Gupta S K, Velpandian T, Mathur P, Sengupta S
Department of Pharmacology, All India Institute of Medical Sciences, New Delhi, India.
Pharmacology. 1998 Mar;56(3):137-43. doi: 10.1159/000028191.
Nimesulide, a selective cyclooxygenase-2-inhibiting nonsteroidal anti-inflammatory drug, has been found to be a potent anti-inflammatory and analgesic drug, when administered orally, rectally or topically. The aim of the present study was to evaluate the comparative efficacy of intramuscularly injected nimesulide with that of diclofenac and to elucidate the pharmacokinetic profile of this formulation. Swiss albino mice were used in the experiment. Analgesic activity was tested using the acetic acid writhing test and the tail-flick latency test. Plasma levels of nimesulide and its active metabolite, hydroxynimesulide, were determined by a HPLC method. A peak analgesic effect was observed between 60 and 120 min, while Cmax (10.6 +/- 3.8 micrograms/ml) of nimesulide was reached at 60 min (Tmax). Analgesia was induced within 15 min of administration of nimesulide and was significantly higher than that of diclofenac at 90 and 120 min posttreatment in the writhing reflex and at 60 and 90 min in the tail-flick latency test. The results indicate that intramuscularly injected nimesulide may be an alternative mode of administration in uncooperative patients or when immediate analgesic effects are warranted.
尼美舒利是一种选择性环氧化酶 -2 抑制性非甾体抗炎药，已发现口服、直肠给药或局部给药时，它是一种强效抗炎和镇痛药。本研究的目的是评估肌肉注射尼美舒利与双氯芬酸的相对疗效，并阐明该制剂的药代动力学特征。实验使用了瑞士白化小鼠。采用醋酸扭体试验和甩尾潜伏期试验检测镇痛活性。通过高效液相色谱法测定尼美舒利及其活性代谢物羟基尼美舒利的血浆水平。在 60 至 120 分钟之间观察到峰值镇痛效果，而尼美舒利的 Cmax（10.6±3.8 微克/毫升）在 60 分钟（Tmax）时达到。尼美舒利给药后 15 分钟内诱导出镇痛作用，在扭体反射中，给药后 90 分钟和 120 分钟以及甩尾潜伏期试验中给药后 60 分钟和 90 分钟时，镇痛效果明显高于双氯芬酸。结果表明，对于不合作的患者或需要立即产生镇痛效果时，肌肉注射尼美舒利可能是一种替代给药方式。
