Qidokan

General characteristics. Structure:

Active ingredient: 250 mg of a terbinafin (in the form of a hydrochloride) in 1 tablet.

Excipients: silicon dioxide colloid (aerosil), calcium stearate, коллидон 30, primelloza (sodium of a kroskarmilloz), sugar milk (lactose), cellulose microcrystallic.

Pharmacological properties:

Pharmacodynamics. тербинафин 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. Scopulariopsis brevicaulis), 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 of 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 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.

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 collects in high concentration in hair follicles, in hair, skin and hypodermic cellulose.

Elimination half-life - 16-18 h, an elimination half-life of a terminal phase - 200-400 h.

It Biotransformirutsya in a liver to inactive metabolites; 80% of the accepted dose are removed through kidneys in the form of metabolites, other part (22%) – through intestines.

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.

Indications to use:

 ● Mycoses of a pilar part of the head (trichophytosis, microsporia).

 ● the Fungus diseases of skin and nails (onychomycoses) caused by Trychophyton (T. rubrum, mentagrophytes, verrucosum, violaceum), Microsporum (M. canis, M. gypseum) and Epidermophytom floccosum.

 ● 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: Inside, after food. Usual dose: 250 mg (1 tablet) of 1 times a day.

Onychomycoses: 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 the 3-month course of treatment is usually sufficient. 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 Candida - 2-4 weeks; at the mycoses of a pilar part of the head caused by Microsporum – 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.

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.

To patients with a liver and renal failure – 0,125 g once a day (at clearance of creatinine less than 50 ml/min. or concentration of creatinine in blood serum more than 300 µmol/l it is necessary to reduce a drug dose twice in comparison with a usual dose).

Features of use:

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.

Irregular use of a terbinafin or the premature termination of treatment can lead to a disease recurrence.

Such factors as 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 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 control the level 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, appetite loss, an excessive abdominal pain, jaundice, darkening of urine or a colourless chair) 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 a gigiyenydlyapredotvrashcheniye 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 drive the car and moving mechanisms: data on influence of drug on ability to drive the car and to perform the works demanding the increased concentration of attention no.

Side effects:

Dispepsichesky disturbances (loss of appetite, nausea, diarrhea, feeling of overflow of a stomach, abdominal pain); skin allergic reactions (urticaria, rash); musculoskeletal reactions (arthralgia, mialgiya), aggravation of a current of a system lupus erythematosus.

Disturbances of flavoring feelings, including their loss (recovery happens within several weeks after the treatment termination).

Extremely seldom (with a frequency of 0,01 - 0,1%) a hepatotoxic action (increase in activity of "hepatic" transaminases, a liver failure).

Malignant exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), psoriazopodobny enanthesis, exacerbation of psoriasis, anaphylactoid reactions, agranulocytosis or thrombocytopenia, neutropenia, lymphopenia.

Interaction with other medicines:

Inhibits an isoenzyme of CYP2D6 and interferes with metabolism of such drugs as tricyclic antidepressants and the selection inhibitors of serotonin reuptake (for example, desipramine, флувоксамин), β-adrenoblockers ((((((((((метопролол, propranolol), antiarrhythmic means (флекаинид, пропафенон), type monoamine oxidase inhibitors B (for example, селегилин) and antipsychotic (for example, Chlorpromazinum, a haloperidol).

Medicines - inductors of isoenzymes of P450 cytochrome (for example, rifampicin) can accelerate removal of a terbinafin from an organism.

Medicines - inhibitors of isoenzymes of P450 cytochrome (for example, 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 semi-removal for 31%.

Does not influence clearance of phenazone, digoxin, warfarin.

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 (clearance of creatinine less than 50 ml/min.), a lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption, 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, alcoholism, oppression of a marrowy hemopoiesis, tumor, metabolism disease, occlusal diseases of vessels of extremities.

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 purpose of absorbent carbon and/or symptomatic therapy.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg. On 7 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3 blister strip packagings together with the application instruction place in a pack from a cardboard.