Terbinafine Canon 250mg N14 Tablets
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Active ingredients
Terbinafin
Release form
Pills
Composition
1 tablet of 250 mg contains: Active ingredient: terbinafine hydrochloride 281.4 mg, in terms of terbinafine 250 mg; Excipients: hyprolose (hydroxypropylcellulose) 11 mg, calcium stearate 3.6 mg, silicon dioxide colloid 4 mg, croscarmellose sodium 10 mg, microcrystalline cellulose 60 mg.
Pharmacological effect
Terbinafine is an allylamine that has a wide spectrum of action against fungi that cause skin, hair and nail diseases, including dermatophytes such as Trychophyton (for example, T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum, T Tonsurans), Microsporum (M. canis), Epidermophyton floccosum, as well as yeast fungi of the genus Candida (for example, C. albicans) and Pityrosporum. In low concentrations, terbinafine has a fungicidal effect against dermatophytes, molds and some dimorphic fungi. Activity against yeast fungi, depending on their type, can be fungicidal or fungistatic.; Terbinafine, inhibiting the enzyme squalene epoxidase in the cell membrane of the fungus (not related to the cytochrome P450 system), specifically inhibits the early stage of sterol synthesis in the cell of the fungus, which leads deficiency of ergosterol, intracellular accumulation of squalene and cell death of the fungus.; When terbinafine is used internally, concentrations are created in the skin, hair and nails that provide fungicidal action.
Pharmacokinetics
After oral administration, terbinafine is well absorbed (more than 70%); The absolute bioavailability of terbinafine due to the “first pass” effect is approximately 50%. After a single dose of terbinafine orally at a dose of 250 mg, its maximum plasma concentration (C max) is reached in 1.5 hours and is 1.3 μg / ml. With continuous use of terbinafine, its C max is increased on average by 25% compared with a single dose; the area under the concentration-time curve (AUC) increases 2.3 times. Based on the increase in AUC, it is possible to calculate the effective half-life (30 hours). Meal moderately affects the bioavailability of the drug (AUC increases by less than 20%), dose adjustment of the drug Terbinafine Canon while taking with food is not required. Terbinafine largely bound 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. Terbinafine penetrates 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 main role played by CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19 isoenzymes. As a result of terbinafine biotransformation, metabolites are formed that do not have antifungal activity and are excreted mainly by the kidneys. Multiple use of terbinafine, leading to an increase in its concentration in serum, is accompanied by a three-phase elimination with a final half-life of about 16.5 days; No changes in the equilibrium concentration of terbinafine are found; in plasma, depending on age. In pharmacokinetic studies, a single dose of terbinafine in patients with concomitant dysfunction kidney (creatinine clearance; less than 50 ml / min) and with liver disease was shown the possibility of reducing the clearance of the drug by 50%.
Indications
Mycoses caused by microorganisms sensitive to terbinafine: Onychomycosis caused by dermatophytes; Mycoses of the scalp; Fungal infections of the skin - treatment of ringworms of the body, legs, feet, and yeast infections of the skin caused by Candida fungi (for example, C. albicans) - in cases where the localization, severity or prevalence of the infection causes the expediency of oral therapy.
Contraindications
hypersensitivity to terbinafine or to any other component of the drug; children up to 3 years old, with body weight less than 20 kg (no data on the application); severe, chronic or active liver disease; renal dysfunction (creatinine clearance less than 50 ml / min or serum creatinine concentration more than 300 mcmol / l), because the use of the drug in this category of patients is not well understood.
Use during pregnancy and lactation
These experimental studies do not suggest an adverse event in relation to fertility and toxic effects on the fetus.; Clinical experience with the use of terbinafine in pregnant women is limited,as a result, you should not use the drug during pregnancy, except in cases where the expected benefit to the mother from therapy exceeds the potential risk to the fetus.; Terbinafine is excreted in breast milk, therefore the drug is contraindicated during breastfeeding.; Data on the effect of the drug on people do not have fertility. Studies in rats did not reveal an undesirable effect on fertility and reproductive ability.
Dosage and administration
The duration of treatment depends on the indication and severity of the disease. The drug is taken orally, regardless of the meal, with a small amount of water. It is advisable to take the drug at the same time. The duration of treatment depends on the indication and severity of the disease.; Adults; 250 mg 1 time per day.; Infections of the skin; Recommended duration of treatment: foot ringworm (interdigital, plantar or socks) - 2-6 weeks; dermatomycosis of the trunk, legs - 2-4 weeks; skin candidiasis - 2-4 weeks. The complete disappearance of the manifestations of infection and complaints associated with it may occur no earlier than a few weeks after mycological cure.; Infections of the hair and scalp; Recommended duration of treatment: mycosis of the scalp - 4 weeks. Mycoses of the scalp are observed mainly in children. Onychomycosis; The duration of treatment in most patients is from 6 to 12 weeks. With onychomycosis of the hands, in most cases 6 weeks of treatment is sufficient. With onychomycosis, in most cases it is enough; 12 weeks of treatment. 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.; Use in children; There is no data on the use of the drug in children under 3 years of age (whose body weight is usually less than 12 kg). The use of the drug for treatment in children weighing less than 20 kg is not recommended due to the impossibility of adequate dose selection.Use in children from 3 to 12 years old with a body weight of more than 20 kg is advisable only in the case when the positive expected effect from the therapy outweighs the potential risk of side effects. The duration of treatment and doses depend on the body weight of the child. In children older than 3 years, the drug is prescribed 1 time per day. A single dose is: for children weighing from 20 to 40 kg -; 125 mg; more than 40 kg - 250 mg.; Use in elderly patients; There is no reason to assume that for elderly patients it is required to change the dosage regimen 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
Terbinafine is generally well tolerated. Side effects are usually mild or moderate and transient. Below are the adverse events that were observed during clinical studies or in the post-registration period. The frequency of side effects was assessed as follows: very often (≥1 / 10); often (≥1 / 100, less than 1/10); infrequently (≥1 / 1000, less than 1/100); rarely (≥1 / 10,000, less than 1/1000); very rarely (less than 1 / 10,000, including isolated cases), the frequency is unknown (the frequency of side effects cannot be estimated based on the available data); Disorders of the blood and lymphatic system; infrequently - anemia; very rarely - neutropenia, agranulocytosis, pancytopenia, thrombocytopenia.; Immune system disorders; very rarely - anaphylactoid reactions (including angioedema), systemic lupus erythematosus (or their exacerbation); Mental disorders, often - depression; rarely - anxiety.; Violations of the nervous system; very often - headache; often - dizziness, taste disturbances, up to their loss (usually recovery occurs within a few weeks after stopping treatment. There are some reports of cases of long-term taste disturbances). In some cases, on the background of taking the drug was observed exhaustion; infrequently - paresthesia, hypoesthesia.; Violations on the part of the organ of vision; infrequently - visual disturbances.; Violations on the part of the organ of hearing and labyrinth disorders; rarely - tinnitus.; Violations on the gastrointestinal tract; very often - bloating, reduction appetite, dyspepsia, nausea, mild abdominal pain,diarrhea; disorders of the liver and biliary tract; rarely - hepatobiliary dysfunction (mainly cholestatic), including liver failure, including very rare cases of severe liver failure (some fatal or requiring liver transplantation; in most cases, liver failure developed, patients had serious concomitant systemic diseases and the causal relationship of liver failure to the drug was associated with tively); hepatitis, jaundice, cholestasis, increased activity of "liver" transaminases.; Violations of the skin and subcutaneous tissue; very often - rash, urticaria; infrequently - photosensitivity reactions; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematoid pustus, erythema multiforme, toxic skin rash, exfoliative dermatitis, bullous dermatitis, psoriasis-like rashes or exacerbation of psoriasis, alopecia. often - arthralgia, myalgia.; General disorders; often - feeling tired; infrequently - increased body temperature.; Laboratory and instrumental data: infrequently - weight reduction (secondarily with respect to taste disturbances); Based on spontaneous messages received during the post-registration period and literature data, the following adverse events have been identified, the frequency of which is due to inaccurate amounts patients can not be installed: Impairment of the immune system; Anaphylactic reactions, a syndrome similar to serum sickness; Disruption of the organ of vision; Blurred vision , loss of visual acuity. Disturbances of the skin and subcutaneous tissues; Drug rash with eosinophilia and systemic symptoms (rash, edema, fever and swollen lymph nodes); Disturbances of the organ of hearing and labyrinth disorders; Deafness, hearing impairment. Disturbances vascular; Vasculitis.; Disturbances of the nervous system; Loss of smell, including for a long period of time, reduced smell.; Disorders of the gastrointestinal tract; Pancreatitis.; Disorders of the musculoskeletal and connector Noah; Rhabdomyolysis; Generaldisorders; Influenza-like syndrome; Laboratory and instrumental data; Increased serum creatine phosphokinase activity.; If any of the side effects indicated in the instruction are compounded, or you notice any other side effects that are not indicated in the instruction, inform your doctor.
Overdose
Symptoms: headache, nausea, pain in the epigastric region and dizziness. The treatment recommended in case of overdose includes measures to remove the drug, primarily by administering activated charcoal and washing the stomach; Symptomatic and supportive therapy is performed if necessary.
Interaction with other drugs
The effect of other drugs on terbinafine; Plasma clearance 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 terbinafine 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 clearance of terbinafine by 33%; Fluconazole increases Cmax and AUC of terbinafine by 52% and 69%, respectively, due to inhibition of the CYP2C9 and CYP3A4 isoenzyme. A similar increase in terbinafine exposure may occur when other drugs inhibiting CYP2C9 and CYP3A4 isoenzymes, such as ketoconazole and amiodarone, are used. Rifampicin may weaken the effect of terbinafine or decrease its plasma concentration. Rifampicin increases the clearance of terbinafine by 100%; the effect of terbinafine on other drugs; Terbinafine inhibits metabolism mediated by isoenzyme 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 (class 1A, 1B, and 1C) and monoamine oxidase B inhibitors of the type - in the case if used at the same time the drug has a small therapeutic concentration range.; Terbinafine reduces the clearance of desipramine by 82%; In studies on healthy volunteers with active metabolism Extrofetorphan (an antitussive and CYP2D6 substrate) terbinafine increased the metabolic coefficient of dextromethorphan / dextrorphan in urine 16-97 times.Thus, terbinafine in individuals with high activity of the CYP2D6 isoenzyme can reduce the activity of the latter. Terbinafine reduces caffeine clearance by intravenous administration by 19%. Drug interactions that do not or have little effect; Terbinafine has little potential to suppress or increase the clearance of most drugs that are metabolized by the cytochrome P450 system (for example, terfenadine, triazolam, tolbutamide, or oral contraceptives), with the exception of those that metabolized with CYP2D6. Terbinafine does not affect the clearance of phenazone or digoxin. Terbinafine does not significantly affect the pharmacokinetics of fluconazole. There were no clinically significant interactions between terbinafine and components of cotrimoxazole (trimethoprim and sulfamethoxazole), zidovudine or theophylline. If you take terbinafine with oral contraceptives at the same time, menstrual disorders may occur, although the frequency of these disorders does not exceed the average frequency of such disorders in patients receiving oral administration. contraceptives. Terbinafine may decrease serum concentration or the severity of the clinical effects of the following drugs; Terbine Athens increases the clearance of cyclosporine by 15%; Interaction with food and beverages; Food slightly affects the bioavailability of terbinafine (an increase in AUC of less than 20%), which does not require changing the dose of the drug.
special instructions
Irregular use or early termination of treatment increases the risk of recurrence of the disease. Before the use of terbinafine pills, it is necessary to analyze the function of the liver. Hepatotoxicity can occur both in patients with previous liver diseases, and without them. During therapy, periodic examination of liver function is recommended (4-6 weeks after starting treatment). Treatment should immediately be discontinued in the event of increased activity of "liver" samples. Patients who are prescribed the drug should be warned that it is necessary to immediately inform the attending physician about the occurrence of symptoms such as persistent nausea, loss of appetite, fatigue, vomiting, pain in the right hypochondrium, jaundice, dark urine or light feces. .In the event of these symptoms, it is necessary to immediately stop taking the drug and conduct a study of liver function. Serious skin reactions (including Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms) were rarely observed while using terbinafine .; When using the drug in pills, extremely rare changes in the cellular composition of the blood were noted (neutropenia, agranulocytosis, thrombocytopenia, pancytopenia). 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, discontinuing therapy with the drug.