Karizon

General characteristics. Structure:

Active agent: 0,5 mg of a klobetazol of propionate in 1 g of cream.

Excipients: methylparahydrooxybenzoate (E218), dinatrium эдетат, paraffin white soft, stearyl alcohol, paraffin, сорбтансексвиолеат, polysorbate 80, glycerin, the water purified.

External use cream.

Pharmacological properties:

Pharmacodynamics. During broad pharmacological tests and tests in public in comparison with other glucocorticoids at test on a blanching test according to Mackenzie and Wells, at a klobetazol of propionate strong vasoconstrictive action, in comparison with strongly active ingredients, such as флуоцинолон, дифлукортолон, betamethasone, and Triamcinolonum which is comparable to theoretical assumptions was revealed.

Antiinflammatory efficiency of a klobetazol of propionate was estimated by conducting tests on a pyrectic erythema, tests by crotonic oil / kerosene and a poisonous ivy. During such researches in comparison with reference drugs – betamethasone valerate, a diflukortona valerate, a fluotsinolona acetonide and Triamcinolonum acetonide – the effect corresponded to theoretical assumptions.

Anti-proliferative action of a klobetazol of propionate, for example, when conducting tests on psoriasis plaques, was more expressed, than at a fluotsinolon of acetonide, betamethasone of valerate and a diflukorton of valerate.

B the qualitative relation the mechanism of antiinflammatory, anti-proliferative and immunomodulatory action for all glucocorticoids – agrees to the standard and partially incomplete and hypothetical representations – schematically, in the simplified form, it is possible to present as follows: molecules of a glucocorticoid form complexes in plasma with kortikoidny receptors of cells – contact separate genes of GRE (gormonresponsivny elements). It induces a transcription of the specific m-RNA-molecules participating in synthesis of lipokortin-proteins on ribosomes. Lipokortina slow down the reactions arising in case of physical, chemical, toxic or immunogeny impact or action of a microbiological pathogenic factor, which are carried out between a phospholipase of A2 and phospholipids and providing arachidonic acid release. The delay or delay of process of release of arachidonic acid normalizes, reduces or blocks the synthesis regulated by metabolism of arachidonic acid with cyclooxygenase and a lipoxygenase and release of prostaglandins of prostacyclins, leukotrienes, VEILS and thromboxanes which as inflammatory mediators influence, for example, vessels, membranes of cells, leukocytes macrophages and their chemotaxis and migration and regulate increase in number of cells. In addition, glucocorticoids have antimitotic effect and slow down synthesis of nucleic acid and a protein. Essential factors of their immunomodulatory and protivoallegrichesky action is interaction of glucocorticoids with V-cells, T-cells and Langergans's cells that slows down advance of antigens and their antagonistic action on synthesis and functions of Interlaken of 1, 2 and other tsitokinin.

Pharmacokinetics. It is easily absorbed through skin. Mainly, it biotransformirutsya in a liver. To be removed with bile or through a large intestine. The general index of removal to a klobetazol of propionate makes 72 hours, about 70% of the general dose. Klobetazol propionate is partially metabolized by oxygenating to 11-keto-derivative.

Indications to use:

Psoriasis (except for widespread blyashechny psoriasis), persistent eczemas, red flat deprive, a diskoidny lupus erythematosus and other zaboyolevaniye of skin which will not respond to treatment less active corticosteroids.

Route of administration and doses:

Cream should be applied once a day, a thin layer.

The total area of drawing should not exceed 20% of all body surface. The course of treatment makes no more than 2-3 weeks.

Features of use:

Not to apply drug on sites around eyes. Not to apply to patients of advanced age drug on big sites of skin. In case of the missed putting drug, next time the dose should not be doubled.

In addition to Karizon cream: at use of drug in genitals and an anus and simultaneous use of latex condoms takes place of decrease in degree of safety when using condoms.

Karizon, cream: cetyl stearyl alcohol and polysorbate 80 can cause limited skin reactions of local character (for example, contact dermatitis).

Ability to influence speed of response at control of motor transport or work with other mechanisms. Does not influence.

Special security measures. Not to apply drug on face skin, intertriginozny sites (area of axillary hollows and genitalias), on the erosive and becoming wet surfaces of skin, a graze and an ulceration. At emergence of infectious infection topical treatment with glucocorticoid drugs should be stopped.

Not to use this drug under occlusive bandages.
For safety for health of the patient Karizon's number of the release applied in any form should not exceed 50 g a week. Prolonged and regular use of a klobetazol of propionate has to be carried out under observation of the doctor.

Side effects:

Side effects, data on which are given below, are classified by bodies and systems and for the frequency of their emergence. On the frequency of emergence are divided into the following categories: very often (≥ 1/10), it is frequent (≥ 1/100 and ≤ 1/10), infrequently (≥ 1/1 000 and ≤ 1/100), is rare (≥ 1/10 000 and ≤ 1/1 000), is very rare (<1/10 000), including isolated cases. Immune system.

Very seldom: hypersensitivity. Local hypersensitivity reactions, such as an erythema, rash, an itch, urticaria, local burning of skin and allergic contact dermatitis, can arise in sites of application and to be similar to symptoms for which treatment drug was appointed.

If there are hypersensitivity signs, use of drug needs to be stopped urgently. Endocrine system. Very seldom: giperkortizolizm signs. As well as at use of other topical corticosteroids, or drawing on big sites can lead prolonged use in a large number to emergence of signs of a giperkortizolizm owing to considerable system absorption. Such cases are most probable at babies and children, and also when using an occlusive bandage. At babies of a diaper work as an occlusive bandage.

Provided that the week dose of drug at adults does not exceed 50 g, any oppression of a hypophysis or adrenal glands will be temporary, with bystry return to a normality as soon as the short course of steroid therapy is stopped. Vascular system.

Infrequently: expansion of superficial blood vessels.

Prolonged and intensive treatment by highly active corticosteroid drugs can lead to expansion of superficial blood vessels, especially during the using of hermetic bandages or rubbing in of drug in skin folds. Skin and hypodermic fabrics.

Infrequently: a local atrophy, atrophic strips on skin.

Very seldom - thinning of skin, pigmentation change, a hypertrichosis, an aggravation of the main symptoms, a pustular form of psoriasis. Prolonged and intensive treatment by highly active corticosteroid drugs can cause atrophic changes, such as atrophic strips on skin and thinning of skin, especially during the using of hermetic bandages or rubbing in of drug in skin folds. In rare instances treatment of psoriasis corticosteroids (or its termination) can provoke a pustular form of a disease.

Interaction with other medicines:

Interaction of drug Karizon cream, with other medicines is still not revealed, however, such opportunity is not excluded concerning such medicines as, for example, diuretics and anticoagulants, and also under unfavorable therapeutic and rezorbtsionny conditions, for example, at strongly injured skin.

Contraindications:

- Pink eels (rozatsea), eels (acne) also perioralnyydermatit.
- Perianal and genital itch.
- The damages of skin caused by viruses (a virus of a herpes simplex, chicken pox).
- Hypersensitivity to drug components.
- The injuries of skin which are initially infected with fungi or bacteria.
- A dermatosis at children aged till 1 year, including a diaper dermatitis and other dermatitis.
- Reaction to inoculations.
- First trimester of pregnancy.

Overdose:

The probability of emergence of acute overdose is very insignificant. In case of chronic overdose or the wrong use there can be giperkortizolizm signs demanding reduction or gradual phase-out of local corticosteroids which needs to be seen off under medical observation, considering risk of emergence of insufficiency of adrenal glands.

Storage conditions:

Period of validity 3 years. After opening of a tuba - 3 months. To store in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Cream - on 15 g, 30 g and 50 g in a tuba, on 1 tuba in a cardboard pack.