Cardiotoxic and antiarrhythmic tertiary amine local anesthetics: sodium channel affinity vs. sodium channel gating.
Tertiary amine local anesthetics (LAs) are clinically valuable agents for controlling pain and for treating some cardiac arrhythmias. These drugs inhibit conduction of electrical activity by blocking voltage-gated sodium channels. Interestingly, LAs can influence the conduction of electrical activity in heart muscle without markedly altering normal skeletal muscle activity. This review discusses the interactions between sodium channels and LAs, the methods used to investigate these interactions, and the mechanisms proposed to explain the greater LA sensitivity of cardiac sodium channels as compared with skeletal muscle sodium channels.
Department of Biological Sciences, Murray State University, Murray, KY 42071, USA. sterling.wright@murraystate.edu
Sterling N
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Wright
D000588:Amines / Q000009:adverse effects*; D000779:Anesthetics, Local / Q000009:adverse effects*; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000009:adverse effects; D006801:Humans; D015640:Ion Channel Gating; D018482:Muscle, Skeletal / Q000378:metabolism; D009206:Myocardium / Q000378:metabolism; D015222:Sodium Channels / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology
D000588:Amines; D000779:Anesthetics, Local; D000889:Anti-Arrhythmia Agents; D015222:Sodium Channels