The anti-inflammatory, analgesic and antipyretic activities of non-narcotic analgesic drug mixtures in rats.
The anti-inflammatory, analgesic and antipyretic activities of non-narcotic analgesic drug mixtures in rats.
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发表时间：
1981-06
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通讯作者：
A. Seegers;L. Jager;P. Zandberg;J. van Noordwijk
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作者：
A. Seegers;L. Jager;P. Zandberg;J. van Noordwijk
已分别和混合检查了非麻醉性镇痛剂对角叉菜胶诱导的成年大鼠后爪水肿和酵母诱导的痛觉过敏和体温过高的影响。使用药物-受体相互作用动力学评价药物的功效。此外，还检验了以下假设：所用药物混合物的抗炎、镇痛和解热活性等于单个药物活性的相加，并且可以从其内在活性和亲和力预测。口服乙酰水杨酸（阿司匹林）、扑热息痛、非那西丁（60、125、250和500 mg. kg-1）和咖啡因（12.5、25、50和100 mg. kf-1）后，观察到对爪水肿、痛觉过敏和体温过高的剂量依赖性抑制。在使用的剂量范围内，扑热息痛、非那西丁和咖啡因的抗炎活性往往小于阿司匹林。咖啡因产生半最大效应的剂量低于阿司匹林，而阿司匹林又与扑热息痛或非那西丁相当。非那西丁和咖啡因的镇痛活性被归类为强于阿司匹林，而对乙酰氨基酚的疗效相似。扑热息痛和阿司匹林作为退热药相当。非那西丁的解热活性高于阿司匹林，而咖啡因的解热活性低于阿司匹林。对于咖啡因，产生半最大效应的剂量低于阿司匹林。在使用的剂量范围内，低剂量的阿司匹林与扑热息痛、非那西丁或咖啡因的混合物显示出抗炎、镇痛和解热活性，与基于添加的预期活性没有差异。顺便说一下，在某些较高剂量水平下，发现药物活性增强，低剂量的三联制剂：阿司匹林+扑热息痛+咖啡因和阿司匹林+非那西丁+咖啡因显示抗炎和解热活性，与基于添加的预期活性没有差异，但在较高剂量的这些组合中观察到的活性表明增强。可以得出结论，在大鼠中，阿司匹林、对乙酰氨基酚、非那西丁和咖啡因的双重和三重组合的抗炎、镇痛和解热活性至少等于基于添加的预期活性。
The effects of non-narcotic analgesics have been examined, separately and in admixture, on carrageenan-induced hind paw oedema and on yeast-induced hyperalgesia and hyperthermia in adult rats. The efficacy of the drugs was evaluated using the kinetics of drug-receptor interaction. In addition, the hypothesis was tested that the anti-inflammatory, analgesic and antipyretic activities of the drug mixtures used equal the addition of the activities of the individual drugs and could be predicted from their intrinsic activities and affinities. Dose-dependent inhibition of paw oedema, hyperalgesia and hyperthermia was observed after oral administration of acetylsalicylic acid (aspirin), paracetamol, phenacetin (60, 125, 250 and 500 mg.kg--1), and caffeine (12.5, 25, 50 and 100 mg.kf--1). Over the dose-ranges used, the anti-inflammatory activities of paracetamol, phenacetin and caffeine tended to be smaller than that of aspirin. The dose producing a semi-maximal effect for caffeine was lower than that for aspirin which in turn was comparable to that for paracetamol or phenacetin. The analgesic activities of phenacetin and caffeine were classified as stronger than that of aspirin, whereas the efficacy of paracetamol was similar. Paracetamol and aspirin were comparable as antipyretics. The antipyretic activity of phenacetin was higher but that of caffeine was lower than that of aspirin. For caffeine the dose producing a semi-maximal effect was lower than that of aspirin. Within the dose-ranges used, low doses of mixtures of aspirin with either paracetamol, phenacetin or caffeine exhibited anti-inflammatory, analgesic and antipyretic activities which were not different from the activities expected on the basis of addition. Incidentally, at some of the higher dose levels potentiation of the activity of the drugs was found. Low doses of the triple combinations: aspirin + paracetamol + caffeine and aspirin + phenacetin + caffeine showed anti-inflammatory and antipyretic activities which were not different from those expected on the basis of addition, but the activities observed with higher doses of these combinations indicated potentiation. It is concluded that, in the rat, the anti-inflammatory, analgesic and antipyretic activities of dual and triple combinations of aspirin, paracetamol, phenacetin and caffeine at least equal the activities expected on the basis of addition.