Absence of an active metabolite for the triazole antifungal pramiconazole

Jannie Ausma, Gennethel Pennick, Hilde Bohets, Vera Van De Velde, Marcel Borgers, Annette Fothergill

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

Pramiconazole is an antifungal with high potential for the treatment of dermatophyte and yeast infections of the skin. It is currently not known whether pramiconazole is active alone as the parent agent or assisted by active metabolites. The in vitro metabolism as well as the metabolic stability of pramiconazole was investigated in subcellular liver fractions and isolated hepatocytes of several species. Results indicate that the metabolism of pramiconazole was slow, since the enzyme-mediated disappearance of pramiconazole was rather slow. To investigate whether pramiconazole was converted into an active metabolite in humans, serum samples from healthy volunteers receiving a daily dose of 100 or 200 mg pramiconazole for one week were assayed with an agar diffusion bioassay and liquid chromatography-tandem mass spectrometry. It was concluded that there was no active metabolite present in serum samples from healthy volunteers after oral dosing of pramiconazole.

Original languageEnglish (US)
Pages (from-to)22-26
Number of pages5
JournalActa Dermato-Venereologica
Volume87
Issue number1
DOIs
StatePublished - Feb 14 2007

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Keywords

  • Dermatophyte
  • Inhibition zone bioassay
  • Metabolism
  • R126638
  • Yeast

ASJC Scopus subject areas

  • Dermatology

Cite this

Ausma, J., Pennick, G., Bohets, H., Van De Velde, V., Borgers, M., & Fothergill, A. (2007). Absence of an active metabolite for the triazole antifungal pramiconazole. Acta Dermato-Venereologica, 87(1), 22-26. https://doi.org/10.2340/00015555-0179