Composition, form of production and packaging
? Ointment for external use 0.1% translucent, soft, oily, from light gray to almost white.
1 g
hydrocortisone 17-butyrate 1 mg
Excipients: polyethylene ointment base (95% vaseline oil, 5% polyethylene) - qs to 1 g.
30 g - aluminum tubes (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Synthetic non-halogenated glucocorticoid drug for external use. The esterification of the hydrocortisone molecule with the residue of butyric acid (butyrate) made it possible to radically increase the activity of the preparation as compared to native hydrocortisone. Has a rapidly advancing anti-inflammatory, anti-edematous, antipruritic effect.
The use of Lokoid in the recommended doses does not cause suppression of the hypothalamic-pituitary-adrenal system. Although the use of the drug in high doses for a long time, especially with the use of occlusive dressings, can lead to an increase in the level of cortisol in the blood plasma, it is usually not accompanied by a decrease in the reactivity of the pituitary-adrenal system, and the withdrawal of the drug 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 blood stream unchanged.
Metabolism
Most hydrocortisone 17-butyrate is metabolized to hydrocortisone and other metabolites directly in the epidermis and, subsequently, in the liver.
Excretion
Metabolites and a small part of unchanged hydrocortisone 17-butyrate are excreted with the kidneys and through the intestine.
INDICATIONS
Surface, uninfected, sensitive to local SCS skin diseases:
- eczema;
- dermatitis (including atopic, contact, seborrheic);
- psoriasis.
DOSING MODE
Outwardly.
Lokoid В® in the form of an ointment is used in subacute and chronic processes, especially in the presence of lichenification, infiltration, dryness.
The drug is applied to the affected skin with a thin layer 1-3 times / day. When there is a positive dynamics, the frequency of application of the drug can be reduced to 2-3 times a week. To improve penetration, the drug is applied by massaging movements. In cases of refractory disease, for example, in the localization of dense psoriatic plaques on the elbow areas, the knees, the drug can be used under occlusive dressings. The dose of the drug used during the week should not exceed 30-60 g.
SIDE EFFECT
Local reactions: skin irritation; in rare cases - other local reactions, characteristic for therapy GCS.
Systemic reactions: with long-term use, application to large surfaces and / or the use of occlusive dressings, side effects characteristic of systemic SCS can be observed. The risk of local and systemic side effects when using Lokoid is lower than using fluorinated steroids.
CONTRAINDICATIONS
- bacterial skin infections (strepto- and staphyloderma, gram-negative folliculitis);
- viral skin infections (simple herpes, chicken pox, shingles);
- fungal skin infections;
- tuberculosis and syphilitic skin lesions;
- parasitic skin infections;
- Neoplastic skin changes (benign and malignant tumors);
- Acne, rosacea, perioral dermatitis;
- Post-vaccination period;
- violation of the integrity of the skin (wounds, ulcers);
- Hypersensitivity to the drug.
Caution should be given to the drug during pregnancy and lactation.
PREGNANCY AND LACTATION
GCS penetrate the placental barrier. Effects on the fetus can be particularly pronounced when applying Lokoid to large areas of the skin.
There is no data on the amount of hydrocortisone excreted in breast milk; it is recommended to take special care when applying Lokoid during lactation.
APPLICATION FOR CHILDREN
Possible use in children from 6 months of age . In cases of use of the drug in children, on the face area or under occlusive dressings, the duration of the course of treatment should be reduced.
When used in children, the skin surface area on which the drug is applied should not exceed 20% of the total.
In childhood, suppression of the function of the adrenal cortex can develop faster. In addition, there may be a decrease in the excretion of growth hormone. When using the drug for a long time, it is necessary to observe the body weight, growth, plasma cortisol level. In a study in children who received 30-60 g of Lokoid per week for 4 weeks compared to 1% hydrocortisone ointment, no child showed any adrenocortical dysfunction, while the difference between hydrocortisone 17-butyrate in this indicator from the usual hydrocortisone was not observed.
SPECIAL INSTRUCTIONS
Do not apply Lokoid В® to the periorbital area due to the risk of developing glaucoma. With a systematic hit on the conjunctiva, there is a risk of increased intraocular pressure.
Any GCS for external use in the form of an ointment is not advisable to use on the scalp, as well as with acute inflammation (especially exudative). For the treatment of steroid-sensitive skin lesions localized in the face, folds, genitalia, as well as on skin areas with abundant hair, it is preferable to use other medicinal forms of Lokoid (cream, crelo).
The drug is preferably not used in the presence of atrophic skin changes.
The risk of local and systemic side effects increases when applied to extensive areas of damage, prolonged use, the 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 any SCS, it is desirable to limit the duration of the drug and prescribe a course dose that is minimal enough to stop the skin process.
Use in Pediatrics
Possible use in children from 6 months of age . In cases of use of the drug in children, on the face area or under occlusive dressings, the duration of the course of treatment should be reduced.
When used in children, the skin surface area on which the drug is applied should not exceed 20% of the total.
In childhood, suppression of the function of the adrenal cortex can develop faster. In addition, there may be a decrease in the excretion of growth hormone. When using the drug for a long time, it is necessary to observe the body weight, growth, plasma cortisol level. In a study in children who received 30-60 g of Lokoid per week for 4 weeks compared to 1% hydrocortisone ointment, no child showed any adrenocortical dysfunction, while the difference between hydrocortisone 17-butyrate in this indicator from the usual hydrocortisone was not observed.
Impact on the ability to drive vehicles and manage mechanisms
Data on the influence of Lokoid on the ability to drive vehicles and work with mechanisms there.
OVERDOSE
There are no data on Lokoid overdose. With prolonged use of the drug in high doses, it is possible to enhance the side effects described above. When symptoms of hypercortisy appear, the drug should be discarded.
DRUG INTERACTION
There are no data on the drug interaction of Lokoid.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 5 years.
