medicalmeds.eu Medicines Antifungal means Атифин®

Атифин®

Producer: Krka Slovenia

Code of automatic telephone exchange: D01BA02

Release form: Firm dosage forms. Tablets.

Indications to use:

General characteristics. Structure:

Active ingredient: 140,5 mg and 281,0 mg of a terbinafin of a hydrochloride that there correspond 125 mg or 250 mg to a terbinafin to the basis.

Excipients: lactoses monohydrate, cellulose microcrystallic, croscarmellose sodium, povidone, talc, silicon colloid anhydrous, magnesium stearate.

Antifungal drug of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Terbinafin treats group of allylamines, possesses a wide range of antifungal action. In low concentration has fungicidal effect on Trychophyton dermatophytes (T. rabrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T.violaceum), Microsporum canis, Epidermophyton floccosum, mold mushrooms (e.g. Aspergillus, Cladosporium, Scopulariopsis brevicalius), barmy mushrooms, mainly Candida albicans, and some dimorphous mushrooms. Renders on mushrooms of Candida and its mitselialny forms depending on a species of a mushroom fungicidal or a fungistasis. Terbinafin breaks an early stage of biosynthesis of the main component of a cellular membrane of a mushroom of ergosterol by enzyme inhibition squalene-epoksidazy. Skvalen-epoksidaza it is not connected with system of P450 (SUR450) cytochrome therefore тербинафин does not influence metabolism of hormones and medicines which metabolism is connected with SUR450. At oral administration collects in skin, nails and in hair in the quantity having fungicidal effect. Multi-colored depriving system treatment, the caused Malassezia furfur, inefficiently.

Pharmacokinetics. at oral administration it is well absorbed, in 0,8 hours a half of the accepted dose is absorbed; in 4,6 hours a half of the accepted dose is distributed in an organism. In 1-2 hours after intake of single 250 mg of a dose the maximum concentration of drug in a blood plasma reaches 0,97 mkg/ml. Bioavailability of 80%. Meal does not influence bioavailability of a terbinafin. Terbinafin intensively contacts proteins of a blood plasma (99%), quickly extends in fabrics, the layer of skin and nail plates gets into dermalny. Gets into a secret of sebaceous glands and accumulates in high concentration in hair follicles, in hair, skin and in hypodermic cellulose. In several weeks of treatment collects in nails in the concentration providing fungicidal action. Semi-removal time - 16-18 h, time of semi-removal of a terminal phase - 200-400 h Biotransformiruyetsya in a liver to inactive metabolites; 80% of the accepted dose are removed with urine in the form of metabolites, other part (20%) - with a fecal masses. It does not kumulirutsya 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 together with breast milk.

Indications to use:

• Mycoses of a pilar part of the head (trichophytosis, microsporia);

• The mycoses of skin and nails caused by Trychophyton (T. rubrum, mentagrophytes, verrucosum, violaceum), Microsporum (M. cards, M. gypseum) and Epidermophyton floccosum;

• Onychomycoses;

• The heavy, widespread dermatomycoses of smooth skin of a trunk and extremities demanding system treatment;

• Candidiases of skin and mucous membranes.

Route of administration and doses:

Drug is accepted inside, after food. 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.
Adults: 250 mg (1 tablet) once a day.

Children:

Body weight of the child	Dose
12-20 kg	62,5 mg (1/2 tablets of 125 mg) of 1 times a day
20-40 kg	125 mg (1 tablet of 125 mg) of 1 times a day

More than 40 kg 250 mg (1 tablet of 250 mg) of 1 times a day.
Duration of treatment is various and depends on indications and weight of an infection.

Disease treatment Duration
Skin infections
Tinea pedis	2-6 weeks
Trichophytosis of smooth skin and inguinal epidermophitia	2-4 weeks
Skin candidiasis	2-4 weeks
Symptoms of an infection can sometimes disappear several weeks later after the end of treatment terbinafiny.
Infections of hair and pilar part of the head
Cutting deprive	4 weeks
Cutting deprive is preferential children's infection.
Onychomycoses	6-12 weeks
Infections of fingers of hands	6 weeks
Infections of toes	12 weeks ( treatment within 6 and more months in certain cases is required)
Long treatment ( more than 3 months) is required from patients with slowly growing nails. The clinical effect can be swept up in several months after the end of treatment depending on time necessary for regeneration of nail fabric.

At the expressed abnormal liver functions and/or kidneys (clearance of creatinine <50 ml/min. or concentration of creatinine in blood more than 300 µmol/l): 125 mg once a day.

Features of use:

With care: liver and/or renal failure, alcoholism; blood diseases; tumors; metabolism diseases; pathology of vessels of extremities, psoriasis.

Irregular use of Atifin or the premature termination of treatment leads to a disease recurrence.

Such factors as e.g. existence of associated diseases, condition of nails at the beginning of a course of treatment also can influence duration of therapy.

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

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. At treatment of an onychomycosis the clinical answer, usually, is observed in several months after mycologic treatment and the termination of a course of treatment that is caused by the speed of growth of a healthy nail. Removal of nail plates at treatment of an onychomycosis of brushes during 3 weeks and an onychomycosis of feet during 6 weeks is not required.

In the presence of a heavy renal failure (clearance of creatinine less than 50 ml/min. or creatinine in blood more than 300 µmol/l), at an abnormal liver function it is necessary to reduce a dose of a terbinafin twice. In the presence of a liver disease the clearance of a terbinafin can be reduced. At reduced function of a liver appoint a half an adult dose. 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 emergence of signs of an abnormal liver function (weakness, persistent nausea, loss of appetite, an abdominal pain, jaundice, darkening of urine or a colourless chair) drug should be cancelled.

Atifin's appointment sick psoriasis demands the increased discretion since it seldom or never тербинафин can provoke an exacerbation of psoriasis. At treatment by Atifin it is necessary to follow the general rules of hygiene for prevention of a possibility of repeated infection through linen and 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.

Reception of a terbinafin during pregnancy is contraindicated due to the lack of enough data on its safety during pregnancy.
Terbinafin is allocated with breast milk therefore its appointment is contraindicated during breastfeeding.

Atifin does not influence ability to drive the car and to perform the works demanding the increased concentration of attention.

Side effects:

Side effects of usually average and easy severity are also temporary. Often found side effects from bodies of system of digestion: the feeling of the crowded stomach, dyspepsia, nausea, loss of appetite, an abdominal pain, diarrhea, is not frequent - disturbance of flavoring perception, including its loss which is recovered in several weeks after the treatment termination; seldom - cholestatic jaundice, hepatitis, asymptomatic increase in level of transaminases of a liver. Despite an absence of proof of a causal relationship of these disturbances with reception of a terbinafin, in case of development of gepatobiliarny dysfunction treatment by Atifin should be stopped.

From TsNS: seldom - paresthesia, a giposteziya, dizziness, it is very rare - a depression, feeling of the increased alarm.

From a musculoskeletal system: often arthralgia, mialgiya. From system of a hemopoiesis: very seldom neutropenia, agranulocytosis, thrombocytopenia.

From immune system: often a small tortoiseshell, a mnogoformny erythema, it is rare - system allergic reactions (reactions similar to a serum disease, a Quincke's disease), is very rare - heavy skin reactions (a toxic epidermal necrolysis, a syndrome Stephens Johnson, photosensitivity). When progressing skin rashes treatment terbinafiny should be stopped.

Others: often a headache, feeling sick, feeling of fatigue, it is very rare - an exacerbation of psoriasis, the strengthened hair loss.

Interaction with other medicines:

Practically does not influence clearance of the drugs which are metabolized with P450 cytochrome participation (e.g. cyclosporine, терфенадин, Tolbutamidum, to triazoles, oral contraceptives).

Inhibits CYP2D6 isoenzyme and interferes with metabolism of such drugs as tricyclic antidepressants and the selection blockers of serotonin reuptake (e.g. desipramine, флувоксамин), 01 - blockers (метопролол, propranolol), antiarrhythmic means (флекаинид, проавфенон), MAO-B - inhibitors (e.g. селегилин) and antipsychotic (e.g. Chlorpromazinum, a haloperidol). Medicinal drugs inductors of SUR450 enzymes (e.g. rifampicin) can accelerate removal of a terbinafin from an organism.

The medicinal drugs-inhibitors SUR450 (e.g. Cimetidinum) can slow down metabolism and removal of a terbinafin from an organism. At simultaneous use of these drugs dose adjustment of a terbinafin can be required. Disturbance of a menstrual cycle at a concomitant use of a terbinafin and oral contraceptives is possible.

Reduces clearance of caffeine by 21% and prolongs time of its half-decay for 31%. Does not influence clearance of antipyrine, digoxin, warfarin.

Ethanol and other gepatotoksichny drugs increase risk of development of hepatotoxic effect.

Contraindications:

Hypersensitivity to a terbinafin and other components of drug; children's age up to 2 years since there is no enough data on drug use by children with body weight less than 12 kg; pregnancy; feeding period breast.