Ultrarapid metabolizers (UMs), up to 7% of Caucasians, require more than average doses of drugs metabolized by CYP2D6 to reach therapeutic plasma concentrations . 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. What is CYP2D6? Primary outcome was the prevalence of patients using at least one drug metabolized 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. Drugs metabolised by CYP2D6. CYP2D6 is a member of the cytochrome P450 family of enzymes involved in the oxidative metabolism of drugs. 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. These substrates compete with hydrocodone and oxycodone for the ability to bind with available CYP2D6. Source: Mayo Clinic. It is not unusual to identify 10 different metabolites of a single drug in blood or urine. Read more about CYPs here. It’s found in the liver and the brain . CYP2D6 is a particularly challenging enzyme to understand and study because of its genetic polymorphism. CYP2D6 is responsible for the metabolism of the second highest number of drugs metabolized by P450 enzymes. From every population, 150 adults using at least one drug were randomly selected. Drug-drug interactions can have a significant impact on CYP2D6-facilitated metabolism (Table 1). 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. CYP2D6 acts on 25% of all prescription drugs. CYP2D6 metabolizes not just hydrocodone and oxycodone, but also anti-nausea medications (Zofran®), tricyclic antidepressants, and other opioids. [33] Approximately 4-7% of the population has a slow acting form of this enzyme and 3% a super-fast acting form. Substrates for CYP2D6 can be found in Table 3.1 . 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 . A small percentage of the population has inactive CYP2D6 enzymes, that cannot metabolize any CYP2D6 substrates, (medications, or foods, whatever). Although it accounts for only 2-5 % of the liver CYPs, CYP2D6 metabolizes 25% of all drugs [3, 4, 5]. There are different CYP2D6 gene versions, or variants, and each has a different effect on how well fluvoxamine is metabolized in the body. (4) "The CYP2D6 genetic test is used to predict how you will respond to a large number of different medications." 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. Function. 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. CYP2D6 gene encoded in humans for the enzyme Cytochrome P450 2D6.It is expressed in the liver and in areas of CNS. 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