Estefin®

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT ESTESIFIN® (ESTESIFIN)

Composition:

Active ingredient: naftifine hydrochloride;

1 g of cream contains naftifine hydrochloride equivalent to 10 mg of 100 % dry substance;

Excipients: isopropyl myristate, cetyl stearyl alcohol, cetyl palmitate, sorbitan laurate, polysorbate 60, benzyl alcohol, sodium hydroxide, purified water.

Pharmaceutical form. Cream.

Main physicochemical properties: white, soft or slightly cheesy lustrous cream with a slight characteristic odor.

Pharmacotherapeutic group.

Antifungal agents for dermatological use. ATC code D01A E22.

Pharmacological properties.

Pharmacodynamics.

Estefin® is an antifungal agent of the allylamine class. Its active ingredient is naftifine hydrochloride, whose mechanism of action is associated with inhibition of ergosterol synthesis.

Naftifine is active against dermatophytes such as Trichophyton, Epidermophyton, and Microsporum, as well as against yeasts (Candida), molds (Aspergillus), and other fungi (e.g., Sporothrix schenckii). Against dermatophytes and Aspergillus species, naftifine exerts a fungicidal effect in vitro; against yeast fungi, it demonstrates either fungicidal or fungistatic activity depending on the microbial strain.

Estefin® also exhibits antibacterial activity against gram-positive and gram-negative microorganisms that may cause secondary bacterial infections accompanying mycotic lesions.

In addition, Estefin® has anti-inflammatory properties, which contribute to rapid relief of inflammatory symptoms and itching.

Pharmacokinetics.

Naftifine hydrochloride is rapidly absorbed and achieves sustained antifungal concentrations in various layers of the skin. Approximately 4% of the applied dose is absorbed through the skin, resulting in very low systemic exposure. Only trace amounts of naftifine are detectable in blood plasma and urine. The active substance is almost completely metabolized; metabolites lack antifungal activity and are excreted in feces and urine. The elimination half-life is 2–4 days.

Clinical characteristics.

Indications.

Topical treatment of fungal infections caused by pathogens sensitive to naftifine:

• fungal infections of the skin and skin folds;
• interdigital mycoses;
• fungal infections of the nails (onychomycoses);
• cutaneous candidiasis;
• pityriasis versicolor;
• inflammatory dermatomycoses, with or without pruritus.

Contraindications.

Hypersensitivity to naftifine or to any of the excipients of the product. The product must not be applied to wound surfaces. Do not use for treatment of the eyes.

Interaction with other medicinal products and other forms of interaction.

Studies on interactions have not been conducted.

Special precautions for use.

The medicinal product should be used only topically for the treatment of nail and skin disorders!

The medicinal product contains cetyl stearyl alcohol, which may cause local skin reactions (e.g. contact dermatitis).

Use during pregnancy or breastfeeding.

Data on the use of naftifine in pregnant women are lacking or limited. Animal studies do not indicate any direct or indirect harmful effects of the drug on reproductive function. The product may be used during pregnancy or breastfeeding only if clearly necessary, following a careful assessment of the benefit-risk ratio determined by the physician.

Breastfeeding mothers should avoid contact of the medicinal product with the infant's skin and gastrointestinal tract.

Ability to affect reaction rate when driving or operating machinery.

No effect.

Method of Administration and Dosage.

Estefin® cream should be applied to the affected skin area and adjacent regions once daily after thorough cleansing and drying of the skin, extending approximately 1 cm beyond the lesion border to include healthy skin.

Duration of treatment:
For dermatomycoses – 2–4 weeks (if necessary, up to 8 weeks);
For candidiasis – 4 weeks;
For nail infections – up to 6 months.

For fungal nail infections, the drug is recommended to be applied twice daily. Prior to the first application, the affected portion of the nail should be trimmed as much as possible using scissors or a nail file (to facilitate this procedure, nails may be softened with a special softening agent as advised by a physician).

To prevent relapses, treatment with the drug should be continued for at least 2 weeks after the main symptoms have disappeared.

Children. There is insufficient data on the efficacy and safety of the drug in children; therefore, Estefin® is not recommended for use in this age group.

Overdose.

Acute overdose with topical application of naftifine has not been reported.

Systemic intoxication is unlikely with topical use, as the amount of active substance absorbed through the skin is minimal.

In case of accidental ingestion, symptomatic treatment should be initiated.

Side effects.

The frequency of side effects is defined as follows: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (< 1/10000), frequency not known (cannot be estimated from the available data).

General disorders: frequency not known – local reactions may occur in isolated cases: dry skin, redness and burning sensation, itching, local irritation.

Skin and subcutaneous tissue disorders with frequency "not known": contact dermatitis and erythema.

Shelf life.

3 years.

Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 30 ºC.

Keep out of reach of children.

Packaging.

15 g in a tube. 1 tube per carton.

Supply category.

Over-the-counter.

Manufacturer.

JSC "Farmak".

Manufacturer's address and place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.