局部麻醉缓释药物的制备及镇痛作用

背景：临床常用的局部麻醉药物体内生物半衰期短,且局部组织的高浓度极易造成药物经血管吸收入血产生中枢神经和心血管毒性。因此,国内外学者开始进行局部麻醉缓释给药系统研究。目的：总结近年局部麻醉缓释药物的制备及镇痛效果的研究现状。方法：由作者应用计算机检索维普数据库中与局部麻醉缓释药物的制备及镇痛作用有关的文章,检索时限1998-01/2009-10。检索关键词：局麻药,微球,乳酸羟基乙酸共聚物,药物体外释放,镇痛。选择33篇文献进行分析。结果与结论：采用W1/O/W2双重乳化-溶剂挥发法、乳化溶剂挥发法、乳化-交联法、高压电场法制备的局麻药载体的微球,形态均圆整,流动性好,80%以上的微球粒径在50~100μm之间,可提高载药量和包封率。在对微球的体外释放性能进行考察时均得到了可延长药物的体外释放时间、相对较平稳的血药浓度、明显的缓释作用和良好安全性的结果。     

局部麻醉缓释药物的制备及镇痛作用

背景:临床常用的局部麻醉药物体内生物半衰期短,局部组织的高浓度极易造成药物经血管吸收入血产生中枢神经和心血管毒性.因此,内外学者开始进行局部麻醉缓释给药系统研究.目的:总结近年局部麻醉缓释药物的制备及镇痛效果的研究现状.方法:由作者应用计算机检索维普数据库中与局部麻醉缓释药物的制备及镇痛作用有关的文章,索时限1998-01/ 2009-10.检索关键词:局麻药,球,酸羟基乙酸共聚物,物体外释放,痛.选择33篇文献进行分析.结果与结论:采用W1/O/W2双重乳化-溶剂挥发法、乳化溶剂挥发法、乳化-交联法、高压电场法制备的局麻药载体的微球,态均圆整,动性好,0%以上的微球粒径在50～100 μm之间,提高载药量和包封率.在对微球的体外释放性能进行考察时均得到了可延长药物的体外释放时间、相对较平稳的血药浓度、明显的缓释作用和良好安全性的结果.     

局部麻醉透皮技术与整形美容手术

术中麻醉根据麻醉药物分布范围可分为全身麻醉和局部麻醉,其中局部麻醉在整形美容手术中的应用较为广泛。传统剂型经皮递送局麻药作用时间较短,且脂溶性差,限制了其在体表透皮方面的应用。近年来,随着麻醉技术的发展,新型体表镇痛局麻药递送系统可将涂抹于皮肤的药物递送至真皮层以阻滞神经末梢痛觉传入,从而达到镇痛的效果,提高了药物递送效率。此外,透皮给药相较于注射给药可显著增加给药安全性和患者舒适度。本文概述了常用的局麻药透皮吸收促进方法以及目前已上市的透皮局麻药物,并结合研究进展对局部麻醉透皮技术在整形美容手术中的应用和发展作一展望。     

医用壳聚糖膜的制备与应用

背景：壳聚糖膜在人工肾膜-透析膜、人工皮肤、口腔溃疡膜、牙周引导组织再生膜、药物载体控释膜及相关组织工程等方面已取得了令人欣慰的成果。目的：总结归纳壳聚糖膜的制备,及目前其在用于局部药物控释的应用。方法：电子检索CNKI数据库、读秀学术搜索等数据库收录的壳聚糖膜的制备和应用于药物控释载体的相关综述和实验研究报告,分析壳聚糖制备的研究进展和应用于药物控释载体的研究进展。结果与结论：共纳入壳聚糖制备与局部药物控释相关文献21篇。壳聚糖的制备条件与其应用于药物控释载体之间有着密不可分的关系,但总结规范及其相关性尚不明朗,尚期待大量研究。对壳聚糖的制备条件与其应用于药物控释载体的关系的研究也仍需要进一步努力,探索适宜壳聚糖膜制备条件,制备成功最适的药物控释载体是研究者的工作重点。     

利多卡因急性中毒反应1例

利多卡因属于酰胺类中效局麻药,适用于各种局部组织麻醉,其起效快、穿透性强,是比较理想的局麻药之一. 1 临床资料 患者,女,40岁,55 kg.因子宫肌瘤拟在持续硬膜外麻醉和骶管麻醉下行子宫全切除术.     

医用壳聚糖膜的制备与应用

背景:壳聚糖膜在人工肾膜-透析膜、人工皮肤、口腔溃疡膜、牙周引导组织再生膜、药物载体控释膜及相关组织工程等方面已取得了令人欣慰的成果.目的:总结归纳壳聚糖膜的制备,及目前其在用于局部药物控释的应用.方法:电子检索CNKI数据库、读秀学术搜索等数据库收录的壳聚糖膜的制备和应用于药物控释载体的相关综述和实验研究报告,分析壳聚糖制备的研究进展和应用于药物控释载体的研究进展.结果与结论:共纳入壳聚糖制备与局部药物控释相关文献21 篇.壳聚糖的制备条件与其应用于药物控释载体之间有着密不可分的关系,但总结规范及其相关性尚不明朗,尚期待大量研究.对壳聚糖的制备条件与其应用于药物控释载体的关系的研究也仍需要进一步努力,探索适宜壳聚糖膜制备条件,制备成功最适的药物控释载体是研究者的工作重点.     

局麻药神经毒性研究近况

自从可卡因首次用作眼手术表面麻醉以来，局麻药用于临床已有一个多世纪的历史。局麻药阻滞神经传导功能的作用在临床麻醉广泛使用中得到了肯定，同时其神经毒性也引起了临床的重视。现就其神经毒性作一综述。     

氯普鲁卡因臂丛阻滞效果分析

作用时间相对短的脂类局麻药盐酸氯普鲁卡因用于临床麻醉在国内已经有许多年，但在臂丛神经阻滞上使用报道并不多。因其起效快、效能强的特点仍值得麻醉医师考虑。本文就其单独使用（脂类）和与酰胺类中效局麻药利多卡因联用以及与单独利多卡因的效果进行分析。     

局部浸润麻醉药的简易配制方法

我院门诊手术室承担需要局部浸润麻醉的手术数量较多，常用的局麻药如利多卡因注射液的浓度均为2％，而在局部浸润麻醉手术中，麻药浓度的选择要根据手术的大小、时间的长短以及患者的身体状况等多种因素决定。如果需要其他浓度的局麻药便要自行配制，现将我们在临床工作中总结出的一种简易的配制方法介绍如下：     

常用局部麻醉技术

1概述1.1局部麻醉的概念麻醉作用限于躯体某一局部的麻醉方法,称为局部麻醉,简称局麻。产生局部麻醉的药物称为麻药。常用的局麻方法有局部浸润麻醉、神经阻滞麻醉和区域阻滞麻醉。另外,近年又出现了局部肿胀麻醉技术,主要用于脂肪抽吸,也是局部麻醉的一种。局麻简便易行,安全性大,并发症     

Efficacy of drugs in regional anesthesia: A review

Local anesthetics and opioids are the most commonly used drugs in regional anesthesia. Several other drugs are used as adjuvants in addition to local anesthetics.We will review the drugs currently used in regional anesthesia. In April 2009 we searched the PubMed database and found 143 articles related to the clinical use of drugs in regional anesthesia; we divided them into 3 major chapters: local anesthetics, opioids and adjuvants.Among local anesthetics, ropivacaine and levobupivacaine can be considered the drugs of choice in neuraxial and peripheral techniques because their toxicity is low even in large volume administration; mepivacaine can be considered the drug of choice in peripheral techniques when a shorter blockade is needed.Sufentanil is the opioid of choice in both neuraxial and peripheral techniques because it appears to improve the quality of anesthesia and to prolong sensory blockade in the postoperative period.Among the adjuvants to local anesthetics, clonidine is by far the most used drug in regional anesthesia; its yield in improving and prolonging the effects of local anesthetics is apparent in neuraxial techniques. Other drugs have been studied as adjuvants to local anesthetics but clinical evidence of their benefit is controversial in many cases and further trials are unquestionably warranted.In conclusion, since many different drugs are available for regional anesthesia, we must choose wisely the one that exhibits the best safety-efficacy profile and that suits the chosen technique and type of anesthesia/analgesia best.     

Caudal anesthesia and its determinant factors

In 130 surgical patients with diseases and injuries in the area of the perineum and lower extremities the clinical effects of three modern local anesthetics: 2% solution of lidocaine, 0.5% solution of bupivacaine, 0.75% solution of ropivacaine and their combinations (2% lidocaine and 0.25% bupivacaine solution 2% lidocaine and ropivacaine 0.375% solution) were followed with regard to the influence of increasing volumes of local anesthetics and different rates of drug administration. It is established that an effective caudal anesthesia is provided with all modern local anesthetics, with increasing use of local anesthetic solution to 40 ml provides duration and the prevalence of sensory and motor blocks, the use of mixture of local anesthetics optimizes the development and maintenance of the caudal blockade.     

药物控释载体材料的研究与应用

背景：作为控制释放体系的药物载体材料大多是高分子材料,但部分纳米无机材料也正逐步应用到药物控释材料体系中并取得了很好的研究成果。因此,药物控释用载体材料的设计与研究应用越来越受到重视。目的：对国内外药物控释载体材料的应用及最新研究进展作一综述。方法：应用计算机检索CNKI和Elsevier SD数据库中1999-01/2011-01关于药物控缓释材料的文章,在标题和摘要中以＂高分子,介孔材料,无机硅,磷酸盐,控释＂或＂polymer,mesoporous materials,Inorganic silicon,calcium phosphate,controlled release＂为检索词进行检索。选择文章内容与药物控缓释有关者,同一领域文献则选择近期发表或发表在权威杂志文章。纳入25篇文献进行综述。结果与结论：药物控缓释载体材料以用药量小、作用时间长、靶向作用好等特点被广泛关注,但是仍存在载药后药物失活,丧失生物活性等缺陷,目前随着复合药物载体材料和经皮给药装置研究的发展,控缓释材料在临床治疗中的应用必将更加广泛。     

Physicochemical interaction of local anesthetics with lipid model systems--correlation with in vitro permeation and in vivo efficacy.

In dermal/transdermal drug administration stratum corneum (SC) is often the rate-limiting step. Furthermore, the intercellular lipid domain of SC is nowadays widely accepted as the major contributor to the skin barrier. The current work investigates whether the difference in the level of topical efficacy of local anesthetic compounds correlates with the type of interaction between the drug and the intercellular lipids of SC. Therefore, local anesthetics of varying topical efficacy were evaluated with respect to their effect on the morphology of various model lipid systems using small and wide angle X-ray diffraction (SWAXD) and differential scanning calorimetry (DSC). The model lipids used were glyceryl monooleate, sphingomyelin and lipids isolated from human SC. Furthermore, partitioning into isolated human SC as well as permeation through isolated human SC and human tape-stripped skin were investigated in vitro.The results indicate that local anesthetics may act as their own permeation enhancers by increasing the degree of hydrocarbon chain fluidity of the intercellular lipids. Eventually these interactions may induce non-lamellar reversed types of liquid crystalline structures locally in SC, which further facilitate the drug mobility. The large difference in topical efficacy of the investigated local anesthetics could not be explained simply by looking at their effect on the phase behavior of lipid model systems. Despite the similarities in physicochemical properties of these substances, the in vitro skin permeability differed markedly (AD>EMLA>lidocaine>prilocaine>sameridine). Thus, it was concluded that sufficient drug permeability over SC is essential to obtain local anesthesia by blocking the superficial nociceptors.     

罗哌卡因联合碳酸利多卡因在臂丛神经阻滞麻醉中的应用

目的 研究罗哌卡因联合碳酸利多卡因在臂丛神经阻滞中的麻醉有效性和安全性。方法选择美国麻醉医师协会（ASA）Ⅰ～Ⅱ级、各类上肢手术的患者80例,随机分成两组,每组40例。A组：0．375％罗哌卡因30ml;B组：0．75％罗哌卡因15ml,联合1．73％碳酸利多卡因15ml,共30ml。按手术部位的不同,分别从肌间沟和腋路给药。观察生理指标变化、麻醉起效时间、麻醉持续时间和麻醉效果及不良反应。结果B组患者麻醉起效时间明显快于A组,差异有统计学意义（P〈0．05）。运动阻滞时间及感觉阻滞时间两组差异无统计学意义（P〉0．05）。麻醉效果B组优者达92．5％,A组麻醉优者达65．0％,A组有4例患者术中感疼痛明显需加用静脉辅镇痛助药物。两组患者均未出现局麻药中毒反应。结论罗哌卡因联合碳酸利多卡因经肌间沟及腋路臂丛神经阻滞,是一种麻醉效果优且安全的方法。     

A clinical trial of the use of 2 forms of bupivacaine hydrochloride (Anecaine and Marcaine) for epidural anesthesia

Two forms of 0.5% bupivacaine hydrochloride, Anecaine (Pliva) (n = 15) and Marcaine (Astra) (n = 15) were used for epidural anesthesia. The clinical picture of conduction block induced by the two local anesthetics varied. It manifested by a shorter latent period of analgesia development at the level of catheter and the drug infusion (LII) and relatively delayed development of analgesia in peripheral zones for Anecaine in comparison with marcaine. The authors conclude that solutions of local anesthetics containing the same active agent in the same concentrations under different commercial names manufactured by different companies may be characterized by different clinical picture of conduction blockade.     

Anesthesia and analgesia in obstetrics

Anesthesia in obstetrics includes the medical attendance of women in the delivery room as well as giving anesthesia for cesarean sections in the operating room. Over the last years the treatment of labor pain with epidural anesthesia has been modified. Whereas a couple of years ago local anesthetics were used almost exclusively, the recent trend goes toward a combination of local anesthetics with opioids. Using this combination the total amount of local anesthetic can be greatly reduced, whilst maintaining most of the motor function during labor. There is evidence the combination of local anesthetics with opioids can reduce the number of operative vaginal deliveries such as vacuum extraction or forceps. The systemic application of opioids remains unaffected by the local application and its significance is unaltered, even though the effectiveness compared to epidural application in managing labor pain is far inferior. Opioids applied systemically often have an unwanted sedative effect in the mother and have the potential for respiratory depression in the newborn. The question, whether epidural anesthesia increases the frequency of cesarean sections remains to be answered. Studies so far present discrepant results and do not show a causal relationship between the use of epidural anesthesia and increase in cesarean section rate. Regarding cesarean sections, there has been a trend in the operative field over the last years towards the use of regional anesthesia. This is the consequence of the fact that anesthesia related mortality during cesarean sections is still mainly due to hypoxia and aspiration during induction of anesthesia. The advantage of spinal anesthesia over epidural anesthesia is faster onset, more reliable sensitive block and a lower failure rate. Downside of the use of spinal anesthesia is a higher incidence of hypotension in the mother, which, however, is not a serious complication if treated adequately. Regarding the continuous application of local anesthetics via a spinal catheter, no definite statements towards benefits compared to other regional techniques can be made due to the lack of adequate amount of patient studies. Theoretically this method seems advantageous as it allows to adjust the administration of local anesthetics and opioids to the individual needs in a very refined way. Emergency situations, such as emergency cesarean sections, life threatening hemorrhage, eclampsia, and HELLP syndrome, are the main risks of the anesthetic practice in obstetrics. Their beneficial outcome is highly dependent on the coordination of logistic problems, good communication and coordination within an interdisciplinary team of obstetricians and anesthesiologists.     

Evaluating skin anesthesia after administration of a local anesthetic system consisting of an S-Caine patch and a controlled heat-aided drug delivery (CHADD) patch in volunteers

OBJECTIVE: The objective of this study was to evaluate the depth and duration of skin anesthesia after the administration of a local anesthetic system consisting of an S-Caine (Zars, Salt Lake City, UT) patch coupled with a controlled heat-aided drug delivery (CHADD; Zars) patch. DESIGN: The study design was a randomized, double-blind, placebo-controlled, two-period crossover trial. PATIENTS: Twelve healthy adult volunteers between the ages of 18 and 50 years were enrolled. INTERVENTIONS AND OUTCOME MEASURES: After administration of the study drug or placebo, vital signs (blood pressure, pulse, respiratory rate) were monitored and recorded, and depth and duration of anesthesia were determined and recorded at defined intervals for 10 to 120 minutes after treatment. Depth of anesthesia was measured with a 21-gauge short-bevel needle attached to a depth gauge, and duration was measured using a 0 to 2 (0 = no sensation, 1 = dull sensation, 2 = sharp scratching sensation) verbal report scale. RESULTS: Statistically significant differences were noted in both depth and duration of anesthesia between the active and placebo groups. The posttreatment mean for anesthetic depth in the active group was 6.8 mm compared with 4.7 mm for control group (p = 0.050). The median anesthetic duration was greater than 120 minutes for the active group compared with less than 10 minutes for the placebo group (p = 0.001). CONCLUSIONS: The local anesthetic system consisting of a combination of S-Caine and CHADD patches provided a statistically significant dermal anesthesia effect compared with placebo in this volunteer study. If confirmed in other studies, this system has promise as a noninvasive method of producing dermal anesthesia for minor surgical procedures or intravenous insertion.     

Local anesthetics as adjuvant analgesics

Local anesthetics administered to block nerve conduction for surgical anesthesia and to provide analgesia in management of acute pain have become a standard of anesthesiology practice. These drugs have had an important role in the multimodality management of chronic pain as well, and this role is expanding since the revival of systemic administration. Local anesthetics are analgesics, albeit not in the traditional clinical and pharmacologic sense. Evidence suggests that intravenous administration is an effective treatment in chronic neuropathic pain syndromes. There is also evidence that intravenous local anesthetics can relieve acute pain. Furthermore, the novel idea that acute procedural and postprocedural pain control with local anesthetics could prevent the development of chronic pain syndromes, including chronic neuropathic pain syndromes, adds another important potential dimension to the role of local anesthetics in pain management.