Androstanols

雄甾烷醇
  • 文章类型: Case Reports
    一个10岁的孩子,绝育的男性,金毛犬被推荐用于手术矫正后代囊肿。肌内注射乙酰丙嗪(0.02mg/kg)和美沙酮(0.5mg/kg)用于镇静,丙泊酚(2mg/kg)和咪达唑仑(0.2mg/kg)静脉内用于麻醉诱导,异氟烷在氧气中用于麻醉维持。罗库溴铵(0.5mg/kg),神经肌肉阻断剂,静脉内给药,以促进手术时眼睛的中央定位。罗库溴铵给药10分钟内,狗变得心动过速和低血压。最初的干预措施并未解决血流动力学异常,但静脉注射苯海拉明(0.8mg/kg)可成功缓解血流动力学异常。狗在整个剩余过程中保持稳定,并经历了平稳和平稳的恢复。虽然很难确认在该临床病例中观察到的血液动力学变化仅由罗库溴铵的给药引起,对心血管变化的观察,事件发生时间和对治疗的反应提示罗库溴铵引起的组胺反应,苯海拉明治疗成功.
    A 10-year-old, neutered male, Golden Retriever dog presented for surgical correction of a descemetocele. Acepromazine (0.02 mg/kg) and methadone (0.5 mg/kg) were administered intramuscularly for sedation, propofol (2 mg/kg) and midazolam (0.2 mg/kg) were administered intravenously for anaesthetic induction and isoflurane in oxygen was utilised for anaesthetic maintenance. Rocuronium (0.5 mg/kg), a neuromuscular blocking agent, was administered intravenously to facilitate central positioning of the eye for surgery. Within 10 min of rocuronium administration, the dog became tachycardic and hypotensive. Hemodynamic aberrations did not resolve with initial interventions but were successfully mitigated with the administration of diphenhydramine (0.8 mg/kg) intravenously. The dog remained stable throughout the remainder of the procedure and experienced a smooth and uneventful recovery. While it is difficult to confirm that the hemodynamic changes observed in this clinical case resulted solely from administration of rocuronium, the observance of the cardiovascular changes, timing of events and response to therapy suggest that rocuronium elicited a histamine response that was successfully treated with diphenhydramine.
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  • 文章类型: Journal Article
    用瑞马唑仑和芬太尼系列阿片类药物诱导的麻醉可以用氟马西尼和纳洛酮逆转。罗库溴铵的伴随性麻痹可以促进气管插管,而sugammadex则是可逆的。一起,这种组合可能提供“常规”或“快速序列”诱导麻醉的完全可逆性。这是否有用,甚至是安全的,需要仔细评估。
    Anaesthesia induced with remimazolam and a fentanyl-series opioid can be reversed with flumazenil and naloxone. Concomitant paralysis with rocuronium can facilitate tracheal intubation whilst being reversible with sugammadex. Together, this combination might offer full reversibility of a \'routine\' or a \'rapid-sequence\' induction anaesthesia. Whether this is useful, or even safe, requires careful evaluation.
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  • 文章类型: Journal Article
    背景:神经肌肉阻断剂的作用可以通过给予新斯的明逆转,当使用四组(TOF)刺激存在两个抽搐时。然而,在老年患者中,关于何时使用新斯的明的可用数据有限.我们假设TOF(TOF-2)后两次抽搐的时间在0.6mg/kg罗库溴铵后比0.9mg/kg罗库溴铵后短。此外,我们假设达到TOF-2的时间在罗库溴铵0.3mg/kg后比在罗库溴铵0.6mg/kg后短.
    方法:这是对50例>80岁的老年患者进行的二次分析;16例患者接受了0.6mg/kg的罗库溴铵,另有16名患者接受了0.9毫克/千克的罗库溴铵;最后,18例患者接受了0.3mg/kg的罗库溴铵。患者接受全静脉麻醉,用加速肌电图监测神经肌肉阻滞。
    结果:罗库溴铵0.6mg/kg后达到TOF-2的时间短于罗库溴铵0.9mg/kg后:37分钟。对59分钟。(差异:22分钟。(95%置信区间(CI):10至33分钟。),p=0.0007)。罗库溴铵0.3mg/kg后的TOF-2时间短于罗库溴铵0.6mg/kg后的时间:19分钟。与37分钟。(差异:18分钟。(95%CI:11至25分钟。),p=0.00006)。然而,接受0.3mg/kg的患者中只有33%获得了完全的效果,即TOF-0。
    结论:达到TOF-2的时间在罗库溴铵0.6mg/kg后比0.9mg/kg后短,在罗库溴铵0.3mg/kg后比0.6mg/kg后短。
    背景:这项工作得到了部门来源的支持。
    背景:这项研究是对两项临床试验的二次分析。
    结果:gov(NCT04512313),(NCT03857750)。
    BACKGROUND: The effect of neuromuscular blocking agents may be reversed by administration of neostigmine, when two twitches are present using train-of-four (TOF) stimulation. However, in elderly patients, limited data are available about when to administer neostigmine. We hypothesised that time to two twitches after TOF (TOF-2) was shorter after rocuronium 0.6 mg/kg than after rocuronium 0.9 mg/kg. Also, we hypothesised that time to TOF-2 would be shorter after rocuronium 0.3 mg/kg than after rocuronium 0.6 mg/kg.
    METHODS: This was a secondary analysis of 50 elderly patients > 80 years; 16 patients received rocuronium 0.6 mg/kg, another 16 patients received rocuronium 0.9 mg/kg; and, finally, 18 patients received rocuronium 0.3 mg/kg. Patients received total intravenous anaesthesia, and neuromuscular block was monitored with acceleromyography.
    RESULTS: Time to TOF-2 was shorter after rocuronium 0.6 mg/kg than after rocuronium 0.9 mg/kg: 37 min. versus 59 min. (difference: 22 min. (95% confidence intervals (CI): 10 to 33 min.), p = 0.0007). Time to TOF-2 after rocuronium 0.3 mg/kg was shorter than after rocuronium 0.6 mg/kg: 19 min. versus 37 min. (difference: 18 min. (95% CI: 11 to 25 min.), p = 0.00006). However, only 33% of the patients receiving 0.3 mg/kg obtained full effect i.e. TOF-0.
    CONCLUSIONS: Time to TOF-2 was shorter after rocuronium 0.6 mg/kg than after 0.9 mg/kg and shorter after rocuronium 0.3 mg/kg than after 0.6 mg/kg.
    BACKGROUND: This work was supported by departmental sources.
    BACKGROUND: This study was a secondary analysis of two clinical trials.
    RESULTS: gov (NCT04512313), (NCT03857750).
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  • 文章类型: Journal Article
    背景:很少有研究通过直接测量浓度来比较高剂量和低剂量罗库溴铵在剖宫产中的作用。因此,我们进行了一项研究,以检查两种剂量的罗库溴铵对母亲和胎儿的血液浓度和临床影响。方法:18例患者随机分为两组:C组(0.6mg/kg),H集团,(1.0mg/kg)。主要结果是比较两组之间的脐静脉罗库溴铵浓度。我们评估了插管的难易程度,从罗库溴铵给药到一些TOF点的时间,麻醉后护理单元(PACU)停留时间,注入瑞芬太尼剂量,母体罗库溴铵浓度,和阿普加得分。结果:在人口统计学数据中没有观察到差异,易于插管,PACU停留时间,1分钟阿普加得分,两组之间的脐静脉血气分析。然而,H组罗库溴铵给药到T3消失的时间短于C组(p=0.009),T1和T2重现时间长于C组(p=0.003,p=0.009).H组的瑞芬太尼给药剂量(p=0.042)低于C组。在脐带夹闭前(p=0.002)和出院时(p<0.001)的脐静脉(p=0.004)和母体静脉中的罗库溴铵浓度在H组中也高于C组。结论:我们观察到PACU停留时间没有延长,H组Apgar评分与C组相比无差异。提示1.0mg/kg罗库溴铵在剖宫产术中对胎儿和母亲无不良影响。
    Background: There have been few studies comparing the effects of high- and low-dose rocuronium during cesarean section by directly measuring the concentration. Therefore, we conducted a study to examine the blood concentrations and clinical effects of both doses of rocuronium on mothers and fetuses. Methods: Eighteen patients were randomly assigned to two groups: C Group (0.6 mg/kg), and H Group, (1.0 mg/kg). The primary outcome was the comparison of umbilical vein rocuronium concentration between two groups. We assessed ease of intubation, time from rocuronium administration to some TOF points, post-anesthesia care unit (PACU) stay time, infused remifentanil dose, maternal rocuronium concentration, and Apgar scores. Results: No differences were observed in demographic data, ease of intubation, PACU stay time, 1 min Apgar scores, umbilical venous blood gas analysis between both groups. However, the time from rocuronium administration to T3 disappearance was shorter (p=0.009) and time to T1 and T2 reappearance were longer (p=0.003, p=0.009) in H group than that in C group. The administered remifentanil dose (p=0.042) was lower in the H group than in the C group. Rocuronium concentrations in the umbilical vein (p=0.004) and maternal vein before cord clamping (p=0.002) and at discharge (p<0.001) were also found to be higher in the H group than in the C group. Conclusions: We observed no prolongation of PACU stay, and no differences in Apgar scores in H group compared to C group. It suggests that 1.0 mg/kg of rocuronium has no negative effects on the fetus and mother in cesarean section.
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  • 文章类型: Journal Article
    目的:在我们的研究中,我们的目的是比较标准的快速顺序插管方案和应用罗库溴铵引发技术对手术时间和血流动力学的影响。
    方法:应用于急诊科并需要快速顺序插管的患者被纳入我们的研究,我们进行了随机对照设计。研究中的随机化是根据病例的到达顺序进行的。标准组进行快速顺序插管。在启动组中,在诱导剂之前约3分钟施用10%的罗库溴铵剂量。插管时间,使用的药物数量,生命体征,记录用于确认插管的插管前后的呼气末CO2水平。
    结果:本研究共纳入52例患者,其中26例患者被纳入标准组,26例患者被纳入启动组。标准组插管时间为121.2±21.9s,启动组计算为68.4±11.6s(p<0.001)。标准组插管后平均动脉压为58.3±26.6mmHg,启动组为80.6±21.1mmHg(p=0.002)。
    结论:观察到罗库溴铵的灌注缩短了插管时间,并更好地保持了血流动力学曲线。
    背景:NCT05343702。
    OBJECTIVE: In our study, we aimed to compare the effect of standard rapid sequence intubation protocol and the application of rocuronium priming technique on the procedure time and hemodynamic profile.
    METHODS: Patients who applied to the emergency department and needed rapid sequence intubation were included in our study, which we conducted with a randomized controlled design. Randomization in the study was made according to the order of arrival of the cases. Rapid sequence intubation was performed in the standard group. In the priming group, 10% of the rocuronium dose was administered approximately 3 min before the induction agent. Intubation time, amount of drug used, vital signs, and end-tidal CO2 level before and after intubation used to confirm intubation were recorded.
    RESULTS: A total of 52 patients were included in the study, of which 26 patients were included in the standard group and 26 patients in the priming group. While intubation time was 121.2±21.9 s in the standard group, it was calculated as 68.4±11.6 s in the priming group (p<0.001). While the mean arterial pressure was 58.3±26.6 mmHg in the standard group after intubation, it was 80.6±21.1 mmHg in the priming group (p=0.002).
    CONCLUSIONS: It was observed that priming with rocuronium shortened the intubation time and preserved the hemodynamic profile better.
    BACKGROUND: NCT05343702.
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  • 文章类型: Journal Article
    Sugammadex,作为Bridion™销售,是一种经批准的基于环糊精(CD)的药物,用于逆转接受手术的成年人的神经肌肉阻滞。Sugammadex与神经肌肉阻断剂(NMBA)罗库溴铵形成包合物,允许肌肉麻痹的快速逆转。已经开发了用于研究CD包合物的计算机方法,旨在准确预测它们的结构,精力充沛,动态,和动力学性质,以及绑定常数。这里,一项旨在从对接计算的角度表征sugammadex-ro库溴铵系统的计算研究,自由分子动力学(MD)模拟,并给出了具有平均力(PMF)计算潜力的偏置元动力学模拟。目的是提供有关该系统的详细信息,以及将其用作验证方法的模型系统。该方法预测结果与最佳结构和结合常数定量值的实验证据一致。有趣的是,与基于静电相互作用的假设相比,对取向的偏好程度较低,这表明这两个方向都可能存在于解决方案中。这些结果表明,该技术可以有效地分析CD包合物,并可用于促进CD新型应用的开发和优化。
    Sugammadex, marketed as Bridion™, is an approved cyclodextrin (CD) based drug for the reversal of neuromuscular blockade in adults undergoing surgery. Sugammadex forms an inclusion complex with the neuromuscular blocking agent (NMBA) rocuronium, allowing rapid reversal of muscle paralysis. In silico methods have been developed for studying CD inclusion complexes, aimed at accurately predicting their structural, energetic, dynamic, and kinetic properties, as well as binding constants. Here, a computational study aimed at characterizing the sugammadex-rocuronium system from the perspective of docking calculations, free molecular dynamics (MD) simulations, and biased metadynamics simulations with potential of mean force (PMF) calculations is presented. The aim is to provide detailed information about this system, as well as to use it as a model system for validation of the methods. This method predicts results in line with experimental evidence for both the optimal structure and the quantitative value for the binding constant. Interestingly, there is a less profound preference for the orientation than might be assumed based on electrostatic interactions, suggesting that both orientations may exist in solution. These results show that this technology can efficiently analyze CD inclusion complexes and could be used to facilitate the development and optimization of novel applications for CDs.
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  • 文章类型: Journal Article
    通过等温滴定量热法和1HNMR光谱法在磷酸盐缓冲盐水中测量柱[6]MaxQ对一组神经肌肉阻断剂和神经递质的结合亲和力。体内功效研究表明,P6MQ螯合了罗库溴铵和维库溴铵,并逆转了它们对四组(TOF)比率恢复的影响。
    The binding affinity of pillar[6]MaxQ toward a panel of neuromuscular blockers and neurotransmitters was measured in phosphate buffered saline by isothermal titration calorimetry and 1H NMR spectroscopy. In vivo efficacy studies showed that P6MQ sequesters rocuronium and vecuronium and reverses their influence on the recovery of the train-of-four (TOF) ratio.
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  • 文章类型: Randomized Controlled Trial
    高体脂百分比患者的药效学可能与肥胖患者相似。这项随机对照临床试验观察了罗库溴铵对不同体脂百分比(PBFs)患者的影响。本研究纳入了在上海市总医院进行全身麻醉下择期泌尿外科或盆腔手术的54例患者;纳入了51例患者进行数据分析。PBF正常(<25%)的患者根据总体重(N-TBW,对照组)。PBF较高(≥25%)的患者根据总体重(H-TBW)计算单剂量的罗库溴铵。PBF和罗库溴铵较高的患者根据无脂质量(H-FFM)给药。一组四个(TOF)-观察加速度描记器用于测量罗库溴铵的作用。H-TBW(91.9±28.8s)的起效时间明显短于N-TBW和H-FFM(p=0.003)。H-TBW的临床持续时间和药理持续时间明显长于其他组(p=0.000和0.000);三组的TOF比值0.25-0.9时间差异有统计学意义(p=0.005)。三组间恢复时间(p=0.103)和恢复指数(p=0.159)差异无统计学意义。基于FFM的罗库溴铵对高PBF患者的影响与正常患者相似。基于TBW计算的单剂量罗库溴铵可能会缩短起效时间,延长临床和药理持续时间,并延长恢复时间。
    The pharmacodynamics in patients with high body fat percentage might be similar to those in obese patients. This randomised controlled clinical trial observed the effects of rocuronium in patients with different percent body fats (PBFs). Fifty-four patients who underwent elective urological or pelvic surgery under general anaesthesia at Shanghai General Hospital were included in the present study; 51 patients were included for data analysis. Patients with normal PBF (<25%) were given a single dose of rocuronium calculated based on total body weight (N-TBW, control group). Patients with a higher PBF (≥25%) were given a single dose of rocuronium calculated based on total body weight (H-TBW). Patients with higher PBF and rocuronium were dosed based on fat-free mass (H-FFM). A train of four (TOF)-Watch acceleromyography monitor was used to measure the effects of the rocuronium. H-TBW (91.9 ± 28.8 s) had significantly shorter onset time than N-TBW and H-FFM (p = 0.003). H-TBW had significantly longer clinical duration time and pharmacological duration time than the other groups (p = 0.000 and 0.000, respectively); the TOF ratio0.25-0.9 time was significantly different among the three groups (p = 0.005). There were no significant differences in the recovery time (p = 0.103) or recovery index (p = 0.159) among the three groups. The effects of rocuronium dosed based on FFM in patients with high PBFs are similar to those in normal patients. A single dose of rocuronium calculated based on TBW might shorten the onset time, prolong the clinical and pharmacological duration times, and prolong the recovery time.
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  • 文章类型: Clinical Trial, Phase III
    暂无摘要。
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  • 文章类型: Letter
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