Ekziter

General characteristics. Structure:

Active agent: a terbinafina a hydrochloride of 281 mg, in terms of тербинафин 250 mg.

Excipients: croscarmellose sodium — 12,3 mg, potato starch — 9,4 mg, povidone (polyvinylpirrolidone) — 12 mg, the water purified — 6,1 mg, magnesium stearate — 3,2 mg.

Pharmacological properties:

Pharmacodynamics. Terbinafin treats group of allylamines, possesses a wide range of antifungal action. In low concentration has fungicidal effect on Trychophyton spp dermatophytes. (T. rubrum, T. mentagrophytes, T. tonsurans, T.verrucosum, T.violaceum), Microsporum can is, Epidermophyton floccosum, barmy mushrooms, mainly Candida albicans. On Candida spp mushrooms. and renders their mitselialny forms depending on a species of a mushroom fungicidal or a fungistasis.
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 not effective at treatment multi-colored depriving, the caused Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics. At oral administration more than 70% are well 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 (Tstakh) about 2 h; maximum concentration (Stakh) about 1 mkg/ml. The area under a curve "concentration — time" (AUC) — 4.5 ¼¬ú*þ/ml, at a concomitant use with AUC food increases by 20%. At long reception Stakh increases by 25%, AUC — by 2.5 times. An effective elimination half-life (T1/2) — about 36 h, terminal T of 1Y 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 (onychomycoses) caused by Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum.
— The heavy, widespread dermatomycoses of smooth skin of a trunk and extremities demanding system treatment.
— Skin candidiases.

Route of administration and doses:

Duration of a course of treatment and the mode of dosing are established in an individual order and depend on localization of process and weight
diseases.
Adult:
Inside, after food. Usual dose: 250 mg of 1 times a day.
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.
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 the mycoses of a pilar part of the head caused by sort Microsporum mushrooms — more than 4 weeks.

To children:
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.
Duration of treatment of mycoses of a pilar part of the head makes about 4 weeks, at Microsporum canis infection — can be longer.
The elderly patient drug is appointed in the same doses, as the adult.
To patients with a renal failure (KK more than 50 ml/min.) тербинафин appoint in a dose 125 mg once a day.

Features of use:

Irregular use of a terbinafin or the premature termination of treatment can lead to a disease recurrence. Such factors as existence of associated diseases, a condition of nails at onychomycoses at the beginning of a course of treatment also can influence duration of therapy.
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 total 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 the decoloured chair) drug should be cancelled.
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 motor transport and to control of mechanisms
Influences of a terbinafin on ability to manage motor transport and to work with mechanisms it was not studied. At development of dizziness against the background of therapy by drug, patients should not manage motor transport and/or to work with mechanisms.

Side effects:

Frequency: very often — more than 1/10, it is frequent — more than 1/100 and less than 1/10, infrequently — more than 1/1000 and less than 1/100, is rare — more than 1/10000 and less than 1/1000, is very rare — less than 1/10000, including separate cases.
- From the alimentary system: very often — the feeling of overflow of a stomach, a loss of appetite, dyspepsia, nausea which are poorly expressed to an abdominal pain, diarrhea.
- From bodies of a hemopoiesis: very seldom — a neutropenia, an agranulocytosis, a pancytopenia. Seldom or never at use of drug development of qualitative or quantitative changes from uniform elements of blood (a neutropenia, an agranulocytosis, thrombocytopenia, a pancytopenia) was noted. In case of development of qualitative or quantitative changes from uniform elements of blood it is necessary to establish the reason of disturbances and to consider a question of a dose decline of drug or if necessary about the therapy termination.
- From immune system: very seldom — anaphylactoid reactions (including a Quincke's disease), a skin and system lupus erythematosus.
- From a nervous system: often — a headache; infrequently — disturbance of flavoring feelings, including their loss (usually recovery happens within several weeks after the treatment termination). There are separate messages on cases of long disturbances of flavoring feelings. In some cases against the background of administration of drug decrease in consumption of food which led to considerable reduction of weight was noted. Very seldom — dizziness, paresthesias, hypesthesias.
- From gepatobiliarny system: seldom — gepatobilparny dysfunction (preferential cholestatic nature), including very exceptional cases of development of a heavy liver failure (some from the death or the demanding transplantations of a liver).
- From integuments: very often — skin reactions (including rash, urticaria); very seldom — Stephens-Johnson's syndrome, a toxic epidermal necrolysis, a psoriazopodobny enanthesis, an exacerbation of the available psoriasis, an alopecia.
- From a musculoskeletal system: very often — an arthralgia, a mialgiya.
- Other: very seldom — feeling of fatigue.

Interaction with other medicines:

The plasma clearance of a terbinafin can accelerate under the influence of drugs — metabolism inductors and to be suppressed under the influence of P450 cytochrome inhibitors.
In need of simultaneous use of the above-stated drugs and a terbinafin the corresponding correction of the mode of dosing of the last can be required.
Cimetidinum reduces plasma clearance of a terbinafin by 33% and increases its concentration in plasma (increase in toxicity of the last). Rifampicin increases clearance of a terbinafin for 100% and reduces its concentration in plasma (decrease in efficiency of a terbinafin). Results of the researches conducted by in vitro and at healthy volunteers show what тербинафин has the insignificant potential for suppression or strengthening of clearance of the majority of drugs which are metabolized with the participation of system of P450 cytochrome (for example, a terfinadina, a triazolama, Tolbutamidum or oral contraceptives), except for those which are metabolized with participation of CYP2D6.
Terbinafin does not influence clearance of antipyrine or digoxin.
At a concomitant use with oral contraceptives disturbance of a menstrual cycle is possible.
Reduces clearance of caffeine at intravenous administration by 19% and increases its concentration in plasma (increase in toxicity of caffeine). In the researches in vitro and in vivo it was shown what тербинафин suppresses the metabolism mediated by enzyme 2D6 (CYP2D6). These data can be clinically significant for those drugs which are metabolized preferential by this enzyme: tritsikpichesky antidepressants, beta adrenoblockers, selective serotonin reuptake inhibitors, antiarrhytmic medicines I of a class, monoaminooxidase inhibitors In type — if the drug used at the same time has the small range of therapeutic concentration.
Terbinafin reduces clearance of desipramine by 82%.
Terbinafin can weaken effect of cyclosporine and reduce its concentration in plasma; increases clearance of cyclosporine for 15%.

Contraindications:

Hypersensitivity to drug components; chronic or active diseases of a liver, a chronic renal failure (clearance of creatinine 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
Renal failure (with clearance of creatinine more than 50 ml/min.), alcoholism, oppression of a marrowy hemopoiesis, a tumor, metabolism disease, occlusal diseases of vessels of extremities.

PREGNANCY AND LACTATION
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, pains in the lower part of a stomach, in epigastric area, the speeded-up urination.
Treatment: a gastric lavage with the subsequent use of absorbent carbon and/or symptomatic therapy.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. To store in unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 250 mg.
On 7,10,14 tablets place in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 10,14, 20,28, 30,40, 50 or 100 tablets place in a container polymeric for medicines. One container or 1, 2, 3, 4,5,6, 8 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard. Period of validity 3 years.
Not to use after expiry date.