In vitro and in vivo studies with flutrimazole, a new imidazole derivative with antifungal activity.

1-[(2-Fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H-imidazole (flutrimazole, UR-4056, CAS 119006-77-8) is a new topical imidazole antifungal agent which displays potent broad-spectrum in vitro activity against dermatophytes, filamentous fungi and yeasts, saprophytic and pathogenic to animals and humans (MIC = 0.025-5.0 micrograms/ml). In most of these studies the activity of flutrimazole was comparable to that of clotrimazole and markedly higher than that of bifonazole (MIC differences of greater than or equal to 1 order of magnitude). Tested against Scopulariopsis brevicaulis (8 strains), both flutrimazole and clotrimazole exhibited fungistatic and fungicidal activity, and clotrimazole appeared something less active (MIC = 0.3-2.5 micrograms/ml) than flutrimazole (MIC = 0.15-0.6 micrograms/ml). In animal experiments, topical application of 1% and 2% flutrimazole, as a cream or solution, was highly effective in models of rat vaginal candidiasis and guinea-pig trichophytosis, giving a rate of cured or cured plus markedly improved animals higher than 80%. Flutrimazole shares the mode of action of other imidazole or triazole-containing antifungals, i.e. inhibition of fungal lanosterol 14 alpha-demethylase, as it strongly inhibits ergosterol biosynthesis in a cell-free homogenate of Candida albicans, with an IC50 value of 0.071 mumol/l.

Incidence of dermatophytoses in rabbit farms in Catalonia, Spain, and its repercussion on human health.

Over the past decades there has been an important increase in the incidence of dermatophytoses in humans as a result of contact with animals, although etiological agents can vary as can the animals transmitting the disease. A large-scale study was carried out in 220 farms raising rabbits for consumption. Most of the farms (85%) were located in the autonomous community of Catalonia (Spain). Mycological studies showed that 79.5% of the rabbits were infected with Trichophyton mentagrophytes var. granulosum. Microsporum canis was isolated in only two animals, which had been imported from France. Healthy animal carriers were detected in 3.2% of the apparently non-infected farms. T. mentagrophytes were also found in samples taken from rabbits' nests and from the surrounding environment of the two infected farms. In a survey carried out among the staff responsible for the care of the animals, 77% of those working on infected farms suffered or had suffered dermatophytic lesions. This was confirmed in 8 out of 10 cases sampled. Attention is drawn to the high incidence of dermatophytoses in rabbits on farms and the importance of T. mentagrophytes as the etiological agent of tinea in people in close contact with infected animals.