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Site-directed deuteration of dronedarone preserves cytochrome P4502J2 activity and mitigates its cardiac adverse effects in canine arrhythmic hearts.
Author: ChanEric Chun Yong, GotoAi, HanMarcus Qingrui, Izumi-NakasekoHiroko, KambayashiRyuichi, KarkhanisAneesh V, KojodjojoPipin, LeowJacqueline Wen Hui, PangJeremy Kah Sheng, SohBoon Seng, SugiyamaAtsushi, VenkatesanGopalakrishnan
Original Abstract of the Article :
Cytochrome P4502J2 (CYP2J2) metabolizes arachidonic acid (AA) to cardioprotective epoxyeicosatrienoic acids (EETs). Dronedarone, an antiarrhythmic drug prescribed for treatment of atrial fibrillation (AF) induces cardiac adverse effects (AEs) with poorly understood mechanisms. We previously demonstr...See full text at original site
Dr.Camel's Paper Summary Blogラクダ博士について
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9532722/
データ提供:米国国立医学図書館(NLM)
A Deuterium Solution: Mitigating the Cardiac Side Effects of Dronedarone
The search for effective treatments for [atrial fibrillation (AF)] is an ongoing quest in the field of [cardiology]. Dronedarone, a widely used antiarrhythmic drug, often comes with unwelcome cardiac side effects. This study, like a brilliant scientist in a lab, explores a novel approach to mitigating these side effects.
The researchers, using their scientific ingenuity, synthesized a deuterated analogue of dronedarone, named poyendarone, and investigated its impact on CYP2J2 activity and cardiac adverse effects. They found that poyendarone, unlike its parent compound, does not inhibit CYP2J2, a crucial enzyme involved in cardioprotection. In fact, poyendarone preserves CYP2J2 activity, leading to reduced cardiac mitochondrial toxicity.
Moreover, poyendarone demonstrated a significant reduction in beat-to-beat variability, a key marker of proarrhythmic risk, compared to dronedarone in cardiomyocytes. These findings, like a desert oasis, offer a glimmer of hope for reducing the cardiac side effects of dronedarone.
A Promising Solution: Deuteration as a Strategy for Improved Cardiac Safety
The study provides compelling evidence for the potential of deuteration as a strategy for enhancing the safety of antiarrhythmic drugs. This innovative approach, like a new trail carved into the desert, could lead to the development of safer and more effective treatments for AF.
A Heartfelt Reminder: Understanding the Potential Benefits and Risks
It's crucial to remember that while this study offers a promising solution, more research is needed to confirm the long-term efficacy and safety of poyendarone. As with any medication, it's important to consult with your healthcare provider to make informed decisions about your treatment options.
Dr.Camel's Conclusion
The search for safer and more effective antiarrhythmic drugs is a constant journey through the vast desert of scientific exploration. This study, like a shining star in the night sky, highlights the potential of deuteration to mitigate the cardiac side effects of dronedarone. With continued research and innovation, we can hope for a future where patients can benefit from effective treatments without compromising their cardiac health.
Date :
- Date Completed n.d.
- Date Revised 2022-10-11
Further Info :
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