作者：施宇翔文愛(ài)東熊利澤張英民

【關(guān)鍵詞】 碳酸利多卡因 關(guān)鍵詞: 碳酸利多卡因;臂叢神經(jīng)阻滯;藥代動(dòng)力學(xué);藥效學(xué) 摘 要:目的 探討碳酸利多卡因在臂叢神經(jīng)阻滯中的臨床藥代動(dòng)力學(xué)及藥效學(xué)特性. 方法 20例實(shí)施臂叢神經(jīng)阻滯患者，隨機(jī)分為鹽酸利多卡因組和碳酸利多卡因組，每組10例，分別給予鹽酸利多卡因或碳酸利多卡因（6mg kg-1 ）.以熒光偏振免疫分析法（FPIA）測(cè)定利多卡因的血藥濃度，以臨床觀察評(píng)價(jià)藥效學(xué)，比較利多卡因鹽酸鹽和碳酸鹽的藥動(dòng)學(xué)和藥效學(xué)的差異. 結(jié)果 碳酸利多卡因和鹽酸利多卡因的主要藥動(dòng)學(xué)參數(shù)達(dá)峰時(shí)間、達(dá)峰濃度及曲線下面積（AUC）分別為（17.2±8.9）和（25.6±9.7）min;（4.2±1.6）和（3.3±1.2）mg L-1 ;（11.8±1.8）和（8.7±1.6）mg h L-1 ;碳酸利多卡因和鹽酸利多卡因的藥效學(xué)參數(shù)麻醉起效時(shí)間、阻滯完善時(shí)間及麻醉持續(xù)時(shí)間分別為（4.9±1.8）和（9.1±2.1）min;（8.9±4.6）和（13.7±5.2）min;（211.3±47.4）和（152.6±31.4）min. 結(jié)論 碳酸利多卡因吸收速率和達(dá)峰時(shí)間均快于其鹽酸鹽，AUC也大于其鹽酸鹽，臨床麻醉起效時(shí)間及阻滯完善時(shí)間均快于其鹽酸鹽，體內(nèi)消除半衰期與鹽酸利多卡因基本一致.

Keywords:lidocaine carbonate;brachial plexus block;phar-macokinetics;pharmacodynamics Abstract:AIM To investigate pharmacokinetics and phar-macodynamics of lidocaine carbonate in the patients duringbrachial plexus block.METHODS 20patients undergoing brachial plexus block were randomly and equally allocated in-to two groups.The patients were given lidocaine carbonate and lidocaine hydrochloride（6mg kg-1 ）respectively.Serum levels of lidocaine were measured using FPIA.Pharmacody-naimcs was evaluated by subjective observation of an anes-thetist.The results of pharmacokinetics and pharmacodyna-mics of lidocaine carbonate were compared with those of lido-caine hydrochloride.RESULTS The peak time，the maxi-mal concentrations and AUC of the lidocaine carbonate group and lidocaine hydrochloride group were（17.2±8.9）vs（25.6±9.7）min，（4.2±1.6）vs（3.3±1.2）mg L-1 ，（11.8±1.8）vs（8.7±1.6）mg h L-1 ，respectively.The onset time，finishing time and persistent time of blockade of the li-docaine carbonate group and lidocaine hydrochloride group were（4.9±1.8）vs（9.1±2.1）min;（8.9±4.6）vs（13.7±5.2）min;（211.3±47.4）vs（152.6±31.4）min，respective┐ly.CONCLUSION The results showed constant of the ab-sorption rate and AUC of lidocaine carbonate were singifi-cantly greater than those of lidocaine hydrochloride.The peak time was shorter than that of lidocaine hydrocloride too.The onset time and finishing time of blockade of lidocaine car-bonate were shorter than those of lidocaine hydrochloride.The study suggested that onset of blockade of lidocaine car-bonate was faster，but elimination of lidocaine in human body was almost the same as that of lidocaine hydrochloride during brachial plexus block. 0 引言 通過(guò)揭示藥物在體內(nèi)的藥動(dòng)藥效規(guī)律，實(shí)現(xiàn)個(gè)體化給藥，達(dá)到提高藥物療效，降低不良反應(yīng)的目的，是目前臨床藥物治療學(xué)的研究重點(diǎn)［1-3］ .利多卡因是臨床常用的酰胺類(lèi)局麻藥，主要用于神經(jīng)阻滯及硬膜外麻醉.以往研究結(jié)果顯示，提高利多卡因溶液的pH值，使藥物的非離子型比例增加，從而促進(jìn)利多卡因的擴(kuò)散，使阻滯起效時(shí)間縮短，效果增強(qiáng)［4-8］ .本實(shí)驗(yàn)對(duì)碳酸利多卡因與鹽酸利多卡因在臂叢神經(jīng)阻滯中的藥代動(dòng)力學(xué)及藥效學(xué)進(jìn)行了比較研究，旨為其在臨床神經(jīng)阻滯中合理應(yīng)用和避免發(fā)生不良反應(yīng)提供理論依據(jù). 1 對(duì)象和方法 1.1 對(duì)象 隨機(jī)選擇美國(guó)麻醉醫(yī)師協(xié)會(huì)（American Society of Anesthesiologists，ASA）Ⅰ～Ⅱ級(jí)的上肢疾患患者20例，年齡（34.3±14.8）歲，體質(zhì)量（63.8±5.7）kg. 1.2 方法 1.2.1 給藥 隨機(jī)分成2組，每組10例，在臂叢神經(jīng)阻滯下進(jìn)行手術(shù).鹽酸組用20g L-1 鹽酸利多卡因（第二軍醫(yī)大學(xué)朝暉制藥廠，批號(hào):010918），碳酸組用20g L-1 碳酸利多卡因（江蘇泰興制藥廠，批號(hào):011022），全部患者均不用術(shù)前藥.肌間溝途徑尋找異感行臂叢阻滯，利多卡因用量按6mg kg-1 計(jì)算. 1.2.2 藥代動(dòng)力學(xué)研究 在臂叢神經(jīng)注入局麻藥后的5，10，20，30，45，60，120，180和360min分別從肘正中靜脈采血1mL，血標(biāo)本離心，取血清，用熒光偏振免疫方法（FPIA）測(cè)定利多卡因的血藥濃度，以3P97藥動(dòng)學(xué)軟件擬和求得利多卡因的藥動(dòng)學(xué)參數(shù). 1.2.3 藥效學(xué)觀測(cè)指標(biāo) 麻醉期間觀察并記錄麻醉起效時(shí)間、阻滯完善時(shí)間和麻醉持續(xù)時(shí)間. 統(tǒng)計(jì)學(xué)處理:血藥濃度數(shù)據(jù)均以3P97藥動(dòng)學(xué)軟件自動(dòng)計(jì)算并判斷房室模型，以梯形法計(jì)算曲線下面積（AUC），以消除相濃度的對(duì)數(shù)與時(shí)間的回歸求得消除半衰期.Tab1用生存分析，Tab2用成組t檢驗(yàn)，數(shù)據(jù)以x ±s表示.