Pharmacological properties
Pharmacodynamics. During extensive pharmacological studies and human trials in comparison with other GCS in the McKenzie and Wells extinction test, clobetasol propionate was found to have a strong vasoconstrictor effect compared to such active substances as fluocinolone, diflucortolone, betamethasone, triamcinolone, which is comparable to theoretical assumptions.
The anti-inflammatory efficacy of clobetasol propionate was evaluated by testing for pyretic erythema, croton oil/kerosene, and poison ivy. In these studies, compared with the reference drugs betamethasone valerate, diflucortone valerate, fluocinolone acetonide, and triamcinolone acetonide, the effect was consistent with theoretical assumptions.
The antiproliferative effect of clobetasol propionate (for example, when testing psoriatic plaques) was found to be more pronounced than that of fluocinolone acetonide, betamethasone valerate, and diflucortone valerate.
In qualitative terms, the mechanism of anti-inflammatory, antiproliferative and immunomodulatory action for all GCS - according to generally accepted, partly incomplete and hypothetical ideas - can be schematically, in a simplified form, presented as follows: GCS molecules form complexes in the plasma with steroid receptors of cells - bind to individual genes of hormone-responsive elements. This induces the transcription of specific m-RNA molecules involved in the synthesis of lipocortin proteins on ribosomes. Lipocortins slow down the reactions that occur in the event of physical, chemical, toxic or immunogenic effects or the action of a microbiological pathogenic factor, which are carried out between phospholipase A 2 and phospholipids and ensure the release of arachidonic acid. Delaying or slowing down the process of arachidonic acid release normalizes, reduces or blocks the synthesis regulated by the metabolism of arachidonic acid from COX and lipoxygenase, as well as the release of prostaglandins, prostacyclin, leukotrienes, platelet-activating factor and thromboxanes, which as inflammatory mediators affect, for example, vessels, cell membranes, leukocytes, macrophages, their chemotaxis and migration, regulate the increase in the number of cells. In addition, GCS have an antimitotic effect and slow down the synthesis of nucleic acid and protein. The essential factors of their immunomodulatory and antiallergic effect are the interaction of glucocorticoids with B cells, T cells and Langerhans cells, which slows down the advancement of antigens, their antagonistic effect on the synthesis and functions of interleukin 1, 2 and other cytokinins.
Pharmacokinetics. Easily absorbed through the skin. Mainly metabolized in the liver. Excreted with bile or through the large intestine. The total elimination index of clobetasol propionate is 72 h, about 70% of the total dose. Clobetasol propionate is partially metabolized by oxidation to the 11-keto derivative.
Indication
Psoriasis (except widespread plaque psoriasis), persistent eczema, lichen planus, discoid lupus erythematosus and other skin diseases that are not amenable to treatment with less active corticosteroids.
Application
Carizon ointment, Carizon fatty ointment, Carizon cream should be applied once a day in a thin layer. The total area of application should not exceed 20% of the entire body surface. The course of treatment is no more than 2-3 weeks.
Carizon solution should be applied once a day in a thin layer. The total area of application should not exceed 20% of the entire body surface. The solution is available in bottles with a dispenser nozzle, which ensures its direct application to the affected areas and avoids abundant wetting of the hair. The course of treatment is no more than 2-3 weeks.
Contraindication
Rosacea, acne and perioral dermatitis; perianal and genital itching; skin lesions caused by viruses (herpes simplex virus, chickenpox); hypersensitivity to the components of the drug; skin lesions primarily infected with fungi or bacteria; dermatoses in children under 1 year of age, including diaper dermatitis and other dermatitis; reaction to vaccination; I trimester of pregnancy.
Side effects
Information on side effects, which is given below, is classified by organs and systems and frequency of occurrence. The frequency of occurrence is divided into the following categories: very often (≥1 / 10), often (≥1 / 100 and ≤1 / 10), infrequently (≥1 / 1,000 and ≤1 / 100), rarely (≥1 / 10,000 and ≤1 / 1,000), very rarely (<1 / 10,000), including isolated cases.
Immune system: very rarely - hypersensitivity. Local hypersensitivity reactions, such as erythema, rash, itching, urticaria, local burning of the skin and allergic contact dermatitis, may occur at the application sites and be similar to the symptoms for which the drug was prescribed.
If signs of hypersensitivity occur, the use of the drug must be discontinued immediately.
Provided that the weekly dose of the drug in adults does not exceed 50 g, any suppression of the pituitary or adrenal glands will be temporary, with a rapid return to normal as soon as the short course of steroid therapy is discontinued.
Vascular system: infrequently - dilation of superficial blood vessels.
Skin and subcutaneous tissue: infrequently - local atrophy, atrophic stripes on the skin; very rarely - thinning of the skin, changes in pigmentation, hypertrichosis, exacerbation of the main symptoms, pustular form of psoriasis.
Prolonged and intensive treatment with highly potent corticosteroids may cause atrophic changes, such as atrophic skin stripes and skin thinning, especially when using occlusive dressings or rubbing the drug into skin folds.
In rare cases, treatment of psoriasis with corticosteroids (or its discontinuation) can trigger a pustular form of the disease.
Special instructions
Do not apply the drug to the skin of the face, intertriginous areas (armpits and genitals), erosive and weeping skin surfaces, abrasions and ulcers. If an infection occurs, topical treatment with glucocorticoid drugs should be discontinued. Do not use this drug under occlusive dressings. For the safety of the patient's health, the amount of Carizone used in any form of release should not exceed 50 g/week. Long-term and regular use of clobetasol propionate should be carried out under the supervision of a physician.
Do not apply the drug to areas of the skin around the eyes. Elderly patients should not apply the drug to large areas of the skin. In case of missed application of the drug, the next dose should not be doubled.
In addition to Carizon fatty ointment, Carizon ointment, Carizon cream. When using the drug in the genital and anal area and simultaneously using latex condoms, there is a decrease in their effectiveness.
Carizon cream. Cetylstearyl alcohol and polysorbate 80 may cause limited local skin reactions (e.g. contact dermatitis).
Carizon oily ointment. Propylene glycol may cause skin irritation.
Carizon ointment. Polysorbate 80 and stearyl alcohol may cause limited local skin reactions (e.g. contact dermatitis).
Carizon solution is easily flammable. Irritating to the mucous membrane of the eyes. Inhalation of the drug vapors can cause drowsiness and confusion, so it is necessary to avoid the drug entering the respiratory tract.
Use during pregnancy and breastfeeding. In the first trimester of pregnancy, the drug is contraindicated. In the next 2 trimesters of pregnancy, the drug is used only if the expected benefit to the mother outweighs the potential risk to the fetus. Do not apply the drug to large areas of skin.
Breastfeeding: The safety of clobetasol propionate during breastfeeding has not been established.
Children. The drug is contraindicated for the treatment of dermatoses in children under 1 year of age, including dermatitis and diaper rash.
The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Does not affect.
Interactions
No interactions of Carizona with other drugs have been identified so far, however, this possibility cannot be ruled out for drugs such as diuretics and anticoagulants, as well as under adverse therapeutic and resorption conditions (e.g., severely damaged skin).
Overdose
The probability of an acute overdose is very small. In case of chronic overdose or misuse, signs of hypercorticism may occur, requiring a reduction or gradual discontinuation of the use of local corticosteroids, which must be carried out under medical supervision, taking into account the risk of adrenal insufficiency.
Storage conditions
At a temperature not exceeding 25 °C.
