Lamisil 250 mg Tablets

Brand name

The drug is known under the trade name Lamisil. This designation is officially registered in pharmaceutical registries and is used to identify the drug in pharmacies, medical institutions and among health care professionals. The name Lamisil has become widely recognized due to its effectiveness in combating fungal infections that require specialized antifungal action. It was chosen by the manufacturers to emphasize the unique properties of the drug and to distinguish it from other products intended for the treatment of similar conditions.

International Nonproprietary Name (INN)

The international nonproprietary name of this medication is terbinafine. This term is accepted by the international community and is used to designate the active substance that provides therapeutic action. Terbinafine belongs to the class of allylamines, known for their ability to effectively inhibit the growth and reproduction of fungi. The name is standardized by the World Health Organization, which allows to unify the prescription and production of this drug in different countries and regions, regardless of brands.

Form of release

The drug is presented in several forms, which makes it convenient for use depending on the localization and nature of the fungal lesion. The main options include:

• Tablets with a dosage of 250 mg of the active ingredient, intended for oral administration by adults and older children
• Cream with a concentration of 1% (10 mg/g), used for external application to affected skin areas.
• Spray with a concentration of 1%, used for skin treatment in hard-to-reach areas.
• Gel with a concentration of 1%, suitable for the treatment of cutaneous fungal infections with marked inflammation.

Each form is tailored to the specific application: tablets are effective for systemic infections such as onychomycosis, while the cream, spray and gel are designed for localized treatment of skin and superficial lesions. The choice of form is determined by the doctor based on the diagnosis and the extent of infection.

Composition

The main active ingredient is terbinafine, an antifungal agent from the group of allylamines. Auxiliary components depend on the form of release. In tablets, the following are used:

• Microcrystalline cellulose - an excipient that provides uniform distribution of the active substance.
• Corn starch - a binder for the formation of the mass.
• Magnesium stearate - a lubricating agent that facilitates the manufacturing process.
• Croscarmellose sodium - disintegrant to accelerate the disintegration of the tablet.
• Silicon dioxide - stabilizer to prevent caking.

The cream contains cetyl alcohol and stearyl alcohol as a base, propylene glycol for moisturizing, benzyl alcohol as a preservative and purified water. The spray includes ethanol as a solvent and the gel includes carbomer as a thickener and isopropanol. The composition of each form is balanced to ensure stability and maximize efficacy during application.

Pharmacologic Properties

Pharmacodynamics

Lamisil has a pronounced fungicidal action aimed at the destruction of fungal cells. It inhibits the enzyme squalene epoxidase in the membranes of fungi, which disrupts the synthesis of ergosterol - a key component of their cell wall. This leads to the accumulation of squalene inside the cell, causing its damage and death. The drug is effective against a wide range of dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast fungi (Candida spp.) and some mold fungi (Aspergillus spp.).

The mechanism of action allows the drug not only to destroy fungi, but also to prevent their further multiplication, which is especially important in chronic infections. When applied topically, Lamisil creates a high concentration in the skin and nails, providing a long-lasting effect. When used systemically, it targets deep and widespread lesions such as onychomycosis.

Pharmacokinetics

Absorption

After oral administration, the active ingredient is absorbed in the gastrointestinal tract, reaching maximum plasma concentration in 1.5-2 hours. Bioavailability is about 70-80% due to the effect of the first passage through the liver. Food intake insignificantly affects absorption, which allows taking tablets independently of meals. When applied topically (cream, spray, gel) absorption through the skin is minimal - less than 5% of the dose enters the systemic bloodstream, which provides local action.

Distribution

The component is well distributed in the body, penetrating the skin, nails, hair and subcutaneous tissue. Binding to plasma proteins reaches 99%, which contributes to the long-term retention of the substance in tissues. After oral administration, the concentration in the skin and nails significantly exceeds the minimum inhibitory concentration for most fungi, which makes the drug effective in systemic infections.

Metabolism

Metabolism occurs in the liver with the participation of cytochrome P450 enzymes (mainly CYP2C9, CYP1A2, CYP3A4). Inactive metabolites such as carboxy-terbinafine and N-desmethyl-terbinafine are formed, which have no antifungal activity. About 70-80% of the administered dose undergoes metabolic transformations.

Excretion

Excretion is mainly through the kidneys (about 70% in the form of metabolites) and partially with bile and feces. The elimination half-life from plasma is 17-36 hours, but from skin and nails - up to several weeks, which provides prolonged effect. When applied topically, excretion of systemic residues is minimal.

Indications for Use

Lamisil is prescribed for the treatment of fungal infections caused by sensitive microorganisms:

• Onychomycosis (fungal lesions of the nails) caused by dermatophytes.
• Mycoses of the skin: dermatophytosis of the feet, inguinal epidermophytosis, trichophytosis of smooth skin.
• Candidosis of the skin and mucous membranes (with systemic use).
• Different colored lichen caused by Malassezia spp. (when applied topically).

Pills are used for widespread and deep infections, whereas cream, spray, and gel are effective for superficial lesions. Prescribing requires confirmation of the fungal nature of the disease.

Contraindications

The use of Lamisil is prohibited in:

• Hypersensitivity to terbinafine or components of the composition.
• Severe hepatic insufficiency (active hepatitis, cirrhosis).
• Severe renal failure (creatinine clearance less than 30 ml/min).
• Children under 2 years of age (for tablets).

Cautious use in psoriasis, systemic lupus erythematosus and alcoholism.

Method of Administration and Dosage

How to take

Lamisil tablets are taken orally, drinking water (150-200 ml), preferably with food to reduce gastric irritation. Cream, spray or gel is applied in a thin layer to clean and dry skin, gently rubbing into the affected areas and adjacent areas. Before applying external forms, it is recommended to avoid contact with water for several hours after application.

Dosages for adults and children

Dosage depends on the form and localization of infection:

• Adults (tablets): 250 mg once a day; the course for onychomycosis - 6-12 weeks, for mycoses of the skin - 2-4 weeks.
• Children over 2 years of age (tablets): 125 mg (body weight 20-40 kg) or 250 mg (more than 40 kg) 1 time a day, the course is determined by a doctor.
• Externally (cream, spray, gel): 1-2 times a day, course 1-2 weeks for dermatophytosis, 2-4 weeks for candidiasis.

Dose adjustment in certain conditions

With renal failure:

• Clearance 30-50 ml/min: 125 mg once daily.
• Clearance less than 30 ml/min: use contraindicated.

In hepatic impairment, the dose is reduced to 125 mg daily or avoid use in severe impairment.

Side Effects

Unwanted reactions include:

• Gastrointestinal: nausea, diarrhea, abdominal pain, decreased appetite.
• Skin: rash, itching, rare: toxic epidermal necrolysis.
• hepatic: increase in transaminases, hepatitis (rare).
• Nervous: headache, dizziness, taste changes.
• Hematologic: neutropenia, thrombocytopenia (rare).

Treatment should be discontinued if symptoms are severe.

Overdose

Symptoms of overdose

Exceeding the dose of Lamisil causes nausea, vomiting, dizziness, pain in the epigastrium, rarely - convulsions.

First aid measures

In overdose:

• Stop taking it.
• Rinse the stomach (within 1-2 hours).
• Take activated charcoal.
• Seek medical attention.

Drug Interactions

Influence on the effects of other drugs

The medication affects:

• Cyclosporine: decrease in blood concentrations.
• Antidepressants (tricyclic): increase in their levels.
• Rifampicin: acceleration of terbinafine excretion.

Compatibility with alcohol and food

Alcohol increases the risk of hepatic impairment and is avoided. Food does not affect absorption.

Special Precautions

Use in pregnancy and breastfeeding

Lamisil is contraindicated in pregnancy (category B) and lactation due to insufficient safety data.

Effects on driving and operating machinery

Dizziness may make it difficult to drive or operate machinery.

Particulars of Use in the Elderly and Children

In the elderly, monitoring of liver and renal function is required. In children under 2 years of age tablets are not used, external forms are allowed with caution.