BINAFINE PILLS 250MG

Composition

1 pill contains:

Active substance: terbinafine hydrochloride;

Excipients: MCC; starch; Povidone; sodium methylparaben; sodium lauryl sulfate; colloidal silicon dioxide; Magnesium stearate; sodium starch glycolate; talc.

pharmachologic effect

Binafine - a broad spectrum antifungal.

Pharmacodynamics

Terbinafine is an allylamine, which has a wide spectrum of action against fungi that cause diseases of the skin, hair and nails, including dermatophytes such asTrichophyton (egT.rubrum, T.mentagrophytes, T.tonsurans, T.verrucosum, T.violaceum), Microsporum (for example M. canis), Epidermophyton floccosumas well as yeast-like fungi of the genusCandida (egCandida albicans) andPityrosporum. In low concentrations, Terbinafine has a fungicidal effect against dermatophytes, mold fungi and some dimorphic fungi. Activity against yeast-like fungi, depending on their species, may be fungicidal or fungistatic.

Terbinafine specifically inhibits the early stage of sterol biosynthesis in the cell of the fungus. This leads to a deficiency of ergosterol and intracellular accumulation of squalene, which causes the death of the fungal cell. The action of terbinafine is carried out by inhibiting the enzyme squalene epoxidase 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 drugs.With the appointment of Binafina inside the skin, hair and nails are concentrations of the drug, providing a fungicidal effect.

Pharmacokinetics

After a single dose of terbinafine orally at a dose of 250 mg Cmax drug in the blood plasma is reached in 2 hours and is 0.97 μg / ml. The period of semi-absorption is 0.8 h; and the half-time is 4.6 hours. A dose adjustment of the drug is not required when taken simultaneously with food. Terbinafine largely binds to plasma proteins (99%), quickly penetrates the dermal layer of the skin and concentrates in the lipophilic horny layer. Terbinafine also penetrates the secret of the sebaceous glands, which leads to the creation of high concentrations in the hair follicles, hair and skin rich in sebaceous glands. It is also shown that terbinafine penetrates into the nail plate in the first few weeks after the start of therapy.

Terbinafine is metabolized rapidly and to a significant extent with the participation of at least seven cytochrome P450 isoenzymes, with the isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19 playing the main role. As a result of terbinafine biotransformation, metabolites are formed that do not possess antifungal activity and are excreted mainly in the urine. Final t1/2 drug - 17 hours. There is no evidence that the drug is cumulated in the body. No C changes detected.ss Binafine in plasma, depending on age, but in patients with impaired renal or liver function, the rate of excretion of the drug can be slowed down, which leads to higher plasma concentrations of terbinafine.In pharmacokinetic studies of a single dose of binafine 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 ringworms of the trunk, legs, feet, and yeast infections of the skin caused by fungi of the genusCandida (egCandida albicans) - in cases where the localization, severity or prevalence of infection determine the appropriateness of oral therapy.

Contraindications

Hypersensitivity to terbinafine or any other component that is part of Binafina.

Use during pregnancy and lactation

Since the clinical experience with Binafina 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 who take Binafine orally should not breastfeed.

special instructions

If in the course of Binafine treatment a patient has symptoms that suggest liver dysfunction, such as unexplained persistent nausea, vomiting, lack of appetite, fatigue, jaundice, pain in the right hypochondrium, dark urine or discolored feces, in this case it is necessary to confirm the hepatic origin of these symptoms (determination of serum concentrations of ALT, ACT) and discontinue treatment with binafine. The patient should be warned about the need to consult a doctor if he develops similar symptoms.Since promising clinical studies on the course of Binafine in patients with concomitant chronic or active liver diseases have not been conducted, its purpose is not recommended for this group of patients.

Patients with impaired renal function (Cl creatinine 300 µmol / l) should receive half the usual dose of the drug. In researchin vitro It was found that terbinafine inhibits metabolism mediated by cytochrome 2D6 enzyme (CYP2D6). Therefore, it is necessary to continuously monitor patients receiving concurrently with Binafine treatment with drugs that are predominantly metabolized with the participation of this enzyme, such as tricyclic antidepressants, beta-adrenergic blockers, SSRIs and MAO inhibitors of type B, in the event that the drug used simultaneously has a small therapeutic range. concentration.

Influence on ability to drive the car and to work with mechanisms. Data on the effect of Binafina on the ability to drive a car and work with mechanisms are missing.

Dosage and administration

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

Adults are usually prescribed Binafine 1 pill (250 mg) 1 time per day.

Infections of the skin. The recommended duration of treatment is ringworm (interdigital, plantar or sock type) - 2-6 weeks; dermatomycosis of the trunk, legs - 2-4 weeks; skin candidiasis - 2-4 weeks.

The complete disappearance of the manifestations of infections and complaints associated with them, can occur only a few weeks after mycological cure.

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 binafine in most patients is from 2 to 6 weeks. With onychomycosis of the hands, in most cases 6 weeks of treatment is enough; with onychomycosis of the feet, in most cases 12 weeks of treatment are sufficient. Some patients who have a reduced growth rate of nails may need longer treatment. The optimal clinical effect is observed several months after mycological cure and cessation of therapy. This is determined by the period of time that is necessary for the growth of a healthy nail.

For children, the drug is prescribed 1 time per day.

Data on the use of the drug in children under 2 years old with a body weight less than 12 kg are missing. In children older than 2 years, tolerability of binafine for oral administration is good.

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

Use in the elderly. There is no reason to assume that elderly people need to change the dosage of the drug or that they have side effects that differ from those of younger patients.In the case of use in this age group of the drug in pills should consider the possibility of concomitant abnormal liver function or kidney.

Side effects

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

Most often (with a frequency of 1 to 10%) symptoms of the gastrointestinal tract are noted (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 impaired taste sensations, including their loss (recovery occurs within a few weeks after stopping treatment); rarely (with a frequency of 0.01 to 0.1%), in connection with treatment with Binafine, hepatobiliary disorders (primarily associated with cholestasis, including cases of hepatic insufficiency) were reported. Cases of liver failure have been reported, some of which have been fatal or liver transplanted, but in most cases the patients had serious comorbidities, and the association of cases of liver failure with Binafine was regarded as questionable. There are reports of very rare (with a frequency of less than 0.01%) serious skin reactions occurring - Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactoid reactions. If a progressive skin rash develops, Binafine treatment should be discontinued.There are also reports of very rare hematological disorders, such as neutropenia, agranulocytosis, 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.

Drug interaction

The results of studies conductedin vitro in healthy volunteers, show that terbinafine has little potential for suppressing or increasing 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 researchin vitrohowever, it was found that terbinafine inhibits CYP2D6-mediated metabolism. This data may be clinically significant for those drugs that are predominantly metabolized by this enzyme, such as tricyclic antidepressants, beta-blockers, SSRIs and type-B MAO inhibitors (if the drug used at the same time has a small therapeutic concentration range).

In patients who simultaneously took Binafine and oral contraceptives, in some cases, the menstrual cycle was irregular, although the incidence of these disorders remained within the range observed in patients using only oral contraceptives.

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

Overdose

Symptoms: headache, dizziness, nausea, pain in the epigastric region.

Treatment: gastric lavage, the appointment of Activated carbon, symptomatic therapy.

Storage conditions

In a dry place, at a temperature of 2-30 ° C.