Binafin, cream 1% 10 g

Binafin is a broad-spectrum antifungal.

Pharmacodynamics

Terbinafine is an allylamine, which has a broad spectrum of action against fungi that cause skin, hair and nail diseases, including dermatophytes.Dermatophytes, such as T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum, Microsporum (e.g. M. canis), Epidermophyton floccosum, and yeast-like fungi of the genus Candida (e.g. Candida albicans) and Pityrosporum. In low concentrations, terbinafine has fungicidal effect against dermatophytes, mold fungi and some dimorphic fungi. Activity against yeast-like fungi, depending on their species, may be fungicidal or fungistatic.

Terbinafine specifically inhibits the early stage of sterol biosynthesis in the fungus cell. This leads to a deficit of ergosterol and intracellular accumulation of squalene, which causes cell death of the fungus. The action of terbinafine is performed by inhibiting the enzyme squaleneepoxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system. Terbinafine has no effect on metabolism of hormones or other drugs. When Binafin is administered orally, concentrations of the drug are created in the skin, hair and nails to provide fungicidal action.

Pharmacokinetics

After a single oral administration of terbinafine at a dose of 250 mg, Cmax of the drug in plasma is reached after 2 hours and is 0.97 µg/ml. Half-absorption period is 0.8 h; and half-distribution period is 4.6 h. There is no need to adjust the dose of the drug in case of concomitant ingestion. Terbinafine is largely bound to blood plasma proteins (99%), rapidly penetrates into the dermal layer of the skin and concentrates in the lipophilic stratum corneum. Terbinafine also penetrates into the sebaceous gland secretion, resulting in high concentrations in hair follicles, hair and sebaceous gland-rich skin. Terbinafine has also been shown to penetrate the nail plates in the first few weeks of therapy.

Terbinafine is metabolized rapidly and to a significant extent with the participation of at least seven cytochrome P450 isoenzymes, with the CYP2C9, CYP1A2,CYP3A4, CYP2C8 and CYP2C19 isoenzymes playing a major role. As a result of biotransformation of terbinafine metabolites are formed that have no antifungal activity and are excreted mainly with the urine. The final T1/2 of the drug is 17 hours. There is no evidence of cumulation of the drug in the body. There are no changes in Css of Binafin in plasma depending on age, but in patients with impaired renal or hepatic function the drug excretion rate may be delayed, which leads to higher plasma concentrations of terbinafine. In pharmacokinetic studies of a single dose of Binafin in patients with concomitant liver disease, it has been shown to reduce drug clearance by 50%.

Indications

Active ingredient

Composition

1 g cream contains:

Active substance:

terbinafine hydrochloride 10 mg;

Associates:

Ketosterol alcohol,

White soft paraffin,

liquid paraffin,

ketomacrogol,

/p>

methylparaben,

propylparaben,

isopropyl myristate,

sodium phosphate sour,

purified water.

How to take, the dosage

Externally. Adults and children 12 years and older can apply Binafin to the skin 1 or 2 times a day. Before applying the cream, the affected areas should be peeled off and dried. The cream is applied in a thin layer to the affected skin and adjacent areas and lightly rubbed.

Infections accompanied by diaper rash (under the breasts, between the fingers, between the buttocks, in the groin area), the areas where the cream is applied can be covered with gauze, especially at night.

The average duration of treatment: dermatomycosis of the trunk, shins and feet – 1 week, 1 time a day; skin candidiasis – 1-2 weeks, 1 or 2 times a day; variegated herpes – 2 weeks, 1 or 2 times a day.

A reduction in the severity of clinical manifestations is usually noted in the first days of treatment. If treatment is irregular or if it is stopped prematurely, there is a risk of a recurrence of the infection. If no signs of improvement are noted after 2 weeks of treatment, the diagnosis must be verified.

The use of the drug in the elderly. There is no reason to believe that dosing should be changed in older patients or that they have adverse events that differ from younger patients.

The use of the drug in children. It is not recommended to use this drug in children younger than 12 years of age.

Special Instructions

It is intended for external use only. Contact with the eyes should be avoided.

Contraindications

Hypersensitivity to terbinafine or any other component of Binafine.

Side effects

In rare cases redness, itching or burning have been observed at the site of application, but these phenomena have rarely made it necessary to discontinue treatment. The above symptoms should be distinguished from allergic reactions (e.g., urticaria), which are rare, but if they occur, treatment should be discontinued.

Overdose

Symptoms: headache, dizziness, nausea, epigastric pain.

Treatment: gastric lavage, administration of activated charcoal, symptomatic therapy.

Pregnancy use

The drug should be used during pregnancy only for very strict indications and if the expected benefits to the mother exceed the potential risk to the fetus and child.

If it is necessary to prescribe the drug during lactation, discontinuation of breastfeeding should be considered.

Similarities