Active substanceTerbinafineTerbinafine
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  • Dosage form: & nbsppills
    Composition:

    Active substance:

    Terbinafine hydrochloride - 281.25 mg

    (in terms of terbinafine - 250 mg)

    Excipients: Croscarmellose sodium 48 mg, microcrystalline cellulose 35.2 mg, lactose monohydrate 23.95 mg, hypromellose hydroxypropyl methylcellulose 6.2 mg, magnesium stearate for the pharmaceutical industry 4 mg, silicon dioxide colloid (aerosil) 1.4 mg.

    Description:

    Tablets are white or white with a yellowish tint of color, flat-cylindrical with a facet and a risk.

    Pharmacotherapeutic group:antifungal agent
    ATX: & nbsp

    D.01.A.E.15   Terbinafine

    Pharmacodynamics:

    Terbinafine belongs to the group of allylamines, it has a wide spectrum of antifungal action. At low concentrations, it has a fungicidal effect on dermatophytes Trychophyton (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (naire. Aspergillus, Cladosporium, Scopulariopsis brevicalius), yeast fungi, mainly Candida albicans, and some dimorphic fungi. On mushrooms Candida-and its filamentous forms, depending on the type of fungus, fungicidal or fungistatic action.

    Terbinafine disrupts the early stage of biosynthesis of the main component of the cellular membrane of the ergosterol fungus by inhibiting the squalene-epoxidase enzyme.

    When administered orally, it is not effective in treating varicoloured hair loss caused by Malassezia furfur.

    Pharmacokinetics:

    when taken orally absorbed well, after 0.8 hours absorbed half of the dose taken !; After 4.6 hours half of the dose taken is distributed in the body. After 1-2 hours after taking a single 250 mg dose, the maximum concentration of the drug in the blood plasma reaches 0.97 μg / ml. Bioavailability of 80%.Eating does not affect the bioavailability of terbinafine.

    Terbinafine binds intensely to plasma proteins (99%), spreads rapidly in tissues, penetrates the dermal layer of the skin and nail plates. Penetrates into the secretion of sebaceous glands and accumulates in high concentrations in the hair follicles, in hair, skin and subcutaneous tissue.

    The half-life is 16-18 hours, the half-life of the terminal phase is 200-400 hours. Biotransformed in the liver to inactive metabolites; 80% of the dose taken is excreted in the urine in the form of metabolites, the rest (22%) - with calves. Not cumulated in the body. The age of the patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with kidney or liver lesions, leading to high concentrations of terbinafine in the blood.

    It is excreted together with breast milk.

    Indications:

    Mycosis of the scalp (trichophytosis, microsporia).

    Mycosis of the skin and nails, conditioned Trychophyton (T. rubrum, mentagrophytes, verrucosum, violaceum), Microsporum (M. canis, M.gypseum) and Epidermophyton floccosum.

    Onychomycosis.

    Heavy, common dermatomycosis smooth skin of the trunk and extremities, requiring systemic treatment.

    Candidiasis of the skin and mucous membranes.

    Contraindications:

    Hypersensitivity to any component of the drug; Children under 3 years old and weighing up to 20 kg (for this dosage form), the period of breastfeeding.

    Carefully:

    hepatic and / or renal failure, alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities.

    Pregnancy and lactation:

    Pregnancy and lactation: the intake of terbinafine during pregnancy is contraindicated due to the lack of sufficient data on its safety during pregnancy.

    Terbinafine is excreted in breast milk, therefore its purpose is contraindicated in the period of breastfeeding.

    Dosing and Administration:

    The duration of the course of treatment and the dosage regimen is set individually and depends on the localization of the process and the severity of the disease.

    Adults:

    Usual dose: 250 mg (1 tablet) once a day.

    Onychomycosis: the duration of therapy is about 6-12 weeks. If the fingers and toes of the hands and feet (with the exception of the thumb of the foot) are affected, or when the patient is young, the duration of treatment may be less than 12 weeks.If a big toe infection is present, a 3-month course of treatment is usually sufficient. In rare cases, with a slower rate of nail growth, longer treatment may be required up to 6 months or more.

    Fungal skin infections: the duration of treatment with interdigital, plantar, or "socks" infection is 2-6 weeks, with mycoses of other parts of the body: shins - 2-4 weeks, trunk - 4 weeks; with fungal infections caused by Candida, 2-4 weeks; with mycosis of the head caused by Microsporum canis - more than 4 weeks.

    Children: usually prescribed 125 mg (1/2 tablet). Duration of treatment of mycosis of the scalp about 4 weeks, when infected Microsporum canis - may be longer. At a weight of 20 to 40 kg, 125 mg once a day.

    At a mass of more than 40 kg-250 mg once a day.

    Older patients prescribe the drug in the same doses as adults.

    In severe violations of the liver and / or kidney function, creatinine clearance <50 ml / min or a creatinine concentration in the blood of more than 300 μmol / l): 125 mg once a day.

    Side effects:

    Dyspeptic disorders (decreased appetite, nausea, diarrhea, feeling of stomach overflow, abdominal pain); skin allergic reactions (urticaria, rash); musculo-skeletal reactions (arthralgia, myalgia), aggravation of the systemic lupus erythematosus.

    Disturbances in taste, including their loss (recovery occurs within a few weeks after cessation of treatment).

    Very rarely: hepatobiliary disorders (cholestatic jaundice), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions, agranulocytosis or thrombocytopenia, neutropenia, lymphopenia.

    Overdose:

    Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region.

    Treatment: gastric lavage followed by prescription of activated charcoal and / or symptomatic therapy.

    Interaction:

    Inhibits isoenzyme CYP2D6 and interferes with the metabolism of drugs such as tricyclic antidepressants and selective blockers of seizure of serotonin (eg Desipramine, fluvoxamine), β1-blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), MAO-B inhibitor (selegiline) and antipsychotic (for example, chlorpromazine, haloperidol).

    Medications - enzyme inducers CYP450 (e.g. rifampicin) can accelerate the excretion of terbinafine from the body.

    Medicinal preparations - inhibitors CYP450 (e.g. cimetidine) can slow the metabolism and excretion of terbinafine from the body. With the simultaneous use of these drugs, a dose adjustment of terbinafine may be required.

    Possible violation of the menstrual cycle with the simultaneous administration of terbinafine and oral contraceptives.

    Reduces the clearance of caffeine by 21%, prolongs its half-life by 31%.

    Does not affect the clearance of phenazone, digoxin, warfarin.

    When combined with ethanol or drugs that have a hepatotoxic effect, there is a risk of developing drug-induced liver damage.

    Special instructions:

    Irregular application of terbinafine or premature termination of treatment lead to a relapse of the disease.

    The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the condition of the nails at the beginning of the course of treatment.

    If after 2 weeks of treatment there is no improvement, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.

    Systemic use in onychomycosis is justified only in case of total defeat of most nails, the presence of pronounced subungual hyperkeratosis, ineffectiveness of previous local therapy.

    In the treatment of onychomycosis, the clinical response is usually observed a few months after mycological cure and cessation of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

    In the presence of severe renal failure (creatinine clearance less than 50 ml / min or creatinine in the blood more than 300 μmol / L), if the liver function is disrupted, the dose of terbinafine should be reduced by half.

    In the presence of liver disease, terbinafine clearance can be reduced.

    With reduced liver function, a half of the adult dose is prescribed. During treatment, it is necessary to control the level of liver transaminases in the blood serum. In rare cases, after 3 months of treatment, there is cholestasis and hepatitis. If there are signs of impaired liver function (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice, darkening of the urine or colorless stools), the drug should be discarded.

    The administration of terbinafine to psoriasis patients requires increased discretion; in very rare cases terbinafine can trigger an outbreak of psoriasis.

    When treating terbinafine, general hygiene rules should be followed to prevent the possibility of re-infection through linens and shoes. In the process of treatment (after 2 weeks) and at the end it is necessary to produce antifungal treatment of shoes, socks and stockings.

    Effect on the ability to drive transp. cf. and fur:terbinafine does not affect the ability to drive and perform work that requires increased concentration.
    Form release / dosage:

    Tablets of 250 mg.

    7 or 10 tablets in a planar cell packaging made of a polyvinylchloride film and aluminum foil.

    1, 2, 3 or 4 contour squares with instructions for use in a pack of cardboard.
    Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
    (10) - packings, cellular, outline (2) - packs, cardboard
    (10) - packings, cellular, outline (3) - packs, cardboard
    (10) - packings, cellular, outline (4) - packs, cardboard
    (10) - packings, cellular planimetric (500) - cardboard boxes
    (7) - packings, cellular, planimetric (1) - packs, cardboard
    (7) - packings, cellular, outline (2) - packs, cardboard
    (7) - packings, cellular planimetric (3) - packs cardboard
    (7) - packings, cellular, outline (4) - packs, cardboard
    (7) - packings, cellular planimetric (500) - cardboard boxes
    Storage conditions:

    Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N001366 / 03
    Date of registration:25.11.2008
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp21.09.2015
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