Terbinafin of 250 mg

General characteristics. Structure:

Active ingredient: a terbinafina of a hydrochloride – 281,0 mg,

in terms of тербинафин – 250,0 mg;

excipients: lactoses monohydrate - 19,97 mg, cellulose microcrystallic - 61,43 mg, potato starch - 2,50 mg, croscarmellose sodium (primelloza) - 24,60 mg, talc - 12,30 mg, magnesium stearate - 4,10 mg, silicon dioxide colloid (aerosil) - 4,10 mg.

Description. Tablets of color, white or white with a grayish shade, round, biconvex.

Pharmacological properties:

Pharmacodynamics. Terbinafin treats group of allylamines, possesses a wide range of antifungal action. In low concentration has fungicidal activity concerning dermatophytes (Trychophyton rubrum, Trychophyton mentagrophytes, Trychophyton verrucosum, Trychophyton violaceum, Trychophyton tonsurans, Microsporum spp., Microsporum canis, Microsporum gypseum, Epidermophyton floccosum); concerning barmy mushrooms (in the main Candida albicans) activity depending on a look has fungicidal or fungistatic character. The mechanism of action of a terbinafin is carried out by skvalenepoksidaza enzyme inhibition in a cellular membrane of a mushroom (does not treat system of P450 cytochrome), specifically suppresses an early stage of synthesis of sterol in a mushroom cell that results in deficit of ergosterol, intracellular accumulation of squalene and death of a cell of a mushroom. Terbinafin has no significant effect on metabolism of hormones or other medicines. Multi-colored depriving system treatment, the caused Malassezia furfur, inefficiently.

Pharmacokinetics. At oral administration more than 70% are well absorbed; absolute bioavailability owing to effect of "the first passing" decreases by 40%. After a single dose inside in a dose of 250 mg time of achievement of the maximum concentration (TCmax) about 2 h; the maximum concentration (Cmax) - 1 mkg/ml. The area under a curve "concentration – time" (AUC) - 4,56 ¼¬ú*þ/ml, at a concomitant use with AUC food increases by 20%. At long reception of Cmax AUC - by 2,5 times increases by 25%. An effective elimination half-life (T 1/2) - about 36 h, terminal T of 1/2 200-400 h (points to long removal from skin and fatty tissue). Equilibrium concentration (Css) does not depend on age. Concentration of a terbinafin in plasma does not depend on a floor. Communication with proteins of plasma - more than 99 %. It is quickly distributed in fabrics, gets into a thermal layer of skin and nail plates. Gets into a secret of sebaceous glands and collects in high concentration in hair follicles, in hair, skin and a hypodermic kletkatka. Is exposed to considerable biotransformation, the formed metabolites have no antifungal activity. 70 % are removed by kidneys.

Does not kumulirut in an organism. The age of patients does not influence pharmacokinetics of a terbinafin, however elimination can decrease at damages of kidneys or a liver, resulting in high concentration of a terbinafin in blood. It is allocated with breast milk.

Indications to use:

- Mycoses of a pilar part of the head (trichophytosis, microsporia).

- The fungus diseases of skin and nails (onychomycoses) caused by Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum spp. (M. canis,
M. gypseum) and Epidermophyton floccocum.

- The heavy, widespread dermatomycoses of smooth skin of a trunk and extremities demanding system treatment.

- Candidiases of skin and mucous membranes when localization, expressiveness or prevalence of an infection cause expediency of peroral therapy.

Route of administration and doses:

Duration of a course of treatment and the mode of dosing is set in an individual order and depends on localization of process and disease severity.

Inside, after food, the adult on 0,25 g of 1 times a day.

To children at body weight more than 40 kg - 250 mg of 1 times a day.

The elderly patient drug is appointed in the same doses, as the adult.

Treatment duration at a dermatomycosis of feet (interdigital, bottom or as socks) - 2-6 weeks, at a dermatomycosis of a trunk, shins - 2-4 weeks, at skin candidiasis - 2-4 weeks, at mycosis of a pilar part of the head - 4 weeks, at an onychomycosis of brushes in most cases is enough 6 weeks of treatment, at an onychomycosis of feet – 12 weeks. Longer term of treatment can be required by some patients at whom the growth rate of nails is reduced.

Features of use:

Unlike a terbinafin for external use тербинафин for intake it is not effective at multi-colored (scaly) herpes.

Irregular use or the early end of treatment increases risk of development of a recurrence.

If in 2 weeks of treatment improvement of a state is not noted, it is necessary to define repeatedly an infestant and its sensitivity to drug.

Before the beginning and in the course of treatment control of indicators of function of a liver is necessary. At identification of the symptoms allowing to assume abnormal liver functions (a loss of appetite, persistent nausea, jaundice, dark urine, excessive fatigue), it is necessary to cancel drug.

During treatment it is necessary to control the level of transaminases of a liver in blood serum. In rare instances in 3 months of treatment there is a cholestasia and hepatitis.

At a chromophytosis only topical treatment is effective.

System use at an onychomycosis is justified only in case of total defeat of the majority of nails, existence of the expressed hyponychial hyperkeratosis, inefficiency of the previous local therapy.

In the course of treatment it is necessary to follow the general rules of hygiene for prevention of a reinfitsirovaniye (through linen, footwear).

In the course of treatment (in 2 weeks) and at the end of it it is necessary to make antifungal processing of footwear, socks and stockings. Such factors as, for example, existence of associated diseases, a condition of nails at the beginning of a course of treatment also can influence duration of therapy. Removal of nail plates at treatment of an onychomycosis of brushes within 3 weeks and an onychomycosis of feet within 6 weeks is not required.

Purpose of a terbinafin sick psoriasis demands extra care as it seldom or never тербинафин can provoke an exacerbation of psoriasis.

Side effects:

Frequency: very often - more than 1/10, it is frequent - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, is rare - more than 1/10000 and less than 1/1000, is very rare - less than 1/10000, including separate cases.

From the alimentary system: very often - feeling of overflow of a stomach, a loss of appetite, dyspepsia, nausea, abdominal pain, diarrhea; seldom - an abnormal liver function; very seldom - a liver failure, up to a lethal outcome.

From bodies of a hemopoiesis: very seldom - a neutropenia, an agranulocytosis, thrombocytopenia, a pancytopenia.

Allergic reactions: very seldom - anaphylactoid reactions (including a Quincke's disease).

From a nervous system: often - a headache; infrequently - taste disturbance, including an ageusia.

From integuments: very often - skin reactions (including rash, urticaria); very seldom - Stephens-Johnson's syndrome, a toxic epidermal necrolysis, psoriazopodobny rash, an exacerbation of the available psoriasis, an alopecia.

From a musculoskeletal system: very often - an arthralgia, a mialgiya. Other: very seldom – fatigue, a skin lupus erythematosus, a system lupus erythematosus or their aggravation.

Interaction with other medicines:

Inductors or inhibitors of microsomal enzymes of a liver can reduce or increase concentration of a terbinafin in plasma that can demand correction of the mode of dosing of the last.

Cimetidinum reduces plasma clearance of a terbinafin by 33 % and increases its concentration in plasma (increase in toxicity of the last).

Rifampicin increases clearance of a terbinafin for 100 % and reduces its concentration in plasma (decrease in efficiency of a terbinafin).

At a concomitant use with oral contraceptives disturbance of a menstrual cycle is possible.

Reduces clearance of caffeine by 19 % and increases its concentration in plasma (increase in toxicity of caffeine).

Inhibits CYP2D6 isoenzyme that can increase toxicity of substrates of this isoenzyme (tricyclic antidepressants, beta adrenoblockers, selective serotonin reuptake inhibitors, antiarrhytmic medicines I of a class, monoaminooxidase inhibitors In) with a narrow therapeutic range.

Raised Cmax and biological availability of desipramine in 2 and 5 times respectively at healthy volunteers with normal activity of an isoenzyme of CYP2D6.

Can weaken effect of cyclosporine and reduce its concentration in plasma; increases clearance of cyclosporine for 15 %.

Reduces a prothrombin time at a concomitant use with warfarin (relationship of cause and effect is not established).

Contraindications:

Hypersensitivity, to any component of drug; deficit of lactase, lactose intolerance, glyukozo-galaktozny malabsorption; pregnancy, the lactation period, children with body weight less than 40 kg (for this dosage form). The tablet contains 250 mg of a terbinafin, without risks, therefore, it is impossible to execute the dosing mode for children with body weight less than 40 kg. Chronic or active diseases of a liver, chronic renal failure (clearance of creatinine less than 50 ml/min.).

Overdose:

Symptoms: a headache, nausea, an abdominal pain, dizziness, the speeded-up urination, rash.

Treatment: a gastric lavage with the subsequent purpose of absorbent carbon and/or symptomatic therapy.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 250 mg. On 7 and 10 tablets in a blister strip packaging. On 1, 2, or 3 blister strip packagings together with the application instruction in a pack from a cardboard.