Population pharmacokinetics of amlodipine in hypertensive children and adolescents

J Clin Pharmacol. 2006 Aug;46(8):905-16. doi: 10.1177/0091270006289844.

Abstract

A population pharmacokinetic study was conducted in 74 hypertensive children (mean age 10.4 +/- 4.4 years [mean +/- SD]) receiving amlodipine (mean dose 0.17 +/- 0.13 mg/kg/d) chronically. Multiple blood samples were obtained from each subject to characterize amlodipine pharmacokinetics. Plasma amlodipine concentrations were determined by liquid chromatography/mass spectrophotometry with multiple-reaction monitoring detection. Population pharmacokinetic analysis was performed using NONMEM. Amlodipine concentrations were similar in subjects dosed either once or twice daily. Amlodipine pharmacokinetics were well described by a 1-compartment model with first-order absorption and elimination. For a subject at the population median weight (45 kg), predicted apparent clearances (CL/F) were 23.7 L/h for males and 17.6 L/h for females, and the apparent volume of distribution (V/F) was 25.1 L/kg. Dosing frequency did not appear to affect amlodipine concentrations in children. Weight-adjusted CL/F and V/F of amlodipine in younger children were significantly greater than in older children, suggesting a need for higher doses when treating young children with amlodipine.

Publication types

  • Clinical Trial
  • Comparative Study

MeSH terms

  • Adolescent
  • Amlodipine / adverse effects
  • Amlodipine / blood
  • Amlodipine / pharmacokinetics*
  • Amlodipine / therapeutic use
  • Antihypertensive Agents / adverse effects
  • Antihypertensive Agents / blood
  • Antihypertensive Agents / pharmacokinetics*
  • Antihypertensive Agents / therapeutic use
  • Child
  • Child, Preschool
  • Female
  • Humans
  • Hypertension / blood*
  • Hypertension / drug therapy*
  • Infant
  • Male
  • Metabolic Clearance Rate
  • Models, Biological

Substances

  • Antihypertensive Agents
  • Amlodipine