Active substanceTerbinafineTerbinafine
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains

    active substance: terbinafine hydrochloride 281.3 mg (equivalent to 250 mg terbinafine) Excipients: microcrystalline cellulose 40.5 mg; sodium carboxymethyl starch (type A) 36.0 mg; hypromellose 7.5 mg; silicon dioxide colloidal 1,2 mg; magnesium stearate 3.5 mg

    Description:

    White or almost white biconvex tablets capsular shaped.On one side of the dividing risk and the engraving "T" on both sides of the risks.

    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,

    fungicidal activity against dermatophytes (Trychophyton rubrum, Trychophyton mentagrophytes, Trychophyton tonsurans, Trychophyton

    verrucosum, Trychophyton violaceum, Microsporum canis, Epidermophyton floccosum), yeast fungi, mainly, Candida albicans. Activity with respect to yeast fungi, depending on their type, may be fungicidal or fungistatic.

    Terbinafine disrupts the early stage of biosynthesis of the main component of the cell membrane of the fungus (ergosterol) by inhibiting the enzyme squalene epoxidase.


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

    Pharmacokinetics:

    When ingestion absorbs more than 70%. 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 (Stach) is 1 μg / ml.Area under the curve "concentration - time" (AUC) - 4.56 μg * h / ml, with simultaneous intake with food AUC increases by 20%. When; ' long-term admission of the Stakh increases by 25%, AUC - 2.5 times. Effective half-life (T1/2) - about 36 hours, terminal T1 / 2 200-400 h (indicates a prolonged excretion of the 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%. It is quickly distributed in the tissues, penetrates the dermal layer, the skin: and the nail plates. Penetrates into the secretion of sebaceous glands and accumulates in high concentrations in the hair follicles, in hair, skin and subcutaneous tissue. It is subject to significant biotransformation, the resulting metabolites do not possess ' antifungal activity. 70% are excreted by the kidneys.

    Do not cum in the body. The age of patients does not affect the pharmacokinetics.: Terbinafine, however, elimination may decrease with kidney or liver lesions, 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 spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum.

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

    - Candidiasis of the skin.

    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 of age and with body weight up to 20 kg (for this dosage form), lactation period, pregnancy.

    Carefully:

    Chronic renal failure (QC more 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, therefore, its purpose is contraindicated in the period of breastfeeding.

    Dosing and Administration:

    Inside, after eating.

    Adults: 250 mg once a day.

    Children over 3 years old:

    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.

    Elderly patients correction of the dose is not required.

    Patients with chronic renal failure (QC greater than 50 mL / min) -125 mg once a day.

    The duration of treatment depends on the indications and severity of the disease. Fungal infections of the skin: the duration of treatment with interdigital, plantar, or "socks" localization of infection is 2-6 weeks; with mycoses of other parts of the body: shins - 2-4 weeks; torso - 2-4 weeks; with fungal infections caused by fungi of the genus Candida - 2-4 weeks; at mycosis of the scalp - about 4 weeks, when infected Microsporum cams - more than 4 weeks.

    Onychomycosis: the duration of therapy is 6-12 weeks on average. 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 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.

    Side effects:

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%,but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including isolated cases.

    From the digestive system: very often - a feeling of overflow of the stomach, a decrease in appetite, indigestion, nausea, abdominal pain, diarrhea; infrequent- or loss of taste sensations (recovery occurs within: a few weeks after discontinuation of treatment), an increase activity "hepatic" transaminases; rarely - cholestasis, jaundice, hepatitis; in some cases, long-term eating disorders, leading to a failure to eat and a significant decrease in body weight, liver failure.

    From the side of the blood and lymphatic system: very rarely - neutropenia, thrombocytopenia, agranulocytosis, lymphopenia, single cases of pancytopenia.

    From the skin: very rarely - psoriasis-like rash, exacerbation of psoriasis, acute generalized pustular exanthema. Allergic reactions: Often- -. rash, hives; very rarely - angioedema, malignant epidermal erythema (Stevens-Johnson syndrome), anaphylactoid reactions, toxic epidermal necrolysis (Lyell's syndrome).

    From the musculoskeletal system: very often - arthralgia, myalgia.

    From the central and peripheral nervous system: often headache; rarely - paresthesia, hyposthenia, dizziness; very rarely - depression, anxiety.

    From the side of the hearing organ and labyrinthine disorders: very rarely - vertigo. Other: rarely - malaise, weakness; very rarely - - systemic lupus erythematosus, including cutaneous form.

    Overdose:

    Symptoms: nausea, vomiting, headache, dizziness, gastralgia, frequent urination, rash.

    Treatment: gastric lavage followed by application activated carbon. If necessary, conduct symptomatic therapy.

    Interaction:

    It is necessary to correct the dose of terbinafine while using cytochrome P450 isoenzymes with inhibitors and inducers that can slow and accelerate the excretion of terbinafine from the body. Tsimitidin reduces the rate of excretion of terbinafine by 30%, and rifampicin increases the rate of excretion of terbinafine by 100%.

    Research in vitro and in .vivo showed that terbinafine, inhibiting the isoenzyme CYP2P6, disrupts the metabolism of tricyclic antidepressants, selective serotonin reuptake inhibitors (desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), monoamine oxidase B inhibitors (selegiline) and antipsychotic drugs (chlorpromazine, haloperidol). Terbinafine does not significantly affect the rate of excretion of tolbutamine, terfenadine, triazolam, oral contraceptives, which are metabolized by other cytochrome P450 isoenzymes (excluding the isoenzyme CYP2P6).

    Terbinafine does not affect the rate of excretion of antipyrine and digoxin.

    With the simultaneous administration of terbinafine and oral contraceptives, a menstrual cycle can develop.

    Terbinafine can enhance the effectiveness of caffeine, by increasing its plasma concentrations and reducing the rate of excretion by 21%. Terbinafine can reduce the rate of excretion of desipramine from the body by 82%

    Terbinafine can reduce the effectiveness of cyclosporine, by reducing its plasma concentration by 15%.

    When used simultaneously with warfarin, it can affect the indices - the prothrombin test: the time of blood coagulation. and the international normalized attitude.

    When combined with ethanol or drugs that have a hepatoxic effect, there is a risk of developed drug lesions of the liver.

    Special instructions:

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

    If after 2 weeks, the treatment of skin infection is not marked improvement, the condition, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.

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

    In the treatment of onychomycosis, a clinical response, confirmed laboratory, 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 the 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. When there are signs of impaired liver function (weakness, persistent nausea, decreased appetite, excessive abdominal pain, jaundice, darkening of urine or discolored feces) the drug should be discarded.

    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:Terbinafine does not affect the ability to drive and work with machinery. However, one should take into account that dizziness may occur during treatment.
    Form release / dosage:

    Tablets 250 mg

    7 tablets in a blister made of polyvinyl chloride and aluminum foil.

    For 1, 2 or 4 blisters together with instructions for use in a cardboard pack.

    Packaging:(7) - blister (1) / 1 blister together with instructions for use in a cardboard box / - cardboard pack
    blister (2) / 2 blisters together with instructions for use in a pack of cardboard / - a pack of cardboard
    blister (4) / 4 blisters together with instructions for use in a pack of cardboard / - a pack of cardboard
    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 expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-000103
    Date of registration:23.12.2010
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Information update date: & nbsp20.09.2015
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