Loceryl

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT LOCERYL® (LOCERYL®)

Composition:

Active substance: amorolfine;

1 ml of the preparation contains amorolfine hydrochloride equivalent to 50 mg of amorolfine;

Excipients: ammonium methacrylate copolymer (type A), butyl acetate, anhydrous ethanol, ethyl acetate, glycerol triacetate.

Pharmaceutical form. Therapeutic nail lacquer.

Main physicochemical properties: clear liquid, colorless to almost colorless.

Pharmacotherapeutic group.

Other antifungal agents for topical use. ATC code D01AE16.

Pharmacological Properties

Pharmacodynamics

Loceryl® 5% nail lacquer (50 mg/mL) is an antifungal agent for topical use. Amorolfine belongs to a new class of chemical compounds; its fungicidal action is based on altering the fungal cell membrane, primarily through its effect on sterol biosynthesis. The content of ergosterol decreases, while at the same time atypical, non-planar sterol intermediates accumulate. This leads to morphological changes in cellular membranes and organelles, resulting in fungal cell death.

Amorolfine is a broad-spectrum antifungal agent. It is highly active against common or occasional causative agents of onychomycosis, including:

Yeast fungi: Candida albicans and other Candida species;

Dermatophytes: Trichophyton rubrum, Trichophyton interdigitale, and Trichophyton mentagrophytes, other Trichophyton species; Epidermophyton floccosum; Microsporum;

Mould fungi: Scopulariopsis;

Dematiaceous (dark) fungi: Hendersonula, Alternaria, Cladosporium;

Species with lower sensitivity: Aspergillus, Fusarium, Mucorales.

Pharmacokinetics

Amorolfine contained in the nail lacquer penetrates into the nail plate and diffuses through it, thus being able to eradicate fungi located in the nail bed that are otherwise difficult to reach. Systemic absorption of the active substance following this mode of application is very low, and its plasma concentration remains below the limit of detection even after one year of use.

Clinical characteristics.

Indications.

For the treatment of onychomycosis without involvement of the nail matrix (onychostroma) as first-line therapy.

Contraindications.

Hypersensitivity to the active substance or to any of the excipients.

Interaction with other medicinal products and other forms of interactions.

Current available data do not indicate the presence of clinically significant interactions.

Special precautions for use

Loceryl® should not be applied to the skin surrounding the nail. Avoid contact of the nail lacquer with eyes, ears, and mucous membranes.

Loceryl® should be used with caution in patients with conditions that predispose them to nail damage (peripheral circulatory disorders, diabetes mellitus, and immunosuppression), as well as in patients with nail dystrophy or severely damaged nails (more than two-thirds of the nail plate destroyed). In such cases, systemic treatment should be considered.

Do not use artificial nails during treatment with Loceryl® nail lacquer.

When working with organic solvents, wear impermeable gloves to prevent dissolution of the lacquer. Cosmetic nail polish may be applied no sooner than 10 minutes after application of Loceryl®. Before reapplying Loceryl®, cosmetic nail polish must be carefully removed.

Systemic or local allergic reactions may occur after using this medicinal product. In such cases, treatment with the lacquer should be discontinued immediately and medical advice sought. The product should be thoroughly removed using a nail polish remover. The medicinal product must not be used again.

This medicinal product contains 552 mg of alcohol (ethanol) per 1 g, equivalent to 55.2% w/w. This may cause a burning sensation on damaged skin. Ethanol is highly flammable; therefore, this product should not be used near open flames, lit cigarettes, or certain devices (e.g., hair dryers).

Use during pregnancy or breastfeeding

There is limited data on the use of amorolfine during pregnancy and breastfeeding. Post-marketing reports include only a small number of pregnant women using topical amorolfine; therefore, the potential risk is unknown. Animal studies have shown reproductive toxicity when the drug was administered at high oral doses.

It is unknown whether amorolfine passes into breast milk.

Loceryl® should not be used during pregnancy and breastfeeding, except in cases of unequivocal necessity.

Effect on ability to drive and use machines

No effect.

Method of administration and dosage.

Apply Loceryl® nail lacquer to affected nails once or twice a week.

The following recommendations should be carefully observed when applying the lacquer:

• Before the first application of Loceryl® nail lacquer, the nails should be thoroughly and carefully cleaned, taking care to avoid contact with the surrounding skin. Affected areas of the nails (particularly the nail surface) should be filed as meticulously as possible. The nail surface should be cleaned and degreased using a swab or wipe moistened with a nail polish remover.
• Using one of the reusable spatulas, apply the lacquer evenly over the entire surface of the affected nail. The reusable spatula should be cleaned each time when moving from one nail to another to prevent contamination of the lacquer. The spatula should be dipped into the lacquer and removed from the bottle without wiping off excess lacquer against the neck of the bottle.
• It is important to clean the reusable spatula with a swab or wipe moistened with nail polish remover after each application, before reusing it on another nail, to avoid contamination of the lacquer.
• If the lacquer has been applied to the outer surface of the cap during use, it is important to clean it with a swab or wipe moistened with nail polish remover to prevent skin contact. The bottle should always be kept tightly closed.

Repeat all the above steps for each affected nail.

Cosmetic nail polish may be applied no sooner than 10 minutes after application of Loceryl® nail lacquer. Treatment should continue without interruption until complete nail renewal and full clinical and mycological healing of affected areas.

The duration of treatment is generally 6 months for fingernails and 9 months for toenails (this primarily depends on the severity of infection, its location, and the extent of nail involvement).

Special recommendations:

• Do not reuse files used for filing infected nails to file healthy nails.
• Before each new application, if necessary, affected nails should be filed and in all cases cleaned with a nail polish remover to remove residual lacquer.
• When working with organic solvents (e.g., white spirit, thinners, etc.), impermeable gloves should be worn to protect nails coated with Loceryl® nail lacquer.

Children.

Due to lack of data, the use of Loceryl® nail lacquer is not recommended in patients under 18 years of age.

Overdose.

Isolated cases of adverse reactions may occur. Nail disorders such as nail discoloration and nail brittleness are possible. Such reactions may also be associated with onychomycosis.

No systemic signs of overdose are expected following topical application of Loceryl® nail lacquer. In case of accidental oral ingestion, appropriate symptomatic treatment should be administered.

Adverse reactions.

* Adverse reactions reported since the product was marketed.

Shelf life. 3 years.

After first opening of the vial, the product is suitable for use within 6 months.

Storage conditions.

Store in the original packaging, out of the reach of children, at a temperature not exceeding 30 °C.

Packaging.

1.25 ml or 2.5 ml or 5 ml in a dark glass vial; 1 vial (together with 30 cleansing swabs, 10 spatulas and 30 nail files) in a cardboard box;

1.25 ml or 2.5 ml or 5 ml in a dark glass vial with an applicator cap; 1 vial (together with 30 cleansing swabs and 30 nail files) in a cardboard box.

Classification.

Over-the-counter (without prescription).

Manufacturer.

GALDERMA LABORATORIES.

Manufacturer's address and location of operations.

ZI Mondazir, 74540 ALBI-SUR-CHERAN, France.