Lamikon (tablets)

General characteristics. Structure:

Active ingredient: terbinafine;

1 tablet contains a terbinafin of a hydrochloride in terms of тербинафин 100% anhydrous substance of 250 mg;

excipients: cellulose microcrystallic, starch corn, silicon dioxide colloid anhydrous, sodium krakhmalglikolit (type A), a gidroksipropilmetiltsellyuloz, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Terbinafin is alilaminy which has a broad spectrum of activity against an infection of skin, hair and nails caused by such dermatophytes as Trichophyton (for example, T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. Violaceum), Microsporum (for example, Microsporum canis), Epidermophyton floccosum and drozhzhepodobny mushrooms of the sort Candida (for example, Candida albicans) and Pityrosporum. In low concentration тербинафин shows fungicidal action concerning dermatophytes, mold and some dimorphous mushrooms. Activity of rather drozhzhepodobny mushrooms, depending on their look, can be fungicidal or fungistatic. Terbinafin specifically stimulates an early stage of biosynthesis of sterols in a mushroom cell. It results in deficit of ergosterol, intracellular accumulation of squalene and death of a cell of a mushroom. Action of a terbinafin is carried out by skvalenepoksidaza enzyme inhibition in a cellular membrane. This enzyme does not belong to system of P450 cytochrome.

At use inside drug collects in skin, hair and nails in concentration which provide fungicidal action.

Pharmacokinetics. After oral administration taking into account metabolism after the first passing through a liver тербинафин it is well absorbed (> 70%), and absolute bioavailability of a terbinafin makes about 50%. The single peroral dose of 250 mg of a terbinafin showed average value of peak concentration in a blood plasma – 1,3 mkg/ml in 1,5 hours after reception. With a condition of a stable state, in comparison with a single dose, peak concentration of a terbinafin was on average 25% higher, and the area under a curve of a blood plasma increased by 2,3 times. On the basis of increase in the area under a curve in a blood plasma it is possible to calculate an effective elimination half-life ≅ 30 hours. The food influences bioavailability of a terbinafin a little (increase in the area under a curve about 20%) that does not demand correction of a dose.

Terbinafin actively contacts proteins of plasma (99%). It quickly diffuses through a derma and concentrates in a lipophilic corneous layer. Terbinafin is also allocated with sebaceous glands and reaches high concentration in hair follicles, hair and skin. It is proved what тербинафин is distributed in nail plates for the first weeks after an initiation of treatment.

Terbinafin is quickly metabolized with participation not less than seven isoenzymes of P450 cytochrome. at the same time the main role is played by isoenzymes of CYP2C9, CYP1A2, CYP3A4, CYP2S8, CYP2S19. Changes of equivalent concentration of a terbinafin in plasma depending on age are not revealed, but patients with a renal failure or a liver can have a slowed-down drug removal speed that results in higher concentration of a terbinafin in blood.

Owing to biotransformation of a terbinafin metabolites which have no antifungal action are formed and removed preferential with urine.

Pharmacokinetic researches of a single dose at patients with a renal failure (clearance of creatinine <50 ml/min.) or with earlier existing diseases of a liver showed that the clearance of a terbinafin can decrease approximately by 50%.

Pharmaceutical harakterist

Main physical and chemical properties: tablets white or almost white, or with a yellowish shade of color, a round form with a flat surface, a facet and risky.

Indications to use:

Onychomycosis (fungal infection of nails) caused by mushrooms dermatophytes.
Mycoses of a pilar part of the head.
Fungal infections of skin (a trichophytosis of smooth skin, a crotch, the dermatomycoses and barmy infections of skin caused by sort Candida mushrooms (for example, Candida albicans)) in such cases when localization of defeats, expressiveness or prevalence of an infection cause expediency of peroral therapy.

Unlike Lamikon for topical administration, a tablet Lamikon is not applied to treatment multi-colored depriving.

Route of administration and doses:

Duration of treatment depends on character and weight of a course of a disease.

Adults.

250 mg of 1 times a day.

Children.

Lamikon appoint to children 6 years with body weight more than 20 kg are more senior.

To children with the body weight from 20 to 40 kg – 125 mg (1/2 tablets of 250 mg) of 1 times a day.

To children with body weight> 40 kg – 250 mg of 1 times a day.

Skin infections.

The recommended treatment duration:
Dermatomycoses of feet: 2-6 weeks;
Trichophytosis of smooth skin, crotch: 2-4 weeks;
Skin candidiasis: 2-4 weeks.

Total disappearance of displays of an infection and the complaints connected with it can come only in several weeks after mycologic recovery.

Infections of a pilar part of the head.

The recommended treatment duration:

Fungal infection of a pilar part of the head – 4 weeks.

The fungal infection of a pilar part of the head is observed preferential at children.

Onychomycosis.

Duration of effective treatment for most of patients – from 6 to 12 weeks.

Onychomycosis on hands.

Duration of therapy is 6 weeks.

Onychomycosis standing.

12 week course are in most cases necessary.

Longer course can be necessary for some patients who have the reduced growth rate of nails.

At fungal infections of nails the optimum clinical effect is observed in several months after mycologic recovery and the termination of therapy. It corresponds to that span which is necessary for growth of a healthy nail.

Features of use:

Lamikon is not recommended to patients with chronic or active damage of a liver. Before Lamikon's appointment it is necessary to estimate a condition of the patient and already existing liver diseases.

Hepatotoxic can occur at patients with the disease of a liver which is already existing earlier and without it. Patients who accept Lamikon have to be warned that it is necessary to report urgently to the doctor about any symptoms of constant nausea not of a clear etiology, anorexia, fatigue, vomiting, pain in the right upper part of an abdominal cavity, jaundice, dark urine or light excrements. Patients with such symptoms have to stop Lamikon's use, and function of a liver of the patient needs to be estimated urgently.

In case of developing of the progressing rash on skin, treatment by Lamikon needs to be stopped.

In case of any pathological changes of a picture of blood at the patients accepting Lamikon it is necessary to recommend possible replacement of drug treatment, including the termination of reception of Lamikon.

At patients with reduced function of kidneys (the clearance of creatinine less than 50 ml/min. or creatinine of blood serum exceeds 300 µmol/l) Lamikon's use was not studied therefore to such patients Lamikon is not recommended to apply.

Ability to influence speed of response at control of motor transport or work with other mechanisms

 

Data on Lamikon's influence on ability to manage motor transport and to work with mechanisms are absent.

Side effects:

Lamikon is well had. Side effects usually poorly or are moderately expressed and have fast-passing character.

At assessment of frequency of emergence of various side reactions such classification is used:

Often meeting (≥10%), extended (from ≥1% to 10%), not extended (from ≥0,1% to <1%), seldom meeting (from ≥0,01% to <0,1%), very seldom meeting

(<0,01%), including single messages.

From system of blood and lymphatic system: very seldom meeting – a neutropenia, an agranulocytosis, thrombocytopenia, a pancytopenia.

From immune system: very seldom meeting – anaphylactoid reactions (including a Quincke's disease), skin and system manifestations of a lupus erythematosus, Stephens-Johnson's syndrome, a toxic epidermal necrolysis (Layell's syndrome), a photosensitization.

From a nervous system: extended – a headache; seldom meeting – disturbance of taste which is usually recovered within several weeks after the treatment termination; very seldom meeting – dizziness, paresthesia and a hypesthesia.

From digestive tract: often meeting – feeling of overflow of a stomach, appetite loss, dyspepsia, nausea, small pain in a stomach, diarrhea.

From gepatobiliarny system: seldom meeting – increase in level of liver enzymes, gepatobiliarny dysfunction (mainly a cholestatic origin). Separate cases of heavy abnormal liver functions such as cholestasia, jaundice, hepatitis are known.

From skin and hypodermic cellulose: often meeting – not heavy skin reactions (rash, an urtikariya); very seldom meeting – acute generalized ekzentematozny пустулёз, psoriazopodobny rashes or an exacerbation of psoriasis, loss of hair though relationship of cause and effect is not proved.

From a musculoskeletal system: often meeting – an arthralgia, a mialgiya.

General frustration: very seldom meeting – fatigue.

Interaction with other medicines:

In a blood plasma drugs which induce metabolism can increase clearance of a terbinafin and it can be lowered by drugs which inhibit P450 cytochrome. In case of need the accompanying therapy by such drugs Lamikon's dose has to be adjusted.

Rifampicin increases clearance of a terbinafin by 100%.

Results of the researches conducted by in vitro and on healthy volunteers show what тербинафин has the insignificant potential for oppression or strengthening of clearance of drugs which are metabolized with participation of system of P450 cytochrome (for example, a terfenadina, a triazolama, Tolbutamidum or oral contraceptives).

Terbinafin does not influence clearance of antipyrine or digoxin.

At patients who at the same time accepted тербинафин and peroral contraceptives, it was in certain cases observed an irregularity of a menstrual cycle though the frequency of these disturbances remained within sizes which were observed at the isolated use of oral contraceptives.

Terbinafin reduces clearance of caffeine which was entered intravenously, for 19%.

In the researches in vitro and in vivo it was revealed that тербинафин CYP2D6 – the mediated metabolism oppresses. These data can be clinically important for drugs which are metabolized by this enzyme, such as tricyclic antidepressants (TSAS), β-blockers, selective serotonin reuptake inhibitors (SSRIs), antiarrhytmic drugs (including a class 1A, 1B, and 1C) and monoamine oxidase inhibitors (MAO-Is) of type B in case drug which is used has the small range of therapeutic concentration.

Terbinafin reduces clearance of desipramine by 82% and increases clearance of cyclosporine by 15%.

Contraindications:

Hypersensitivity to a terbinafin or excipients of drug.

Overdose:

It is known of several cases of overdose (intake to 5 g of a terbinafin).

Symptoms: a headache, nausea, vomiting, pain in epigastriums and dizziness.

Treatment: gastric lavage, reception of absorbent carbon, and, if necessary, use of symptomatic therapy.

Use during pregnancy or feeding by a breast

 

Clinical experience of use of Lamikon for treatment of pregnant women is limited therefore during pregnancy drug can be used only in that case when the expected advantage for mother exceeds potential risk for a fruit.

Terbinafin gets into breast milk therefore in case of need uses of drug for the women nursing for treatment it is necessary to stop breastfeeding.

Children

 

Lamikon appoint to children 6 years with body weight more than 20 kg are more senior if the advantage of use, according to the doctor, exceeds potential risk.

Storage conditions:

Period of validity 2 years. Not to use drug after the termination of the period of validity specified on packaging. To store in protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 7 tablets in the blister. On 2 blisters enclosed in a pack.