Pharmacokinetics of aditoprim in goats using a radioassay

M. Perwaiz Iqbal, N. Mahboobali, Sarfaraz K. Niazi, M. Anwar Mahmood

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


A simple, highly sensitive radioassay was developed for the activity of a newly discovered inhibitor of dihydrofolate reductase (DHFR), aditoprim. The procedure is based on the inhibition of binding of [3H]‐methotrexate ([3H]MTX) with bacterial dihydrofolate reductase by the antifolate, aditoprim. The analytic sensitivity using this binding inhibition method was less than 5 ng in plasma. The procedure developed requires no extraction of the drug from the plasma. The variation of simultaneous duplicate determinations was 6·3 per cent, whereas the variability of plasma samples assayed on different days was less than 11 per cent. The assay developed was applied to study the pharmacokinetics of aditoprim in the goat. In comparison with trimethoprim (TMP), the new inhibitor of DHFR, aditoprim, had a longer half‐life and a larger volume of distribution, suggesting enhanced and prolonged antibacterial activity of aditoprim over TMP.

Original languageEnglish
Pages (from-to)533-541
Number of pages9
JournalBiopharmaceutics and Drug Disposition
Issue number6
Publication statusPublished - 1990


  • Aditoprim
  • Goat
  • Pharmacokinetics
  • Radioassay
  • Trimethoprim


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