European Journal of Clinical Pharmacology

, Volume 24, Issue 2, pp 267–271 | Cite as

Clinical effect and pharmacokinetics of trimethoprim-sulphadiazine in children with urinary tract infections

  • J. Aarbakke
  • O. Opshaug
  • A. Digranes
  • A. Høylandskjær
  • G. Fluge
  • H. Fellner


The clinical effect and pharmacokinetics of the combination trimethoprim (TMP)-sulphadiazine (SD) were studied in 18 children with acute urinary tract infections (UTI), aged 2–56 months. A suspension of TMP-SD (9+41 mg/ml) was taken orally twice daily for 10 days. Various doses of TMP (2.9–3.7 mg/kg/day) and SD (12.9–16.7 mg/kg/day) were also given to children of different ages. After 2–4 days of treatment, bacterial cultures of urine were negative and C-reactive protein in serum, WBC count and ESR in all patients had become normal. Steady state serum levels for both components were reached after 4 or more days of treatment. At steady state, mean peak serum concentrations of TMP and SD of 1.4 µg/ml and 27 µg/ml, respectively, were found within 2–4 h after a fasting morning dose. The biological half-lives of TMP and SD were of the same order of magnitude, but the total clearance of TMP was 5 times greater than that of SD. The concentrations of TMP-SD in urine were invariably more than 10 times the minimum inhibitory concentrations (MIC) for the causative organisms (tested at the ratios 1:20 and 1:4 of TMP and SD). Non-metabolized SD constituted 77% of total SD in urine of infants, and 55% of total SD in children of 1 year or more. The TMP-SD combination showed a satisfactory clinical effect and favourable pharmacokinetic properties in children with UTI.

Key words

trimethoprim sulphadiazine urinary tract infection children pharmacokinetics urinary concentrations 


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Copyright information

© Springer-Verlag 1983

Authors and Affiliations

  • J. Aarbakke
    • 1
  • O. Opshaug
    • 2
  • A. Digranes
    • 3
  • A. Høylandskjær
    • 1
  • G. Fluge
    • 2
  • H. Fellner
    • 4
  1. 1.Department of Pharmacology, Gade InstituteUniversity of BergenBergenNorway
  2. 2.Department of Pediatrics, Gade InstituteUniversity of BergenBergenNorway
  3. 3.Department of Microbiology and Immunology, Gade InstituteUniversity of BergenBergenNorway
  4. 4.AB AstraSødertäljeSweden

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