DB00663 - Flumethasone Pivalate
| Identification | |
|---|---|
| Name | Flumethasone Pivalate |
| Accession Number | DB00663 (APRD00975) |
| Type | small molecule |
| Description | Flumethasone pivalate is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic and vasoconstrictive properties. As it is a privalate salt, its anti-inflammatory action is concentrated at the site of application. This local effect on diseased areas results in a prompt decrease in inflammation, exudation and itching. |
| Structure |
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| Categories (*) | |
| Molecular Weight | 494.5679 |
| Groups | approved |
| Monoisotopic Weight | 494.247995294 |
| Pharmacology | |
| Indication | For the treatment of contact dermatitis, atopic dermatitis, exczema, psoriasis, diaper rash and other skin conditions |
| Mechanism of action | Flumethasone is a glucocorticoid receptor agonist. This complex binds to the nucleus causing a variety of genetic activation and repressions. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Flumethasone binds to plasma transcortin, and it becomes active when it is not bound to transcortin. |
| Absorption | Minimal if applied topically |
| Protein binding | Not Available |
| Biotransformation | Primarily hepatic |
| Route of elimination | Not Available |
| Toxicity | Can lead to signs of irritation such as burning sensation, itching or skin rash at the site of application; hypersensitivity reactions. |
| Affected organisms |
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| Interactions | |
| Drug Interactions | Not Available |
| 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 | 1.1669 |