Binafine Tablets 250mg N14
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Active ingredients
Terbinafin
Release form
Pills
Composition
Terbinafine 250 mg; terbinafine hydrochloride 283 mg; Auxiliary substances: microcrystalline cellulose, starch, povidone, sodium methylparaben, sodium lauryl sulfate, colloidal silicon dioxide, magnesium stearate, sodium starch glycolate, talc.
Pharmacological effect
Antifungal drug is allylamine. It has a wide range of actions .; Active against fungi that cause diseases of the skin, hair and nails: Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum, Micosporum canis, Epidermophyton floccosum, as well as the Candida kind of yeast-like fungi, as well as Epidermophyton floccosum, and also Candida fungi, as well as Epidermophyton floccosum, and also Candida fungi, Microforum canis, Epidermophyton floccosum, and also Candida fungi, as well as the fungi that cause diseases of the fungi that cause skin diseases. Pityrosporum .; In low concentrations, has a fungicidal effect against dermatophytes, mold fungi and some dimorphic fungi. The effect on yeast-like fungi can be fungicidal or fungistatic, depending on the type of fungus .; Terbinafine specifically inhibits the early stage of sterol biosynthesis in the cell of the fungus. This leads to a deficiency of ergosterol and to the 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.
Pharmacokinetics
Absorption; After a single dose of terbinafine orally at a dose of 250 mg Cmax in plasma is reached in 2 hours and is 0.97 mcg / ml. The period of semi-absorption is 0.8 hours. Eating does not affect the bioavailability of terbinafine .; With topical application of the cream less than 5% of the dose is absorbed, thus, the systemic effect of the drug is minimal .; Distribution; Plasma protein binding is 99%. The half-distribution period is 4.6 hours. It quickly penetrates the dermal layer of the skin and accumulates in the lipophilic stratum corneum. Terbinafine also penetrates the secret of the sebaceous glands, which during the first few weeks leads to the creation of high fungicidal concentrations in hair follicles, nails, and skin rich in sebaceous glands .; Metabolism; Terbinafine rapidly biotransformed in the liver with the active participation of the isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8, CYP2C19 to form inactive metabolites .; Terbinafine is excreted in breast milk. Excreted mainly with urine in the form of metabolites. T1 / 2 is 17 hours.There is no evidence of drug cumulation in the body .; Pharmacokinetics in special clinical situations; No changes in Css terbinafine, depending on age; In patients with impaired liver or kidney function, the rate of excretion of the drug may be slowed down, which leads to higher plasma concentrations of terbinafine. In pharmacokinetic studies after taking a single dose of binafine in patients with concomitant liver diseases, it was shown that the clearance of terbinafine could be reduced by 50%.
Indications
For pills; - onychomycosis caused by fungi dermatophytes; - mycosis of the scalp; - mycoses of the skin of the body, legs, feet, caused by dermatophytes and yeast-like fungi of the genus Candida in cases where the localization, severity and prevalence of infection determine the appropriateness of oral therapy .; For the cream; - fungal infections of the skin caused by dermatophytes such as Trichophyton (including Trichophyton cos;;;;;;;; br br br br br br; - yeast infections of the skin, mainly caused by Candida spp. (including Candida albicans); - versicolor versicolor (Pityriasis versicolor), caused by Pityrosporum orbiculare (also known as Malassezia furfur) .; Unlike binafina in the form of a cream, the use of pills for the treatment of multi-colored depriving is ineffective.
Contraindications
- Hypersensitivity to terbinafine or any other component of the drug.
Use during pregnancy and lactation
Use of the drug during pregnancy is possible only in the case when the intended benefit to the mother exceeds the potential risk to the fetus .; Terbinafine is excreted in breast milk, so if you need to use the drug during lactation, breastfeeding should be stopped.
Dosage and administration
Children over the age of 2 years, the drug in the form of pills administered 1 time / day. A single dose depends on the body weight of the child. The duration of therapy depends on the indications and the severity of the disease .; Adults in the form of pills prescribed 250 mg 1 time / day. The duration of therapy depends on the indications and the severity of the disease .; With onychomycosis, patients with a reduced growth rate of the nail may require 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 .; Patients with impaired renal function (CC <50 ml / min or serum creatinine concentration more than 300 mcmol / l) should be halved; 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 .; Adults and children over 12 years old should take 1-2 times a day in the form of a cream. Before applying the cream, you must clean and dry the affected skin. The cream is applied with a thin layer on the affected skin and surrounding areas and lightly rubbed. For infections with diaper rash (under the mammary glands, in the interdigital spaces, between the buttocks, in the inguinal region), the cream can be applied under the dressing, especially at night .; Reducing the severity of clinical manifestations is usually observed in the first days of treatment. In the case of irregular use or premature termination of treatment there is a risk of recurrence of the disease. If after 2 weeks of treatment there are no signs of improvement, the diagnosis should be verified .; Elderly patients are prescribed the drug in the same doses as adults, but when prescribing pills, the presence of concomitant hepatic or renal dysfunction in patients of this age group should be considered.
Side effects
On the part of the digestive system: often (1-10%) - dyspepsia, mild abdominal pain, feeling of fullness in the stomach, nausea, loss of appetite, diarrhea; sometimes (0.1-1%) - a violation of taste, including their loss (restored after a few weeks after stopping treatment); rarely (0.01–0.1%) - hepatobiliary disorders primarily associated with cholestasis. 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 their association with Binafine was considered doubtful .; From the musculoskeletal system: often (1-10%) - myalgia, arthralgia .; From the hematopoietic system: very rarely - neutropenia, agranulocytosis,thrombocytopenia .; Local reactions: rarely - hyperemia, itching or burning sensation at the site of application of the cream, which rarely lead to the need to discontinue therapy .; Allergic reactions: often (1-10%) - skin rash, urticaria; very rarely (<0.01%) - toxic epidermal necrolysis, Stevens-Johnson syndrome, anaphylactoid reactions. If a progressive skin rash develops, Binafine treatment should be discontinued .; Other: very rarely - alopecia (a causal relationship with the use of the drug has not been established) .; Binafine is generally well tolerated. Side effects observed when taking Binafina, usually mild or moderately pronounced and are transient in nature.
Overdose
There are reports of several cases of overdose of binafine (the accepted dose was up to 5 g) .; Symptoms: headache, nausea, pain in the epigastric region, dizziness .; Treatment: gastric lavage followed by the use of activated carbon. If necessary, symptomatic therapy is carried out .; Data on terbinafine overdose when applied externally is not. If, by chance, the drug is ingested, one can expect the development of the same side effects as with an overdose of pills.
Interaction with other drugs
The results of studies conducted in healthy volunteers show that Binafine has little ability to reduce or increase the clearance of drugs that are metabolized with the participation of the cytochrome P450 system (including cycloserine, tolbutamide, triazolam, oral contraceptives) .; In vitro studies have revealed that terbinafine inhibits CYP2D6-mediated metabolism. This may be clinically significant while prescribing drugs that are metabolized by this enzyme; such as tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors and MAO inhibitors of type B (especially in cases where the simultaneously used drug has a small therapeutic concentration range) .; In patients who simultaneously take Binafine and oral contraceptives, in some cases, the menstrual cycle is irregular, although the frequency of these disorders remains within the values observed in patients who use only oral contraceptives .; The general clearance of terbinafine can be accelerated by drugs that speed up metabolism (rifampicin) and can be slowed down by drugs that inhibit cytochrome P450 (cimetidine).If necessary, the simultaneous use of these drugs may require adequate dose adjustment .; Drug interaction Binafina in the form of a cream is not described.
special instructions
If a patient develops symptoms of liver dysfunction (weakness, nausea, lack of appetite, vomiting, jaundice, pain in the right hypochondrium, dark urine, or brightening feces) during treatment with binafine, then laboratory confirmation of abnormal liver function (determination of ALT, AST) and cancel the drug. The patient should be warned about the need to consult a doctor if he develops similar symptoms .; It is necessary to constantly monitor patients receiving concurrently with Binafine treatment with drugs mainly metabolized with the participation of the CYP2D6 isoenzyme (including tricyclic antidepressants, beta-adrenoblockers, selective serotonin reuptake inhibitors and MAO inhibitors of type B), especially in cases where at the same time used the drug has a small range of therapeutic concentration .; Terbinafine in the form of a cream is intended for external use only. Avoid getting the cream on the mucous membrane of the eyes .; Use in Pediatrics; There are no data on the use of Binafine pills in children under 2 years of age (whose body weight is less than 12 kg). Binafina tolerability for oral administration is good in children over 2 years old .; It is not recommended to use Binafine cream in children under 12 years old .; Influence on the ability to drive vehicles and control mechanisms; Data on the effect of Binafina on the ability to drive a car and work with mechanisms is absent.