Экзифин®

General characteristics. Structure:

Active agent: a terbinafina a hydrochloride of 281,31 mg (in terms of 250 mg of a terbinafin). Excipients: cellulose microcrystallic, sodium glycollate starched, starch prezhelatinizirovanny, magnesium stearate, silicon colloid anhydrous.

Description: White or almost white round biconvex tablets with a smooth surface on both sides.

Pharmacological properties:

Pharmacodynamics. Terbinafin treats group of allylamines, possesses a wide range of antifungal action. In low concentration has fungicidal effect on Trychophyton dermatophytes (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T.violaceum), Microsporum canis, Epidermophyton floccosum, mold mushrooms (e.g. Aspergillus, Cladosporium, Scopulariopsis brevicalius), barmy mushrooms, mainly Candida albicans, and some dimorphous mushrooms. Renders on mushrooms of Candida and its 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 of ergosterol by enzyme inhibition squalene-epoksidazy. Skvalen-epoksidaza it is not connected with system of P450 (SUR450) cytochrome therefore тербинафин does not influence metabolism of hormones and medicines which metabolism is connected with SUR450.
At oral administration collects in skin, nails and in hair in quantity, having fungicidal effect.
Multi-colored depriving system treatment, the caused Malassezia furfur, inefficiently.

Pharmacokinetics. At oral administration it is well absorbed, in 0,8 hours a half of the accepted dose is absorbed; in 4,6 hours a half of the accepted dose is distributed in an organism. In 1-2 hours after intake of single 250 mg of a dose the maximum concentration of drug in a blood plasma reaches 0,97 mkg/ml. Bioavailability of 80%. Meal does not influence bioavailability of a terbinafin. 1/5
Terbinafin intensively contacts proteins of a blood plasma (99%), quickly extends in fabrics, gets into a thermal layer of skin and nail plates. Gets into a secret of sebaceous glands and accumulates in high concentration in hair follicles, in hair, skin and in hypodermic cellulose. In several weeks of treatment collects in nails in the concentration providing fungicidal action. Semi-removal time - 16-18 h, time of semi-removal of a terminal phase - 200-400 h.
It Biotransformirutsya in a liver to inactive metabolites; 80% of the accepted dose are removed with urine in the form of metabolites, other part of 20% fecal masses. It does not kumulirutsya 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 together with breast milk.
Multi-colored depriving system treatment, the caused Malassezia furfur, inefficiently.

Indications to use:

Mycoses of a pilar part of the head (trichophytosis, microsporia). The mycoses of skin and nails caused by Trychophyton (T. rubrum, mentagrophytes, verrucosum, violaceum), Microsporum (M. canis, M. gypseum) Epidermophytom floccosum. Onychomycoses. The heavy, widespread dermatomycoses of smooth skin of a trunk and extremities demanding system treatment. Candidiases of skin and mucous membranes.

Route of administration and doses:

Duration of a course of treatment and the mode of dosing is set in an individual order and depends on localization of process and disease severity. Adult: Usual dose: 250 mg (1 tablet) once a day.

Therapy Onikhomikozy:prodolzhitelnost about 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 treatment can be less than 12 weeks. At a foot thumb infection the 3-month course of treatment is usually sufficient. In rare instances at the slowed-down growth rate of nails more prolonged treatment up to 6 and more months can be required.
2/5 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, a trunk - 4 weeks;
at the mycoses caused by Candida, 2-4 weeks;
at the mycoses of the head caused by Microsporum canis - more than 4 weeks.
To children: usually appoint 125 mg (1/2 tablets). Duration of treatment of mycoses of a pilar part of the head about 4 weeks, at Microsporum canis infection - can be longer.
At body weight less than 20 kg - 62,5 mg (1/4 tablets) of 1 times a day.
Weighing from 20 to 40 kg - 125 mg (1/2 tablets) of 1 times a day.
Weighing more than 40 kg - 250 mg (1 tablet) of 1 times a day.
The elderly patient drug is appointed in the same doses, as the adult. At the expressed abnormal liver functions and/or kidneys (clearance of creatinine <50 ml/min. or concentration of creatinine in blood more than 300 µmol/l): 125 mg once a day.

Features of use:

Irregular use of a terbinafin or the premature termination of treatment leads to a disease recurrence.
Such factors as e.g. existence of associated diseases, condition of nails 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, usually, is 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 during 3 weeks and an onychomycosis of feet during 6 weeks is not required.

In the presence of a heavy renal failure (clearance of creatinine less than 50 ml/min. or creatinine in blood more than 300 µmol/l), at an abnormal liver function it is necessary to reduce a dose of a terbinafin twice.

In the presence of a liver disease the clearance of a terbinafin can be reduced.

At reduced function of a liver appoint a half an adult dose. During treatment it is necessary to control the level of transaminases of a liver 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, loss of appetite, an abdominal pain, jaundice, darkening of urine or a colourless chair) drug should be cancelled.

Purpose of a terbinafin sick psoriasis demands the increased discretion since it seldom or never тербинафин can provoke the outbreak 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 (each 2 weeks) and at the end of it it is necessary to make antifungal processing of footwear, socks and stockings.

Influence on ability to drive the car and working mechanisms: тербинафин does not influence ability to drive the car and to perform the works demanding the increased concentration of attention.

Side effects:

Side effects of usually average and easy severity are also temporary. Often found side effects from bodies of system of digestion: the feeling of the crowded stomach, dyspepsia, nausea, loss of appetite, an abdominal pain, diarrhea, is not frequent - disturbance of flavoring perception, including its loss which is recovered in several weeks after the treatment termination; seldom - a cholestasia, jaundice, hepatitis, asymptomatic increase in level of transaminases of a liver. Despite an absence of proof of a causal relationship of these disturbances with reception of a terbinafin, in case of development of gepatobiliarny dysfunction treatment by Ekzifin should be stopped. From TsNS: seldom - paresthesia, a gipoesteziya, dizziness, it is very rare - a depression, feeling of the increased alarm. From a musculoskeletal system: often arthralgia, mialgiya. From system of a hemopoiesis: very seldom neutropenia, agranulocytosis, thrombocytopenia. From immune system: often a small tortoiseshell, a mnogoformny erythema, it is rare - system allergic reactions (reactions similar a serum disease, an angio-odem), is very rare - heavy skin reactions (a toxic epidermal necrolysis, a syndrome Stephens-Johnson, photosensitivity). When progressing skin rashes treatment terbinafiny should be stopped. Other: often a headache, feeling sick, feeling of fatigue, it is very rare - a psoriasis ekzatserbation, the strengthened hair loss.

Interaction with other medicines:

Practically does not influence clearance of the drugs which are metabolized with P450 cytochrome participation (e.g. cyclosporine, терфенадин, Tolbutamidum, to triazoles, oral contraceptives).

Inhibits CUP2D6 isoenzyme and interferes with metabolism of such drugs as tricyclic antidepressants and the selection blockers of serotonin reuptake (e.g. desipramine, флувоксамин), [31 - blockers (метопролол, propranolol), antiarrhythmic means (флекаинид, проавфенон), MAO-B - inhibitors (e.g. селегилин) and antipsychotic (e.g. Chlorpromazinum, a haloperidol). Medicinal drugs inductors of SUR450 enzymes (e.g. rifampicin) can accelerate removal of a terbinafin from an organism.  

The medicinal drugs-inhibitors SUR450 (e.g. Cimetidinum) can slow down metabolism and removal of a terbinafin from an organism. At simultaneous use of these drugs dose adjustment of a terbinafin can be required. Disturbance of a menstrual cycle at a concomitant use of a terbinafin and oral contraceptives is possible.
Reduces clearance of caffeine by 21% and prolongs time of its half-decay for 31%. Does not influence clearance of antipyrine, digoxin, warfarin.
Ethanol and other gepatotoksichny drugs increase risk of development of hepatotoxic effect.

Contraindications:

Hypersensitivity to any component of drug; children's age up to 2 years since there is no enough data on drug use by children with body weight less than 12 kg; pregnancy; feeding period breast.
With care: Liver and/or renal failure, alcoholism; blood diseases; tumors; metabolism diseases; pathology of vessels of extremities, psoriasis.
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, pains in the lower part of a stomach, in epigastric area.
Treatment: a gastric lavage with the subsequent purpose of absorbent carbon and/or symptomatic therapy.

Storage conditions:

Period of validity 3 years. Not to use after the period of validity specified on packaging. Storage conditions In the dry place protected from light at a temperature up to 25 °C. In the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 250 mg: On 4 tablets in PVC / aluminum blisters. On 4, 5, 7, or 10 blisters are packed into a cardboard pack with the Application instruction.