Source: Registered Drug Product Database (NG) Publisher: Kremoint Pharma Pvt. Ltd., B-8 Additional MIDC, Ambernath, Ambernath (E). Thane 421506
1. Clobetasol propionate
Like other topical corticosteroids, has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
2. Clotrimazole alters the permeability of the fungal cell wall and inhibits the activity of enzymes within the cell. It specifically inhibits the biosynthesis of ergosterol and other sterols required for cell membrane production. Clotrimazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms and the uptake of purine, impair triglyceride and/or phospholipid biosynthesis, and inhibit the movement of calcium and potassium ions across the cell membrane by blocking the ion transport pathway known as the Gardos channel.
The extent of percutaneous absorption of topical corticosteroids, including clobetasol propionate, is determined by many factors, including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings.
As with all topical corticosteroids, clobetasol propionate can be absorbed from normal skin. Inflammation and/or other disease processes in the skin may increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. Once absorbed through the skin, topical corticosteroids enter pharmacokinetic pathways similarly to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids, including clobetasol propionate and its metabolites, are also excreted into the bile.
This Cream has been shown to depress the plasma levels of adrenal cortical hormones following repeated nonocclusive application to diseased skin in patients with psoriasis and eczematous dermatitis. These effects have been shown to be transient and reversible upon completion of a two-week course of treatment.
Pharmacokinetic investigations after dermal application have shown that clotrimazole is practically not absorbed from intact or inflamed skin into the human blood circulation. The resulting peak serum concentrations of clotrimazole were below the detection limit of 0.01 microg/ml, reflecting that clotrimazole applied topically does not lead to measurable systemic effects or side effects.
Not applicable.
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