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Toxicokinetics of Amphetamines: Metabolism and Toxicokinetic Data of Designer Drugs, Amphetamine, Methamphetamine, and Their N-Alkyl Derivatives

Thomas Kræmer, Hans H Maurer

Therapeutic Drug Monitoring April 1, 2002 DOI: 10.1097/00007691-200204000-00009 (opens in new tab)

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AI-extracted from the abstract
Characteristics Review Peer reviewed
Topics MDMA
Keywords Toxicokinetics Methamphetamine Designer drug Pharmacology Benzphetamine Pharmacokinetics Cytochrome p450
Citations 232
Key findings Amphetamine-like designer drugs and N-alkylated derivatives are metabolized by cytochrome P450 isoenzymes, with many acting as prodrugs that yield active amphetamine or methamphetamine, which has implications for forensic toxicology.

Abstract

This paper reviews the toxicokinetics of amphetamines. The designer drugs MDA (methylenedioxy-amphetamine, R,S-1-(3;,4;-methylenedioxyphenyl)2-propanamine), MDMA (R,S-methylenedioxymethamphetamine), and MDE (R,S-methylenedioxyethylamphetamine), as well as BDB (benzodioxolylbutanamine; R,S-1-(1;,3;-benzodioxol-5;-yl)-2-butanamine or R,S-1-(3;,4;-methylenedioxyphenyl)-2-butanamine) and MBDB (R,S-N-methyl-benzodioxolylbutanamine), were taken into consideration, as were the following N-alkylated amphetamine derivatives: amphetaminil, benzphetamine, clobenzorex, dimethylamphetamine, ethylamphetamine, famprofazone, fencamine, fenethylline, fenproporex, furfenorex, mefenorex, mesocarb, methamphetamine, prenylamine, and selegiline. English-language publications from 1995 to 2000 were reviewed. Papers describing identification of metabolites or cytochrome P450 isoenzyme-dependent metabolism and papers containing pharmacokinetic/toxicokinetic data were considered and summarized. The implications of toxicokinetics for toxicologic assessment or for interpretation in forensic cases are discussed.

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