Pharmacokinetics of co-trimazine after single and multiple doses

N. Leone, N. Barzaghi, M. Monteleone, E. Perucca, R. Cerutti, A. Crema

Research output: Contribution to journalArticle

Abstract

Plasma and urinary levels of trimethoprim (TMP), sulfadiazine (SDZ) and N4-acetylsulfadiazine (N4-SDZ) were determined after administration of 1 g cotrimazine (equivalent to 180 mg TMP and 820 mg SDZ) (Kombinax®) as a single dose and again once daily for 7 days to 6 normal subjects. Both TMP and SDZ were rapidly absorbed from the gastrointestinal tract with peak plasma levels being achieved within 4 h in all subjects. Elimination half-lives ranged from 8 to 13 h for TMP and from 9 to 15 h for SDZ. Approximately 50% of the administered dose of SDZ was recovered in urine within 24 h of the single dose (32% as unchanged drug and 17% as the N4-acetyl-metabolite). For TMP, the urinary recovery during the 24 h following the single dose averaged 39%. Mean plasma levels of TMP, SDZ and N4-SDZ at steady state were moderately higher than those observed after a single dose, but no change in absorption or disposition kinetics of these compounds was seen after repeated dosing.

Original languageEnglish
Pages (from-to)70-74
Number of pages5
JournalArzneimittel-Forschung/Drug Research
Volume37
Issue number1
Publication statusPublished - 1987

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Sulfadiazine
Trimethoprim
Pharmacokinetics
Plasmas
Metabolites
Gastrointestinal Tract
Urine
Recovery
Kinetics
Pharmaceutical Preparations
trimethoprim drug combination sulfadiazine

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Pharmacology

Cite this

Leone, N., Barzaghi, N., Monteleone, M., Perucca, E., Cerutti, R., & Crema, A. (1987). Pharmacokinetics of co-trimazine after single and multiple doses. Arzneimittel-Forschung/Drug Research, 37(1), 70-74.

Pharmacokinetics of co-trimazine after single and multiple doses. / Leone, N.; Barzaghi, N.; Monteleone, M.; Perucca, E.; Cerutti, R.; Crema, A.

In: Arzneimittel-Forschung/Drug Research, Vol. 37, No. 1, 1987, p. 70-74.

Research output: Contribution to journalArticle

Leone, N, Barzaghi, N, Monteleone, M, Perucca, E, Cerutti, R & Crema, A 1987, 'Pharmacokinetics of co-trimazine after single and multiple doses', Arzneimittel-Forschung/Drug Research, vol. 37, no. 1, pp. 70-74.
Leone N, Barzaghi N, Monteleone M, Perucca E, Cerutti R, Crema A. Pharmacokinetics of co-trimazine after single and multiple doses. Arzneimittel-Forschung/Drug Research. 1987;37(1):70-74.
Leone, N. ; Barzaghi, N. ; Monteleone, M. ; Perucca, E. ; Cerutti, R. ; Crema, A. / Pharmacokinetics of co-trimazine after single and multiple doses. In: Arzneimittel-Forschung/Drug Research. 1987 ; Vol. 37, No. 1. pp. 70-74.
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