More info
Active ingredients
Terbinafin
Release form
Pills
Composition
1 tablet contains: Active ingredient: terbinafine (in the form of hydrochloride) - 250 mg; Excipients: magnesium stearate; silica colloidal anhydrous; methyl hydroxypropyl cellulose; sodium glycolate starch; MCC.
Pharmacological effect
antifungal, fungicidal, fungistatic
Pharmacokinetics
After oral administration, terbinafine is well absorbed (more than 70%); The absolute bioavailability of terbinafine due to the effect of the first passage is approximately 50%. After a single dose of terbinafine orally at a dose of 250 mg of its Cmax in plasma is reached in 1.5 hours and is 1.3 μg / ml. With continuous use of terbinafine, its Cmax increased on average by 25%, compared with a single dose; AUC increased 2.3 times. Based on the increase in AUC, it is possible to calculate the effective T1 / 2 - 30 h. Eating a little effect on the bioavailability of the drug (AUC increases by less than 20%), therefore, do not require dose adjustment of the drug Lamisil while taking it with food. Terbinafine degree binds to plasma proteins (99%). It quickly penetrates the dermal layer of the skin and concentrates 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, 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 quickly and to a significant extent with the participation of at least 7 cytochrome P450 isoenzymes, with the CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C9 isoenzymes playing the main role, and CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C9 isoenzymes play the main role. As a result of terbinafine biotransformation, metabolites are formed that do not have antifungal activity and are excreted mainly in the urine. No changes in plasma equilibrium concentration of terbinafine are observed depending on age. In pharmacokinetic studies of a single dose of Lamisil in patients with concomitant renal impairment (Cl creatinine less than 50 ml / min) and with liver disease was shown the possibility of reducing Cl drug by 50%.
Contraindications
Hypersensitivity to terbinafine or to any other ingredient of the drug.
Dosage and administration
The duration of treatment depends on the indication and severity of the disease. There are no data on the use of the drug in children under 2 years of age (whose body weight is usually less than 12 kg). In children older than 2 years, Lamisil tolerability for oral administration is good. Body Weight Dozhemene 20 kg 62.5 mgot 20 to 40 kg 125 mg more than 40 kg 250 mg Adults are prescribed 250 mg 1 time / day. The recommended duration of treatment for ringworm (interdigital, plantar foot or type of socks) - 2-6 weeks; with ringworm of the trunk, legs - 2-4 weeks; with candidiasis of the skin - 2-4 weeks. The complete disappearance of the manifestations of infection and complaints associated with it, can occur only a few weeks after mycological cure. The recommended duration of treatment for mycosis of the scalp is 4 weeks. Mycoses of the scalp are observed mainly in children. In onychomycosis, the duration of effective treatment is in most patients from 6 to 12 weeks. With onychomycosis of the hands, in most cases 6 weeks of treatment is sufficient. With onychomycosis, in most cases, 12 weeks of treatment is 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 necessary for the regrowth of a healthy nail. There is no reason to assume that elderly people need to change the dosage of the drug or that they have adverse reactions 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
From the side of the hematopoietic system: very rarely - neutropenia, agranulocytosis, pancytopenia. In very rare cases, when using the drug, the development of qualitative or quantitative changes in the form of blood cells (neutropenia, agranulocytosis, thrombocytopenia, pancytopenia) was noted. In the case of the development of qualitative or quantitative changes on the part of the blood cells, it is necessary to establish the cause of the disorders and consider reducing the dose of the drug or, if necessary, stopping therapy with Lamisil. From the immune system: very rarely - anaphylactoid reactions (including angioedema)cutaneous and systemic lupus erythematosus. From the nervous system: often - headache; sometimes - taste disorders, including their loss (usually recovery occurs within a few weeks after stopping treatment); very rarely - dizziness, paresthesia, hypoesthesia. There are separate reports of cases of long-lasting taste disturbances. In some cases, the intake of the drug showed a decrease in food intake, which led to a significant decrease in weight. From the hepatobiliary system: rarely - hepatobiliary dysfunction (mostly cholestatic), including very rare cases of severe liver failure (some are fatal or require liver). In most cases, when liver failure developed, patients had serious concomitant systemic diseases and a causal relationship to liver failure with Lamisil was doubtful. abdominal pain, diarrhea. From the side of the skin and subcutaneous tissue: very often mild skin reactions (rash, urticaria); very rarely - serious skin reactions (including Stevens-Johnson syndrome, toxic epidermal necrolysis); psoriasis-like skin rash or exacerbation of psoriasis. Cases of hair loss have been reported very rarely, although the causal relationship of this phenomenon with the intake of the drug has not been established. In the event that a progressive skin rash develops, treatment should be stopped. On the part of the musculoskeletal system: very often - arthralgia, myalgia. Others: very rarely - a feeling of fatigue.
Overdose
Symptoms: there are reports of several cases of overdose (the accepted dose of the drug was up to 5 g), in which headache, nausea, pain in the epigastric region and dizziness were noted. activated carbon and gastric lavage.
Interaction with other drugs
Effect of other drugs on terbinafine.Plasma Cl of terbinafine can be accelerated under the influence of drugs, metabolism inducers, and suppressed under the influence of cytochrome P450 inhibitors. If necessary, the simultaneous use of the above drugs and Lamisil may require an appropriate correction of the dosing regimen of the latter. Cimetidine may enhance the effect of terbinafine or increase its concentration in plasma. Cimetidine reduces the Cl of terbinafine by 33%. Rifampicin may weaken the effect of terbinafine or reduce its concentration in plasma. Rifampicin increases the terbinafine Cl by 100%. The effect of terbinafine on other drugs. In vitro and healthy volunteer studies have shown that terbinafine has little potential for suppressing or enhancing the Cl of most drugs that are metabolized with the cytochrome P450 system (for example, terfenadine, triazolam, tolbutamide, or oral contraceptives), with the exception of those metabolized with the participation of CYP2D6. Terbinafine does not affect Cl antipyrine or digoxin. There are reports of several cases of menstrual irregularities in patients treated with Lamisil is associated with oral contraceptives, although the frequency of these disorders does not exceed the average frequency of such disorders in patients who take only oral contraceptives. Terbinafine may increase the effect of caffeine or increase its concentration in plasma. Terbinafine reduces Cl of caffeine with a / in the introduction of 19%. In studies in vivo and in vitro, it was shown that terbinafine inhibits metabolism mediated by the enzyme 2D6 (CYP2D6). These data may be clinically significant for those drugs that are metabolized mainly by this enzyme: tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors, antiarrhythmic drugs of class (1A, 1B and 1C) and MAO B type inhibitors - in that case if used at the same time the drug has a small therapeutic concentration range. Terbinafine reduces Cl desipramine by 82%. Terbinafine may weaken the effect of cyclosporine and reduce its concentration in plasma. Terbinafine increases Cl cyclosporine by 15%.