Landiolol hydrochloride
(Synonyms: 盐酸兰地洛尔; ONO1101 hydrochloride) 目录号 : GC36422
Landiolol hydrochloride (ONO-1101) is the hydrochloride salt form of Landiolol, which is an ultra-short-acting β1 selective adrenoceptor antagonist.
Cas No.:144481-98-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Landiolol hydrochloride (ONO-1101) is the hydrochloride salt form of Landiolol, which is an ultra-short-acting β1 selective adrenoceptor antagonist.
[1] Masaki Okajima, et al. World J Crit Care Med. 2015, 4(3): 251–257.
| Cas No. | 144481-98-1 | SDF | |
| 别名 | 盐酸兰地洛尔; ONO1101 hydrochloride | ||
| Canonical SMILES | O=C(OC[C@H]1OC(C)(C)OC1)CCC2=CC=C(OC[C@@H](O)CNCCNC(N3CCOCC3)=O)C=C2.[H]Cl | ||
| 分子式 | C25H40ClN3O8 | 分子量 | 546.05 |
| 溶解度 | DMSO: 250 mg/mL (457.83 mM) | 储存条件 | Store at 2-8°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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8313 mL | 9.1567 mL | 18.3133 mL |
| 5 mM | 0.3663 mL | 1.8313 mL | 3.6627 mL |
| 10 mM | 0.1831 mL | 0.9157 mL | 1.8313 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。
Evaluating the Therapeutic Efficacy and Safety of Landiolol hydrochloride for Management of Arrhythmia in Critical Settings: Review of the Literature
Vasc Health Risk Manag 2020 Apr 3;16:111-123.PMID:32308404DOI:10.2147/VHRM.S210561.
Background: Landiolol hydrochloride, a highly cardio-selective beta-1 blocker with an ultra-short-acting half-life of 4 minutes, was originally approved by Japan for treatment of intraoperative tachyarrhythmias. This review aims to provide an integrated overview of the current state of knowledge of Landiolol hydrochloride in the management of arrhythmia in critical settings. Methods: We searched MEDLINE, EMBASE, and the Cochrane Library to retrieve relevant articles with a total of 65 records identified. Results: The high β1 selectivity (β1/β2 ratio of 255:1) of landiolol causes a more rapid heart rate (HR) decrease compared to esmolol while avoiding decreases in mean arterial blood pressure. Recently, it has been found useful in left ventricular dysfunction patients and fatal arrhythmia requiring emergency treatment. Recent random clinical trials (RCT) have revealed therapeutic and prophylactic effects on arrhythmia, and very low-dose landiolol might be effective for preventing postoperative atrial fibrillation (POAF) and sinus tachycardia. Likewise, landiolol is an optimal choice for perioperative tachycardia treatment during cardiac surgery. The high β1 selectivity of landiolol is useful in heart failure patients as a first-line therapy for tachycardia and arrhythmia as it avoids the typical depression of cardiac function seen in other β-blockers. Application in cardiac injury after percutaneous coronary intervention (PCI), protection for vital organs (lung, kidney, etc.) during sepsis, and stabilizing hemodynamics in pediatric patients are becoming the new frontier of landiolol use. Conclusion: Landiolol is useful as a first-line therapy for the prevention of POAF after cardiac/non-cardiac surgery, fatal arrhythmias in heart failure patients and during PCI. Moreover, the potential therapeutic effect of landiolol for sepsis in pediatric patients is currently being explored. As positive RCT results continue to be published, new clinical uses and further clinical studies in various settings by cardiologists, intensivists and pediatric cardiologists are being conducted.
Efficacy and safety of landiolol, an ultra-short-acting β1-selective antagonist, for treatment of sepsis-related tachyarrhythmia (J-Land 3S): a multicentre, open-label, randomised controlled trial
Lancet Respir Med 2020 Sep;8(9):863-872.PMID:32243865DOI:10.1016/S2213-2600(20)30037-0.
Background: Tachycardia and atrial fibrillation frequently occur in patients being treated for sepsis or septic shock and have a poor prognosis. Treatments for tachyarrhythmias are often ineffective or contraindicated in this setting. We aimed to investigate the efficacy and safety of landiolol, an ultra-short-acting β-blocker, for treating sepsis-related tachyarrhythmias. Methods: We did a multicentre, open-label, randomised controlled trial at 54 hospitals in Japan. Patients admitted to the intensive care units who received conventional treatment for sepsis, according to clinical guidelines for the management of sepsis, and who subsequently developed a tachyarrhythmia, were enrolled. The main inclusion criteria were 20 years of age or older, diagnosis of sepsis according to Third International Consensus Definitions for Sepsis and Septic Shock criteria, administration of catecholamine necessary to maintain mean arterial pressure at 65 mm Hg or more for at least 1 h, and heart rate of 100 beats per min (bpm) or more maintained for at least 10 min without a change in catecholamine dose with diagnosis of atrial fibrillation, atrial flutter, or sinus tachycardia. Only patients who developed these symptoms and signs within 24 h before randomisation, and within 72 h after entering an intensive care unit, were prospectively assigned to receive conventional sepsis therapy alone (control group) or conventional sepsis therapy plus landiolol (landiolol group) in an open-label manner. Landiolol hydrochloride was intravenously infused at an initial dose of 1 μg/kg per min within 2 h after randomisation and the dose could be increased per study protocol to a maximum of 20 μg/kg per min. Patients in both groups received conventional therapy (Japanese Clinical Practice Guidelines for the Management of Sepsis and Septic Shock 2016), including respiratory and fluid resuscitation, antimicrobials, and catecholamines. The treating physicians were required to stabilise the patient's haemodynamic status before randomisation. Randomisation was done using a central randomisation system and dynamic allocation with the minimisation method by institution, heart rate at randomisation (≥100 to <120 bpm or ≥120 bpm), and age (<70 years or ≥70 years). The primary outcome was the proportion of patients with heart rate of 60-94 bpm at 24 h after randomisation. Patients without heart rate data at 24 h after randomisation were handled as non-responders. The primary outcome was analysed using the full analysis set on an as-assigned basis, while safety was analysed using the safety analysis set according to the treatment received. This study was registered with the Japan Pharmaceutical Information Center Clinical Trials Information database, number JapicCTI-173767. Findings: Between Jan 16, 2018 and Apr 22, 2019, 151 patients were randomly assigned, 76 to the landiolol group and 75 to the control group. A significantly larger proportion of patients in the landiolol group had a heart rate of 60-94 bpm 24 h after randomisation than in the control group (55% [41 of 75] vs 33% [25 of 75]), with a between-group difference of 23·1% (95% CI 7·1-37·5; p=0·0031). Adverse events were observed in 49 (64%) of 77 patients in the landiolol group and in 44 (59%) of 74 in the control group, with serious adverse events (including adverse events leading to death) in nine (12%) of 77 and eight (11%) of 74 patients. Serious adverse events related to landiolol occurred in five (6%) of 77 patients, including blood pressure decreases in three patients (4%) and cardiac arrest, heart rate decrease, and ejection fraction decrease occurred in one patient each (1%). Interpretation: Landiolol resulted in significantly more patients with sepsis-related tachyarrhythmia achieving a heart rate of 60-94 bpm at 24 h and significantly reduced the incidence of new-onset arrhythmia. Landiolol was also well tolerated, but it should be used under appropriate monitoring of blood pressure and heart rate owing to the risk of hypotension in patients with sepsis and septic shock. Funding: Ono Pharmaceutical Co.
Effect of Landiolol hydrochloride on Hemodynamics in a Histamine-Induced Shock Model
Drugs R D 2021 Sep;21(3):321-329.PMID:34128200DOI:10.1007/s40268-021-00354-3.
Background and objective: Anaphylactic shock is a serious adverse drug reaction that can occur in response to contrast media used during coronary computed tomography angiography. The imaging quality of coronary computed tomography angiography is improved by β-blockers, which decrease heart rate. In this study, we sought to analyze anaphylactic shock treatment in patients receiving short-acting β1-blockers. Methods: We examined the influence of epinephrine and glucagon on hemodynamics during β-blocker treatment, using a dog histamine shock model; the β1-blocker Landiolol hydrochloride was used. The effects of these drugs were assessed by recording changes relative to established baselines. Results: Histamine and landiolol decreased mean blood pressure. Histamine exerted no apparent effect on heart rate, whereas landiolol decreased heart rate. Further, landiolol reduced histamine-mediated increases in the force of cardiac contraction. Increasing the doses of epinephrine and glucagon ameliorated anaphylactic shock-induced deterioration in hemodynamic parameters in subjects receiving landiolol. Conclusions: In patients receiving landiolol for coronary computed tomography angiography, deterioration in hemodynamic parameters due to anaphylactic shock can be mitigated by increasing the doses of epinephrine and glucagon. Clinicians should thus prepare appropriate amounts of epinephrine and glucagon prior to coronary computed tomography angiography.
Safety and Efficacy of Landiolol hydrochloride in Children with Tachyarrhythmia of Various Etiologies
Pediatr Cardiol 2021 Dec;42(8):1700-1705.PMID:34097085DOI:10.1007/s00246-021-02653-7.
The safety and efficacy of landiolol have not been fully elucidated in pediatric patients. This study aimed to clarify the safety and efficacy of landiolol in a pediatric cohort. We retrospectively assessed the clinical features of 21 pediatric patients who were administered landiolol at our hospital. We also investigated the rates of sinus rhythm conversion and heart rate response. The median patient age was 7 months (interquartile range 1-13 months). The etiology of tachyarrhythmia was junctional ectopic tachycardia in 10 patients (47.6%), atrial tachycardia in 10 patients (47.6%), and ventricular tachycardia in 1 patient (4.8%). Of the 21 children, 18 (85.7%) had congenital heart defects, including 14 (77.8%) in whom a landiolol infusion was performed perioperatively. The landiolol infusion was effective in 18 pediatric patients (85.7%), as measured by the conversion to sinus rhythm or a reduced heart rate. Atrial tachycardia in the perioperative period was terminated in all patients. Of 7 patients with tachyarrhythmias unrelated to the perioperative period, landiolol was effective in 5. No adverse effects were reported in any patient. Landiolol infusion is effective and safe in pediatric patients with tachyarrhythmia of various etiologies, especially those with atrial tachyarrhythmia during the perioperative period.
Landiolol hydrochloride for prevention of atrial fibrillation during esophagectomy: a randomized controlled trial
JA Clin Rep 2020 May 11;6(1):34.PMID:32394218DOI:10.1186/s40981-020-00338-3.
Introduction: Landiolol hydrochloride reduces the incidence of perioperative atrial fibrillation (AF) in cardiac surgery; however, little evidence is available regarding its effects in other types of surgery, including esophagectomy. We assessed the hypothesis that landiolol reduces perioperative AF and other complications associated with esophagectomy. Methods: This single-center, randomized, double-blind, parallel-group study enrolled patients scheduled for esophagectomy. Patients were divided into those given landiolol at 3 μg/kg/min or placebo for 24 h. The primary outcome was the proportion of patients who developed AF within 96 h starting at 9:00 AM on the day of surgery. The secondary outcomes were the proportion of patients whose AF appeared within 24 h, other complications based on the Clavien-Dindo classification, and the intensive care unit and hospital stays. Results: Despite early study termination, 80 patients were screened, and 56 were enrolled (28/group) from September 2016 to June 2018. AF occurred within 96 h of surgery in six (21.4%) patients in the landiolol group and five (17.9%) patients in the placebo group (odds ratio, 1.26; 95% confidence interval, 0.33-4.7) and within 24 h of surgery in three (10.7%) patients in the landiolol group and two (7.1%) patients in the placebo group. There were no significant differences in the incidence of complications or in the number of intensive care unit or hospital stays between the groups. Conclusion: Although our small sample size prevents definitive conclusions, landiolol might not reduce the occurrence of AF or other complications. Trial registration: UMIN, UMIN000024040. Registered 13 September 2016, http://www.umin.ac.jp/ctr/index/htm.