What does CYP2D6 do in the human body?

What does CYP2D6 do in the human body?

CYP2D6 is involved in the metabolism of many CNS drugs such as antidepressants, antipsychotics and opioids, as well as in the metabolism of endogenous neuroactive substrates (i.e. neuroactive monoamines, endocannabinoids and endomorphines).

What drugs are metabolised by CYP2D6?

Multiple tricyclic antidepressants, β blockers, haloperidol, sertraline, paroxetine, and thioridazine are among the common drugs metabolized by CYP2D6.

What is hepatic enzyme CYP2D6 metabolism?

Cytochrome P450 2D6 (CYP2D6) is an enzyme involved in the metabolism of many drugs active in the central nervous system, such as antidepressants, antipsychotics and central opioids. 1. This enzyme is coded by a polymorphic gene, with 7% of the Caucasian population showing no enzymatic activity (‘poor metabolizers’).

What percent of drugs are metabolized by CYP2D6?

25%
CYP2D6 is a major gene member of this superfamily as it carries out metabolism of 25% of drugs currently available in the market.

What is the role of the CYP2D6 in the drugs metabolism in general?

Cytochrome P450 CYP2D6 is the most extensively characterized polymorphic drug-metabolizing enzyme. The CYP2D6 enzyme catalyses the metabolism of a large number of clinically important drugs including antidepressants, neuroleptics, some antiarrhythmics, lipophilic β-adrenoceptor blockers and opioids.

What drugs are metabolized by UGT1A4?

The UGT1A4 enzyme mediates the metabolism of important psychotropic medications, including some tricyclic antidepressants, antipsychotics, and mood stabilizers1–20. Therefore, genetic polymorphisms in this gene may have pharmacological importance.

What does the CYP2D6 * 10 allele do?

The CYP2D6*10 “C100T” mutation in patients leads to reduced enzyme activity and decrease of appropriate response to drug treatments, such as tamoxifen, codeine, antidepressants, and antipsychotics.

What happens when a CYP2D6 substrate is taken with a CYP2D6 inhibitor?

For those drugs that are metabolized by CYP2D6 to inactive metabolites, CYP2D6 inhibitors may result in toxicity. For drugs that are converted to active metabolites by CYP2D6, the addition of a CYP2D6 inhibitor will tend to inhibit the efficacy of the drug.

What is the importance of CYP2D6?

The CYP2D6 gene encodes an enzyme important in the metabolism of many commonly used medications. Variation in CYP2D6 is associated with inter-individual differences in medication response, and genetic testing is used to optimize medication therapy.

What does a CYP2D6 inhibitor do?

CYP2D6 Inhibitors Drugs that inhibit CYP2D6 activity are likely to increase the plasma concentrations of certain medications, and, in some cases, adverse outcomes will occur (see Table 3 below right for a list of known inhibitors).

What does ultrarapid metabolizer mean?

Ultrarapid Metabolizer (UM) – This means there are two copies of a CYP2C19 gene with increased activity. This results in very high CYP2C19 activity. About 5 out of 100 people have this gene status. Certain drugs should be used with caution and patients may need to have their doses of some medications adjusted.

Why is CYP1A2 important?

CYP1A2 has been shown to be important for dosing of several antipsychotics and for assessing both drug efficacy and adverse drug reactions. CYP1A2 is the main CYP isoform involved in clozapine metabolism [16]. This is likely by induction of CYP1A2, causing it to play a larger role in the generation of active drugs.