Canespie Bifonazole 10Mg/Ml Topical Spray Solution 30 Ml

Canespie Bifonazole 10Mg/Ml Topical Spray Solution 30 Ml

Action and mechanism

• Antifungal. Bifonazole is an antifungal with imidazole structure and essentially fungistatic activity. It inhibits ergosterol production by binding to the heme site of cytochrome P450, a cofactor of the enzyme lanosterol-14alpha-demethylase. The decrease in ergosterol levels, together with the accumulation of lanosterol, leads to structural and functional alterations of the cell membrane, increasing its permeability and promoting cell lysis. Resistance mechanisms: Occasional cases of resistance to bifonazole, both primary and secondary, have been reported. In general, the following mechanisms of resistance to azole antifungals have been described:

• Alterations in membrane permeability.

• Development of efflux pumps.

• Alterations of the target, by overproduction of the enzyme or by mutations in the ER11 gene encoding lanosterol-14alpha-desmethylase.

• Increased fungal cytochrome P450 activity, requiring higher doses of antifungal drug. Microbial sensitivity/resistance: it has a broad spectrum, being effective against the following fungi:

• Dermatophytes: Trychophyton spp. (T. rubrum, T. mentagrophytes), Ephidermophyton floccosum, Microsporum sp. (M. canis).

• Yeasts: Candida spp., Torulopsis glabrata, Malassezia spp. (M. furfur).

• Dysmorphic fungi: Coccidioides immitis, Blastomyces dermatitidis, Sporothrix schenckii).

• Other fungi: Aspergillus spp. Decreased sensitivity to azole antifungals has been reported in certain species of Candida spp. other than C. albicans, which may lead to infections in immunocompromised or diabetic patients.

Pharmacokinetics

Topical, parenteral route:

• Absorption: it has a good ability to penetrate skin layers, reaching concentrations of 1 mg/cm3 (stratum corneum) to 5 mcg/cm3 (stratum capillary) within 6 h of application. The residence time in the skin is 48-72 hours. In contrast, systemic absorption is very low (0.6-0.8%), although bioavailability may increase in case of skin inflammation or occlusive conditions, up to values of 2-4%. Cp is normally undetectable (< 0.1 ng/ml).

• Distribution: not established.

• Metabolism: extensive in liver (95%).

• Elimination: in urine (45%) and faeces (40%), with a t1/2 of 25 h.

Indications

Treatment of [ATHLETE'S FOOT]. Official recommendations regarding the appropriate use of antifungals, especially those related to resistance problems, should be taken into account.

Posology

Canespie bifonazole topical solution:

• Adults: 1-2 sprays, 1 time a day, preferably at bedtime.

• Children and adolescents < 18 years of age: * Adolescents from 12 years of age: same as adults. * Children < 12 years: not recommended.

• Elderly: no specific dosage recommendations have been made. Duration of treatment: about 3 weeks of continuous treatment is usually required. If after 7 days of treatment symptoms continue or worsen, consult a doctor and/or pharmacist.

• Missed dose: administer the missed dose as soon as possible, unless the next dose is soon to be administered. Administer the next dose at the usual time. Do not double the next dose.

Posology in renal insufficiency

No specific dosage recommendations have been made.

Posology in hepatic insufficiency

No specific dosage recommendations have been made.

Guidelines for correct administration

Cream, topical solution: apply and massage to promote absorption.

Carefully wash and dry the infected area before each application. Avoid application to the eyes or mucous membranes. Wash hands after each application. Avoid occlusive dressings.

Contraindications

[ALLERGY TO AZOLIC ANTIFUNGICALS] or to any other component of the medicinal product.

Precautions

Occlusive dressings. Avoid occlusive dressings as they may promote systemic absorption.

Do not apply to eyes or mucous membranes. In case of accidental contact with eyes, rinse thoroughly with water and consult an ophthalmologist.

Advice to the patient

• Treatment does not exclude the need to follow basic hygiene and body care measures to prevent the risk of re-infection. In the case of foot infections, it is recommended to change socks after each application and to wear well-ventilated shoes. It is recommended to avoid fibre socks or shoes with rubber soles. In addition, precautions should be taken to avoid infecting others, such as avoiding sharing socks, shoes or towels, and not walking barefoot.

• Do not forget to apply bifonazole every day, and for the period of time prescribed by your doctor, even if the symptoms have disappeared. Premature discontinuation may encourage the reappearance of symptoms and the development of resistance.

• Do not cover the area of application with occlusive dressings.

Special warnings

Re-evaluate the diagnosis and consider alternative therapies if symptoms continue or worsen after 4 weeks of treatment (or 7 days in case of athlete's foot).

Interactions

Oral anticoagulants. Bifonazole may increase INR after topical administration. The significance seems very low, due to its low systemic absorption, but should be taken into account in case of administration on large skin surfaces or if the patient applies occlusion. No specific studies of interactions with other topically administered medicinal products have been performed, so it is recommended to avoid the application of other drugs where bifonazole has been applied.

Pregnancy

Safety in animals: Bifonazole was not teratogenic in animals. Abortion and increased foetal mortality have been reported following oral administration in rodents (rat, rabbit). In rats, delayed foetal ossification was also observed, but this could be due to maternotoxicity, as a decrease in maternal weight was also reported. Bifonazole crosses the placenta in rats. Safety in humans: no adequate and well-controlled studies in humans are available. Avoid use during pregnancy and in women of childbearing age who are not using effective contraception during treatment. Effects on fertility: Bifonazole did not cause side effects on fertility in female rats after oral administration. No specific human studies have been performed.

Lactation

Safety in animals: bifonazole and its metabolites are excreted in rat milk, although no specific studies have been conducted on the safety in humans: it is not known whether it is excreted in milk, and what consequences this may have for the nursing infant. It is recommended to discontinue or avoid breast-feeding.

Children

Bifonazole has been used in the treatment of athlete's foot in adolescents aged 12 years and older at the same doses as in adults. Select presentations especially indicated for use in adolescents (see information on the different presentations available). Not recommended for use in children < 12 years of age.

Elderly

No specific studies have been performed in these patients.

Effects on driving

Not expected to have a significant effect.

Adverse reactions

Adverse reactions are generally mild and usually limited to local effects. Adverse reactions are described according to each frequency range as very frequent (>10%), frequent (1-10%), infrequent (0.1-1%), rare (0.01-0.1%), very rare (<0.01%) or of unknown frequency (cannot be estimated from available data).

- Dermatological: frequency unknown [CONTACT DERMATITIS], [ALLERGIC DERMATITIS], [ERTHEEMA], [PRURITIS], [EXEMPTEMATIC ERUPTIONS], [URTICARIA], appearance of [AMPOLLS], [EXFOLIATORY DERMATITIS], [SKIN DRYNESS], [CUTANEOUS IRRITATION], [EDEMA], pain or burning sensation at the site of application.

Overdose

• Symptoms: In case of excessive application, local reactions such as swelling, redness or burning sensation may occur. Nausea, vomiting and dizziness have been observed after accidental ingestion. Actions to be taken:

• Antidote: no specific antidote.

• General elimination measures: In case of excessive application it may be sufficient to wash the area and temporarily stop treatment. In case of symptomatic intoxication by accidental ingestion, gastric lavage may be necessary, with protection of the airways.

• Treatment: symptomatic.