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

Active ingredient

Composition

1 g of the ointment contains:

The active ingredient:

hydrocortisone 17-butyrate – 1 mg;

Excipients:

Polyethylene ointment base (Vaseline oil 95%, PE 5%).

How to take, the dosage

Externally. Locoid® in the form of an ointment is used in subacute and chronic processes, especially in the presence of lichenification, infiltration and dryness.

The drug is applied to the affected areas of the skin in thin layers 1-3 times a day. If there is positive effect the frequency of use can be reduced to 2-3 times a week.

To improve penetration the drug is applied by massaging.

In cases of resistant course of the disease such as localization of dense psoriatic plaques on the elbow areas and knees the drug can be used under occlusive dressings.

The dose of the drug used over a week should not exceed 30-60 g.

Special Instructions

Lokoid® should not be applied to the periorbital area due to the risk of glaucoma. There is a risk of increased intraocular pressure if systemic contact with the conjunctiva occurs.

Any GCS for external use in the form of ointment should not be used on the scalp and in acute inflammation (especially exudative). Lokoid®, cream and Lokoid Crelo® are indicated for the treatment of steroid-sensitive skin lesions in the face, folds, genital area and areas with abundant hair coverings.

The drug should not be used in the presence of atrophic skin changes.

The risk of local and systemic side effects increases with extensive application, prolonged use, use of occlusive dressings, and use in children.

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

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

Pediatric use

Perhaps use in children from 6 months of age. When the drug is used in children, in the face area or under occlusive dressings, the duration of treatment should be shortened.

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

In children, suppression of adrenal cortical function may develop more rapidly. In addition, a decrease in growth hormone excretion may be observed. When using the drug for a long time it is necessary to monitor body weight, growth, plasma cortisol levels. In the study in children receiving 30-60 g of Locoid® a week for 4 weeks in comparison with using 1% hydrocortisone ointment no disorders of adrenal cortex function were revealed in any child, i.e. no difference of hydrocortisone 17-butyrate in this parameter from usual hydrocortisone was observed.

Influence on the ability to drive and operate machinery

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

Contraindications

Side effects

Local reactions: skin irritation, in rare cases – other local reactions typical for local steroid therapy.

Systemic reactions: with long-term use, application on large surfaces and/or use of occlusive dressings the side effects typical for systemic GCS may be observed.

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

Overdose

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

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