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Active ingredients
Terbinafin
Release form
Pills
Composition
1 tablet contains: Active ingredient: terbinafine hydrochloride 281.31 mg (corresponds to 250 mg of terbinafine); ; Excipients: MCC - 47 mg; sodium starch glycolate - 36.69 mg; pregelatinized starch - 25 mg; anhydrous colloidal silicon - 3 mg; magnesium stearate - 7 mg.
Pharmacological effect
Terbinafine belongs to the group of allylamines, has a broad spectrum of antifungal action. In low concentrations, it has a fungicidal effect on dermatophytes Trychophyton (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (eg. Aspergillus, Cladosporium, Scopulariophoraphiophorathiophora, pyropycosis, mold fungi (for example Aspergillus, Cladosporium, Scopulariomerosis Mushrooms, mold fungi (eg Aspergillus, Cladosporium, Scopulariophorathiophorathiophorathis, Otiscerans, T. violaceumum) fungi, mainly Candida albicans, and some dimorphic fungi. Candida fungi and its mycelial forms have, depending on the type of fungus, an antifungal or fungistatic effect .; Terbinafine violates the early stage of the biosynthesis of the main component of the cell membrane of the fungus ergosterol by inhibiting the enzyme squalene epoxidase. Squalene epoxidase is not associated with the cytochrome P450 (CYP450) system, therefore, terbinafine does not affect the metabolism of hormones and drugs, the metabolism of which is associated with CYP450 .; When administered orally, it accumulates in the skin, nails and hair in an amount that has a fungicidal effect. Systemic treatment of multi-colored lichen caused by Malassezia furfur is ineffective.
Pharmacokinetics
When taken orally, it is well absorbed. After 0.8 hours, half the dose taken is absorbed; After 4–6 hours, half of the dose taken is distributed in the body. After 1–2 hours after ingestion of a single dose of 250 mg Cmax in the blood plasma reaches 0.97 mg / ml. Bioavailability 80%. Eating does not affect the bioavailability of terbinafine .; When applied topically - absorption <5%, has a slight systemic effect .; Terbinafine intensively binds to plasma proteins (99%), spreads rapidly in tissues, penetrates into the dermal layer of the skin and nail plates. It penetrates the secret of the sebaceous glands and accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue. After a few weeks of treatment accumulates in the nails in concentrations that provide fungicidal action. T1 / 2 - 11–18 h, T1 / 2 of the terminal phase - 200–400 h; Biotransformed in the liver to inactive metabolites; 80% of the taken dose is excreted in the urine as metabolites, the rest - 20% with feces. Not cumulated in the body.The age of patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood .; It is excreted in breast milk.
Indications
- onychomycosis caused by dermatophytes; - mycosis 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, Candida albicans) - in cases where localization, severity or prevalence of infection determine the appropriateness of oral therapy.
Contraindications
children's age up to 2 years, because there is not enough data on the use of the drug in children weighing less than 12 kg; pregnancy; breastfeeding period .;
Use during pregnancy and lactation
Contraindicated
Dosage and administration
Inside 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 (1 tablet) 1 time per day .; Onychomycosis: the duration of therapy is about 6-12 weeks. If the nails of the fingers of the hands and feet are affected (except for the big toe) or when the patient is young, the duration of treatment may be less than 12 weeks. With an infection of the big toe, a 3-month course of treatment is usually sufficient. In rare cases, with a slower growth rate of nails, it may require longer treatment - up to 6 months or more .; Fungal infections of the skin: the duration of treatment for interdigital, plantar or sock-like localization of the infection is 2-6 weeks; with mycoses of other parts of the body: the legs - 2–4 weeks, the body - 4 weeks; for mycosis caused by Candida, 2–4 weeks; for head mycosis caused by Microsporum canis - more than 4 weeks .; Children; Usually prescribed 125 mg (1/2 tablet) .; The duration of treatment of mycosis of the scalp is about 4 weeks, while infection with Microsporum canis may be longer .; With a body weight less than 20 kg - 62.5 mg (1/4 tablet) 1 time per day; from 20 to 40 kg - 125 mg (1/2 pills) once a day; more than 40 kg - 250 mg (1 tablet) 1 time per day .; Special patient groups; Elderly patients are prescribed in the same doses as adults .; In cases of marked impaired liver and / or kidney function (creatinine Cl, 300 μmol / l) - 125 mg 1 time per day.
Side effects
On the part of the digestive system: often - a feeling of a full stomach, dyspepsia, nausea, loss of appetite, abdominal pain, diarrhea; not often - a violation of taste perception, incl. loss of taste, which is restored within a few weeks after cessation of treatment; rarely - cholestasis, jaundice, hepatitis, asymptomatic increase in liver transaminase levels. Despite the unproven causation of these disorders with the use of terbinafine, in the case of hepatobiliary dysfunction, treatment with Exifin should be stopped .; From the side of the central nervous system: rarely - paresthesia, hypesthesia, dizziness; very rarely - depression, a feeling of heightened anxiety .; On the part of the musculoskeletal system: often - arthralgia, myalgia .; On the part of the hematopoietic system: very rarely - neutropenia, agranulocytosis, thrombocytopenia .; On the part of the immune system: often - urticaria, erythema multiforme; rarely, systemic allergic reactions (reactions like serum sickness, angioedema); very rarely, severe skin reactions (toxic epidermal necrolysis, Stevens-Johnson syndrome, photosensitivity). With the progression of skin rash, treatment with terbinafine should be discontinued .; Others: often - headache, feeling unwell, feeling tired; very rarely - exacerbation of psoriasis, increased hair loss.
Overdose
Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region .; Treatment: gastric lavage followed by the appointment of activated carbon and / or symptomatic therapy.
Interaction with other drugs
Virtually no effect on clearance of drugs metabolized with cytochrome P450 (for example, cyclosporine, terfenadine, tolbutamide, triazoles, oral contraceptives) .; Inhibits CYP2D6 isoenzyme and interferes with the metabolism of drugs such as tricyclic antidepressants and selective serotonin uptake blockers (for example, desipramine, fluvoxamine), beta-adrenoblockers (metoprolol, propranolol), anti-arrhythmic agents (flekainid, propafenone), and human beings, human beings, human beings, human beings, human beings, human beings, human beings, human beings, human beings, human beings, human beings, human beings, and human beings. and antipsychotic (for example, chlorpromazine, haloperidol) agents. Drug enzyme inducers CYP450 (for example rifampicin) can accelerate the excretion of terbinafine from the body .; Medicinal preparations inhibiting CYP450 (for example, cimetidine) can slow down the metabolism and excretion of terbinafine from the body.With the simultaneous use of these drugs may require dose adjustment of terbinafine .; Possible violation of the menstrual cycle while taking terbinafine and oral contraceptives .; Reduces caffeine clearance by 21% and prolongs its half-life by 31%; Does not affect the clearance of antipyrine, digoxin, warfarin .; Ethanol and other hepatotoxic drugs increase the risk of a hepatotoxic effect.
special instructions
Irregular use of terbinafine or premature discontinuation of treatment leads to a relapse of the disease .; Such factors as, for example, the presence of concomitant diseases, the condition of the nails at the beginning of the course of treatment can also influence the duration of therapy .; If after 2 weeks of treatment of a skin infection there is no improvement in the condition, it is necessary to re-determine the causative agent and its sensitivity to the drug .; Systemic use in onychomycosis is justified only in the case of a total lesion of most nails, the presence of pronounced subungual hyperkeratosis, the ineffectiveness of the previous local therapy. In the treatment of onychomycosis, the clinical response is usually observed several months after mycological cure and cessation of treatment, due to the rate of growth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks is not required .; In the presence of severe renal failure (Cl creatinine 300 μmol / l), in violation of liver function, the dose of terbinafine should be reduced by half .; In the presence of liver disease, the clearance of terbinafine may be reduced. With reduced liver function, half of the adult dose is prescribed. During treatment, it is necessary to control the level of liver transaminases in the serum. In rare cases, after 3 months of treatment, cholestasis and hepatitis occur. If there are signs of abnormal liver function (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice, dark urine or colorless stools), the drug should be discontinued .; Appointment of terbinafine to patients with psoriasis requires increased diligence, because in very rare cases, terbinafine can trigger an outbreak of psoriasis .; When treating with terbinafine, the general rules of hygiene should be followed to prevent the possibility of re-infection through underwear and shoes.In the process of treatment (every 2 weeks) and at the end it is necessary to produce antifungal treatment of shoes, socks and stockings .; Influence on the ability to drive and work mechanisms: terbinafine does not affect the ability to drive and perform work that requires increased concentration of attention.