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Class I Antiarrhythmic Drugs: Na+ Channel Blockers

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Antiarrhythmic Drugs

Part of the book series: Current Cardiovascular Therapy ((CCT))

Abstract

Class I antiarrhythmic agents or Na+ channel blockers are among the first drugs that have been used for several decades, and are divided into three groups, according to their cellular electrophysiologic effects. The sodium ion currents or INa enter the cell very fast during phase-0 of action potential and is responsible for depolarization.

Sodium channel blockers, therefore prolong conduction time, and refractoriness of the atria, ventricle, and the Purkinje system. These agents are effective against many arrhythmias such as atrial fibrillation and flutter.

Their most important side effects are proarrhythmia and inducing torsades de pointes. With introduction of newer antiarrhythmic agents, INa blockers are less frequently used.

INa currents are controlled and modulated by several genes and the most common being the SCN5A gene. Mutations in SCN5A gene cause several genetic syndromes such as Brugada syndrome, LQT3 syndrome, familial AF, and many others. The novel indications of INa blockers such as low dose quinidine in Brugada syndrome, and Mexiletine in LQT3 syndrome, provide new therapeutic options in patients with sodium channelopathies.

Discoveries of ion channels and their respective genes as well as their mutations are discussed in this chapter, including the most recently published guidelines of respective societies.

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Abbreviations

AAD:

Antiarrhythmic drug

AF:

Atrial fibrillation

AP:

Action potential

APD:

Action potential duration

ATP:

Adenosine triphosphate

AVNRT:

Atrioventricular nodal reentrant tachycardia

AVRT:

Atrioventricular reentrant tachycardia

CAD:

Coronary artery disease

CHF:

Congestive heart failure

CPVT:

Catecholaminergic polymorphic ventricular tachycardia

DAD/EAD:

Delayed/early afterdepolarization

ECG:

Electrocardiogram

ERP:

Effective refractory period

ICD:

Implantable cardioverter-defibrillator

LQT3:

Long QT 3 (syndrome)

LV:

Left ventricular

LVH:

Left ventricular hypertrophy

SCD:

Sudden cardiac death

TdP:

Torsades de Pointes

VF:

Ventricular fibrillation

VT:

Ventricular tachycardia

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Acknowledgements

We wish to thank Sarah Janell Honoré for her superb assistance in the preparation of this manuscript.

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Authors and Affiliations

  1. Heart and Rhythm Medical Group, Monte Sereno, CA, USA

    Mohammad Shenasa, Mohammad-Ali Shenasa & Mariah Smith

  2. Department of Cardiovascular Services, O’Connor Hospital, San Jose, CA, USA

    Mohammad Shenasa

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  1. Department of Cardiology, University Hospital of Sabadell, Institut d’Investigació i Innovació I3PT, University Autonoma of Barcelona, Sabadell, Spain

    Antoni Martínez-Rubio

  2. Department of Pharmacology, School of Medicine, Universidad Complutense, CIBERCV, Madrid, Spain

    Juan Tamargo

  3. “Carol Davila” University of Medicine, Colentina University Hospital, Bucharest, Romania

    Gheorghe- Andrei Dan

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Shenasa, M., Shenasa, MA., Smith, M. (2020). Class I Antiarrhythmic Drugs: Na+ Channel Blockers. In: Martínez-Rubio, A., Tamargo, J., Dan, G . (eds) Antiarrhythmic Drugs. Current Cardiovascular Therapy. Springer, Cham. https://doi.org/10.1007/978-3-030-34893-9_2

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