Vernakalant
(Synonyms: 维那卡兰,RSD1235) 目录号 : GC37897
Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
Cas No.:794466-70-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
[1] I. Stiell, et al. EDWARD A. PANACEK, MD, MPH| VOLUME 48, ISSUE 4, SUPPLEMENT , 46-47,
| Cas No. | 794466-70-9 | SDF | |
| 别名 | 维那卡兰,RSD1235 | ||
| Canonical SMILES | COC1=C(C=C(C=C1)CCO[C@H]2[C@@H](CCCC2)N3CC[C@H](C3)O)OC | ||
| 分子式 | C20H31NO4 | 分子量 | 349.46 |
| 溶解度 | Soluble in DMSO | 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 | 2.8616 mL | 14.3078 mL | 28.6156 mL |
| 5 mM | 0.5723 mL | 2.8616 mL | 5.7231 mL |
| 10 mM | 0.2862 mL | 1.4308 mL | 2.8616 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。
Introducing Vernakalant into Clinical Practice
Arrhythm Electrophysiol Rev 2019 Mar;8(1):70-74.PMID:30918671DOI:10.15420/aer.2018.71.2.
Vernakalant is an antiarrhythmic drug licensed for the pharmacological cardioversion of recent onset AF. Randomised clinical trials, backed up by real-world experience, have confirmed its efficacy at restoring sinus rhythm. Vernakalant can be administered simply with a short time to action, facilitating early discharge from hospital in selected patients in place of electrical cardioversion. The authors explore the data behind Vernakalant and discuss how it can be introduced into clinical practice.
Vernakalant in the management of atrial fibrillation
Ann Pharmacother 2008 Apr;42(4):533-42.PMID:18334607DOI:10.1345/aph.1K542.
Objective: To review the pharmacology and clinical evidence of the use of Vernakalant in the management of atrial fibrillation (AF). Data sources: Peer-reviewed articles published in the English language were identified from MEDLINE and Current Contents databases (both 1966-March 5, 2008) using the search terms RSD 1235 and Vernakalant. Citations from available articles and recent meeting abstracts were reviewed for additional references. During the preparation of this article, Vernakalant was being reviewed by the Food and Drug Administration (FDA). Therefore, information posted on the FDA Web site was also evaluated. Study selection and data extraction: Phase 2 and Phase 3 clinical studies of both intravenous and oral Vernakalant were reviewed. The design and results of the studies were critically evaluated. Data synthesis: Vernakalant is a sodium and ultra-rapid potassium channel blocker with atrial selective effects. In 2 clinical studies evaluating use of intravenous Vernakalant in cardioversion of patients with recent-onset AF, Vernakalant improved the chance of restoration of normal sinus rhythm (combined results 51% vs 3.8% with placebo; p < 0.001). In postoperative AF, intravenous Vernakalant also improved the chance of restoration of normal sinus rhythm (45% vs 15% with placebo; p = 0.0002). Early Phase 2 studies demonstrated that oral Vernakalant 300 mg or 600 mg twice daily successfully maintained sinus rhythm compared with placebo. No proarrhythmias relating to Vernakalant have been reported to date. Common adverse effects include dysgeusia, sneezing, and paresthesia. Conclusions: Vernakalant is a new atrial-selective antiarrhythmic agent. Phase 3 clinical trials of the intravenous formulation and early Phase 2 studies of the oral formulation demonstrated Vernakalant to be efficacious and safe in converting recent-onset AF to sinus rhythm. Further studies are needed to explore the efficacy and safety of Vernakalant use in patients with severe heart failure and AF, as well as its relative efficacy and safety compared with other antiarrhythmic agents, especially with long-term use.
Vernakalant: A novel agent for the termination of atrial fibrillation
Am J Health Syst Pharm 2010 Jul 15;67(14):1157-64.PMID:20592320DOI:10.2146/ajhp080501.
Purpose: The pharmacology, pharmacokinetics, safety, clinical efficacy, and role of intravenous Vernakalant hydrochloride for the rapid conversion of atrial fibrillation (AF) to normal sinus rhythm are reviewed. Summary: Vernakalant, currently being evaluated by the Food and Drug Administration (FDA), for the termination of atrial fibrillation, differs in pharmacology from other antiarrhythmics; it achieves action potential interference through blockade of sodium and potassium currents. Vernakalant's actions appear to be directed at relatively atrial-selective potassium currents, which result in lengthening of the atrial action potential and prolongation of the atrial action potential plateau, while not significantly affecting the Q-T interval or the ventricular effective refractory period. As a result, the proarrhythmic effects observed with all other agents approved by FDA for the treatment of AF are eliminated. In clinical trials of Vernakalant versus placebo, a statistically significant number of patients converted to normal sinus rhythm after receiving Vernakalant. For patients with atrial fibrillation continuing for 3-72 hours, the median time to conversion was between 8 and 14 minutes, with 79% of those who converted remaining in sinus rhythm at 24 hours. Conclusion: Intravenous Vernakalant, a novel, relatively atrial-selective antiarrhythmic agent, appears to offer an effective and safe approach to the rapid conversion of recent-onset AF to normal sinus rhythm.
Intravenous Vernakalant: a review of its use in the management of recent-onset atrial fibrillation
Drugs 2011 Jan 22;71(2):237-52.PMID:21275448DOI:10.2165/10489050-000000000-00000.
Intravenous Vernakalant (Brinavess®) is an atrial-repolarization-delaying agent that is currently approved in the EU for the rapid conversion of recent-onset atrial fibrillation to sinus rhythm. Vernakalant blocks atrial-specific potassium and sodium ion channels, prolonging atrial refractory periods and rate-dependently slowing atrial conduction, without promoting ventricular arrhythmia. In pivotal randomized, phase III trials, intravenous Vernakalant 3 mg/kg administered as a 10-minute infusion, followed by a 2 mg/kg 10-minute infusion after 15 minutes if atrial fibrillation persisted, was effective in the rapid termination of recent-onset atrial fibrillation in nonsurgical patients (≥3 hours' to ≤7 days' duration) and in those with postoperative atrial fibrillation (3-72 hours' duration) following cardiac surgery. Conversion to sinus rhythm occurred rapidly following infusion of Vernakalant, with the majority of patients converting after the first dose, and conversion to sinus rhythm was generally associated with a rapid resolution of symptoms. These antiarrhythmic effects of Vernakalant were durable, with most responders remaining in sinus rhythm 24 hours after treatment initiation. In nonsurgical patients with recent-onset atrial fibrillation of 3-48 hours' duration, Vernakalant was more effective than intravenous amiodarone, with a significantly higher proportion of patients converting to sinus rhythm within the first 90 minutes of treatment. Vernakalant was generally well tolerated in clinical trials, with most adverse events being of mild or moderate severity and not treatment limiting. Increases in QRS or QT intervals were transient, and there was no increased incidence of ventricular arrhythmia observed with Vernakalant compared with placebo. Therefore, intravenous Vernakalant provides an effective option for the management of recent-onset atrial fibrillation.
Vernakalant. Too dangerous in atrial fibrillation
Prescrire Int 2012 May;21(127):119-22.PMID:22827000doi
The usual aim of treatment for patients with symptomatic paroxysmal or recent-onset atrial fibrillation, including after cardiac surgery, is to slow the heart rate. Electrical and drug (amiodarone) cardioversion are other options. Vernakalant, an antiarrhythmic drug, has been authorised in the European Union for rapid reduction of recent-onset atrial fibrillation. It is only available in an injectable form. Vernakalant has not been compared in clinical trials with treatments slowing the heart rate, or with electrical cardioversion. The only available comparison with another antiarrhythmic agent is a clinical pharmacology study versus amiodarone, a slow-acting drug, based on the rate of cardioversion at 90 minutes in 240 patients. As expected, given the brief observation period, the rate was significantly higher with Vernakalant (51.7% versus 5.2%). During clinical evaluation, 6 deaths occurred in the Vernakalant groups versus none in the other groups (placebo or amiodarone). The main adverse effects of Vernakalant are cardiac arrhythmias (ventricular arrhythmia, torsades de pointes, bradycardia) and severe hypotension. Altered taste, sneezing, paraesthesia, nausea and pruritus were frequent, and respiratory and neuropsychological effects were also reported. A trial in atrial flutter was interrupted when cases of cardiogenic shock occurred. Interactions are to be expected with drugs that prolong the QT interval, and also with drugs that lower the heart rate or the blood potassium concentration. In practice, it is better to continue to use amiodarone for drug cardioversion and to avoid using Vernakalant.