Terbinafine, pills 250mg 14pcs

Composition

1 tablet contains:

active substances:

terbinafine hydrochloride 250 mg;

excipients:

Colloidal silicon dioxide,

calcium stearate monohydrate (calcium stearic acid 1-water),

potato starch,

microcrystalline cellulose (MCC-200),

lactose monohydrate,

crospovidone (polyplasdon XL-10),

crospovidone (polyplasdon XL),

povidone K 90 (plasdon K-90) – 5 mg

Pharmacological action

Terbinafine belongs to the group of allylamines, has a wide spectrum of antifungal action. In low concentrations, it has a fungicidal effect on Trychophyton dermatophytes (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (for example. Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans. For fungi Candida spp. and their mycelial forms have a fungicidal or fungistatic effect, depending on the type of fungus.

Terbinafine disrupts the early stage of biosynthesis of the main component of the fungal cell membrane, ergosterol, by inhibiting the squalene oxidase enzyme.

When administered orally, it is not effective in the treatment of multicolored lichen caused by Pityrosporum ovale, Pityrosporum orbiculare, Malassezia furfur.

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 dose of 250 mg, the maximum concentration of the drug in blood plasma reaches 0.97 mcg / ml. Bioavailability is 80%. Food intake does not affect the bioavailability of terbinafine.

Terbinafine binds intensively to plasma proteins (99%), is rapidly distributed in tissues, and penetrates the dermal layer of the skin and nail plates. Penetrates the secret of the sebaceous glands and accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue.

The half-life is 16-18 hours, the terminal phase half — life is 200-400 hours.

Biotransformed in the liver to inactive metabolites. 80% of the dose is excreted by the kidneys in the form of metabolites, the rest (20%) is excreted through the intestine.

It does not accumulate in the body. The age of patients does not affect the pharmacokinetics of terbinafine, but elimination may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood.

It is excreted in breast milk.

Indications

• Mycoses of the scalp (trichophytosis, microsporia).
• Fungal diseases of the skin and nails (onychomycosis) caused by Trychophyton (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaccum), Microsporum (M. sapis, M. gypseum) and Epidermophyton floccosum.
• Severe, widespread dermatomycosis of smooth skin of the trunk and limbs, requiring systemic treatment.
• Candidiasis of the skin and mucous membranes.

Use during pregnancy and lactation

No teratogenic properties of terbinafine were found in experimental studies.

The use of the drug during pregnancy is possible in cases where the intended benefit to the mother exceeds the possible risk to the fetus. Terbinafine is excreted in breast milk.

If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be decided.

Contraindications

• chronic or active liver disease;
• chronic renal failure (CC less than 50 ml/min);
• children’s age (up to 3 years) and weighing up to 20 kg (for this dosage form);
• lactation;
• lactase deficiency, lactose intolerance, malabsorption glucosegalactose;
• hypersensitivity to terbinafine or any other components of the drug.

Care should be taken when:

• renal failure (with creatinine clearance greater than 50 ml/min);
• alcoholism;
• suppression of bone marrow hematopoiesis;
• tumors;
• metabolic diseases;
• occlusive diseases of the vessels of the extremities;
• cutaneous lupus erythematosus or systemic lupus erythematosus.

Side effects

Dyspeptic disorders (decreased appetite, nausea, diarrhea, feeling of fullness of the stomach, abdominal pain); allergic skin reactions (urticaria, rash); musculoskeletal reactions (arthralgia, myalgia), aggravation of the course of systemic lupus erythematosus. Disorders of taste sensations, including their loss (recovery occurs within a few weeks after discontinuation of treatment).

Extremely rarely (with a frequency of 0.01–0.1%), a hepatotoxic effect is observed (increased activity of “hepatic” transaminases, liver failure).

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

Interaction

Inhibits the CYP2P6 isoenzyme and interferes with the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (for example, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), monoamine oxidase B-type inhibitors (for example, selegiline) and antipsychotics (for example, chlorpromazine, haloperidol) means.

Drugs that are inducers of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the elimination of terbinafine from the body.

Drugs that inhibit cytochrome P450 isoenzymes (for example, cimetidine) can slow down the metabolism and elimination of terbinafine from the body. Terbinafine dosage adjustment may be required when these drugs are used concomitantly. Menstrual disorders may occur when taking terbinafine and oral contraceptives at the same time.

Terbinafine reduces the clearance of caffeine by 21% and prolongs its half-life by 31%. It does not affect the clearance of phenazone, digoxin, or warfarin.

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

How to take, course of use and dosage

For adults: Inside, after eating. The usual dose is 250 mg once a day.

Children over 3 years of age: 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 the course of treatment and the dosage regimen are determined individually and depend on the localization of the process and the severity of the disease.

Onychomycosis: the average duration of therapy is 6-12 weeks. If the nails of the fingers and feet are affected (with the exception of the big toe), or if the patient is young, the duration of treatment may be less than 12 weeks. For a big toe infection, a 3-month course of treatment is usually sufficient.

Some patients who have a reduced rate of nail growth may require a longer treatment period.

Fungal infections of the skin: the duration of treatment for interdigital, plantar or “sock” type localization of infection is 2-6 weeks; for mycoses of other parts of the body: legs – 2-4 weeks, trunk – 2-4 weeks; for mycoses caused by fungi of the genus Candida – 2-4 weeks; for mycoses of the scalp caused by fungi of the genus Microsporum – more than 4 weeks.

The duration of treatment for mycoses of the scalp is about 4 weeks, if infected with Microsporum canis-it can be longer.

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

Patients with hepatic or renal insufficiency – 125 mg once a day.

Overdose

Symptoms: headache, dizziness, nausea, vomiting, epigastric pain, frequent urination, rash.

Treatment: measures to remove the drug (gastric lavage, taking activated charcoal); if necessary, symptomatic maintenance therapy.

Special instructions

Irregular use of terbinafine or premature discontinuation of treatment may lead to relapse of the disease. The duration of therapy may also be affected by factors such as the presence of concomitant diseases, the condition of nails with onychomycosis at the beginning of the course of treatment.

If there is no improvement in the condition after 2 weeks of treatment for a skin infection, 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 nails, the presence of pronounced subungual hyperkeratosis, and the ineffectiveness of previous local therapy.

In the treatment of onychomycosis, a laboratory-confirmed clinical response is usually observed several months after mycological treatment and discontinuation of treatment, due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

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

During treatment, it is necessary to monitor the activity of hepatic transaminases in the blood serum.

In rare cases, cholestasis and hepatitis occur after 3 months of treatment. If signs of impaired liver function appear (weakness, persistent nausea, loss of appetite, excessive abdominal pain, jaundice, dark urine or discolored stools), the drug should be discontinued.

Prescribing terbinafine to patients with psoriasis requires caution, because in very rare cases, terbinafine can provoke an exacerbation of psoriasis.

When treating with terbinafine, general hygiene rules should be observed to prevent the possibility of re-infection through underwear and shoes. During the course of treatment (after 2 weeks) and at the end of it, it is necessary to perform antifungal treatment of shoes, socks and stockings.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

4 years

Active ingredient

Terbinafine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Nursing mothers as prescribed by a doctor, Adults as prescribed by a doctor, Children over 3 years of age, Children as prescribed by a doctor

Indications

Thrush, Nail Fungus, Skin Fungus, Scalp Fungus