Lamisil, pills 250mg, 14pcs

Composition

1 tablet contains:

Active ingredient:

terbinafine (in the form of hydrochloride)250 mg;

Auxiliary substances:

magnesium stearate;

colloidal anhydrous silicon dioxide;

methylhydroxypropylcellulose;

sodium glycolate starch;

MCC.

Pharmacological action

LAMIZIL-broad-spectrum antifungal, fungistatic, fungicidal.

Pharmacodynamics

Terbinafine is an allylamine that has a broad spectrum of action against fungi that cause diseases of the skin, hair and nails, including dermatophytes such as Trichophyton (for example, T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum (for example, M. canis), Epidermophyton floccosum, as well as yeast fungi of the genus Candida(for example, C. albicans) and Pityrosporum. In low concentrations, terbinafine has a fungicidal effect against dermatophytes, mold and some dimorphic fungi. Activity against yeast fungi, depending on their type, can be fungicidal or fungistatic.

Terbinafine specifically inhibits the early stage of sterol biosynthesis in the fungal cell. This leads to ergosterol deficiency and intracellular squalene accumulation, which causes fungal cell death. The action of terbinafine is carried out by inhibiting the enzyme squalene oxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system.

When prescribing the drug Lamizil® inside, concentrations of the drug are created in the skin, hair and nails, providing a fungicidal effect.

Pharmacokinetics

After oral use, terbinafine is well absorbed (>70%); the absolute bioavailability of terbinafine due to the first-pass effect is approximately 50%. After a single oral dose of 250 mg of terbinafine, its Cmax in plasma is reached in 1.5 hours and is 1.3 mcg / ml. With constant terbinafine intake, its Cmax increased by an average of 25%, compared with a single dose; AUC increased by 2.3 times. Based on the increase in AUC, the effective T1/2 — 30 h can be calculated. Food intake slightly affects the bioavailability of the drug (AUC increases by less than 20%), so no dose adjustment of Lamizil® is required when taken simultaneously with food.

Terbinafine is largely bound to plasma proteins (99%). It quickly penetrates the dermal layer of the skin and concentrates in the lipophilic stratum corneum. Terbinafine also penetrates the secret of the sebaceous glands, which leads to the creation of high concentrations in hair follicles, hair and in the skin rich in sebaceous glands. It is also shown that terbinafine penetrates the nail plates in the first few weeks after the start of therapy.

Terbinafine is metabolized rapidly and significantly with the participation of at least 7 cytochrome P 450 isoenzymes, with the main role played by the isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. As a result of biotransformation of terbinafine, metabolites are formed that do not have antifungal activity and are mainly excreted in the urine.

There were no changes in the steady-state concentration of terbinafine in plasma depending on age.

In pharmacokinetic studies of a single dose of Lamizil® in patients with concomitant renal impairment (creatinine clearance

Indications

• onychomycosis caused by fungi dermatophytes;
• mycoses of the scalp;
• fungal infections of the skin-treatment of dermatomycosis of the trunk, legs, feet, as well as yeast infections of the skin caused by fungi of the genus Candida (for example, Candida albicans) — in cases where the localization, severity or prevalence of infection makes oral therapy advisable.

Note:  unlike Lamizil ® for topical use, Lamizil® for oral use is not effective in multi-colored lichen.

Contraindications

Hypersensitivity to terbinafine or any other ingredient of the drug.

Side effects

From the hematopoietic system:  very rarely — neutropenia, agranulocytosis, pancytopenia. In very rare cases, when using the drug, the development of qualitative or quantitative changes in the formed blood elements (neutropenia, agranulocytosis, thrombocytopenia, pancytopenia) was noted. If there are qualitative or quantitative changes in the blood cells, the cause of the disorders should be determined and consideration should be given to reducing the dose of the drug or, if necessary, discontinuing Lamizil®therapy.

From the immune system:  very rarely — anaphylactoid reactions (including angioedema), cutaneous and systemic lupus erythematosus.

Nervous system disorders:  often-headache; sometimes – disturbances of taste sensations, including their loss (usually recovery occurs within a few weeks after discontinuation of treatment); very rarely — dizziness, paresthesia, hypesthesia. There are isolated reports of cases of prolonged taste disturbances. In some cases, while taking the drug, there was a decrease in food intake, which led to a significant reduction in weight.

From the side of the hepatobiliary system:  rarely — hepatobiliary dysfunction (mainly of a cholestatic nature), including very rare cases of severe liver failure (some fatal or requiring liver transplantation). In most cases where hepatic insufficiency developed, patients had serious concomitant systemic diseases and a causal relationship of hepatic insufficiency with taking Lamizil® it was questionable.

From the digestive system:  very often — a feeling of fullness of the stomach, loss of appetite, dyspepsia, nausea, mild abdominal pain, diarrhea.

Skin and subcutaneous tissue disorders:  very often-mild skin reactions (rash, urticaria); very rarely — serious skin reactions (including Stevens-Johnson syndrome, toxic epidermal necrolysis); psoriasis-like skin rashes or exacerbations of psoriasis. Very rarely, there were cases of hair loss, although the causal relationship of this phenomenon with taking the drug has not been established. If a progressive skin rash develops, treatment should be discontinued.

Musculoskeletal disorders:  very often — arthralgia, myalgia.

Other services:  very rarely — feeling tired.

Interaction

The effect of other drugs on terbinafine. Plasma Cl of terbinafine can be accelerated under the influence of drugs that induce metabolism, and suppressed under the influence of cytochrome P450 inhibitors. If necessary, the simultaneous use of the above drugs and the drug Lamizil® appropriate adjustment of the latter’s dosage regimen may be required.

Cimetidine may enhance the effect of terbinafine or increase its plasma concentration. Cimetidine reduces the Cl of terbinafine by 33%.

Rifampicin may weaken the effect of terbinafine or reduce its plasma concentration. Rifampicin increases the Cl of terbinafine by 100%.

The effect of terbinafine on other drugs. The results of studies conducted in vitro and in healthy volunteers show that terbinafine has little potential to inhibit or enhance the Cl of most drugs that are metabolized with the participation of the cytochrome p450 system (for example, terfenadine, triazolam, tolbutamide or oral contraceptives), with the exception of those that are metabolized with the participation of CYP2D6.

Terbinafine does not affect the Cl of antipyrine or digoxin.

Several cases of menstrual irregularities have been reported in patients treated with Lamizil® in combination with oral contraceptives, although the frequency of these disorders does not exceed the average frequency of such disorders in patients taking oral contraceptives only.

Terbinafine may enhance the effect of caffeine or increase its plasma concentration. Terbinafine reduces the Cl of caffeine when administered intravenously by 19%.

In vivo and in vitro studies have shown that terbinafine inhibits metabolism mediated by the enzyme 2D6 (CYP2D6). These data may be clinically relevant for those drugs that are primarily metabolized by this enzyme: tricyclic antidepressants, beta-blockers, selective serotonin reuptake inhibitors, class 1A,1B, and 1C antiarrhythmic drugs, and type B MAO inhibitors — if the drug used simultaneously has a small therapeutic concentration range.

Terbinafine reduces the Cl of desipramine by 82%.

Terbinafine may weaken the effect of cyclosporine and reduce its plasma concentration. Terbinafine increases cyclosporine Cl by 15%.

How to take it, course of use and dosage

Inside.

The duration of treatment depends on the indication and severity of the disease.

Children

Data on the use of the drug in children under 2 years of age (whose body weight is usually less than 12 kg) are not available.

The drug is prescribed 1 time a day. A single dose depends on body weight and is: for children with a body weight of less than 20 kg-62.5 mg; from 20 to 40 kg-125 mg; more than 40 kg-250 mg. In children over 2 years of age, the oral tolerability of Lamizil® is good.

Adults

The recommended dose is 250 mg once a day.

Skin infections

Recommended duration of treatment: dermatomycosis of the feet (interdigital, plantar or sock-like) – 2-6 weeks; dermatomycosis of the trunk, legs-2-4 weeks; candidiasis of the skin-2-4 weeks.

Complete disappearance of infection symptoms and complaints associated with it may occur no earlier than a few weeks after mycological treatment.

Infections of the hair and scalp

Recommended duration of treatment: mycosis of the scalp-4 weeks. Mycoses of the scalp are observed mainly in children.

Onychomycosis

The duration of treatment in most patients is from 6 to 12 weeks. In most cases,6 weeks of treatment is sufficient for onychomycosis of the hands. With onychomycosis of the feet, in most cases,12 weeks of treatment is sufficient. Some patients who have a reduced rate of nail growth may require longer treatment. The optimal clinical effect is observed several months after mycological treatment and discontinuation of therapy. This is determined by the time period that is necessary for the growth of a healthy nail.

Use in the elderly. There is no reason to assume that the elderly need to change the dosage regimen of the drug or that they have side effects that differ from those in younger patients. If the drug is used in tablets in this age group, the possibility of concomitant liver or kidney dysfunction should be taken into account.

Overdose

Symptoms: several cases of overdose (up to 5 g of the drug taken) have been reported, with headache, nausea, epigastric pain and dizziness.

Treatment: symptomatic and supportive therapy, measures to remove the drug, primarily by prescribing activated charcoal and gastric lavage.

Form of production

Tablets

Storage conditions

In a dark place, at a temperature not exceeding 30 °C

Shelf life

5 years

Active ingredient

Terbinafine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets