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bupivacaine
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     Table 1.
     表1
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     Bupivacaine for brachial plexus block
     应用丁哌卡因于臂丛神经阻滞
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     Synthesis of Bupivacaine Hydrochloride by Triphosgene
     三光气法合成盐酸布比卡因
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     Figs 2 and refs 11.
     图2参11
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This study reported 1164 operative cases receiving bupivacaine hydrochloride as anes-thesia in different concentrations, with or without adrenaline, for epidural, spinal andperipheral nerve regional blocks, as compared at random with lidocaine-tetracaine mixtureor tetracaine alone. The data confirmed that the latency and the duration of complete block with bupiva-caine was the same as that with the above mentioned mixture solutions; but the durationof the action and the postoperative analgesia were significantly...

This study reported 1164 operative cases receiving bupivacaine hydrochloride as anes-thesia in different concentrations, with or without adrenaline, for epidural, spinal andperipheral nerve regional blocks, as compared at random with lidocaine-tetracaine mixtureor tetracaine alone. The data confirmed that the latency and the duration of complete block with bupiva-caine was the same as that with the above mentioned mixture solutions; but the durationof the action and the postoperative analgesia were significantly longer than that with themixture solutions. The duration of action was bowever affected by the sites of block. Bupivacaine in concentration of either 0.25% or 0.5% only resulted in slight hemodyna-mic change and there was no respiratory depression observed. This study revealed thatregional block with bupivacaine was more adequate for cervical-upper thoracic epiduralanesthesia, orthopedic surgery and cesarean section. The dosage of bupivacaine used in this study was 2.2~3.2mg/kg; and no toxic reactionhad ever happened, since the plasma concentration of bupivacaine was much lower than itsconvulsive level. In conclusion, bupivacaine was an effective, safe and long action anesthe-tic.

报告应用不同浓度的国产布比卡因加/不加肾上腺素于硬膜外、脊麻、神经阻滞等部位麻醉1164例。并与同期内随机抽样用地卡因和利多卡因混合液、地卡因、普普卡因作阻滞的病例作了对比。布比卡因的作用、潜伏期、达到完全阻滞的时间均与混合液或地卡因相同,而维持时间及术后镇痛时间则较后者明显延长。其维持时间的长短随阻滞部位而异。应用布比卡因0.25%、0.5%浓度,血液动力学改变轻微,对呼吸无抑制。因而尤其适用于颈上、胸部、硬膜外、剖腹产及骨科矫形手术的麻醉。本组用药量为2.2~3.2mg/kg,远低于血浆致痉水平,故认为布比卡因为一有效安全的长效麻醉剂。

A HPLC method for the determination of lidocaine, bupivacaine and tetracaine in human plasma with verapamil as internal standard has been established. This method was carried out on an ODS column using modified methanol (0.51 ml of n-butylamine and 0.3 ml of glacial acetic acid added to 300 ml of MeOH)-water (75:25) as mobile phase operated in recycling mode. The procedure is as follows: transfer 1.0 ml of plasma into a 12 ml glass centrifuge tube, add one drop of 2 N NaOH solution (if tetracaine is present,...

A HPLC method for the determination of lidocaine, bupivacaine and tetracaine in human plasma with verapamil as internal standard has been established. This method was carried out on an ODS column using modified methanol (0.51 ml of n-butylamine and 0.3 ml of glacial acetic acid added to 300 ml of MeOH)-water (75:25) as mobile phase operated in recycling mode. The procedure is as follows: transfer 1.0 ml of plasma into a 12 ml glass centrifuge tube, add one drop of 2 N NaOH solution (if tetracaine is present, one drop of 10% sodium metabisulfite solution and 0.1 ml of 2 N NaOH solution must be added to the specimen tube before collecting the sample in order to prevent hydrolysis), add 40μ1 of the internal standard (0.16μg/μ1)and 8 ml of ethyl ether-dichloromethane (10/8,V/V). shake for 10 minutes and centrifuge for 5 minutes at 3000g. Transfer the organic phase into another tube and evaporate to dryness at 50℃. Reconstitute the residuew ith 50μl of mobile phase and inject 20μl into the chromatograph using the following conditions: column, 15×0.46 cm packed with ODS (YWG-C_(18)H_(37), 10μm); flow rate, 1.5 ml/min; UV detector, 220 nm; range 5 mV; Chart speed, 5 mm/min.This method is simple, rapid, sensitive and has a good linearity. The absolute recoveries were found to be 101±3.6% for lidocaine, 89.3±4.1% for bupivacaine and 80±10.1% for tetracaine. Precisioin studies for both within day and day-to-day at different concentrations provided CV values of less than 10% except tetracaine which produced a CV of 10.5% for within day precision at high concentration.

应用改性甲醇—水为流动相,在YWG—C_(18)H_(37)反相柱上,以异搏定(verapamil)为内标,建立了适合于临床生化研究和药物代谢动力学研究的同时或分别测定人血浆中利多卡因(lidocaine),布比卡因(bupivacaine)和丁卡因(tetracaine)的高效液相色谱法。本法简便、快速、灵敏、重现性好,流动相可循环使用。利多卡因、布比卡因和丁卡因的平均回收率分别为101±3.6%,89.3±4.1%和80±10.1%,不同浓度水平测定结果的日内和日间变异系数一般小于10%,其检定限度(信噪比>3)分别为0.03,0.05和0.1μg/ml。

Using Clark oxygen electrode, the normal rate of respiration of Schistosoma japonicum were determined in vitro. The rate of respiration of adult schistosomes was found to be 1.47+0.19 nmol O2/pair of worm/min or 6.89+1.13 nmol O_2/mg dry wt/min. It was 2.5 fold higher than that obtained by manometric method. This indicates that S. japonicum did have an active aerobic metabolism. Both in vitro and in vivo experiments showed that potassium antimony tartrate inhibited markedly the respiration of the worms, whereas...

Using Clark oxygen electrode, the normal rate of respiration of Schistosoma japonicum were determined in vitro. The rate of respiration of adult schistosomes was found to be 1.47+0.19 nmol O2/pair of worm/min or 6.89+1.13 nmol O_2/mg dry wt/min. It was 2.5 fold higher than that obtained by manometric method. This indicates that S. japonicum did have an active aerobic metabolism. Both in vitro and in vivo experiments showed that potassium antimony tartrate inhibited markedly the respiration of the worms, whereas the rate of glycolysis was affected only slightly. Our results seemed to be inconsistent with those suggested by Bueding who had attributed the mode of action of antimonial drugs to the inhibition of phosphofructokinase.Diamide, a well-known specific sulfhydryl agent, was shown to inhibit similarly the respiration of schistosomes. This led us to assume that antimonial drugs might act on important enzyme systems containing SH-groups.Pyquiton was similar to local anesthetics (lidocaine and bupivacaine) in that they stimulated the respiration of worms in vitro. It is interesting to note that all these compounds have a glycinamide structure (Fig 1). Thus, it appears that the mode of action of pyquiton may be related to that of local anesthetics, acting on worm tegument and influencing the permeability of cations.Pyquiton did show a slight effect on the glycolysis of schistosomes. But the ratio of the amount of lactic acid formed to that of the combined consumption of glycogen and glucose remained to be 1.

在应用氧电极技术测定日本血吸虫呼吸率的基础上,观察了酒石酸锑钾和吡喹酮对血吸虫呼吸和糖酵解的影响。结果表明:酒石酸锑钾对虫的呼吸呈明显的抑制;吡喹酮对虫的呼吸先刺激,在作用1 h后则表现为轻度抑制;在对呼吸有显著影响的浓度下,对虫的糖酵解并无明显影响。此外,用巯基抑制剂双酰胺、局部麻醉药利多卡因、布比卡因对血吸虫的呼吸进行了比较观察。

 
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