Vemakalant (CAS: 794466-70-9) is a small molecule antiarrhythmic agent used for the treatment of atrial fibrillation. Vemakalant was first approved by the US Food and Drug Administration (FDA) under the brand name Kynapid in 2010. This article will provide an overview of vemakalant, including its chemical properties, health benefits, potential effects, product mechanism, safety, side effects, dosing information, and a conclusion on its use.
Chemical Properties The chemical name for vemakalant is N-(2-hydroxy-5-(4-(4-methylpiperazin-1-yl)phenyl)benzyl)acetamide. Its molecular formula is C24H31N3O3, and it has a formula weight of 409.53 g/mol. The CAS number for this compound is 794466-70-9.
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Health Benefits Vemakalant is primarily used for the treatment of atrial fibrillation, which is a type of cardiac arrhythmia characterized by irregular and rapid heartbeat. It works by blocking certain ion channels in the heart, specifically the rapidly activating delayed rectifier potassium currents (IKr), thereby prolonging the action potential duration and preventing the occurrence of arrhythmias. By blocking these ion channels, vemakalant can help restore normal heart rhythm and improve symptoms associated with atrial fibrillation.
Potential Effects In clinical trials, vemakalant has been shown to be highly effective at improving cardioversion rates in patients with recent-onset atrial fibrillation. It has also been found to be well-tolerated, with few serious side effects reported. Additionally, vemakalant has demonstrated good pharmacokinetic properties, meaning it is well-absorbed and distributed throughout the body, and is metabolized and eliminated from the body in a predictable manner.
Product Mechanism Vemakalant is a selective blocker of the IKr potassium channels in the heart. It works by binding to the open state of the channel, thereby slowing channel closing and prolonging the action potential duration. This effect leads to a decrease in the frequency and duration of atrial fibrillation episodes.
Safety Overall, vemakalant has been found to be safe and well-tolerated in clinical trials. However, like all medications, it does carry some risks of side effects and adverse events. Patients taking vemakalant should be monitored regularly for any signs of allergic reactions, liver dysfunction, or other serious side effects.
Side Effects Some of the most common side effects reported with vemakalant include nausea, headache, and dizziness. These side effects are usually mild to moderate in severity and go away on their own over time. More serious side effects, such as QT prolongation or hypotension, are rare but can occur in some patients.
Dosing Information Vemakalant is typically administered intravenously by a healthcare provider. The recommended dose for patients with atrial fibrillation is 30 mg infused over 10 minutes. If cardioversion does not occur within 15 minutes, an additional 10-minute infusion of 20 mg may be given.
Conclusion Vemakalant is a highly effective and well-tolerated medication used for the treatment of atrial fibrillation. As a selective blocker of IKr potassium channels in the heart, it helps restore normal heart rhythm and improve symptoms associated with this condition. While it does carry some risks of side effects and adverse events, overall, it has been found to be safe and effective in clinical trials. Patients taking vemakalant should work closely with their healthcare providers to ensure proper dosing and monitoring for any potential side effects
