哌库溴铵前处理对琥珀胆碱的肌震颤及肌松效应的影响

目的：观察哌库溴铵前处理对琥珀胆碱肌震颤的预防作用及对其肌松效应的影响。方法：３６例择期手术病人随机分成三组，Ⅰ组静注琥珀胆碱１ｍｇ／ｋｇ（对照组）。Ⅱ、Ⅲ组静注哌库溴铵１５μｇ／ｋｇ后３．５分钟分别注入琥珀胆碱１ｍｇ／ｋｇ和１．５ｍｇ／ｋｇ。结果：哌库溴铵前处理能有效地消除琥珀胆碱引起的肌震颤，但使１ｍｇ／ｋｇ琥珀胆碱的起效时间延长、阻滞程度降低、气管插管条件变差、肌松恢复时间缩短。当琥珀胆碱的剂量增至１．５ｍｇ／ｋｇ时，肌松效应恢复满意。结论：哌库溴铵前处理使琥珀胆碱的肌松效应减弱，故琥珀胆碱的插管剂量应增至１．５ｍｇ／ｋｇ，以获得满意的肌松。     

维库溴铵对琥珀胆碱肌松效应的影响

研究维库溴铵（Ｖ）作用的不同的不同消退期给予琥珀胆碱的肌松效应。方法：５５例全麻择期手术病人，按维库溴铵作用的不同消退期（５０％或７５％）和琥珀胆碱的剂量（１．０ｍｇ／ｋｇ或１．５ｍｇ／ｋｇ），随机分为六组。１－４组在维库溴铵作用消退５０％或７５％时，分别给予胆碱１．０ｍｇ／ｋｇ和１．５ｍｇ／ｋｇ；５、６组分别阳琥胆三１．ｍｇ／ｋｇ和１．５ｍｇ／ｋｇ作为对照。结果１－４组的琥珀胆碱使用时间比对照组     

两类肌松药间的相互作用与影响

两类肌松药给药顺序不同，相互作用结果相反。琥珀胆碱或十甲铵强化其后所给筒简明毒，泮库溴铵，维库溴铵，阿曲库铵，哌库溴铵的阻滞效应，如先以筒箭毒，三碘季铵酚，维库溴铵等作预处理，与其后所给琥珀胆碱，十甲铵的相互影响则表现为拮抗。其机理至今尚不完全清楚，可能以神经肌肉接头处的相互作用为主。     

两类肌松药间的相互作用与影响

两类肌松药给药顺序不同,相互作用结果相反。琥珀胆碱或十甲铵强化其后所给筒箭毒、泮库溴铵、维库溴铵、阿曲库铵、哌库溴铵的阻滞效应;如先以筒箭毒、三碘季铵酚、维库溴铵等作预处理,与其后所给琥珀胆碱、十甲铵的相互影响则表现为拮抗,其机理至今尚不完全清楚,可能以神经肌肉接头处的相互作用为主。     

ORG9487对拇内收肌和喉内收肌的神经肌肉阻滞

ORG9487是新型速效非去极化类固醇肌松药。该 药对拇内收肌的起作用时间与1mg·kg~(-1)的琥珀胆碱类似,估计ORG9487的ED_(90)约为1.15mg·kg~(-1),但作用持续时间比琥珀胆碱稍长。注ORG9487 1.5mg·kg~(-1)后,四个成串刺激(TOF)和T_1恢复到90％的时间为16.4min;而注琥珀胆碱1mg·kg~(-1)则为10.6min。已证明维库溴铵和罗库溴铵引起喉内收肌和拇内收肌松弛的起效时间有差异,以维库溴铵起效较快。作者为了     

潘库溴铵与维库溴铵,阿曲库铵合用的实验研究

目的：将结构相近的潘库溴铵与维库溴铵和结构不同的潘库溴铵与阿曲库铵合用，比较其作用效果以判别相互作用的类型。方法：以刺激电极和力－位移换能器监测兔胫前肌的阻滞程度。选１５只新西兰白兔通过累积给药法求得兔三种药物的ＥＤ５０值。再将２０只新西兰白兔随机分为４组，分别采用潘库溴铵与维库溴铵、阿曲库铵合用、按不同顺序给药的方法。每种肌松药剂量为１／２×ＥＤ５０。结果：潘库溴铵与阿曲库铵合用，Ｔ１抑制９２％～９７％，明显高于５０％（Ｐ＜０．０１），提示有协同作用；而潘库溴铵与维库溴铵合用，Ｔ１仅抑制３９％～５２％。结论：非去极化肌松药间之相互作用与药物结构相关。     

罗库溴铵与琥珀胆碱对脑血管血流动力学的影响及比较

研究罗库溴铵与琥珀胆碱对脑血管血流动力学的影响，以进一步证明作为全麻诱导用药，前者取代后者的合理性。方法：４６例择期病人随机分成两组，罗库溴铵组（Ｒ组）２１例，琥珀胆碱组（Ｓ组）２５例。全麻诱导应用芬太尼和硫喷妥钠后，Ｒ组静注罗库溴铵０．９ｍｇ／ｋｇ，Ｓ组静注琥珀胆碱１．５ｍｇ／ｋｇ。分别于全麻诱导前后，静注肌松药后１、５、１０分钟时检测ＣＶＤＩ。结果：（１）两组全麻醉诱导后平均，最小脑血流量（Ｑ     

瑞库溴铵的临床药理学

瑞库溴铵是维库溴铵的衍生物,因其具有起效快、作用时间短的特点,有可能替代琥珀胆碱作为快速诱导插管的短时效非去极化肌松药,成为最近临床研究的热点药物之一。     

普鲁卡因对维库溴铵阻滞过程,效应影响的时量研究

定量观测了普鲁卡因对静滴维库溴铵的阻滞过程、时效及两药对血清胆碱酯酶活性的影响。结果发现，（１）单纯静滴维库溴铵或配伍静滴普鲁卡因对血清胆碱酯酶活性影响轻微；（２）普鲁卡因能增强静滴维库溴铵的阻滞效应；（３）静滴普鲁卡因初始期增强维库溴铵的神经肌肉接头后膜阻滞作用，不影响其接头前膜的效应，对接头前膜的增加作用于２０～４０分钟出现，并保持在静滴普鲁卡因的全程中；（４）普鲁卡因延长维库溴铵阻滞后Ｔ１（四次成串刺激中第一个颤搐反应）恢复至２５％的时间，但不影响Ｔ；２５％自主或桔抗后恢复至Ｔ１、ＴＲ（四次成串刺激中第四与第一个颤搐反应之比）达７０％的时间。     

琥珀胆碱对罗库溴铵肌松作用的影响

目的：本试验应用ＰＩ控制器自动化反馈控制罗库溴铵的输注,将肌松维持在恒定水平,通过确定罗库溴铵的稳态输注速率,来研究琥珀胆碱对罗库溴铵肌松作用的影响。方法：选择１４例ＡＳＡ分级Ⅰ～Ⅱ级的手术病人,随机分成对照组（７例）和试验组（７例）。对照组在麻醉诱导后,静注０．６ｍｇ／ｋｇ罗库溴铵进行气管插管;试验组则静注１．５ｍｇ／ｋｇ琥珀胆碱后气管插管,待肌松作用完全恢复后,再静注０．６ｍｇ／ｋｇ罗库溴铵,     

The effect of succinylcholine on atracurium–induced neuromuscular block

Background : The interaction between prior succinylcholine and atracurium has been found only after full recovery of succinylcholine block. We investigated whether the effect of succinylcholine on atracurium block may depend on the level of recovery from succinylcholine.
Methods : Fifty patients in 4 groups received atracurium 0.2 mg/ kg when first response (Tl) in train–of–four (TOF) after succinylcholine 1 mg/kg had recovered to 5%, 25%, 75% or 100%. A control group received only atracurium. The following indices were compared: the time from injection of atracurium to maximum block (onset time) and to return of Tl to 25% (duration 25%), maximal depression of Tl, time from 25% to 75% recovery of Tl (interval 25–75%) and time from injection of atracurium to a TOF ratio of 0.75 (duration TOF 0.75).
Results : Onset time was shorter, max Tl depression was greater and duration 25% increased the more succinylcholine recovery progressed. Neither interval 25–75% nor duration TOF 0.75 varied with the level of recovery from succinylcholine. The control group showed a shorter latency and onset time compared to the early (5%) recovery group and a longer onset time and less depressed Tl compared to the late (100%) recovery group. There was no difference between the control group and the early or late recovery groups, respectively for duration 25% or duration TOF 0.75.
Conclusion : The effect of prior administration of succinylcholine on atracurium block depends on the state of recovery from succinylcholine and concerns both its potency, onset and duration characteristics.     

Effect of cimetidine on neuromuscular blockade by succinylcholine and pancuronium

The effect of cimetidine on neuromuscular blockade by succinylcholine and pancuronium was investigated in 54 adult patients scheduled for elective surgery. The neuromuscular blocking properties were estimated with single twitch height (T1) which was obtained by measuring the acceleration of adduction of the thumb in response to the ulnar nerve stimulation under N2O-fentanyl anesthesia. In cimetidine group, cimetidine 200 mg was administered orally on the night before surgery and 90 mins before anesthesia. Succinylcholine 1 mg.kg-1 (n = 14) or 1.5 mg.kg-1 (n = 20) was injected intravenously, and the onset time (from injection to 0% T1), the duration of maximal block (0% T1), and the recovery time from injection to 50% and 75% of control twitch height were evaluated. ED25 and ED50 of pancuronium were calculated from the dose response curve obtained by incremental administration of the drug (n = 20) whose total cumulative dose was 0.1 mg.kg-1. The recovery index of pancuronium was determined by measuring the 25%-75% recovery time. There was no significant difference between cimetidine pretreated patients and non-pretreated patients regarding these parameters of neuromuscular blockade with both succinylcholine and pancuronium. In conclusion, cimetidine has no influence on neuromuscular blockade of succinylcholine and pancuronium under N2O-fentanyl anesthesia.     

Evolution of vecuronium requirements for stable mechanical effect: comparison with or without previous succinylcholine administration

To evaluate possible interactions between residual succinylcholine and vecuronium, the amount of vecuronium required to maintain the twitch height (TH) at 10% of its initial value was measured over a 90-min period by the on-demand infusion method in two series of 15 adult patients (ASA class I-II). One group, the vecuronium treatment (V) group, received 70 micrograms X kg-1 of vecuronium and the on-demand infusion. The second group, the succinylcholine-vecuronium treatment group (SV), was given 30 micrograms X kg-1 of vecuronium and on-demand infusion 5 min after the complete recovery of TH after administration of 1 mg X kg-1 of succinylcholine. During the first 10 min, the amount of vecuronium required to maintain TH at 10% of its control was significantly greater in the group given V than in the group given SV, 15122 +/- 856 (mean +/- SEM) vs 9851 +/- 486 micrograms X m-2 X hr-1 (P less than 0.001). Thereafter, the amount of vecuronium required to maintain TH at 10% of control was similar: 2808 +/- 275 and 3068 +/- 206 micrograms X m-2 X hr-1. When the infusion of vecuronium was stopped after 90 min, the time required for spontaneous recovery from 25 to 75% of control TH levels was similar: 20.1 +/- 3.3 min in the group given V and 18.9 +/- 2.5 min in the group given SV (not significant). We conclude that after a vecuronium on-demand infusion of long duration (lasting more than 90 min), previous succinylcholine administration does not interfere with late vecuronium requirements and the spontaneous rate of recovery of TH.     

Atracurium and vecuronium: repeated bolus injection versus infusion.

The purpose of this study was to compare the characteristics of recovery from neuromuscular blockade after either atracurium or vecuronium given by intravenous infusion or by repeated injection. Four groups of 10 patients each were studied during nitrous oxide narcotic anesthesia. An initial intravenous dose of 2 x ED95 of either muscle relaxant was followed by an intravenous infusion started at 5% recovery of control twitch tension and adjusted for 95% block or by repeated injection of 0.6 x ED95 administered whenever twitch tension had returned to 25% of control. There were no significant differences between the maintenance doses required based on method of administration: atracurium repeated injection, 1.6 +/- 0.3 x ED95 h-1; atracurium infusion, 1.7 +/- 0.3 x ED95 h-1; vecuronium repeated injection, 1.8 +/- 0.5 x ED95 h-1; and vecuronium infusion, 1.6 +/- 0.4 x ED95 h-1. Nevertheless, differences of up to 20 min were noted in the recovery indices in the following order: atracurium repeated injection = atracurium infusion less than vecuronium repeated injection less than vecuronium infusion. A single dose of neostigmine (7 micrograms/kg) significantly reduced the recovery indices, thereby eliminating their differences.     

Early and late reversal of rocuronium and vecuronium with neostigmine in adults and children.

We investigated the influence of the timing of neostigmine administration on recovery from rocuronium or vecuronium neuromuscular blockade. Eighty adults and 80 children were randomized to receive 0.45 mg/kg rocuronium or 0.075 mg/kg vecuronium during propofol/fentanyl/N2O anesthesia. Neuromuscular blockade was monitored by train-of-four (TOF) stimulation and adductor pollicis electromyography. Further randomization was made to control (no neostigmine) or reversal with 0.07 mg/kg neostigmine/0.01 mg/kg glycopyrrolate given 5 min after relaxant, or first twitch (T1) recovery of 1%, 10%, or 25%. Another eight adults and eight children received 1.5 mg/kg succinylcholine. At each age, spontaneous recovery of T1 and TOF was similar after rocuronium and vecuronium administration but was more rapid in children (P < 0.05). Spontaneous recovery to TOF0.7 after rocuronium and vecuronium administration in adults was 45.7 +/- 11.5 min and 52.5 +/- 15.6 min; in children, it was 28.8 +/- 7.8 min and 34.6 +/- 9.0 min. Neostigmine accelerated recovery in all reversal groups (P < 0.05) by approximately 40%, but the times from relaxant administration to TOF0.7 were similar and independent of the timing of neostigmine administration. Recovery to T1 90% after succinylcholine was similar in adults (9.4 +/- 5.0 min) and children (8.4 +/- 1.1 min) and was shorter than recovery to TOF0.7 in any reversal group after rocuronium or vecuronium administration. Recovery from rocuronium and vecuronium blockade after neostigmine administration was more rapid in children than in adults. Return of neuromuscular function after reversal was not influenced by the timing of neostigmine administration. These results suggest that reversal of intense rocuronium or vecuronium neuromuscular blockade need not be delayed until return of appreciable neuromuscular function has been demonstrated. Implications: These results suggest that reversal of intense rocuronium or vecuronium neuromuscular blockade need not be delayed until return of appreciable neuromuscular function has been demonstrated. Although spontaneous and neostigmine-assisted recovery is more rapid in children than in adults, in neither is return of function as rapid as after succinylcholine administration.     

Does vecuronium accumulate in the renal transplant patient?

Twenty ASA physical status Class III patients undergoing cadaver renal transplantation were studied. After 90 per cent T1 recovery, as determined by train-of-four measurement, from 1.0 mg.kg-1 succinylcholine to facilitate tracheal intubation, nine patients received atracurium 0.25 mg.kg-1 (Group I) and 11 patients received vecuronium 0.05 mg.kg-1 (Group II) intravenously. The following measurements were made: time to maximum block onset (first dose Max), injection to start of recovery (start REC1), injection to 25 per cent T1 twitch recovery (REC 251), injection to 75 per cent T1 (REC 75(1], injection to 90 per cent T1 (REC 90(1] and time from 25-75 per cent recovery T1 (REC 25-75(1]. Maximum blockade (Max block 1) was also measured. At 90 per cent T1 recovery, if time permitted, an identical dose of the appropriate relaxant was administered. Time from second dose to onset of maximum block (second dose Max) and 90 per cent recovery after second dose (REC 90(2] were then measured. At the conclusion of surgery, neuromuscular blockade was reversed with neostigmine 2.5 mg and glycopyrrolate 0.5 mg. One way ANOVA was performed to determine significance between the groups and a p less than 0.05 was considered significant. A paired t test was also performed between REC 90(1) and REC 90(2) for atracurium and vecuronium respectively. A p less than 0.05 was again considered significant. Measurement of first dose Max, start REC1, REC25(1), REC 75(1), REC 90(1), REC 25-75(1) and Max block 1 revealed no difference between the patients receiving an initial dose of atracurium and those receiving vecuronium.(ABSTRACT TRUNCATED AT 250 WORDS)     

Prediction of the maintenance dose of vecuronium for continuous infusion]

The purpose of this study is to examine how to predict the optimal maintenance dose of vecuronium for continuous infusion, knowing the recovery time from the block induced by the first bolus injection. All patients studied were undergoing surgical procedures and were anesthetized using thiopental, vecuronium, 50% nitrous oxide and 2% enflurane in oxygen. Mechanical twitch responses of adductor pollicis muscle caused by the stimulation of the ulnar nerve supramaximally were monitored. Vecuronium concentrations in the plasma were measured using high performance liquid chromatography. The experiments consisted of two phases. Phase 1.: To demonstrate the relationship between the recovery time (T0-T25) and the maintenance dose. Thirty patients were studied in this phase. A bolus injection was given as the first dose (1.5 mg.kg-1). During the recovery from the first block, recovery time (T1) was measured and the second dose (2 mg) was injected at the T25 (25% control twitch height). After waiting the recovery until the T25, the third dose (2 mg) was injected. The duration (T2) (min) between the second and the third injection was measured. The maintenance dose-recovery time curve was obtained. Y = 52.70.exp (-17.50 X) + 1224.53.exp (-224.27X), X = recovery time (min), Y = maintenance dose (mg.hr-1). Phase 2.: Thirty patients were studied in this phase. Patients received infusions after the bolus injection. The infusion rates were obtained from the maintenance dose-recovery time curve.(ABSTRACT TRUNCATED AT 250 WORDS)     

Comparison of tracheal intubating conditions and neuromuscular blocking profiles after intubating doses of mivacurium chloride or succinylcholine in surgical outpatients

Thirty ASA physical status I or II outpatients scheduled to undergo short procedures (less than 1 hr in duration) requiring tracheal intubation received either 1.0 mg/kg succinylcholine or 0.20 mg/kg (2.5 x ED95) or 0.25 mg/kg (3 x ED95) mivacurium. A N2O/O2/narcotic anesthetic technique was utilized and the ulnar nerve was stimulated with subcutaneous electrodes placed at the wrist. Tracheal intubation was attempted in all patients either 2 min after mivacurium or 1 min after succinylcholine. Intubation conditions were not different between the succinylcholine and mivacurium groups or between the two mivacurium groups. The onset and duration of neuromuscular blockade were shorter with succinylcholine than with mivacurium. Suppression of the T1 response to 90% of baseline occurred in 0.9 min with 1.0 mg/kg succinylcholine and at 2.2 and 1.5 min respectively, with 0.20 mg/kg and 0.25 mg/kg mivacurium. Initial recovery of the T1 response occurred at 6.4 min after 1.0 mg/kg succinylcholine and 12.7 and 13.6 min respectively after 0.20 mg/kg and 0.25 mg/kg mivacurium. Subsequent to initial recovery from the intubating dose of relaxant, infusions of mivacurium or succinylcholine were administered to maintain approximately 95% block. The mean infusion rates were 6.6 micrograms.kg-1.min-1 mivacurium and 41.2 micrograms.kg-1.min-1 for succinylcholine. Spontaneous recovery from neuromuscular blockade occurred more quickly after succinylcholine than after mivacurium: the time from cessation of infusion to recovery of T1 to 95% of baseline was 6.5 min in patients given succinylcholine and 16.7 min in patients given mivacurium. When reversal was in order, residual mivacurium-induced blockade was readily antagonized by 0.045 mg/kg neostigmine.(ABSTRACT TRUNCATED AT 250 WORDS)     

Clinical pharmacology of mivacurium chloride: a review.

Mivacurium chloride (Mivacron) is a new benzylisoquinolinium choline-like diester neuromuscular blocking drug with an onset of action at equipotent doses that is comparable to atracurium and vecuronium but slower than succinylcholine. Its clinical duration (injection-25% recovery and injection-95% recovery) is twice that of succinylcholine but one-half to one-third that of atracurium and vecuronium. Mivacurium is easy to use as a continuous infusion and when used this way its recovery characteristics are unchanged. It is readily antagonized by anticholinesterase drugs. The ED95 in adults under narcotic-based anesthesia is 0.07-0.08 mg/kg. At twice the ED95 (0.15 mg/kg) onset time is about 2 to 3 minutes, duration to 25% recovery is 15 to 20 minutes, and 5-95% recovery time about 14 minutes. The mean infusion rate in adults is 6 micrograms/kg/min (range 2-15) with a 5-95% recovery time of 14 minutes. Enflurane and isoflurane require a 20-30% decrease in dosage; halothane, enflurane, and isoflurane prolong the duration of mivacurium 25-30%. The ED95 in children 2 to 12 years of age is slightly higher (0.09-0.11 mg/kg) with a faster onset and shorter duration. In these young patients, a dose of 0.2 mg/kg has an onset comparable to succinylcholine. Being chemically related to atracurium, mivacurium may cause histamine release. When administered rapidly at doses of 0.2 mg/kg or greater in adults, histamine release and transient hypotension have been observed. Doses of 0.2 mg/kg or higher are not recommended by the manufacturer. Mivacurium is metabolized by plasma cholinesterase. In vitro, the rate is about 70% that of succinylcholine. In patients with normal or slightly less than normal plasma cholinesterase activity, no prolonged durations of action have been observed. In patients heterozygous for the atypical gene and at a dose of 0.2 mg/kg, 50% prolongation has been shown. Those individuals homozygous for the atypical gene are exquisitely sensitive to mivacurium and have a markedly prolonged blockade that is readily reversible. In these patients and those with acquired deficiencies, mivacurium should not be used. The duration of action in elderly patients is comparable to that in the young, while in prerenal transplant patients, its duration is prolonged by about 50%, and in prehepatic transplant patients, duration of block is increased threefold. Mivacurium possesses the advantages of short duration, unchanged recovery characteristics following infusions (without phase II block or tachyphylaxis), and precise control.(ABSTRACT TRUNCATED AT 250 WORDS)     

Mivacurium or Vecuronium for paediatric ENT surgery Clinical experience and cost analysis

BACKGROUND: The present study compared the quality of neuromuscular block and costs after equipotent doses of mivacurium and vecuronium in the context of paediatric ENT surgery. METHODS: A total of 30 children undergoing elective tonsillectomy were included and randomised in two groups (n = 15 for each) according to the neuromuscular blocking agent (NMBA) used. Anaesthesia was induced with alfentanil (15 micrograms/kg), propofol (3 mg/kg) and either 0.2 mg/kg mivacurium or 0.14 mg/kg vecuronium. For maintenance of anaesthesia propofol (8-12 mg/kg/h) was given. Neuromuscular block was assessed by electromyography using train-of four stimulation and the following parameters were quantified: Twitch height (T1) 2 min after the initial bolus of the myorelaxant; duration until recovery to 10% T1, number and duration of bolus injections of the myorelaxant needed to maintain neuromuscular block to a T1 < 10%. In addition, the intubating conditions, number of patients needing pharmacological reversal at the end of surgery, adverse reactions and the costs for neuromuscular block and pharmacological antagonization were assessed. RESULTS: Intubation conditions were comparable between both study groups: mivacurium--excellent: 7, good: 5, not acceptable: 1; vecuronium--excellent: 11, good: 4 (n.s.). T1 at 2 min was 16 (15)% for mivacurium and 6 (9)% for vecuronium (P < 0.05). Time to 10% T1 recovery was 6.1 (1.7) min for mivacurium and 21.8 (3.7) min for vecuronium (P < 0.01). In the mivacurium group 7 repetitive doses (range: 4-18) were needed to maintain T1 < 10% during surgery, whereas children treated with vecuronium needed only 1 maintenance dose (range: 0-2) (P < 0.01). Two children in the mivacurium group and 11 in the vecuronium group required pharmacological reversal of the NMB at the end of surgery (P < 0.01). The overall costs of NMB were significantly higher in the mivacurium group as compared to vecuronium 12.88 (4.5) Euro vs 9.96 (2.4) Euro; P < 0.05. CONCLUSIONS: In conclusion, mivacurium-induced NMB is of very short duration in paediatric patients, and therefore repetitive doses are required to maintain a deep neuromuscular block. Nevertheless, residual paralysis is less frequent after mivacurium. The neuromuscular block after mivacurium was more expensive and residual paralysis less frequent compared to vecuronium.