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

Excipients: before the preparation of a tablet with a mass of 0.390 g of silicon, colloidal dioxide is 2 mg; Calcium stearate monohydrate (calcium stearic acid 1-wave) - 2 mg Potato starch - 29 mg Microcrystalline cellulose (MCC-200) - 47 mg Lactose monohydrate-8 mg Crospovidone (polyplasdone XL -10) - 8 mg Crospovidone (polyplasdone XL) - 8 mg Povidone K 90 (plasdone K-90) 5 mg

Description:

Tablets are white or almost white in color, with a weak specific odor, a flat-cylindrical shape 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 Trychophyton spp. (T. rubrum, T. mentagrophytes, T. tonsurans, T.vermcosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, moldy mushrooms (eg, Scopulariopsis brevicaulis), yeasts mushrooms, the main manner Candida albicans. On mushrooms Candida spp. and their filamentous forms in depending on the type of fungus fungicidal or fungistatic action.

Terbinafine disrupts the early stage of biosynthesis of the main component of the cell membrane of the fungus (ergosterol) by inhibiting the enzyme squalene epoxidase.

When administered orally, it is not effective in the treatment of multi-colored lichen, caused by Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics:

When taken orally, more than 70% is absorbed well; Absolute bioavailability due to the effect of "first passage" is reduced by 40%. After a single oral intake at a dose of 250 mg, the time to reach the maximum concentration (TCmax) is about 2 hours; the maximum concentration (C max) is 1 μg / ml. Area under the curve "concentration - time" (AUC) - 4.56 μg * h / ml, with simultaneous intake with food AUC increases by 20%. With prolonged admission, the Stakh increases by 25%, AUC - 2.5 times. The effective half-life (T1 / 2) is about 36 hours, terminal T1/2 200-400 h (indicates a prolonged excretion of the skin and adipose tissue). The equilibrium concentration (Css) does not depend on age. The concentration of terbinafine in plasma does not depend on sex.

The connection with plasma proteins is more than 99%. Rapidly distributed 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. Subject to significant biotransformation, the resulting metabolites do not have antifungal activity. 70% are excreted by the kidneys.

Do not cum 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.

Excreted in breast milk.

Indications:

- Mycosis of the scalp (trichophytosis, microsporia).

-fungal diseases of the skin and nails (onychomycosis), conditioned Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum.

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

- Candidiasis of the skin and mucous membranes.

Contraindications:

Hypersensitivity to the components of the drug; chronic or active liver disease, chronic renal failure (creatinine clearance less than 50 ml / min), children under 3 years old and weighing up to 20 kg (for this dosage form), lactation period, pregnancy, lactase deficiency, lactose intolerance , glucosogalactose malabsorption.

Carefully:

Renal insufficiency (with creatinine clearance more than 50 ml / min), alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive 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 excreted in breast milk, so its purpose is contraindicated during breastfeeding.

Dosing and Administration:

The duration of the course of treatment and the dosage regimen are set individually and depend on the localization of the process and the severity of the disease.

Adults:

Inside, after eating. Usual dose: 250 mg once a day.

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

Fungal skin infections: duration of treatment with interdigital, plantar or as a "socks" of infection localization is 2-6 weeks, with mycoses of other parts of the body: shins - 2-4 weeks, trunks - 2-4 weeks; with fungal infections caused by fungi of the genus Candida - 2-4 weeks;

with mycosis of the scalp caused by fungi of the genus Microsporum - More than 4 weeks.

For children:

With a body weight of 20 to 40 kg, 125 mg once a day.

With a body weight of more than 40 kg, 250 mg once a day.

The duration of mycosis treatment of the scalp is about 4 weeks, when infected Microsporum canis - may be longer.

Older patients prescribe the drug in the same doses as adults.

Patients with hepatic and renal insufficiency terbinafine prescribe a dose of 125 mg once a day.

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. Disturbances in taste, including their loss (recovery occurs within a few weeks after cessation of treatment). Rarely (with a frequency of 0.01-0.1%) observed 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 use of activated charcoal and / or symptomatic therapy.

Interaction:

Inhibits isoenzyme CYP2D6 and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (eg, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), monoamine oxidase B inhibitors (e.g., selegiline) and antipsychotic (for example, chlorpromazine, haloperidol) facilities.

Drugs - inductors of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the metabolism and 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.

Terbinafine reduces 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 hepatoxic effect, there is a risk of developing drug damage to the liver.

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 with onychomycosis 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, a clinical response, confirmed laboratory, usually observed a few months after mycological cure and the termination of the course of treatment, which is due to the rate of regrowth of a healthy nail.Removal of nail plates in the treatment of onychomycosis of brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

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

During treatment, it is necessary to monitor the activity of the "Hepatic" transaminases in the blood 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, decreased appetite, excessive abdominal pain, jaundice, darkening of the urine, or discolored stools), the drug should be discontinued.

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:

Form release / dosage:

Tablets 250 mg.

Packaging:For 10 or 14 tablets in a contour mesh box made of a polyvinyl chloride film and aluminum foil with a thermo lacquer. One or two 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:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008787/10

Date of registration:26.08.2010

The owner of the registration certificate:MOSCOW PHARMACEUTICAL FACTORY, CJSC MOSCOW PHARMACEUTICAL FACTORY, CJSC Russia

Manufacturer: & nbsp

MOSCOW PHARMACEUTICAL FACTORY, CJSC Russia

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Terbinafine-MFF (Terbinafine-MFF)