Bifonazole, Urea

Pharmacological properties

The active substance of the drugs Canespor® and Canespor® Kit is bifonazole, an imidazole derivative with a wide spectrum of antimycotic activity. drugs are active against dermatophytes, yeast, molds and other fungi (malassezia furfur, corynebacterium minutissimum). bifonazole, unlike other azoles and fungicidal drugs, inhibits the biosynthesis of ergosterol not at one but at two different levels. inhibition of ergosterol synthesis leads to structural and functional disorders of the cytoplasmic membrane of pathogens.

MIC for these types of fungi is 0.062–16 μg / ml of substrate or less. Bifonazole has fungicidal activity against dermatophytes, including Trichophytosis pathogens.

Bifonazole has a pronounced fungicidal effect on dermatophytes at a concentration of 5 μg / ml and duration of action is 6 hours. On yeast fungi, for example, fungi of the genus Candida, at a concentration of 1-4 μg / ml, bifonazole acts mainly fungistatically, at a concentration of 20 μg / ml - fungicidal . In addition, the active substance exhibits a fungistatic effect in concentrations that are 2–10 times lower than the MIC values. Already at 3 μg / ml of the substrate, the proliferating mycelium Trichophyton mentagrophytes is rapidly inhibited.

In gram-positive cocci, with the exception of enterococci, the MIC of bifonazole is 4–16 μg / ml. In corynebacteria MIC - 0.5–2 μg / ml.

Bifonazole is effective in conditions of resistance of pathogens to other antifungal drugs. Very rarely, primary resistance to bifonazole in sensitive fungal species may occur. Studies to date have not revealed the development of secondary resistance in primary sensitive strains.

Urea, which is part of the drug Canespor^® set, softens keratinized tissues. Urea is a natural substance that is found in the human body. As part of the ointment, urea softens the keratin of the infected nail, which allows the painless part of the nail to be removed non-invasively. In vitro studies have shown that urea increases the depth of penetration of bifonazole into the affected nail. Thus, the combination of bifonazole and urea enhances the antimycotic effect.

Pharmacokinetics Bifonazole penetrates well into affected areas of the skin. 6 hours after application, the concentration of bifonazole in various layers of the skin reaches from 1000 μg / cm³ in the upper layer of the epidermis up to 5 μg / cm³ in papillary. All concentrations determined in this way are within the confirmed antimycotic activity.

The duration of stay on the skin, which is defined as a protective effect, is for the drug Canespor^® cream for at least 48–72 hours

The significant duration of the drug Canespor^® cream on the skin in concentrations with an antifungal effect and taking into account the fungicidal type of action are the basis for a single use in local therapy.

In the course of studies on absorption after topical application on intact human skin, serum concentrations are always below the definition line (1 ng / ml), only with inflamed skin, slight absorption is confirmed. You should not expect a systemic effect from such low concentrations of the active substance (usually less than 5 ng / ml). In the treatment of nails with Canespor^® Set, the level of bifonazole in blood plasma in all cases was below the detection threshold (less than 1 ng / ml).

Indications

Canespor® cream. treatment:

• fungal skin diseases caused by pathogens sensitive to bifonazole (dermatophytes; yeast, molds and other fungal infections; Malassezia furfur and Corynebacterium minutissimum);
• superficial candidiasis and mycosis of the skin (including foot mycosis and interdigital spaces, mycosis of the hands, mycosis of smooth skin and folds of the skin of the body);
• multi-colored lichen;
• erythrasma;
• treatment of the nail bed during the course of treatment of fungal diseases of the nails (onychomycosis) after removal of the nail plate.

Canespor^® set. Treatment for fungal infections of fingernails and toenails with atraumatic nail removal and simultaneous antimycotic effect.

Application

Canespor® cream.apply once a day, preferably in the evening before bedtime. apply a thin layer on the affected area of ​​the skin and rub. To ensure a lasting effect, treatment with Canespor® Cream must be carried out during the indicated treatment periods, even after the symptoms disappear. usual courses of treatment: mycosis of the feet and interdigital spaces - 3 weeks; mycoses of brushes, smooth skin and folds of the skin of the body - 2-3 weeks; multi-colored lichen, erythrasma - 2 weeks; superficial candidiasis of the skin - 2-4 weeks. a small amount of cream is usually enough to treat a palm-sized patch of skin.

Canespor^® the cream is used after the treatment of the nail with Canespor^® set. The nail bed is treated with Canespor^® cream 1 time per day for 4 weeks.

Children. Based on the available clinical data, there is no reason to assume toxic effects in children. However, for children under the age of 3 years (including newborns), the drug should be used only under the supervision of a doctor.

Canespor^® set. The drug is applied to the affected nail 1 time per day in such an amount as to cover the entire surface with a thin layer. Treatment with the drug should be carried out carefully every day and continued until the softened nail affected by the fungus can be removed. This usually lasts 7-14 days and depends on the spread of the infection and the thickness of the nail.

Seal the treated nail with a patch for 24 hours. Replace the patch 1 time per day. After removing the patch, wash the fingers with the affected nails in warm water for about 10 minutes, then remove the softened affected substance of the nail with a scraper, and then dry the nail. In the future, the drug Canespor^® set apply as above.

There is no need to cover the skin around the nail. But in some cases, irritation may appear. Therefore, the edge of the skin surrounding the nail must be smeared with zinc paste or other anti-inflammatory drug for topical application before fixing the patch. Canespor^® set, ointment for external use, affects only the nails affected by the fungus, healthy areas remain unchanged.

After removing the nail, before continuing the antimycotic treatment, the doctor must make sure that the onycholysis is completely completed, and, if necessary, conduct a final cleaning of the nail bed.

After removal of the nail, which is the result of antimycotic therapy with Canespor^® set, the nail bed must be treated with Canespor^® cream 1 time per day for about 4 weeks.

The order of use of the drug

1. Wash your leg or hand in warm water and then wipe thoroughly.

2. Apply a dose of ointment to the nail. Do not press or rub it.

3. Place half of the patch under the toe or palm. The patch can be cut according to the size of the nail.

4. Wrap the edges of the patch up and squeeze them well.

5. After that, put the other half of the patch on the nail, wrapping the adhesive ends down. Good to press.

6. A correctly positioned patch acts as a protective sheath on a damaged nail. Keep this occlusive dressing on your nail for 24 hours.

7. After 24 hours, remove the patch. Wash your leg or hand again with warm water and dry well.

8. Using a scraper, carefully remove the softened part of the affected nail.

Perform the operations described above carefully daily. The procedure must be repeated until the nail bed is completely cleansed. This usually takes 7-14 days.

If after 7-14 days all affected areas of the nail are not removed and the nail bed does not become smooth, you should consult a doctor.

The drug Canespor^® the set acts directly on the damaged nail, healthy areas remain unchanged. After the nail is removed, it is necessary to carry out antifungal treatment with Canespor cream^® for about 4 weeks.

Children.Given the available clinical data, there is no reason to assume toxic effects in children. However, for children aged 1 to 3 years, the drug should be used only under the supervision of a doctor.

Contraindications

Known hypersensitivity to the active substance or to any other auxiliary substance. Canespor® cream is also contraindicated for the preparation: hypersensitivity to the antifungal drugs of the imidazole group. treatment of children with diaper rash. the drug is not for vaginal use. treatment of scalp infections. do not use the drug until the affected part of the nail plate is removed to treat fungal diseases of the nails.

Side effects

Canespor® Cream

General violations and changes in the place of use. May cause local skin reactions (e.g. contact dermatitis), pain and swelling of the skin at the site of use.

From the immune system. In very rare cases, systemic hypersensitivity reactions are possible.

On the part of the skin and subcutaneous tissue. The development of contact dermatitis, allergic dermatitis, erythema, eczema, skin itching, rash, hives, blisters, peeling, dryness, irritation, maceration and a sensation of heat on the skin.

All side effects disappear after discontinuation of the drug.

Cetostearyl alcohol can cause skin irritation at the site of use (e.g. contact dermatitis). With increased sensitivity to cetostearyl alcohol, allergic reactions on the skin can occur.

Canespor^® set. In the treatment of fungal diseases of the nails, it is possible to develop skin and subcutaneous tissue disorders along the edges or on the nail bed in the form of contact dermatitis, maceration, skin exfoliation, nail peeling, nail discoloration, erythema, skin irritation, limb pain, itching, rashes. Possible pain and swelling of the skin at the site of application, eczema, urticaria, blisters, dryness, sensation of heat on the skin. These side effects disappear after discontinuation of treatment.

special instructions

Avoid contact with eyes. do not swallow. Keep out of the reach of children.

Patients with allergic reactions to other antifungal drugs from the imidazole group (e.g. econazole, clotrimazole, miconazole) should use Canespor^® carefully.

If symptoms persist, consult a doctor.

Antifungal treatment of the skin of the nail roller with the use of the drug Canespor^® the cream can be carried out as part of the treatment of nail mycosis only after preliminary keratolytic removal of the infected area of ​​the nail.

Persistent therapeutic effect of the drug Canespor^® the set depends mainly on the removal of the affected area of ​​the nail and the continued treatment of the nail bed with Canespor^®, cream, or other dosage form of bifonazole.

Allergic reactions to the patch are possible, but are very rare. In case of allergic reactions consult your doctor. You can use another waterproof dressing or surgical fingertip.

Canespor^® the kit can cause local skin reactions (contact dermatitis) due to lanolin content.

Use during pregnancy or lactation. Pregnancy. Preclinical studies and pharmacokinetic data in the human body do not indicate the harmful effects of bifonazole on the mother and child, if Canespor^® used during pregnancy. But clinical data are not available. In the first trimester of pregnancy, it is advisable to avoid the use of bifonazole.

The period of breastfeeding. It is not known whether bifonazole passes into human breast milk. Studies of pharmacodynamics and toxicological data in animals indicate the excretion of bifonazole and its metabolites in breast milk. Therefore, breast-feeding should be discontinued during bifonazole treatment.During breast-feeding, bifonazole should not be applied to the chest area.

Fertility. Preliminary clinical studies have not found that bifonazole can suppress male or female fertility. As a result of clinical studies of urea, no data were found regarding its damaging effect on sperm or female fertility.

The ability to influence the reaction rate when driving vehicles or other mechanisms. This drug does not affect or has very little effect on the ability to drive vehicles or other mechanisms.

Interactions

There is evidence of a possible interaction between topical bifonazole and warfarin, which leads to an increase in the international normalized ratio (risk of bleeding). if bifonazole is used in patients who are treated with warfarin, then appropriate monitoring should be carried out.

Overdose

There have been no reports of overdose during treatment with Canespor®.

After a single cutaneous application, there is no risk of acute intoxication. An overdose is possible when applied to large areas of the skin or with careless oral administration.

Storage conditions

Canespor® cream: for this medicine, special storage conditions are not required.

Canespor^® set: store at a temperature not exceeding 30 ° C.