Lokoid

General characteristics. Structure:

Active agent: hydrocortisone 17 butyrate of-1 mg,
Excipients: a polyethylene ointment basis (a liquid paraffin of 95%, polyethylene of 5%) - q.s. to 1,0 g.

Description: translucent, from light gray till almost white color homogeneous soft, fat ointment.

Pharmacological properties:

Локоид® is the synthetic not halogenated glucocorticosteroid for external use. Etherification of a molecule of a hydrocortisone the rest of butyric acid (butyrate) allowed to increase considerably activity of drug in comparison with a native hydrocortisone. Локоид® renders quickly coming antiinflammatory, antiedematous, antipruritic action. 
Lokoid's use in the recommended doses does not cause suppression гипоталамо - pituitary and adrenal system. Though use of high doses of drug for a long time, especially when using occlusive bandages, can lead to increase in maintenance of cortisol in a blood plasma, it usually is not followed by decrease in reactivity of pituitary and adrenal system, and drug withdrawal leads to bystry normalization of products of cortisol.
 
Pharmacokinetics.
Absorption
After application there is an accumulation of active agent in epidermis, generally in a granular layer, system absorption is insignificant. A small amount of a hydrocortisone 17 butyrates is soaked up in a system blood stream in not changed look.
Metabolism
The most part of a hydrocortisone 17 butyrates is metabolized to a hydrocortisone and other metabolites directly in epidermis and in the subsequent in a liver.
Removal
Metabolites and insignificant part of not changed hydrocortisone 17 butyrates are removed by kidneys and through intestines.

Indications to use:

Skin diseases, superficial, not infected, sensitive to local glucocorticosteroids:
- dermatitis, including atopic, contact, seborrheal;
- eczema;
- psoriasis

Route of administration and doses:

Outwardly.
Lokoid in the form of ointment is used at subacute and chronic processes, in particular in the presence of lichenification, infiltration, dryness.
Drug is applied on affected areas of skin with a thin layer by 1-3 times a day. At emergence of positive dynamics frequency rate of use of drug can be reduced to 2-3 weekly. For penetration improvement drug is applied with the massing movements. In cases of a resistant course of diseases, for example at localization of dense psoriasis plaques on elbow areas, knees, drug can be used under occlusive bandages. The drug dose used within a week should not exceed 30-60 g.

Features of use:

It is not necessary to apply Локоид on periorbital area in connection with risk of development of glaucoma. At systematic hit on a conjunctiva there is a risk of increase in intraocular pressure.
In the form of ointment it is not desirable to apply any glucocorticosteroids to external use on a pilar part of the head, and also at an acute inflammation (especially exudative). For treatment the steroid - the sensitive skin defeats which are localized in a face, folds, genitalias and also on sites of skin with plentiful indumentum is more preferable to use other dosage forms of Lokoid (cream, kret).
 It is not desirable to use drug in the presence of atrophic changes of skin.
 The risk of emergence of local and system side effects increases when drawing by extensive sites of defeat, prolonged use, use of occlusion and at children's age.
In the absence of effect within 2 weeks of continuous treatment, it is necessary to specify the diagnosis.
As well as when using any glucocorticosteroid drug, it is desirable to limit duration of use and a course dose minimum sufficient for stopping of skin process.
 
Use in pediatrics
Use for children from 6 monthly age is possible. In cases of use of drug for children, or under occlusive bandages duration of a course of treatment needs to be reduced by area of the person.
When using at children the surface area of skin on which drug is applied should not exceed 20% of the general.
 At children's age suppression of function of bark of adrenal glands can quicker develop. Besides, decrease in excretion of a growth hormone can be observed. At drug use it is necessary to watch the body weight, growth, plasma cortisol level for a long time. In a research at the children receiving 30-60 g of Lokoid a week for 4 weeks in comparison with 1% hydrocortisone ointment at one child dysfunctions of bark of adrenal glands, at the same time differences of a hydrocortisone 17 butyrates on this indicator from a usual hydrocortisone were not revealed it was not observed.
 
Influence on ability to manage vehicles and to work with mechanisms
There are no data on Lokoid's influence on ability to manage vehicles and to work with mechanisms.

Side effects:

Local reactions: Irritation of skin, in rare instances – other local reactions characteristic of outside steroid therapy.
System reactions:
At prolonged use, drawing on big surfaces and/or use of occlusion the side effects characteristic of system glucocorticosteroids can be observed. The risk of emergence of local and system side effects at Lokoid's use is lower, than when using of the fluorinated steroids.

Interaction with other medicines:

There are no data on medicinal interactions of Lokoid.

Contraindications:

- hypersensitivity to a hydrocortisone or auxiliary components of drug.
- bacterial infections of skin (strepto-and staphylodermas, gram-negative folliculitis, etc.);
- viral infections of skin (herpes simplex, chicken pox, shingles, etc.)
- fungal infections of skin;
- tubercular and syphilitic damages of skin;
- parasitic infections of skin;
- neoplastic changes of skin (benign and malignant tumors);
- acne, rozatsea, perioral dermatitis;
- postvaccinal period;
- disturbance of integrity of integuments (wound, ulcer);
 
With care: pregnancy, lactation period.

Pregnancy and lactation
Glucocorticosteroids get through a placenta. Impact on a fruit can be especially expressed when putting drug on big surfaces. There are no data on quantity of the hydrocortisone which is allocated with breast milk; it is recommended to observe extra care at purpose of drug in the period of a lactation.

Overdose:

There are no data on Lokoid's overdose. At prolonged use of drug in high doses strengthening of the side effects described above is possible. At emergence of symptoms of a hypercorticoidism drug should be cancelled.

Storage conditions:

At a temperature not above 25 °C. In the place, unavailable to children. A period of validity - 5 years. Not to use after a period of validity.

Issue conditions:

Without recipe

Packaging:

Ointment for external use of 0,1%.
On 30 g of ointment place in an aluminum tuba with an aluminum membrane and the screw-on cap from polyethylene of high density. On 1 tuba together with the application instruction in a cardboard pack.