Single-dose pharmacokinetics of methylphenidate in CYP2D6 extensive and poor metabolizers

J Clin Psychopharmacol. 2000 Jun;20(3):347-9. doi: 10.1097/00004714-200006000-00009.

Abstract

Six adults phenotyped as either extensive (N = 4) or poor (N = 2) metabolizers for cytochrome P450 (CYP) 2D6 were given a 10-mg oral dose of methylphenidate (MPH) on two separate occasions with and without quinidine, a potent CYP2D6 inhibitor. Quinidine had no significant effect on the pharmacokinetics of either MPH or ritalinic acid, its major metabolite, in either group of CYP2D6 metabolizers. These data suggest a lack of involvement of CYP2D6 in the metabolism of MPH. Drugs that are inhibitors of CYP2D6 when taken concurrently with MPH should not affect its plasma concentration.

Publication types

  • Clinical Trial

MeSH terms

  • Adolescent
  • Adult
  • Area Under Curve
  • Central Nervous System Stimulants / pharmacokinetics*
  • Chromatography, Liquid
  • Cytochrome P-450 CYP2D6 / genetics
  • Cytochrome P-450 CYP2D6 / metabolism*
  • Cytochrome P-450 CYP2D6 Inhibitors
  • Enzyme Inhibitors / pharmacology
  • Female
  • Half-Life
  • Humans
  • Male
  • Mass Spectrometry
  • Methylphenidate / analogs & derivatives
  • Methylphenidate / blood
  • Methylphenidate / pharmacokinetics*
  • Middle Aged
  • Phenotype
  • Polymorphism, Genetic
  • Quinidine / antagonists & inhibitors

Substances

  • Central Nervous System Stimulants
  • Cytochrome P-450 CYP2D6 Inhibitors
  • Enzyme Inhibitors
  • Methylphenidate
  • Cytochrome P-450 CYP2D6
  • ritalinic acid
  • Quinidine