Active substanceTerbinafineTerbinafine
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: terbinafine hydrochloride in terms of terbinafine 125 mg and 250 mg;

    Excipients: giprolase (hydroxy propyl cellulose), calcium stearate, silicon dioxide colloid (aerosil), croscarmellose sodium (impellose), microcrystalline cellulose.

    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, moldy mushrooms (ex. Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans. On mushrooms Candida spp. and their 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 cell membrane of the ergosterol fungus by inhibiting the enzyme squalene epoxidase.

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

    Pharmacokinetics:

    When taken orally, more than 70% is absorbed well; Absolute bioavailability due to the effect of "first passage" is reduced by 40%. After a single oral intake at a dose of 250 mg, the time to reach the maximum concentration (TCmax) is about 2 hours; the maximum concentration (Cmax) is approximately 1 μg / ml. Area under the curve "concentration - time" (AUC) - 4.5 mcg / ml, with simultaneous intake with food AUC increases by 20%. With long-term admission, C max is increased by 25%, AUC - 2.5 times. The effective half-life (T1 / 2) is about 36 hours, terminal T1 / 2 200-400 hours (indicates a prolonged excretion of skin and adipose tissue). The equilibrium concentration (Css) does not depend on age. The concentration of terbinafine in plasma does not depend on sex.

    The connection with plasma proteins is more than 99%. Rapidly distributed 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. Subject to significant biotransformation, the resulting metabolites do not have antifungal activity. 70% are excreted by the kidneys. Do not cum in the body. The age of the patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood.

    Excreted in breast milk.

    Indications:

    - Mycosis of the scalp (trichophytosis, microsporia).

    - Fungal diseases of the skin and nails (onychomycosis), caused by Trychophyton (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaccum), Microsporum (M. canis, M. gypseum) and Epidermophyton floccosum.

    - 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), lactation period, pregnancy.

    Carefully:Renal insufficiency (with creatinine clearance less than 50 ml / min), 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 during pregnancy. 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 are set individually and depend on the localization of the process and the severity of the disease.

    Adults:

    Inside, after eating.Usual dose: 250 mg once a day.

    Onychomycosis: the duration of therapy on average 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 if the patient is young, the duration of the treatment may be less than 12 weeks. If infection of the thumb of the foot is usually enough 3-month course of treatment. Some patients who have a reduced rate of nail growth may need a longer period of treatment.

    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 - 2-4 weeks; with fungal infections caused by fungi of the genus Candida - 2-4 weeks;

    with mycosis of the scalp caused by fungi of the genus Microsporum - More than 4 weeks.

    Children: usually prescribed 125 mg. The duration of mycosis treatment of the scalp is about 4 weeks, when infected Microsporum canis - may be longer.

    With a body weight of 20 to 40 kg, 125 mg once a day.

    With a body weight of more than 40 kg, 250 mg once a day.

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

    Patients with hepatic and renal insufficiency terbinafine prescribe a dose of 125 mg once a day.

    Side effects:

    Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less than 1/10000, including individual cases.

    From the nervous system: often - headache; infrequent - a violation of taste, including their loss (usually recovery occurs within a few weeks after cessation of treatment); very rarely - a decrease in appetite and weight loss, dizziness, paresthesia, hyperoscension.

    From the skin:

    very often - skin reactions (including rash, hives);

    very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, psoriasis-like rashes on the skin, exacerbation of existing psoriasis, alopecia. In case of progressing skin rash, treatment with terbinaphin should be discontinued.

    From the hepatobiliary system: rarely - hepatobiliary dysfunction (mostly of a cholestatic nature), very rarely - severe hepatic insufficiency (some with fatal outcome or requiring liver transplantation).

    In most cases, when hepatic insufficiency developed, patients had serious comorbid systemic diseases and the cause-and-effect relationship with terbinafine was doubtful.

    From the digestive system: very often - a feeling of overflow of the stomach, a decrease in appetite, indigestion, nausea, mild abdominal pain, diarrhea.

    From the musculoskeletal system:

    very often - arthralgia, myalgia.

    From the hematopoiesis: very rarely - neutropenia, agranulocytosis, pancytopenia. In the case of qualitative or quantitative changes in the blood constituents, consideration should be given to reducing the dose of the drug or, if necessary, to discontinue therapy.

    From the immune system:

    Very rarely - anaphylactoid reactions (including angioedema), cutaneous and systemic lupus erythematosus.

    Other: very rarely - a feeling of fatigue.

    Overdose:

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

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

    Interaction:

    Inhibits isoenzyme CYP2P6 and interferes with the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (for example,desipramia, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), monoamine oxidase B type inhibitors (eg, selegiline) and antipsychotic (for example, chlorpromazine, haloperidol) facilities.

    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.

    Terbinafine reduces 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 hepatoxic effect, there is a risk of developing drug damage to the liver.

    Special instructions:

    Irregular application of terbinafine or premature termination of treatment can 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 with onychomycosis at the beginning of the course of treatment.

    If after 2 weeks of treatment for a skin infection there is no improvement, it is necessary to repeatedly identify the pathogen and its sensitivity to the drug.

    Systemic use in onychomycosis is justified only in case of total nasal discharge, presence of pronounced subungual hyperkeratosis, ineffectiveness of previous local therapy.

    In the treatment of onychomycosis, a clinical response, confirmed laboratory, usually occurs 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 activity of hepatic 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, excessive abdominal pain, jaundice, darkening of the urine or discolored stool), the drug should be discontinued.

    The administration of terbinafine to psoriasis patients requires caution. 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) and at the end of it, it is necessary to produce antifungal treatment of shoes, socks and stockings.

    Effect on the ability to drive transp. cf. and fur:
    Form release / dosage:

    Tablets 125 mg and 250 mg.

    For 7 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 1, 2, 3, 4 contour mesh packages together with the instruction for use are placed 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
    (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
    Storage conditions:

    List B. In a dry, protected spotlight at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003798 / 01
    Date of registration:16.10.2009
    The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia
    Information update date: & nbsp20.09.2015
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