Termicon (Terbinafine) 250 mg

Instructions for Termicon

Composition Termicon:

Terbinafine hydrochloride 281.25 mg, which corresponds to the content of Terbinafine 250 mg Excipients: sodium starch glycolate, microcrystalline cellulose, lactose, hypromellose (hydroxypropyl methyl cellulose), magnesium stearate, colloidal silicon dioxide (aerosil)

Pharmacodynamics Termicon:

Antifungal drug Termicon, allylamine. It has a wide range of antifungal effects. 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 drug has a fungicidal or fungistatic effect. Termicon disrupts the early stage of biosynthesis of the main component of the cell membrane of the ergosterol fungus by inhibiting the squalene epoxidase enzyme. This leads to a deficiency of ergosterol and to intracellular accumulation of squalene, which causes the 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 taken orally Termikon it is not effective in treating multi-colored lichen caused by Pityrosporum orbiculare (Malassezia furfur).

Indications Termikon:

• mycoses of the scalp (trichophytosis, microsporia)
• skin and nail mycoses due to Trichophyton rubrum
• Trichophyton mentagrophytes
• Trichophyton tonsurans
• Trichophyton verrucosum
• Trichophyton violaceum
• Microsporum canis
• Microsporum gypseum and Epidermophyton floccosum
• onychomycosis
• severe common dermatomycosis of smooth skin of the trunk and limbs, requiring systemic
• candidiasis of the skin and mucous membranes

Pharmacokinetics Termikon:

Absorption After oral administration Termicon, 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 Cmax of Terbinafine in plasma, it is reached after 1-2 hours and amounts to 0.97 μg / ml. Bioavailability is 80%. Eating does not affect the bioavailability of Terbinafine. Distribution Binding to blood plasma proteins - 99%. 4.6 hours after ingestion, half the dose taken is distributed in the body. The drug quickly penetrates the dermal layer of the skin and nail plates.

It penetrates the secret of the sebaceous glands, accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue. Does not cumulate in the body.

Terbinafine is excreted in breast milk. Metabolism Biotransformed in the liver with the formation of inactive metabolites. Excretion In the form of metabolites with urine, about 80% of the dose taken is excreted, the rest with feces (22%). Pharmacokinetics in special clinical cases The age of patients does not affect the pharmacokinetics of Terbinafine, however, excretion of the drug may decrease with damage to the kidneys or liver, leading to high concentrations of Terbinafine in the blood. T1 / 2 is 16-18 hours. T1 / 2 in the terminal phase is 200-400 hours.

Side effects Termikon:

• From the digestive system
• dyspepsia, loss of appetite
• nausea
• diarrhea, a feeling of fullness of the stomach
• abdominal pain
• taste disturbances
• including their loss (recovery occurs within a few weeks after stopping therapy)
• very rarely - hepatobiliary disorders (cholestatic jaundice)
• From the musculoskeletal system: arthralgia, myalgia. From the hemopoietic system: agranulocytosis, thrombocytopenia, neutropenia
• Allergic reactions: urticaria, rash; very rarely - toxic epidermal necrolysis (Lyell syndrome), anaphylactoid reactions, malignant exudative erythema (Stevens-Johnson syndrome)

Special conditions Termikon:

It should be borne in mind that irregular use or early termination of therapy increases the risk of relapse. The duration of therapy Termicon can be determined by the presence of concomitant diseases, the condition of the nails at the beginning of the course of therapy. If after 2 weeks of treatment with Termicon there is no improvement, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug Termikon. Systemic use in onychomycosis is justified only in the case of a total lesion of most nails, the presence of severe subungual hyperkeratosis, and the ineffectiveness of previous local therapy. In the therapy of onychomycosis, a clinical response is usually observed several months after mycological cure and cessation of therapy, due to the rate of growth of a healthy nail. Removal of nail plates in of onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks is not required. During treatment, the activity of hepatic transaminases in the blood serum should be monitored. In rare cases, after 3 months of treatment, cholestasis and hepatitis develop. If symptoms of liver dysfunction are identified (weakness, persistent nausea, lack of appetite, abdominal pain, jaundice, dark urine or colorless stool), the drug should be discontinued. With extreme caution, the drug should be prescribed to patients with psoriasis, since in very rare cases terbinafine can provoke an exacerbation of psoriasis. During treatment with the drug, general hygiene rules should be followed to prevent the possibility of reinfection through 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.

With the development of allergic reactions, the drug Termikon should be discontinued. Use in pediatrics Thermicon® is contraindicated in children under 3 years of age and children weighing up to 20 kg. The effect on the ability to drive vehicles and control 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.

Drug Interactions Termikon:

Terbinafine inhibits the CYP2D6 isoenzyme and slows the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake blockers (e.g. desipramine, fluvoxamine), beta1-blockers (metoprolol, propranolol), antiarrhythmic drugs (such as flecainide, propaphenone, inhibitor, selegiline) and antipsychotic drugs (e.g., chlorpromazine, haloperidol). Inducers of isoenzymes of the cytochrome P450 system (for example, rifampicin) can accelerate the excretion of Terbinafine from the body, inhibitors of isoenzymes of the cytochrome P450 system (for example, cimetidine) can slow it down.
With simultaneous use with such drugs, dose adjustment of tebinafine may be required. With the simultaneous administration of Terbinafine and oral contraceptives, a menstrual cycle is possible. Terbinafine reduces the clearance of caffeine by 20% and increases its T1 / 2 by 31%. Terbinafine does not affect the clearance of antipyrine, digoxin, warfarin.

Dosage Termikon:

The duration of the course of treatment and the dosage regimen is set 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 / (after eating). With onychomycosis, the duration of treatment is about 6-12 weeks. With onychomycosis of the hands and feet (with the exception of the big toe), or in young patients, the duration of therapymay be less than 12 weeks. With a big toe infection, a treatment course of 3 months is usually sufficient.

In rare cases, with a slowed nail growth rate, longer treatment may be required - up to 6 months or more. For children with a body weight of 20 to 40 kg, the drug is prescribed in a dose of 125 mg (1/2 tablet) 1 time /, with a body weight of more than 40 mg - 250 mg 1 time /
The duration therapy for mycosis Termikon of the scalp is about 4 weeks. In cases where the causative agent is Microsporum canis, treatment may be longer.
For elderly patients, the drug is prescribed in the same doses as adults. In severe renal failure (CC <50 ml / min or serum creatinine content> 300 μmol / L), in case of impaired renal function, the dose should be reduced by 2 times, for adults - 125 mg 1 time /

Overdose Termicon:

• nausea
• vomiting
• pain in the lower abdomen and epigastric region
• dizziness