药品详细
Etodolac (依托度酸 )
化学结构式图
中文名
依托度酸
英文名
Etodolac
分子式
Not Available
化学名
2-{1,8-diethyl-1H,3H,4H,9H-pyrano[3,4-b]indol-1-yl}acetic acid
分子量
Average: 287.3535
Monoisotopic: 287.152143543
Monoisotopic: 287.152143543
CAS号
41340-25-4
ATC分类
M01A 未知
药物类型
small molecule
阶段
商品名
Etodolac [Usan:Ban:Inn];Etodolacetodolic acid;Etodolaco [INN-Spanish];Etodolacum [INN-Latin];Etodolic Acid;Lodine;Lodine XL;Ultradol;
同义名
etodolac;
基本介绍
Etodolac is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic properties. Its therapeutic effects are due to its ability to inhibit prostaglandin synthesis. It is indicated for relief of signs and symptoms of rheumatoid arthritis and osteoarthritis.
生产厂家
- Aaipharma llc
- Actavis elizabeth llc
- Apotex inc
- Apotex inc etobicoke site
- Endo pharmaceuticals inc
- Genpharm inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Mylan laboratories inc
- Mylan pharmaceuticals inc
- Point holdings inc
- Ranbaxy laboratories ltd
- Sandoz inc
- Taro pharmaceutical industries ltd
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- Watson laboratories inc florida
- Wyeth pharmaceuticals inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Capsule | Oral | 200 mg |
| Capsule | Oral | 300 mg |
| Tablet | Oral | 400 mg |
| Tablet | Oral | 500 mg |
| Tablet, extended release | Oral | 400 mg |
| Tablet, extended release | Oral | 500 mg |
| Tablet, extended release | Oral | 600 mg |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Etodolac CR 600 mg 24 Hour tablet | 2.76 USD | tablet |
| Lodine 400 mg tablet | 2.65 USD | tablet |
| Lodine 500 mg tablet | 1.8 USD | tablet |
| Etodolac CR 500 mg 24 Hour tablet | 1.6 USD | tablet |
| Etodolac 500 mg tablet | 1.52 USD | tablet |
| Etodolac 400 mg tablet | 1.5 USD | tablet |
| Etodolac CR 400 mg 24 Hour tablet | 1.46 USD | tablet |
| Etodolac 300 mg capsule | 1.31 USD | capsule |
| Apo-Etodolac 200 mg Capsule | 0.8 USD | capsule |
| Apo-Etodolac 300 mg Capsule | 0.8 USD | capsule |
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 acute and long-term management of signs and symptoms of osteoarthritis and rheumatoid arthritis, as well as for the management of pain. | |||||||||||||||||||||||||||||||||||
| Pharmacodynamics | Etodolac is an anti-inflammatory agent with analgesic and antipyretic properties. It is used to treat osteoarthritis, rheumatoid arthritis and control acute pain. The therapeutic effects of etodolac are achieved via inhibition of the synthesis of prostaglandins involved in fever, pain, swelling and inflammation. Etodolac is administered as a racemate. As with other NSAIDs, the S-form has been shown to be active while the R-form is inactive. Both enantiomers are stable and there is no evidence of R- to S- conversion in vivo. | |||||||||||||||||||||||||||||||||||
| Mechanism of action | Similar to other NSAIDs, the anti-inflammatory effects of etodolac result from inhibition of the enzyme cycooxygenase (COX). This decreases the synthesis of peripheral prostaglandins involved in mediating inflammation. Etodolac binds to the upper portion of the COX enzyme active site and prevents its substrate, arachidonic acid, from entering the active site. Etodolac was previously thought to be a non-selective COX inhibitor, but it is now known to be 5 – 50 times more selective for COX-2 than COX-1. Antipyresis may occur by central action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat loss. | |||||||||||||||||||||||||||||||||||
| Absorption | Based on mass balance studies, the systemic bioavailability of etodolac from either the tablet or capsule formulation is at least 80%. | |||||||||||||||||||||||||||||||||||
| Volume of distribution |
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| Protein binding | > 99% bound, primarily to albumin | |||||||||||||||||||||||||||||||||||
| Metabolism |
Etodolac is extensively metabolized in the liver. Renal elimination of etodolac and its metabolites is the primary route of excretion (72%). Metabolites found in urine (with percents of the administered dose) are: unchanged etodolac (1%), etodolac glucuronide (13%), hydroxylated metabolites (6-, 7-, and 8-OH; 5%), hydroxylated metabolite glucuronides (20%), and unidentified metabolites (33%). Fecal excretion accounts for 16% of its elimination.
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| Route of elimination | It is not known whether etodolac is excreted in human milk; however, based on its physical-chemical properties, excretion into breast milk is expected. Etodolac is extensively metabolized in the liver. The hydroxylated-etodolac metabolites undergo further glucuronidation followed by renal excretion and partial elimination in the feces (16% of dose). Approximately 1% of a etodolac dose is excreted unchanged in the urine with 72% of the dose excreted into urine as parent drug plus metabolite. | |||||||||||||||||||||||||||||||||||
| Half life | Terminal t1/2, 7.3 ± 4.0 hours. Distribution t1/2, 0.71 ± 0.50 hours | |||||||||||||||||||||||||||||||||||
| Clearance |
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| Toxicity | Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of etodolac. Etodolac may increase blood pressure and/or cause fluid retention and edema. Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Anaphylactoid and serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) have been reported. Common adverse events include abdominal pain, constipation, diarrhea, dyspepsia, flatulence, GI bleeding, GI perforation, nausea, peptic ulcer, vomiting, renal function abnormalities, anemia, dizziness, edema, liver function test abnormalities, headache, prolonged bleeding time, pruritus, rash, tinnitus. Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain. | |||||||||||||||||||||||||||||||||||
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 145-148 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The NSAID, etodolac, may increase the anticoagulant effect or acenocoumarol. |
| Alendronate | Increased risk of gastric toxicity |
| Anisindione | The NSAID, etodolac, may increase the anticoagulant effect of anisindione. |
| Cyclosporine | Monitor for nephrotoxicity |
| Dicumarol | The NSAID, etodolac, may increase the anticoagulant effect of dicumarol. |
| Ginkgo biloba | Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. |
| Methotrexate | The NSAID, etodolac, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity. |
| Timolol | The NSAID, Etodolac, may antagonize the antihypertensive effect of Timolol. |
| Trandolapril | The NSAID, Etodolac, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Etodolac is initiated, discontinued or dose changed. |
| Treprostinil | The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Etodolac. Monitor for increased bleeding during concomitant thearpy. |
| Warfarin | The antiplatelet effects of etodolac 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
- Avoid alcohol.
- Food increases the peak plasma concentration of extended-release tablets with no effect on extent of absorption.
- Food increases the time to peak concentration of regular release oral formulations by 1.4 to 3.8 hours with no effect on extent of absorption.
- Take with food to reduce gastric irritation.
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