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Active ingredients
Bifonazole
Release form
Cream
Composition
100 g ointment contains: active ingredients: bifonazole 1 g, urea 40 g; auxiliary ingredients: beeswax white 5 g, white petrolatum 34 g, lanolin 20 g
Pharmacological effect
Bifonazole, the active substance of Mycopres cream, is a derivative of imidazole and has a wide spectrum of antimycotic action. Bifonazole has a fungicidal action against dermatophytes (in particular, against Trichophyton spp.). The full fungicidal effect is achieved when the concentration of bifonazole is 5 μg / ml and the duration of exposure is at least 6 hours. Bifonazole has a fungistatic effect on yeast and mold fungi, as well as Malassezia furfur. With the defeat of yeast fungi, for example, Candida species, at a concentration of 1-4 μg / ml, the fungistatic effect of bifonazole is observed predominantly; For the fungicidal effect, a bifonazole concentration of 20 mcg / ml is required. Bifonazole is also active against Corynebacterium minutissimum (MIC from 0.5 to 2 mcg / ml), gram-positive cocci, with the exception of enterococci (MIC from 4 to 16 mcg / ml). Resistant strains of fungi are very rare. Studies have not confirmed the development of secondary resistance in primary sensitive strains. Bifonazole inhibits ergosterol biosynthesis at two different levels, which distinguishes it from other antifungal drugs and other azole derivatives. This double action leads to structural and functional damage to the cytoplasmic membrane of fungi.
Pharmacokinetics
Bifonazol penetrates well into the affected skin layers. 6 hours after application, concentrations in different layers of the skin reach from 1000 μg / cm3 in the upper layer of the epidermis (in the stratum corneum) to 5 μg / cm3 in the papillary layer. Thus, all concentrations obtained are within the range of antifungal activity. When applied to intact skin, a small amount of bifonazole is absorbed (0.6-0.8% of the drug dose); the concentration level of bifonazole in the blood plasma is always below the detection limit (i.e. <1 ng / ml). Insignificant absorption is detected only after applying the cream bifonazola on inflamed skin (2-4% of the dose). Thus, since very low concentrations of bifonazole are created in the blood plasma when applied topically (usually not higher than 5 ng / ml), no systemic effects are observed. The duration of stay in the skin (determined by the protective action against fungal infection in guinea pigs) - 48-72 h. Bifonazole crosses the placental barrier in rats.
Indications
Fungal skin diseases caused by dermatophytes, yeast-like, mold fungi, as well as Malassezia furfur and Corynebacterium minutissimum: - foot mycoses (foot skin dermatophytosis and foot interdigital dermatophytosis); - Mycoses of the hands (dermatophytosis of the skin of the hands and interdigital dermatophytosis); - dermatophytosis of smooth skin of the body; - dermatophytosis of the groin area; - superficial candidiasis of the skin; - pityriasis versicolor; - Erythrasma.
Contraindications
- Hypersensitivity to bifonazole or any other component of the drug. With care: - pregnancy and lactation period; - childhood.
Precautionary measures
During pregnancy (II and III trimester) (see section Use during pregnancy and during breastfeeding). Infant age. Use with caution in patients who have an increased sensitivity to other antifungal drugs from the group of imidazole derivatives (econazole, clotrimazole, miconazole ).
Use during pregnancy and lactation
Pregnancy Absorption of bifonazol with external use of the drug is negligible (see Pharmacokinetics section). The data of preclinical and pharmacokinetic studies show that bifonazole does not have any negative effect on the organism of the mother and fetus. Clinical studies in pregnant women were not conducted. As a precaution, bifonazole should be avoided during the first trimester of pregnancy. In the II and III trimester of pregnancy, the use of the drug is possible if the potential benefit to the mother exceeds the possible risk to the fetus. The period of breastfeeding Absorption of bifonazole with external use of the drug is insignificant (see Pharmacokinetics section), it is not known whether bifonazole penetrates into breast milk in women. The data obtained on experimental animals show that bifonazole is excreted in breast milk. If necessary, the use of the drug during breastfeeding should decide on its termination. Fertility Safety data obtained from preclinical studies suggest that the use of bifonazole does not have any negative effect on male and female fertility.
Dosage and administration
Externally, the cream is applied with a thin layer to the affected skin 1 time a day, preferably at night, and gently rubbed. To achieve a satisfactory outcome, treatment must be continuous. The duration of therapy is usually: - for mycoses of the feet (dermatophytosis of the skin of the feet and interdigital foot dermatophytosis): 3 weeks; - for mycoses of the hands (dermatophytosis of the skin of the hands and interdigital dermatophytosis), skin of the body (dermatophytosis of smooth skin) and skin folds (inguinal dermatophytosis): 2-3 weeks; - with pityriasis versicolor erythrasma: 2 weeks; - with superficial skin candidiasis: 2-4 weeks. For a surface treatment that is approximately equal to the area of the palm, a sufficiently small amount of cream (a column of cream about 1 cm long). Separate studies in children was not conducted. Based on a review of clinical data, no evidence of the development of adverse side effects when using the drug in children. However, in children, the drug Mycospor, a cream for external use, should be used only under the supervision of a physician. If there is no improvement within 7 days or the condition has worsened, it is necessary to consult a doctor.
Side effects
General disorders and local reactions: pain at the site of application, peripheral edema (at the site of application). Skin and subcutaneous tissue disorders: contact dermatitis, allergic dermatitis, erythema, itching, rash, urticaria, blisters, peeling and dry skin, eczema, skin irritation, maceration, burning sensation of the skin. Side effects are reversible and disappear after drug withdrawal.
Overdose
The risk of acute intoxication is absent, as overdose (application to large areas of skin under conditions favorable for absorption) after a single application of the drug on the skin or accidental ingestion is unlikely.
Interaction with other drugs
The absorption of bifonazol when externally administered is insignificant. Cases of interaction with other drugs are unknown.
special instructions
Use with caution in patients who have an increased sensitivity to other antifungal drugs from the group of imidazole derivatives (econazole, clotrimazole, miconazole). Avoid getting the cream in the eyes.In case of hypersensitivity in cetostearyl alcohol, it is recommended to use instead of the cream dosage forms of bifonazole that do not contain cetostearyl alcohol (for example, Micospor solution for external use of 1%). Use in pediatrics There have been no separate studies in children. Based on a review of clinical data, no evidence of the development of adverse side effects when using the drug in children. However, in children under 1 year old, Microspor Cream should be used only under the supervision of a physician.