Bifosin^® (Cream) Instructions for Use

Marketing Authorization Holder

Sintez PJSC (Russia)

ATC Code

D01AC10 (Bifonazole)

Active Substance

Bifonazole (Rec.INN registered by WHO)

Dosage Forms

	Bifosin®	Cream for external use 1%: 30 g tube
		Powder for external use 1%: 30 g jar
		Solution for external use 1%: 15 g dropper bottle
		Spray for external use 1%: 20 ml bottle

Dosage Form, Packaging, and Composition

Cream for external use 1% colorless with a whitish or grayish tint or colorless with a grayish-cream tint, homogeneous.

Excipients: macrogol 400 (polyethylene oxide 400), macrogol 4000 (polyethylene oxide 4000), propylene glycol.

30 g – aluminum tubes (1) – cardboard packs.

Powder for external use 1% white or light cream with a grayish tint; the preparation must pass completely through silk sieve No. 46.

Excipients: zinc oxide – 150 mg/g, corn starch, talc.

30 g – polyethylene jars (1) – cardboard packs.

Solution for external use 1% transparent, colorless or slightly colored.

Excipients: macrogol 400 (polyethylene oxide 400).

15 ml – dark glass dropper bottles (1) – cardboard packs.

Spray for external use 1% in the form of a transparent colorless or slightly colored liquid.

Excipients: propylene glycol – 0.3 ml, isopropanol – 0.4 ml, macrogol 400 (polyethylene oxide 400) – up to 1 ml.

20 ml – polymer bottles (1) with a sprayer – cardboard packs.

Clinical-Pharmacological Group

External antifungal drug

Pharmacotherapeutic Group

Antifungal agent

Pharmacological Action

Broad-spectrum antifungal drug for external use, an imidazole derivative. It acts fungicidally against dermatophytes (Trichophyton, Microsporum, Epidermophyton), fungistatically against yeast-like and mold fungi (Aspergillus ferrus, Scopulariopsis brevicaulis), Malassezia furfur. Active against bacteria of the gram-positive rod Corynebacterium minutissimum (MIC ranges from 0.5 to 2 µg/ml) and against gram-positive cocci (MIC 4-16 µg/ml), except for Enterococcus spp.

The target of the drug’s action is ergosterol – the most important component of the fungal membrane. Bifonazole suppresses the synthesis of ergosterol at two stages of its formation, which leads to structural and functional damage to the cytoplasmic membrane of fungi.

The minimum effective concentration is 5 ng/ml with an exposure duration of at least 6 hours; at a concentration of 3 ng/ml, the growth of rapidly proliferating mycelium of Trichophyton mentagrophytes is inhibited.

It has a fungistatic effect on yeast-like fungi of the genus Candida, and at concentrations of 20 ng/ml – a fungicidal effect.

Pharmacokinetics

Absorption

Penetrates well into the affected layers of the skin. Absorption – 0.6-0.8%, the concentration of bifonazole in blood plasma is not determined. When the cream is applied to the affected skin, absorption is 2-4%, concentration in blood plasma is 2 ng/ml.

Distribution

6 hours after application, the concentration of bifonazole in the skin reaches or many times exceeds the minimum effective concentration for the main fungi causing dermatomycoses: 1 mg/cm² in the upper layer of the epidermis (Stratum corneum) and 5 mg/cm² in the Stratum papillare.

The duration of bifonazole in the skin is 36-48 hours (when using the cream – 48-72 hours).

Elimination

T_1/2 from the skin is 19-32 hours (depending on its density).

Indications

Treatment of skin lesions caused by dermatophytes, yeast-like, mold fungi, as well as Malassezia furfur and Corynebacterium minutissimum

• Mycoses of the feet and hands;
• Dermatomycosis of smooth skin;
• Pityriasis versicolor;
• Superficial skin candidiasis;
• Erythrasma;
• Dermatomycosis of the scalp (powder for external use, solution for external use, spray for external use).

ICD codes

Dosage Regimen

The drug should be applied once a day, at night.

Cream for external use, powder for external use or solution for external use is applied in a thin layer to the affected area of the skin and rubbed in thoroughly.

Spray for external use is sprayed onto the affected areas in an amount sufficient for their thorough moistening, and, in addition, is applied to adjacent areas of both affected and intact skin.

For an area the size of a palm, a strip of cream 0.5-1 cm long or a few drops of solution (approximately 3 ml) is usually sufficient.

To achieve a satisfactory result, treatment must be continuous and continued for the following recommended periods: for mycoses of the feet and interdigital spaces of the feet – 3-4 weeks, for dermatomycosis of smooth skin – 2-3 weeks, for superficial skin candidiasis – 2-4 weeks, for pityriasis versicolor, erythrasma – 2 weeks, for dermatomycosis of the scalp – 4 weeks.

After the disappearance of clinical manifestations of mycosis, Bifosin^® continues to be used for the purpose of preventing relapse, applying the drug once a day for 2 weeks.

Spray for external use, solution for external use and powder for external use are preferable for the treatment of dermatomycosis of the scalp.

Adverse Reactions

Local reactions hyperemia, skin irritation, burning sensation, allergic reactions, eczema, skin itching, vesicular rash, maceration, peeling, hyperemia; very rarely – the development of allergic dermatitis.

Side effects are reversible and disappear after discontinuation of therapy.

Contraindications

• Lactation period (breastfeeding);
• Increased sensitivity to the components of the drug.

With caution: infant age (up to 1 year), pregnancy (I trimester).

Use in Pregnancy and Lactation

Research data show that the drug does not have any negative effect on the body of the mother and fetus.

The use of the drug in the first trimester of pregnancy is possible only for strict indications. In the II and III trimesters of pregnancy, the drug is used according to indications, since the drug is used externally and does not have a systemic effect.

During the lactation period, breastfeeding should be discontinued.

Pediatric Use

The use of Bifosin^® in infants is possible only under the careful supervision of a physician.

With caution: infant age (up to 1 year).

Special Precautions

In the absence or insufficient effectiveness, the patient should be additionally examined (state of immunity, blood, endocrine system, microcirculation of the affected area) and treatment should be adjusted according to the examination results.

Avoid getting the drug into the eyes.

Use in pediatrics.

Use in infants (under 1 year of age) is possible only under the supervision of a physician.

Effect on the ability to drive vehicles and mechanisms

The drug does not affect the ability to drive vehicles, mechanisms and engage in other hazardous activities that require special attention and quick reactions.

Overdose

Extremely low systemic absorption of the drug with external use makes overdose practically impossible.

Drug Interactions

The drug can be used simultaneously with other drugs, since no drug interaction reactions have been identified.

Storage Conditions

The drug in the form of a cream for external use, powder for external use and solution for external use should be stored in a dry, light-protected place at a temperature from 15°C (59°F) to 25°C (77°F).

Shelf Life

Shelf life – 2 years.

The drug in the form of a spray for external use should be stored in a light-protected place at a temperature not exceeding 25°C (77°F). Shelf life – 2 years.

The drug should be stored out of the reach of children.

Dispensing Status

The drug is approved for use as an over-the-counter product.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.