Termicon^® (Tablets, Cream, Spray) Instructions for Use

ATC Code

D01BA02 (Terbinafine)

Active Substance

Terbinafine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antifungal drug

Pharmacotherapeutic Group

Antifungal agents used in dermatology; systemic antifungal agents

Pharmacological Action

An antifungal drug, an allylamine. It has a broad spectrum of antifungal action.

Active against dermatophytes: Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum, Microsporum canis, Epidermophyton floccosum. In low concentrations, it has a fungicidal effect on dermatophytes, molds (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 fungal cell membrane, ergosterol, by inhibiting the enzyme squalene epoxidase. This leads to a deficiency of ergosterol and 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 fungal cell membrane.

When taken orally, it is not effective in the treatment of pityriasis versicolor caused by Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics

Absorption

After oral administration, the drug is well absorbed from the gastrointestinal tract. Half of the administered dose is absorbed within 0.8 hours.

After a single dose of 250 mg, C_max of terbinafine in blood plasma is reached in 1-2 hours and is 0.97 µg/ml. Bioavailability is 80%. Food intake does not affect the bioavailability of terbinafine.

Distribution

Binding to plasma proteins is 99%.

Half of the administered dose is distributed in the body 4.6 hours after administration. The drug quickly penetrates into the dermal layer of the skin and nail plates. It penetrates into the secretion of the sebaceous glands, accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue. It does not accumulate in the body.

Terbinafine is excreted in breast milk.

Metabolism

It is biotransformed in the liver to form inactive metabolites.

Excretion

About 80% of the administered dose is excreted in the urine as metabolites, the rest is excreted in the feces (22%).

Pharmacokinetics in special clinical cases

The age of patients does not affect the pharmacokinetics of terbinafine, but the elimination of the drug may be reduced in cases of 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);
• Mycoses of the skin and nails caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum, Microsporum canis, Microsporum gypseum and Epidermophyton floccosum;
• Onychomycosis;
• Severe widespread dermatomycosis of the smooth skin of the trunk and extremities requiring systemic treatment;
• Candidiasis of the skin and mucous membranes.

ICD codes

Dosage Regimen

Spray

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.

For external use, the drug is prescribed to adults 1-2 times/day, depending on the indications. Before applying the drug, it is necessary to clean and dry the affected areas. The drug is sprayed onto the affected skin and adjacent areas in an amount sufficient to moisten them, and, in addition, is applied to the adjacent areas of intact skin.

The dosage regimen for elderly patients is the same as for younger adults.

Cream

Termicon^® is prescribed externally for adults and children over 12 years of age.

Before applying the cream, it is necessary to clean and dry the affected areas. The cream is applied 1-2 times/day in a thin layer to the affected skin and adjacent areas, rubbing gently.

For infections accompanied by intertrigo (under the breasts, in the interdigital spaces, between the buttocks, in the groin area), the areas where the cream is applied can be covered with gauze, especially at night.

The average duration of treatment for dermatomycosis of the trunk, shins, feet is 1 time/day for 1 week; for skin candidiasis – 1-2 times/day for 1-2 weeks; for pityriasis versicolor – 1-2 times/day for 2 weeks.

A decrease in the severity of clinical manifestations is usually noted in the first days of treatment. In case of irregular treatment or premature discontinuation, there is a risk of recurrence of the infection. If no signs of improvement are noted after 1-2 weeks of treatment, the diagnosis should be verified.

The dosage regimen of the drug for elderly patients is the same as for patients of other age groups.

Tablets

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.

Orally, adults are prescribed the drug at a dose of 250 mg 1 time/day (after meals).

For onychomycosis, the duration of treatment is about 6-12 weeks. For 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. For an infection of the big toe, a course of treatment of 3 months is usually sufficient. In rare cases, with a slow rate of nail growth, longer treatment may be required – up to 6 or more months.

For dermatomycosis of the feet (interdigital, plantar or sock-type) the duration of treatment is from 2 to 6 weeks; for dermatomycosis of the shins – from 2 to 4 weeks; for dermatomycosis of the trunk – 4 weeks; for candidiasis of the skin and mucous membranes from 2 to 4 weeks.

For mycosis of the scalp caused by Microsporum canis, the recommended duration of treatment is more than 4 weeks.

Children weighing from 20 to 40 kg are prescribed the drug at a dose of 125 mg (1/2 tab.) 1 time/day, with a body weight over 40 kg – 250 mg 1 time/day. The duration of treatment for mycoses of the scalp is about 4 weeks. In cases where the causative agent is Microsporum canis, treatment may be longer.

Elderly patients are prescribed the drug in the same doses as adults.

In case of severe renal failure (creatinine clearance <50 ml/min or serum creatinine level >300 µmol/l), in case of impaired renal function, the dose of the drug should be reduced by half, for adults – 125 mg 1 time/day.

Adverse Reactions

From the digestive system dyspepsia, decreased appetite, nausea, diarrhea, feeling of stomach fullness, abdominal pain, taste disorders, including their loss (recovery occurs within a few weeks after discontinuation of treatment); very rarely – hepatobiliary disorders (cholestatic jaundice).

From the musculoskeletal system arthralgia, myalgia.

From the hematopoietic 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;
• Period of breastfeeding;
• Children under 3 years of age and children weighing less than 20 kg;
• Hypersensitivity to the components of the drug.

With caution, the drug should be used orally in case of renal and/or hepatic insufficiency, alcoholism, bone marrow hematopoiesis depression, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities.

Use in Pregnancy and Lactation

Experience with the use of the drug Termicon^® during pregnancy is limited, so its prescription during pregnancy is contraindicated.

Terbinafine is excreted in breast milk, so if it is necessary to prescribe the drug during lactation, the issue of stopping breastfeeding should be decided.

In experimental studies, no teratogenic effect of terbinafine was detected. To date, no malformations have been reported with the use of terbinafine.

Use in Hepatic Impairment

With caution, the drug should be prescribed orally and externally in case of hepatic insufficiency.

Use in Renal Impairment

Patients with renal insufficiency are prescribed 125 mg 1 time/day orally.

With caution, the drug should be prescribed externally in case of renal insufficiency

Pediatric Use

Contraindicated: children under 3 years of age and children weighing less than 20 kg.

Geriatric Use

Elderly patients are prescribed the drug in the same doses as adults.

Special Precautions

It should be taken into account that irregular use or premature termination of treatment increases the risk of relapse.

The duration of therapy may be determined by the presence of concomitant diseases, the condition of the nails at the beginning of the course of treatment.

If no improvement is noted after 2 weeks of treatment with Termicon^®, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.

Systemic use for onychomycosis is justified only in case of total damage to most nails, the presence of severe subungual hyperkeratosis, and ineffectiveness of previous local therapy. In the treatment of onychomycosis, a clinical response is usually observed several months after mycological cure and the end of the course of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment 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, cholestasis and hepatitis develop after 3 months of treatment. If symptoms of liver dysfunction are detected (weakness, persistent nausea, lack of appetite, abdominal pain, jaundice, dark urine or colorless feces), it is necessary to discontinue the drug.

The drug should be prescribed with particular caution 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 observed to prevent the possibility of re-infection through linen and shoes. During (after 2 weeks) and at the end of treatment, antifungal treatment of shoes, socks and stockings should be carried out.

If allergic reactions develop, the drug should be discontinued.

Use in pediatrics

Termicon^® is contraindicated for use in children under 3 years of age and children weighing less than 20 kg.

Effect on ability to drive vehicles and mechanisms

Terbinafine does not affect the ability to drive vehicles and perform work requiring increased concentration and speed of psychomotor reactions.

Overdose

Symptoms nausea, vomiting, pain in the lower abdomen and epigastric region, dizziness.

Treatment gastric lavage followed by the administration of activated charcoal and/or symptomatic therapy.

Drug Interactions

Terbinafine inhibits the CYP2D6 isoenzyme and slows down the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (e.g., desipramine, fluvoxamine), beta₁-blockers (metoprolol, propranolol), antiarrhythmic drugs (flecainide, propafenone), MAO type B inhibitors (e.g., selegiline) and antipsychotic drugs (e.g., chlorpromazine, haloperidol).

Inducers of cytochrome P450 isoenzymes (e.g., rifampicin) may accelerate the elimination of terbinafine from the body, inhibitors of cytochrome P450 isoenzymes (e.g., cimetidine) may slow it down. When used concomitantly with such drugs, dose adjustment of terbinafine may be required.

With the simultaneous use of terbinafine and oral contraceptives, menstrual cycle disturbances are possible.

Terbinafine reduces the clearance of caffeine 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, when used concomitantly with Termicon^®, increase the risk of hepatotoxicity.

Storage Conditions

List B. The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.