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

Active substance: terbinafine hydrochloride 281 mg, in terms of terbinafine 250 mg. Excipients: croscarmellose sodium - 12.3 mg, potato starch - 9.4 mg, povidone (polyvinylpyrrolidone) - 12 mg, purified water - 6.1 mg, magnesium stearate - 3.2 mg.

Description:

Tablets are white or almost white in a flat-cylindrical form, with a facet on both sides and a risk on one side.

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, yeast grains, mainly Candida albicans. On mushrooms Candida spp, and their filamentous forms, depending on the type of fungus, fungicidal or fungistatic action.

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

When oral administration is not effective in the treatment of "multicolored lichen, caused by Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics:

When taken orally, more than 70% is absorbed well; Absolute bioavailability due to the effect of "first passage" is reduced by 40%. After single oral intake at a dose of 250 mg time to reach the maximum concentration (ТСmах) about 2 hours; the maximum concentration (Stach) is approximately 1 μg / ml. Area under the curve "concentration - time" (AUC) - 4.5 μg * h / ml, with simultaneous intake with food AUC increases by 20%. With prolonged admission, the Stakh increases by 25%, AUC - 2.5 times. The effective half-life (T1 / 2) is about 36 hours, terminal T1 / 2 200-400 hours (indicates a prolonged excretion of 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 into the secretion of sebaceous glands and accumulates in high concentrations in the hair follicles, in hair, skin and podkozhnoy cellulose. Subject to significant biotransformation, the resulting metabolites do not have antifungal activity. 70% are excreted by the kidneys.

Do not cum in the body. The age of patients does not affect the pharmacokinetics of terbinafine, however, elimination may decrease with renal or hepatic involvement, 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. violaceum), 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.

Contraindications:

Hypersensitivity to the components of the drug; chronic or active liver disease, chronic renal failure (creatinine clearance less than 50 ml / min), children under 3 years of age and with a body weight of up to 20 kg (for this dosage form), lactation period, pregnancy.

Carefully:

Renal insufficiency (with creatinine clearance more than 50 ml / min), alcoholism, oppression of bone marrow hematopoiesis, tumors, metabolic diseases, occlusive diseases of the vessels of the extremities.

Pregnancy and lactation:

The intake of terbinafine during pregnancy is contraindicated due to the lack of sufficient data on its safety during pregnancy.

Terbinafine is excreted in breast milk, therefore its purpose is contraindicated in the period of breastfeeding.

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 fingernails of the fingers are bruised and stop (except for the thumb of the foot), or at a young age of the patient, 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 longer duration of treatment.

Fungal skin infections: the duration of treatment with interdigital, plantar, or "socks" localization of infection is 2-6 weeks, with mycoses of other parts of the body: shins - 2-4 weeks, trunks - 2-4 weeks;

With fungal infections caused by fungi of the genus Candida - 2-4 weeks; with mycosis of the scalp caused by fungi of the genus Microsporum - More than 4 weeks.

For children:

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.

The elderly the drug is prescribed in the same doses as for adults.

Patients with renal insufficiency (KC more than 50 ml / min) terbinafine prescribe a dose of 125 mg once a day.

Side effects:

Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less than 1/10000, including individual cases.

From the digestive system: very often - a feeling of overflow

stomach, decreased appetite, indigestion, nausea, mild abdominal pain, diarrhea.

From the hematopoiesis: very rarely - neutropenia, agranulocytosis, pancytopenia. In very rare cases, the use of the drug marked the development of qualitative or quantitative changes in the form of blood elements (neutropenia, agranulocytosis, thrombocytopenia, pancytopenia). In the case of qualitative or quantitative changes in the blood constituents, the cause of the disturbances should be established and the issue of reducing the dose of the drug or, if necessary, discontinuing therapy, should be considered.

From the immune system: very rarely anaphylactoid reactions (including angioedema, swelling and systemic lupus erythematosus.__________________________________________

From the nervous system: often - headache; infrequent - a violation of taste

sensations, including their loss (usually recovery occurs within

weeks after the cessation of treatment). There are separate reports on

cases of long disturbances of taste sensations. In some cases, while taking the drug, a decrease in food intake was noted, which led to a significant reduction in weight. Very rarely - dizziness, paresthesia,

i .

hypoesthesia.

From the hepatobiliary system: rarely hepatobiliary dysfunction (mostly of the cholestatic nature), including very rare cases of severe hepatic insufficiency (some with fatal outcome or requiring liver transplantation).

6 2 3 85

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From the skin: very often - skin reactions (including rashes, hives); very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, psoriasis-like rashes on the skin, exacerbation of existing psoriasis, alopecia.

From the musculoskeletal system: very often - arthralgia, myalgia. Other: very rarely - a feeling of fatigue.

Overdose:

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

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

Interaction:

The plasma clearance of terbinafine can be accelerated under the influence of drugs - inducers of metabolism, and suppressed under the influence of inhibitors of cytochrome P450.

If it is necessary to simultaneously apply the above drugs and terbinafine, a corresponding correction of the dosage regimen of the latter may be required.

Cimetidine reduces the plasma clearance of terbinafine by 33% and increases its plasma concentration (increased toxicity of the latter).

Rifampicin increases terbinafine clearance by 100% and reduces its concentration in plasma (decreased terbinafine efficacy).

The results of studies conducted in vitro and in healthy volunteers, show that terbinafine has little potential to suppress or enhance the clearance of most drugs that are metabolized by the cytochrome P450 system (eg, terfenadine, triazolam, tolbutamide or oral contraceptives), except for those that are metabolized with CYP2D6.

Terbinafine does not affect the clearance of the antipyrine or digoxin.

With simultaneous administration with oral contraceptives, a menstrual cycle disorder is possible.

Reduces caffeine clearance by intravenous administration by 19% and increases its plasma concentration (increased caffeine toxicity).

In studies in vitro and in vivo it was shown that terbinafine suppresses metabolism, mediated by enzyme 2D6 (CYP2D6). These data can be clinically significant for those drugs that are metabolized primarily by this enzyme: tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors, class I antiarrhythmic drugs, monoamine oxidase B type inhibitors, if the concomitant drug has a small range of therapeutic concentration.

Terbinafine reduces the clearance of desipramine by 82%.

Terbinafine can weaken the action of cyclosporine and reduce its concentration in the plasma; increases the clearance of cyclosporine by 15%.

Special instructions:

Irregular application of terbinafine or premature termination 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 with onychomycosis is justified only in the case of total defeat of most nails, the presence of pronounced subungual hyperkeratosis, ineffectiveness of prior 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 "hepatic" transaminases in the blood serum.

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

When treating terbinafine, 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 produce antifungal treatment of shoes, socks and stockings.

Effect on the ability to drive transp. cf. and fur:The effects of terbinafine on the ability to drive vehicles and work with mechanisms have not been studied. With the development of dizziness against the background of drug therapy, patients should not drive vehicles and / or work with mechanisms.

Form release / dosage:

Tablets 250 mg.

By 7, 10, 14 tablets are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered. 10, 14, 20, 28, 30, 40, 50 or 100 tablets are placed in a polymer container for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008610/10

Date of registration:24.08.2010

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Exeter (Exiter)