Summary
CYP1A2 inhibitors are compounds that reduce the activity of the CYP1A2 enzyme, which can reduce drug metabolism, potentially impacting the effects of drug therapy.
CYP1A2 is a cytochrome P450 (CYP) enzyme found mostly in the liver that is involved in the metabolism of any medications that are CYP1A2 substrates; it is perhaps most well-known for its involvement in the metabolism of caffeine.[1] CYP1A2 inhibitors can reduce the body’s metabolism of these substances. CYP1A2 may also play a role in the bioactivation of some carcinogens, like heterocyclic and aromatic amines.[2]
The table below outlines some of the most common or clinically relevant CYP1A2 inhibitors.[3][1][4] Importantly, this list is not exhaustive.
| CYP1A2 Inhibitors |
|---|
| Acyclovir |
| Allopurinol |
| Amiodarone |
| Caffeine |
| Cimetidine |
| Ciprofloxacin |
| Echinacea |
| Ethinyl estradiol (oral contraceptives) |
| Famotidine |
| Fluvoxamine |
| Isoniazid |
| Piperine |
| Propranolol |
| Quercetin |
| Resveratrol |
| Terbinafine |
| Verapamil |
References
- ^Zanger UM, Schwab MCytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.Pharmacol Ther.(2013-Apr)
- ^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)
- ^Hakkola J, Hukkanen J, Turpeinen M, Pelkonen OInhibition and induction of CYP enzymes in humans: an update.Arch Toxicol.(2020-Nov)