药品详细
Ketorolac (酮咯酸 )
化学结构式图
中文名
酮咯酸
英文名
Ketorolac
分子式
Not Available
化学名
5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
分子量
Average: 255.2686
Monoisotopic: 255.089543287
Monoisotopic: 255.089543287
CAS号
66635-83-4
ATC分类
M01A 未知;S01B 抗炎药
药物类型
small molecule
阶段
商品名
Acular;Acular LS;Acular Preservative Free;Toradol;
同义名
Ketoralac;Ketorolac Tromethamine;Ketorolaco [Spanish];Ketorolacum [Latin];
基本介绍
A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)
生产厂家
- Akorn inc
- Akorn strides llc
- Alcon inc
- Allergan
- Allergan inc
- Amphastar pharmaceutical inc
- Apotex inc richmond hill
- Apothecon inc div bristol myers squibb
- App pharmaceuticals llc
- Baxter healthcare corp anesthesia and critical care
- Baxter healthcare corp anesthesia critical care
- Bedford laboratories div ben venue laboratories inc
- Claris lifesciences ltd
- Gland pharma ltd
- Hospira inc
- Luitpold pharmaceuticals inc
- Mylan pharmaceuticals inc
- Pliva inc
- Roche palo alto llc
- Roxane laboratories inc
- Roxro pharma inc
- Sandoz canada inc
- Sun pharma global inc
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- Wockhardt ltd
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Liquid | Intramuscular | |
| Solution | Intramuscular | |
| Solution | Ophthalmic | |
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Acular 0.5% Solution 10ml Bottle | 254.39 USD | bottle |
| Acular 0.5% Solution 5ml Bottle | 122.36 USD | bottle |
| Ketorolac Tromethamine 0.4% Solution 5ml Bottle | 109.72 USD | bottle |
| Ketorolac tromethamine powder | 71.05 USD | g |
| Acular 0.5% Solution 3ml Bottle | 59.34 USD | bottle |
| Acular ls 0.4% ophth sol | 24.46 USD | ml |
| Acular 0.5% eye drops | 18.68 USD | ml |
| Ketorolac 30 mg/ml syringe | 8.77 USD | ml |
| Ketorolac 15 mg/ml syringe | 8.39 USD | ml |
| Acuvail 0.45% ophth solution | 4.17 USD | each |
| Ketorolac Tromethamine 30 mg/ml | 3.9 USD | ml |
| Acular 0.5 % Solution | 3.78 USD | ml |
| Toradol 10 mg/ml | 2.52 USD | ml |
| Ketorolac im 30 mg/ml syring | 2.11 USD | ml |
| Apo-Ketorolac 0.5 % Solution | 2.11 USD | ml |
| Ratio-Ketorolac 0.5 % Solution | 2.11 USD | ml |
| Toradol 10 mg tablet | 1.53 USD | tablet |
| Ketorolac Tromethamine 10 mg tablet | 1.06 USD | tablet |
| Ketorolac 10 mg tablet | 0.93 USD | tablet |
| Toradol 10 mg Tablet | 0.76 USD | tablet |
| Apo-Ketorolac 10 mg Tablet | 0.43 USD | tablet |
| Novo-Ketorolac 10 mg Tablet | 0.43 USD | tablet |
| Nu-Ketorolac 10 mg Tablet | 0.43 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 the short-term (~5 days) management of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting. | ||||||
| Pharmacodynamics | Ketorolac, an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain. It is a peripherally acting analgesic. The biological activity of ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine possesses no sedative or anxiolytic properties. | ||||||
| Mechanism of action | Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to indomethacin and tolmetin. Ketorolac tromethamine is a racemic mixture of [-]S- and [+]R-enantiomeric forms, with the S-form having analgesic activity. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis leading to decreased formation of precursors of prostaglandins and thromboxanes from arachidonic acid. The resultant reduction in prostaglandin synthesis and activity may be at least partially responsible for many of the adverse, as well as the therapeutic, effects of these medications. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity. However, inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation may also contribute to the analgesic effect. In terms of the ophthalmic applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels in aqueous humor, secondary to inhibition of prostaglandin biosynthesis. | ||||||
| Absorption | Rapidly and completely absorbed after oral administration | ||||||
| Volume of distribution |
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| Protein binding | 99% | ||||||
| Metabolism |
Primarily hepatic. Less than 50% of a dose is metabolized. The major metabolites are a glucuronide conjugate, which may also be formed in the kidney, and p-hydroxy ketorolac. Neither metabolite has significant analgesic activity. |
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| Route of elimination | The principal route of elimination of ketorolac and its metabolites is renal. Approximately 6% of a dose is excreted in the feces. | ||||||
| Half life | 2.5 hours for the S-enantiomer compared with 5 hours for the R-enantiomer | ||||||
| Clearance |
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| Toxicity | LD50 = 189 mg/kg (rat, oral). | ||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 165-167 oC (tromethamine salt) | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The NSAID, ketorolac, may increase the anticoagulant effect of acenocoumarol. |
| Acetylsalicylic acid | Acetylsalicylic acid may increase the adverse GI effects ketorolac. |
| Alendronate | Increased risk of gasrtic toxicity |
| Anisindione | The NSAID, ketorolac, may increase the anticoagulant effect of anisindione. |
| Dicumarol | The NSAID, ketorolac, may increase the anticoagulant effect of dicumarol. |
| Ginkgo biloba | Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided. |
| Ketoprofen | Concomitant use of ketoprofen and ketorolac, two NSAIDs, is contraindicated due to the risk of additive or synergistic NSAID toxicities (e.g. GI bleeding, ulceration, renal dysfunction, etc). |
| Lithium | The NSAID, ketorolac, may decrease the renal excretion of lithium. Increased risk of lithium toxicity. |
| Methotrexate | The NSAID, ketorolac, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity. |
| Probenecid | Probenecid increases toxicity of ketorolac |
| Sulindac | May cause additive or synergistic NSAID toxicities (e.g. GI bleeding, renal dysfunction, etc.). Concomitant therapy is contraindicated. |
| Telmisartan | Concomitant use of Telmisartan and Ketorolac may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment. |
| Tiaprofenic acid | Concomitant therapy is contraindicated due to the risk of synergistic NSAID toxicity. |
| Timolol | The NSAID, Ketorolac, may antagonize the antihypertensive effect of Timolol. |
| Tolmetin | Risk of adverse NSAID toxic effects (e.g. GI bleeding, renal dysfunction). Concomitant therapy is contraindicated. |
| Trandolapril | The NSAID, Ketorolac, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Ketorolac is initiated, discontinued or dose changed. |
| Treprostinil | The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketorolac. Monitor for increased bleeding during concomitant thearpy. |
| Warfarin | The antiplatelet effects of ketorolac 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 with food to reduce GI irritation
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