Resman-Targoff B H
Department of Pharmacy Practice, College of Pharmacy, University of Oklahoma, Oklahoma City 73190.
DICP. 1990 Nov;24(11):1098-104. doi: 10.1177/106002809002401115.
Ketorolac tromethamine is a pyrrolo-pyrrole nonsteroidal antiinflammatory drug (NSAID) with potent analgesic effects when administered intramuscularly for the treatment of acute pain. Ketorolac is well absorbed and has a rapid onset of action. Maximum plasma concentrations are achieved in 45-50 minutes and peak analgesic effects in about one to two hours following intramuscular injection. Ketorolac is more than 99 percent bound to plasma proteins and has a mean apparent volume of distribution of 0.11-0.25 L/kg. About 91 percent of a dose is excreted in urine, mostly as inactive metabolites, and approximately 6 percent is eliminated in feces. The elimination half-life, approximately four to six hours, increases in elderly patients and those with renal impairment. Its analgesic effectiveness was similar or superior to that of morphine, meperidine, or pentazocine in single-dose studies of patients with postoperative pain or renal colic and greater than that of placebo in patients with chronic cancer pain. The adverse effects are generally mild to moderate, self-limiting, and similar to those seen with other prostaglandin inhibitors. Ketorolac has a reversible inhibitory effect on platelet aggregation. It can cause dose-related gastric ulcerations, even when administered parenterally. Ketorolac is a promising parenteral alternative to oral NSAIDs and a nonnarcotic alternative to opioid analgesics. Additional multiple-dose studies are needed to more clearly define its place in therapy.
酮咯酸氨丁三醇是一种吡咯并吡咯类非甾体抗炎药（NSAID），肌内注射用于治疗急性疼痛时具有强效镇痛作用。酮咯酸吸收良好，起效迅速。肌内注射后45 - 50分钟达到血浆最大浓度，约1 - 2小时达到镇痛峰值效应。酮咯酸与血浆蛋白的结合率超过99%，平均表观分布容积为0.11 - 0.25 L/kg。约91%的剂量经尿液排泄，主要以无活性代谢物形式排出，约6%经粪便排出。消除半衰期约为4 - 6小时，在老年患者和肾功能损害患者中会延长。在术后疼痛或肾绞痛患者的单剂量研究中，其镇痛效果与吗啡、哌替啶或喷他佐辛相似或更优，在慢性癌痛患者中优于安慰剂。不良反应一般为轻至中度，具有自限性，与其他前列腺素抑制剂所见不良反应相似。酮咯酸对血小板聚集有可逆性抑制作用。即使经胃肠外给药，它也可引起剂量相关的胃溃疡。酮咯酸是口服NSAIDs有前景的胃肠外替代药物，也是阿片类镇痛药的非麻醉性替代药物。需要更多的多剂量研究来更明确其在治疗中的地位。
