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Halcinonide Cream

Function and Efficacy

Pharmacology: 1. Anti-inflammatory effect This product is a topical drug, a highly effective fluorinated and chlorinated corticosteroid with anti-inflammatory, anti-pruritic and vasoconstrictive effects. This product replaces the 21-hydroxyl group with a chlorine atom on the skeleton of triamcinolone. The anti-inflammatory potency multiple determined by the vasoconstriction test is 360. There is evidence that the intensity of the vasoconstriction test is consistent with the efficacy. Its anti-inflammatory and antipruritic mechanism is to increase the responsiveness of the receptor to catecholamine, increase the production of cAMP by activating adenylate cyclase, and reduce the destruction of cAMP by inhibiting phosphoethylesterase, resulting in an increase in the annual concentration of cAMP in cells and inhibiting the release of histamine. The effect of this product in inhibiting the proliferation of granulomas in rats and mice is similar to that of dexamethasone. Using the formaldehyde-induced heel swelling method for mice and rats, this product and dexamethasone both have significant inhibitory effects, while hydrocortisone with a 5-fold higher dose has no inhibitory effect. This product has a significant weight loss effect on the thymus and spleen. 2 Selective pharmacological effects on various types of cells: reduce the number of T lymphocytes, monocytes, and eosinophils, inhibit lymphocyte proliferation and cytokine production, inhibit macrophage differentiation and phagocytic activity, inhibit neutrophil adhesion, reduce vascular endothelial cell permeability, inhibit fibroblast proliferation and collagen synthesis, and inhibit sebaceous gland cell activity. 3 Anti-proliferative effect This product has an anti-mitotic effect. It reduces the transcription of PNA, thereby reducing DNA synthesis, and also affects DNA repair, resulting in thinning of the epidermis, especially the greatest impact on collagen synthesis. 4 Immunosuppressive effect This product binds to the corticosteroid receptors in the cytoplasm, causing a series of reactions and activating the expression of lytic genes in the cells; it induces nuclear DNA lysis in lymphocytes and directly kills lymphocytes. Toxicity: In acute toxicity test, the LD50 of female mice injected intramuscularly was 84 mg/kg, and the LD50 of male mice was 35 mg/kg; the LD50 of male mice injected intraperitoneally was 215 mg/kg; no animal death was observed after oral administration of 250-1500 mg/kg. In subacute toxicity test, the main manifestations were damage to the thymus and lymphocytes. There is no research on the teratogenicity of topical application of this product, but the risk of teratogenicity in people who have not taken the drug orally is higher than that of the general population. Large-scale application of this product or packaged medication has been found to inhibit the hypothalamus-pituitary-adrenal axis (HPA axis).

Ingredients

The main ingredients of this product are: Halcinonide (clofluocinolone, halcinonide). Its chemical name is: 16alpha;, 17-[(1-methylethylidene)bis(oxy)]-11?-hydroxy-21-chloro-9-fluoropregn-4-ene-3,20-dione. Molecular formula: C24H32ClFO5 Molecular weight: 454.9.

Name Description Content CAS NO. Manufacturer
HalcinonideIngredients

It has anti-inflammatory, anti-itching and vasoconstrictive effects. It increases the reactivity of β receptors to catecholamine, increases the production of cAMP by activating adenylate cyclase, and reduces the destruction of cAMP by inhibiting phosphoethylesterase, resulting in an increase in the concentration of cAMP in cells and inhibiting the release of histamine. Its effect in inhibiting the proliferation of granulomas in rats and mice is similar to that of dexamethasone. It has a significant weight-loss effect on the thymus and spleen. It reduces the number of T lymphocytes, monocytes, and eosinophils, inhibits lymphocyte proliferation and cytokine production, inhibits macrophage differentiation and phagocytic activity, inhibits neutrophil adhesion, reduces the permeability of vascular endothelial cells, inhibits fibroblast proliferation and collagen synthesis, and inhibits sebaceous gland cell activity. It has an anti-mitotic effect, which reduces the transcription of PNA, thereby reducing the synthesis of DNA, and also affects the repair of DNA, resulting in thinning of the epidermis, especially the greatest effect on collagen synthesis. By binding to the cytoplasmic corticosteroid receptors, a series of reactions occur, activating the expression of lytic genes in the cells; it induces nuclear DNA cleavage in lymphocytes and directly kills lymphocytes.

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3093-35-4 9

Appearance

This product is a milky white cream.

Indication

Contact eczema, atopic dermatitis, neurodermatitis, small-scale psoriasis, lichen sclerosus atrophicus, lichen planus, discoid lupus erythematosus, seborrheic dermatitis (non-facial) hypertrophic scars.

Usage and Dosage

Apply to the affected area once in the morning and evening.

Adverse Reactions

A small number of patients experience burning sensation, stinging, and temporary itching at the site of application. Long-term use may cause dilation of skin capillaries (especially on the face), skin atrophy, and stretch marks (prone to adolescents). Skin atrophy may be followed by purpura, ecchymosis, skin fragility, hirsutism, folliculitis, miliary papules, skin depigmentation, and delayed ulcer healing. The packing method is prone to secondary fungal infection in skin folds. When absorbed through the skin for a long time, systemic adverse reactions may occur.

Precautions

Allergic reactions to the drug. Primary skin lesions caused by bacteria, fungi, viruses and parasites. Ulcerative lesions. Acne, rosacea. Use on the eyelids (risk of causing glaucoma). Exudative skin diseases.

Special Population Medication

Precautions for children: Not yet clear. Precautions for pregnancy and lactation: Not yet clear. Precautions for the elderly: Not yet clear.

Drug Interactions

Not yet clear

Storage

Store tightly closed at room temperature.

Packaging Specification

10g:10mg

Validity Period

24 months

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