Exifin tablets 250mg, No. 16

• Mycoses of the scalp (trichophytosis, microsporia);

• mycoses of the skin and nails caused by Trychophyton (T. rubnim, T. mentagrophytes, T. verrucosum, T. violaceum). Microsporum (M. canis, M. gypseum) and Epidermophylom floccosum;

• onychomycosis;

• severe, widespread dermatomycosis of the smooth skin of the trunk and extremities, requiring systemic treatment;

• candidiasis of the skin and mucous membranes.

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.

Onychomycosis

Usual dose: 250 mg once a day.

The duration of therapy is about 6-12 loops.

With the defeat of the nails of the fingers and toes (with the exception of the thumb moans), or at a young age of the patient, the duration of treatment may be less than 12 weeks.

For a big toe infection, a 3-month course of treatment is usually sufficient. In rare cases, when the rate of nail growth is slow, a longer treatment up to 6 months or more may be required.

Fungal skin infections. The duration of treatment for interdigital, plantar or sock-like localization of infection is 2-6 weeks, with mycoses of other parts of the body: legs - 2-4 weeks, trunk - 4 weeks, with mycoses caused by Candida - 2-4 weeks; with mycoses of the head caused by Microsporum canis - more than 4 weeks.

Children are usually prescribed 125 mg (1/2 tablet). The duration of treatment for mycoses of the scalp is about 4 weeks, if infected with Microsporum canis, it can be longer. With a body weight of less than 20 kg - 62.5 mg (1/4 tablet) 1 time / day, with a weight of 20 to 40 kg - 125 mg (1/2 tablet) 1 time / day, with a weight of more than 40 kg - 250 mg ( 1 tablet) 1 time / day.

Elderly patients are prescribed the drug in the same vines as adults. With severe violations of the liver and / or kidneys (CC 50 ml / min or the concentration of creatinine in the blood more than 300 ?mol / l) - 125 mg 1 time / day.

The tablets are white or almost white, round, biconvex, smooth on both sides.

1 tab.

terbinafine hydrochloride 281.31 mg,

which corresponds to the content of terbinafine 250 mg

Excipients: microcrystalline cellulose (type 102) - 47 mg, sodium starch glycolate (type A) - 36.96 mg, pregelatinized starch - 25 mg, colloidal anhydrous silicon - 3 mg, magnesium stearate - 7 mg.

• Children under 2 years of age, because there is not enough data on the use of the drug by children weighing less than 12 kg;

• pregnancy;

• lactation period;

• hypersensitivity to the components of the drug.

  Precautions: hepatic and / or renal failure; alcoholism; blood diseases; tumors; metabolic diseases; limb vascular pathology, psoriasis.

pharmachologic effect

Terbinafine belongs to the group of allylamines. Possesses a wide spectrum of antifungal action. In low concentrations, it has a fungicidal effect on Trychophyton dermatophytes (T. rubrum, T. menlagrophytes, T. tonsurans, T. verrucosum, T. violaccum), Microsporum canis, Epidermophyton floccosum, mold fungi (for example, Aspergillus, Cladosporium, Scopulariius) yeast fungi, mainly Candida albicans, and some dimorphic fungi. Depending on the type of fungus, it has a fungicidal or fungistatic effect on Candida fungi and its mycelial forms. Terbinafine disrupts the early stage of biosynthesis of the main component of the cell membrane of the fungus ergostrol by inhibiting the enzyme squalene epoxidase. Squalene epoxidase is not associated with the cytochrome P450 (CYP450) system,therefore, terbinafine does not affect the metabolism of hormones and drugs, the metabolism of which is associated with CYP450. After oral administration, it accumulates in the skin, nails and hair in an amount that has a fungicidal effect. Systemic treatment of varicoloured lichen due to Malassezia furfur is ineffective.

Pharmacokinetics

When taken orally, it is well absorbed, after 0.8 hours, half of the dose taken is absorbed; after 4.6 hours, half of the dose taken is distributed in the body. 1-2 hours after ingestion of a single 250 mg dose Cmax of the drug in blood plasma reaches 0.97 ?g / ml. Bioavailability is 80%. Reception of food does not affect the bioavailability of terbinafine. Terbinafine binds intensively to blood plasma proteins (99%), quickly spreads in tissues, and penetrates into the dermal layer of the skin and nape plates. Penetrates into the secretion of the sebaceous glands and accumulates in high concentrations in hair follicles, hair, skin and subcutaneous tissue. Already after a few weeks of treatment, it accumulates in the nails and in concentrations that provide a fungicidal effect. T1 / 2 - 16-18 hours T1 / 2 of the terminal phase - 200-400 hours Biotransformed in the liver to inactive metabolites:80% of the dose taken is excreted in the urine in the form of metabolites, the rest (20%) with feces. Does not accumulate 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 in breast milk.

Side effect

Side effects are usually moderate to mild and temporary.

From the digestive system: often - a feeling of a full stomach, dyspepsia, nausea, loss of appetite, abdominal pain, diarrhea; infrequently - violation of taste perception, incl. loss that recovers a few weeks after stopping treatment; rarely - cholestasis, jaundice, hepatitis, asymptomatic increase in the level of liver gransaminases. Despite the lack of evidence of the causal relationship of these disorders with the use of terbinafine, if hepatobiliary dysfunction develops, treatment with Exifin should be discontinued.

From the side of the central nervous system: rarely - paresthesia, hypesthesia, dizziness; very rarely - depression, a feeling of increased anxiety.

From the musculoskeletal system: often - arthralgia, myalgia.

From the hematopoietic system: very rarely - neutropenia, agranulocytosis, thrombocytopenia.

From the immune system: often - urticaria, erythema multiforme, rarely systemic allergic reactions (reactions similar to serum sickness, angioedema); very rarely - severe skin reactions (toxic epidermal necrolysis, Stevens-Johnson syndrome, photosensitivity).

If the skin rash progresses, treatment with terbinafine should be discontinued.

Others: often - headache, feeling unwell, feeling tired; very rarely - exacerbation of psoriasis, increased hair loss

Application during pregnancy and lactation

Contraindicated during pregnancy and lactation.

Application for violations of liver function

Carefully. With severe violations of liver function - 125 mg 1 time / day.

Application for impaired renal function

Carefully. With severe impairment of function or kidney (CC 50 ml / min or the concentration of creatinine in the blood is more than 300 ?mol / l) - 125 mg 1 time / day.

Application in children

Contraindicated: children under 2 years of age, because there is not enough data on the use of the drug by children weighing less than 12 kg. Children are usually prescribed 125 mg (1/2 tablet). The duration of treatment for mycoses of the scalp is about 4 weeks, if infected with Microsporum canis, it can be longer. With a body weight of less than 20 kg - 62.5 mg (1/4 tablet) 1 time / day, with a weight of 20 to 40 kg - 125 mg (1/2 tablet) 1 time / day, with a weight of more than 40 kg - 250 mg ( 1 tablet) 1 time / day.

Use in elderly patients

Elderly patients are prescribed the drug in the same vines as adults.

special instructions

Irregular use of terbinafine or premature discontinuation of treatment leads to a relapse of the disease. The duration of therapy can also 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 the skin infection there is no improvement in the condition, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug. Systemic use in onychomycosis is justified only in the case of total damage to most of the nails, the presence of pronounced subungual hyperkeratosis, and the ineffectiveness of previous local therapy. In the treatment of onychomycosis, the clinical response is usually observed several months after the mycological cure and discontinuation 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 the hands within 3 weeks. and onychomycosis of the feet for 6 weeks. not required. In the presence of severe renal failure (creatinine clearance less than 50 ml / min or creatinine in the blood more than 300 ?mol / l), in case of impaired liver function, the dose of terbinafine should be halved. In the presence of liver disease, terbinafine clearance may be reduced. With reduced liver function, half the adult dose is prescribed. During treatment, it is necessary to monitor the level of liver transaminases in the blood serum. In rare cases, after 3 months of treatment, cholestasis and hepatitis occur. If signs of liver dysfunction appear (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice, dark urine or colorless stools), the drug should be discontinued.Prescribing terbinafine to patients with psoriasis requires increased caution. in very rare cases, terbinafine can trigger an outbreak of psoriasis. When treating terbinafia, general hygiene rules should be followed to prevent the possibility of re-infection through underwear and shoes. During treatment (every 2 weeks) and at the end of it, it is necessary to carry out antifungal treatment of shoes, socks and stockings.

Influence on the ability to drive vehicles and use mechanisms

Terbinafine does not affect the ability to drive and perform work that requires increased concentration.

Overdose

Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region. Treatment: gastric lavage followed by activated charcoal and / or symptomatic therapy

Drug interactions

Virtually no effect on the clearance of drugs metabolized with the participation of cytochrome P450 (for example, cyclosporine, terfenadine, tolbutamide, triazolam, oral contraceptives). It inhibits CYP206 and interferes with the metabolism of drugs such as tricyclic antidepressants and selective serotonin uptake blockers (desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmics (flecainide, proavfenone), such as MAO-inhibitors , haloperidol). Medicines - inducers of CYP450 enzymes (for example, rifampicin) can accelerate the elimination of terbinafine from the body. Medicines - CYP450 inhibitors (for example, cimetidine) can slow down the metabolism and excretion of terbinafine from the body.With the simultaneous use of these drugs, dose adjustment of terbinafine may be required. Possible menstrual irregularities while taking terbinafine and oral contraceptives. Reduces the clearance of caffeine by 21% and extends its half-life by 31%. Does not affect the clearance of antipyrine, digoxin, warfarin. Ethanol and other hepatotoxic drugs increase the risk of developing hepatotoxic effects.