Terbinafin-Tev

General characteristics. Structure:

Active agent: a terbinafina a hydrochloride of 281,3 mg (250 mg of a terbinafin are equivalent)
excipients: cellulose of microcrystallic, 40,5 mg; carboxymethylstarch (type A), 36,0 mg; gipromelloza, 7,5 mg; silicon dioxide of colloid 1,2 mg; magnesium stearate of 3,5 mg

Description
White or almost white biconvex tablets of a kapsulovidpy form. On one of the parties dividing risk and an engraving of "T" on both parties risks.

Pharmacological properties:

Pharmacodynamics. Terbinafin treats group of allylamines, possesses a wide range of antifungal action. In low concentration, mainly, Candida albicans has fungicidal activity concerning dermatophytes (Trychophyton rubrum, Trychophyton mentagrophytcs, Trychophyton tonsurans, Trychophyton verrucosum, Trychophyton violaccum, Microsporum canis, Epidermophyton floccosum), barmy mushrooms. Activity concerning barmy mushrooms, depending on their look, can be fungicidal or fungistatic.

Terbinafin breaks an early stage of biosynthesis of the main component of a cellular membrane of a mushroom (ergosterol) by skvalenepoksidaza enzyme inhibition.

At oral administration it is inefficient at treatment multi-colored depriving, the caused Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics. At intake more than 70% are absorbed. Absolute bioavailability owing to effect of "the first passing" decreases by 40%. After a single dose inside in a dose of 250 mg time of achievement of the maximum concentration (TCmax) about 2 h; the maximum concentration (Cmax) - 1 mkg/ml. The area under a curve "concentration - time" (AUC) - 4.56 mkg x h/ml, at a concomitant use with AUC food increases by 20%. At long reception of Cmax AUC - by 2.5 times increases by 25%. An effective elimination half-life (T1/2) - about 36 h, terminal T1/2 200-400 h (points to long removal from skin and fatty tissue). Equilibrium concentration (Css) does not depend on age. Concentration of a terbinafin in plasma does not depend on a floor.

Communication with proteins of plasma - more than 99%. It is quickly distributed in fabrics, gets into a thermal layer of skin and nail plates. Gets into a secret of sebaceous glands and collects in high concentration in hair follicles, in hair, skin and hypodermic cellulose. Is exposed to considerable biotransformation, the formed metabolites have no antifungal activity. 70% are removed by kidneys. Does not kumulirut in an organism. The age of patients does not influence pharmacokinetics of a terbinafin, however elimination can decrease at damages of kidneys or a liver, resulting in high concentration of a terbinafin in blood. It is allocated with breast milk.

Indications to use:

- Mycoses of a pilar part of the head (trichophytosis, microsporia).
- The fungus diseases of skin and nails (onikhompkoza) caused by Trychophyton spp. (T. rubrum, T. mcntagrophytcs, T. vcrrucosum, T. violaceum), Microsporum spp. (M. canis, M. gypscum) and Epidcrmophyton floccosum.
- The heavy, widespread dermatomycoses of smooth skin of a trunk and extremities demanding system treatment.
- Skin candidiases.

Route of administration and doses:

Inside, after food.

Adult
250 mg of 1 times a day.

To children 3 years are more senior
At body weight from 20 to 40 kg - 125 mg of 1 times a day.
At body weight more than 40 kg - 250 mg of 1 times a day.

It is not required to elderly patients of dose adjustment.

To patients from a chronic renal failure (KK more than 50 ml/min.) - 125 mg once a day.

Duration of treatment depends on indications and disease severity.

Fungal infections of skin: treatment duration at interdigital, bottom or as "socks" of localization of an infection makes 2-6 weeks; at mycoses of other body parts: shins - 2-4 weeks, trunks — 2-4 weeks; at the mycoses caused by sort Candida mushrooms - 2-4 weeks; at mycoses of a pilar part of the head - about 4 weeks, at Microsporum canis infection - more than 4 weeks.

Onychomycosis: therapy duration on average 6-12 weeks. At damage of nails of fingers of brushes and feet (except for a foot thumb), or at young age of the patient duration of treatment can be less than 12 weeks. At an infection of a thumb of foot of usually rather 3-month course of treatment. Longer term of treatment can be required by some patients at whom the growth rate of nails is reduced.

Features of use:

Irregular use of a terbinafin or the premature termination of treatment can lead to a disease recurrence. If in 2 weeks of treatment of a skin infection improvement of a state is not noted, it is necessary to define repeatedly an infestant and its sensitivity to drug.

System use at an onychomycosis is justified only in case of defeat of the majority of nails, existence of the expressed hyponychial hyperkeratosis, inefficiency of the previous local therapy. At treatment of an onychomycosis the clinical answer confirmed laboratory is usually observed in several months after mycologic treatment and the termination of a course of treatment that is caused by the speed of growth of a healthy nail. Removal of nail plates at treatment of an onychomycosis of brushes within 3 weeks and an onychomycosis of feet within 6 weeks is not required.

In the presence of a liver disease the clearance of a terbinafin can be reduced. During treatment it is necessary to carry out control of indicators of activity of "hepatic" transaminases in blood serum.

In rare instances in 3 months of treatment there is a cholestasia and hepatitis. At emergence of signs of an abnormal liver function (weakness, persistent nausea, a loss of appetite, an excessive abdominal pain, jaundice, darkening of urine or decoloured by kcal) drug should be cancelled.

Purpose of a terbinafin sick psoriasis demands care since it seldom or never тербинафин can provoke an exacerbation of psoriasis.

At treatment terbinafiny it is necessary to follow the general rules of hygiene for prevention of a possibility of repeated infection through linen and footwear. In the course of treatment (in 2 weeks) and at the end of it it is necessary to make antifungal processing of footwear, socks and stockings.

Influence on ability to driving of the car and to control of mechanisms
Terbinafin does not exert impact on ability to drive the car and to work with the equipment. However it is necessary to take into account that during treatment there can be dizziness.

Side effects:

Frequency of development of side effects is classified according to recommendations of 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%; seldom - not less than 0,01%, but less than 0,1%; very seldom - less than 0,01%, including isolated cases.

From the alimentary system: very often - feeling of overflow of a stomach, a loss of appetite, dyspepsia, nausea, an abdominal pain, diarrhea; infrequently - disturbances or loss of flavoring feelings (recovery happens within several weeks after the treatment termination), increase in activity of "hepatic" transaminases; seldom - a cholestasia, jaundice, hepatitis; in some cases - the long frustration of flavoring feelings leading to refusal of meal and considerable decrease in body weight, a liver failure.

From blood and lymphatic system: very seldom - a neutropenia, thrombocytopenia, an agranulocytosis, a lymphopenia, isolated cases of a pancytopenia.

From integuments: very seldom — psoriazopodobny rash, an exacerbation of psoriasis, an acute generalized pustular dieback.

Allergic reactions: very often - rash, urticaria; very seldom - a Quincke's disease, a malignant epidermal erythema (Stephens-Johnson's syndrome), anaphylactoid reactions, a toxic epidermal necrolysis (Lyell's disease).

From a musculoskeletal system: very often — an arthralgia, a mialgiya.

From the central and peripheral nervous system: often — a headache; seldom - paresthesia, a giposteziya, dizziness; very seldom - a depression, feeling of alarm.

From an acoustic organ and labyrinth disturbances: very seldom - вертиго.

Others: seldom - an indisposition, weakness; very seldom - a system lupus erythematosus, including a skin form.

Interaction with other medicines:

Dose adjustment of a terbinafin at simultaneous use with inhibitors and inductors of isoenzymes of P450 cytochrome which can slow down and accelerate removal of a terbinafin from an organism is required. Cimetidinum reduces the speed of removal of a terbinafin by 30%, and rifampicin increases the speed of removal of a terbinafin by 100%. The researches in vitro and in vivo showed what тербинафин, inhibiting CYP2P6 isoenzyme, breaks metabolism of tricyclic antidepressants, selective serotonin reuptake inhibitors (desipramine, флувоксамин), beta adrenoblockers (метопролол, propranolol), antiarrhythmic means (a flekainid, a propafenon), monoamine oxidase inhibitors B (селегилин) and antipsychotic means (Chlorpromazinum, a haloperidol).

Terbinafin significantly does not influence the speed of removal of a tolbutamin, terfinadin, triazolam, peroral contraceptive means which are metabolized by means of other isoenzymes of P450 cytochrome (except for CYP2P6 isoenzyme).

Terbinafin does not influence the speed of removal of antipyrine and digoxin. At a concomitant use of a terbinafin and peroral contraceptive means disturbance of a menstrual cycle can develop. Terbinafin can increase efficiency of caffeine, due to increase in its concentration in plasma and reductions in the rate of removal from an organism for 21%.

Terbinafin can lower the speed of removal from a desipramine organism by 82%.

Terbinafin can lower efficiency of cyclosporine, due to decrease in its concentration in plasma by 15%.

At simultaneous use with warfarin can influence indicators of the prothrombin test: a blood clotting time and the international normalized relation.

At combined use with the ethanol or drugs possessing gepatoksichesky action there is a risk of development of medicinal damage of a liver.

Contraindications:

Hypersensitivity to drug components; chronic or active diseases of a liver, a chronic renal failure (the clearance of creatinine (CC) less than 50 ml/min.), children's age up to 3 years and with body weight to 20 kg (for this dosage form), the lactation period, pregnancy.

With care
Chronic renal failure (KK more than 50 ml/min.), alcoholism, oppression of a marrowy hemopoiesis, tumor, metabolism disease, occlusal diseases of vessels of extremities.

Use at pregnancy and feeding by a breast
Reception of a terbinafin during pregnancy is contraindicated due to the lack of enough data on its safety during pregnancy. Terbinafin is allocated with breast milk therefore its appointment is contraindicated during breastfeeding.

Overdose:

Symptoms: nausea, vomiting, a headache, dizziness, a gastralgia, the speeded-up urination, rash.
Treatment: a gastric lavage with the subsequent use of absorbent carbon. If necessary carry out symptomatic therapy.

Storage conditions:

To store at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets of 250 mg.
On 7 tablets in the blister from polyvinylchloride and aluminum foil.
On 1,2 or 4 blisters together with the application instruction in a cardboard pack.