Composition, form of production and packaging
Tablets 1 tab.
terbinafine (in the form of hydrochloride) 250 mg
Excipients: microcrystalline cellulose (type 102) - 47 mg, sodium starch glycolate (type A) - 36.96 mg, pregelatinized starch - 25 mg, magnesium stearate - 7 mg, silicon colloidal anhydrous - 3 mg.
4 things. - blisters (4) - packs of cardboard.
4 things. - blisters (5) - packs of cardboard.
4 things. - blisters (7) - packs of cardboard.
4 things. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Terbinafine belongs to the group of allylamines. Has a wide range of antifungal action. At low concentrations, it has a fungicidal effect on Trychophyton dermatophytes (T. rubrum, T. menlagrophytes, T. tonsurans, T. verrucosum, T.violaccum), Microsporum canis, Epidermophyton floccosum, mold fungi (eg, Aspergillus, Cladosporium, Scopulariopsis brevicalius) yeast fungi, mainly Candida albicans, and some dimorphic fungi. Candida fungi and its mycelial forms, depending on the type of fungus, have a fungicidal or fungistatic effect. Terbinafine disrupts the early stage of biosynthesis of the main component of the cellular membrane of the ergostrotal fungus by inhibiting the squalene-epoxidase enzyme. Squalene-epoxidase is not associated with the cytochrome P450 (CYP450) system, so terbinafine does not affect the metabolism of hormones and drugs whose metabolism 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 varicolored lichen, caused by Malassezia furfur, is ineffective.
PHARMACOKINETICS
When oral intake is well absorbed, after 0.8 h half of the dose is absorbed; After 4.6 h half of the dose taken is distributed in the body. After 1-2 hours after ingestion of a single 250 mg dose of C max drug in the blood plasma reaches 0.97 Ојg / ml. Bioavailability - 80%. The intake of food does not affect the bioavailability of terbinafine.
Terbinafine binds intensely to blood plasma proteins (99%), spreads rapidly in tissues, penetrates the dermal layer of the skin and the new platelets. Penetrates the secretion of sebaceous glands and accumulates in high concentrations in the hair follicles, in hair, skin and in the subcutaneous tissue. After a few weeks of treatment, it accumulates in nails and in concentrations that provide a fungicidal effect. T 1/2 - 16-18 h. T 1/2 of the terminal phase - 200-400 h.
Biotransformed in the liver to inactive metabolites: 80% of the accepted dose is excreted in the urine in the form of metabolites, the rest (20%) with fecal masses. Do not cum in the body. The age of the 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 together with breast milk.
INDICATIONS
- mycoses of the scalp (trichophytosis, microsporia);
- mycosis of the skin and nails, caused by Trychophyton (T. rubnim, T. mentagrophytes, T. verrucosum, T. violaceum). Microsporum (M. canis, M. gypseum) and Epidermophylum floccosum;
- onychomycosis;
- severe, common dermatomycosis of the smooth skin of the trunk and extremities, requiring systemic treatment;
Candidiasis of the skin and mucous membranes.
DOSING MODE
The duration of the course of treatment and the dosage regimen is established individually and depends on the localization of the process and the severity of the disease.
Onychomycosis
Usual dose: 250 mg 1 time / day. The duration of therapy is about 6-12 loops. If the fingernails of the hands and feet are injured (except for the large finger, groans), or when the patient is young, the duration of the treatment may be less than 12 weeks. With a large toe infection, a 3-month course of treatment is usually sufficient. In rare cases, with a slower rate of nail growth, longer treatment may be required up to 6 months or more.
Fungal infections of the skin.
The duration of treatment with interdigital, plantar, or "socks" localization of infection is 2-6 weeks, with mycoses of other parts of the body: shins - 2-4 weeks, trunks - 4 weeks, with mycoses caused by Candida - 2-4 weeks; with mycosis head caused by Microsporum canis - more than 4 weeks.
Children are 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.
At a body weight of less than 20 kg , 62.5 mg (1/4 tablet) once a day, at a weight of 20 to 40 kg , 125 mg (1/2 tablet) once a day, at a mass greater than 40 kg , 250 mg 1 tablet) 1 time / day.
Older patients are prescribed in the same vines as adults.
In severe violations of the liver and / or kidney function (SC 50 ml / min or creatinine concentration in the blood more than 300 Ојmol / l) - 125 mg 1 time / day.
SIDE EFFECT
Side effects are usually of medium and mild severity and are temporary.
From the digestive system: often - a feeling of a full stomach, dyspepsia, nausea, loss of appetite, abdominal pain, diarrhea; infrequent - a violation of taste perception, incl. loss, which is restored a few weeks after the cessation of treatment; rarely - cholestasis, jaundice, hepatitis, an asymptomatic increase in the level of liver granasaminase. Despite the lack of evidence of a causal relationship of these disorders with the use of terbinafine, in the case of development of hepatobiliary dysfunction treatment Exifin should be discontinued.
From the side of the central nervous system: rarely - paresthesia, hypoesthesia, dizziness; very rarely - depression, a feeling of heightened anxiety.
From the musculoskeletal system: often - arthralgia, myalgia.
From the hemopoietic system: very rarely - neutropenia, agranulocytosis, thrombocytopenia.
From the immune system: often - hives, 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 rashes, treatment with terbinafine should be discontinued.
Other: often - headache, poor health, feeling tired; it is very rare - exacerbation of psoriasis, increased hair loss.
CONTRAINDICATIONS
- Children's age to 2 years, tk. there is insufficient data on the use of the drug by children weighing less than 12 kg;
- Pregnancy;
- the period of breastfeeding;
- Hypersensitivity to the components of the drug.
With caution: hepatic and / or renal insufficiency; alcoholism; blood diseases; tumors; metabolic diseases; pathology of the vessels of the extremities, psoriasis.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Carefully.
In severe disorders of the function or kidneys (SC 50 ml / min or creatinine concentration in the blood more than 300 Ојmol / l) - 125 mg 1 time / day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Carefully.
At the expressed infringements of function of a liver - 125 mg 1 time / sut.
APPLICATION FOR CHILDREN
Contraindicated:
- Children's age to 2 years, tk. There is not enough data on the use of the drug by children weighing less than 12 kg.
Children are 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.
At a body weight of less than 20 kg , 62.5 mg (1/4 tablet) once a day, at a weight of 20 to 40 kg , 125 mg (1/2 tablet) once a day, at a mass greater than 40 kg , 250 mg 1 tablet) 1 time / day.
APPLICATION IN ELDERLY PATIENTS
Older patients are prescribed in the same vines as adults.
SPECIAL INSTRUCTIONS
Irregular application of terbinafine or premature discontinuation of treatment leads to a relapse of the disease.
The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the condition of the nails at the beginning of the course of treatment.
If after 2 weeks of treatment of skin infection there is no improvement, it is necessary to re-determine the pathogen and its sensitivity to the drug.
Systemic use in onychomycosis is justified only in case of total defeat of most nails, the presence of pronounced subungual hyperkeratosis, ineffectiveness of previous local therapy. In the treatment of onychomycosis, the clinical response is usually observed a few months after mycological cure and cessation of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis for 3 weeks. and onychomycosis of the feet for 6 weeks. not required.
In the presence of severe renal failure (creatinine clearance less than 50 ml / min or creatinine in the blood more than 300 Ојmol / L), if the liver function is disrupted, the dose of terbinafine should be reduced by half.
In the presence of liver disease, the terbinafine clearance can be reduced.
With reduced liver function, appoint a half-adult dose. During treatment, it is necessary to control the level of liver transaminases in the blood serum. In rare cases, after 3 months of treatment, there is cholestasis and hepatitis. If there are signs of impaired liver function (weakness, persistent nausea, loss of appetite, abdominal pain, jaundice, darkening of the urine or colorless stools), the drug should be discarded.
The administration of terbinafine to psoriasis patients requires increased discretion; in very rare cases terbinafine can trigger an outbreak of psoriasis.
When treating terbinafions, general hygiene rules should be followed to prevent the possibility of re-infection through linen and shoes. In the process of treatment (every 2 weeks) and at the end of it, it is necessary to produce antifungal treatment of shoes, socks and stockings.
Impact on the ability to drive vehicles and manage mechanisms
Terbinafine does not affect the ability to drive and perform work that requires increased concentration.
OVERDOSE
Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region.
Treatment: gastric lavage followed by prescription of activated charcoal and / or symptomatic therapy
DRUG INTERACTION
Virtually no effect on the clearance of drugs metabolized with the participation of cytochrome P450 (eg, cyclosporine, terfenadine, tolbutamide, triazolam, oral contraceptives).
It inhibits CYP206 and interferes with the metabolism of such drugs as tricyclic antidepressants and selective serotonin uptake blockers (desipramine, fluvoxamine), beta adrenoblockers (metoprolol, propranolol), antiarrhythmics (flecainide, proavfenon), MAO inhibitors of type B (sellegin) and antinsychotic (chlorpromazine , haloperidol).
Drugs - inducers of CYP450 enzymes (for example, rifampicin) can accelerate the excretion of terbinafine from the body.
Drugs - inhibitors of CYP450 (for example, cimetidine) can slow the metabolism and excretion of terbinafine from the body. With the simultaneous use of these drugs, a dose adjustment of terbinafine may be required.
Possible violation of the menstrual cycle with the simultaneous administration of terbinafine and oral contraceptives.
Decreases 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 developing a hepatotoxic effect.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dry place protected from light, out of the reach of children, at a temperature of up to 25 В° C. Shelf life - 3 years.
