Source: Health Products Regulatory Authority (IE) Revision Year: 2020 Publisher: Recordati Industria Chimica e Farmaceutica SpA, Via Matteo Civitali, 20148, Milan, Italy
ATC code: G01AF12
Fenticonazole is a broad-spectrum antimycotic agent.
In vitro: high fungistatic and fungicidal activity against dermatophytes (all species of Trichophyton, Microsporum and Epidermophyton), against Candida albicans and against the other agents responsible for mycotic infections of skin and mucous membranes.
In vivo: healing of vaginal mycoses due to Candida within 5 days in mice.
Fenticonazole also shows antibacterial activity against Gram-positive micro-organisms. Supposed mode of action: block of oxidative enzymes leading to accumulation of peroxides and necrosis of fungal cells; direct action on the membrane.
Pharmacokinetic studies have revealed no transcutaneous absorption either in man or in animals and a very low vaginal absorption.
LD50 mice: oral>3000mg/kg; i.p 1276mg/kg (M), 1265mg/kg (F)
LD50 rats: oral>3000mg/kg; s.c.>750mg/kg; i.p. 440mg/kg (M), 309mg/kg (F)
Chronic toxicity: following oral administration of 40-80-160mg/kg/day for 6 months in rats and dogs, fenticonazole was well tolerated, although some evidence of light and moderate general toxicity occurred (increase in liver weight at 160mg/kg without histopathological alterations in rats, and a transient increase in serum SGPT at 80 and 160mg/kg, together with an increase in liver weight in dogs).
Fenticonazole does not interfere with the function of male and female gonads, and does not modify the first phases of reproduction. Studies in reproductive toxicology revealed, as for other imidazole derivatives, an embryolethal effect at high dosages (>20mg/kg). Fenticonazole has shown no teratogenic effects in rats and rabbits and has revealed no mutagenic potential in six mutagenicity tests.
Satisfactory results were obtained in tolerability tests performed in guinea pigs, rabbits as well as in mini-pigs, the skin of which is similar to that of humans, as far as morphology, functionality and sensitivity to irritating agents are concerned. Fenticonazole has shown no evidence of sensitisation, phototoxicity and photoallergy. Pharmacokinetic studies have revealed no transcutaneous absorption either in man or in animals and a very low vaginal absorption.
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