Summary
CYP2D6 inhibitors are compounds that reduce the activity of the CYP2D6 enzyme, which can reduce drug metabolism, potentially impacting the effects of drug therapy.
CYP2D6 is a cytochrome P450 (CYP) enzyme involved in the metabolism of any medications that are CYP2D6 substrates, which includes many commonly used medications. CYP2D6 inhibitors can reduce the body’s metabolism of these medications. Compared to other drug-metabolizing CYP enzymes, CYP2D6 demonstrates the highest levels of genetic single-nucleotide polymorphism. This results in varying levels of enzyme function across the population, which can influence the safety and effectiveness of some medications.[1]
The table below outlines some of the most common or clinically relevant CYP2D6 inhibitors.[2][3][4] Importantly, this list is not exhaustive.
| CYP2D6 Inhibitors |
|---|
| Aprepitant |
| Bupropion |
| Doxepin |
| Duloxetine |
| Fluoxetine |
| Haloperidol |
| Methadone |
| Mirabegron |
| Paroxetine |
| Quinidine |
| Sertraline |
| Terbinafine |
References
- ^Zhao M, Ma J, Li M, Zhang Y, Jiang B, Zhao X, Huai C, Shen L, Zhang N, He L, Qin SCytochrome P450 Enzymes and Drug Metabolism in Humans.Int J Mol Sci.(2021-Nov-26)
- ^Song Y, Li C, Liu G, Liu R, Chen Y, Li W, Cao Z, Zhao B, Lu C, Liu YDrug-Metabolizing Cytochrome P450 Enzymes Have Multifarious Influences on Treatment Outcomes.Clin Pharmacokinet.(2021-May)
- ^Zanger UM, Schwab MCytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.Pharmacol Ther.(2013-Apr)
- ^Hakkola J, Hukkanen J, Turpeinen M, Pelkonen OInhibition and induction of CYP enzymes in humans: an update.Arch Toxicol.(2020-Nov)