Kumpulainen Elina, Kokki Hannu, Laisalmi Merja, Heikkinen Marja, Savolainen Jouko, Rautio Jarkko, Lehtonen Marko
Department of Pharmacology and Toxicology, University of Kuopio, Kuopio, Finland.
J Clin Pharmacol. 2008 Apr;48(4):495-501. doi: 10.1177/0091270007313389. Epub 2008 Feb 13.
Ketorolac is a potent nonsteroidal anti-inflammatory analgesic used in postoperative pain management. Ketorolac elicits its analgesic action by inhibiting the cyclo-oxygenase enzyme in peripheral tissues and in the spinal cord. Central nervous system penetration of parenteral ketorolac has been evaluated in adults but not in children. In the present study we investigated ketorolac cerebrospinal fluid penetration via spinal anesthesia in 30 healthy children undergoing surgery in the lower part of the body. A single cerebrospinal fluid and blood sample was obtained between 11 minutes and 6 hours after receiving ketorolac 0.5 mg x kg(-1) IV. Ketorolac concentrations were determined by gas chromatography with mass spectrometric detection. Ketorolac was detected from 22 of the 30 cerebrospinal fluid samples, and the concentrations ranged between 0.2 and 7.6 microg x L(-1) (median, 0.6 microg x L(-1)). The cerebrospinal fluid to unbound plasma concentration-ratio ranged between 0.01 and 0.69 (median, 0.08). These low concentrations indicate that ketorolac does not readily penetrate cerebrospinal fluid in children.
酮咯酸是一种强效非甾体抗炎镇痛药，用于术后疼痛管理。酮咯酸通过抑制外周组织和脊髓中的环氧化酶发挥镇痛作用。已对成人静脉注射酮咯酸后中枢神经系统的渗透情况进行了评估，但尚未在儿童中进行评估。在本研究中，我们调查了30名接受下半身手术的健康儿童在脊髓麻醉下酮咯酸的脑脊液渗透情况。在静脉注射0.5mg/kg的酮咯酸后11分钟至6小时之间采集了一份脑脊液和血液样本。通过气相色谱-质谱检测法测定酮咯酸浓度。在30份脑脊液样本中的22份中检测到了酮咯酸，其浓度范围在0.2至7.6μg/L之间（中位数为0.6μg/L）。脑脊液与非结合血浆浓度比在0.01至0.69之间（中位数为0.08）。这些低浓度表明酮咯酸在儿童中不易渗透到脑脊液中。
