Designer drugs that are potent inhibitors of CYP2D6.

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Pritzker D, Kanungo A, Kilicarslan T, Tyndale RF, Sellers EM

Designer drugs that are potent inhibitors of CYP2D6.

J Clin Psychopharmacol. 2002 Jun;22(3):330-2. doi: 10.1097/00004714-200206000-00015.

PubMed ID

12006905 [ View in PubMed

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Abstract

Some abused drugs are substrates of CYP2D6 (e.g., paramethoxyamphetamine, methylenedioxy-methamphetamine). CYP2D6 inhibition by concurrently used drugs of abuse could potentiate such drugs and increase acute toxicity. Ten designer drugs were tested as inhibitors of CYP2D6. Only 1-methyl-4-phenyl-4-propionoxypiperidine (MPPP) and 1-[2-phenylethyl]-4-phenyl-4-acetoxypiperidine (PEPAP) interacted significantly (Ki 1.6 microM and 0.3 microM, respectively). Both are synthetic analogues of meperidine sold as "synthetic heroin." No CYP2D6-mediated metabolites were detected for either compound. Concurrent oral use of CYP2D6 substrates with MPPP and PEPAP may represent a kinetic drug interaction risk, but this risk must be confirmed clinically.

DrugBank Data that Cites this Article

Drugs

1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine	Cytochrome P450 2D6	Protein	Humans	Unknown	Inhibitor	Details