Lamifen tablets 250 mg. №28

Description

Lamifen №28 Storage
active substance: terbinafine;

1 tablet contains terbinafine hydrochloride in a dose equivalent to 250 mg of terbinafine;

Excipients: microcrystalline cellulose, copovidone, polyethylene glycol (macrogol) 6000, potato starch, hypromellose (hydroxypropylmethylcellulose 50 cP), sodium starch glycolate (type A), croscarmellose sodium, silicon dioxide colloidal dioxide.

Lamifen №28 Dosage form
Tablets.

Basic physical and chemical properties: tablets of the flat-cylindrical form with a line and a facet, white or almost white color.

Lamifen №28 Pharmacotherapeutic group
Antifungal drugs for use in dermatology. Antifungal drugs for systemic use. Terbinafine. ATX code D01B A02.

Lamifen №28 Pharmacological properties

Pharmacodynamics

Terbinafine is an allylamine that has a broad spectrum of antifungal activity against skin, hair and nail infections caused by dermatophytes such as Trichophyton (eg T. rubrum,

T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum (eg Microsporum canis), Epidermophyton floccosum and yeasts of the genus Candida (eg Candida albicans) and Pityrosporum. At low concentrations, terbinafine has a fungicidal effect on dermatophytes, molds and some dimorphic fungi. The activity against yeast fungi can be fungicidal or fungistatic, depending on their species.

Terbinafine specifically promotes the early stage of sterol biosynthesis in the fungal cell. This leads to ergosterol deficiency and intracellular accumulation of squalene, which causes fungal cell death. The action of terbinafine is carried out by inhibiting the enzyme squalene epoxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system.

When used orally, the drug accumulates in the skin in concentrations that provide a fungicidal effect of the drug.

Pharmacokinetics

After oral administration, terbinafine is well absorbed (> 70%); the absolute bioavailability of terbinafine, which is part of Lamifen® in tablets, as a result of presystemic metabolism is about 50%. A single oral dose of 250 mg terbinafine showed a mean peak plasma concentration of 1.30 μg / ml 1.5 hours after dosing. At steady state compared to a single dose, the maximum concentration of terbinafine was on average 25% higher, and the plasma AUC increased 2.3 times. Based on the increase in plasma AUC, an effective half-life (~ 30 hours) can be calculated. Food intake has a moderate effect on the bioavailability of terbinafine (increased AUC by less than 20%), but not enough to require dose adjustment.

Terbinafine is highly bound to plasma proteins. It diffuses rapidly through the dermis and is concentrated in the lipophilic stratum corneum.

Indication
Fungal infections of the skin and nails caused by Trichophyton (eg T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum:

ringworm (trichophytia of smooth skin, trichophytia of the perineum and dermatophytia of the feet), when the location of the lesion, the severity or prevalence of the infection determine the appropriateness of oral therapy;
onychomycosis.

Contraindication
Hypersensitivity to terbinafine or to any of the excipients.