Active substanceTerbinafineTerbinafine
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  • Dosage form: & nbspPills
    Composition:

    1 tablet contains:

    Active substance: terbinafine hydrochloride - 281.25 mg, in terms of terbinafine - 250 mg.

    Excipients: hypromellose 15 cf., croscarmellose sodium, microcrystalline cellulose PH 101, microcrystalline cellulose PH 102, silicon dioxide colloid, magnesium stearate.

    Description:Round tablets are white, with a risk on one side, with a bevel.
    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 Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum, Microsporum canis, Epidermophyton floccosum, molds (for example Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans, and some dimorphic fungi. On mushrooms Candida and its mycelial forms, depending on the type of fungus, fungicidal or fungistatic action.

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

    When administered orally, it is ineffective in treating varicoloured hair loss caused by Pityrosporum ovale, Malassezia furfur.

    Pharmacokinetics:

    Well absorbed when taken orally, after 0.8 hours absorbed half of the dose; 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 a high concentration 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.

    Biotransformiruetsya in the liver with the formation of inactive metabolites; about 80% of the dose taken is excreted through the kidneys in the form of metabolites, the rest (20%) through the intestine. Do not cumulate. Excreted in breast milk. In patients with renal and / or hepatic insufficiency, the rate of excretion decreases.

    Indications:

    Mycosis of the scalp (trichophytosis, microsporia).

    Mycosis of the skin and nails, conditioned Trichophyton (eg, T.mbrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis, 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 terbinafine or other ingredients of the drug; children under 3 years old and weighing up to 20 kg (for this dosage form), pregnancy and lactation.Chronic or active liver disease, chronic renal failure (creatinine clearance less than 50 ml / min).

    Carefully:

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

    Pregnancy and lactation:the intake of terbinafine during pregnancy is contraindicated because of the lack of sufficient data on its safety in pregnant women. Terbinafine excreted in breast milk, so its purpose is contraindicated during 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 per day (1 tablet) 1 time per day.

    Onkkhomikoz: 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" localization of infection is 2-6 weeks, with fungal infections of other parts of the body: shins - 2-4 weeks, trunks - 4 weeks; with fungal infections caused by Candida 2-4 weeks; with mycosis of the head caused by Microsporum canis - More than 4 weeks. Elderly patients do not need dose adjustment.

    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.

    Patients with renal insufficiency (with creatinine clearance less than 50 ml / min) - 125 mg (1/2 tablets) 1 time per day.

    Side effects:

    On the part of the digestive system: indigestion, abdominal pain, feeling of stomach overflow, nausea, loss of appetite, diarrhea; sometimes a violation of taste, including their loss (restored several weeks after cessation of treatment); extremely rare (with a frequency of 0.01-0.1%) - hepatobiliary disorders (cholestatic jaundice,increased activity of "liver" transaminases, hepatic insufficiency).

    From the musculoskeletal system: arthralgia, myalgia.

    From the hemopoietic system: extremely rarely - agranulocytosis or thrombocytopenia, neutropenia, lymphopenia.

    Allergic reaction: urticaria, rash, extremely rarely - malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome) anaphylactoid reactions.

    Exacerbation of systemic lupus erythematosus.

    Overdose:

    Symptoms: dizziness, headache, nausea, vomiting, pain in the lower abdomen, in the epigastric region, frequent urination.

    Treatment: gastric lavage followed by administration of activated charcoal; if necessary, symptomatic maintenance therapy.

    Interaction:

    Inhibits isoenzyme CYP2D6 and interferes with the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (eg, desipramine, fluvoxamine), (3- adrenoblockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), MAO-B inhibitor (selegiline) antipsychotic (for example, chlorpromazine, haloperidol).

    Drugs - inductors of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the excretion of terbinafine from the body.

    Drugs - inhibitors of cytochrome P450 isoenzymes (for example, 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.

    Decreases caffeine clearance by 21% and 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 discontinuation of treatment leads 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 for the duration of therapy affects only with onychomycosis. If after 2 weeks of treatment there is noimprovement of the condition, it is necessary to repeatedly identify 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, a clinical response is usually observed a few months after mycological cure, confirmed laboratory and discontinuation of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of the brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

    When treating liver disease, terbinafine clearance can be reduced.

    During treatment, it is necessary to monitor the activity of hepatic transaminases in the blood serum. In rare cases, after 3 months of treatment, there is cholestasis and hepatitis. If there is evidence of liver dysfunction (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice, darkening of the urine or discolored stool), the drug should be discontinued.

    The administration of terbinafine to psoriasis patients requires increased discretion;in very rare cases terbinafine can provoke an exacerbation 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), as well as in 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.

    For 14 tablets in a blister of film (polyvinyl chloride-polyethylene-PVCH) and aluminum foil.

    For 1 or 2 blisters of 14 tablets, together with instructions for use in the pack.

    Storage conditions:List B. Store in a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008994/10
    Date of registration:31.08.2010
    The owner of the registration certificate:Nobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh. Turkey
    Manufacturer: & nbsp
    Representation: & nbspNobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh.Russia
    Information update date: & nbsp20.09.2015
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