药品详细
Valdecoxib (戊地昔布 )
化学结构式图
中文名
戊地昔布
英文名
Valdecoxib
分子式
Not Available
化学名
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide
分子量
Average: 314.359
Monoisotopic: 314.072513014
Monoisotopic: 314.072513014
CAS号
181695-72-7
ATC分类
M01A 未知
药物类型
small molecule
阶段
商品名
Bextra;
同义名
valdecoxib;
基本介绍
Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke.
生产厂家
- Gd searle llc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
化合物类型
| Type | small molecule |
| Classes | Not Available |
| Substructures | Not Available |
适应症
ANTIINFLAMMATORY AND ANTIRHEUMATIC 消炎抗风湿;
药理
| Indication | For the treatment of osteoarthritis and dysmenorrhoea | ||||||||||||||||||||||||||||||||||||||||
| Pharmacodynamics | Valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib is used for its anti-inflammatory, analgesic, and antipyretic activities in the management of osteoarthritis (OA) and for the treatment of dysmenorrhea or acute pain. Unlike celecoxib, valdecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism. | ||||||||||||||||||||||||||||||||||||||||
| Mechanism of action | Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does not inhibit platelet aggregation. | ||||||||||||||||||||||||||||||||||||||||
| Absorption | Oral bioavailability is 83%. | ||||||||||||||||||||||||||||||||||||||||
| Volume of distribution |
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| Protein binding | 98% | ||||||||||||||||||||||||||||||||||||||||
| Metabolism |
Hepatic (involves CYP3A4 and 2C9)
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| Route of elimination | Valdecoxib is eliminated predominantly via hepatic metabolism with less than 5% of the dose excreted unchanged in the urine and feces. About 70% of the dose is excreted in the urine as metabolites, and about 20% as valdecoxib N-glucuronide. | ||||||||||||||||||||||||||||||||||||||||
| Half life | 8-11 hours | ||||||||||||||||||||||||||||||||||||||||
| Clearance |
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| Toxicity | Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare. | ||||||||||||||||||||||||||||||||||||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Fluconazole | Fluconazole may increase the effect and toxicity of valdecoxib. |
| Ketoconazole | Ketoconazole may increase the effect and toxicity of valdecoxib. |
| Lithium | The COX-2 inhibitor increases serum levels of lithium |
食物相互作用
Not Available
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