Exifin - instructions for use, dose, side effects, contraindications

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 (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum. moldy mushrooms (ex. Aspergillus, Cladosporium. Scopulariopsis brevicalius), yeast fungi, mainly Candida albicans, and some dimorphic fungi. On mushrooms Candida and its mycelial 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 the ergosterol fungus by inhibiting the squalene-epoxidase enzyme. Squalene-epoxidase is not associated with the cytochrome P450 (CD450) system, so terbinafine does not affect the metabolism of hormones and drugs, the metabolism of which is associated with SUR450.

When administered orally, it accumulates in the skin, nails and hair in an amount that has a fungicidal effect.

Systemic treatment of varicolored lichen caused by Malassezia furfur, inefficient.

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 dose taken 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 μg / ml. Bioavailability of 80%. Food intake does not affect the bioavailability of terbinafine.

Terbinafine binds intensely to plasma proteins (99%). quickly spreads in the tissues, penetrates the dermal layer of the skin and the nail plates. Penetrates the secretion of sebaceous glands and accumulates in high concentrations in the hair follicles, in hair, skin and in the subcutaneous tissue. After a few weeks of treatment, it accumulates in the nails in concentrations that provide fungicidal action. The half-life is 16-18 hours. The half-life of the germinal phase is 200-400 hours.

Biotraneformirhegsya in the liver to inactive metabolites: 80% Pripyat dose is excreted in the urine in the form of metabolites, the rest (20%) - with the feces. Not cumulated in the body. The age of the patients does not affect the pharmacokinetics of herbinafine. however, elimination may decrease with kidney or liver damage, leading to high concentrations of herbathin in the blood.

It is excreted together with breast milk.

Systemic treatment of varicolored lichen caused by Malassezia furfur, inefficient.

Indications:

- Mycosis of the scalp (trichophytosis, microsporia).

- Mycosis of the skin and nails, conditioned Trx chophvton (T. rubrum. mentagrophytes. verrucosum, violaceum). Microsporum (M. canis, M. gypseum) and Epidennophytom floccosum.

- Onychomycosis.

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

- Candidiasis of the skin and mucous membranes.

Contraindications:

Hypersensitivity to any component of the drug: children under 2 years of age, t. there is not enough data on the use of the drug by children weighing less than 12 kg, pregnancy, the period of breastfeeding.

Carefully:hepatic and / or renal insufficiency; alcoholism: blood diseases: tumors; metabolic diseases; pathology of the vessels of the extremities, psoriasis.

Pregnancy and lactation:

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

Terbipafine is excreted in breast milk. therefore its or his purpose is counter-indicative in the period of thoracal feeding.

Dosing and Administration:

The duration of the course of treatment and the dosage regimen is set individually and depends on the localization of the process and the severity of the disease. Adults:

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

Onychomycosis: Duration of therapy is about 6-12 weeks. If the fingers and toenails are injured (except for the big toe), or if the patient is young, the duration of the treatment may be less than 12 weeks. With a large toe infection, a 3-month course of treatment is usually sufficient. In rare cases, with a slower rate of nail growth, longer treatment may be required up to 6 months or more.

Fungal skin infections: The duration of treatment with interdigital, plantar, or "socks" localization of infection is 2-6 weeks .. with mycosis of other parts of the body: shins - 2-4 weeks .. trunk - 4 weeks: with mycoses caused by Candida. 2-4 weeks;

with mycosis of the head caused by Microsporum canis - more than 4 weeks.

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

With a body weight of less than 20 kg, 62.5 mt (1/4 tablet) once a day.

At a weight of 20 to 40 kg, 125 mg (1/2 tablet) 1 time per day.

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

The elderly the drug is prescribed in the same doses as for adults.

If the liver and / or night (creatinine clearance <50 ml / min or a creatinine concentration in the blood of more than 300 μmol / l): 125 mt 1 time per day.

Side effects:

Side effects are usually of medium and mild severity and are of a temporary nature. Frequently occurring side effects fromopaboutaboutsystems Pseekingevary: feeling of a full stomach, dyspepsia, nausea, loss

appetite, abdominal pain, diarrhea, not often - a violation of taste perception, in g.ch. loss of it, which is restored a few weeks after the cessation of treatment; rarely - cholestasis. jaundice, hepatitis, an asymptomatic increase in the level of liver transaminases. Despite the lack of proof of the causal connection of these violations with the use of terbinafine. If hepatobiliary dysfunction develops, Exifin should be discontinued.

On the part of the PNC: rarely - paresthesia, hypoesthesia. dizziness, very rarely depression, a feeling of heightened anxiety.

FROMabout the sides of the musculoskeletal systema: often arthralgia. myalgia.

Co hand sisteats of thebranchesorations: very rarely neutropenia, agranulocytosis, thrombocytopenia.

From the immune system: often urticaria, multiforme-erythema, rarely systemic allergic reactions (reactions like serum sickness, our modem). very rarely severe skin reactions (toxic epidermal necrolysis, Stevens-Johnson syndrome, photosensitivity). With the progression of skin rashes, terbinafine should be discontinued. Othera: often headache, poor health, a feeling of fatigue, very rarely - exacerbation of psoriasis, increased hair loss.

Overdose:

Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region.

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

Interaction:

Virtually does not affect the clearance of drugs metabolized with the participation of cytochrome P450 (nair, ciclosporin, terfenadine. tolbutamide. triazo. oral contraceptives).

Inhibits isoenzyme СУР206 and interferes with the metabolism of such drugs as tricyclic antidepressants and selective blockers of seizure a sero gonima (nair, desipramine, fluvoxamine), (β1-blockers (metoprolol, propranolol). antiarrhythmic agents (flecainide proavfenon).MAO-B-inhibitors (e.g. selegiline) and antipsychotic (ex. chlorpromazine, haloperidol).

Medicinal preparations-inductors of enzymes СУР450 (ex. rifampicin) can narrow the excretion of terbinafine from the body.

Medicinal preparations-inhibitors СУР450 (ex. 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 antipyrine, digoxin, warfarin.

Ethanol and other hepatotoxic drugs increase the risk of developing a hepatotoxic effect.

Special instructions:

Irregular application of terbinafine or premature discontinuation of treatment leads 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 of skin infection there is no improvement, it is necessary to re-determine 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 cessation of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis for 3 weeks. and onychomycosis of the feet for 6 weeks is not required.

In the presence of severe renal failure (creatinine clearance less than 50 ml / min or creatinine in the blood more than 300 μmol / l), if the liver function is disrupted, the dose of terbinafine should be reduced by half.

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

With reduced liver function, appoint a half-adult dose. During treatment, it is necessary to control the level of liver transaminases in the blood serum. In rare cases, after 3 months of treatment, there is cholestasis and hepatitis. When there are signs of impaired liver function (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice,darkening of the urine or colorless stools), the drug should be discarded.

The administration of terbinafine to psoriasis patients requires increased discretion; in very rare cases terbinafine can trigger an outbreak 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 (every 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:terbinafine does not affect the ability to drive and perform work that requires increased concentration.

Form release / dosage:

Pills.

Packaging:

For 4 tablets in PVC / aluminum blister, 4, 5, 7 or 10 blisters together with instructions for use are placed in a cardboard box.

For 16 tablets in PVC / aluminum blister, 1 blister along with instruction on application placed in a cardboard box.

Storage conditions:

In dry, dark place at a temperature of up to 25 ° C.

In a place inaccessible to children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N011536 / 01

Date of registration:14.10.2011

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

Dr. Reddy`c Laboratoris Ltd. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp19.09.2015

Illustrated instructions

Instructions

Exifin® (Exifine®)