Designer drugs that are potent inhibitors of CYP2D6
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-p...
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| Veröffentlicht in: | Journal of clinical psychopharmacology 2002-06, Vol.22 (3), p.330-332 |
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| container_issue | 3 |
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| container_title | Journal of clinical psychopharmacology |
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| creator | PRITZKER, David KANUNGO, Anish KILICARSLAN, Tansel TYNDALE, Rachel F SELLERS, Edward M |
| description | 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. |
| doi_str_mv | 10.1097/00004714-200206000-00015 |
| format | Article |
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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. 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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.</description><subject>Biological and medical sciences</subject><subject>Cytochrome P-450 CYP2D6 - metabolism</subject><subject>Cytochrome P-450 CYP2D6 Inhibitors</subject><subject>Designer Drugs - pharmacokinetics</subject><subject>Designer Drugs - pharmacology</subject><subject>Drug addictions</subject><subject>Enzyme Inhibitors - pharmacokinetics</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - enzymology</subject><subject>Toxicology</subject><issn>0271-0749</issn><issn>1533-712X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkMFOwzAMhiMEYmPwCigXjoE4bpL2iDYGSJPgsAOcqiRNt6KtnZLuwNuTscIsW7al77fknxAK_B54oR94ikxDxgTngqu0sVQgz8gYJCLTID7OyZgLDYzrrBiRqxi_EpFpIS_JCJJOFVyOCc58bFatD7QK-1Wk_dr01ARPd13v25427bqxTd-FSLuaTj_fxUxdk4vabKK_GfqELOdPy-kLW7w9v04fF8xhBj3DQuYFKKklVhJyYWoEjyb3h7lKk0FnAQtutZECuFTOCi9qsGgdVzgh-fGsC12MwdflLjRbE75L4OXBhvLPhvLfhvLXhiS9PUp3e7v11Uk4_J2AuwEw0ZlNHUzrmnjiUOkMU_4A4A5ivw</recordid><startdate>20020601</startdate><enddate>20020601</enddate><creator>PRITZKER, David</creator><creator>KANUNGO, Anish</creator><creator>KILICARSLAN, Tansel</creator><creator>TYNDALE, Rachel F</creator><creator>SELLERS, Edward M</creator><general>Lippincott Williams & Wilkins</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20020601</creationdate><title>Designer drugs that are potent inhibitors of CYP2D6</title><author>PRITZKER, David ; KANUNGO, Anish ; KILICARSLAN, Tansel ; TYNDALE, Rachel F ; SELLERS, Edward M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c341t-39589165753d5182af31e3a8e182ade3aa3cb1390b7a521056cb2e2f1b3bc063</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Biological and medical sciences</topic><topic>Cytochrome P-450 CYP2D6 - metabolism</topic><topic>Cytochrome P-450 CYP2D6 Inhibitors</topic><topic>Designer Drugs - pharmacokinetics</topic><topic>Designer Drugs - pharmacology</topic><topic>Drug addictions</topic><topic>Enzyme Inhibitors - pharmacokinetics</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Microsomes, Liver - drug effects</topic><topic>Microsomes, Liver - enzymology</topic><topic>Toxicology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>PRITZKER, David</creatorcontrib><creatorcontrib>KANUNGO, Anish</creatorcontrib><creatorcontrib>KILICARSLAN, Tansel</creatorcontrib><creatorcontrib>TYNDALE, Rachel F</creatorcontrib><creatorcontrib>SELLERS, Edward M</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Journal of clinical psychopharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>PRITZKER, David</au><au>KANUNGO, Anish</au><au>KILICARSLAN, Tansel</au><au>TYNDALE, Rachel F</au><au>SELLERS, Edward M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Designer drugs that are potent inhibitors of CYP2D6</atitle><jtitle>Journal of clinical psychopharmacology</jtitle><addtitle>J Clin Psychopharmacol</addtitle><date>2002-06-01</date><risdate>2002</risdate><volume>22</volume><issue>3</issue><spage>330</spage><epage>332</epage><pages>330-332</pages><issn>0271-0749</issn><eissn>1533-712X</eissn><coden>JCPYDR</coden><abstract>Some abused drugs are substrates of CYP2D6 (e.g., paramethoxyamphetamine, methylenedioxy-methamphetamine). 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| ispartof | Journal of clinical psychopharmacology, 2002-06, Vol.22 (3), p.330-332 |
| issn | 0271-0749 1533-712X |
| language | eng |
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| source | MEDLINE; Journals@Ovid Complete |
| subjects | Biological and medical sciences Cytochrome P-450 CYP2D6 - metabolism Cytochrome P-450 CYP2D6 Inhibitors Designer Drugs - pharmacokinetics Designer Drugs - pharmacology Drug addictions Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Humans Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - enzymology Toxicology |
| title | Designer drugs that are potent inhibitors of CYP2D6 |
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