Pharmacological properties
Pharmacodynamics. The active ingredient of the drugs Kanespor® and Kanespor® Set is bifonazole - an imidazole derivative with a wide spectrum of antifungal activity. The drugs are active against dermatophytes, yeasts, 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.
The MIC for these types of fungi is 0.062-16 μg/ml substrate or less. Bifonazole has fungicidal activity against dermatophytes, including trichophyton pathogens.
Bifonazole has a pronounced fungicidal effect on dermatophytes at a concentration of 5 μg/ml and a duration of action of 6 hours. On yeast fungi, for example, fungi of the genus Candida, at a concentration of 1-4 μg/ml bifonazole acts predominantly fungistatically, at a concentration of 20 μg/ml - fungicidally. In addition, the active substance exhibits a fungistatic effect at concentrations that are 2-10 times lower than the MIC value. Already at 3 μg/ml of substrate, a rapid decrease in the proliferating mycelium of Trichophyton mentagrophytes was noted.
In gram-positive cocci, with the exception of enterococci, the MIC of bifonazole is 4-16 μg/ml. In corynebacteria, the MIC is 0.5-2 μg/ml.
Bifonazole is effective in conditions of resistance of pathogens to other antifungal drugs. Very rarely, primary resistance to bifonazole may be detected in sensitive fungal species. Studies to date have not revealed the development of secondary resistance in initially sensitive strains.
Urea, which is part of the drug Kanespor ® set, softens keratinized tissues. Urea is a natural substance found in the human body. In the composition of the ointment, urea softens the keratin of the infected nail, which allows for a non-invasive, painless removal of the affected part of the nail. 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 antifungal effect.
Pharmacokinetics. Bifonazole penetrates well into the affected skin areas. 6 hours after application, the concentration of bifonazole in different layers of the skin reaches from 1000 μg / cm 3 in the upper layer of the epidermis to 5 μg / cm 3 in the papillary. All concentrations determined in this way are within the limits of confirmed antimycotic activity.
The duration of stay on the skin, which is defined as a protective effect, is at least 48-72 hours for the drug Kanespor ® cream.
The significant duration of the drug Kanespor ® cream on the skin in concentrations with antifungal action and taking into account the fungicidal type of action is the basis for a single use in local therapy.
In studies of absorption after topical application to intact human skin, serum concentrations were always below the detection limit (1 ng/ml), only with inflamed skin was a slight absorption confirmed. No systemic effect should be expected from such low concentrations of the active substance (usually less than 5 ng/ml). When treating nails with the drug Kanespor ® Kit, the level of bifonazole in blood plasma was in all cases below the detection limit (less than 1 ng/ml).
Indication
Canespor® cream. treatment:
fungal skin diseases caused by pathogens sensitive to bifonazole (dermatophytes; yeasts, molds and other fungal infections; Malassezia furfur and Corynebacterium minutissimum); superficial candidiasis and mycoses of the skin (including mycoses of the feet and interdigital spaces, mycoses of the hands, mycoses of smooth skin and skin folds of the body); lichen varicolor; erythrasma; treatment of the nail bed during the course of treatment of fungal nail diseases (onychomycosis) after removal of the nail plate.
Kanespor ® set. Treatment of fungal infections of fingernails and toenails with atraumatic nail removal and simultaneous antifungal action.
Application
Kanespor® cream. Apply once a day, preferably in the evening before bedtime. Apply a thin layer to the affected area of skin and rub in. To ensure a long-lasting effect, treatment with Kanespor® cream must be continued for the specified treatment periods, even after the symptoms have disappeared. Typical treatment courses: mycoses of the feet and interdigital spaces - 3 weeks; mycoses of the hands, smooth skin and skin folds of the body - 2-3 weeks; lichen varicolor, erythrasma - 2 weeks; superficial candidiasis of the skin - 2-4 weeks. A small amount of cream is usually enough to treat a palm-sized area of skin.
Kanespor ® cream is used after treating the nail with Kanespor ® set. The nail bed is treated with Kanespor ® cream once a day for 4 weeks.
Children. Based on the available clinical data, there is no reason to assume toxic manifestations in children. However, children under 3 years of age (including newborns) should use the drug only under medical supervision.
Cover the treated nail with a plaster for 24 hours. Replace the plaster once a day. After removing the plaster, wash the fingers with the affected nails in warm water for about 10 minutes, then remove the softened affected nail substance with a scraper, then dry the nail. In the future, use the Kanespor ® kit as described above.
It is not necessary to cover the skin around the nail. However, in some cases, irritation may occur. Therefore, the edge of the skin surrounding the nail should be smeared with zinc paste or another anti-inflammatory drug for topical use before fixing the patch. Kanespor ® set, an ointment for external use, affects only the nails affected by the fungus, healthy areas remain unaffected.
After nail removal, before continuing antifungal treatment, the doctor should ensure that onycholysis is completely complete and, if necessary, perform a final cleaning of the nail bed.
After removal of the nail resulting from antifungal therapy with the drug Kanespor ® set, the nail bed must be treated with Kanespor ® cream once a day for approximately 4 weeks.
How to use the drug
1. Wash your leg or arm in warm water and then dry it thoroughly.
2. Apply a dose of ointment to the nail. Do not press on it or rub it.
3. Place half of the patch under the toe or palm. The patch can be cut to fit the size of the nail.
4. Fold the edges of the patch up and press them well.
5. Then place the other half of the patch on the nail, wrapping the sticky ends down. Press well.
6. When properly positioned, the patch acts as a protective covering on the damaged nail. This occlusive dressing should be kept on the nail for 24 hours.
7. After 24 hours, remove the patch. Wash the leg or arm thoroughly again with warm water and dry well.
8. Using a scraper, carefully remove the softened part of the affected nail.
Carefully perform the above operations every day. The procedure must be repeated until the nail bed is completely clean. This usually takes 7-14 days.
If after 7-14 days all the affected areas of the nail are not removed and the nail bed does not become smooth, you should consult a doctor.
The Kanespor ® kit is applied directly to the damaged nail, leaving the healthy areas untouched. After the nail is removed, antifungal treatment with Kanespor ® cream should be carried out for approximately 4 weeks.
Children: Based on available clinical data, there is no reason to assume toxic effects in children. However, children aged 1 to 3 years should only be given the drug under medical supervision.
Contraindication
Known hypersensitivity to the active substance or to any of the excipients. Canespor® cream is also contraindicated for: hypersensitivity to imidazole antifungals. Treatment of children with diaper rash. The drug is not for vaginal use. Treatment of scalp infections. Do not use the drug before removing the affected part of the nail plate for the treatment of fungal nail diseases.
Side effects
Canespor® cream
General disorders and administration site conditions: May cause local skin reactions (e.g. contact dermatitis), pain and swelling of the skin at the application site.
On the part of the immune system: In very rare cases, systemic hypersensitivity reactions are possible.
Skin and subcutaneous tissue disorders: Contact dermatitis, allergic dermatitis, erythema, eczema, skin itching, rash, urticaria, blisters, peeling, dryness, irritation, maceration and a feeling of heat on the skin.
All side effects disappear after discontinuation of the drug.
Cetostearyl alcohol may cause skin irritation at the site of application (e.g. contact dermatitis). In case of hypersensitivity to Cetostearyl alcohol, allergic skin reactions may occur.
Kanespor ® set. In the treatment of fungal nail diseases, the development of skin and subcutaneous tissue disorders at the edges or on the nail bed is possible in the form of contact dermatitis, maceration, skin peeling, nail peeling, nail discoloration, erythema, skin irritation, pain in the extremities, itching, rashes. Pain and swelling of the skin at the site of application, eczema, urticaria, blisters, dryness, a feeling of heat on the skin are possible. These side effects disappear after discontinuation of treatment.
Special instructions
Avoid contact with eyes. Do not swallow. Keep out of reach of children.
Patients with allergic reactions to other antifungal drugs from the imidazole group (e.g. econazole, clotrimazole, miconazole) should use Kanespor® with caution.
If symptoms persist, you should consult a doctor.
Antifungal treatment of the skin of the nail bed using the drug Kanespor ® cream can be carried out as part of the therapy of nail mycosis only after prior keratolytic removal of the infected area of the nail.
The sustained therapeutic effect of the drug Kanespor ® kit depends primarily on the removal of the affected area of the nail and continued treatment of the nail bed with Kanespor ®, cream, or another dosage form of bifonazole.
Kanespor® kit may cause local skin reactions (contact dermatitis) due to the lanolin content.
Use during pregnancy or breastfeeding. Pregnancy. Preclinical data and pharmacokinetic data in humans do not indicate a harmful effect of bifonazole on the mother and child if Kanespor ® is used during pregnancy. However, clinical data are lacking. In the first trimester of pregnancy, it is advisable to avoid the use of bifonazole.
Breastfeeding. It is not known whether bifonazole is excreted in human breast milk. Pharmacodynamic and toxicological studies in animals indicate excretion of bifonazole and its metabolites in breast milk. Therefore, breastfeeding should be discontinued during treatment with Bifonazole. Bifonazole should not be applied to the chest area during breastfeeding.
Fertility: Preliminary clinical studies have not shown that bifonazole can inhibit male or female fertility. Clinical studies of urea have not revealed any evidence of its damaging effects on sperm or female fertility.
Ability to influence the reaction speed when driving vehicles or other mechanisms. This medicine has no or very slight influence on the ability to drive vehicles or other mechanisms.
Interactions
There is evidence of a possible interaction between topically applied bifonazole and warfarin, leading to an increase in the international normalized ratio (risk of bleeding). If bifonazole is used in patients treated with warfarin, appropriate monitoring should be carried out.
Overdose
There have been no reports of overdose during treatment with Canespor®.
There is no risk of acute intoxication after a single external application. Overdose is possible when applied to large areas of skin or with careless oral administration.
Storage conditions
Canespor® cream: this medicinal product does not require any special storage conditions.
Kanespor ® kit: store at a temperature not exceeding 30 °C.
