Toxicokinetics of amphetamines: metabolism and toxicokinetic data of designer drugs, amphetamine, methamphetamine, and their N-alkyl derivatives

Ther Drug Monit. 2002 Apr;24(2):277-89. doi: 10.1097/00007691-200204000-00009.


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.

Publication types

  • Review

MeSH terms

  • Amphetamines / chemistry
  • Amphetamines / metabolism
  • Amphetamines / pharmacokinetics*
  • Designer Drugs / chemistry
  • Designer Drugs / metabolism
  • Designer Drugs / pharmacokinetics*
  • Forensic Medicine / methods*
  • Humans
  • Methamphetamine / chemistry
  • Methamphetamine / metabolism
  • Methamphetamine / pharmacokinetics


  • Amphetamines
  • Designer Drugs
  • Methamphetamine