Tioconazole is a new imidazole antifungal agent with broad-spectrum activity. Its in vitro activity against common dermal pathogens is generally better than miconazole by a factor of 2-8. This activity is paralleled by good topical efficacy in a guinea pig dermatomycosis model. Pharmacokinetic studies in animals have demonstrated minimal systemic exposure following dermal application. Acute general pharmacology studies have shown that the compound is well tolerated in animals and unlikely to produce side-effects in man.
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Difference in percutaneous absorption and intracutaneous distribution in guinea pigs among topical antifungal drugs (tioconazole solution, tioconazole cream, miconazole nitrate solution and bifonazole solution).
Biol Pharm Bull
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Department of Clinical Pharmacology, Pfizer Global R & D, Tokyo Laboratories, Pfizer Japan Inc., Shinjuku Bunka Quint Bldg., 3-22-7 Yoyogi, Shibuya-ku, Tokyo 151-8589, Japan.
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Drug Metab Dispos
April 1991
Dept. of Drug Metabolism, Pfizer Central Research, Sandwich, U.K.
A comparative study of 1-substituted imidazole and 1,2,4-triazole antifungal compounds as inhibitors of testosterone hydroxylations catalysed by mouse hepatic microsomal cytochromes P-450.
Biochem Pharmacol
December 1988
Biological Laboratory, The University, Canterbury, Kent, U.K.
Three imidazole antifungal agents, ketoconazole, miconazole and tioconazole, and a group of structurally related 1-substituted imidazole and 1,2,4-triazole compounds were evaluated as inhibitors of the oxidative metabolism of testosterone catalysed by mouse hepatic microsomal cytochromes P-450. Spectroscopic studies showed that both imidazoles and triazoles interacted with ferric cytochrome P-450 in hepatic microsomes to produce type II difference spectra which could be distinguished by their different absorbance maxima; 429-430 nm and 425-426 nm respectively. Compound 4, which possesses both types of functional group, produced a spectrum which resembled that of imidazole compounds, indicating that the imidazole moiety had a higher affinity than the triazole for the haem of cytochromes P-450 present in microsomes.
View Article and Find Full Text PDFTioconazole, an imidazole antifungal agent, was administered orally at 100 mg/kg/day to pregnant rats according to two regimens; in one, treatment started on day 15 post-insemination (p.i.) and in the other it started on day 18 p.
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