DB00838 - Clocortolone
| Identification | |||||||
|---|---|---|---|---|---|---|---|
| Name | Clocortolone | ||||||
| Accession Number | DB00838 (APRD00877) | ||||||
| Type | small molecule | ||||||
| Description | Clocortolone is a medium potency corticosteroid that is often used as a topical cream for the relief of inflammatory oand pruritic (itching) arising from steroid-responsive dermatoses of the scalp. | ||||||
| Structure |
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| Categories (*) | |||||||
| Molecular Weight | 410.907 | ||||||
| Groups | approved | ||||||
| Monoisotopic Weight | 410.166015296 | ||||||
| Pharmacology | |||||||
| Indication | For short-term topical treatment of the inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp. | ||||||
| Mechanism of action | The precise mechanism of the antiinflammatory activity of topical steroids in the treatment of steroid-responsive dermatoses, in general, is uncertain. 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. These enzyme transcriptional changes are mediated by the drug binding first to the glucocorticoid receptor. This complex can migrate to the cell nucleus which then binds to DNA initiating genetic activation and repression of various genes. | ||||||
| Absorption | Topical corticosteroids can be absorbed from intact healthy skin. The extent of percutaneous absorption of topical corticosteroids is determined by many factors, including the vehicle and the integrity of the epidermal barrier. Occlusion, inflammation and/or other disease processes in the skin may also increase percutaneous absorption. | ||||||
| Protein binding | Not Available | ||||||
| Biotransformation | Metabolized, primarily in the liver, and then excreted by the kidneys. | ||||||
| Route of elimination | Not Available | ||||||
| Toxicity | Topically applied clocortolone can be absorbed in sufficient amounts to produce systemic effects. Symptoms of overdose include thinning of skin and suppression of adrenal cortex (decreased ability to respond to stress). | ||||||
| Affected organisms |
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| Interactions | |||||||
| Drug Interactions |
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| Food Interactions | Not Available | ||||||
Targets
| Glucocorticoid receptor | |
|---|---|
| Name | Glucocorticoid receptor |
| Gene Name | NR3C1 |
| Pharmacological action | yes |
| Actions | agonist |
| References |
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| DTHybrid score | 0.778 |