Terbizil - instructions for use, dose, side effects, contraindications

Excipients: silicon dioxide colloid 3.9 mg, magnesium stearate 3.9 mg, hypromellose 11.7 mg, microcrystalline cellulose 44.4 mg, sodium carboxymethyl-starch, type "A" 44.85 mg.

Description:White or almost white, round, biconvex tablets,with a risk on one side and with an engraving "250" - on the other.

Pharmacotherapeutic group:Antifungal agent.

ATX: & nbsp

D.01.A.E.15 Terbinafine

Pharmacodynamics:

Terbinafine belongs to the group of allylamines, it has a wide spectrum of antifungal action. At low concentrations, it has a fungicidal effect on dermatophytes Trychophyton spp. (T. rubrum, T. mentagrophytes, T. tonsurans, T.verrucosum, T.violaceum), Microsporum canis, Epidermophyton floccosum, moldy mushrooms (ex. Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans. On mushrooms Candida spp. and their mycelial forms render a fungicidal or fungistatic action depending on the type of the fungus.

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

When administered orally, it is not effective in treating varicoloured hair loss caused by Pityrosporum ovale, Pityrosporum orbiculare, Malassezia furfur.

Pharmacokinetics:

When oral intake is well absorbed more than 70%, absolute bioavailability due to the effect of "first passage" is about 50%. After a single oral intake at a dose of 250 mg, the time to reach the maximum concentration in the plasma (Tgramx) is about 1.5 h; the maximum concentration (Stach) is 1.3 μg / ml.

Area under the curve "concentration - time" (AUC) - 4.56 μg^xh / ml, with simultaneous intake with food AUC increases by 20%. With prolonged admission, the Stakh increases by 25%, AUC - 2.3 times. The effective half-life (T1 / 2) is about 30 hours, the terminal T1 / 2 is 200-400 h (indicating a prolonged excretion from the skin and adipose tissue). The equilibrium concentration (Css) does not depend on age. The concentration of terbinafine in plasma does not depend on sex. The connection with plasma proteins is more than 99%. Rapidly distributed in tissues, penetrates the dermal layer of the skin and nail plates. Penetrates the secretion of sebaceous glands, and accumulates in high concentrations in the hair follicles, in hair, skin and subcutaneous tissue. Exposed to a significant metabolism, the resulting metabolites do not have antifungal activity. 70% are excreted by the kidneys. Do not cum in the body. The age of the patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with liver and kidney damage, leading to high concentrations of terbinafine in the blood. Excreted in breast milk.

Indications:

Mycosis of the scalp (trichophytosis, microsporia).

- Fungal diseases of the skin and nails (onychomycosis), caused by Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaccum), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum.

- Heavy, common dermatomycosis smooth skin of the trunk and extremities, requiring systemic treatment.

- Candidiasis of the skin and mucous membranes.

Contraindications:

Hypersensitivity to the active ingredient or to any of the excipients;

Acute or chronic liver disease;

Children under 2 years of age (efficacy and safety not established);

Lactation period.

Carefully:

With caution: pregnancy; kidney failure; alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities.

Pregnancy and lactation:

There are no data on the safety of terbinafine during pregnancy. therefore terbinafine should be used during pregnancy only if the intended benefit to the mother exceeds the possible risk to the fetus.

Lactation period

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

Dosing and Administration:

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.

Adults:

Inside, after eating.Usual dose: 250 mg once a day.

Onychomycosis: the duration of therapy on average 6-12 weeks. If the fingers and toes of the hands and feet (with the exception of the thumb of the foot) are affected, or when the patient is young, the duration of treatment may be less than 12 weeks. If infection of the thumb of the foot is usually enough 3-month course of treatment. Some patients who have a reduced rate of nail growth may need a longer period of treatment.

Fungal skin infections: the duration of treatment with interdigital, plantar, or "socks" localization of infection is 2-6 weeks, with fungal infections of other parts of the body: shins - 2-4 weeks, trunks - 2-4 weeks; with fungal infections caused by fungi of the genus Candida - 2-L weeks;

with mycosis of the scalp caused by fungi of the genus Microsporum - More than 4 weeks.

For children:

Usually appoint 125 mg.

With a body weight of 20 to 40 kg, 125 mg once a day.

With a body weight of more than 40 kg, 250 mg once a day.

The duration of mycosis treatment of the scalp is about 4 weeks, when infected Microsporum canis - may be longer.

Older patients prescribe the drug in the same doses as adults.

Patients with hepatic and renal insufficiency Terbizil is prescribed in a dose of 125 mg once a day.

Side effects:

From the side of the digestive tract: often: a feeling of overflow of the stomach, nausea, abdominal pain, diarrhea, decreased appetite; in isolated cases (0.1-1%) - a violation of taste, including their loss (recovery occurs within a few weeks after cessation of treatment); rarely (0.01-0.1%) - hepatotoxic effect (increased activity "hepatic" enzymes, hepatic insufficiency).

From the central nervous system: often: headache, dizziness.

On the part of the hematopoiesis 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: often: rash, hives; very rarely: psoriasis-like rashes on the skin, exacerbation of psoriasis, Stevens-Johnson syndrome, toxic epidermal necrolysis, hair loss, acute generalized exanthematous pustulosis.
From the musculoskeletal system and connective tissue: often: arthralgia, myalgia.
General disorders: very rarely: fatigue.

Overdose:

Symptoms: nausea, vomiting, headache, dizziness, pain in the epigastric region, in the lower abdomen, frequent urination.

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

Interaction:

Inhibits isoenzyme CYP2D6 and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (eg, desipramine, fluvoxamine), p-adrenoceptor blockers (metoprolol, propranolol), antiarrhythmic agents (flecainide, propafenone), monoamine oxidase B type inhibitors (eg, selegiline) and antipsychotic (for example, chlorpromazine, haloperidol) facilities.

Drugs - inductors of cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the metabolism and excretion of terbinafine from the body. Drugs - inhibitors of cytochrome P450 isoenzymes (for example, cimetidine) can slow the metabolism and excretion of terbinafine from the body. With the simultaneous use of these drugs, a dose adjustment of terbinafine may be required.

Possible violation of the menstrual cycle with the simultaneous administration of terbinafine and oral contraceptives.

Terbinafine reduces caffeine clearance by 19% and prolongs its half-life by 31%. Does not affect the clearance of phenazone, digoxin, warfarin.

When combined with ethanol or drugs that have a hepatoxic effect, there is a risk of developing drug damage to the liver.

Special instructions:

Unlike Terbizil® cream, the tablets are not effective against multi-colored lichen caused by the pathogen Malassezia furfur.

Irregular application of Terbizil® or premature discontinuation of treatment can lead to a relapse of the disease.

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

If after 2 weeks of treatment for a skin infection there is no improvement, it is necessary to repeatedly identify the pathogen and its sensitivity to the drug.

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

In the treatment of onychomycosis, a clinical response, confirmed laboratory, is usually observed a few months after mycological cure and cessation of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

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

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

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

In case of severe renal impairment (creatinine clearance <50 ml / min or creatinine> 300 μmol / L) and liver dysfunction, the dose of Terbizil® should be reduced in half.

The use of terbizil® with psoriasis requires caution, because in very rare cases, the drug may trigger an exacerbation of psoriasis.

When treating Terbizil®, general hygiene rules should be followed to prevent the possibility of re-infection through linens and shoes. In the process of treatment (after 2 weeks) and at the end of it, it is necessary to perform antifungal treatment of shoes, socks and stockings.

Effect on the ability to drive transp. cf. and fur:

Data that indicate the influence of Terbizil® on the ability to drive a car and perform work that requires increased concentration of attention is not available.

Form release / dosage:

Tablets 250 mg:

For 14 tablets in a blister of AL/ PVC. 1 or 2 blisters in a cardboard box with the attached instruction for use.

Packaging:(14) - blister (1) / For 14 tablets in a blister of AL / PVC. 1 or 2 blisters in a cardboard box with the attached instruction for use. "in bulk": 620 - 640 blisters, each containing 14 tablets each, are placed in a box. The box is supplied with a label. / - Cardboard tutu
(14) - blister (2) / For 14 tablets in a blister of AL / PVC. 1 or 2 blisters in a cardboard box with the attached instruction for use. "in bulk": 620 - 640 blisters, each containing 14 tablets each, are placed in a box. The box is supplied with a label. / - Cardboard tutu

Storage conditions:

Store at a temperature of 15-30 ° C, in a place protected from light.

Keep out of the reach of children!

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013952 / 01

Date of registration:22.12.2011

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER OJSC Hungary

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp18.09.2015

Illustrated instructions

Instructions

Terbisil® (Terbisil®)