What does it mean to be a poor metabolizer of CYP2D6?

What does it mean to be a poor metabolizer of CYP2D6?

A deficiency of the CYP2D6 enzyme is inherited as an autosomal recessive trait; these subjects (7% of Caucasians, about 1% of Orientals) are classified as poor metabolizers. Of these, more than 15 encode an inactive or no enzyme at all. Others encode enzyme with reduced, ‘normal’ or increased enzyme activity.

What does CYP2D6 do in the body?

Cytochrome P450 2D6 (CYP2D6) is part of the cytochrome P450 family of proteins in the body. It is responsible for breaking down many medicines that are commonly used.

What medications are metabolized by CYP2D6?

CYP2D6 metabolizes around 25% of currently prescribed drugs, including various antidepressants, neuroleptics, beta-blockers, opioids, antiemetics, and antiarrhythmics.

How do you know if you’re an ultra-rapid metabolizer?

Contact your doctor immediately if you experience extreme sleepiness, confusion, or shallow breathing. These symptoms may indicate that you are an “ultra-rapid metabolizer of codeine”. As a result, there is too much morphine in the body and more side effects of morphine than usual.

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 happens if you inhibit CYP2D6?

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).

Is Adderall metabolized by CYP2D6?

Amphetamines and amphetamine derivatives are known to be metabolized, to some degree, by cytochrome P450 2D6 (CYP2D6) and display minor inhibition of CYP2D6 metabolism [see CLINICAL PHARMACOLOGY].

Is alcohol metabolized by CYP2D6?

In rat brain, CYP2D is induced by ethanol (Warner and Gustafsson 1994) and in humans, ethanol and tobacco use may alter, or be altered by, CYP2D6 enzyme activity (Llerena et al. 1996; Boustead et al.

What happens if you can’t metabolize something?

Non-Responders: If Your Body Doesn’t Metabolize Drugs As Expected. When you take a pill, your digestive system breaks it down just like food. Your body metabolizes and absorbs it through the bloodstream. Some people metabolize medication differently from the majority of the population.

What is the outcome of having a poor metabolism phenotype?

The poor metabolizer (PM) phenotype occurs when both alleles of either CYP2D6 or CYP2C19 carry inactivating mutations and give rise to synthesis of enzyme with impaired activity or no synthesis of enzyme at all.

What foods inhibit CYP2D6?

Considerable evidence from both in vitro and animal studies suggests that CYP2D6 activity can be inhibited by goldenseal [59, 60], milk thistle [61, 62], kava kava [59, 63-65], Echinacea [59], and St. John’s wort [59, 66-68].

How does the CYP2D6 gene affect drug metabolism?

There are several important variants in the CYP2D6 gene which can cause the enzyme to function differently — either speeding up or slowing down the rate at which medications are broken down. A fast metabolism is usually called an ‘extensive metabolizer’, while slow (or no) enzyme function is called ‘poor metabolizer’.

What is a slow CYP2D6 enzyme?

A fast CYP2D6 enzyme function is usually called an ‘extensive metabolizer’ Slow (or no) enzyme function is referred to as a ‘poor metabolizer’. A variant that slows down the CYP2D6 isn’t always bad.

What are the guidelines for the treatment of CYP2D6 UM?

The Clinical Pharmacogenetics Implementation Consortium (CPIC) recommends that for an individual identified as a CYP2D6 UM, another analgesic should be used to avoid the risk of severe toxicity with a “normal” dose of codeine.

Are there genetic variants of CYP2D6?

There are many genetic variants that impact the function of CYP2D6 causing a wide variety of reactions to some commonly used medications. The CYP2D6 enzyme metabolizes (breaks down) about 25% of pharmaceutical drugs including SSRIs, opioids, tamoxifen, dextromethorphan, and beta-blockers.