Брамизил®

General characteristics. Structure:

Active ingredient: 0,125 g or 0,25 g of a terbinafin in 1 tablet.

Excipients: microcrystallic cellulose, a gipromeloza, sodium glikolit starch, aerosil (silicon dioxide colloid), magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Terbinafin, represents allylamine and possesses a wide range of antifungal action. It is active concerning such dermatophytes as Trichophyton (T.rubrum, T.mentagrophytes, T.tonsurans, T.verrucosum, T.violaceum), Microsporum canis, Epidermophyton floccosum. In low concentration has fungicidal effect concerning dermatophytes, mold mushrooms (Aspergillus, Cladosporium, Scopulariopsis brevicaulis, etc.) and some dimorphous mushrooms. Action on barmy mushrooms of the sort Candida and its mitselialny forms can be fungicidal or fungistatic, depending on a species of a mushroom. Terbinafin is active also concerning Pityrosporum - the activator multi-colored (scaly) depriving of Pityriasis versicolor caused by Pityrosporum ovale.

Terbinafin breaks the synthesis of ergosterol happening in mushrooms by inhibition of enzyme of the skvalenepoksidaza located on a cellular membrane of a mushroom. It leads to deficit of ergosterol and to intracellular accumulation of squalene that causes death of a cell of a mushroom.

Pharmacokinetics. Food does not influence bioavailability. After a single dose of a terbinafin inside in a dose of 250 mg the maximum concentration of drug in a blood plasma is reached in 2 hours and makes 0,97 mkg/ml. Drug is well absorbed at oral administration (about 70%), bioavailability makes 40%. Terbinafin intensively contacts proteins of a blood plasma (99%), quickly gets into a thermal layer of skin and collects in a corneous layer of skin and nail plates, providing fungicidal action. Quickly gets into a secret of sebaceous glands, leading to creation of high concentration in hair follicles, hair, in skin, hypodermic cellulose.

It Biotransformirutsya in a liver with formation of inactive metabolites; about 70% of the accepted dose are removed with urine.

The elimination half-life of drug makes about 17 hours. An elimination half-life in a terminal phase - 200-400 h. It does not kumulirutsya in an organism. Changes of equilibrium concentration of a terbinafin depending on age are not revealed, at patients with a renal failure or at patients with cirrhosis the speed of removal of drug can be slowed down that results in higher concentration of a terbinafin in a blood plasma.

Indications to use:

- onychomycoses;
- mycoses of a pilar part of the head (trichophytosis, microsporia);
- fungus diseases of smooth skin - treatment of widespread dermatomycoses of a trunk and extremities;
- candidiases of skin and mucous, the sorts Candida caused by mushrooms - when localization or prevalence of process cause expediency of peroral therapy.

Route of administration and doses:

Duration of a course of treatment and the mode of dosing is set individually and depends on localization of process and disease severity.

The adult usually appoint inside after food 1 tab. (250 mg) once a day. To patients with a liver and renal failure - 1/2 tablets (125 mg) once a day.

Mycoses of integuments. The recommended treatment duration:
- a dermatomycosis of feet (interdigital, bottom or as "socks"): 2-6 weeks;
- a dermatomycosis of a trunk, extremities - 2-4 weeks;
- candidiasis of skin and mucous - 2-4 weeks.

Total disappearance of clinical displays of a disease is observed, as a rule, in several weeks after mycologic treatment

Mycoses of a pilar part of the head. The recommended treatment duration:
- mycosis of a pilar part of the head - about 4 weeks.
- mycoses of a pilar part of the head are observed preferential at children.

Onychomycoses. Duration of a course of treatment drug at most of patients makes 6 - 12 weeks. At an onychomycosis of brushes in most cases makes 6 weeks, and at an onychomycosis of feet - 12 weeks. More prolonged treatment can be required by some patients who have the reduced growth rate of nails. The optimum clinical effect is observed several months later after mycologic treatment and the termination of therapy. It is defined by that span which is necessary for growth of a healthy nail.

Use of drug for children. To children drug is appointed since two years. The dose depends on the body weight of the child and makes:
- for children with body weight to 20 kg - 62,5 mg/days (1/4 tablets);
- from 20 kg to 40 kg - 125 mg/days (½ tablets);
- more than 40 kg - 250 mg/days (1 tablet).

Data on use of drug for children under two years (with body weight less than 12 kg) are not available.

Features of use:

Irregular use or the early end of treatment increases risk of development of a recurrence.

If in 2 weeks of treatment improvement of a state is not noted, it is necessary to define repeatedly an infestant and its sensitivity to drug. It is necessary to be careful at Bramizil's appointment inside the patient with abnormal liver functions and (or) kidneys. At identification of the symptoms allowing to assume abnormal liver functions (lack of appetite, fatigue, persistent nausea, jaundice, dark urine), it is necessary to cancel drug. Patients with chronic abnormal liver functions and kidneys should appoint a half of the usual recommended dose of drug and to control indicators of functions of a liver and kidneys in the course of treatment.

Unlike Bramizil for topical administration, Bramizil of a tablet is not effective at multi-colored herpes.

In process and at the end of treatment it is necessary to make antifungal processing of footwear, socks and stockings.

Pregnancy and lactation. Experience of use of drug at pregnancy is limited therefore it is not necessary to apply Bramizil at pregnancy. Terbinafin is allocated with breast milk therefore in need of purpose of drug it is necessary to resolve an issue of the breastfeeding termination.

Influence on ability to drive the car and to work with mechanisms. Data on Bramizil's influence on ability to drive the car and to work with mechanisms are absent.

Side effects:

Bramizil in general is had well. Side effects are usually expressed poorly or moderately and have passing character.

At intake can be observed:
- from digestive tract and a liver: dyspepsia, abdominal pains, feeling of overflow of a stomach, nausea, appetite loss, diarrhea; sometimes disturbance of flavoring feelings, including their loss (it is recovered in several weeks after the treatment termination);
- from a musculoskeletal system: muscle pains, joint pains.
- from system of a hemopoiesis: a neutropenia, an agranulocytosis, thrombocytopenia, it is rare - a lymphopenia.
- allergic reactions: skin rash in the form of spots, blisters, it is rare - a toxic epidermal necrolysis, Stephens-Johnson's syndrome, anaphylactoid reactions.

Interaction with other medicines:

Terbinafin in vitro has extremely small ability to change clearance of the majority of drugs which are metabolized with the participation of system of P 450 cytochrome (for example, cyclosporine, a terfenadin, Tolbutamidum, a triazolam or oral contraceptives).

At the women who are at the same time accepting тербинафин and oral contraceptives, disturbance of a menstrual cycle can be observed. The general clearance of a terbinafin can accelerate medicines which cause induction of enzymes of P450 cytochrome (for example, rifampicin) and can be slowed down by medicines - inhibitors of the tsitokhromny P450 system (for example, Cimetidinum), in need of simultaneous use of these drugs dose adjustment can be required.

Reduces clearance of caffeine by 20%.

Bramizil does not influence clearance of antipyrine, digoxin, warfarin.

Ethanol and other gepatotoksichny drugs increase risk of development of a hepatotoxic.

Contraindications:

Hypersensitivity to the terbinafin or any other component which is a part of drug.

With care - alcoholism, diseases of blood, a tumor, a metabolism disease, pathology of vessels of extremities. Children's age - up to 2 years.

Overdose:

So far cases of overdose of Bramizil at intake in the recommended doses are not described. At acute overdose of drug development of nausea, vomiting, pains in epigastric area is possible.

Treatment: a gastric lavage with the subsequent purpose of absorbent carbon; in case of need - a symptomatic maintenance therapy.

Storage conditions:

List B. In protected from light and the place, unavailable to children, at a temperature not above 25 °C. 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 125 mg or 250 mg. On 10, 14 tablets in banks polymeric. On 10, 14 tablets in a blister strip packaging. 1, 2 blister strip packagings, each can together with the application instruction are placed in a pack from a cardboard.