Termicon, pills 250mg, 28pcs

Composition

Active ingredient:

• Terbinafine hydrochloride – 281.25 mg (in terms of terbinafine-250 mg)

Auxiliary substances:

• croscarmellose sodium-48 mg,
• microcrystalline cellulose-35.2 mg,
• lactose monohydrate-23.95 mg,
• hypromellose (hydroxypropylmethylcellulose) – 6.2 mg,
• magnesium stearate for the pharmaceutical industry-4 mg,
• colloidal silicon dioxide (aerosil) – 1.4 mg

Pharmacological action

Pharmacotherapy group antifungal agent

ATX code D01 BA02

Pharmacological properties

Pharmacodynamics : terbinafine belongs to the group of allylamines, has a wide spectrum of antifungal action. In low concentrations, it has a fungicidal effect on dermatophytes Trychophyton (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporumcanis, Epidermophytonfloccosum, mold fungi (for example. Aspergillus, Cladosporium, Scopulariopsisbrevicalius), yeast fungi, mainly Candidaalbicans, and some dimorphic fungi. It has a fungicidal or fungistatic effect on Candida fungi and its mycelial forms, depending on the type of fungus.

Terbinafine disrupts the early stage of biosynthesis of the main component of the fungal cell membrane, ergosterol, by inhibiting the squalene epoxidase enzyme.

When administered orally, it is not effective in the treatment of multicolored lichen caused by Malasseziafurfur.

Pharmacokinetics: when taken orally, it is well absorbed, after 0.8 hours half of the dose taken is absorbed; after 4.6 hours, half of the dose taken is distributed in the body. 1-2 hours after ingestion of a single 250 mg dose, the maximum concentration of the drug in blood plasma reaches 0.97 mcg / ml. Bioavailability is 80%. Food intake does not affect the bioavailability of terbinafine.

Terbinafine binds intensively to plasma proteins (99%), spreads rapidly in tissues, penetrates the dermal layer of the skin and nail plates. Penetrates the secret of the sebaceous glands and accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue.

The elimination half-life is 16-18 hours, the terminal phase half – life is 200-400 hours.

Biotransformed in the liver to inactive metabolites; 80% of the dose is excreted in the urine in the form of metabolites, the rest (22%) – with feces. It does not accumulate in the body. The age of patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood.

It is excreted together with breast milk.

Indications

Mycoses of the scalp (trichophytosis, microsporia).

Mycoses of the skin and nails caused by Trychophyton (T. rubrum, mentagrophytes, verrucosum, violaceum), Microsporum (M. canis, M. gypseum) and Epidermophytonfloccosum.

Onychomycosis.

Severe, widespread dermatomycosis of smooth skin of the trunk and limbs, requiring systemic treatment.

Candidiasis of the skin and mucous membranes.

Use during pregnancy and lactation

The data of experimental studies do not give grounds to assume the presence of adverse events in relation to fertility and toxic effects on the fetus. Since clinical experience with terbinafine in pregnant women is very limited, the drug should not be used during pregnancy, except in cases where the expected benefit of therapy exceeds the potential risk to the fetus.

Terbinafine is excreted in breast milk, so women taking terbinafine orally should not breastfeed.

Contraindications

Hypersensitivity to terbinafine or to any other component of the drug; children under 3 years of age and weighing up to 20 kg (for this dosage form).

Severe, chronic, or active liver disease.

It is not recommended to use terbinafine in patients with impaired renal function (creatinine clearance less than 50 ml / min or serum creatinine concentration more than 300 mmol / l), since the use of the drug in this category of patients has not been sufficiently studied.

With caution

Liver function disorders, inhibition of bone marrow hematopoiesis, cutaneous lupus erythematosus or systemic lupus erythematosus, psoriasis.

Side effects

Thermicon®is generally well tolerated. Side effects are usually mild to moderate and transient.

When assessing the frequency of drug side effects, the following gradations are used: “very common “(≥1/10), ” common “(≥1/100 <1/10), “infrequent” (≥1/1000 <1/100), ” rare “(≥1/10000 <1/1000), ” very rare” (

Disorders of the blood and lymphatic system: infrequently-anemia; very rarely-neutropenia, agranulocytosis, pancytopenia, thrombocytopenia.

Immune system disorders: very rarely-anaphylactoid reactions (including angioedema), cutaneous and systemic lupus erythematosus (or their exacerbation).

Mental disorders: often-depression; infrequently-anxiety.

Nervous system disorders: very often – headache; often dizziness, impaired taste sensations, up to their loss (usually recovery occurs within a few weeks after stopping treatment). In some cases, while taking terbinafine, exhaustion was noted. There are separate reports of cases of prolonged taste disturbances; infrequently-paresthesia, hypesthesia.

Visual disturbances: infrequently-visual disturbances.

Hearing disorders and labyrinth disorders: infrequently-tinnitus.

Liver and biliary tract disorders: rare – hepatobiliary dysfunction (mainly of a cholestatic nature), including hepatic insufficiency, including very rare cases of severe liver failure (some fatal or requiring liver transplantation; in most cases, when liver failure developed, patients had serious concomitant systemic diseases and the causal relationship of liver failure with terbinafine was questionable), hepatitis, jaundice, cholestasis, increased activity of the liver in patients with terbinafine. “liver” enzymes.

Disorders of the digestive system: very often – bloating, decreased appetite, dyspepsia, nausea, mild abdominal pain, diarrhea.

Skin and subcutaneous tissue disorders: very common – rash, urticaria; infrequently-photosensitivity reactions; very rare-Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, erythema multiforme, toxic skin rash, exfoliative dermatitis, bullous dermatitis, psoriasis-like skin rashes or exacerbations of psoriasis, alopecia.

Musculoskeletal and connective tissue disorders: very often arthralgia, myalgia.

General disorders: often-feeling tired; infrequently-fever.

Laboratory and instrumental data: infrequently – weight loss (secondary to impaired taste sensations).

Based on spontaneous reports received in the post-marketing period and literature data, the following adverse events were identified, the frequency of which cannot be determined due to the inaccurate number of patients.

Immune system disorders: anaphylactic reactions, serum sickness-like syndrome.

Visual disorders: visual impairment.

Skin and subcutaneous tissue disorders: drug-induced rash with eosinophilia and systemic symptoms (rash, swelling, fever, and enlarged lymph nodes).

Hearing disorders and labyrinth disorders: hearing loss, hearing impairment.

Vascular disorders: vasculitis.

Nervous system disorders: loss of sense of smell, including for a long period of time, decreased sense of smell.

Disorders of the digestive system: pancreatitis.

Musculoskeletal and connective tissue disorders: rhabdomyolysis.

Common disorders: flu-like syndrome.

Laboratory and instrumental data: increased serum creatine phosphokinase activity.

If you notice any side effects of the drug, tell your doctor.

Interaction

Inhibits the CYP2D6 isoenzyme and interferes with the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake blockers (eg. Desipramine, fluvoxamine), beta_-1blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), MAO-B inhibitors (selegiline) and antipsychotics (for example, chlorpromazine, haloperidol).

Drugs that are inducers of the CYP450 enzyme (e. g. rifampicin) can accelerate the elimination of terbinafine from the body.

Drugs that inhibit CYP450 (e. g. cimetidine) can slow down the metabolism and elimination of terbinafine from the body. Terbinafine dosage adjustment may be required when these drugs are used concomitantly.

Menstrual disorders may occur when taking terbinafine and oral contraceptives at the same time.

Reduces caffeine clearance by 21% and extends its half-life by 31%.

It does not affect the clearance of phenazone, digoxin, or warfarin.

When combined with ethanol or drugs that have a hepatotoxic effect, there is a risk of developing drug-induced liver damage.

How to take it, course of administration and dosage

The duration of the course of treatment and the dosage regimen are determined individually and depend on the localization of the process and the severity of the disease.

The drug is used inside, regardless of food intake, washed down with water. It is advisable to use the drug at the same time.

For adults:

The usual dose is 250 mg (1 tablet) once a day.

Onychomycosis: the duration of therapy is about 6-12 weeks.

With onychomycosis of the hands, in most cases,6 weeks of treatment is sufficient.

With onychomycosis of the feet, in most cases,12 weeks of treatment is sufficient. Some patients who have a reduced rate of nail growth may require longer treatment.

The optimal clinical effect is observed several months after mycological treatment and discontinuation of therapy. This is determined by the time period that is necessary for the growth of a healthy nail.

Fungal infections of the skin: the duration of treatment for interdigital, plantar or “sock” localization of infection is 2-6 weeks, for mycoses of other parts of the body: legs-2-4 weeks, trunk-4 weeks, for mycoses caused by Candida-2-4 weeks, for mycoses of the head caused by Micisporumcanis-more than 4 weeks.

For children:

A single dose depends on body weight and is: for children with a body weight of 20 to 40 kg – 125 mg (1/2 tablet 250 mg); with a body weight of more than 40 kg-250 mg.

The drug is prescribed 1 time a day.

The duration of treatment for mycoses of the scalp is about 4 weeks, with infection with Micisporumcanis-it can be longer.

For the elderly, the drug is prescribed in the same doses as for adults. If the drug is used in tablets in this age group, the possibility of concomitant liver or kidney dysfunction should be taken into account.

Overdose

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

Treatment: gastric lavage followed by use of activated charcoal and / or symptomatic therapy.

Special instructions

Irregular use of terbinafine or premature discontinuation of treatment may lead to relapse of the disease.

The duration of therapy may also be affected by factors such as the presence of concomitant diseases, the condition of the nails at the beginning of the course of treatment.

If after 2 weeks of treatment there is no improvement in the condition, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.

Systemic use in onychomycosis is justified only in the case of total damage to most nails, the presence of pronounced subungual hyperkeratosis, and the ineffectiveness of previous local therapy.

In the treatment of onychomycosis, a clinical response is usually observed several months after mycological treatment and discontinuation of treatment, 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.

In the presence of severe renal insufficiency (creatinine clearance less than 50 ml / min or blood creatinine more than 300 mmol / l), with impaired liver function, the dose of terbinafine should be halved.

In the presence of liver disease, the clearance of terbinafine may be reduced.

With reduced liver function, half the adult dose is prescribed.

Before starting the use of terbinafine tablets, it is necessary to conduct an analysis of liver function. Hepatotoxicity can occur both in patients with previous liver diseases and without them.

During therapy, a periodic study of liver function is recommended (4-6 weeks after the start of treatment). Treatment with terbinafine should be stopped immediately if the activity of “liver tests” increases.

Patients who are prescribed terbinafine should be warned to immediately inform the attending physician about the occurrence of symptoms such as persistent nausea, decreased appetite, fatigue, vomiting, pain in the right hypochondrium, jaundice, dark urine or light feces while taking the drug.

If such symptoms occur, you should immediately stop taking the drug and conduct a liver function study.

Serious skin reactions (including Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia and systemic symptoms) were extremely rare with terbinafine.

Prescribing terbinafine to patients with psoriasis requires increased caution, as in very rare cases, terbinafine can trigger an outbreak of psoriasis.

When using terbinafine tablets, extremely rare cases of changes in the cellular composition of blood (neutropenia, agranulocytosis, thrombocytopenia, pancytopenia) were noted. In case of qualitative or quantitative changes in the blood cells, the cause of the disorders should be determined and consideration should be given to reducing the dose of the drug or, if necessary, discontinuing therapy with terbinafine.

Terbinafine has been shown to inhibit metabolism mediated by isoenzyme 2D6 (CYP2D6).

Therefore, it is necessary to constantly monitor patients receiving concomitant treatment with terbinafine with drugs that are mainly metabolized with the participation of this enzyme (such as tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors, IC class antiarrhythmic drugs and type B monoamine oxidase inhibitors) if the drug used simultaneously has a small therapeutic concentration range.

When treating with terbinafine, general hygiene rules should be observed to prevent the possibility of re-infection through underwear and shoes. During the course of treatment (after 2 weeks) and at the end, it is necessary to perform antifungal treatment of shoes, socks and stockings.

Influence on the ability to drive vehicles and mechanisms

The effect of terbinafine on the ability to drive vehicles and work with mechanisms has not been studied. If dizziness develops during drug therapy, patients should not drive vehicles and / or work with mechanisms.

Form of production

Tablets of 250 mg

.7 or 10 tablets in a contour cell package made of polyvinyl chloride film and aluminum foil.

1,2,3 or 4 contour cell packages with instructions for use in a cardboard pack.

Storage conditions

Store in a dry place, protected from light, out of reach of children.

Shelf

life is 4 years. Do not use after the expiration date indicated on the package.

Active ingredient

Terbinafine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Fungus, Scalp Fungus, Nail Fungus, Skin Fungus