Locoid

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

Composition:

Active substance: hydrocortisone 17-butyrate;

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

Excipient: polyethylene oleogel.

Pharmaceutical form. Ointment.

Main physicochemical properties: transparent, soft, greasy ointment of light gray to whitish color.

Pharmacotherapeutic group. Corticosteroids for dermatological use.

ATC code D07AB02.

Pharmacological properties.

Pharmacodynamics.

Hydrocortisone 17-butyrate is an active synthetic non-halogenated corticosteroid for topical use. It exerts anti-inflammatory, anti-edematous, and antipruritic effects rapidly. Its efficacy is comparable to that of halogenated steroids. Application in recommended doses does not cause suppression of the hypothalamic-pituitary-adrenal system. Although prolonged use of large doses, especially under occlusive dressings, may lead to increased plasma cortisol levels, this is not accompanied by reduced responsiveness of the pituitary-adrenal system, and discontinuation of the drug results in rapid normalization of cortisol production.

Pharmacokinetics.

Absorption. After 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 in 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.

Superficial non-infected dermatoses responsive to topical corticosteroids (eczema, allergic and contact dermatitis, neurodermatitis, psoriasis), not associated with microorganisms and expected to respond inadequately to treatment with mild potency agents.

Continuation of treatment or maintenance therapy of dermatoses previously treated with more potent corticosteroids.

Contraindications.

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

Interaction with other medicinal products and other forms of interaction.

Data on drug interactions with Locoid® ointment are not available.

Special precautions for use

Do not apply the ointment to the eyelids due to the risk of contact with the conjunctiva and the increased risk of developing common glaucoma or subcapsular cataract.

The skin of the face, genital area, and scalp is most sensitive to corticosteroids. Therefore, only low-potency corticosteroids should be used for treating lesions in these areas.

It may sometimes be appropriate to apply a dressing with or without air access to the affected area, or to use an occlusive dressing.

The effect of corticosteroids may be enhanced by application under an occlusive dressing, which increases drug penetration (approximately by a factor of 10) through the stratum corneum of the epidermis. However, this also increases the risk of adverse effects.

It should be noted that when corticosteroids are applied over large skin areas, especially when using (polyethylene) dressings or in skin fold areas, increased systemic absorption of the drug may occur, potentially leading to suppression of adrenocortical function.

Adrenal cortex suppression may develop rapidly in children. Suppression of growth hormone production may also occur. If long-term treatment is necessary, it is advisable to regularly monitor the child's height and body weight, as well as plasma cortisol levels.

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

Application of the drug to the face, skin folds, and other areas of thin skin may lead to skin atrophy and increased drug absorption.

Topically applied 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 systemic toxicity due to impaired skin barrier function. Steroids may be used in scalp psoriasis or chronic plaque psoriasis of the hands and feet. Careful monitoring of patients is essential.

Visual disturbances

Visual disturbances may occur with both systemic and topical use of corticosteroids. If a patient experiences symptoms such as blurred vision or other visual disturbances, an ophthalmological consultation should be sought to evaluate possible causes, including cataract, glaucoma, or rare conditions such as central serous chorioretinopathy (CSC), which has been reported after systemic or topical corticosteroid use.

Use during pregnancy or breastfeeding

Pregnancy

Corticosteroids cross the placenta. To date, there is no clear evidence of teratogenic effects in humans similar to those observed in animal studies. Topical application of corticosteroids in high doses to pregnant animals has been associated with fetal developmental abnormalities such as cleft palate and intrauterine growth retardation. Furthermore, preclinical data do not provide additional information beyond the existing clinical experience with the drug.

With systemic administration of high doses of corticosteroids, effects on the fetus or newborn have been reported (fetal growth retardation, adrenocortical suppression).

Despite limited data on topical corticosteroid use in pregnant women, due to their limited systemic absorption, weak- and moderate-potency corticosteroids (class 1 and class 2), such as hydrocortisone, may be used for short periods and over limited skin areas. The aforementioned adverse effects cannot be excluded with prolonged use or application over large skin areas. Such use should only be considered when specifically indicated.

Breastfeeding

Locoid® ointment may be used in breastfeeding women only for short-term treatment and on small skin areas. For long-term treatment or application over large areas or on damaged skin, breastfeeding should be discontinued.

Ability to affect reaction speed when driving or operating machinery

There are no data regarding the effect of Locoid® ointment on the ability to drive or operate machinery. An effect is not expected.

Dosage and Administration.

Apply a small amount of the preparation to the skin 1–3 times daily. When the condition improves, usually once daily application or 2–3 times per week is sufficient.

The total weekly dose should not exceed 30–60 g.

Locoid® should be applied as a thin, even layer to affected skin areas. The preparation may be gently rubbed into the skin to enhance penetration.

To achieve a better therapeutic effect, an occlusive dressing may be applied.

Children.

Can be used in children aged 3 months and older.

Overdose.

With chronic overdose or inappropriate use, adverse effects described in the section "Adverse Reactions" may occur.

If symptoms of hypercorticism are observed, treatment should be discontinued.

Adverse reactions.

Systemic adverse reactions with topical corticosteroids in adults are rare but may be serious, particularly in cases of prolonged use leading to adrenal cortical suppression.

The risk of systemic effects is increased under the following circumstances: use under occlusive dressing (plastic wrap or application in skin folds); application to large areas of skin; prolonged treatment duration; use in children (children are particularly susceptible due to their thin 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).

The risk of local adverse reactions increases with the potency of the preparation and duration of treatment. Use under occlusive dressing (plastic wrap or application in skin folds) increases this risk. The skin of the face, scalp, and genital area is particularly susceptible to adverse reactions. Inappropriate use, as well as the presence of bacterial, parasitic, fungal, or viral infections, may mask and/or exacerbate manifestations of these conditions.

Reporting of suspected adverse reactions.

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

Shelf life. 5 years.

Storage conditions.

Store at temperatures not exceeding 25 °C. Keep out of reach of children.

Packaging.

30 g ointment in an aluminum tube; 1 tube per 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.