Composition, form of production and packaging
Tablets are white or white with a yellowish tint of color, flat-cylindrical, with a facet and a risk.
1 tab.
terbinafine hydrochloride 281.25 mg,
which corresponds to the content of terbinafine 250 mg
[PRING] sodium starch glycolate, microcrystalline cellulose, lactose, hypromellose (hydroxypropylmethylcellulose), magnesium stearate, silicon dioxide colloid (aerosil).
7 pcs. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antifungal drug, allylamine. Has a wide range of antifungal action.
It is active against dermatophytes: Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum, Microsporum canis, Epidermophyton floccosum. At low concentrations, it has a fungicidal effect on dermatophytes, mold fungi (including Aspergillus, Cladosporium, Scopulariopsis brevicaulis) and some dimorphic fungi. On yeast fungi of the genus Candida (mainly Candida albicans) and their mycelial forms, depending on the species, the preparation has a fungicidal or fungistatic effect.
Thermicone В® disrupts the early stage of biosynthesis of the main component of the cellular membrane of the ergosterol fungus by inhibiting the enzyme squalene epoxidase. This leads to a deficit 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 located on the cell membrane of the fungus.
When ingestion is not effective in the treatment of varicolored lichen, caused by Pityrosporum orbiculare (Malassezia furfur).
PHARMACOKINETICS
Suction
After ingestion, the drug is well absorbed from the digestive tract. After 0.8 h, half of the dose taken is absorbed.
After a single dose of 250 mg C max terbinafine in blood plasma is achieved after 1-2 hours and is 0.97 Ојg / ml. Bioavailability is 80%. Eating does not affect the bioavailability of terbinafine.
Distribution
Binding to blood plasma proteins - 99%.
After 4.6 hours after administration, half of the dose taken is distributed in the body. The drug quickly penetrates the dermal layer of the skin and nail plates. Penetrates into the secretion of sebaceous glands, accumulates in high concentrations in the hair follicles, in hair, skin and subcutaneous tissue. Do not cum in the body.
Terbinafine is excreted in breast milk.
Metabolism
Biotransformiruetsya in the liver with the formation of inactive metabolites.
Excretion
In the form of metabolites with urine, about 80% of the dose taken, the rest - with feces (22%).
Pharmacokinetics in special clinical cases
The age of the patients does not affect the pharmacokinetics of terbinafine, however, excretion of the drug may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood.
T 1/2 is 16-18 hours. T 1/2 in the terminal phase is 200-400 hours.
INDICATIONS
- mycoses of the scalp (trichophytosis, microsporia);
- skin and nail mycoses caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum, Microsporum canis, Microsporum gypseum and Epidermophyton 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 determined individually and depends on the localization of the process and the severity of the disease.
Inside adults, the drug is prescribed 250 mg 1 time / day (after meals).
With onychomycosis, the duration of treatment is about 6-12 weeks. With onychomycosis of the hands and feet (except for the big toe), or in young patients, the duration of treatment may be less than 12 weeks. When infection of the thumb of the foot is usually enough treatment course at 3 months. In rare cases, slower growth of nails may require longer treatment - up to 6 months or more.
With dermatomycosis of the foot (interdigital, plantar or as a socks), the duration of treatment is 2 to 6 weeks; with shin dermatomycosis - from 2 to 4 weeks; with torso dermatomycosis - 4 weeks; with candidiasis of the skin and mucous membranes from 2 to 4 weeks.
With mycosis of the scalp caused by Microsporum canis, the recommended duration of treatment is more than 4 weeks.
Children with a body weight of 20 to 40 kg of the drug prescribed in a dose of 125 mg (1/2 tab.) 1 time / day, with a body weight of more than 40 mg - 250 mg 1 time / day. The duration of mycosis treatment of the scalp is about 4 weeks. In cases where the pathogen is Microsporum canis, the treatment may be longer.
Older patients are prescribed the drug in the same doses as adults.
For renal insufficiency of severe degree (CC <50 ml / min or serum creatinine content> 300 Ојmol / L), in case of renal dysfunction, the dose of the drug should be reduced 2 times, for adults 125 mg 1 time / day.
SIDE EFFECT
On the part of the digestive system: dyspepsia, decreased appetite, nausea, diarrhea, a feeling of stomach overflow, abdominal pain, taste disorders, including their loss (recovery occurs within a few weeks after cessation of treatment); very rarely - hepatobiliary disorders (cholestatic jaundice).
From the musculoskeletal system: arthralgia, myalgia.
On the part of the hematopoiesis system: agranulocytosis, thrombocytopenia, neutropenia.
Allergic reactions: urticaria, rash; very rarely - toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions, malignant exudative erythema (Stevens-Johnson syndrome).
CONTRAINDICATIONS
- Pregnancy;
- the period of breastfeeding;
- Children under 3 years old and children weighing up to 20 kg;
- Hypersensitivity to the components of the drug.
With caution should be taken internally with renal and / or hepatic insufficiency, alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities.
PREGNANCY AND LACTATION
Experience in the use of the drug Termikon В® in pregnancy is limited, so its use in pregnancy is contraindicated.
Terbinafine is excreted in breast milk, therefore, if it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be resolved.
In experimental studies teratogenicity of terbinafine was not revealed. To date, no developmental deficiencies have been reported with terbinafine.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal insufficiency inside are prescribed 125 mg once a day.
With caution should prescribe the drug externally with renal failure
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution should be given to the drug inside and outwardly with hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated: children under 3 years old and children weighing up to 20 kg.
APPLICATION IN ELDERLY PATIENTS
Older patients are prescribed the drug in the same doses as adults.
SPECIAL INSTRUCTIONS
It should be borne in mind that irregular use or early termination of treatment increases the risk of relapse.
The duration of therapy can be determined by the presence of concomitant diseases, the state of the nails at the beginning of the course of treatment.
If after 2 weeks of treatment with Termicon 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 is usually observed a few months after mycological cure and discontinuation 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.
During treatment should monitor the activity of hepatic transaminases in the blood serum. In rare cases, after 3 months of treatment, cholestasis and hepatitis develop. If symptoms of liver dysfunction (weakness, persistent nausea, lack of appetite, abdominal pain, jaundice, dark urine or colorless feces) are detected, it is necessary to cancel the drug.
With extreme caution, the drug should be given to patients with psoriasis, as in very rare cases terbinafine can provoke an exacerbation of psoriasis.
When treating the drug, you should follow the general rules of hygiene to prevent the possibility of re-infection through the underwear and shoes. In the process (after 2 weeks) and at the end of treatment it is necessary to produce antifungal treatment of shoes, socks and stockings.
When developing allergic reactions, the drug should be discarded.
Use in Pediatrics
Thermicone В® is contraindicated in children under 3 years of age and in children weighing up to 20 kg .
Impact on the ability to drive vehicles and manage mechanisms
Terbinafine does not affect the ability to drive vehicles and perform work that requires an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: nausea, vomiting, pain in the lower abdomen and epigastric region, dizziness.
Treatment: gastric lavage followed by prescription of activated charcoal and / or symptomatic therapy.
DRUG INTERACTION
Terbinafine inhibits the CYP2D6 isoenzyme and slows the metabolism of such drugs as tricyclic antidepressants and selective serotonin reuptake inhibitors (eg, desipramine, fluvoxamine), beta 1 -adrenoceptor blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), MAO inhibitors type B (for example , selegiline) and antipsychotic drugs (eg, chlorpromazine, haloperidol).
Inductors of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the excretion of terbinafine from the body, inhibitors of cytochrome P450 isoenzymes (eg, cimetidine) can slow it down. With simultaneous use with such drugs, a dose adjustment for tebinafine may be required.
With simultaneous administration of terbinafine and oral contraceptives, a menstrual cycle disorder is possible.
Terbinafine reduces caffeine clearance by 20% and increases its T 1/2 by 31%.
Terbinafine does not affect the clearance of antipyrine, digoxin, warfarin.
Ethanol and other hepatotoxic drugs with simultaneous application with Termicin increase the risk of hepatotoxicity.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, protected from light at a temperature of no higher than 25 В° C. Shelf life - 3 years.
