of its genetic polymorphism. Ultrarapid metabolizers (UMs), up to 7% of Caucasians, require more than average doses of drugs metabolized by CYP2D6 to reach therapeutic plasma concentrations . They may respond partially when the drug is metabolized by a number of different enzymes, and sometimes in these situations the other enzymes can compensate to some degree for the inactive CYP2D6. A small percentage of the population has inactive CYP2D6 enzymes, that cannot metabolize any CYP2D6 substrates, (medications, or foods, whatever). CYP2D6 gene encoded in humans for the enzyme Cytochrome P450 2D6.It is expressed in the liver and in areas of CNS. Read more about CYPs here. CYP2D6 is responsible for the metabolism of the second highest number of drugs metabolized by P450 enzymes. Primary outcome was the prevalence of patients using at least one drug metabolized by CYP2D6. About 35% of the population are carriers of a non-functional CYP2D6 allele, which especially elevates the risk of adverse drug events (ADEs) when these individuals are taking multiple drugs. CYP2D6 is a member of the cytochrome P450 family of enzymes involved in the oxidative metabolism of drugs. (4) "The CYP2D6 genetic test is used to predict how you will respond to a large number of different medications." CYP2D6 is among the most promiscuous of these enzymes, involved in the metabolism of approximately 20% of drugs in clinical use, and displays large individual-to-individual variability in activity due to genetic polymorphisms. These substrates compete with hydrocodone and oxycodone for the ability to bind with available CYP2D6. Drugs can have multiple sites of metabolism, and the metabolites themselves can also undergo secondary metabolism. The CYP2D6 (sounds like “sip-2-dee-6”) gene encodes an enzyme that is involved in the metabolism of fluvoxamine. The prevalence of patients using at least one CYP2D6 substrate in different populations was compared with the general population using chi(2) statistics. These are enzymes that eliminate most of the drugs and toxins from the human body . Although it accounts for only 2-5 % of the liver CYPs, CYP2D6 metabolizes 25% of all drugs [3, 4, 5]. CYP2D6 metabolizes not just hydrocodone and oxycodone, but also anti-nausea medications (Zofran®), tricyclic antidepressants, and other opioids. There are different CYP2D6 gene versions, or variants, and each has a different effect on how well fluvoxamine is metabolized in the body. [33] Approximately 4-7% of the population has a slow acting form of this enzyme and 3% a super-fast acting form. Drugs metabolised by CYP2D6. Variants in the gene that code for CYP2D6 may influence pharmacokinetics of CYP2D6 substrates, and may predict or explain non-standard dose requirement, therapeutic failure or adverse reactions. Drug-drug interactions can have a significant impact on CYP2D6-facilitated metabolism (Table 1). It is responsible for the metabolism and elimination of approximately 25% of clinically used drugs, in a process referred to as O-demethylation. CYP2D6 acts on 25% of all prescription drugs. What is CYP2D6? It’s found in the liver and the brain . Drugs may be metabolized by only one CYP450 enzyme (e.g., metoprolol by CYP2D6) or by multiple enzymes (e.g., warfarin [Coumadin] by CYP1A2, CYP2D6, and CYP3A4).13 Drugs … Genetic Variant Information. From every population, 150 adults using at least one drug were randomly selected. It is not unusual to identify 10 different metabolites of a single drug in blood or urine. CYP2D6 is one of the cytochrome P450 monooxygenases (CYPs). Background Information for CYP2D6: Characteristics: The cytochrome P450 (CYP) isozyme 2D6 is involved in the metabolism of many drugs. Source: Mayo Clinic. Function. Substrates for CYP2D6 can be found in Table 3.1 . 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