|Accession Number||DB00223 (APRD00921)|
Diflorasone is a topical corticosteroid used to treat itching and inflammation of the skin.
|Brand mixtures||Not Available|
|Mass Spec||Not Available|
|Class||Steroids and Steroid Derivatives|
|Subclass||Gluco/mineralocorticoids, Progestogins and Derivatives|
|Direct parent||Gluco/mineralocorticoids, Progestogins and Derivatives|
|Alternative parents||Hydroxysteroids; Ketosteroids; Halogenated Steroids; Iridoids and Derivatives; Cyclohexanols; Tertiary Alcohols; Cyclic Alcohols and Derivatives; Ketones; Fluorohydrins; Polyamines; Enolates; Primary Alcohols; Organofluorides; Alkyl Fluorides; Aldehydes|
|Substituents||3-keto-steroid; 20-keto-steroid; 9-halo-steroid; 6-halo-steroid; 17-hydroxy-steroid; 11-hydroxy-steroid; 11-noriridane monoterpene; monoterpene; cyclohexanol; tertiary alcohol; cyclic alcohol; secondary alcohol; ketone; halohydrin; fluorohydrin; polyamine; enolate; primary alcohol; alcohol; organofluoride; organohalogen; carbonyl group; alkyl halide; alkyl fluoride; aldehyde|
|Classification description||This compound belongs to the gluco/mineralocorticoids, progestogins and derivatives. These are steroids whose structure is based on an hydroxylated prostane moiety.|
|Indication||For relief of the inflammatory and pruritic manifestations of corticosteroid responsive dermatoses.|
|Pharmacodynamics||Like other topical corticosteroids, diflorasone has anti-inflammatory, antipruritic, and vasoconstrictive properties. Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Diflorasone is a potent topical corticosteroid that should not be used with occlusive dressings. It is recommended that treatment should be limited to 2 consecutive weeks and therapy should be discontinued when adequate results have been achieved.|
|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.|
|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.|
|Volume of distribution||Not Available|
|Protein binding||Bound to plasma proteins in varying degrees.|
Metabolized, primarily in the liver, and then excreted by the kidneys.
|Route of elimination||Not Available|
|Half life||Not Available|
|Toxicity||Topically applied diflorasone 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).|
|SNP Mediated Effects||Not Available|
|SNP Mediated Adverse Drug Reactions||Not Available|
|Predicted ADMET features|
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Lincoln, F.H., Schneider, W.P. and Spero, G.B.; U.S. Patent 3,557,158; January 19,1971; assigned to The Upjohn Company.
|General Reference||Not Available|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||show(26.8 KB)|
|Drug Interactions||Not Available|
|Food Interactions||Not Available|
Pharmacological action: yes
- Pearce DJ, Spencer L, Hu J, Balkrishnan R, Fleischer AB Jr, Feldman SR: Class I topical corticosteroid use by psoriasis patients in an academic practice. J Dermatolog Treat. 2004 Jul;15(4):235-8. Pubmed