维库溴铵和阿曲库铵预处理对琥珀胆碱的肌震颤及肌松效应的影响

目的 观察维库溴铵和阿曲库铵预处理对琥珀胆碱肌震颤的预防及对其肌松效应的影响。方法 ３０例全麻病人根据不同预处理药分成３组,即０．９％生理盐水（对照组）;０．０１ｍｇ／ｋｇ维库溴铵组和０．０５ｍｇ／ｋｇ阿中铵组,每组１０例。预处理４分后静注琥珀胆囊１．５ｍｇ／ｋｇ。采用ＰａｒａＧｒａｐｈ监测肌松。结果 阿曲库铵预处理能基本消除琥珀胆碱引起的肌震颤,维库溴铵只能减轻或部分消除琥珀胆碱引起的肌震颤。但     

国产维库溴铵的临床肌松效应观察

目的 比较国产维库溴铵与进口同类产品的临床肌松效能以及对血液对力学的影响。方法 ＡＳＡ Ⅰ～Ⅱ级手术病人２６例，随机分为两组（ｎ＝１３）。记录肌松的起效时间，无反应期，四个成串刺激（ＴＯＦ）恢复２５％、５０％、７５％的恢复时间和恢复指数，观察插管条件，连续记录诱导插管期间ＭＡＰ、ＨＲ的变化。结果 两组气管插管优良率均为１００％。两组的起效时间、无反应期、ＴＯＦ恢复时间、恢复指数经统计学处理差异均无     

罗库溴铵、维库溴铵和阿曲库铵用于全麻气管插管肌松效应的对比研究

目的观察比较罗库溴铵、维库溴铵及阿曲库铵在全麻诱导气管插管时的肌松效应及不良反应。方法ASAⅠ~Ⅱ级择期全麻下行腹腔镜胆囊切除手术患者120例,随机分为:罗库溴铵组(Ⅰ组)、维库溴铵组(Ⅱ组)、阿曲库铵组(Ⅲ组),每组给2倍ED95剂量肌松剂。Ⅰ组按用量再分为:Ⅰa组(2倍ED95,0.6 mg/kg)、Ⅰb组(3倍ED95,0.9 mg/kg)2个亚组。每组各30例。麻醉诱导依次静注咪达唑仑0.06 mg/kg、芬太尼4μg/kg,异丙酚2 mg/kg后,Ⅰa、Ⅰb组分别静注罗库溴铵0.6 mg/kg、罗库溴铵0.9 mg/kg,Ⅱ组静注维库溴铵0.15 mg/kg,Ⅲ组静注阿曲库铵0.5 mg/kg。观察各组气管插管时的肌松效果及不良反应。结果Ⅰ组的起效时间及插管状态优良率均明显高于Ⅱ、Ⅲ组,Ⅰb组的插管条件好于Ⅰa组。Ⅰ组的支气管痉挛、皮疹等不良反应的发生率明显低于其他组,对循环系统的影响也较小。结论罗库溴铵比维库溴铵、阿曲库铵起效快,恢复迅速,不良反应少,是较好的全麻气管插管肌松药。     

国产维库溴铵的临床应用

维库溴铵是一种理想的中、短效非去极化肌松剂。本文研究了异氟醚、安氟醚、异丙酚对国产维库溴铵肌松作用的影响,及国产维库溴铵对循环系统的影响。资料和方法　36例ＡＳＡⅠ—Ⅱ级的全麻手术病人,随机分为3组:安氟醚组、异氟醚组、异丙酚组,每组12人。病人年龄17～58岁,体重45～68ｋｇ。麻醉诱导3组病人均用芬太尼01ｍｇ,硫喷妥钠6ｍｇ·ｋｇ-1,维库溴铵01ｍｇ·ｋｇ-1静脉注射。麻醉维持:异氟醚组吸入15%～18%浓度的异氟醚,安氟醚组吸入18%～24%的安氟醚。异丙酚组微泵持续注入异丙酚5～7ｍｇ·ｋｇ-1·ｈ-1。应用ＴＯＦ(ＤａｔｅｘＥｎ…     

罗库溴铵对维库溴铵药效的影响及其先一药法的应用

目的：研究罗库溴铵对追加的维库溴铵肌松效应的影响及罗库溴铵－维库溴铵先后给药法的临床价值。方法：观察２倍ＥＤ９５剂量的罗库溴铵（０．６ｍｇ．ｋｇ＾－１）、维库溴铵（０．１ｍｇ．ｋｇ＾－１）分别诱导时的时效及插管条件,以及插管后对追加的１倍ＥＤ９５剂量的维库溴铵的起效及维持时间的影响。结果：罗库溴铵阻滞起效时间显著快于维库溴铵（Ｐ〈０．０１）,二者产生的插管条件及维持时间相似;罗库溴铵插管后对追加的     

成年女性肥胖对维库溴铵肌松的影响

目的　研究成年女性肥胖因素对维库溴铵肌松作用的影响。方法　选择 30名成年女性病人 ,ASAⅠ～Ⅱ级 ,年龄 2 5～ 5 5岁。按体重指数将病人分成三组 ,Ⅰ组为正常对照组 ,Ⅱ组为超重组 ,Ⅲ组为肥胖组。用肌松监测仪给予四个成串刺激 (TOF :频率 2Hz,波宽 2 0 0 μS ,电流强度 5 0mA ,间隔 15s) ,计算机自动记录维库溴铵插管剂量 (0 15mg/kg)的起效时间 (注药结束到T1抑制达 95 %时间 ) ,时效 [注药结束到T1恢复到对照 (Tc)2 5 %的时间 ]。结果　给予诱导插管剂量 (0 15mg/kg)的维库溴铵后 ,与正常对照组相比 [起效时间 (15 5 8±33 70 )s和时效 (36 5± 7 3)min],肥胖组起效时间显著缩短 [(12 1 6± 2 7 4 1)s ,(P <0 .0 5 ) ],时效显著增加[(44 7± 8 7)min ,(P <0 .0 5 ) ]。结论　在临床麻醉中 ,成年女性病人按实际体重给予维库溴铵时 ,肌松作用加强。     

罗库溴铵和维库溴铵用于气管插管困难病人的比较

近期对 2 0例估计插管困难的手术病人 ,采用非去极化肌松药罗库溴铵和维库溴铵配合麻醉药诱导插管 ,并对两种肌松药进行比较 ,发现罗库溴铵更有利于插管操作成功 ,现报告如下。资料与方法　 2 0例需气管插管全麻的手术病人 ,ＡＳＡＩ级 12例 ,Ⅱ级 8例 ,男 11例 ,女 9例 ,年龄 18～ 5 6岁 ,体重 78～ 96ｋｇ。肥胖伴颈短13例 ,肥胖伴张口 <6 0ｃｍ 7例。 2 0例病人按Ｍａｌｌａｍｐａｔｉ评估均属第三类 ,只能见到硬腭或软腭。全部病例术前无心肺肝肾和神经肌肉功能性疾病 ,无水电解质紊乱。麻醉诱导 :将病人随机分为两组 ,每组 10例。Ａ组…     

维库溴铵的合成

目的合成维库溴铵。方法以5α-雄甾-2-烯-17-酮为原料经酯化、氧化、开环、还原、乙酰化、最后与溴甲烷成盐等6步反应合成维库溴铵。结果与结论维库溴铵的结构经红外光谱、差热分析、核磁共振谱、质谱确证,总收率为13.7%。     

喉罩复合无肌松麻醉对脑动脉瘤栓塞术应激的影响

目的：探讨喉罩复合无肌松麻醉对脑动脉瘤栓塞术应激的影响。方法选择实施脑动脉瘤栓塞术的患者80例,将其随机分为观察组和对照组各40例,观察组应用喉罩复合无肌松麻醉,对照组应用气管插管联合肌松药麻醉,比较诱导前（T0）、诱导后插管或喉罩前（T1）、插管或喉罩时（T2）、置入插管或喉罩1 min时（T3）两组患者的心率、平均动脉压及其血糖和皮质醇的变化情况。结果观察组麻醉诱导期间心率和平均动脉压及血糖和皮质醇变化差异无统计学意义（P〉0.05）,对照组T1、T2、T3时间点的心率显著快于T0时间点（P〈0.05）,平均动脉压显著高于T0时间点（P〈0.05）,血糖和皮质醇水平均显著高于T0时间点（P〈0.05）。结论喉罩通气复合无肌松平衡麻醉应用于脑动脉瘤栓塞术,能显著降低患者应激反应,维持循环功能稳定。     

A comparison of the potency and specificity of the direct muscle relaxant activity of azumolene and dantrolene

Dantrolene is a unique directly acting skeletal muscle relaxant that is clinically useful in the treatment of chronic muscle spasticity and malignant hyperthermia. Azumolene is a new dantrolene-like drug that has better aqueous solubility and that may also be of use in the treatment of acute muscle spasm. Potency of both compounds was determined in the anesthetized, curarized rat gastrocnemius (using different routes of administration) and the isolated chick biventer muscle preparations. The specificity of effects in vitro was evaluated by comparing effects in the chick biventer with those seen in the rat aortic strip. Route of administration governed potency for both drugs, with rank order i.v., i.p., and i.d. being the least potent. In vivo, dantrolene was approximately twice as potent as azumolene when administered by any of the routes tested. However, both drugs are equipotent in vitro. Reasons for the discrepancy between in vivo and in vitro potencies are discussed. The muscle relaxant effects of both azumolene and dantrolene are specific for skeletal muscle, being 10-fold more potent in skeletal than in arterial smooth muscle. The reasons for this specificity are probably due to basic differences in the physiology of smooth and skeletal muscle. We conclude that the new agent, azumolene, is a specific, potent skeletal muscle relaxant with properties qualitatively similar to those of dantrolene.     

镇定麻醉和肌松剂配合机械通气抢救危重哮喘30例

目的：探讨镇静麻醉和肌松剂配合机械通气抢救危重哮喘的价值。方法：静脉应用镇静麻醉和肌松剂，经气管插管或气管切开后接呼吸机行机械通气，常规心电舱护，对症处理，待病情稳定后停机拔管。结果：30例危重哮喘患者，经使用镇静麻醉和肌松剂后，人机对抗消失。机械通气后缺氧及二氧化碳潴留明显纠正。气管插管或切开后72小时～15天，平均7日撤机。结论：使用镇静麻醉和肌松剂配合机械通气是抢救危重哮喘的有效方法。     

Magnesium sulfate enhances non-depolarizing muscle relaxant vecuronium action at adult muscle-type nicotinic acetylcholine receptor in vitro

Aim:

To investigate the effect of magnesium sulfate and its interaction with the non-depolarizing muscle relaxant vecuronium at adult muscle-type acetylcholine receptors in vitro.

Methods:

Adult muscle-type acetylcholine receptors were expressed in HEK293 cells. Drug-containing solution was applied via a gravity-driven perfusion system. The inward currents were activated by brief application of acetylcholine (ACh), and recorded using whole-cell voltage-clamp technique.

Results:

Magnesium sulfate (1–100 mmol/L) inhibited the inward currents induced ACh (10 μmol/L) in a concentration-dependent manner (IC₅₀=29.2 mmol/L). The inhibition of magnesium sulfate was non-competitive. In contrast, vecuronium produced a potent inhibition on the adult muscle-type acetylcholine receptor (IC₅₀=8.7 nmol/L) by competitive antagonism. Magnesium sulfate at the concentrations of 1, 3, and 6 mmol/L markedly enhanced the inhibition of vecuronium (10 nmol/L) on adult muscle-type acetylcholine receptors.

Conclusion:

Clinical enhancement of vecuronium-induced muscle relaxation by magnesium sulfate can be attributed partly to synergism between magnesium sulfate and non-depolarizing muscle relaxants at adult muscle-type acetylcholine receptors.     

支气管镜下小儿气道异物取出术中2种肌松药疗效观察

目的观察罗库溴铵和维库溴铵用于支气管镜下小儿气道异物取出术的肌松效果。方法将气管、支气管异物患儿120例随机分为A1组、A2组、W1组和W2组,每组30例。所有患儿常规麻醉后,各组静脉注射相应剂量的肌松药（A1组注射罗库溴铵0.075mg/kg,A2组注射罗库溴铵0.15mg/kg,W1组注射维库溴铵0.05mg/kg,W2组注射维库溴铵0.1mg/kg）。术后比较各组手术时间及苏醒时间。结果各组手术时间比较差异无统计学意义（P〉0.05）。A1组苏醒时间最短为（27.3±6.7）min,其次为A2组、W1组和W2组,差异均有统计学意义（P〈0.05）。结论罗库溴铵用于小儿气管支气管异物取出术起效快,安全性高,是一种较好的肌松药。     

肌松剂在有创机械通气治疗淡水近乎淹溺致急性呼吸窘迫综合征中的运用

目的:探讨目前具有争议的肌松剂(维库溴铵)在有创机械通气治疗淡水近乎淹溺致急性呼吸窘迫综合征(ARDS)中的价值和运用时机.方法:分析我院2001年至今收治的31例淡水近乎淹溺敛ARDS患者,使用肌松剂存活患者作为治疗组,未使用肌松剂患者作为对照组,比较两组患者的血气分析及相关并发症、住院时间、住院费用.结果:治疗组24 h血气分析优于对照组,相关并发症及住院时间、住院费用无明显增加.结论:淹溺患者临床上常出现ARDS,给予足量镇静与镇痛药物治疗,仍达不到治疗目标,可考虑使用肌松剂;时间选择上宜早不宜晚,防止多器官功能不全综合征(MODS)的发生.     

Synthesis and pharmacological screening for muscle relaxant,anticonvulsant, and sedative activities of certain Organic compounds produced by Michael addition

Michael addition of certain nucleophiles on alpha, beta-unsaturated ketones 1 led to the formation of adducts 2-7 as well as the reaction of arylidene derivatives with secondary amines afforded the amino compounds 9 and 11. Also, dialkylmalonates were treated with alpha-cyano cinnamide to afford 13. On the other hand, double Michael cycloaddition of ethylcyanoacetate or tetrachlorophthalic anhydride to the suitable divinylketone were synthesized to produce 15-17. Selected compounds (13 and 6) were screened for muscle relaxant, anticonvulsant, and sedative activities using established pharmacological models. Their activities were compared with that of phenobarbital sodium taken as standard. Compound 6 was the most potent muscle relaxant while compounds 13a and 13c offered the highest anticonvulsant activity. Meanwhile compound 13c showed the highest potentiation of phenobarbital induced sleep in mice.     

Some actions of chandonium iodide, a new short-acting muscle relaxant, in anaesthetized cats and on isolated muscle preparations

1. The actions of the new skeletal muscle relaxant chandonium (HS310) on the cardiovascular, respiratory and skeletal muscle systems of the cat under chloralose anaesthesia and on chick and rat isolated skeletal muscle preparations have been described. 2. In the cat chandonium exhibited a potent, competitive, non-depolarizing neuromuscular blocking action that was rapid in onset and of short duration. It possessed a selective atropine-like action at the cardiac vagus neuro-effector junction but little or no ganglion blocking activity. Neither adrenergic neurone nor α-adrenoceptor blocking properties were evident. 3. Unlike tubocurarine, chandonium was without effect on the airways system of the anaesthetized cat. 4. Chandonium possessed weak anticholinesterase action. It is conceivable that this effect may contribute to its short duration of action. 5. The results from these studies suggest that chandonium may have possible clinical applications as a short-acting muscle relaxant.     

Muscle relaxant and neurotoxic activities of intrathecal baclofen in rats

Intrathecal baclofen therapy by the continuous intrathecal infusion of baclofen has been shown to be an effective treatment for spasticity in patients with spinal cord injury, cerebral palsy, traumatic brain injury, multiple sclerosis and other disorders. To demonstrate the efficacy and safety of intrathecal baclofen therapy, we investigated the muscle relaxant and neurotoxic activities of intrathecal baclofen in rats, compared with intravenous baclofen. Intrathecal and intravenous administration of baclofen dose-dependently inhibited the anemic decerebrate rigidity with ED₅₀ values of 0.31 μg/animal (=1.1–1.3 μg/kg) and 0.43 mg/kg, respectively. Intrathecal administration of baclofen induced no noticeable changes in a spontaneous electroencephalogram at 30 μg/animal. Intravenous administration of baclofen induced an abnormal electroencephalogram with flat waves in all the animals and the no-observed-effect level was estimated to be 5 mg/kg. In some animals, intravenous administration of baclofen induced sporadic spikes or sharp waves with background flat waves, indicating inhibitory and excitatory effects on the central nervous system. In conclusion, intrathecal administration of baclofen dose-dependently inhibited anemic decerebrate rigidity in rats and the effective dose was more than 300 times lower than that of intravenous baclofen. The safety margin of intrathecal baclofen was greater than that of intravenous baclofen (≥97 versus 12). These results suggest that intrathecal baclofen therapy is superior to systemic baclofen therapy in both efficacy and safety.