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Background: Sugammadex reverses the neuromuscular blocking effects of rocuronium by chemical encapsulation. The efficacy, safety, and pharmacokinetics of sugammadex for reversal of profound rocuronium-induced neuromuscular blockade were evaluated.

Methods: Ninety-eight male adult patients were randomly assigned to receive sugammadex (1, 2, 4, 6, or 8 mg/kg) or placebo at 3, 5, or 15 min after 0.6 mg/kg rocuronium. Patients were anesthetized with propofol and fentanyl. The primary endpoint of the study was the time to achieve a recovery of train-of-four ratio to 0.9. Neuromuscular blockade was measured using acceleromyography. Concentrations of rocuronium and sugammadex were determined in venous blood and urine samples. A population pharmacokinetic model using NONMEM (GloboMax LLC, Hanover, MD) was applied.

Results: The mean time to recovery of the train-of-four ratio to 0.9 after dosing at 3, 5, and 15 min decreased from 52.1, 51.7, and 35.6 min, respectively, after administration of placebo to 1.8, 1.5, and 1.4 min, respectively, after 8 mg/kg sugammadex. Sugammadex was safe and well tolerated. However, 20.4% of patients showed signs of inadequate anesthesia after its administration. The median cumulative excretion of rocuronium in the urine over 24 h was 26% in the placebo group and increased to 58-74% after 4-8 mg/kg sugammadex. The mean plasma clearances of sugammadex and rocuronium were 0.084 and 0.26 l/min, respectively.  相似文献   


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《Transplantation proceedings》2019,51(7):2265-2267
IntroductionSugammadex has the steroid-encapsulating effect that reverses neuromuscular block induced by aminosteroid neuromuscular-blocking agents. Sugammadex can interact with other drugs that have the same steroidal structure with rocuronium, such as corticosteroids. Corticosteroids play a crucial role in the immunosuppression of kidney transplantation. The purpose of this study was to determine if there are any differences in grafted kidney function in recipients of kidney transplantation when sugammadex or neostigmine is given to the recipient.MethodsThe study included 42 recipients of kidney transplant, with complete, readable medical charts and anesthetic records. Fourteen recipients’ neuromuscular block was reversed with sugammadex (group S) and 28 recipients’ neuromuscular block was reversed with neostigmine (group N). We tested noninferiority for serum creatinine during the preoperative period and 5 days after transplantation. Short-term (28 days) outcomes of kidney transplantations were assessed by the incidence of acute rejection episodes, graft failure, length of stay at hospital, and mortality.ResultsThere were no significant differences in demographic characteristics, serum creatinine values, short-term outcomes, and graft survival rates at 28 days’ postoperatively between group S and group N (P > .05).ConclusionsOur data showed no difference in risk of serious adverse effects on short-term graft functions in patients who underwent kidney transplantation. However, considering the sugammadex-corticosteroids interaction, the immunosuppression and long-term effects on grafted kidney functions, current safety experience is insufficient to support the recommendation of routine sugammadex use in this population. These results need to be confirmed by sufficiently powered, controlled, pharmacokinetic, and pharmacodynamic studies on larger patient populations.  相似文献   

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异氟醚和地氟醚对罗库溴铵肌松作用的影响   总被引:2,自引:1,他引:1  
目的:观察1.0MAC异氟醚或地氟醚对罗库溴铵增效作用的影响。方法:选择18例择期手术病人随机分为地氟醚和异氟醚组,每组在静脉诱导麻醉后,先测得维持90%肌松并达到稳定后罗库溴铵的注射速率,然后吸入异氟醚或地氟醚,使呼气末浓度为1.0MAC,再调整罗库溴铵的注入速率,维持90%的肌松,观察吸入全麻后罗库溴铵的注射速率随时间变化的趋势。结果:异氟醚、地氟醚均显著降低了罗库溴铵的注入速率,且随吸入时间  相似文献   

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Background: The purpose of this study was to determine the changes in the plasma concentration of rocuronium and the reversal of its neuromuscular blockade after the intravenous infusion of Org 25969, the novel neuromuscular block-reversal agent, in anesthetized guinea pigs.

Methods: Rocuronium was infused for 1 h at a rate of 12-19 nmol[middle dot]kg-1[middle dot]min-1 to produce a steady-state 90% neuromuscular block. After 30 min, a concomitant infusion of either the reversal agent Org 25969 at a rate of 50 nmol[middle dot]kg-1[middle dot]min-1 or an infusion of an equivalent volume of saline was started. The time course of plasma concentrations of rocuronium was determined by use of liquid chromatography-mass spectrometry/mass spectrometry.

Results: In both treatment groups, a steady-state plasma concentration of rocuronium was obtained after 30 min. In the saline-treated group, the plasma concentration of rocuronium and depth of block remained constant. In the Org 25969 group, neuromuscular block was reversed while the rocuronium infusion was ongoing. Simultaneously, an increase in the total plasma concentration of rocuronium (free and complexed) was observed, even though the infusion rate of rocuronium was not changed. Compared with the saline-treated group, a small increase in the postmortem bladder concentration of rocuronium was detected.  相似文献   


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Background

The use of neuromuscular blocking agents may affect intraoperative neuromonitoring during thyroid surgery. A selective neuromuscular recovery protocol was evaluated in a retrospective cohort study during human thyroid neural monitoring surgery.

Methods

One hundred and twenty-five consecutive patients undergoing thyroidectomy with intraoperative neuromonitoring followed a selective neuromuscular block recovery protocol—single intubating dose of rocuronium followed by sugammadex if needed at the first vagal stimulation (V1).

Results

Data from 120 of 125 patients could be analysed. Fifteen (12.5%) patients needed sugammadex reversal to obtain an EMG response at the first vagal stimulation (V1). In the remaining 105 patients, spontaneous recovery of rocuronium-induced neuromuscular block was sufficient for a successful first vagal stimulation (V1).

Conclusions

In patients undergoing thyroid surgery, routine reversal of rocuronium block with sugammadex is not mandatory for reliable intraoperative neuromonitoring. A selective neuromuscular block recovery approach may be a valuable and more cost-efficient alternative to routine reversal.
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Background: Reversal of rocuronium-induced neuromuscular blockade can be accomplished by chemical encapsulation of rocuronium by sugammadex, a modified [gamma]-cyclodextrin derivative. This study investigated the efficacy and safety of sugammadex in reversing rocuronium-induced profound neuromuscular blockade at 5 min in American Society of Anesthesiologists physical status I and II patients.

Methods: Forty-five American Society of Anesthesiologists physical status I and II patients (aged 18-64 yr) scheduled to undergo surgical procedures (anticipated anesthesia duration >= 90 min) were randomly assigned to a phase II, multicenter, assessor-blinded, placebo-controlled, parallel, dose-finding study. Anesthesia was induced and maintained with propofol and an opioid. Profound neuromuscular blockade was induced with 1.2 mg/kg rocuronium bromide. Sugammadex (2.0, 4.0, 8.0, 12.0, or 16.0 mg/kg) or placebo (0.9% saline) was then administered 5 min after the administration of rocuronium. Neuromuscular function was monitored by acceleromyography, using train-of-four nerve stimulation. Recovery time was the time from the start of administration of sugammadex or placebo, to recovery of the train-of-four ratio to 0.9. Safety assessments were performed on the day of the operation and during the postoperative and follow-up period.

Results: A total of 43 patients received either sugammadex or placebo. Increasing doses of sugammadex reduced the mean recovery time from 122 min (spontaneous recovery) to less than 2 min in a dose-dependent manner. Signs of recurrence of blockade were not observed. No serious adverse events related to sugammadex were reported. Two adverse events possibly related to sugammadex were reported in two patients (diarrhea and light anesthesia); however, both patients recovered without sequelae.  相似文献   


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目的:比较七氟烷对顺式阿曲库铵和罗库溴铵肌松效应的影响。方法:择期手术患者240例,随机分为顺式阿曲库铵组(CIS120例)和罗库溴铵组(ROC120例)。两组患者再随机分为丙泊酚组(60例)和七氟烷组(60例),均静脉注射咪达唑仑、芬太尼和丙泊酚行麻醉诱导,丙泊酚组靶控输注丙泊酚维持麻醉,设定血浆靶控浓度2~6μg/mL,输注丙泊酚5min后静脉注射顺式阿曲库铵0.15mg/kg或罗库溴铵0.6mg/kg;七氟烷组在呼气末七氟烷浓度稳定于1MAC5min后静脉注射顺式阿曲库铵0.15mg/kg或罗库溴铵0.6mg/kg。结果:CIS两组,起效时间差异无统计学意义(P〉0.05);七氟烷组完全肌松时间、维持时间与丙泊酚组比较均显著延长(P〈0.01)。ROC两组,起效时间差异无统计学意义(P〉0.05);七氟烷组完全肌松时间、维持时间与丙泊酚组比较均显著延长(P〈0.01)。结论:七氟烷对顺式阿曲库铵及罗库溴铵的肌松均有增效作用。  相似文献   

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《Anesthesiology》2008,109(2):188-197
Background: Sugammadex (Org 25969), a novel, selective relaxant binding agent, was specifically designed to rapidly reverse rocuronium-induced neuromuscular blockade. The efficacy and safety of sugammadex for the reversal of profound, high-dose rocuronium-induced neuromuscular blockade was evaluated.

Methods: A total of 176 adult patients were randomly assigned to receive sugammadex (2, 4, 8, 12, or 16 mg/kg) or placebo at 3 or 15 min after high-dose rocuronium (1.0 or 1.2 mg/kg) during propofol anesthesia. The primary endpoint was time to recovery of the train-of-four ratio to 0.9. Neuromuscular monitoring was performed using acceleromyography.

Results: Sugammadex administered 3 or 15 min after injection of 1 mg/kg rocuronium decreased the median recovery time of the train-of-four ratio to 0.9 in a dose-dependent manner from 111.1 min and 91.0 min (placebo) to 1.6 min and 0.9 min (16 mg/kg sugammadex), respectively. After 1.2 mg/kg rocuronium, sugammadex decreased time to recovery of train-of-four from 124.3 min (3-min group) and 94.2 min (15-min group) to 1.3 min and 1.9 min with 16 mg/kg sugammadex, respectively. There was no clinical evidence of reoccurrence of neuromuscular blockade or residual neuromuscular blockade. Exploratory analysis revealed that prolongation of the corrected QT interval considered as possibly related to sugammadex occurred in one patient. Another two patients developed markedly abnormal arterial blood pressure after sugammadex that lasted approximately 15 min.  相似文献   


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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,  相似文献   

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Background: Mivacurium, a nondepolarizing muscle relaxant, is hydrolyzed by butyrylcholinesterase. The use of butyrylcholinesterase for antagonism of profound mivacurium-induced blockade has not been studied in humans. In part 1 of this two-part study, the authors examined the relationship between the posttetanic count (PTC) and recovery from profound mivacurium-induced blockade. In part 2, an attempt was made to antagonize a quantified level of profound mivacurium-induced blockade using either butyrylcholinesterase, edrophonium, or neostigmine.

Methods: Eighty-seven ASA physical status 1 or 2 adult patients were given 0.15 mg *symbol* kg sup -1 mivacurium during fentanyl-thiopental-nitrous oxide-isoflurane anesthesia. They were randomly assigned to eight groups. Neuromuscular function was monitored by recording the mechanomyographic response of the adductor pollicis to PTC and train-of-four (TOF) stimulation in all patients except those in group 1 where the TOF was the only pattern used. In part 1, neuromuscular function was allowed to recover spontaneously in ten patients (group 1; control-TOF) until TOF ratio (the amplitude of the fourth evoked response as a fraction of the first evoked response: T4/T1) had reached 0.75. The temporal relationship between PTC and the first reaction to TOF stimulation was determined in another 21 patients, and neuromuscular function in 10 of these patients was allowed to recover spontaneously until TOF ratio had reached 0.75 (group 2; control-PTC). In part 2, the antagonism of mivacurium-induced profound (PTC greater or equal to 1; groups 3-6) and 90% block (groups 7-8) of twitch height were investigated in another 56 patients. Groups 3 and 7 received neostigmine 0.06 mg *symbol* kg sup -1 whereas groups 4 and 8 received edrophonium 1 mg *symbol* kg sup -1, respectively. Groups 5 and 6 received exogenous human butyrylcholinesterase equivalent to activity present in 25 or 70 ml *symbol* kg sup -1 of human plasma, respectively.

Results: Neither butyrylcholinesterase nor edrophonium shortened the times from first PTC response to TOF = 0.75 compared to group 2. Neostigmine resulted in prolongation of recovery time. There was a linear relationship (r = -0.80; P = 0.00001) between PTC and time of onset of TOF response.  相似文献   


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The required characteristics of neuromuscular blockers for rapid sequence induction (RSI) are clearly defined: nearly immediate effectiveness and short duration of effect. These demands are not only necessary for ideal conditions of quick endotracheal intubation without mask-bag intermediate ventilation but are also essential to enable a quick return to sufficient spontaneous breathing in case of a cannot intubate cannot ventilate situation. Until recently only succinylcholine had these characteristics; however, a considerable number of dangerous side effects and contraindications had to be accepted. In 1996, rocuronium was introduced, which was capable of immediately establishing good intubation conditions similar to succinylcholine. However, the median duration of effect is 45–60 min and it therefore contains a risk if the patient cannot be ventilated and oxygenated. Therefore, rocuronium is considered a good alternative but not a complete substitute for succinylcholine. The introduction of sugammadex in 2008 for quick reversal of rocuronium changed matters. Comparative studies from the past 4 years dealing with rocuronium/sugammadex versus uccinylcholine in RSI showed that rocuronium and sugammadex combined enabled a significantly faster return to sufficient spontaneous ventilation in emergency situations and also proved that the use of rocuronium significantly reduced the degree of desaturation during the interval between injection and ventilation postintubation. Conclusion: rocuronium used in hospital is a very good substitute for succinylcholine as a neuromuscular blocker during RSI as long as sugammadex is at hand for reversal. It remains to be considered that in a situation with severe problems of the airway and breathing, which are the main preclinical indications for intubation, a forward strategy for ventilation of the patient is the only acceptable way in most cases and the return to spontaneous breathing is not an alternative. Therefore, the value of sugammadex and also of succinylcholine is limited for these situations. Additionally, economic factors such as storage conditions for rocuronium and the cost of sugammadex must also be considered.  相似文献   

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Background: Patients receiving chronic carbamazepine therapy have shortened recovery times from a neuromuscular block induced by vecuronium. The current study investigates the pharmacokinetic or pharmacodynamic mechanisms responsible for this observation.

Methods: Pharmacokinetics and pharmacodynamics of 0.1 mg/kg intravenous bolus vecuronium in ten epileptic patients receiving chronic carbamazepine therapy were compared to that of ten control subjects. All patients were scheduled for neurosurgery while anesthetized with isoflurane and sufentanil. Arterial blood samples were collected for 6 h. Plasma vecuronium concentrations were measured by high-performance liquid chromatography coupled to electrochemical detection. The adductor pollicis force of contraction was recorded after supramaximal ulnar nerve stimulation. Plasma vecuronium concentrations were fitted to a two-compartment pharmacokinetic model, and the effect compartment equilibration rate constant was derived with a nonparametric link model. The effect compartment concentrations were fitted to a sigmoid Emax model. Results were compared using Student's t-test for independent samples.

Results: ln the carbamazepine group, the mean recovery times to T1 25% were shorter (28.1+/-3.4 vs. 47.3+/-5.1 min in control subjects; P = 0.007), and the T1 25% to T1 75% recovery index was decreased (7.6+/-1.2 vs. 21.9+/-6.8 min in control subjects; P = 0.025). No changes in onset times were observed. Clearance was 9.0+/-1.2 ml *symbol* kg sup -1 *symbol* min sup -1 versus 3.8+/-0.3 in the control group (P = 0.003), whereas no changes in volumes of distribution at steady-state were observed. Therefore, the mean residence time was halved (17.8+/-2.5 vs. 31.9+/-2.5 min in control subjects; P = 0.001). No differences in the effect compartment equilibration rate constant, vecuronium effect compartment concentration present at a 50% block (EC50), or slope of the sigmoid between the two groups were found.  相似文献   


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《Renal failure》2013,35(10):1019-1024
Background: This study investigated the effect of injection of rocuronium or sugammadex alone and rocuronium + sugammadex on urea, creatinine, electrolyte levels, and histopathological findings in rats. Methods: Thirty-six Sprague-Dawley male rats were divided to receive intravenously 16 or 96 mg/kg sugammadex, 1 mg/kg rocuronium, 1 mg/kg rocuronium + 16 mg/kg sugammadex, or 1 mg/kg rocuronium + 96 mg/kg sugammadex. The control group received an equal volume of physiological serum. Rats receiving rocuronium were ventilated until resumption of spontaneous ventilation and followed for 72 h. Blood samples were withdrawn from the tail vein to measure urea, creatinine, and electrolyte values; then both kidneys were excised, and the tissues were used for histopathological examination. Results: Rats receiving rocuronium and high doses of sugammadex (96 mg/kg) showed increased glomerular vacuolation, tubular dilatation, vascular vacuolation and hypertrophy, lymphocyte infiltration, and tubular cell sloughing compared to the control group (p = 0.002). Biochemical markers of renal function were not significantly altered after treatment with high doses of sugammadex. Conclusion: The elimination half-life of the rocuronium–sugammadex complex was found to be greater than that of free rocuronium or sugammadex, which led to marginal histopathological changes in the kidney without affecting any renal functions.  相似文献   

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