Desensitization of the isolated bovine iris sphincter muscles by pilocarpine

We investigated the effect of pilocarpine on the bovine iris sphincter. This muscle contracted in a dose-dependent manner from 2 × 10^–6 M, with a maximal response at 3 × 10^–3 M. The ED₅₀ values was (1.6 ± 0.3) × 10^–4M. Pilocarpine generated a desensitization while desensitization was not significant in the case of other cholinergic agents such as acetylcholine (Ach) and carbachol. Desensitization was profoundly increased in the presence of Ach, neostigmine or eserine: the responses to the second and third trials of pilocarpine were reduced to approximately 8–10% or 30% of the corresponding first responses. Pilocarpine reportedly releases transmitters and alters choline-acetyltransferase activity.These results taken together suggest that either variable Ach synthesis, inhibitory transmitter release or possible toxic action in high concentrations may be involved in the pilocarpine-induced responses of the bovine iris sphincter muscle. The desensitization and parital agonist-antagonist action of pilocarpine could not explain the characteristics of the bovine iris sphincter muscle.     

新斯的明拮抗阿曲库铵的效果及其对Q-T离散度的影响

目的研究老年人使用不同剂量新斯的明拮抗国产阿曲库铵肌松恢复作用的效果及对Q-T离散度的影响。方法80例ASAⅠ～Ⅱ级老年患者，随机分为4组，每组20例，一组为对照组，其它三组分别给予新斯的明20、40、60μg／kg，观察其拮抗阿曲库铵肌松作用的恢复时间及对Q-T离散度的影响。结果对照组和新斯的明20μg／kg组产生的肌松恢复时间明显长于40、60μg／kg组；而40、60μg／kg组产生的效果相似。新斯的明20μg／kg对Q-T离散度影响不明显，而40、60μg／kg组Q-T离散度明显增大。结论老年人在使用新斯的明拮抗肌松作用时，剂量由20μg／kg增加到40μg／kg，可使肌松恢复加快，但增大Q-T离散度。     

Effect of neostigmine at different levels of mivacurium-induced neuromuscular blockade

The effectiveness of neostigmine 40 μg/kg for antagonism of two different levels of neuromuscular blockade, induced by a bolus dose of mivacurium 0.15 mg/kg, was studied in 45 patients. The patients were anaesthetized with thiopentone, fentanyl, nitrous oxide in oxygen, and enflurane. Neostigmine was administered at either 10% recovery of the twitch height (TH10) at the adductor pollicis muscle ( n =14) or upon reappearance of the first response at the orbicularis oculi muscle (OO1) after train-of-four (TOF) stimulation ( n = 16), the latter representing a deeper degree of neuromuscular blockade. Fifteen of the 45 patients did not receive neostigmine (control group). Neostigmine administration at OO1 rather than at TH10 at the adductor pollicis muscle caused reversal of neuromuscular blockade to occur 8 min earlier and shortened the time to reach 25% recovery of the twitch height (TH25) at the adductor pollicis muscle by about 5 min, compared with the control group. However, the time needed to reach a T4/T1 ratio ≥0.8 was similar in both the early and late neostigmine administration groups, being 9 min faster than in the control group. It can be concluded that there is no advantage in administering neostigmine at profound neuromuscular blockade to achieve clinically adequate recovery (T4/T1 ratio ≥0.8). However, the time between injection of mivacurium and TH25 may be shortened by using neostigmine at profound neuromuscular blockade, a procedure which may be useful in case of unpredictably difficult intubation, since diaphragmatic movements usually reappear at TH25.     

足三里注射新斯的明对急性重症脑梗死患者自主排便功能影响的疗效观察

目的:评估足三里注射新斯的明对急性重症脑梗死患者自主排便功能影响。方法:回顾性分析2018年9月~2019年8月我院血管外科监护室收治的急性重症脑梗死患者63例,对照组30例患者予开塞露、灌肠人工辅助排便措施,治疗组33例患者予足三里注射新斯的明,观察2组患者治疗前后患者肠鸣音,治疗后24 h内自主排便次数、便血、大便失禁、瞳孔缩小等指标,评估疗效。结果:治疗组治疗前患者肠鸣音(0.6±0.9)次/min,治疗后患者肠鸣音(4.3±3.2)次/min,差异有统计学意义(P<0.05);对照组治疗后24 h内自主排便次数(0.3±0.8)次,治疗组治疗后24 h内自主排便次数(2.6±3.0)次,差异有统计学意义(P<0.05);对照组治疗后肠鸣音增加(1.2±1.5)次,治疗组治疗后肠鸣音增加(3.7±3.1)次,差异有统计学意义(P<0.05);所有患者无瞳孔缩小表现。结论:足三里注射新斯的明可促进急性重症脑梗死患者胃肠道蠕动,恢复自主排便功能,且不影响病情观察。     

新斯的明复合美托洛尔在不停跳冠状动脉搭桥术中控制心率的应用研究

目的探讨新斯的明复合美托洛尔在非体外循环冠状动脉旁路移植术中控制心率的疗效及安全性。方法 14例冠心病患者,ASAⅡ~Ⅲ级,采用气管插管静吸复合全麻,术中行有创动脉血压、心电图、脉搏氧饱和度、呼气末二氧化碳分压、心排血量、体循环阻力、肺动脉压力、肺毛细血管楔压、尿量、肛温监测。手术方式均为非体外循环下行冠状动脉旁路移植术。术中心率〉90次/min时,在确保一定的麻醉深度及容量负荷的前提下静注美托洛尔6~10mg后效果不佳者,给予少量新斯的明（0.2~0.4mg）。结果 10例患者使用新斯的明0.2mg后心率减少慢8~15次/min,其余4例患者静注新斯的明0.2mg后减慢心率作用不明显,加用0.1~0.2mg后心率减慢13~28次/min。本组患者术后恢复顺利,10例术后4~7h拔除气管导管,4例术后7~24h拔除气管导管。结论在不停跳冠状动脉搭桥术过程中,心率较快且难控制时,在保证一定麻醉深度及容量负荷的前提下,使用较大剂量美托洛尔效果欠佳时,复合使用小剂量新斯的明控制心率是安全有效的。     

新斯的明足三里注射联合清胰汤治疗重症胰腺炎并发胃肠麻痹疗效观察

目的观察新斯的明足三里注射联合清胰汤治疗重症胰腺炎并发胃肠麻痹的疗效。方法将82例重症胰腺炎并发胃肠麻痹患者随机分为A、B、C、D 4组,均给予常规治疗。在此基础上B组予清胰汤鼻饲,C组予新斯的明足三里穴位注射,D组予清胰汤鼻饲及新斯的明足三里穴位注射。观察4组治疗后血淀粉酶、血钙及腹部胃肠道症状体征改善情况,评价疗效。结果 B、C、D组胃肠功能恢复情况均优于A组,且时间快。B组、C组之间比较无显著性差异。D组较B组、C组胃肠功能恢复快,疗效更好。结论新斯的明足三里穴位注射联合清胰汤治疗重症胰腺炎更能有效缓解胃肠道麻痹,促进肠功能恢复,缩短治疗时间。     

Combined administration of anisodamine and neostigmine produces anti-shock effects: involvement of α7 nicotinic acetylcholine receptors

Aim:

To evaluate the anti-effects of anisodamine and neostigmine in animal models of endotoxic and hemorrhagic shock.

Methods:

Kunming mice were injected with lipopolysaccharide (LPS 30 mg/kg, ip) to induce endotoxic shock. Anisodamine (12.5, 25, and 50 mg/kg, ip) and neostigmine (12.5, 25, and 50 μg/kg, ip) were administered immediately after LPS injection. Survival rate was monitored, and the serum levels of TNF-α and IL-1β were analyzed using ELISA assays. The effects of anisodamine and neostigmine were also examined in α7 nicotinic acetylcholine receptor (α7 nAChR) knockout mice with endotoxic shock and in Beagle dogs with hemorrhagic shock.

Results:

In mice with experimental endotoxemia, combined administration of anisodamine and neostigmine significantly increased the survival rate and decreased the serum levels of inflammatory cytokines, as compared to those produced by either drug alone. The anti-shock effect of combined anisodamine and neostigmine was abolished in α7 nAChR knockout mice. On the other hand, intravenous injection of the combined anisodamine and neostigmine, or the selective α7 nAChR agonist PNU282987 exerted similar anti-shock effects in dogs with hemorrhagic shock.

Conclusion:

The results demonstrate that combined administration of anisodamine and neostigmine produces significant anti-shock effects, which involves activation of α7 nAChRs.     

肠鸣音与胃肠运动相关性的初步观察

目的 观察肠鸣音与胃肠运动的相关性. 方法 2组健康成人志愿者,每组6例,分别注射甲硫酸新斯的明和山莨菪碱注射液. 结果 注射新斯的明后肠鸣音有逐步增多的趋势,第3、5、6、7、8时段的肠鸣音脉冲次数与注射前相比,差异有显著性(P＜0.05或0.01);注射山莨菪碱后肠鸣音明显减少,第2、3、4、5、6、7、8时段的肠鸣音脉冲次数与注射前相比,差异有显著性(P＜0.05或0.01). 结论 肌肉注射促进胃肠运动药物可随着药效作用时间而同步出现肠鸣音增多,而抑制胃肠运动药物则出现肠鸣音同步减少,从药效学的角度证明了肠鸣音与胃肠运动具有相关性.     

Intraarticular neostigmine for postoperative analgesia

The aim of this randomised double-blind study was to assess the analgesic efficacy of intraarticular neostigmine applied postoperatively following arthroscopic procedures of the knee joint. Patients, aged 19 to 70 years, were randomised into two groups. Group I received 500 μg of neostigmine + 10 ml NaCl intraarticularly at the end of surgery, prior to the arthroscope being removed. Group II received 10 ml of physiologic saline intraarticularly. Pain scores were assessed postoperatively using the visual analogue scale (0=no pain, 10=unbearable pain at rest or with activity). In addition, side effects and sedation scores were recorded. Vital signs and the above scores were recorded before the first analgesic request and at 1, 2, 3, 6, 9, 12, 18 and 24 hours postoperatively. For rescue medication patients received a loading dose of morphine hydrochloride postoperatively, followed by patient controlled analgesia.Fifteen patients per group were included for statistical evaluation in this study. The two groups demonstrated no significant difference with respect to demographic parameters, postoperative pain scores at rest or during activity, and with respect to postoperative analgesic consumption.In this study no significant analgesic effect was observed following intraarticular application of neostigmine 500 μg.     

Neuromuscular block and current treatment strategies for its reversal in children

Even though neuromuscular blocking agents are an essential part of balanced anesthesia and the risks of residual paralysis are well documented, many anesthetists seldomly monitor neuromuscular block. Classical reversal agent neostigmine is unable to antagonise a deep neuromuscular block and is rather slow to antagonise even a moderate block. These caveats may have introduced a practice to use muscle relaxants mainly for an endotracheal intubation. This review presents current views on the effects of muscle relaxants and their reversal agents in pediatric patients. This may help clinicians to reconsider the value of muscle relaxants during anesthesia in children.