Disopyramide Phosphate

Disopyramide Phosphate is a class Ia anti-arrhythmic used in ventricular arrhythmias by stabilizing cardiac electrical activity.

Structure of Disopyramide Phosphate

  • Disopyramide phosphate is a class IA antiarrhythmic agent with a quinuclidine core structure. It features a dibenzodioxepin ring system linked to a quinuclidine moiety and a diethylamino group.
  • Chemical Formula: C₂₀H₂₉N₃O₄S·H₃PO₄
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Structure of Disopyramide Phosphate

Mode of Action

  • Class IA Antiarrhythmic: Inhibits fast sodium channels, prolongs action potential duration and refractory period.
  • Potassium Channel Blockade: Extends repolarization by blocking potassium efflux.
  • Anticholinergic Effects: Exhibits antimuscarinic activity, which can lead to side effects like dry mouth and blurred vision.
  • Effect on Heart Rate: Converts atrial fibrillation to sinus rhythm and prevents reentrant arrhythmias.
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Uses

  • Ventricular Arrhythmias: Treats ventricular tachycardia and ventricular fibrillation.
  • Atrial Arrhythmias: Manages atrial fibrillation and atrial flutter.
  • Reentrant Arrhythmias Prevention: Effective in preventing recurrence post-cardiac events.
  • Antiarrhythmic Prophylaxis: Used after myocardial infarction to prevent arrhythmias.

Structure-Activity Relationship (SAR)

  • Quinuclidine Core: Essential for blocking fast sodium channels and prolonging the action potential.
  • Dibenzodioxepin Ring System: Enhances lipophilicity, improving membrane permeability and binding affinity to cardiac ion channels.
  • Diethylamino Group: Increases affinity for sodium channels and contributes to antimuscarinic side effects.
  • Substituents: Modifications on the aromatic rings can influence potency and selectivity for ion channels.
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Synthesis

synthesis of disopyramide phosphate

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