艾司洛尔预注射对预防颈丛阻滞后心血管副反应的观察

颈丛阻滞常可引起心率增快 ,血压增高 ,被认为是颈动脉窦及迷走神经被阻滞 ,交感神经活性增强所致 [1 ]。我们采用艾司洛尔预注射的方法 ,抑制颈丛阻滞后的心血管副反应 ,取得了良好的效果 ,现介绍如下。1　临床资料和方法1.1　一般资料　选择 ASA I～ 级 ,择期行甲状腺瘤或囊     

An Accurate Prediction of the pH Change Due to Degradation: Correction for a “Produced” Secondary Buffering System

Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxy-ester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a secondary buffer and minimizes the change in pH due to degradation. Equations are presented to calculate the change in the pH when the primary degradation product acts as a secondary buffer. This information can be used in the development of a parenteral product to predict, a priori, the concentration of buffer necessary for optimal pH maintenance. This knowledge can reduce the number of formulation screens required to determine the necessary buffer capacity for optimal drug stability.     

Bolus doses of esmolol for the prevention of perioperative hyper-tension and tachycardia

The effectiveness of esmolol, an ultra short-acting cardioselective beta blocker, in the prevention and treatment of post-intubation haemodynamic perturbations, was investigated. Forty-eight ASA physical status I and II patients undergoing hysterectomy were randomly assigned to receive a single intravenous bolus of placebo, esmolol 100 mg, or esmolol 200 mg in a double-blind fashion. This was administered over 15 sec, and immediately followed by thiopentone 3-5 mg.kg-1, succinylcholine 1.5 mg.kg-1, and tracheal intubation 90 sec later. The heart rate following induction of anaesthesia was lower in the esmolol 200 mg group (P less than 0.01); following intubation, the increase in heart rate in the placebo group was greater than in the esmolol groups (P less than 0.05). The systolic blood pressure post-induction was lower in the esmolol 200 mg group (P less than 0.05); following intubation, however, no significant differences were seen among groups in systolic, diastolic, or mean blood pressures. Following tracheal intubation, the incidence of ventricular arrhythmias was lower in the esmolol groups (P less than 0.05). In summary, esmolol in 100 mg and 200 mg doses was effective in mitigating the haemodynamic response following tracheal intubation.     

艾司洛尔预防气管内插管心血管反应的临床观察

研究艾司洛尔静注预防气管插管时心血管反应的效果。将９０例ＡＳＡⅠ～Ⅱ级择期全麻下手术患者随机分为３组,Ａ组（ｎ＝３０）静注艾司洛尔１ｍｇ．ｋｇ－１,Ｂ组（ｎ＝３０）静注艾司洛尔２ｍｇ．ｋｇ－１,Ｃ组（ｎ＝３０）为对照组,静注同等容量的生理盐水。观察注药前、插管前及插管后１ｍｉｎ、２ｍｉｎ、３ｍｉｎ、５ｍｉｎ、１０ｍｉｎ时,心率、收缩压和舒张压的变化。结果显示：Ａ组和Ｂ组均能较好地缓解窥喉和气管插管时心率增快和血压升高的心血管反应,效果尤以Ｂ组为佳;３组中各有１例发生心动过缓和低血压,未见哮喘和过敏。研究提示：艾司洛尔能安全有效地减轻插管时的心血管反应。     

A comparison of esmolol and labetalol for the treatment of perioperative hypertension in geriatric ambulatory surgical patients

This is an open randomized study comparing the efficacy and safety of i.v. esmolol and labetalol in the treatment of perioperative hypertension in ambulatory surgery. Twenty-two elderly patients undergoing cataract surgery under local anaesthesia were studied. The main inclusion criteria were development of systolic blood pressure greater than 200 mmHg or diastolic greater than 100 mmHg. Esmolol was given as a bolus 500 micrograms.kg-1 i.v. followed by a maintenance infusion (150-300 micrograms.kg-1.min-1). Labetalol was given as a bolus of 5 mg i.v. followed by 5 mg increments as needed up to a maximum of 1 mg.kg-1. Esmolol and labetalol both produced reductions in systolic and diastolic blood pressure (P less than 0.05) within ten minutes of administration which lasted for at least two hours. Reduction of blood pressure by esmolol was accompanied by a decrease in HR (P less than 0.05). Two patients developed extreme bradycardia (HR less than 50 beats.min-1) and esmolol had to be discontinued. Labetalol, in contrast, induced only a moderate decrease in HR. None of the patients treated with labetalol experienced any prolonged side effects such as orthostatic hypotension. In conclusion, esmolol may produce considerable bradycardia in elderly patients when hypertension is not accompanied by tachycardia. Labetalol was easier to administer in the ambulatory setting and one-tenth the cost of esmolol.     

艾司洛尔对气管插管期间脑电双频指数的影响

目的　探讨艾司洛尔对气管插管期间血流动力学和脑电双频指数(BIS)的影响。方法　30例行腹腔镜胆囊切除术的患者,随机分为2组:艾司洛尔组(试验组)和生理盐水组(对照组)。全麻诱导: 2组均靶控输注异丙酚,血浆浓度为4μg·mL-1, 维库溴铵0. 1mg·kg-1。试验组在异丙酚输注5min后,予艾司洛尔1mg·kg-1, 并以150μg·(kg·min)-1维持;对照组予生理盐水。异丙酚输注10min后,行气管插管。观察诱导前、插管前及插管后1, 3, 5min平均动脉压(MAP)、心率(HR)及BIS的变化。结果　插管后1, 3min,对照组MAP、HR显著高于诱导前,试验组与诱导前比较差异无显著性。插管后1, 3min,对照组BIS较插管前显著升高,试验组BIS与插管前比较差异无显著性。结论　气管插管时,艾司洛尔即可减轻病人的心血管反应,又可抑制插管刺激引起的大脑皮层兴奋性的增加。     

艾司洛尔治疗儿童重症手足口病疗效的系统评价和Meta分析

目的:系统评价艾司洛尔治疗儿童重症手足口病的临床疗效。方法：计算机检索中国学术期刊全文数据库、万方数据库、维普数据库、中国生物医学文献数据库、PubMed、EMBase、the Cochrance Library数据库,收集从建库至2018年12月所有艾司洛尔治疗儿童重症手足口病的随机对照试验（对照组采用常规治疗,试验组在常规治疗基础上加用艾司洛尔）。提取符合纳入标准的文献并进行质量评价,运用RevMan 5.3进行Meta分析。结果：共纳入6项研究,包括700例患儿。Meta分析结果显示,实验组治疗后血清内乳酸脱氢酶（LDH）、肌酸激酶（CK）、肌酸激酶同工酶（CK-MB）、去甲肾上腺素（NE）均低于对照组（P<0.05）。结论：对于重症手足口病患儿,在常规治疗基础上加用艾司洛尔可提高疗效。     

艾司洛尔联合右美托咪定对重型颅脑创伤患者去骨瓣 减压术后脑代谢及预后的影响

目的　探讨艾司洛尔联合右美托咪定对重型颅脑创伤去骨瓣减压术患者脑脊液（CSF）中乳酸、S100B表达,颅内压（ICP）以及预后的影响。方法　选取2015年1月—2018年12月行单侧去骨瓣减压的重型颅脑创伤患者60例为观察对象,采用随机信封法分为艾司洛尔联合右美托咪定治疗组（联合治疗组,30例）与单用右美托咪定治疗组（对照组,30例）。记录治疗前和治疗后1、3、7 d颅内压变化及CSF中乳酸和S100B蛋白水平,比较2组患者治疗后14 d格拉斯哥昏迷（GCS）评分和美国国立卫生研究院卒中量表（NIHSS）评分及不良反应发生情况。出院后共随访6个月,采用Glasgow预后分级（GOS）评价2组患者的预后。结果　联合治疗组患者治疗后1、3、7 d其CSF乳酸含量、S100B水平和ICP均低于对照组（P＜0.05）;联合治疗组治疗后14 d GCS评分及NIHSS评分高于对照组（P＜0.01）;出院后6个月随访时2组患者GOS评分差异无统计学意义（P＞0.05）。结论　艾司洛尔联合右美托咪定联合治疗可降低重型颅脑创伤去骨瓣术患者CSF乳酸水平和S100B蛋白表达,改善患者的短期预后,但并未改善长期预后。     

Protective effects of a magnesium magnetic isotope (Mg25)‐exchanging nanoparticle (25MgPMC16) on mitochondrial functional disorders in esmolol‐induced cardiac arrest in rats

1 In cardiac surgery, agents are needed to produce temporary cardiac arrest (cardioplegia). One of these agents is esmolol (ESM) which is a short‐acting selective beta‐1 adrenergic receptor antagonist and its overdose causes diastolic ventricular arrest. 2 The ²⁵MgPMC₁₆ (porphyrin adducts of cyclohexil fullerene‐C60) is known as a nanoparticle which has a cardioprotective effect when the heart is subjected to stressful conditions. 3 In this study, we aimed to confirm the deleterious effects of ESM overdose on cardiac mitochondria and identify any protective effects of ²⁵MgPMC₁₆ in male Wistar rats. Esmolol 100 mg kg^?1 (LD50 = 71 mg kg^?1) was injected intravenously (i.v.) into tail vein to induce cardiac arrest. This dose was obtained from an ESM dose–response curve which induces at least 80% arrest in rats. 4 ²⁵MgPMC₁₆ at three different doses (45, 90 and 224 mg kg^?1) was injected i.v. as pretreatment, eight hours before ESM injection. ²⁵MgCl₂ or ²⁴MgPMC₁₆ were used as controls. Following cardiac arrest, the heart was removed and the mitochondria extracted. Mitochondrial viability and the adenosine 5′‐diphosphate sodium salt hydrate/Adenosine 5′‐triphosphate disodium salt hydrate (ADP/ATP) ratio were measured as biomarkers of mitochondrial function. 5 Results indicate that ²⁵MgPMC₁₆ caused a significant increase in mitochondrial viability and decrease in ADP/ATP ratio. No significant changes were seen with ²⁴MgPMC₁₆ or ²⁵MgCl₂. It is concluded that cardiac arrest induced by ESM overdose leads to a significant decrease in mitochondrial viability and their ATP levels, whereas pretreatment by ²⁵MgPMC₁₆ can protect mitochondria by increasing ATP level through liberation of Mg into cells and the improvement of hypoxia.