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

microcrystalline cellulose, starch, povidone, sodium methylparaben, sodium lauryl sulfate, colloidal silicon dioxide, magnesium stearate, sodium starch glycolate,talc.

Description:

From white to white with a yellowish hue of color, round, biconvex tablets.

From white to white with a yellowish shade of color, round flat tablets with cut edges and a dividing notch on one side.

Pharmacotherapeutic group:Antifungal agent

ATX: & nbsp

D.01.A.E.15 Terbinafine

Pharmacodynamics:

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

Terbinafine specifically suppresses the early stage of biosynthesis of sterols in the fungal cell. This leads to ergosterol deficiency and intracellular accumulation of squalene, which causes fungal cell death.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 medications.

When Binafin is administered inside the skin, hair and nails, the concentrations of the drug are created to ensure fungicidal action.

Pharmacokinetics:

After a single oral administration of terbinafine at a dose of 250 mg, the maximum plasma concentration in the blood is reached after 2 hours and is 0.97 μg / ml. The half-absorption period is 0.8 hours; and the half-distribution period is 4.6 hours. It is not necessary to correct the dose of the drug while taking it with food. Terbinafine largely binds to blood plasma proteins (99%), quickly penetrates the dermal layer of the skin and is concentrated in the lipophilic stratum corneum. Terbinafine also penetrates into the secretion of sebaceous glands, which leads to the creation of high concentrations in the hair follicles, hair, and in the skin, rich in sebaceous glands. It is also shown that terbinafine penetrates into the nail plates in the first few weeks after initiation of therapy.

Terbinafine is metabolized rapidly and to a significant extent with the participation of at least seven isoenzymes of cytochrome P450, with the main role being played by isozymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. As a result of the biotransformation of terbinafine, metabolites are formed that do not possess antifungal activity and are excreted mainly in the urine. The final half-life of the drug is 17 hours. There is no evidence of cumulation of the drug in the body. There were no changes in the equilibrium concentration of Binafin in plasma, depending on the age, but in patients with impaired renal or hepatic function the rate of excretion of the drug may be slowed, which leads to higher concentrations of terbinafine in the 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 demonstrated.

Indications:

Onychomycosis caused by mushrooms dermatophytes; mycoses of the scalp;

Fungal skin infections - treatment of dermatomycosis of the trunk, shins, feet, and yeast infections of the skin caused by fungi of the genus Candida (eg, Candida albicans) - in those cases where the localization, severity or prevalence of infection determines the advisability of oral therapy.

Note: unlike Binafin for topical use, Binafine tablets are not effective in multi-colored limes.

Contraindications:Hypersensitivity to terbinafine or any other component that is part of Binafin.

Pregnancy and lactation:

Since the clinical experience of Binafin in pregnant women is very limited, the drug should not be used during pregnancy, unless the potential therapeutic effect exceeds the possible risk of therapy. Terbinafine excreted in breast milk, so women who receive Binafin inside should not breast-feed.

Dosing and Administration:

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

Children

Data on the use of the drug in children younger than 2 years (body weight of which is usually less than 12 kg) - are absent.

The drug is prescribed once a day.

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

Adults

Adults usually appoint Binafin according to Table 1.(250 mg) once daily.

Infections of the skin

Recommended duration of treatment:

Dermatomycosis of the feet (interdigital, plantar or as a socks): 2-6 weeks;

Dermatomycosis of the trunk, legs - 2-4 weeks;

Candidiasis of the skin - 2-4 weeks.

Complete disappearance of manifestations of infections and complaints associated with it can occur only a few weeks after mycological cure.

Hair and scalp infections

Recommended duration of treatment:

Mycosis of the scalp: 4 weeks

Mycoses of the scalp are mainly seen in children.

Onychomycosis

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

Application in the elderly

There is no reason to assume that for elderly people it is required to change the dosage of the drug or that they have side effects that differ from those in younger patients. In case of use in this age group of the drug in tablets, the possibility of concomitant impairment of liver or kidney function should be considered.

Use in children

In children older than 2 years, Binafin's tolerance for oral administration is good.

Side effects:

Binafin as a whole is well tolerated. Side effects are usually mild or moderate and are transient. Most often (with a frequency of 1 to 10%) there are symptoms from the gastrointestinal tract (feeling of overflow of the stomach, loss of appetite, dyspepsia. Nausea, mild abdominal pain, diarrhea), mild skin reactions (rash, urticaria), muscular - Skeletal reactions (arthralgia, myalgia). With a frequency of 0.1 to 1%, there are violations of taste, including their loss (recovery occurs within a few weeks after cessation of treatment); Rarely with a frequency of 0.01 to 0.1% in connection with treatment Binafin reported hepatobiliary disorders (primarily associated with cholestasis, including cases of liver failure).There are reports of cases of liver failure, some of which lead to death or liver transplantation, but in most cases, patients had serious concomitant diseases and the association of cases of hepatic insufficiency with Binafin was regarded as questionable.

There are reports of very rare (with a frequency of less than 0.01%) occurring 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, thrombocytopenia. There are reports of very rare cases of hair loss, although the causal relationship of this phenomenon with the use of the drug has not been established.

Overdose:

There have been reports of several cases of Binafin overdose (the accepted dose was up to 5 g), which included headache, nausea, epigastric pain and dizziness.

Recommended in case of an overdose, treatment includes measures to remove the drug,primarily by prescribing activated charcoal, washing the stomach, and, if necessary, using symptomatic maintenance therapy.

Interaction:

The results of studies conducted in vitro in healthy volunteers, show that terbinafine has little potential to suppress or enhance the clearance of most drugs that are metabolized by the cytochrome P450 system (eg, cyclosporine, terfenadine, tolbutamide, triazolam or oral contraceptives).

In studies in vitro, However, it was found that terbinafine suppresses CYP2D6-mediated metabolism. These, obtained in experiments in vitro, the data may be clinically significant for those drugs that are predominantly metabolized by this enzyme, such as tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors and monoamine oxidase B type inhibitors, if the concomitant drug has a small range of therapeutic concentration. In patients who simultaneously took Binafin and oral contraceptives,in some cases, the irregularity of the menstrual cycle was noted, although the frequency of these disorders remained within the range noted in patients using only oral contraceptives.

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

Special instructions:

If during the treatment with Binafin, the patient has symptoms suggestive of liver dysfunction, such as unexplained persistent nausea, vomiting, lack of appetite, fatigue, jaundice, pain in the right hypochondrium, dark urine or discolored stool, in this case it is necessary to confirm the hepatic origin of these symptoms (determination of serum ALT concentrations, ACT) and cancel treatment with Binafine. The patient should be warned about the need to see a doctor if there are any similar symptoms.

Since prospective clinical studies on the study of course use of Binafin in patients with concomitant chronic or active liver disease have not been conducted, its appointment to this contingent of patients is not recommended.

Patients with impaired renal function (creatinine clearance less than 50 ml / min or serum creatinine level greater than 300 μmol / L) should receive half the usual dose of the drug.

In studies in vitro it was revealed that terbinafine suppresses metabolism mediated by cytochrome enzyme 2D6 (CYP2D6). Therefore, continuous monitoring of patients receiving concomitantly metabolized with Binafin with drugs predominantly metabolized with this enzyme, such as tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors and type B monoamine oxidase inhibitors, should be performed if the concomitant drug has a small range of therapeutic concentration.

Effect on the ability to drive transp. cf. and fur:

Data on the influence of Binafin on the ability to drive a car and work with mechanisms are absent.

Form release / dosage:

Tablets of 125 mg, 250 mg 250 mg.

Packaging:

For 10, 14, 20 tablets in a blister of PVC-aluminum foil.

For 1 or 2 blisters are placed in a cardboard box along with instructions for use.

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014467 / 01-2002

Date of registration:17.11.2008

Expiration Date:Unlimited

The owner of the registration certificate:SHREYA LIFE SENENSIZ Pvt.Ltd. SHREYA LIFE SENENSIZ Pvt.Ltd. India

Manufacturer: & nbsp

SHREYA LIFE SCIENCES, Pvt.Ltd. India

Representation: & nbspSHREYA LIFE SENENSIZ Pvt.Ltd. SHREYA LIFE SENENSIZ Pvt.Ltd. India

Information update date: & nbsp11.02.2017

Illustrated instructions

Instructions

Binafin (Binafin)