Expiration date: 01/2025
Release form and composition:
Tablets white or white with a yellowish sheen color, ploskotsylindriceskie, chamfered and mark.
1 tablet contains terbinafine hydrochloride 281.25 mg
EMCO corresponds to the content of terbinafine 250 mg
Excipients: sodium starch of glycolate, cellulose microcrystalline, lactose, hypromellose (hydroxypropyl methylcellulose), magnesium stearate, silicon dioxide colloidal (Aerosil).
Pharmacological action:
Antifungal agent, allilamin. It has a broad spectrum of antifungal activity.
Active against dermatophytes: Trichphytn rubrum, Trichphytn mentagrphytes, Trichphytn tnsurans, Trichphytn verrucsum, Trichphytn viaceum, Micrsprum canis, Epidermphytn fccsum. In low concentrations has a fungicidal effect on dermatophytes, mould fungi (including Aspergius, Cadsprium, Scpuaripsis brevicauis) and certain dimorphic fungi. In yeast fungi of the genus Candida (mainly Candida abicans) and filamentous forms, depending on the species, the drug has fungicidal or fungistatic.
Termicon® violates the early stage of the biosynthesis of the main components of the cell membrane of the fungus ergosterol by inhibiting enzyme squalene epoxidase. This leads to a deficiency of ergosterol and to an intracellular accumulation of squalene, which causes cell death of the fungus. The action of terbinafine by inhibiting the enzyme squalene epoxidase, located on the cell membrane of the fungus.
If ingestion is not effective in the treatment of multi-colored lichen, called Pityrsprum rbicuare (Maasseia furfur).
Pharmacokinetics:
Suction
After ingestion the drug is well absorbed from the gastrointestinal tract. Through 0.8 h absorbed half the dose.
After receiving a single dose of 250 mg C max terbinafine in plasma achieved through 1-2 h and is 0.97 µg/ml. Bioavailability of 80%. Eating does not affect the bioavailability of terbinafine.
Distribution
Linking blood plasma proteins - 99%.
Through 4.6 hours after taking half the dose distributed in the body. The drug quickly penetrates the dermal layer of the skin and the nail plate. Penetrates the sebum, accumulates in high concentrations in hair follicles, hair, skin and subcutaneous tissue. Not koumouliruet in the body.
Terbinafine is excreted in breast milk.
Metabolism
Biotransformiroetsa in the liver to form inactive metabolites.
Excretion
In the form of metabolites with urine output of about 80% of the dose, the remainder from faeces (22%).
Pharmacokinetics in special clinical cases
The age of patients did not affect the farmakokinetiku terbinafine, however, the excretion of the drug may be reduced in patients with lesions of the liver or kidneys, resulting in high concentrations of terbinafine in the blood.
T1/2 is 16-18 h. T1/2 the terminal phase - 200-400 h
Indications:
— mycosis of the scalp (trichophytosis, microsporia)
— mycoses of the skin and nails caused by Trichphytn rubrum, Trichphytn mentagrphytes, Trichphytn tnsurans, Trichphytn verrucsum, Trichphytn viaceum, Micrsprum canis, gypseum and Micrsprum Epidermphytn fccsum
— onychomycosis
— heavy common dermatomycosis smooth skin of the trunk and extremities, requiring systemic treatment
— candidiasis of skin and mucous membranes.
Dosing regimen:
The duration of treatment and dosage regimen is determined individually and depends on the location and severity of the disease.
Inside adults the preparation appoint 250 mg 1 times/day (after meals).
Onychomycosis the duration of treatment is about 6-12 weeks. In onychomycosis of the hands and feet (except the big toe), or in young patients the duration of treatment may be less than 12 weeks. For infections of the big toe is usually sufficient treatment in 3 months. In rare cases, the slow rate of nail growth may require a longer treatment - up to 6 months or more.
When ringworm of the feet (interdigital, plantar or the type of socks) the duration of treatment is from 2 to 6 weeks for the ringworm of calves - 2 to 4 weeks for the ringworm of the body - 4 weeks candidiasis of the skin and mucous membranes 2 to 4 weeks.
When fungal infection of the scalp caused by Micrsprum canis recommended duration of treatment - more than 4 weeks.
Children weighing 20 to 40 kg drug appointed dose of 125 mg (1/2 tab.) 1 time/day, with weighing more than 40 mg - 250 mg 1 time/day. Duration of treatment fungal infections of the scalp is about 4 weeks. In cases where the causative agent is Micrsprum canis, treatment may be longer.
Elderly patients the drug is prescribed in the same doses, as adults.
In renal failure, severe (??t50 ml/min or content of serum creatinine gt300 µmol/l), when violation of the kidney dose should be reduced in 2 times, adult - 125 mg 1 times/day.
Side effects:
From the digestive system: dyspepsia, loss of appetite, nausea, diarrhea, feeling of fullness of stomach, pain in the abdomen, breach of taste sensations, including their loss (recovery occurs within several weeks after discontinuation of treatment) very rare hepatobiliary disorders (cholestatic jaundice).
From the side of musculoskeletal system: arthralgia, myalgia.
With the hematopoietic system: agranulocytosis, thrombocytopenia, neutropenia.
Allergic reactions: urticaria, rash very rare - toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions, malignant exudative erythema (Stevens-Johnson syndrome).
Contraindications:
— pregnancy
— breastfeeding
— children up to age 3 years and children weighing up to 20 kg
— hypersensitivity to the drug.
With caution the drug should be used orally for kidney and/or liver failure, alcoholism, oppression kostnomozgovy blood, tumors, metabolic diseases, occlusal diseases of blood vessels of the extremities.
Pregnancy and lactation:
Experience with the drug Termicon® when pregnancy is limited, therefore, his appointment during pregnancy is contraindicated.
Terbinafine is excreted in breast milk, so if necessary, the appointment of the drug during lactation should decide the issue of termination of breastfeeding.
In experimental studies teratogenic effects of terbinafine have not been identified. So far not reported any defects with the use of terbinafine.
Special instructions:
Note that the irregular use or premature termination of treatment increases the risk of relapse.
The duration of treatment may be determined by the presence of comorbidities, the condition of the nails at the beginning of treatment.
If after 2 weeks of treatment with Termicon not marked improve condition, you have to re-determine the causative agent and its sensitivity to the drug.
Systemic application in onychomycosis justified only in the case of total destruction of most of the nails, presence of a pronounced subungual hyperkeratosis, the ineffectiveness of the previous local therapy. In the treatment of onychomycosis clinical response is usually seen after some months after mycological cure and cessation of treatment, due to the speed of regrowth of healthy nail. Removal of nail plates in treatment of onychomycosis of hands for 3 weeks and stop for onychomycosis 6 weeks is required.
During treatment should monitor the activity of hepatic transaminases in serum. In rare cases, through 3 months of treatment developed cholestasis and hepatitis. The detection of symptoms of liver dysfunction (weakness, persistent nausea, lack of appetite, abdominal pain, jaundice, dark urine or colourless stool), you should stop the drug.
With caution should appoint drug patients with psoriasis, as very rare cases, terbinafine may cause exacerbation of psoriasis.
When drug treatment should follow the General rules of hygiene to prevent reinfection through underwear and shoes. In the process (through 2 ned.) and at the end of the treatment, it is necessary to produce the antifungal treatment of footwear, socks and stockings.
In developing allergic reactions the drug should be discontinued.
Use in Pediatrics
Termicon® is contraindicated for use in children under 3 years and children weighing up to 20 kg.
Effects on ability to drive vehicles and management mechanisms
Terbinafine does not affect the ability to drive vehicles and perform work requiring increased concentration of attention and speed of psychomotor reactions.
Overdose:
Symptoms: nausea, vomiting, pain in the lower abdomen and epigastric area, dizziness.
Treatment: gastric lavage with subsequent appointment activated charcoal and/or symptomatic therapy.
Drug interactions:
Terbinafine inhibits the CYP2D6 isoenzyme and slows down the metabolism of such drugs as tricyclic antidepressants and selective blockers of serotonin reuptake (e.g., desipramine, fluvoxamine), beta1-blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenon), inhibitors of MAO type b (e.g. selegiline) and antipsychotic drugs (e.g. chlorpromazine, haloperidol).
Inducers of isoenzymes of cytochrome P450 (e.g., rifampicin) can accelerate the excretion of terbinafine from the body, inhibitors of isoenzymes of cytochrome P450 (eg, cimetidine) can slow it down. While the use of such drugs may require dose adjustment terbinafine.
While taking terbinafine and oral contraceptives may be a violation of the menstrual cycle.
Terbinafine decreases the clearance of caffeine by 20% and increases T1/2 by 31%.
Terbinafine does not affect the clearance of antipyrine, digoxin, warfarin.
Ethanol and other hepatotoxic medications with simultaneous use with Termicon increase the risk of hepatotoxicity.
Terms and conditions of storage:
List B. the Drug should be stored out of the reach of children, protected from light place at temperature not exceeding 25°C. shelf Life - 3 years.
