Composition, form of production and packaging
Tablets are white or almost white in color, round, biconvex, with a risk on one side.
1 tab.
terbinafine hydrochloride 252 mg,
which corresponds to the content of terbinafine 250 mg
[PRING] hypromellose, corn starch, calcium stearate, silicon dioxide colloid, talc purified, paraffin liquid light, microcrystalline cellulose, sodium croscarmellose, sodium carboxymethyl starch.
14 pcs. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Terbinafine, the active ingredient of Terbinox, is an allylamine and has a broad spectrum of antifungal activity. At low concentrations, it has a fungicidal effect on Trichophyton dermatophytes (T. rubrum, T.mentagrophytes, T.verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (Aspergillus, Cladosporium, Scopulariopsis brevicalius), yeast fungi, mainly Candida albicans and some dimorphic fungi. The action on yeast fungi of the genus Candida and its mycelial forms can be fungicidal or fungistatic, depending on the species of the fungus.
Terbinafine disrupts the early stage of biosynthesis of the main component of the cellular membrane of the ergosterol fungus by inhibiting the squalene-epoxidase enzyme.
When administered orally, it is ineffective in the treatment of varicolored lichen caused by Malassezia furfur.
PHARMACOKINETICS
When oral intake is well absorbed, after 0.8 h half of the dose is absorbed; After 4.6 h half of the dose taken is distributed in the body. After 1-2 hours after ingestion of a single dose of 250 mg C max of the drug in the blood plasma reaches 0.97 Ојg / ml. Bioavailability - about 40% (the effect of "first passage"). Eating does not affect the bioavailability of terbinafine.
Terbinafine binds intensely to blood plasma proteins (99%), spreads rapidly 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 subcutaneous tissue.
T 1/2 - 16-18 h, T 1/2 of the terminal phase - 200-400 h. Biotransformed in the liver to inactive metabolites; 80% of the accepted dose is excreted through the kidneys in the form of metabolites, the rest (22%) - through the intestine. 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.
Excreted in breast milk.
INDICATIONS
- mycoses of the scalp (trichophytosis, microsporia);
- skin and nail mycoses caused by Trichophyton (T. rubrum, T.mentagrophytes, T.verrucosum, T. violaceum), Microsporum (M.canis, M.gypseum) and Epidermophyton floccosum;
- onychomycosis;
- severe, common dermatomycosis of the smooth skin of the trunk and extremities, requiring systemic treatment;
Candidiasis of the skin and mucous membranes.
DOSING MODE
The duration of the course of treatment and the dosage regimen is determined individually and depends on the localization of the process and the severity of the disease.
Adults: usual dose - 250 mg (1 tab.) 1 time / day.
Onychomycosis: the duration of therapy is about 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 a big toe infection is present, a 3-month course of treatment is usually sufficient. In rare cases, slower growth of nails may require longer treatment - up to 6 months or more.
Fungal skin infections: the duration of treatment with interdigital, plantar or socks-like infection localization is 2-6 weeks, with mycoses of other parts of the body: shins - 2-4 weeks, trunk - 4 weeks; with mycoses caused by Candida- 2-4 weeks; with mycosis of the head caused by Microsporum canis - more than 4 weeks.
Children: usually prescribed 125 mg. The duration of treatment of mycosis of the scalp about 4 weeks, with infection of Microsporum canis- may be longer. With abody weight of less than 20 kg , 62.5 mg once a day. With a body weight of 20 kg to 40 kg - 125 mg 1 time / day. With a body weight of more than 40 kg - 250 mg 1 time / day.
Older patients prescribe the drug in the same doses as adults.
With severe liver and / or kidney dysfunction (creatinine clearance <50 ml / min or creatinine concentration in the blood more than 300 Ојmol / l) -125 mg 1 time / day.
SIDE EFFECT
On the part of the digestive system: dyspeptic disorders (decreased appetite, nausea, diarrhea, a feeling of stomach overflow, abdominal pain), taste disorders, including their loss (recovery occurs within a few weeks after cessation of treatment); extremely rarely - a hepatotoxic effect (increased liver transaminase activity, hepatic insufficiency), hepatobiliary disorders (cholestatic jaundice).
Allergic reactions: urticaria, rash; very rarely - malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions.
From the musculoskeletal system: arthralgia, myalgia.
From the hemopoietic system: extremely rare - agranulocytosis or thrombocytopenia, neutropenia.
CONTRAINDICATIONS
- children's age till 3 years;
- Pregnancy;
- lactation period;
- Hypersensitivity to any component of the drug.
With caution: hepatic and / or renal failure, 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.
APPLICATION FOR FUNCTIONS OF THE LIVER
With severe renal dysfunction (creatinine clearance <50 ml / min or a creatinine concentration in the blood of more than 300 Ојmol / l) -125 mg 1 time / day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
At the expressed infringements of function of a liver- 125 mg 1 time / sut.
APPLICATION FOR CHILDREN
Children: usually prescribed 125 mg. The duration of treatment of mycosis of the scalp about 4 weeks, with infection of Microsporum canis- may be longer. With abody weight of less than 20 kg , 62.5 mg once a day. With a body weight of 20 kg to 40 kg - 125 mg 1 time / day. With a body weight of more than 40 kg - 250 mg 1 time / day.
APPLICATION IN ELDERLY PATIENTS
Older patients prescribe the drug in the same doses as adults.
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 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 is usually observed a few months after mycological cure and discontinuation 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 severe renal failure (creatinine clearance less than 50 ml / min or creatinine in the blood more than 300 Ојmol / L), if the liver function is disrupted, the dose of terbinafine should be reduced by half. In the presence of liver disease, the terbinafine clearance can be reduced. With reduced liver function, a half of the adult dose is prescribed. During treatment, it is necessary to control the level of liver 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, loss of appetite, abdominal pain, jaundice, darkening of the urine or colorless stools), the drug should be discarded.
The administration of terbinafine to psoriasis patients requires increased discretion; in very rare cases terbinafine can trigger an outbreak of psoriasis. When treating terbinafine, general hygiene rules should be followed to prevent the possibility of re-infection through linen and shoes. During the treatment (after 2 weeks) and at the end of the course of treatment, it is necessary to produce antifungal treatment of shoes, socks and stockings.
Impact on the ability to drive vehicles and manage mechanisms
Terbinafine does not affect the ability to drive and perform work that requires increased concentration.
OVERDOSE
Symptoms: nausea, vomiting, pain in the lower abdomen, in the epigastric region.
Treatment: gastric lavage followed by prescription of activated charcoal and / or symptomatic therapy.
DRUG INTERACTION
Inhibits the isozyme CYP2D6 and prevents the metabolism of drugs such as tricyclic antidepressants and selective blockers of the seizure of serotonin (desipramine, fluvoxamine), beta 1 -adrenoceptors (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), MAO inhibitors type B (selegiline) and antipsychotic (chlorpromazine, haloperidol).
Medications-inductors of enzymes CYP450 (rifampicin) can accelerate the excretion of terbinafine from the body.
Drugs inhibitors of CYP450 (cimetidine) can slow down metabolism and remove 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.
Decreases caffeine clearance by 21% and prolongs its half-life by 31%.
Does not affect the clearance of phenazone, digoxin, warfarin.
Ethanol and other hepatotoxic drugs increase the risk of developing a hepatotoxic effect.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. Keep out of reach of children, protected from light at a temperature of no higher than 30 В° C. Shelf life - 5 years. Do not use after the expiration date printed on the package.
