Composition, form of production and packaging
Tablets are white or white with a yellowish tint of color with a facet and a risk.
terbinafine (in the form of hydrochloride) 250 mg
[PRING] microcrystalline cellulose 0.08 g, giprolose (hydroxypropyl cellulose) 0.025 g, croscarmellose sodium 0.08 g, silicon dioxide colloid 0.01 g, calcium stearate 0.005 g, lactose monohydrate to obtain a tablet weighing 0.5 g.
7 pcs. - packings of cellular contour (1) - packs cardboard.
7 pcs. - packings cellular planimetric (2) - packs cardboard.
7 pcs. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
Terbinafine is an allylamine that has a broad spectrum of action against fungi that cause skin, hair and nail diseases, including dermatophytes. At low concentrations, it has a fungicidal effect on the Tryphophyton spp. Dermatophytes. (T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (eg, Aspergillus, Cladosporium, Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans. At low concentrations terbinafine has a fungicidal effect against dermatophytes, molds and some dimorphic fungi. Activity with respect to yeast fungi, depending on their type, may be fungicidal or fungistatic.
Terbinafine specifically suppresses the early stage of biosynthesis of sterols in the fungal cell. This leads to a deficiency of ergosterol and to intracellular accumulation of squalene, which causes death of the fungal cell. The action of terbinafine is carried out by inhibiting the enzyme squalene epoxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system. Terbinafine does not affect the metabolism of hormones or other medications.
When taking terbinafine inside the skin, hair and nails are created concentrations of the drug, providing fungicidal effect.
When administered orally, it is not effective in treating multicolored lichen caused by Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).
After a single administration of terbinafine inwards at a dose of 250 mg, its C max in plasma is reached after 2 hours and is 0.97 Ојg / ml. The half-absorption period is 0.8 hours, the half-distribution period is 4.6 hours. Connection with blood plasma proteins - 99%. With a simultaneous admission with food, dose adjustment is not required.
Terbinafine rapidly penetrates the skin and accumulates in the sebaceous glands. High concentrations are created in the hair follicles and hair, after a few weeks of application penetrates the nail plates. It accumulates in the stratum corneum (the concentration increases 10 times for 2 days after taking 250 mg, 70 times for 12 days) and nails (the diffusion rate exceeds the growth rate of the nail) in concentrations providing fungicidal action.
Terbinafine is metabolized in the liver with the formation of inactive metabolites. T 1/2 is 16-18 hours. T 1/2 of the terminal phase is 200-400 hours. It is excreted mainly by the kidneys (70%) in the form of metabolites, and also through the skin. There is no evidence of cumulation of the drug in the body. Excreted in breast milk. There were no changes in the equilibrium concentration of terbinafine in plasma depending on the age, but patients with impaired renal or hepatic function may have a slowed-off rate, which leads to higher concentrations of terbinafine in the blood.
- fungal diseases of the skin and nails (onychomycosis), caused by Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violacium), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum;
- mycoses of the scalp (trichophytosis, microsporia);
- severe, common dermatomycosis of the smooth skin of the trunk and extremities, requiring systemic treatment;
Candidiasis of the skin and mucous membranes.
Inside, after eating. Usual dose: 250 mg once a day.
Children older than 3 years:
With a body weight of 20 to 40 kg , 125 mg once a day.
With a body weight of more than 40 kg , 250 mg once a day.
The duration of the course of treatment and the dosage regimen are set individually and depend on the localization of the process and the severity of the disease.
Onychomycosis: the duration of therapy is an average of 6-12 weeks. If the fingers and toes of the hands and feet (with the exception of the thumb of the foot) are affected, or when the patient is young, the duration of treatment may be less than 12 weeks. If infection of the thumb of the foot is usually enough 3-month course of treatment.
Some patients who have a reduced rate of nail growth may need a longer period of treatment.
Fungal skin infections: 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 - 2-4 weeks; with mycoses caused by fungi of the genus Candida - 2-4 weeks; with mycosis of the scalp caused by fungi of the genus Microsporum - more than 4 weeks.
The duration of treatment of mycosis of the scalp is about 4 weeks, with infection of Microsporum canis - may be more prolonged.
Older patients prescribe the drug in the same doses as adults.
Patients with hepatic or renal insufficiency - 125 mg once a day.
Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less than 1/10000, including individual cases.
On the part of the digestive system: very often - a feeling of overflow of the stomach, a decrease in appetite, dyspepsia, nausea, abdominal pain, diarrhea; rarely - a violation of liver function; very rarely - liver failure, up to a lethal outcome.
On the part of the organs of hematopoiesis: very rarely - neutropenia, agranulocytosis, thrombocytopenia, pancytopenia.
Allergic reactions: very rarely anaphylactoid reactions (including angioedema).
From the nervous system: often - headache; infrequently - a violation of taste, including agevziyu.
From the skin: very often - skin reactions (including rash, urticaria); very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, psoriasis-like rash, exacerbation of existing psoriasis, alopecia.
From the musculoskeletal system: very often - arthralgia, myalgia.
Other: very rarely - fatigue; cutaneous lupus erythematosus, SLE or their exacerbation.
- chronic or active liver disease;
- chronic renal failure (CC less than 50 ml / min);
- Children's age (up to 3 years) and with a body weight of up to 20 kg (for this dosage form);
- lactation period;
- Lactase deficiency, lactose intolerance, glucosogalactose malabsorption;
- Hypersensitivity to terbinafine or other components of the drug.
Care should be taken when:
- Renal insufficiency (with SC more than 50 ml / min);
- oppression of bone marrow hematopoiesis;
- metabolic diseases;
- occlusive diseases of the vessels of the extremities;
- cutaneous lupus erythematosus or systemic lupus erythematosus.
PREGNANCY AND LACTATION
Since studies on the safety of terbinafine in pregnant women have not been conducted, the drug should not be prescribed during pregnancy.
Terbinafine is excreted in breast milk, therefore its purpose is contraindicated in the period of breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in chronic renal failure (CC less than 50 ml / min).
Use with caution in renal failure (with QC greater than 50 mL / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in chronic or active liver disease.
Use with caution in case of liver failure.
APPLICATION FOR CHILDREN
Contraindicated in children under 3 years old and weighing up to 20 kg.
APPLICATION IN ELDERLY PATIENTS
Older patients prescribe the drug in the same doses as adults.
Irregular application or early termination of treatment increases the risk of relapse.
The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the condition of the nails with onychomycosis at the beginning of the course of treatment.
If after 2 weeks of treatment for a skin infection there is no improvement, it is necessary to repeatedly identify 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, a clinical response, confirmed laboratory, 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 of brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.
In the presence of liver disease, terbinafine clearance can be reduced. During treatment, it is necessary to monitor the activity of "hepatic" 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, decreased appetite, excessive abdominal pain, jaundice, darkening of the urine, or discolored stools), the drug should be discontinued.
The administration of terbinafine to psoriasis patients requires caution. In very rare cases, terbinafine can provoke an exacerbation of psoriasis.
When treating terbinafine, general hygiene rules should be followed to prevent the possibility of re-infection through linen and shoes. In the process of treatment (after 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
There is no data on the effect of terbinafine on the ability to drive vehicles and mechanisms.
Symptoms: headache, dizziness, nausea, vomiting, pain in the epigastric region, frequent urination, rash.
Treatment: measures to remove the drug (gastric lavage, reception of activated charcoal); if necessary, symptomatic maintenance therapy.
It inhibits the isoenzyme CYP2D6 and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (eg, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), monoamine oxidase B inhibitors (eg selegiline ) and antipsychotic (for example, chlorpromazine, haloperidol) funds.
Medications-inducers of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate metabolism and excretion of terbinafine from the body. Drugs - inhibitors of cytochrome P450 isoenzymes (eg, cimetidine) can slow down metabolism and remove terbinafine from the body. With the simultaneous use of these preparations, a dose adjustment of terbinafine may be required.
Possible violation of the menstrual cycle with the simultaneous administration of terbinafine and oral contraceptives.
Terbinafine reduces caffeine clearance by 21% and prolongs its half-life by 31%. Does not affect the clearance of phenazone, digoxin, warfarin.
When combined with ethanol or drugs that have a hepatotoxic effect, there is a risk of developing drug-induced liver damage.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
In a dry, protected from light place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 3 years.