Locoid, ointment 0.1% 30 g

Lokoid is an anti-inflammatory topical, antipruritic, antiedematous.

Pharmacodynamics

Lokoid^® is a synthetic nonhalogenated GCS for external use. The esterification of the hydrocortisone molecule with an oily acid residue (butyrate) has radically increased the activity of the drug compared to native hydrocortisone. Locoid^® has a rapid onset anti-inflammatory, anti-edematous, antipruritic effect.

The use of Locoid^® in recommended doses does not cause suppression of the hypothalamic-pituitary-adrenal system. Although long-term use of high doses of the drug, especially with occlusive dressings, may result in increased plasma cortisol levels, this is not usually accompanied by a decrease in pituitary-adrenal reactivity, and withdrawal of the drug results in rapid normalization of cortisol production.

Pharmacokinetics

Absorption

After application, the active substance accumulates in the epidermis, mainly in the granular layer, with little systemic absorption. A small amount of hydrocortisone 17-butyrate is absorbed into the systemic bloodstream unchanged.

Metabolism

Most hydrocortisone 17-butyrate is metabolized to hydrocortisone and other metabolites directly in the epidermis and subsequently in the liver.

Elimination

The metabolites and a small portion of unchanged hydrocortisone 17-butyrate are excreted by the kidneys and through the intestine.

Indications

Arthritis
bronchial asthma, allergies, eczema, neurodermatitis, psoriasis
conjunctivitis, stye, prevention and treatment of shock

Pharmacological effect

Lokoid – local anti-inflammatory, antipruritic, decongestant.

Pharmacodynamics

Lokoid® is a synthetic non-halogenated corticosteroid for external use. Esterification of the hydrocortisone molecule with a butyric acid residue (butyrate) made it possible to radically increase the activity of the drug compared to native hydrocortisone. Lokoid® has a rapid onset anti-inflammatory, anti-edematous, antipruritic effect.

The use of Lokoid® in recommended doses does not cause suppression of the hypothalamic-pituitary-adrenal system. Although the use of large doses of the drug for a long time, especially when using occlusive dressings, can lead to an increase in plasma cortisol levels, this is usually not accompanied by a decrease in the reactivity of the pituitary-adrenal axis, and drug withdrawal leads to a rapid normalization of cortisol production.

Pharmacokinetics

Suction

After application, the active substance accumulates in the epidermis, mainly in the granular layer; systemic absorption is negligible. A small amount of hydrocortisone 17-butyrate is absorbed into the systemic circulation unchanged.

Metabolism

The majority of hydrocortisone 17-butyrate is metabolized to hydrocortisone and other metabolites directly in the epidermis and subsequently in the liver.

Removal

Metabolites and a small part of unchanged hydrocortisone 17-butyrate are excreted by the kidneys and through the intestines.

Special instructions

Locoid® should not be applied to the periorbital area due to the risk of developing glaucoma. In case of systematic contact with the conjunctiva, there is a risk of increasing intraocular pressure.

It is undesirable to use any GCS for external use in the form of an ointment on the scalp, as well as in acute inflammation (especially exudative). For the treatment of steroid-sensitive skin lesions localized in the face, folds, genitals, as well as on areas of skin with abundant hair, it is preferable to use Lokoid®, cream and Lokoid Crelo®.

It is not advisable to use the drug in the presence of atrophic skin changes.

The risk of local and systemic side effects increases when applied to large areas of the affected area, long-term use, use of occlusive dressings and in childhood.

If there is no effect within 2 weeks of continuous treatment, the diagnosis should be clarified.

As with the use of any GCS, it is advisable to limit the duration of use and the course dose to the minimum sufficient to stop the skin process.

Use in pediatrics

Can be used in children from 6 months of age. In cases of use of the drug in children, in the face or under occlusive dressings, the duration of treatment should be reduced.

When used in children, the surface area of ​​the skin to which the drug is applied should not exceed 20% of the total.

In childhood, suppression of adrenal function may develop more quickly. In addition, a decrease in growth hormone excretion may occur. When using the drug for a long time, it is necessary to monitor body weight, height, and plasma cortisol levels. In a study in children who received 30–60 g of Lokoid® per week for 4 weeks, in comparison with the use of 1% hydrocortisone ointment, not a single child had dysfunction of the adrenal cortex, i.e. There were no differences between hydrocortisone 17-butyrate and conventional hydrocortisone in this indicator.

Impact on the ability to drive vehicles and operate machinery

There is no data on the effect of Lokoid® on the ability to drive vehicles and operate machinery.

Active ingredient

Hydrocortisone

Composition

1 g ointment contains:

Active substance:

hydrocortisone 17-butyrate – 1 mg;

Excipients:

polyethylene ointment base (vaseline oil 95%, PE 5%).

Contraindications

Ulcerative lesions of the eye and skin
wounds, tuberculosis of the eye and skin
fungal and viral infections of the eyes and skin
arterial hypertension
peptic ulcer of the stomach and duodenum, active forms of tuberculosis, diabetes mellitus

Side Effects

Local reactions: skin irritation, in rare cases – other local reactions characteristic of local steroid therapy.

Systemic reactions: with long-term use, application to large surfaces and/or use of occlusive dressings, side effects characteristic of systemic corticosteroids may be observed.

The risk of local and systemic side effects when using Lokoid® is lower than when using fluorinated steroids.

Overdose

Symptoms: with prolonged use of the drug in high doses, the side effects described above may increase. If symptoms of hypercortisolism appear, the drug should be discontinued.

Storage conditions

At a temperature not exceeding 25 °C.

Shelf life

5 years

Manufacturer

Temmler Italia S.r.L., Italy