Locoid creme

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT LOCOID CRELO

Composition:

Active substance: hydrocortisone 17-butyrate;

1 g of emulsion contains 1 mg of hydrocortisone 17-butyrate;

Excipients: cetyl stearyl alcohol, macrogol cetostearyl ether, white soft paraffin, paraffin, borage oil, propylene glycol, butylhydroxytoluene (E 321), propylparahydroxybenzoate (E 216), butylparahydroxybenzoate, sodium citrate, citric acid anhydrous, purified water.

Pharmaceutical form. Cutaneous emulsion.

Main physicochemical properties: almost white emulsion.

Pharmacotherapeutic group. Corticosteroids for dermatological use.

ATC code: D07AB02.

Pharmacological Properties

Pharmacodynamics

Hydrocortisone 17-butyrate is an active synthetic non-halogenated corticosteroid intended for topical use. It exerts anti-inflammatory, anti-edematous, and antipruritic effects. Its efficacy is comparable to that of halogenated steroids. When used at recommended doses, it does not cause suppression of the hypothalamic-pituitary-adrenal (HPA) axis. Although prolonged use of large doses, particularly under occlusive dressings, may lead to increased plasma cortisol levels, the responsiveness of the pituitary-adrenal system remains unaffected, and cortisol production normalizes after discontinuation of the drug.

The uniqueness of the Lokoid Creme formulation lies in its buffered oil-in-water emulsion, which enables the application of the preparation for the treatment of weeping lesions on exposed skin areas and lesions of the scalp.

Pharmacokinetics

Absorption: After topical application, the active substance accumulates in the epidermis, predominantly in the stratum granulosum.

Metabolism: Hydrocortisone 17-butyrate, absorbed through the skin, is metabolized to hydrocortisone and other metabolites directly within the epidermis and subsequently in the liver.

Elimination: Metabolites and a minor portion of unchanged hydrocortisone 17-butyrate are excreted in urine and feces.

Clinical characteristics.

Indications.

Conditions that respond to treatment with topical corticosteroids (e.g., eczema, dermatitis, psoriasis). Topical corticosteroids are generally not indicated for the treatment of psoriasis, but may be acceptable except for widespread plaque psoriasis, provided that precautions are observed (see section "Special precautions for use").

Contraindications.

Except in cases of treatment in combination with appropriate chemotherapeutic agents:

• Skin lesions (wounds) caused by bacterial infections (e.g., pyoderma, syphilitic or tuberculous lesions), viral infections (e.g., varicella, herpes simplex, herpes zoster, common warts, flat warts, genital warts, molluscum contagiosum); infections caused by fungi and yeasts; parasitic infections (e.g., scabies);
• ulcerative skin lesions;
• adverse reactions caused by corticosteroids (e.g., perioral dermatitis, striae);
• ichthyosis, juvenile plantar dermatosis, acne vulgaris, rosacea, skin capillary fragility, skin atrophy;
• hypersensitivity allergic reactions to components of the drug or to corticosteroids (the latter are rare);
• skin neoplasms.

Interaction with other medicinal products and other forms of interaction.

Interaction studies have not been conducted.

Special precautions for use.

Systemic adverse reactions with topical corticosteroids in adults are extremely rare but may be serious, particularly adrenal cortical suppression with prolonged use of the drug.

Risk of systemic effects is increased in the following cases:

• application over large skin areas, especially when using occlusive dressings or application to skin folds;
• prolonged treatment;
• use in children (due to thinner skin and relatively larger body surface area);
• presence of components or excipients that enhance penetration through the stratum corneum and/or potentiate the effect of the active substance (e.g. propylene glycol).

Risk of local adverse reactions increases with the potency of the drug and duration of treatment. Use with occlusive dressings or application to skin folds further increases this risk. Facial skin, scalp, and genital areas are particularly susceptible to adverse reactions. Inappropriate use, as well as presence of bacterial, parasitic, fungal, or viral infections, may mask and/or exacerbate manifestations of these diseases.

The ointment should not be applied to the eyelids due to the possibility of contact with the conjunctiva and increased risk of developing common glaucoma or subcapsular cataract.

Topical corticosteroids may be hazardous in patients with psoriasis for several reasons, including rebound syndrome due to development of tolerance, risk of generalized pustular psoriasis, or local and systemic toxic effects resulting from impaired skin barrier function. Steroids may be used in cases of scalp psoriasis or chronic plaque psoriasis of hands and feet. Careful monitoring of patients is essential.

Children, including infants. Adverse effects may occur in infants with excessive use. Particular caution is required in dermatoses of infants, especially diaper dermatitis. In such patients, treatment course should generally not exceed 7 days.

Adrenal cortex suppression (Cushing's syndrome) may develop rapidly in children. Suppression of growth hormone production and intracranial hypertension may also occur. Signs of intracranial hypertension include bulging fontanelle, headache, and bilateral optic disc swelling. If long-term treatment is necessary, regular monitoring of the child's height and body weight, as well as plasma cortisol levels, is advisable.

In comparative studies, no significant differences in adrenal cortical function were observed in children treated with Locoid Crelo or 1% hydrocortisone at doses of 30–60 grams per week for 4 weeks.

Excipients contained in the medicinal product.

Cetostearyl alcohol and butylated hydroxytoluene may cause local skin reactions (e.g. contact dermatitis). Propylene glycol may cause skin irritation. Butylated hydroxytoluene may cause eye and mucous membrane irritation (e.g. nasal mucosa). Propyl- and butylparahydroxybenzoates may cause delayed allergic reactions.

Use during pregnancy or breastfeeding.

Pregnancy. Data on the use of hydrocortisone butyrate in pregnant women are lacking or limited. Animal studies indicate reproductive toxicity of the drug. Corticosteroids cross the placenta. Systemic administration of high doses of corticosteroids has been associated with effects on the fetus or newborn (fetal growth retardation, adrenal cortical suppression).

Despite limited information on topical use of corticosteroids during pregnancy, and considering the low systemic absorption of drugs in this class, short-term use of weak and moderate potency corticosteroids (class 1 and class 2), such as hydrocortisone, on limited skin areas may be considered. However, the aforementioned effects cannot be excluded with prolonged use or application over large skin areas. Such use should only be undertaken when specifically indicated.

Breastfeeding. Hydrocortisone butyrate/metabolites pass into breast milk; however, when Locoid Crelo is used at therapeutic doses, no effect on breastfed newborns/infants is expected. Locoid Crelo may be used in breastfeeding women only for short-term treatment and on small skin areas. Breastfeeding should be discontinued during long-term treatment or when applying the drug to large areas of affected skin.

Ability to influence reaction speed when driving vehicles or operating machinery.

There are no data on the effect of the medicinal product Locoid Crelo on the ability to drive vehicles or operate machinery; such effects are not anticipated.

Dosage and Administration

For topical use only.

Apply a small amount of the preparation in a thin, even layer to the affected areas no more than twice daily.

This formulation allows the drug to be used both for lesions accompanied by scaling and for weeping lesions.

Dosage

The total cumulative dose should not exceed 30–60 g of Locoid Creme per week.

Adults and elderly patients

Adults and elderly patients should receive the same dosage, as there are no clinical data indicating that elderly patients require a different dosing regimen.

Children

Prolonged treatment should be avoided whenever possible.

From 3 months to 1 year of age

The treatment duration should not exceed 7 days, if possible.

Overdose.

Excessive use under occlusive dressing may lead to suppression of adrenal glands. There are no specific antidotes or treatment procedures. If any adverse effects occur, treatment should be discontinued and symptomatic therapy initiated.

Adverse Reactions.

Uncommon (>1/10000, <1/1000)

Disorders of the skin and subcutaneous tissue:

• dermatitis, eczema, striae, contact dermatitis;
• contact allergy, pustular acne;
• skin atrophy, often irreversible, accompanied by epidermal thinning, telangiectasia, purpura, and striae;
• depigmentation, hypertrichosis;
• rosacea-like and perioral dermatitis, with or without skin atrophy;
• rebound effect, which may lead to steroid dependence;
• delayed wound healing;
• skin infection, redness, irritation, burning, rash, itching, dry skin, folliculitis, miliaria, acne, maceration.

Endocrine disorders: adrenocortical suppression, Cushing's syndrome, hyperglycemia, glucosuria, growth retardation, and intracranial hypertension.

Very rare (<1/10000, including isolated reports)

Disorders of the eye organs: increased intraocular pressure and risk of cataract development (with systematic exposure of the drug to the conjunctiva).

Immune system disorders: hypersensitivity reactions.

Reporting suspected adverse reactions

It is important to report suspected adverse reactions after marketing authorization of the medicinal product. This allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions via the national reporting system.

Shelf life. 2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach and sight of children.

Packaging.

30 g of emulsion in a bottle; 1 bottle in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

Temmler Italia S.r.l.

Temmler Italia S.r.l.

Manufacturer's address and place of business.

Via delle Industrie, 2, 20061, Carugate (MI), Italy.

Via delle Industrie, 2, 20061, Carugate (MI), Italy.