Pharmacokinetics of imidazole antimycotics

Abstract

Summary According to data on the imidazole antimycotics at present on the market, none of these products satisfactorily fills the gaps which exist in the treatment for mycoses of internal organs, although they have brought considerable progress in the topical treatment of mycoses. On the basis of their very broad spectrum and high intensity of activity under suitable test conditions, and the comparatively tolerable amount of side effects in man, the present imidazole antimycotics are considered to be an encouraging start for future development of derivatives which will lead to products with considerably better pharmacokinetic, and therefore better therapeutic, properties.

Tioconazole, a New Broad-Spectrum Antifungal Agent: Preclinical Studies Related to Vaginal Candidiasis

“…The main effect was a reversible induction of liver microsomal enzymes which is consistent with previous reports on this class of com pound [8][9][10][11]. Tioconazole has no mutagenic, cytogenetic or teratogenic effects.…”

Tioconazole in the Treatment of Fungal Infections of the Skin

“…No de tectable systemic absorption of tioconazole was observed as judged by bioassay of plasma samples (lower limit of sensitivity 0.1 mg). Systemic absorption in volunteers after application to stripped and occluded skin was similar to that reported for other imidazoles [3,4).…”

New class of antifungal agents: jasplakinolide, a cyclodepsipeptide from the marine sponge, Jaspis species

“…A unique attribute of this compound is its ability to kill the fungus at the same concentration as that required to inhibit growth. This is a departure from the activity seen with the imidazole antifungal agents, which are fungicidal only at high concentrations and after prolonged incubation (9,10). The in vitro activity of jasplakinolide is good against all the Candida strains tested except C. tropicalis (Table 1), which is resistant to its action.…”

“…The mechanism of action is primarily fungistatic, with fungicidal activity only at high concentrations and with increased incubation time (9,10). We describe here the in vitro and in vivo activity of jasplakinolide, a novel compound of a new class with fungicidal activity.…”