Binafin, pills 250mg, 14pcs

Composition

1 tablet contains:

Active ingredient:

terbinafine hydrochloride;

Auxiliary substances:

MCC;

starch;

povidone;

sodium methylparaben;

sodium lauryl sulfate;

colloidal silicon dioxide;

magnesium stearate;

sodium starch glycolate;

talc.

Pharmacological action

Binafin is a broad-spectrum antifungal agent.

Pharmacodynamics

Terbinafine is an allylamine that has a broad spectrum of action against fungi that cause diseases of the skin, hair and nails, including dermatophytes such as Trichophyton (for example, T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum (for example, M. canis), Epidermophyton floccosum, as well as yeast-like fungi of the genus Candida (for example, Candida albicans) and Pityrosporum. In low concentrations, terbinafine has a fungicidal effect against dermatophytes, mold fungi and some dimorphic fungi. Activity against yeast-like fungi, depending on their type, can be fungicidal or fungistatic.

Terbinafine specifically inhibits the early stage of sterol biosynthesis in the fungal cell. This leads to ergosterol deficiency and intracellular squalene accumulation, which causes fungal cell death. The action of terbinafine is carried out by inhibiting the enzyme squalene oxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system. Terbinafine does not affect the metabolism of hormones or other medications. When Binafin is administered orally, concentrations of the drug are created in the skin, hair and nails that provide a fungicidal effect.

Pharmacokinetics

After a single oral use of terbinafine at a dose of 250 mg, the Cmax of the drug in blood plasma is reached in 2 hours and is 0.97 mcg / ml. The half-absorption period is 0.8 hours; and the half-distribution period is 4.6 hours. No dose adjustment is required when taken simultaneously with food. Terbinafine is largely bound to plasma proteins (99%), quickly penetrates the dermal layer of the skin and is concentrated in the lipophilic stratum corneum. Terbinafine also penetrates the secret of the sebaceous glands, which leads to the creation of high concentrations in hair follicles, hair and in the skin rich in sebaceous glands. It is also shown that terbinafine penetrates the nail plates in the first few weeks after the start of therapy.

Terbinafine is metabolized rapidly and significantly with the participation of at least seven cytochrome P 450 isoenzymes, with the main role played by the isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. As a result of biotransformation of terbinafine, metabolites are formed that do not have antifungal activity and are mainly excreted in the urine. The final T1 / 2 of the drug is 17 hours. There is no evidence of accumulation of the drug in the body. There were no changes in Binafine’s Css in plasma depending on age, but in patients with impaired renal or hepatic function, the rate of drug elimination may be slowed, which leads to higher concentrations of terbinafine in blood plasma. In pharmacokinetic studies of a single dose of Binafin in patients with concomitant liver diseases, the possibility of reducing the clearance of the drug by 50% was shown.

Indications

• onychomycosis caused by fungi dermatophytes;
• mycoses of the scalp;
• fungal infections of the skin-treatment of dermatomycosis of the trunk, legs, feet, as well as yeast infections of the skin caused by fungi of the genus Candida (for example, Candida albicans) — in cases where the localization, severity or prevalence of infection makes oral therapy advisable.

Use during pregnancy and lactation

Since the clinical experience of using Binafin in pregnant women is very limited, the drug should not be used during pregnancy, unless the potential therapeutic effect does not exceed the possible risk of therapy.

Terbinafine is excreted in breast milk, so women receiving Binafine orally should not breastfeed.

Contraindications

Hypersensitivity to terbinafine or any other component of Binafine.

Side effects

Binafin is generally well tolerated. Side effects are usually mild or moderate and transient.

Most often (with a frequency of 1 to 10%) there are symptoms from the gastrointestinal tract (feeling of fullness of the stomach, loss of appetite, dyspepsia, nausea, mild abdominal pain, diarrhea), mild skin reactions (rash, urticaria), musculoskeletal reactions (arthralgia, myalgia). With a frequency of 0.1 to 1%, there are violations of taste sensations, including their loss (recovery occurs within a few weeks after discontinuation of treatment); rarely (with a frequency of 0.01 to 0.1%), hepatobiliary disorders (primarily associated with cholestasis, including cases of liver failure) have been reported in connection with Binafin treatment.

There are reports of liver failure, some of which resulted in death or liver transplantation, but in most cases patients had serious comorbidities, and the association of cases of liver failure with the use of Binafin was considered doubtful. There are reports of very rare (with a frequency of less than 0.01%) serious skin reactions-Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactoid reactions.

If a progressive skin rash develops, treatment with Binafin should be discontinued. There are also reports of very rare hematological disorders, such as neutropenia, agranulocytosis, and thrombocytopenia. There are reports of very rare cases of hair loss, although the causal relationship of this phenomenon with taking the drug has not been established.

Interaction

The results of in vitro studies conducted in healthy volunteers show that terbinafine has little potential to inhibit or increase the clearance of most drugs that are metabolized with the participation of the cytochrome p450 system (for example, cyclosporine, terfenadine, tolbutamide, triazolam or oral contraceptives).

In vitro studies, however, have shown that terbinafine inhibits CYP2D6-mediated metabolism. These data may be clinically relevant for those drugs that are primarily metabolized by this enzyme, such as tricyclic antidepressants, beta-blockers, SSRIs, and MAO type B inhibitors (if the drug used simultaneously has a small therapeutic concentration range).

In some cases, irregular menstrual cycles were observed in patients taking Binafin and oral contraceptives at the same time, although the frequency of these disorders remained within the value observed in patients using only oral contraceptives.

On the other hand, the total clearance of terbinafine may be accelerated by those drugs that accelerate metabolism (such as rafampicin) and may be slowed by drugs that inhibit cytochrome P450 (such as cimetidine). In cases where the concomitant use of these drugs is necessary, an adequate dose adjustment of Binafin may be required.

How to take, course of use and dosage

Inside. The duration of treatment depends on the indication and severity of the disease.

Adults are usually prescribed Binafin 1 tablet (250 mg) once a day.

Skin infections. Recommended duration of treatment-dermatomycosis of the feet (interdigital, plantar or sock-like) – 2-6 weeks; dermatomycosis of the trunk, legs-2-4 weeks; candidiasis of the skin-2-4 weeks.

Complete disappearance of symptoms of infections and complaints associated with them may occur only a few weeks after mycological treatment.

Infections of the hair and scalp. The recommended duration of treatment for mycosis of the scalp is 4 weeks. Mycoses of the scalp are observed mainly in children.

Onychomycosis. The duration of effective treatment with Binafin in most patients is from 2 to 6 weeks. For onychomycosis of the hands,6 weeks of treatment is sufficient in most cases; for onychomycosis of the feet,12 weeks of treatment is sufficient in most cases. Some patients who have a reduced rate of nail growth may require longer treatment. The optimal clinical effect is observed several months after mycological treatment and discontinuation of therapy. This is determined by the time period that is necessary for the growth of a healthy nail.

Children are prescribed the drug 1 time a day.

There are no data on the use of the drug in children under 2 years of age with a body weight of less than 12 kg. In children over 2 years of age, the oral tolerability of Binafin is good.

A single dose depends on body weight and is for children with a body weight of less than 20 kg — 62.5 mg (1/4 tablet of 250 mg or 1/2 tablet of 125 mg); from 20 kg to 40 kg-125 mg (1 tablet of 125 mg or 1/2 tablet of 250 mg); more than 40 kg-250 mg (1 tablet of 250 mg).

Use in the elderly. There is no reason to assume that the elderly need to change the dosage of the drug or that they have side effects that differ from those in younger patients.If the drug is used in tablets in this age group, the possibility of concomitant liver or kidney dysfunction should be taken into account.

Overdose

Symptoms: headache, dizziness, nausea, epigastric pain.

Treatment: gastric lavage, use of activated charcoal, symptomatic therapy.

Special instructions

If during treatment with Binafin, the patient has phenomena that suggest liver function disorders, such as unexplained persistent nausea, vomiting, lack of appetite, fatigue, jaundice, pain in the right hypochondrium, dark urine or discolored feces, in this case, the liver origin of these symptoms should be confirmed (determination of serum concentrations of ALT, ACT) and treatment with Binafin should be discontinued. The patient should be warned about the need to consult a doctor in case of similar symptoms. Since promising clinical studies on the course use of Binafin in patients with concomitant chronic or active liver diseases have not been conducted, its use to this cohort of patients is not recommended.

Patients with impaired renal function (creatinine clearance 300 mmol/L) should receive half the usual dose of the drug. In vitro studies have shown that terbinafine inhibits metabolism mediated by the cytochrome 2D6 (CYP2D6) enzyme. Therefore, it is necessary to constantly monitor patients receiving simultaneous treatment with Binafin with drugs that are mainly metabolized with the participation of this enzyme, such as tricyclic antidepressants, beta-blockers, SSRIs and MAO type B inhibitors, if the drug used simultaneously has a small therapeutic concentration range.

Influence on the ability to drive a car and work with mechanisms. There are no data on the effect of Binafin on the ability to drive a car and work with mechanisms.

Form of production

Tablets

Storage conditions

In a dry place, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Terbinafine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets