药品详细
Meloxicam (美洛昔康 )
化学结构式图
中文名
美洛昔康
英文名
Meloxicam
分子式
Not Available
化学名
4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-2H-1$l^{6},2-benzothiazine-3-carboxamide
分子量
Average: 351.401
Monoisotopic: 351.034747299
Monoisotopic: 351.034747299
CAS号
71125-38-7
ATC分类
M01A 未知
药物类型
small molecule
阶段
商品名
Apo-meloxicam;Co Meloxicam;Dom-meloxicam;Gen-meloxicam;Metacam;Mobic;Mobicox;Movalis;Movatec;Novo-meloxicam;Parocin;PHL-meloxicam;PMS-meloxicam;Ratio-meloxicam;Tenaron;
同义名
Meloxicamum [latin];
基本介绍
Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve the symptoms of arthritis, primary dysmenorrhea, fever; and as an analgesic, especially where there is an inflammatory component. It is closely related to piroxicam. In Europe it is marketed under the brand names Movalis, Melox, and Recoxa. In North America it is generally marketed under the brand name Mobic. In Latin America, the drug is marketed as Tenaron. [Wikipedia]
生产厂家
- Actavis totowa llc
- Apotex inc etobicoke site
- Aurobindo pharma ltd
- Beijing double crane pharmaceutical co ltd
- Beijing yabao biopharmaceutical co ltd
- Boehringer ingelheim pharmaceuticals inc
- Breckenridge pharmaceutical inc
- Caraco pharmaceutical laboratories ltd
- Carlsbad technology inc
- Corepharma llc
- Dr reddys laboratories inc
- Genpharm inc
- Glenmark generics ltd
- Lupin pharmaceuticals inc
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Roxane laboratories inc
- Strides arcolab ltd
- Taro pharmaceutical industries ltd
- Teva pharmaceuticals usa
- Unichem laboratories ltd
- Watson laboratories inc
- Zydus pharmaceuticals usa inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Suspension | Oral | 7.5 mg/5 ml |
| Tablet | Oral | 15 mg |
| Tablet | Oral | 7.5 mg |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Meloxicam 7.5 mg/5ml Suspension 100ml Bottle | 86.99 USD | bottle |
| Meloxicam bp powder | 56.61 USD | g |
| Mobic 15 mg tablet | 7.37 USD | tablet |
| Meloxicam 15 mg tablet | 4.94 USD | tablet |
| Mobic 7.5 mg tablet | 4.74 USD | tablet |
| Meloxicam 7.5 mg tablet | 3.23 USD | tablet |
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
ANTIINFLAMMATORY AND ANTIRHEUMATIC 消炎抗风湿;
药理
| Indication | For symptomatic treatment of arthritis and osteoarthritis. | ||||||
| Pharmacodynamics | Meloxicam is an nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Prostaglandins are substances that contribute to inflammation of joints. Meloxicam inhibits prostaglandin synthetase (cylooxygenase 1 and 2) and leads to a decrease of the synthesis of prostaglandins, therefore, inflammation is reduced. | ||||||
| Mechanism of action | Anti-inflammatory effects of meloxicam are believed to be due to inhibition of prostaglandin synthetase (cylooxygenase), leading to the inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis may be associated with the analgesic and antipyretic effects of meloxicam. | ||||||
| Absorption | Absolute bioavailability = 89% | ||||||
| Volume of distribution |
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| Protein binding | 99.4% bound, primarily to albumin | ||||||
| Metabolism |
Meloxicam is almost completely metabolized into inactive metabolites by the cytochrome P450 (CYP450) isozymes. CYP2C9 is primarily responsible for metabolism of meloxicam while CYP3A4 plays a minor role. An intermediate metabolite, 5'-hydroxymethyl meloxicam, is further metabolized to 5'-carboxy meloxicam, the major metabolite. Peroxidase activity is thought to produce the two other inactive metabolites of meloxicam. |
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| Route of elimination | Meloxicam is almost completely metabolized to four pharmacologically inactive metabolites. Meloxicam excretion is predominantly in the form of metabolites, and occurs to equal extents in the urine and feces. Only traces of the unchanged parent compound are excreted in the urine (0.2%) and feces (1.6%). The extent of the urinary excretion was confirmed for unlabeled multiple 7.5 mg doses: 0.5%, 6% and 13% of the dose were found in urine in the form of meloxicam, and the 5'-hydroxymethyl and 5'-carboxy metabolites, respectively. | ||||||
| Half life | 15-20 hours | ||||||
| Clearance |
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| Toxicity | LD50, Acute: 84 mg/kg (Rat); Oral 470 mg/kg (Mouse); Oral 320 mg/kg (Rabbit) | ||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 254 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | Meloxicam may increase the anticoagulant effect of acenocoumarol. |
| Anisindione | Meloxicam may increase the anticoagulant effect of anisindione. |
| Dicumarol | Meloxicam may increase the anticoagulant effect of dicumarol. |
| Ginkgo biloba | Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. |
| Lithium | Meloxicam increases serum levels of lithium |
| Telmisartan | Concomitant use of Telmisartan and Meloxicam may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment. |
| Timolol | The NSAID, Meloxicam, may antagonize the antihypertensive effect of Timolol. |
| Trandolapril | The NSAID, Meloxicam, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Meloxicam is initiated, discontinued or dose changed. |
| Treprostinil | The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meloxicam. Monitor for increased bleeding during concomitant thearpy. |
| Voriconazole | Voriconazole may increase the serum concentration of meloxicam by decreasing its metabolism via CYP2C9 and CYP3A4. Monitor for changes in the therapeutic and adverse effects of meloxicam if voriconazole is initiated, discontinued or dose changed. |
| Warfarin | The antiplatelet effects of meloxicam may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy. |
食物相互作用
- Take without regard to meals.
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