Life

Is Adderall metabolized by CYP2D6?

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].

What enzyme metabolizes stimulants?

In vitro human studies show that the metabolism of most amphetamine-like psychostimulants is regulated by the polymorphic cytochrome P450 isozyme CYP2D6.

What is the function of CYP2D6?

In particular, CYP2D6 is responsible for the metabolism and elimination of approximately 25\% of clinically used drugs, via the addition or removal of certain functional groups – specifically, hydroxylation, demethylation, and dealkylation. CYP2D6 also activates some prodrugs.

How does enzyme induction affects drug metabolism?

Enzyme induction refers to an increase in the rate of hepatic metabolism, mediated by increased transcription of mRNA encoding the genes for drug-metabolizing enzymes. This leads to a decrease in the concentrations of drugs metabolized by the same enzyme.

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What happens if a drug is not metabolized?

If your body metabolizes a drug too slowly, it stays active longer, and may be associated with side effects. Because of this, your doctor may characterize you as being one of four metabolizer types, with respect to a specific enzyme. Poor metabolizers have significantly reduced or non-functional enzyme activity.

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 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).

Can CYP2D6 be induced?

Thus, our data suggest that CYP2D6 may be induced in pregnancy owing to the elevated cortisol concentration present in the plasma. Others have suggested that CYP2D6 is induced in pregnant CYP2D6-humanized mice as a result of elevated hepatic concentrations of all-trans retinoic acid (Koh et al., 2014).