Litvak K M, McEvoy G K
AHFS Drug Information, American Society of Hospital Pharmacists, Bethesda, MD 20814.
Clin Pharm. 1990 Dec;9(12):921-35.
Clinical studies of the injectable nonsteroidal anti-inflammatory agent (NSAIA) ketorolac tromethamine are reviewed, and the chemistry, pharmacology, pharmacokinetics, drug interactions, and adverse effects of ketorolac are described. Ketorolac exhibits anti-inflammatory, analgesic, and antipyretic activity. Although the exact mechanisms of action have not been determined, its effects appear to be associated principally with the inhibition of prostaglandin synthesis. After oral, i.m., or i.v. administration, ketorolac and its metabolites are excreted mainly in urine. Ketorolac tromethamine has been used for the symptomatic relief of moderate to severe postoperative pain, including that associated with abdominal, gynecologic, oral, orthopedic, or urologic surgery. Ketorolac has also been used for the relief of acute renal colic, pain associated with trauma, and visceral pain associated with cancer. When administered i.m., ketorolac produced analgesia comparable to that of i.m. doses of meperidine, pentazocine, or morphine. The most common adverse effects associated with short-term administration are nervous system and gastrointestinal effects; these are usually mild and occur in about 39% of patients. Unlike opiate analgesics, ketorolac does not appear to cause tolerance or physical dependence in patients receiving long-term therapy. Ketorolac tromethamine has been administered concomitantly with morphine or meperidine without apparent adverse interaction. For short-term pain management, an initial i.m. ketorolac tromethamine loading dose of 30 or 60 mg is recommended. Ketorolac tromethamine appears to be as effective as morphine or meperidine for short-term management of moderate to severe postoperative pain. It lacks the respiratory depressant effects of opiate analgesics but shares the toxic potentials of other NSAIAs.
本文回顾了注射用非甾体抗炎药（NSAIA）酮咯酸氨丁三醇的临床研究，并描述了酮咯酸的化学、药理、药代动力学、药物相互作用及不良反应。酮咯酸具有抗炎、镇痛和解热活性。尽管确切作用机制尚未明确，但其作用似乎主要与抑制前列腺素合成有关。口服、肌内注射或静脉注射后，酮咯酸及其代谢产物主要经尿液排泄。酮咯酸氨丁三醇已用于中度至重度术后疼痛的症状缓解，包括与腹部、妇科、口腔、骨科或泌尿外科手术相关的疼痛。酮咯酸也用于缓解急性肾绞痛、创伤相关疼痛及癌症相关的内脏疼痛。肌内注射时，酮咯酸产生的镇痛效果与肌内注射度冷丁、喷他佐辛或吗啡相当。短期给药最常见的不良反应是神经系统和胃肠道反应；这些反应通常较轻，约39%的患者会出现。与阿片类镇痛药不同，酮咯酸在接受长期治疗的患者中似乎不会引起耐受性或身体依赖性。酮咯酸氨丁三醇已与吗啡或度冷丁联合使用，未出现明显不良相互作用。对于短期疼痛管理，建议初始肌内注射酮咯酸氨丁三醇负荷剂量为30或60mg。酮咯酸氨丁三醇在短期管理中度至重度术后疼痛方面似乎与吗啡或度冷丁一样有效。它缺乏阿片类镇痛药的呼吸抑制作用，但具有其他非甾体抗炎药的潜在毒性。
