Verleye M, Heulard I, Gillardin J M
Laboratoires Biocodex, Zac de Mercières, Compiègne, 60200, France.
Pharmacol Res. 2000 May;41(5):539-42. doi: 10.1006/phrs.1999.0619.
To justify the inclusion of phenazone, independently of its anti-inflammatory properties, in combination with a local anaesthetic, such as lidocaine, in some ear drop medications, we have studied the effect of this compound on the local anaesthetic activity of lidocaine in an animal model, that of sciatic nerve blockade in mice. Lidocaine and phenazone were tested alone and in combination at various concentrations. The local anaesthetic activity was estimated as the loss of motor activity of the hindlimb after topical injection of the drugs in the region of the sciatic nerve. Lidocaine, at concentrations ranging from 0.03 to 0.25%, induced a concentration-dependent anaesthetic effect. Phenazone alone had no effect at 0.25-1%. When combined, the two compounds acted synergistically. The local anaesthesia induced by lidocaine plus phenazone was significantly more intense and longer lasting than that induced by lidocaine alone. Phenazone enhanced the potency of lidocaine in this animal model. It is suggested that the potentiated local anaesthetic effect of the combination may be partly due to enhanced local bioavailability of lidocaine.
为了证明在一些滴耳液药物中，非那宗（独立于其抗炎特性之外）与局部麻醉剂（如利多卡因）联合使用的合理性，我们在动物模型（小鼠坐骨神经阻滞模型）中研究了该化合物对利多卡因局部麻醉活性的影响。分别以不同浓度单独测试了利多卡因和非那宗，并对二者进行了联合测试。通过在坐骨神经区域局部注射药物后后肢运动活性的丧失来评估局部麻醉活性。浓度范围为0.03%至0.25%的利多卡因可产生浓度依赖性麻醉效果。0.25% - 1%的非那宗单独使用时无效果。联合使用时，两种化合物产生协同作用。利多卡因加非那宗诱导的局部麻醉比单独使用利多卡因诱导的局部麻醉显著更强且持续时间更长。在该动物模型中，非那宗增强了利多卡因的效力。提示联合用药增强的局部麻醉效果可能部分归因于利多卡因局部生物利用度的提高。
