Sycha Thomas, Anzenhofer Sebastian, Lehr Stephan, Schmetterer Leopold, Chizh Boris, Eichler Hans-Georg, Gustorff Burkhard
Department of Neurology, Medical University of Vienna, Währinger-Gürtel 18-20 A-1090 Vienna, Austria Department of Anesthesia and General Intensive Care Medicine, Medical University of Vienna, Vienna, Austria Department of Clinical Pharmacology, Medical University of Vienna,Vienna, Austria Institute for Medical Computersciences, Medical University of Vienna, Vienna, Austria GlaxoSmithKline, Addenbrooke's Centre for Clinical Investigation, Cambridge, UK.
Pain. 2005 Feb;113(3):316-322. doi: 10.1016/j.pain.2004.11.002.
The analysis of drug's influence on peripheral and central sensitisation can give useful information about its mode of action and can lead to more efficacy in the treatment of pain. Peripheral inflammation is associated with peripheral expression and up-regulation of cyclooxygenase 2 (COX-2) in the CNS. The relative contribution of COX-2 mediated central sensitisation may be prominent under inflammatory conditions. In this randomized, double blinded, placebo controlled cross-over trial the effects of multidoses of the COX-2 selective inhibitor rofecoxib on primary and secondary hyperalgesia were evaluated in the UVB pain model. Twenty-four hours after local UVB irradiation at the upper leg of 42 healthy volunteers heat pain perception (HPPT) and heat pain tolerance thresholds (HPTT) were assessed within the inflammation. The area of secondary hyperalgesia was determined by pin prick test. Subjects received oral rofecoxib 50, 250, 500 mg or placebo. Pain testing was repeated after 3 and 6 h. Compared to placebo, rofecoxib significantly increased HPPT (1.55 and 1.08 degrees C, P<0.0001 and P=0.0333), HPTT (1.74 and 1.58 degrees C, P<0.0001 and P<0.0001), and reduced the mean area of secondary hyperalgesia by 15.6% (P=0.007) and 16.8% (P<0.001) after 3 and 6 h. No significant difference between the three dosage groups was observed. These data confirm peripheral effects of rofecoxib in a human inflammatory UV-B pain model and provide circumstantial evidence that even a standard clinical dose of rofecoxib reduces central hyperalgesia in inflammatory pain. We confirm that the effect of single oral dose of rofecoxib plateaus at 50 mg.
分析药物对外周和中枢敏化的影响可以提供有关其作用方式的有用信息,并可能提高疼痛治疗的疗效。外周炎症与中枢神经系统中环氧合酶2(COX-2)的外周表达和上调有关。在炎症条件下,COX-2介导的中枢敏化的相对作用可能较为突出。在这项随机、双盲、安慰剂对照的交叉试验中,在紫外线B(UVB)疼痛模型中评估了多剂量COX-2选择性抑制剂罗非昔布对原发性和继发性痛觉过敏的影响。42名健康志愿者的大腿上部接受局部UVB照射24小时后,在炎症区域内评估热痛觉(HPPT)和热痛耐受阈值(HPTT)。通过针刺试验确定继发性痛觉过敏区域。受试者口服罗非昔布50、250、500mg或安慰剂。3小时和6小时后重复进行疼痛测试。与安慰剂相比,罗非昔布显著提高了HPPT(分别提高1.55和1.08摄氏度,P<0.0001和P=0.0333)、HPTT(分别提高1.74和1.58摄氏度,P<0.0001和P<0.0001),并在3小时和6小时后使继发性痛觉过敏的平均面积分别减少了15.6%(P=0.007)和16.8%(P<0.001)。三个剂量组之间未观察到显著差异。这些数据证实了罗非昔布在人类炎症性UV-B疼痛模型中的外周作用,并提供了间接证据表明,即使是标准临床剂量的罗非昔布也能减轻炎症性疼痛中的中枢性痛觉过敏。我们证实,罗非昔布单次口服剂量的作用在50mg时达到平稳状态。