Flucinar®

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

Composition:

Active substance: fluocinolone;

1 g of gel contains fluocinolone acetonide 0.25 mg;

Excipients: propylene glycol, ethanol 96%, disodium edetate, citric acid monohydrate, methylparaben (E 218), propylparaben (E 216), triethanolamine, carbomer, purified water.

Pharmaceutical form. Gel.

Main physico-chemical properties: colorless transparent gel with slight opalescence and the odor of ethyl alcohol.

Pharmacotherapeutic group. Corticosteroids for dermatological use.

ATC code D07AC04.

Pharmacological Properties.

Pharmacodynamics.

Fluocinolone acetonide is a highly active synthetic glucocorticoid for topical use. When applied as a 0.025% gel, it exerts a potent anti-inflammatory, antipruritic, anti-allergic, and vasoconstrictive effect. It possesses lipophilic properties and is readily absorbed through the skin. Already after application of 2 g of the gel, production of adrenocorticotropic hormone (ACTH) by the pituitary gland may be reduced due to suppression of the hypothalamic-pituitary-adrenal axis.

The mechanism of anti-inflammatory action of fluocinolone acetonide has not been fully elucidated. It is believed that this agent reduces inflammatory processes by inhibiting the production of prostaglandins and leukotrienes, resulting from decreased phospholipase A2 activity and release of arachidonic acid from cell membrane phospholipids. The anti-allergic effect is achieved by suppressing the development of local hypersensitivity reactions. Due to its local vasoconstrictive action, the risk of exudative reactions is reduced. It decreases protein synthesis and collagen deposition. It accelerates protein breakdown in the skin and suppresses proliferative processes.

Pharmacokinetics.

Absorption. Absorption of fluocinolone acetonide through the skin is enhanced when applied to sensitive skin areas, such as skin folds and the face, as well as to skin with damaged epidermis or existing inflammatory processes. Use of occlusive dressings increases skin temperature and moisture, which also enhances absorption of fluocinolone acetonide. In addition, absorption is increased with frequent application and over large skin areas. Skin absorption is higher in adolescents than in adults.

Biotransformation and elimination. Fluocinolone acetonide readily penetrates the stratum corneum of the skin, where it gradually accumulates and can still be detected 15 days after application. It is not biotransformed in the skin. After systemic absorption, it is primarily metabolized in the liver. It is excreted in urine and, to a lesser extent, in bile, mainly as conjugates with glucuronic acid, and also in small amounts unchanged.

Safety preclinical data.

Single-dose toxicity. Fluocinolone acetonide is intended for topical (external) use only. The toxicity of this compound after oral or parenteral administration has not been studied. It can be assumed that the toxicity after single administration of fluocinolone acetonide does not significantly differ from the toxicity of other fluorinated glucocorticosteroids.

Genotoxicity. No mutagenic effects of fluocinolone acetonide have been studied. However, tests have been conducted to evaluate the mutagenic potential of other glucocorticosteroids with a similar chemical structure. Fluticasone propionate was not mutagenic in the Ames test performed on Escherichia coli bacteria, in a gene conversion test conducted on Saccharomyces cerevisiae yeast, and in a mutagenicity test on Chinese hamster ovary cells. No mutagenic effects of fluticasone were observed in tests performed on human lymphocytes in vitro (in test tubes), nor clastogenic activity in the micronucleus test in mice.

Studies with hydrocortisone and prednisolone also did not show any mutagenic effects.

Carcinogenicity. There are no data indicating that topical application of glucocorticosteroids promotes the development of skin cancer in humans.

Toxic effects on reproductive function and offspring development. The effect of fluocinolone acetonide on fertility has not yet been fully studied. However, the effects of other glucocorticosteroids on fertility have been demonstrated.

Clinical characteristics.

Indications.

Short-term treatment of acute and severe non-infectious inflammatory skin diseases (without exudation) accompanied by persistent pruritus or hyperkeratosis and responsive to glucocorticoid therapy: seborrheic dermatitis, lichen urticatus, atopic dermatitis, allergic contact eczema, erythema multiforme, lupus erythematosus, psoriasis of hairy skin areas, advanced psoriasis, lichen planus.

Contraindications.

• Hypersensitivity to fluocinolone acetonide or other glucocorticosteroids or to any of the excipients of the medicinal product.
• Bacterial, viral, and fungal skin infections.
• Facial rosacea and common acne.
• Perioral dermatitis.
• Children under 2 years of age.

Interaction with other medicinal products and other forms of interaction.

No interactions have been observed with topical application of glucocorticosteroids.

Systemically acting glucocorticosteroid preparations enhance the efficacy of the medicinal product, but simultaneously increase the likelihood of adverse effects. Concomitant use with nonsteroidal anti-inflammatory drugs increases the risk of developing systemic and local adverse effects. Reduces the activity of antihypertensive, diuretic, antiarrhythmic, and potassium-containing medicinal products. Diuretic medicinal products (except potassium-sparing diuretics) increase the risk of developing hypokalemia.

Flucinar® gel may enhance the action of immunosuppressive agents and reduce the effect of immunostimulating medicinal products.

Special precautions for use.

The gel is particularly suitable for treating hairy skin and for patients who poorly tolerate the base of ointments and creams. The gel formulation allows application in small amounts, thus enabling lower doses of the drug to be used over large skin areas, as well as application to hairy areas of the body.

Do not use concomitantly with other topical medicinal products.

The drug should be discontinued in patients who develop symptoms of irritation, allergy (itching, burning, or redness), or superinfection.

Do not use the drug continuously for more than 2 weeks. Prolonged use over large skin areas increases the frequency of adverse effects and the risk of developing edema, arterial hypertension, hyperglycemia, and reduced resistance of the body.

Avoid contact of the drug with mucous membranes, application over large skin areas, use under occlusive dressings, and avoid use in children.

Due to the higher body surface area to body weight ratio in children compared to adults, there is an increased risk of systemic adverse effects from corticosteroids, including hypothalamic-pituitary-adrenal (HPA) axis suppression and induction of Cushing's syndrome. Corticosteroid treatment may impair growth and development in children.

With topical application of the drug, suppression of adrenocorticotropic hormone (ACTH) production by the pituitary due to suppression of the adrenal-pituitary axis, decreased blood cortisol levels, and development of iatrogenic Cushing's syndrome may occur; these effects are reversible upon discontinuation of the drug. During prolonged treatment, periodic monitoring of adrenal cortex function by measuring blood and urinary cortisol levels, as well as adrenal response to ACTH stimulation, is recommended.

If infection develops at the site of gel application, appropriate antibacterial or antifungal therapy should be initiated. If infection symptoms do not resolve, the drug should be discontinued during the treatment of the infection.

Avoid applying the drug to the eyelids or skin around the eyes in patients with closed-angle or open-angle glaucoma, as well as in patients with cataracts, due to the potential for worsening of disease symptoms.

Visual disturbances may occur with the use of systemic and topical corticosteroids.

If symptoms such as blurred vision or other visual disturbances occur, patients should consult an ophthalmologist to evaluate possible causes, which may include cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which has been reported with systemic and topical corticosteroid use.

Use on the face, axillae, and groin area should be limited to cases of special necessity, as increased absorption and a high risk of adverse effects (e.g., telangiectasia, perioral dermatitis) are possible, even after short-term use.

The drug should be used with caution in patients with subcutaneous tissue atrophy, particularly in elderly individuals.

During treatment, it is recommended to wear loose-fitting clothing. For skin conditions associated with infection, it is recommended to use the drug in combination with antimicrobial agents.

Do not apply on the skin of the breasts.

1 g of gel contains propylene glycol 150 mg, ethanol 150 mg, propyl parahydroxybenzoate 0.80 mg, and methyl parahydroxybenzoate 1.50 mg.

Parahydroxybenzoates may cause allergic reactions (possibly delayed).

Propylene glycol may cause skin irritation.

Use during pregnancy or breastfeeding.

The drug should not be used during pregnancy or breastfeeding.

Pregnancy. Data on the use of fluocinolone in pregnant women are lacking or limited.

Flucinar gel may be prescribed to pregnant women only if the benefit to the mother outweighs the potential risk to the fetus. This medicinal product should not be used during the first trimester of pregnancy.

Animal studies have shown that glucocorticosteroids have teratogenic effects, even at low oral doses. Teratogenic effects have also been observed in animals after topical application of potent corticosteroids. However, no studies on the teratogenic effects of topical fluocinolone acetonide during pregnancy in humans have been conducted.

Animal studies with other glucocorticosteroids have shown reproductive toxicity (see section "Preclinical safety data" above).

Breastfeeding. The decision whether to discontinue breastfeeding or discontinue Flucinar gel therapy should be made, taking into account the benefits of breastfeeding for the child and the benefits of therapy for the mother.

It is unknown to what extent fluocinolone acetonide or its metabolites are excreted in breast milk following topical use of the gel. Risk to newborns/infants cannot be excluded.

Fertility. There are no data on the effect of fluocinolone on human fertility (see section "Preclinical safety data" above).

Ability to affect reaction rate while driving or operating machinery.

The medicinal product has no effect or has negligible effect on the ability to drive or operate machinery.

Method of Administration and Dosage

Apply the gel in a thin layer to the affected skin area. Initially, apply the gel 2–3 times daily; after alleviation of acute inflammatory symptoms, reduce application to no more than 1–2 times daily. Treatment should not be continued continuously for longer than 2 weeks. Do not use on facial skin for longer than 1 week. During one week, no more than 15 g of gel (1 tube) is recommended.

If deeper penetration of the active substance is required, the gel may be gently rubbed into the skin at the application site. Do not apply the gel under occlusive dressings. Loose-fitting clothing is recommended during treatment.

Use with caution and under physician supervision in children aged 2 years and older, applying the product only once daily on a small skin area; do not apply to the child's facial skin.

Children

The drug is contraindicated in children under 2 years of age.

Overdose

Prolonged use over large skin areas may lead to overdose symptoms manifested by intensification of local adverse effects (edema, arterial hypertension, hyperglycemia, decreased immunity, glucosuria), and in severe cases, development of Cushing's syndrome. In case of overdose, discontinue the drug or switch to corticosteroids with weaker potency.

Adverse reactions.

The adverse reactions of the medicinal product listed below are classified by organ systems according to MedDRA [Medical Dictionary for Regulatory Activities]. The frequency of adverse reactions is defined as follows: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1,000, <1/100); rare (≥1/10,000, <1/1,000); very rare (<1/10,000); not known (frequency cannot be estimated from available data).

Due to the absorption of individual active substances into the blood, systemic adverse effects of fluocinolone acetonide are also possible. These occur predominantly during prolonged use of the medicinal product, application over a large body surface area, under occlusive dressing, or when used in children.

Systemic adverse effects of fluocinolone acetonide, typical for corticosteroids in general, include: suppression of the hypothalamic-pituitary-adrenal (HPA) axis function, Cushing's syndrome, growth suppression and impaired development in children, hyperglycemia, glucosuria, hypertension, and decreased immunity.

This enables monitoring of the benefit-risk balance when using this medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua/.

Shelf life. 3 years.

Storage conditions. Store at a temperature not exceeding 25 °C. Do not freeze. Keep out of reach of children.

Packaging. 15 g in a tube; 1 tube per carton.

Prescription status. Prescription-only.

Manufacturer. Jelfa Pharmaceutical Plant A. T.

Manufacturer's address and place of business.
58-500 Jelenia Góra, ul. Wincentego Pola 21, Poland.