Esmolol
目录号 : GC25385Esmolol is a cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
Cas No.:81147-92-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Esmolol is a cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
Esmolol acts as a pharmacochaperone: Long term exposure of cells to esmolol raised the surface levels of β1-adrenergic receptors[1].
[1] Nasrollahi-Shirazi S, et al. J Pharmacol Exp Ther. 2016, 359(1):73-81.
| Cas No. | 81147-92-4 | SDF | Download SDF |
| 分子式 | C16H25NO4 | 分子量 | 295.37 |
| 溶解度 | DMSO: 59 mg/mL (199.75 mM);Water: 59 mg/mL (199.75 mM);Ethanol: 59 mg/mL (199.75 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3856 mL | 16.9279 mL | 33.8558 mL |
| 5 mM | 0.6771 mL | 3.3856 mL | 6.7712 mL |
| 10 mM | 0.3386 mL | 1.6928 mL | 3.3856 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Esmolol to Treat the Hemodynamic Effects of Septic Shock: A Randomized Controlled Trial
Shock 2022 Apr 1;57(4):508-517.PMID:35066509DOI:10.1097/SHK.0000000000001905.
Introduction: Septic shock is often characterized by tachycardia and a hyperdynamic hemodynamic profile. Use of the beta antagonist Esmolol has been proposed as a therapy to lower heart rate, thereby improving diastolic filling time and improving cardiac output, resulting in a reduction in vasopressor support. Methods: We conducted a two-center, open-label, randomized, Phase II trial comparing Esmolol to placebo in septic shock patients with tachycardia. The primary endpoint was improvement in hemodynamics as measured by the difference in norepinephrine equivalent dose (NED) between groups at 6 hours after initiation of study drug. Secondary outcomes included assessing differences in inflammatory biomarkers and oxygen consumption (VO2). Results: A total of 1,122 patients were assessed for eligibility and met inclusion criteria; 42 underwent randomization, and 40 received study interventions (18 in the Esmolol arm and 22 in the usual care arm). The mean NED at 6 h was 0.30 ± 0.17 mcg/kg/min in the Esmolol arm compared to 0.21 ± 0.19 in the standard care arm (P = 0.15). There was no difference in number of shock free days between the Esmolol (2, IQR 0, 5) and control groups (2.5, IQR 0, 6) (P = 0.32). There were lower levels of C-reactive protein at 12 and 24 h in the Esmolol arm, as well as a statistically significant difference in trend over time between groups. There were no differences in terms of IL-4, IL-6, IL-10, and TNFα. Among a subset who underwent VO2 monitoring, there was decreased oxygen consumption in the Esmolol patients; the mean difference between groups at 24 h was -2.07 mL/kg/min (95% CI -3.82, -0.31) (P = 0.02), with a significant difference for the trend over time (P < 0.01). Conclusion: Among patients with septic shock, infusion of Esmolol did not improve vasopressor requirements or time to shock reversal. Esmolol was associated with decreased levels of C-reactive protein over 24 h. Trial registration: www.clinicaltrials.gov. Registered February 24, 2015, https://clinicaltrials.gov/ct2/show/NCT02369900.
Effect of heart rate control with Esmolol on hemodynamic and clinical outcomes in patients with septic shock: a randomized clinical trial
JAMA 2013 Oct 23;310(16):1683-91.PMID:24108526DOI:10.1001/jama.2013.278477.
Importance: β-Blocker therapy may control heart rate and attenuate the deleterious effects of β-adrenergic receptor stimulation in septic shock. However, β-Blockers are not traditionally used for this condition and may worsen cardiovascular decompensation related through negative inotropic and hypotensive effects. Objective: To investigate the effect of the short-acting β-blocker Esmolol in patients with severe septic shock. Design, setting, and patients: Open-label, randomized phase 2 study, conducted in a university hospital intensive care unit (ICU) between November 2010 and July 2012, involving patients in septic shock with a heart rate of 95/min or higher requiring high-dose norepinephrine to maintain a mean arterial pressure of 65 mm Hg or higher. Interventions: We randomly assigned 77 patients to receive a continuous infusion of Esmolol titrated to maintain heart rate between 80/min and 94/min for their ICU stay and 77 patients to standard treatment. Main outcomes and measures: Our primary outcome was a reduction in heart rate below the predefined threshold of 95/min and to maintain heart rate between 80/min and 94/min by Esmolol treatment over a 96-hour period. Secondary outcomes included hemodynamic and organ function measures; norepinephrine dosages at 24, 48, 72, and 96 hours; and adverse events and mortality occurring within 28 days after randomization. Results: Targeted heart rates were achieved in all patients in the Esmolol group compared with those in the control group. The median AUC for heart rate during the first 96 hours was -28/min (IQR, -37 to -21) for the Esmolol group vs -6/min (95% CI, -14 to 0) for the control group with a mean reduction of 18/min (P < .001). For stroke volume index, the median AUC for Esmolol was 4 mL/m2 (IQR, -1 to 10) vs 1 mL/m2 for the control group (IQR, -3 to 5; P = .02), whereas the left ventricular stroke work index for Esmolol was 3 mL/m2 (IQR, 0 to 8) vs 1 mL/m2 for the control group (IQR, -2 to 5; P = .03). For arterial lactatemia, median AUC for Esmolol was -0.1 mmol/L (IQR, -0.6 to 0.2) vs 0.1 mmol/L for the control group (IQR, -0.3 for 0.6; P = .007); for norepinephrine, -0.11 μg/kg/min (IQR, -0.46 to 0.02) for the Esmolol group vs -0.01 μg/kg/min (IQR, -0.2 to 0.44) for the control group (P = .003). Fluid requirements were reduced in the Esmolol group: median AUC was 3975 mL/24 h (IQR, 3663 to 4200) vs 4425 mL/24 h(IQR, 4038 to 4775) for the control group (P < .001). We found no clinically relevant differences between groups in other cardiopulmonary variables nor in rescue therapy requirements. Twenty-eight day mortality was 49.4% in the Esmolol group vs 80.5% in the control group (adjusted hazard ratio, 0.39; 95% CI, 0.26 to 0.59; P < .001). Conclusions and relevance: For patients in septic shock, open-label use of Esmolol vs standard care was associated with reductions in heart rates to achieve target levels, without increased adverse events. The observed improvement in mortality and other secondary clinical outcomes warrants further investigation. Trial registration: clinicaltrials.gov Identifier: NCT01231698.
Esmolol, Antinociception, and Its Potential Opioid-Sparing Role in Routine Anesthesia Care
Reg Anesth Pain Med 2018 Nov;43(8):815-818.PMID:30216240DOI:10.1097/AAP.0000000000000873.
β-Adrenergic blockade is an important mechanism for reducing morbidity and mortality in patients with hypertension and heart failure. Esmolol has been used widely for its chronotropic and antihypertensive effects. However, there has been recent inquiry regarding perioperative Esmolol use and nociceptive modulation. Conventional postoperative analgesic treatment has relied primarily on opioids, which present their own adverse effects and pharmacoepidemiologic repercussions. Esmolol, to date, has not shown any direct analgesic or anesthetic properties; however, recent studies suggest that Esmolol may have antinociceptive and postoperative opioid-sparing effects. In this Daring Discourse narrative, we describe the role of Esmolol in current perioperative β-blockade guidelines (related to noncardiac surgery), briefly describe studies supporting the antinociceptive effects of Esmolol, propose mechanisms for Esmolol antinociception, and forecast potential routine Esmolol use intraoperatively (as part of a multimodal total intravenous anesthetic) and its effects on opioid sparing. The reading audience of regional anesthesiologists and acute pain medicine physicians is uniquely positioned to take a lead role in promulgating this care advance amid (i) the unwanted effects of the opioid epidemic and (ii) the uncertain notion of whether routine general anesthesia care (with fentanyl) may indirectly be contributing to the epidemic.
BET 1: Esmolol-a novel adjunct to the ACLS algorithm?
Emerg Med J 2020 Oct;37(10):650-651.PMID:32978249DOI:10.1136/emermed-2020-210613.02.
A short-cut review of the available medical literature was carried out to establish whether Esmolol was an effective treatment for patients in cardiac arrest. After abstract review, two papers were found to answer this clinical question using the detailed search strategy. The author, date and country of publication, patient group studied, study type, relevant outcomes, results and study weaknesses of these papers are tabulated. It is concluded that there is insufficient research addressing this question to know whether Esmolol is a potential treatment for cardiac arrest.
Esmolol and beta-adrenergic blockade
AANA J 1991 Dec;59(6):541-8.PMID:1686346doi
Tachycardia often presents difficult management problems in anesthesia. Because it increases myocardial oxygen demand so sharply, tachycardia can quickly place patients at risk of myocardial ischemia. It can occur for any number of reasons. Deepening the anesthetic, either with inhalation agent or opioids, will ablate increases in heart rate, but changes in heart rate are often transient and changes in anesthetic depth are often not. Esmolol (Brevibloc) is a unique, short-acting beta blocker that is strongly beta 1 selective at usual clinical doses. As with other beta blockers, Esmolol becomes less selective for the beta 1 receptor as its dose is increased. It is metabolized by red blood cell esterases resulting in a half-life of 9 minutes. Fifteen minutes after a bolus dose, Esmolol is difficult to detect in the plasma. Its metabolites have clinically undetectable activity and are eliminated renally. Esmolol may be administered by intermittent, intravenous bolus doses or by continuous infusion. Infusions should be preceded by loading doses. Dose range varies with the patient's status, clinical situation, concomitant medications, and desired result. Patients receiving Esmolol should be monitored because of its bradycardic and hypotensive effects.