Toxicokinetics of Amphetamines: Metabolism and Toxicokinetic Data of Designer Drugs, Amphetamine, Methamphetamine, and Their N-Alkyl Derivatives
Therapeutic Drug Monitoring – April 01, 2002
Source: OpenAlex
Summary
Amphetamines, including designer drugs like MDMA and MDA, have complex toxicokinetics that significantly impact forensic toxicology. A review of English-language publications from 1995 to 2000 analyzed over 100 studies, focusing on the metabolism of various amphetamine derivatives through cytochrome P450 enzymes. Key findings highlighted that up to 80% of identified metabolites influence neurotransmitter receptor behavior, crucial for understanding drug effects. These insights are vital for toxicologic assessments and interpreting forensic cases involving these substances, underscoring their diverse pharmacological profiles.
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.