Pharmacokinetics of dapsone administered daily and weekly in human immunodeficiency virus-infected children

Antimicrob Agents Chemother. 1999 Nov;43(11):2586-91. doi: 10.1128/AAC.43.11.2586.

Abstract

Although dapsone is a commonly used alternative agent for prophylaxis against Pneumocystis carinii pneumonia in children intolerant to trimethoprim-sulfamethoxazole, there are few data that describe dapsone pharmacokinetics in children. We studied dapsone pharmacokinetics in 30 children (median age, 2.8 years; age range, 0. 3 to 12 years) receiving a new proprietary liquid preparation by three dosing regimens (1 mg/kg of body weight daily, 2 mg/kg daily, or 4 mg/kg weekly). Dosing of children with 2 mg/kg daily or 4 mg/kg weekly resulted in peak concentrations equivalent to those reached in adults receiving 100-mg tablets daily. For the entire population, the median half-life was 22.2 h (range, 7.1 to 40.3 h), the median oral clearance was 0.0365 liter/kg/h (range, 0.0104 to 0.1021 liter/kg/h), and the median oral apparent volume of distribution was 1.13 liters/kg (range, 0.50 to 2.32 liters/kg). The median dapsone oral clearance was significantly increased in those infants less than 2 years of age compared to the oral clearance in those over 2 years of age (0.0484 versus 0.0278 liter/kg/h; P = 0.011). These data suggest that absorption of this liquid preparation is adequate and that the concentrations in the sera of children receiving 2 mg/kg daily or 4 mg/kg weekly are equivalent to those seen in adults receiving standard dapsone dosing. Dapsone oral clearance appears to be increased in children under 2 years of age.

Publication types

  • Clinical Trial
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adolescent
  • Anti-Infective Agents / blood
  • Anti-Infective Agents / pharmacokinetics*
  • Anti-Infective Agents / therapeutic use
  • Child
  • Child, Preschool
  • Chromatography, High Pressure Liquid
  • Dapsone / blood
  • Dapsone / pharmacokinetics*
  • Dapsone / therapeutic use
  • Female
  • HIV Infections / metabolism*
  • Humans
  • Infant
  • Male
  • Pneumonia, Pneumocystis / prevention & control

Substances

  • Anti-Infective Agents
  • Dapsone