Tebicur^® (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 drugs for the treatment of skin diseases; antifungal drugs for systemic use

Pharmacological Action

An antifungal agent belonging to the allylamine group, it has a broad spectrum of antifungal action. At low concentrations, it exerts a fungicidal effect on dermatophytes Trichophyton spp. (Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Trichophyton verrucosum, Trichophyton violaceum), Microsporum canis, Epidermophyton floccosum, and mold fungi (for example, Scopulariopsis brevicaulis).

On yeast fungi, mainly Candida albicans, and their mycelial forms, it exerts, depending on the fungal species, a fungicidal or fungistatic effect.

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

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

Pharmacokinetics

When taken orally, it is well absorbed, with absorption exceeding 70%; the absolute bioavailability of terbinafine due to the first-pass effect is approximately 50%. After a single oral dose of 250 mg, its maximum plasma concentration (C_max) is reached within 1.5 hours and is 1.3 µg/ml. The area under the curve (AUC) is 4.56 µg×h/ml, and when taken with food, the AUC increases by 20%. With long-term use, C_max increases by 25%, and the AUC increases by 2.3 times. Plasma protein binding is 99%.

It is rapidly distributed in tissues, penetrates the dermal layer of the skin and nail plates. It penetrates into sebaceous gland secretion and accumulates in high concentrations in hair follicles, hair, skin, and subcutaneous tissue. It undergoes significant metabolism, and the resulting metabolites do not possess antifungal activity. Renal excretion is 70%. The effective half-life (T_1/2) is 30 hours, and the terminal half-life is 200-400 hours (indicating prolonged elimination from the skin and adipose tissue). It does not accumulate in the body.

Indications

Mycoses of the scalp (tinea capitis); fungal diseases of the skin and nails (onychomycosis) caused by Trichophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum; 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

Cream, Spray

Apply externally 1-2 times a day.

For adults and children 12 years and older, before applying the cream, it is necessary to clean and dry the affected areas. Apply the cream once or twice daily in a thin layer to the affected skin and adjacent areas and rub in 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.

Duration of treatment and frequency of application of the drug

Dermatomycosis of smooth skin and tinea cruris (including tinea corporis, tinea cruris): 1 week, twice a day (morning and evening).

Tinea pedis: 1 week, twice a day between the toes (morning and evening), 2 weeks, once a day (top and sides of the foot).

Fungal skin infections caused by yeasts (cutaneous candidiasis): 1 week, once a day.

Tinea versicolor: 2 weeks, once a day.

If after 1-2 weeks of treatment there are no signs of improvement, the diagnosis should be verified.

Elderly patients (over 65 years)

No dose adjustment is required in the elderly.

Tablets

Take orally.

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

Adults – at a dose of 250 mg once a day.

Children – at a dose of 125 mg once a day.

Adverse Reactions

From the digestive system: frequently – feeling of stomach fullness, nausea, abdominal pain, diarrhea, decreased appetite; in isolated cases ( 0.1-1%) – taste disturbances, including loss of taste (recovery occurs within several weeks after discontinuation of treatment); rarely ( 0.01-0.1%) – hepatotoxic effect (increased activity of liver enzymes, liver failure).

From the central nervous system: frequently – headache, dizziness.

From the hematopoietic system: very rarely ( <0.01%) – neutropenia, agranulocytosis, thrombocytopenia.

From the immune system: rarely – anaphylactoid reactions, including angioedema, exacerbation of systemic lupus erythematosus.

From the skin and subcutaneous tissue: frequently – rash, urticaria; very rarely – psoriasis-like skin rashes, exacerbation of psoriasis, Stevens-Johnson syndrome, toxic epidermal necrolysis, hair loss, acute generalized exanthematous pustulosis.

From the musculoskeletal system: frequently – arthralgia, myalgia.

General reactions: very rarely – fatigue.

Contraindications

Acute or chronic liver diseases; children under 2 years of age; lactation period; hypersensitivity to terbinafine.

With caution

Pregnancy; renal failure; alcoholism; bone marrow depression; tumors; metabolic diseases; occlusive vascular diseases of the extremities.

Use in Pregnancy and Lactation

There are no data on the safety of terbinafine use during pregnancy. Therefore, Terbinafine should be used during pregnancy only if the intended benefit to the mother outweighs the potential risk to the fetus.

Terbinafine is excreted in breast milk. Its use during breastfeeding is contraindicated.

Use in Hepatic Impairment

Contraindicated in acute or chronic liver diseases.

Use in Renal Impairment

The drug should be prescribed with caution in renal failure.

Pediatric Use

Contraindicated for use in children under 2 years of age (efficacy and safety have not been established).

Geriatric Use

For elderly patients, the drug is prescribed in the same doses as for adults.

Special Precautions

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

The duration of therapy can also be influenced by factors such as the presence of concomitant diseases, the condition of the nails at the beginning of the treatment course for onychomycosis.

If after 2 weeks of treatment for a skin infection there is no improvement, it is necessary to re-identify the causative agent of the disease and its sensitivity to the drug.

Systemic use for onychomycosis is justified only in cases of total involvement of most nails, the presence of pronounced subungual hyperkeratosis, and ineffectiveness of previous local therapy.

When treating onychomycosis, a clinical response, confirmed by laboratory tests, is usually observed several months after mycological cure and the end of the treatment course, which is due to the rate of regrowth of a healthy nail. Removal of nail plates during 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 liver disease, the clearance of terbinafine may be reduced.

During treatment, it is necessary to monitor the indicators of liver enzyme activity in the blood serum.

In rare cases, after 3 months of treatment, cholestasis and hepatitis may occur. If signs of impaired liver function appear (weakness, persistent nausea, loss of appetite, excessive abdominal pain, jaundice, dark urine, or discolored stools), the drug should be discontinued.

In severe renal impairment (creatinine clearance <50 ml/min or blood creatinine >300 µmol/l) and impaired liver function, the dose of terbinafine should be reduced by half.

Use in patients with psoriasis requires caution, as in very rare cases the drug may provoke an exacerbation of psoriasis.

During treatment with terbinafine, general hygiene rules should be observed to prevent the possibility of reinfection through underwear and shoes. During treatment (after 2 weeks) and at the end of it, antifungal treatment of shoes, socks, and stockings should be carried out.

Drug Interactions

It inhibits the isoenzyme CYP2D6 and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (for example, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), MAO-B inhibitors (for example, selegiline) and antipsychotic agents (for example, chlorpromazine, haloperidol).

Drugs that are inducers of cytochrome P450 isoenzymes (for example, rifampicin) may accelerate the metabolism and elimination of terbinafine from the body. Drugs that are inhibitors of cytochrome P450 isoenzymes (for example, cimetidine) may slow down the metabolism and elimination of terbinafine from the body. When these drugs are used concomitantly, adjustment of the terbinafine dose may be required.

Menstrual cycle disturbances are possible with the simultaneous use of terbinafine and oral contraceptives.

Terbinafine reduces the clearance of caffeine by 19% and prolongs its half-life (T_1/2) by 31%.

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

When used concomitantly with ethanol or drugs that have hepatotoxic effects, there is a risk of drug-induced liver damage.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.