what drugs are metabolized by cyp2d6

Primary outcome was the prevalence of patients using at least one drug metabolized by CYP2D6. Drugs metabolised by CYP2D6. What is CYP2D6? 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. Ultrarapid metabolizers (UMs), up to 7% of Caucasians, require more than average doses of drugs metabolized by CYP2D6 to reach therapeutic plasma concentrations . 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. CYP2D6 is responsible for the metabolism of the second highest number of drugs metabolized by P450 enzymes. A small percentage of the population has inactive CYP2D6 enzymes, that cannot metabolize any CYP2D6 substrates, (medications, or foods, whatever). These substrates compete with hydrocodone and oxycodone for the ability to bind with available 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. The other side of the range of metabolic capacity is ultrarapid drug metabolism, a result of excessively high CYP2D6 enzyme activity. These are enzymes that eliminate most of the drugs and toxins from the human body . It is responsible for the metabolism and elimination of approximately 25% of clinically used drugs, in a process referred to as O-demethylation. Genetic Variant Information. It is not unusual to identify 10 different metabolites of a single drug in blood or urine. Drug-drug interactions can have a significant impact on CYP2D6-facilitated metabolism (Table 1). Function. CYP2D6 acts on 25% of all prescription drugs. CYP2D6 is a member of the cytochrome P450 family of enzymes involved in the oxidative metabolism of drugs. It’s found in the liver and the brain . Substrates for CYP2D6 can be found in Table 3.1 . CYP2D6 gene encoded in humans for the enzyme Cytochrome P450 2D6.It is expressed in the liver and in areas of CNS. (4) "The CYP2D6 genetic test is used to predict how you will respond to a large number of different medications." Source: Mayo Clinic. Read more about CYPs here. 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. 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 … Background Information for CYP2D6: Characteristics: The cytochrome P450 (CYP) isozyme 2D6 is involved in the metabolism of many drugs. Drugs can have multiple sites of metabolism, and the metabolites themselves can also undergo secondary metabolism. The prevalence of patients using at least one CYP2D6 substrate in different populations was compared with the general population using chi(2) statistics. Although it accounts for only 2-5 % of the liver CYPs, CYP2D6 metabolizes 25% of all drugs [3, 4, 5]. [33] Approximately 4-7% of the population has a slow acting form of this enzyme and 3% a super-fast acting form. From every population, 150 adults using at least one drug were randomly selected. CYP2D6 is a particularly challenging enzyme to understand and study because of its genetic polymorphism. The CYP2D6 (sounds like “sip-2-dee-6”) gene encodes an enzyme that is involved in the metabolism of fluvoxamine. There are different CYP2D6 gene versions, or variants, and each has a different effect on how well fluvoxamine is metabolized in the body. 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