The Use of Bifonazole in the First 2 Years of Life

Abstract

We have studied the activity of bifonazole in patients in the first 2 years of life suffering from napkin dermatitis in which Candida was verified by culture tests. The patients were chosen from children recovered in the departments of Pediatric “Bambino Gesu” Hospital Clinic and from the Outpatients Department. In five hospitalized patients the following parameters were checked before the treatment and after 3 weeks of therapy: hemochromecytometric test, glycemia, azotemia, creatininemia, bilirubinemia, GOT, GPT, LDH, ALP, ALS; the parameters did not show any change between the checks. Every patient underwent a topical treatment with bifonazole 1% cream for 3 weeks: the results were very good with only a few patients having slight redness at the end of therapy, which disappeared without any further treatment.

Bifonazole is a new broad-spectrum antimycotic and it is a non-halogenated derivative of imidazole, synthetised from Bayer’s AG Research Laboratories. The chemical structure is l-(4-biphenyl) benzyl-imidazol; its characteristic molecular structure and chemical-Physical attributes: lipophilia, solubility in lipid solvents and in alcohol, and insolubility in water (less than 0.1 mg in 100 ml at pH 6) conditions its pharmacological activity. Bifonazole is a powerful inhibitor of the demethylation reaction dependent from cytochrome P₄₅₀, and thus of the metabolic passage reaction from 24-metrhylen-dihydro-lanosterol to dimethylsterol, precursor of the constitutive sterols of the cellular membrane. In cell membranes sterols have the function of increasing the physical stability of the phospholipid phases [1], avoiding phase transitions between liquid and crystalline lipid phases. Bifonazole, moreover, effectively inhibits microsomal HMG-CoA-reductase, used in one of the first stages in the metabolic chain of sterol biosynthesis, so that the cell membrane of dermatophytes is damaged significantly. A peculiar characteristic of bifonazole’s pharmacodynamics is the capability of the molecule to remain inside the pathogen cell for a long time, continuing the inhibitory action.