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Active ingredients
Terbinafin
Release form
Pills
Composition
1 tablet, film coated contains: Active substance: nifuroksazid 100 mg. Excipients: colloidal silicon dioxide (Aerosil hydrophilic 200) 3.0 mg, potato starch 179.0 mg, gelatin 11.0 mg, talc 6.0 mg, magnesium stearate 1.0 mg. Tablet shell: hypromellose 3.0 mg, titanium dioxide 0.252 mg, talc 0.062 mg, polyethylene glycol 20 000 0.01 mg, dye quinoline yellow 0.112 mg.
Pharmacological effect
Antifungal medication. Terbinafine is an allylamine derivative. It has a wide range of antifungal action. In therapeutic concentrations, terbinafine has a fungicidal effect on: dermatophytes - Trichophyton, Microsporum, Epidermophyton; yeast-like fungi: The genus Candida: Candida albicans; some dimorphic fungi. Pityrosporum orbiculare: Malassezia furfur. Activity against yeast fungi, depending on their species, can be fungicidal or fungistatic. Terbinafine specifically inhibits the early stage of biosynthesis of sterols in the cell of the fungus by inhibiting the enzyme squalene epoxidase in the cell membrane 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. Squalene epoxidase does not belong to the cytochrome P450 system, therefore, 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 C max in plasma is reached after 2 hours and amounts to 0.97 mcg / ml. Eating does not affect the bioavailability of terbinafine. When applied topically, less than 5% of the dose is absorbed. Distributed Plasma protein binding is 99%. When applied topically, 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 leads to the creation of high concentrations in the hair follicles and nails. During the first few weeks after starting the drug inside, terbinafine accumulates in the skin and nail plates in concentrations that provide fungicidal action. Terbinafine is excreted in breast milk. Metabolism and excretion of Terbinafine is metabolized in the liver to form inactive metabolites. Most of the inactive metabolites (71%) are excreted in the urine, a smaller part (22%) - in the feces. T1 / 2 is from 11 to 17 hours. There is no evidence that the drug is cumulated in the body.Pharmacokinetics in special clinical situations In patients with impaired liver or kidney function, the rate of excretion of terbinafine from the body may decrease.
Indications
Onychomycoses, mycoses of the skin, severe common mycoses (body, legs, feet), mycoses of the scalp caused by dermatophytes.
Contraindications
Hypersensitivity to the drug; pregnancy and lactation (breastfeeding); children's age up to 2 years.
Use during pregnancy and lactation
Due to the fact that data on the safety of terbinafine use in pregnant women are not available, Terbisil in this category of patients is used only in cases where the expected positive effect outweighs the potential risk. Terbinafine is excreted in breast milk, so the use of the drug during lactation is contraindicated.
Dosage and administration
Inside, after eating. The duration of the course of treatment and the dosage regimen are set individually and depend on the localization process and the severity of the disease. Adults. The usual dose is 250 mg / day. Onychomycosis: the duration of treatment is on average 6–12 weeks. If the nails of the fingers of the hands and feet (except for the big toe) are affected or in young patients, the treatment can be less than 12 weeks. With an infection of the big toe, a 3-month course of treatment is usually sufficient. Some patients who have reduced growth rate of the nails may require a longer period of treatment. Fungal infections of the skin: the duration of treatment for interdigital, plantar or sock-type localization of the infection is 2–6 weeks, for mycoses of the legs - 2–4 weeks, and the body –– 2–4 weeks; for fungal infections caused by Candida, 2–4 weeks; with mycoses of the scalp caused by fungi of the genus Microsporum, more than 4 weeks. Children. Usually prescribed 125 mg. With a body weight of 20 to 40 kg - 125 mg / day. With a body weight of more than 40 kg - 250 mg / day. The duration of treatment of mycosis of the scalp is about 4 weeks, while infection with Microsporum canis can be longer. Elderly patients are prescribed in the same doses as adults. Terbisil is prescribed in a dose of 125 mg per day in patients with hepatic and renal insufficiency.
Side effects
On the part of the digestive system: often - feeling of fullness in the stomach, loss of appetite, dyspepsia, nausea, mild abdominal pain, diarrhea; rarely, disturbances or loss of taste (recovery occurs within a few weeks after stopping treatment); in some cases - cholestasis, jaundice, hepatitis (although the causal relationship of these disorders with the administration of Terbisil has not been established, in the case of hepatobiliary dysfunction, treatment with the drug should be canceled). From the hematopoietic system: in some cases - neutropenia, thrombocytopenia. Allergic reactions: often - rash, urticaria: in some cases - Stevens-Johnson syndrome, toxic epidermal necrolysis (with the development of progressive skin rash, treatment with Terbisil should be stopped).
Overdose
Symptoms: nausea, vomiting, pain in the lower abdomen. Treatment: gastric lavage followed by the use of activated carbon. If necessary, conduct symptomatic therapy.
Interaction with other drugs
Terbisil has a slight ability to slow down or increase the clearance of drugs that are metabolized by isoenzymes of the cytochrome P 450 system (cyclosporine, tolbutamide, oral contraceptives). Terbinafine excretion can be accelerated by drugs that induce the induction of microsomal liver enzymes (rifampicin). Drugs inhibiting cytochrome P 450 (cimetidine) isoenzymes slow down terbinafine excretion. If necessary, the simultaneous use of these drugs may require dose adjustment Terbisil.e
special instructions
Use in patients with impaired liver function Patients with severely impaired liver function should reduce the dose of the drug Use in cases of impaired renal function Patients with severe impaired renal function (CC less than 50 ml / min or serum creatinine levels should be reduced by half . It should be borne in mind that if a patient has abnormal liver function (weakness, nausea of unclear etiology, lack of appetite, jaundice, dark urine or lightening feces) during treatment with Terbisil, the patient should be discontinued. During treatment, it is necessary to control the level of hepatic transaminases.When treating with Terbisil, the general rules of hygiene should be followed to prevent the possibility of re-infection (through underwear or shoes). It should be borne in mind that the irregular use or premature withdrawal of the drug leads to a relapse of the disease.