Corticolacon
Pharmacological action - dermatotropic, immunosuppressive, anti-inflammatory local.
Corticolacon is the preparation in the form of a cream containing a synthetic glucocorticosteroid with a moderately dosed immunosuppressant.
Corticolacon is a complex moderately dosed remedy for external use. The cream is designed for use in difficult to resist, persistent dermatoses with autoimmune chronicity of the inflammatory process in their pathogenetic basis.
Composition:
Mometasone furoate 0.1%
Pimecrolimus 0.3%
Pharmacology
Mechanism of action of the constituent components
Mometasone
Like other topical glucocorticosteroids, it has anti-inflammatory, antipruritic and vasoconstrictive properties. Mometasone acts by inducing proteins that inhibit phospholipase A2, collectively known as lipocortins. These proteins are thought to control the biosynthesis of strong inflammatory mediators by inhibiting the release of arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Pimecrolimus
Specifically binds to the cytosolic receptor macrophilin-12 of T lymphocytes and inhibits calcium-dependent phosphatase, calcineurin. As a result, it suppresses T-lymphocyte activation by blocking the transcription of early cytokines. In particular, at nanomolar concentrations, it inhibits the synthesis of pro-inflammatory cytokines - interleukin-2 and interferon-gamma (Th1-type) as well as interleukin-4 and interleukin-10 (Th2-type) in human T-cells. Pimecrolimus prevents the release of pro-inflammatory cytokines as well as inflammatory mediators from mast cells in vitro in response to antigen/IgE stimulation. Pimecrolimus has no effect on keratinocytes, fibroblasts and endothelial cells.
Pharmacokinetics
Corticolacon causes a slight decrease in adrenal GCS secretion. The extent of percutaneous absorption of Corticolacon is determined by many factors, including the carrier and the integrity of the epidermal barrier. Hydrocortisone occlusion dressings applied for up to 24 h did not increase penetration, but hydrocortisone occlusion for 96 h markedly increased penetration. Inflammation and/or other painful processes in the skin may increase percutaneous absorption.
Indications for use
Treatment of inflammatory and pruritic dermatoses in patients over 5 years of age.
Contraindications
Hypersensitivity; children under 5 years of age.
Use during pregnancy and lactation
Adequate and well-controlled studies in pregnant women have not been conducted. Therefore, Corticolacon in the form of cream should be used during pregnancy only if the potential benefit exceeds the possible risk to the fetus.
Mometasone in Corticolacon has been shown to be detectable in maternal milk when administered systemically and may inhibit growth, interfere with endogenous GCS production, or cause other adverse effects. It is not known whether topical administration of GCS leads to systemic absorption sufficient to produce detectable amounts of GCS in the mother's milk.
It is not known whether pimecrolimus penetrates into breast milk.
Side effects
In controlled clinical trials involving 812 patients, the incidence of adverse reactions associated with the use of mometasone as part of the formulation was 4.8%. Adverse reactions reported included burning, itching, skin atrophy, tingling/ tingling, and furunculosis.
Because adverse reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Reports of local adverse reactions include irritation, dryness, folliculitis, hypertrichosis, acne, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, skin atrophy, stricture, and sweating. These adverse reactions may occur more frequently with occlusive dressings.
No cases of contact sensitization, phototoxicity, photoallergy, or cumulative inflammatory reaction have been reported in safety studies of pimecrolimus and mometasone in cream form.
Dosage and administration
Externally, a thin layer of cream applied to the affected skin once a day.
Precautions
General
Once control is achieved, use of Corticolacon should be discontinued. If no improvement is seen within 2 weeks, reassessment may be necessary.
Corticolacon should not be used with occlusive dressings. Avoid application to the face, groin or armpits. Avoid contact with the eyes.
Corticolacon in cream form is intended for external use only. Corticolacon is not intended for ophthalmic or intravaginal use.
Effects on the endocrine system
Systemic absorption of the constituent Corticolacon cream may cause reversible suppression of the HPA axis with possible development of glucocorticosteroid insufficiency. This may occur during treatment or after withdrawal. Manifestations of Cushing's syndrome, hyperglycemia and glucosuria may also be caused in some patients by systemic absorption of topical GCS during treatment. Factors predisposing to suppression of the HPA axis include the use of highly active GCS, large surface area treated, prolonged use, use of occlusive dressings, impaired protective function of the skin barrier, hepatic insufficiency, and young age.
Because of the possibility of systemic absorption, the use of topical GCSs may require periodic evaluation of patients for signs of HPA axis suppression, which can be done with an ACTH stimulation test.
If HPA axis suppression is confirmed on examination, attempts should be made to phase out Corticolacon, reduce the frequency of use, or replace it with a less active GCS. Recovery of HPA axis function usually occurs immediately after withdrawal of topical GCS. Infrequently, signs and symptoms of GCS insufficiency may occur, requiring additional use of systemic GCS. Children may be more susceptible to systemic effects of topical GCS when used in similar doses due to a larger skin surface area to body weight ratio.
Ophthalmic adverse reactions
Topical GCS use may increase the risk of posterior subcapsular cataracts and glaucoma. Cataracts and glaucoma have been reported in the post-registration period with topical GCS including Corticolacon (see "Adverse Reactions"). Corticolacon should be avoided in the eyes. The patient should be informed of any symptoms of visual disturbance, and if they occur, consideration should be given to referring the patient to an ophthalmologist for evaluation.
Allergic Contact Dermatitis
If irritation occurs, the use of Corticolacon should be discontinued and appropriate therapy administered. Allergic contact dermatitis when using GCS is usually diagnosed in the absence of healing rather than in a clinical exacerbation. Such a diagnosis must be confirmed by appropriate diagnostic tests.
Associated skin infections
If concomitant skin infections are present or develop, an appropriate antifungal or antibacterial drug should be prescribed. If a positive response does not occur in the short term, topical use of Corticolacon should be discontinued until proper infection control has been achieved.
Because of the greater skin surface area to body weight ratio, children are at higher risk of HPA axis suppression and development of Cushing's syndrome when treated with topical GCSs than adults. Therefore, they are also at higher risk of developing HPA insufficiency during and/or after treatment withdrawal. Pediatric patients, more so than adults, may be more susceptible to the development of skin atrophy, including the appearance of striae, when treated with topical GCS. A higher risk of HPA axis suppression in children is seen when topical GCS is used on a surface area greater than 20% of the body area.
In children treated with topical GCS, suppression of the HPA axis, development of Cushing's syndrome, delayed linear growth, delayed weight gain, and development of intracranial hypertension have been reported. Manifestations of adrenal insufficiency in children include low plasma cortisol levels and lack of response to ACTH stimulation. Manifestations of intracranial hypertension include swollen fontanelles, headaches, and bilateral papilledema of the optic disc. Corticolacon should not be used in the treatment of diaper dermatitis.
Manufacturer
«Dong-Pha» South Korea
Storage conditions
Keep at a temperature not more than 25 ° C.
Keep out of reach of children!
Shelf life
3 years.
Do not use after expiration date stated on the package.
