Terbinafine-OBL - instructions for use, dose, side effects, contraindications

Excipients: silicon dioxide colloid (aerosil), calcium stearate, kollidon 30, impellose (croscarmellose sodium), milk sugar (lactose), microcrystalline cellulose.

Description:Tablets are white or almost white in color, flat-cylindrical, with a facet and a risk.

Pharmacotherapeutic group:Antifungal agent

ATX: & nbsp

D.01.A.E.15 Terbinafine

Pharmacodynamics:

Terbinafine belongs to the group of allylamines, it has a wide spectrum of antifungal action. At low concentrations, it has a fungicidal effect on dermatophytes Trichophyton (T. rubrum, T. mentagrophytes, T. tonsurans, T.verrucosum, T.violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (ex. Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans. On mushrooms Candida spp. and their filamentous forms, depending on the type of fungus, fungicidal or fungistatic action.

Terbinafine disrupts the early stage of biosynthesis of the main component of the cellular membrane of tribe ergosterol by inhibiting the enzyme squalene oxidase.

When administered orally, it is ineffective in treating varicoloured hair loss caused by Pityrosporum ovale, Pityrosporum orbiculare, Malassezia furfur.

Pharmacokinetics:

When taken orally, it is absorbed well, after 0.8 hours half of the dose is absorbed; After 4.6 hours half of the dosed dose is distributed in the body. After 1-2 hours after taking a single 250 mg dose, the maximum concentration of the drug in the blood plasma reaches 0.97 m kg / ml. Bioavailability of 80%.Food intake does not affect the bioavailability of terbinafine.

Terbinafine binds intensely to blood plasma proteins (99%), spreads rapidly in tissues, penetrates the dermal layer of the skin and nail plates. Penetrates into the secretion of sebaceous glands and accumulates in high concentrations in the hair follicles, in hair, skin and subcutaneous tissue.

The half-life is 16-18 hours, the half-life of the terminal phase is 200-400 hours. Biotransformed in the liver to inactive metabolites; 80% of the accepted dose is excreted through the kidneys in the form of metabolites, the rest (22%) - through the intestine.

He is cumulated in the body. The age of the patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood.

It is excreted together with breast milk.

Indications:

- Mycosis by the scalp (trichophytosis, microsporia).

- DSkin and nail diseases (onychomycosis) caused by Trychophyton (T. rubrum, mentagrophytes, verrucosum. violaceum), Microsporum (M. canis, M. gypscum) and Epidermophytom floccosum.

- Heavy, common dermatomycosis smooth skin of the trunk and extremities, requiring systemic treatment.

- Candidiasis of the skin and mucous membranes.

Contraindications:

Hypersensitivitythe to the components of the drug; chronic or active liver disease, chronic renal failure(clearancewith creatinine less than 50 ml / min), lactose intolerance, lactase deficiency or glucose-galactose malabsorption, children's age up to 3 years and with a body weight of up to 20 kg (for this dosage form), lactation period, pregnancy.

Carefully:Renal insufficiency, alkogolism, oppression of the medullary hematopoiesis, tumors, bfall ill metabolism, occlusal diseases of the vessels of the extremities.

Pregnancy and lactation:

The intake of terbinafine during pregnancy is contraindicated due to the lack of sufficient data on its safety during pregnancy.

Terbinafine is excreted in breast milk, therefore its purpose is contraindicated in the period of breastfeeding.

Dosing and Administration:

The duration of the course of treatment and the dosage regimen is established on an individual basis and depends on the localization of the process and the severity of the disease.

Adults:

Inside, after eating.

Usual dose: 250 mg (1 tablet) once a day.

Onychomycosis: the duration of therapy is 6-12 weeks on average.If the fingers and toes of the hands and feet (with the exception of the thumb of the foot) are damaged, or if the patient is young, the duration of the treatment may be less than 12 weeks. If a big toe infection is present, a 3-month course of treatment is usually sufficient. Some patients who have a reduced rate of nail growth may need a longer period of treatment.

Fungal skin infections: duration of treatment npand interdigital, plantar, or "socks" localization of infection is 2-6 weeks, with fungal infections of other parts of the body: shins - 2-4 weeks, trunks - 2-4 weeks; with fungal infections caused by Candida - 2-4 weeks; with mycosis of the scalp caused by Microsporum - More than 4 weeks.

For children: usually prescribed 125 mg (1/2 tablet). Duration of treatment of mycosis of the scalp about 4 weeks, after infection Microsporum canis - may be longer.

At a weight of 20 to 40 kg - 125 mg (1/2 tablet) once a day.

At a weight of more than 40 kg - 250 mg (1 tablet) once a day.

The elderly the drug is administered in the same doses as and adults.

Patients with hepatic and renal insufficiency - 0,125 g once a day (with creatinine clearance less than 50 ml / min or a serum creatinine concentration of more than 300 μmol / L, the dose of the drug should be reduced by a factor of 2 compared to the usual dose).

Side effects:

Dyspeptic disorders (decreased appetite, nausea, diarrhea, feeling of stomach overflow, abdominal pain); skin allergic reactions (urticaria, rash); musculo-skeletal reactions (arthralgia, myalgia), aggravation of the systemic lupus erythematosus.

Disorders of gustatory sensations, including their loss (recovery occurs within a few weeks after cessation of treatment).

Very rarely (with a frequency of 0.01-0.1%) hepatotoxic effect (increased activity of "liver" transaminases, hepatic insufficiency).

Malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), psoriasis-like skin rashes, exacerbation of psoriasis, anaphylactoid reactions, agranulocytosis or thrombocytopenia, neutropenia, lymphopenia.

Overdose:

Symptoms: nausea, vomiting, headache, dizziness, pain in the lower abdomen, in the epigastric region, frequent urination.

Treatment: gastric lavage followed by the administration of activated charcoal and / or symptomatic therapy.

Interaction:

Inhibits isoenzyme CYP2D6 and interferes with the metabolism of drugs such as tricyclic antidepressants and selective inhibitors of serotonin uptake (eg, desipramine, fluvoxamine), β-adrenoblockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), monoamine oxidase B type inhibitors (eg, selegiline) and antipsychotic (for example, chlorpromazine, haloperidol).

Drugs - inductors of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the excretion of terbinafine from the body.

Drugs - inhibitors of cytochrome P450 isoenzymes (for example, cimetidine) can slow the metabolism and excretion of terbinafine from the body. With the simultaneous use of these drugs, a dose adjustment of terbinafine may be required.

Possible violation of the menstrual cycle with the simultaneous administration of terbinafine and oral contraceptives.

Decreases caffeine clearance by 21% and prolongs its half-life by 31%.

Does not affect the clearance of phenazone, digoxin, warfarin.

When combined with ethanol or drugs that have a hepatotoxic effect, there is a risk of developing drug-induced liver damage.

Special instructions:

Irregular application of terbinafine or premature termination of treatment can lead to a relapse of the disease.

The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the condition of the nails at the beginning of the course of treatment.

If after 2 weeks of treatment for a skin infection there is no improvement, it is necessary to repeatedly identify the pathogen and its sensitivity to the drug.

Systemic use in onychomycosis is justified only in case of total defeat of most nails, the presence of pronounced subungual hyperkeratosis, ineffectiveness of previous local therapy.

In the treatment of onychomycosis, the clinical response is usually observed a few months after mycological cure and discontinuation of treatment, which is due to the rate of regrowth of a healthy nail.

Removal of nail plates in the treatment of onychomycosis of the brushes for 3 weeks and onychomycosis of the feet for 6 weeks is notit takes.

In the presence of liver disease, terbinafine clearance can be reduced.

During treatment, it is necessary to monitor the level of hepatic transaminases in the serum. In rare cases, after 3 months of treatment, there is cholestasis and hepatitis. If there are signs of impaired liver function (weakness, persistent nausea, loss of appetite, excessive abdominal pain, jaundice, darkening of the urine or colorless stools), the drug should be discarded.

The administration of terbinafine to psoriasis patients requires caution. in very rare cases terbinafine can provoke an exacerbation of psoriasis.

When treating terbinafine, general hygiene rules should be followed to prevent the possibility of re-infection through linens and shoes. In the process of treatment (after 2 weeks) and at the end of it, it is necessary to produce antifungal treatment of shoes, socks and stockings.

Effect on the ability to drive transp. cf. and fur:Data the effect of the drug on the ability to drive and perform work that requires increased concentration of attention, there.

Form release / dosage:

Tablets, 250 mg.

Packaging:

For 7 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002630 / 01

Date of registration:22.07.2008 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp10.01.2017

Illustrated instructions

Instructions

Terbinafine-OBL (Terbinafine-OBL)