Tigal-Sanovel - instructions for use, doses, side effects, contraindications

active substance: terbinafine hydrochloride 281.25 mg (equivalent 250 mg terbinafine) Excipients: carboxymethyl starch sodium, hypromellose, microcrystalline cellulose, silicon dioxide colloid, magnesium stearate.

Description:Round flat tablets are white or almost white with 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, molds (for example, Scopulariopsis brevicalius), yeast-like fungi, mainly Candida albicans, and some dimorphic fungi. On mushrooms Candida spp. and their filamentous forms, depending on the type of fungus, have a fungicidal and fungistatic effect.

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

Pharmacokinetics:

When taken orally, it is absorbed well; absolute bioavailability due to the "first pass" effect of about 40%. After a single oral intake at a dose of 250 mg, the time to reach the maximum concentration (TCmax) is 1.67 hours; the maximum concentration (C max) is 0.99 μg / ml. Area under the curve "concentration - time" (AUC) - 4.34 mcg / mL, with simultaneous intake with food AUC increases by approximately 20%.

Terbinafine binds intensely to plasma proteins (99%). High concentrations are created in the hair follicles and hair. After a few weeks, the treatment also penetrates the nail plate, accumulates in the stratum corneum and nails in concentrations that provide fungicidal action.

Subject to significant biotransformation, the resulting metabolites do not have antifungal activity.

The effective half-life (T1 /₂) - about 36 hours, terminal T1_/2 200-400 h (indicates a prolonged excretion of the skin and adipose tissue). It is excreted through the skin, by the kidneys (70%) in the form of metabolites.

Do not cum in the body. The age of the 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:

- 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 Epidermophytum floccosum.

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

- Candidiasis of the skin and mucous membranes.

Contraindications:

- hypersensitivity to terbinafine and other components of the drug;

- children's age up to 3 years and with a body weight of less than 20 kg (for this dosage form);

- Chronic or active liver disease;

- Chronic renal failure (creatinine clearance less than 50 ml / min);

- lactation period;

- pregnancy.

Carefully:

renal failure (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, cutaneous lupus erythematosus or systemic lupus erythematosus.

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:

Inside, after eating.

The duration of the course of treatment and the dosage regimen is set individually and depends on the localization of the process and the severity of the disease.

Adults:

250 mg (1 tablet) once a day.

Onychomycosis: duration of therapy is about 6-12 weeks. If lesions of the fingers of the hands and feet (except for the thumb of the foot) are lost, or the patient is young, the duration of the treatment may be less than 12 weeks. In case of infection of the thumb, usually a three-month course of therapy is usually sufficient. In rare cases, with a slower rate of nail growth, longer treatment may be required up to 6 months or more.

Fungal skin infections: duration of treatment with interdigital, plantar or as a "socks" of infection localization is 2-6 weeks; with myosides 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.

Elderly patients dosage adjustment is not required.

Patients with hepatic and / or renal insufficiency (creatinine clearance <50 ml / min or a creatinine concentration in the blood of more than 300 μmol / l): 125 mg once a day.

For children:

Usually appoint 125 mg / day (1/2 tablet). The duration of treatment of mycosis of the scalp is about 4 weeks, when infected Microsporum canis - may be longer.

Weight of child's body	Dose
20-40 kg	125 mg (1/2 tablet) once a day
More than 40 kg	250 mg (1 tablet) 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 of the stomach, a decrease in appetite, indigestion, nausea, abdominal pain, diarrhea; rarely - a violation of liver function; very rarely - liver failure, up to a lethal outcome.

From the hematopoiesis: very rarely - neutropenia, agranulocytosis, thrombocytopenia, pancytopenia.

Allergic reactions: very rarely anaphylactoid reactions (including

angioedema).

From the nervous system: often - headache; infrequently - a violation of taste, including agevziyu.

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

From the musculoskeletal system: very often - arthralgia, myalgia.

Other: very rarely - fatigue; cutaneous lupus erythematosus, systemic redlupus or their exacerbation.

Overdose:

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

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

Interaction:

Inducers or inhibitors of microsomal liver enzymes may decrease or increase the concentration of terbinafine in the plasma, which may require correction of the dosage regimen of the latter.

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 plasma concentration (decreased terbinafine efficacy).

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

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

Inhibits isoenzyme CYP2D6, which can increase the toxicity of substrates of this isoenzyme (tricyclic antidepressants, beta-adrenoblockers, selective serotonin reuptake inhibitors, class I antiarrhythmics, MAO B inhibitors) with a narrow therapeutic range.

Increased Cmax and AUC desipramine in 2 and 5 times, respectively, in healthy volunteers with normal isoenzyme activity CYP2D6.

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

Reduces prothrombin time while taking with warfarin (cause-effect relationship not established).

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 two 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 laboratoryally, is usually observed a few months after mycological recovery and discontinuation of treatment,which is due to the rate of growth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of the brushes for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

In the presence of liver disease, the 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 abdominal pain, jaundice, darkening of the urine, or discolored stools), the drug should be discontinued.

The appointment of Tigal-sanovel with psoriasis requires increased circumspection; in very rare cases terbinafine can provoke an exacerbation of psoriasis.

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:

Tigal-sanovel does not affect the ability to drive a car and perform work that requires increased concentration.

Form release / dosage:

Tablets 250 mg.

For 14 tablets in a blister of PVC-aluminum foil. For 1.2 blisters together with instructions for use are placed in a cardboard box.

Packaging:(14) - packings, cellular, outline (1) - packs, cardboard
(14) - packings, cellular, outline (2) - packs, cardboard

Storage conditions:In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the time specified on the package

Terms of leave from pharmacies:On prescription

Registration number:LP-000205

Date of registration:11.02.2011

The owner of the registration certificate:Sanovel Pharmaco-industrial trading companySanovel Pharmaco-industrial trading company Turkey

Manufacturer: & nbsp

SANOVEL PHARMACEUTICAL PRODUCTS IND., Inc. Turkey

Representation: & nbspSANOVEL branch of the company pharmaco-industrial trading companySANOVEL branch of the company pharmaco-industrial trading companyRussia

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Tigal-Sanovel (Tigal-Sanovel)