Active substanceTerbinafineTerbinafine
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  • Dosage form: & nbspPills
    Composition:

    1 tablet contains:

    active substance: terbinafine hydrochloride (equivalent to

    terbinafine) 140.625 mg (125 mg) / 281.25 mg (250 mg); Excipients: sodium carboxymethyl starch - 22.625 mg / 45.25 mg; hypromellose - 6.0 mg / 12.0 mg; silicon dioxide colloidal - 0.75 mg / 1.5 mg; potato starch - 29.0 mg / 58.0 mg; magnesium stearate 1.0 mg / 2.0 mg.

    Description:white or almost white, round, biconvex tablets, with a circular risk in the middle of the tablet and engraved "TER 125 "for tablets of 125 mg or "TER 250 "for tablets 250 mg on one side.
    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. Active against dermatophytes Trychophyton (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum, T. monsurans), Microsporum canis, Epidermophyton floccosum; molds (Scopulariopsis brevicaulis), yeast fungi of the genus Candida (FROM. albicans) and some dimorphic fungi.

    The effect on yeast fungi and its micellar forms can be fungicidal or fungistatic, depending on the type of fungus. Terbinafine specifically suppresses the early stage of the sterol biosynthesis in the fungal cell. This leads to a deficiency of ergosterol and to intracellular accumulation of squalene, which causes death of the fungal cell. 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 P450 system. Terbinafine does not affect the metabolism of hormones or other medications.

    Pharmacokinetics:

    After a single administration of terbinafine inwards at a dose of 250 mg, the maximum concentration (Cmax) of the drug in the blood plasma is achieved after 2 hours and is 0.97 μg / ml. Terbinafine well absorbed by oral intake, 0.8 hours absorbed half of the dose, after 4.6 hours half of the dose is distributed in the body. Food intake has an insignificant effect on bioavailability, so dose adjustment is not required.

    Terbinafine binds well to blood plasma proteins (99%), quickly penetrates the dermal layer of the skin and accumulates in the stratum corneum and nail plates, providing fungicidal action. Quickly penetrates into the secretion of the sebaceous glands, leading to the creation of a high concentration in the hair follicles, hair, in the skin, subcutaneous fat.

    Terbinafine undergoes rapid metabolism involving at least seven isoenzymes of cytochrome P450, with the main role being played by isozymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. As a result of biotransformation, metabolites are formed that do not possess antifungal activity. The half-life (T1/2) of terbinafine is 17 hours, T1/2 the terminal phase is 200-400 h.It is excreted by the kidneys in the form of metabolites (about 70%), the rest with the intestine.

    Do not cumulate. Excreted in breast milk.

    The patient's age does not affect the pharmacokinetics of terbinafine, but the rate of excretion may decrease with kidney and liver damage, leading to high concentrations of terbinafine in the blood.

    Indications:

    - onychomycosis;

    - mycoses of the scalp (trichophytosis, microsporia);

    - dermatomycosis (trunk and extremities), as well as yeast infections of the skin and mucous membranes caused by fungi poflf Candida (candidiasis) - in those cases where the localization, severity or prevalence of infection causes the advisability of oral therapy.

    Note: Terbinafine Sandoz® for oral use is not is effective for the treatment of varicoloured (pitybearing) lichen.

    Contraindications:

    - hypersensitivity to terbinafine or other components of the drug;

    - lactation period;

    - pregnancy;

    - children's age (up to 3 years and with a body weight of up to 20 kg);

    - chronic or active liver disease;

    - chronic renal failure (with creatinine clearance below 50 ml / min).

    Carefully:alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities, renal failure (with creatinine clearance above 50 ml / min), cutaneous lupus erythematosus, systemic lupus erythematosus, psoriasis, metabolic diseases.
    Pregnancy and lactation:

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

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

    Dosing and Administration:

    Inside, after eating. The duration of the course of treatment and the dosing regimen are determined individually and depend on the localization of the process and the severity of the course of the disease.

    Adults:

    250 mg once a day.

    Onychomycosis: duration of therapy is about 6 to 12 weeks. If the fingernails of the fingers and feet are damaged (except for the thumb of the foot), the duration of the treatment may be less than 12 weeks. Some patients who have a reduced rate of nail growth may require longer treatment.The optimal clinical effect is observed several months after mycological cure and discontinuation of therapy. This is determined by the time period that is necessary for the growth of a healthy nail.
    Mycosis of the scalp: duration of treatment 4 weeks. Dermatomycosis: recommended duration of treatment for dermatomycosis of feet (interdigital, plantar localization or localization of infection by the type of "socks") - 2 - 6 weeks; with dermatomycosis of the trunk, shins - 2 - 4 weeks; in mycosis, with fungal infections caused by fungi of the genus Candida 2-4 weeks.

    Children over 3 years:

    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.

    Duration of treatment of mycosis of the scalp about 4 weeks, when infected Microsporum cams - may be longer. Pa1} To patients with renal insufficiency Creatinine clearance> 50 ml / min or serum creatinine concentration> 300 μmol / L) - 125 mg once a day. Elderly patients dosage adjustment is not required. When prescribing the drug, elderly patients need to monitor the function of the liver and kidneys.
    Side effects:

    Most side effects are transient, transient in long-term treatment.

    According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, < 1/100), rarely (> 1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

    From the gastrointestinal tract:

    Often: nausea, abdominal pain, indigestion, diarrhea, bloating, decreased appetite; frequency unknown: pancreatitis.

    From the liver and biliary tract:

    rarely: hepatic insufficiency, up to a lethal outcome, increased activity of "liver" transaminases; frequency unknown: hepatitis, jaundice, stasis of bile.

    From the immune system.

    rarely: cutaneous lupus erythematosus, systemic lupus erythematosus; frequency is unknown: anaphylactic reactions, serum sickness. Allergic reactions: very common: rash, hives;

    rarely: anaphylactoid reactions, angioedema,

    polymorphic erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), acute generalized exentematous pustulosis;

    frequency is unknown: photosensitivity, polymorphic photo dermatosis.

    From the skin and subcutaneous tissues:

    rarely: psoriasis-like rash or exacerbation of psoriasis, alopecia.

    From the musculoskeletal and connective tissue: Often: arthralgia, myalgia; frequency unknown: rhabdomyolysis.

    On the part of the hematopoiesis system:

    rarely: neutropenia, lymphopenia, agranulocytosis, thrombocytopenia, pancytopenia;

    frequency unknown: anemia, increased activity of creatine phosphokinase in the blood.

    From the central and peripheral nervous system: often: headache;

    rarely: weakening of taste sensations, loss of taste sensations; rarely: dizziness, paresthesia, hypoesthesia;

    frequency is unknown: loss of smell, decreased sense of smell, anxiety, depression.

    From the sense organs:

    frequency unknown: ringing in the ears, hearing loss, gipakuziya.

    From the side of the cardiovascular system, the frequency is unknown: vasculitis.

    Other:

    rarely: fatigue, fatigue;

    frequency is unknown: pyrexia, malaise, weight loss,

    influenza-like syndrome.
    Overdose:

    Symptoms: dizziness, headache, nausea, vomiting, gastralgia, pain in the lower abdomen, frequent urination, rash.

    Treatment: Activated carbon, if necessary, symptomatic maintenance therapy.

    Interaction:

    Terbinafine is an inhibitor of the isoenzyme CYP2D6. This must be taken into account when prescribing the drug Terbinafine Sandoz® together with drugs that are metabolized with the participation of isoenzyme CYP2D6.

    Therefore, if a patient takes tricyclic antidepressants, selective serotonin reuptake inhibitors (desipramine, fluvoxamine), monoamine oxidase inhibitors of type B (selegiline), β-adrenoblockers (metoprolol, propranolol), antiarrhythmic (flecainide, propafenone) and antipsychotic agents (chlorpromazine, haloperidol), appoint Terbinafine Sandoz® should be taken with caution or it is necessary to correct its dose.

    The plasma clearance of terbinafine can be accelerated under the influence of drugs - inducers of cytochrome P450 (for example, rifampicin) and suppressed under the influence of cytochrome P450 inhibitors (for example, cimetidine).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.

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

    Rifampicin increases the clearance of terbinafine by 100% and reduces its concentration in the blood plasma (decreased terbinafine efficacy).

    Terbinafine reduces the clearance of caffeine by 19% and increases its concentration in blood plasma.

    When used simultaneously with warfarin terbinafine reduces prothrombin time (cause-effect relationship not established). Terbinafine can relax the action of cyclosporine and reduce its concentration in the blood plasma, increases the clearance of cyclosporine by 15%. Terbinafine does not affect the clearance of antipyrine, digoxin and phenazone. Terbinafine has no significant effect on the pharmacokinetics of fluconazole. There were no clinically significant interactions between terbinafine and cotrimoxazole components (trimethoprim, sulfamethoxazole), zidovudine, or theophylline.

    Terbinafine reduces the clearance of desipramine by 82%.

    Cimetidine reduces the plasma clearance of terbinafine by 33% and increases its concentration in the blood plasma (increased toxicity of the latter).
    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 condition of the nails (with onychomycosis) 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, a clinical response is usually observed a few months after mycological cure, confirmed by laboratory, and the cessation of treatment, which is due to the speed

    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.

    If there are liver diseases, 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, abdominal pain, jaundice, darkening of urine or acholic (colorless) feces), the drug should be discarded.

    The use of terbinafine in patients with psoriasis requires increased caution, because 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 at the end of treatment, it is necessary to produce antifungal treatment of shoes, socks and stockings.

    During the treatment, it is necessary to follow the general rules of hygiene to prevent reinfection (through underwear, shoes).

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

    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. If there is dizziness, do not drive vehicles or mechanisms.
    Form release / dosage:

    Tablets 125 mg or 250 mg.

    By 7, 10, 14, 21, 28, 42 tablets in a blister made of polyvinyl chloride and aluminum foil;

    on 1, 2, 3, 4, 6, 14 blisters on 7 tablets in a cardboard pack; 1, 2, 3, 10 blisters of 10 tablets each in a cardboard box; 1, 2, 3, 7 blisters with 14 tablets each in a cardboard box; 1, 2 blisters with 21 tablets each in a cardboard box; 1, 2 blisters of 28 tablets each in a cardboard box; 1, 2 blisters for 42 tablets in a cardboard box;

    For tablets 250 mg additionally:

    8 tablets in a blister of polyvinyl chloride and aluminum foil; on 1, 7 blisters on 8 tablets in a cardboard pack;

    In each pack put the instructions for use. For 14, 28, 56, 100 tablets in polyethylene bottles with screw caps. 1 bottle per cardboard pack together with instructions for use.

    Packaging:(10) - blisters (1) - packs of cardboard
    (10) - blisters (10) - packs of cardboard
    (10) - blisters (2) - packs cardboard
    (10) - blisters (3) - packs cardboard
    (100) - polyethylene bottles (1) - packs cardboard
    (14) - blisters (1) - packs cardboard
    (14) - blisters (2) - packs cardboard
    (14) - blisters (3) - packs cardboard
    (14) - blisters (7) - packs cardboard
    (14) - polyethylene bottles (1) - packs cardboard
    (21) - blisters (1) - packs cardboard
    (21) - blisters (2) - packs cardboard
    (28) - blisters (1) - packs cardboard
    (28) - blisters (2) - packs cardboard
    (28) - polyethylene bottles (1) - cardboard packs
    (42) - blisters (1) - packs cardboard
    (42) - blisters (2) - packs cardboard
    (56) - polyethylene bottles (1) - packs cardboard
    (7) - blisters (1) - packs cardboard
    (7) - blisters (14) - packs cardboard
    (7) - blisters (2) - packs cardboard
    (7) - blisters (3) - packs cardboard
    (7) - blisters (4) - packs cardboard
    (7) - blisters (6) - packs cardboard
    (8) - blisters (1) - packs cardboard
    (8) - blisters (7) - packs cardboard
    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Special precautions when destroying an unused preparation

    There is no need for special precautions when destroying an unused preparation.

    Shelf life:

    4 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-010031/09
    Date of registration:09.12.2009
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp20.09.2015
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