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How the Deuteration of Dronedarone Can Modify Its Cardiovascular Profile: In Vivo Characterization of Electropharmacological Effects of Poyendarone, a Deuterated Analogue of Dronedarone.

Author: ChanEric Chun Yong, ChibaKoki, GotoAi, Hagiwara-NagasawaMihoko, Izumi-NakasekoHiroko, KambayashiRyuichi, KondoYoshiki, LeowJacqueline Wen Hui, MatsumotoAkio, NunoiYoshio, SugiyamaAtsushi, VenkatesanGopalakrishnan, YeoZhi Jie

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

Deuteration of dronedarone, resulting in poyendarone, improved its cardiovascular profile. Poyendarone demonstrated similar pharmacokinetics to dronedarone but reduced β-adrenoceptor blocking activity and cardio-suppressive effects. It showed higher atrial selectivity in prolonging the effective refractory period, making it a promising anti-atrial fibrillatory drug candidate.
Paper Details　
Original Abstract of the Article :
Since deuterium replacement has a potential to modulate pharmacodynamics, pharmacokinetics and toxicity, we developed deuterated dronedarone; poyendarone, and assessed its cardiovascular effects. Poyendarone hydrochloride in doses of 0.3 and 3 mg/kg over 30 s was intravenously administered...See full text at original site
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引用元：
https://doi.org/10.1007/s12012-019-09559-0

データ提供：米国国立医学図書館（NLM）

Deuteration of Dronedarone: Modifying its Cardiovascular Profile

This study investigates the cardiovascular effects of poyendarone, a deuterated analogue of dronedarone, a drug used to treat atrial fibrillation. The study administered different doses of poyendarone to anesthetized dogs and monitored their cardiovascular responses. The researchers found that poyendarone, compared to dronedarone, showed similar pharmacokinetics but reduced beta-adrenoceptor blocking activity and cardio-suppressive effects. The study also found that poyendarone did not significantly inhibit IKr, a potassium channel current, and showed higher atrial selectivity in prolonging the effective refractory period of the atrium versus ventricle.

Deuteration: A Potential Approach to Enhancing Drug Efficacy

The study's findings suggest that deuteration, the replacement of hydrogen atoms with deuterium, can be a potential approach to modifying the cardiovascular profile of drugs like dronedarone. The study's results show that poyendarone, the deuterated analogue of dronedarone, exhibits a favorable cardiovascular profile with reduced side effects.

Navigating Cardiovascular Health: A Journey Towards Precision Medicine

The desert landscape is a testament to the power of adaptation and resilience. Similarly, navigating cardiovascular health requires a careful approach, considering individual needs and the potential impact of medications. This study highlights the potential of deuteration as a tool for improving the safety and efficacy of cardiovascular drugs, leading us towards a future of personalized medicine.

Dr. Camel's Conclusion

This study showcases the exciting possibilities of drug design and development. Deuteration, a subtle modification to a drug's structure, can have a significant impact on its pharmacological properties. This research offers a promising glimpse into the future of drug development, where tailored treatments can be designed to address individual needs and minimize side effects.
Date :
  1. Date Completed 2021-01-18
  2. Date Revised 2021-01-18
Further Info :

Pubmed ID

31898152

DOI: Digital Object Identifier

10.1007/s12012-019-09559-0

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SNS
PICO Info
in preparation
Languages

English

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