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抗不律性特性を有する新型抗風性剤であるラノラジンによる電気生理学的効果

Charles Antzelevitch¹, Luiz Belardinelli, Andrew C Zygmunt

¹Masonic Medical Research Laboratory, 2150 Bleecker St, Utica, NY 13501, USA. ca@mmrl.edu

|August 11, 2004

まとめ

抗血管性薬であるラノラジン (Ranolazine) は,心臓細胞のイオンチャネルとアクションポテンシャルに影響を及ぼします. その効果は,アンギナの治療を超えて,潜在的な抗不律性活動を示唆します.

科学分野:

心血管電気生理学心血管電気生理学
薬理学薬理学とは
心臓のイオンチャネル

背景:

ラノラジン (Ranolazine) は,抗発血効果を持つ新しい抗血管性剤です.
治療用濃度で心拍数や血圧を低下させることなく機能します.
その電気生理学的効果は,詳細な調査を必要とします.

研究の目的:

ラーノラジンの電気生理学的効果を調べる.
心臓製剤におけるイオンチャネルとアクションポテンシャルへの影響を調査する.
その潜在的な抗不律性特性を評価するために.

主な方法:

犬の心室製剤から得られたトランスメブランアクションポテンシャル (AP) と擬似ECGの記録.
隔離された犬の心室筋細胞からの全細胞の電流記録.
ランオラジンの様々なイオン電流に対する効果の評価は,I(Kr),遅いI(Na),および遅いI(Ca) を含む.

主要な成果:

ラーノラジンは,主要イオン流 (I(Kr),遅いI(Na),遅いI(Ca)) およびI(Na-Ca) を阻害しました.
エピカルディアのAP期間を延長したが,ミオカルディアのAP期間を短縮し,リポラライゼーション (TDR) のトランムラル分散を減少させた.
ラーノラジンは早期のアフターデポラライゼーション (EADs) を抑制し,Torsade de Pointes (TdP) のようなプロアリズム的イベントを誘導しませんでした.

結論:

ラーノラジンのイオンチャネル効果は,慢性アミオダロンに匹敵する.
EADを抑制し,TDRを軽減する薬剤の能力は,潜在的な抗不律性の活性を示しています.
これらの発見は,ラノラジンが抗性特性を超えた利点を提供することを示唆しています.

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