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酮咯酸。对其药效学和药代动力学特性以及治疗潜力的综述。

Ketorolac. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential.

作者信息

Buckley M M, Brogden R N

机构信息

ADIS Drug Information Services, Auckland, New Zealand.

出版信息

Drugs. 1990 Jan;39(1):86-109. doi: 10.2165/00003495-199039010-00008.

DOI:10.2165/00003495-199039010-00008
PMID:2178916
Abstract

Ketorolac is a non-steroidal agent with potent analgesic and moderate anti-inflammatory activity. It is administered as the tromethamine salt orally, intramuscularly, intravenously, and as a topical ophthalmic solution. Clinical studies indicate single-dose efficacy greater than that of morphine, pethidine (meperidine) and pentazocine in moderate to severe postoperative pain, with some evidence of a more favourable adverse effect profile than morphine or pethidine. In single-dose studies ketorolac has also compared favourably with aspirin, paracetamol (acetaminophen) and a few other non-steroidal anti-inflammatory drugs. If further investigation confirms the initially favourable findings regarding efficacy and tolerability, ketorolac will be a useful alternative to opioid agents in postsurgical pain. It may well also find use in acute musculoskeletal pain, where it appears at least as effective as other agents with which it has been compared. From the limited clinical data available, ketorolac also seems promising in the treatment of ocular inflammatory conditions. Additional multiple-dose studies are required to evaluate fully the potential of ketorolac in the management of chronic pain states where it has shown superior efficacy to aspirin. In summary, ketorolac offers promise as an alternative to opioid and to other nonsteroidal analgesics in ameliorating moderate to severe postsurgical pain, and with wider clinical experience may find a place in the treatment of acute musculoskeletal and other pain states, and ocular inflammatory conditions.

摘要

酮咯酸是一种具有强效镇痛和中度抗炎活性的非甾体类药物。它以 tromethamine 盐的形式口服、肌内注射、静脉注射,并制成局部眼科溶液使用。临床研究表明,在中度至重度术后疼痛中,酮咯酸单剂量的疗效优于吗啡、哌替啶(度冷丁)和喷他佐辛,并且有证据表明其不良反应谱比吗啡或哌替啶更有利。在单剂量研究中,酮咯酸与阿司匹林、对乙酰氨基酚(扑热息痛)及其他一些非甾体类抗炎药相比也具有优势。如果进一步的研究证实了最初关于疗效和耐受性的良好发现,酮咯酸将成为术后疼痛中阿片类药物的有用替代品。它很可能也可用于急性肌肉骨骼疼痛,在这方面它似乎至少与已与其比较的其他药物一样有效。从现有的有限临床数据来看,酮咯酸在治疗眼部炎症性疾病方面似乎也很有前景。需要进行更多的多剂量研究,以全面评估酮咯酸在治疗慢性疼痛状态方面的潜力,在这些慢性疼痛状态中它已显示出优于阿司匹林的疗效。总之,酮咯酸有望成为阿片类药物和其他非甾体类镇痛药的替代品,用于缓解中度至重度术后疼痛,随着临床经验的积累,它可能在急性肌肉骨骼疼痛和其他疼痛状态以及眼部炎症性疾病的治疗中占有一席之地。

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Ketorolac for postoperative pain management in children.酮咯酸用于儿童术后疼痛管理
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Optimizing pain management and pupil dilation in cataract surgery: a systematic review and meta-analysis of phenylephrine/ketorolac (OMIDRIA®).优化白内障手术中的疼痛管理和瞳孔散大:去氧肾上腺素/酮咯酸(OMIDRIA®)的系统评价和荟萃分析
Graefes Arch Clin Exp Ophthalmol. 2025 Mar 29. doi: 10.1007/s00417-025-06811-y.
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Anaphylactic shock induced by intravenous ketorolac: A case report.静脉注射酮咯酸诱发过敏性休克:一例报告。

本文引用的文献

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The analgesic and anti-inflammatory profile of (+/-)-5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2a]pyrrole-1-carboxylic acid (RS-37619).(±)-5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1-羧酸(RS-37619)的镇痛和抗炎特性
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Anti-inflammatory and analgetic properties of d-2-(6'-methoxy-2'-naphthyl)-propionic acid (naproxen).d-2-(6'-甲氧基-2'-萘基)丙酸(萘普生)的抗炎和镇痛特性。
J Pharmacol Exp Ther. 1971 Oct;179(1):114-23.
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The analgesic and anti-inflammatory profile of ketorolac and its tromethamine salt.
Heliyon. 2025 Jan 28;11(3):e42236. doi: 10.1016/j.heliyon.2025.e42236. eCollection 2025 Feb 15.
4
Characterization of HPMC and PEG 400 Mucoadhesive Film Loaded with Retinyl Palmitate and Ketorolac for Intravaginal Administration.用于阴道给药的负载棕榈酸视黄酯和酮咯酸的羟丙基甲基纤维素及聚乙二醇400黏膜黏附膜的特性研究
Int J Mol Sci. 2024 Nov 26;25(23):12692. doi: 10.3390/ijms252312692.
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Revisiting and Updating the Interaction between Human Serum Albumin and the Non-Steroidal Anti-Inflammatory Drugs Ketoprofen and Ketorolac.重新审视和更新人血清白蛋白与非甾体抗炎药酮洛芬和酮咯酸的相互作用。
Molecules. 2024 Jun 24;29(13):3001. doi: 10.3390/molecules29133001.
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The Additive Antinociceptive Effect of Resveratrol and Ketorolac in the Formalin Test in Mice.白藜芦醇与酮咯酸在小鼠福尔马林试验中的相加镇痛作用
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Prog Biomater. 2023 Mar;12(1):25-40. doi: 10.1007/s40204-022-00210-w. Epub 2022 Nov 8.
8
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酮咯酸及其 tromethamine 盐的镇痛和抗炎特性。
Drugs Exp Clin Res. 1985;11(8):479-92.
4
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Ketorolac tromethamine as compared with morphine sulfate for treatment of postoperative pain.酮咯酸氨丁三醇与硫酸吗啡用于治疗术后疼痛的比较。
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Effectiveness of ketorolac tromethamine 0.5% ophthalmic solution for chronic aphakic and pseudophakic cystoid macular edema.0.5%酮咯酸氨丁三醇滴眼液治疗慢性无晶状体眼和人工晶状体眼黄斑囊样水肿的有效性
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A multiple-dose comparison of ketorolac tromethamine with diflunisal and placebo in postmeniscectomy pain.
J Clin Pharmacol. 1986 Nov-Dec;26(8):700-5. doi: 10.1002/j.1552-4604.1986.tb02976.x.
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Ketorolac and acetaminophen for orthopedic postoperative pain.
Clin Pharmacol Ther. 1986 Jan;39(1):89-93. doi: 10.1038/clpt.1986.15.