Fairley J W, Reynolds F
Br J Anaesth. 1981 Nov;53(11):1211-6. doi: 10.1093/bja/53.11.1211.
The duration of action and vascular effects of L(+) and D(-) and racemic mepivacaine were investigated in a double-blind study in 23 fit volunteers. Isosmolar 0.1-ml intradermal injections of a range of concentrations of each agent from 0.011% to 2.7%, and physiological saline were given in duplicate to at least 14 subjects. Local colour changes were observed 5-10 min after injection, and analgesia to pinprick was tested at 5-min intervals thereafter until full recovery. Both isomers were vasoconstrictor at concentrations of 0.3% and less; at greater concentration the L isomer produced more vasodilation and haemorrhagic change. The duration of action of both isomers increased with concentration between 0.05 and 0.9%, but the L isomer was significantly longer acting than the D at 0.3% and more. The log dose-duration curve could be interpreted as linear between 0.1 and 0.9% with the slope of L isomer being twice as steep as the D. The findings for racemic mepivacaine were between those of the two isomers. The longer duration of analgesia of L-mepivacaine was not associated with superior vasoconstrictor power.
在一项针对23名健康志愿者的双盲研究中,对左旋(L(+))、右旋(D(-))和消旋甲哌卡因的作用持续时间及血管效应进行了研究。以0.1毫升等渗皮内注射的方式,给至少14名受试者重复注射浓度范围为0.011%至2.7%的每种药物以及生理盐水。注射后5 - 10分钟观察局部颜色变化,此后每隔5分钟测试对针刺的镇痛效果,直至完全恢复。两种异构体在浓度为0.3%及更低时均为血管收缩剂;浓度更高时,左旋异构体产生更多的血管舒张和出血变化。两种异构体的作用持续时间在0.05%至0.9%之间随浓度增加,但是在0.3%及更高浓度时,左旋异构体的作用持续时间明显长于右旋异构体。对数剂量 - 作用持续时间曲线在0.1%至0.9%之间可解释为线性,左旋异构体的斜率是右旋异构体的两倍。消旋甲哌卡因的研究结果介于两种异构体之间。左旋甲哌卡因较长的镇痛持续时间与其较强的血管收缩能力无关。