The disposition of oral amodiaquine in Papua New Guinean children with falciparum malaria

Br J Clin Pharmacol. 2005 Mar;59(3):298-301. doi: 10.1111/j.1365-2125.2004.02257.x.

Abstract

Aims: We assessed the disposition of oral amodiaquine (AQ) and CYP2C8 polymorphism in 20 children with falciparum malaria.

Methods: AQ and DEAQ concentrations were determined with SPE-HPLC method. CYP2C8 genotypes were assessed by PCR-RFLP method.

Results: AQ was not detectable beyond day 3 postdose. Cmax for DEAQ was reached in 3.0 days. The mean values for t1/2, MRT, and AUCtotal were 10.1 days, 15.5 days and 4512.6 microg l(-1) day, respectively. All the children were CYP2C8* homozygous.

Conclusion: Our data are consistent with those previously reported, and the AQ regimen seems pharmacokinetically adequate in the absence of CYP2C8 polymorphism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Amodiaquine / administration & dosage
  • Amodiaquine / pharmacokinetics*
  • Antimalarials / administration & dosage
  • Antimalarials / pharmacokinetics*
  • Aryl Hydrocarbon Hydroxylases / genetics
  • Child
  • Child, Preschool
  • Chromatography, High Pressure Liquid
  • Cytochrome P-450 CYP2C8
  • Genotype
  • Humans
  • Infant
  • Malaria, Falciparum / metabolism*
  • Polymerase Chain Reaction / methods
  • Polymorphism, Restriction Fragment Length

Substances

  • Antimalarials
  • Amodiaquine
  • Aryl Hydrocarbon Hydroxylases
  • CYP2C8 protein, human
  • Cytochrome P-450 CYP2C8