药品详细
Clobetasol(氯倍他索)
化学结构式图
中文名
氯倍他索
英文名
Clobetasol
分子式
C22H28ClFO4
化学名
(1R,2S,10S,11S,13S,14R,15S,17S)-14-(2-chloroacetyl)-1-fluoro-14,17-dihydroxy-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
分子量
Average: 410.907
Monoisotopic: 410.166015296
Monoisotopic: 410.166015296
CAS号
25122-46-7
ATC分类
D07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A derivative of prednisolone with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than fluocinonide, it is used topically in treatment of psoriasis but may cause marked adrenocortical suppression. [PubChem]
生产厂家
- Actavis mid atlantic llc
- Altana inc
- Connetics corp
- E fougera div altana inc
- Galderma laboratories inc
- Galderma laboratories l p
- Galderma laboratories lp
- Hi tech pharmacal co inc
- Nycomed us inc
- Perrigo co
- Perrigo israel pharmaceuticals ltd
- Stiefel a gsk co
- Stiefel laboratories inc
- Taro pharmaceuticals inc
- Taro pharmaceuticals usa inc
- Teva pharmaceuticals usa
- Tolmar inc
- Wockhardt eu operations (swiss) ag
封装厂家
- Accra Pac Inc.
- Ameri-Pac Inc.
- A-S Medication Solutions LLC
- Contract Pharm
- Dermalogix
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- DPT Laboratories Ltd.
- E. Fougera and Co.
- Galderma Laboratories
- GlaxoSmithKline Inc.
- Glenmark Generics Ltd.
- Hi Tech Pharmacal Co. Inc.
- Inyx Usa Ltd.
- Nycomed Inc.
- Palmetto Pharmaceuticals Inc.
- Perrigo Co.
- Pharma Pac LLC
- Pharmaderm
- Pharmedix
- Physicians Total Care Inc.
- Prasco Labs
- Preferred Pharmaceuticals Inc.
- Quality Care
- Rebel Distributors Corp.
- Stat Rx Usa
- Stiefel Labs
- Taro Pharmaceuticals USA
- Teva Pharmaceutical Industries Ltd.
- Watson Pharmaceuticals
- Wockhardt Ltd.
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes | Not Available |
| Substructures | Not Available |
适应症
药理
| Indication | For short-term topical treatment of the inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp. |
| Pharmacodynamics | Like other topical corticosteroids, clobetasol has anti-inflammatory, antipruritic, and vasoconstrictive properties. It is a very high potency 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. Initially, however, clobetasol, like other corticosteroids, bind to the glucocorticoid receptor, which complexes, enteres the cell nucleus and modifies genetic transcription (transrepression/transactivation). |
| 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 | Not Available |
| Metabolism |
Metabolized, primarily in the liver, and then excreted by the kidneys.
|
| Route of elimination | 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. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Oral LD50 in rat and mouse is >3000 mg/kg. Topically applied clobetasol 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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| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Aldesleukin | Corticosteroids such as clobetasol may diminish the antineoplastic effect of aldesleukin. Avoid conccurent use of corticosteroids with aldesleukin. |
| Telaprevir | Corticosteroids such as clobetasol may decrease the serum concentration of telaprevir. Telaprevir may increase the serum concentration of corticosteroids. Concurrent use of telaprevir and systemic corticosteroids is not recommended. When possible, consider alternatives, and if such a combination is necessary, use extra caution, monitoring patients for excessive systemic steroid effects as well as for diminished telaprevir effects. |
食物相互作用
Not Available
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