Engelhardt G, Homma D, Schlegel K, Utzmann R, Schnitzler C
Department of Pharmacologic Research, Dr. Karl Thomae GmbH, Biberach/Riss, Germany.
Inflamm Res. 1995 Oct;44(10):423-33. doi: 10.1007/BF01757699.
The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs. With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenan-induced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration. Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain. In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeast-induced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid. Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm. Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam. The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.
在多种动物模型中研究了新型非甾体抗炎药美洛昔康的抗炎、镇痛和解热特性，并与吡罗昔康、双氯芬酸、吲哚美辛及其他几种非甾体抗炎药的特性进行了比较。就单次口服剂量的总体效果而言，美洛昔康对角叉菜胶诱导的大鼠水肿的抗渗出作用超过了比较中所包括的所有非甾体抗炎药。此外，在佐剂诱导的大鼠关节炎、大鼠肉芽肿袋模型和大鼠棉球试验中，美洛昔康在所检测的所有化合物中显示出最大的效力。与吲哚美辛不同，在大鼠角叉菜胶胸膜炎模型中，美洛昔康既引起渗出液体积的剂量依赖性减少，又抑制白细胞迁移。美洛昔康对大鼠的炎性疼痛显示出强烈而持久的作用。与其他非甾体抗炎药一样，但与安乃近不同，美洛昔康在用于确定弱中枢镇痛作用的热板和尾夹试验中没有效果。与安乃近不同而与吲哚美辛一样，美洛昔康在内脏扩张性疼痛模型中没有效果。与其他非甾体抗炎药一样，在抗炎剂量范围内，美洛昔康对正常体温大鼠的体温没有影响，但确实以剂量依赖性方式降低了大鼠酵母诱导的发热。与吡罗昔康一样，美洛昔康对用氧嗪酸处理的大鼠有促尿酸尿作用。低剂量美洛昔康抑制豚鼠缓激肽诱导和血小板活化因子诱导的支气管痉挛，但对乙酰胆碱诱导的支气管痉挛没有影响。吡罗昔康在大鼠胃中的致溃疡作用比美洛昔康更大。就抑制佐剂性关节炎而言，美洛昔康在大鼠中的治疗范围比吡罗昔康、吲哚美辛、双氯芬酸和萘普生大几倍。
