Active substanceTerbinafineTerbinafine
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  • Dosage form: & nbsppills
    Composition:

    One tablet contains:

    Active substance: terbinafine hydrochloride 281.3 mg, in terms of terbinafine (100% substance) 250 mg;

    Excipients: microcrystalline cellulose (for medical purposes), crospovidone (kollidone CL-M), Povidone - K30 (kollidon 30), silicon dioxide colloid (aerosil), benzoic acid, magnesium stearate.

    Description:Tablets of flat-cylindrical form with a risk, white or white with a yellowish tint of color.
    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. verrucosum, T. violaceum, T. tonsurans), Microsporum canis, Epidermophyton floccosum, mold fungi (eg, 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 disrupts the early stage of biosynthesis of the main component of the cell 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.

    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. 1-2 hours after ingestion of a single 250 mg dose, the maximum concentration of the drug in the blood plasma reaches 0.97 μg / ml. Bioavailability of 80%. Food intake 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. It penetrates into the secretion of the sebaceous glands and accumulates in a high concentration in the hair follicles, in the hair, in the skin and in the 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 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, but the rate of excretion can decrease with renal and hepatic damage, leading to high concentrations of terbinafine in the blood.

    Excreted in 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) 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 the components of the drug, chronic or active liver disease, chronic renal failure (creatinine clearance less than 50 ml / min), children under 3 years old and weighing up to 20 kg (for this dosage form), the period of breastfeeding.

    Carefully:renal failure, alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities.
    Pregnancy and lactation:

    The intake of terbinafine during pregnancy is contraindicated due to the lack of sufficient data on its safety in pregnant women.

    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 determined individually and depends on the localization of the process and the severity of the disease.

    Adults:

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

    Onychomycosis: 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 damaged or the patient's young agethe 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 mycosis 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.

    Elderly patients correction of the dose is not required.

    Children: usually prescribed 125 mg / day (1/2 tablet). Duration of mycosis treatment ^ the scalp about 4 weeks, when infected Microsporum cams - may be longer.

    At a weight of 20 kg 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 (when creatinine clearance is more than 50 ml / min) - 125 mg (1/2 tablet) once a 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 reactions: 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 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 inhibitors of serotonin uptake (eg, desipramine, fluvoxamine), P-adrenoblockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), MAO-B-inhibitors (selegiline) and 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 or early termination of treatment increases the risk of relapse. The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the state 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 at the 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 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 brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

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

    During treatment, it is necessary to monitor the level of hepatic transaminases in the 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 linen and shoes. In the process of treatment (after 2 weeks), as well as at the end of treatment, it is necessary to produce antifungal treatment of shoes, socks and stockings.

    Effect on the ability to drive transp. cf. and fur:

    Data on the effect of the drug on the ability to drive a car and perform work that requires increased concentration of attention are not available.

    Form release / dosage:

    Tablets of 250 mg.

    For 7 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered. One or two contour mesh packages together with instructions for use in a pack of cardboard.

    Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
    (10) - packings, cellular, outline (2) - packs, cardboard
    (7) - packings, cellular, planimetric (1) - packs, cardboard
    (7) - packings, cellular, outline (2) - packs, cardboard
    Storage conditions:

    List B. Store at a temperature not exceeding 20 ° C.

    Keep out of the reach of children.

    Shelf life:2 years.Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N002270 / 01
    Date of registration:12.09.2008
    The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp21.09.2015
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