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Active ingredient: Procainamide - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antiarrhythmic Agents

Dosage Forms

  • Capsule
  • Liquid
  • Solution
  • Tablet (extended-release)

Brands / Synonyms

Biocoryl; Novocainamid; Novocainamide; Novocaine Amide; Novocamid; Procainamide; Procainamide Hcl; Procaine Amide; Procamide; Procan; Procan Sr; Procanbid; Procapan; Promine; Pronestyl; Pronestyl-SR; Pronestyl-Sr

Indications

For the treatment of life-threatening ventricular arrhythmias.

Pharmacology

Procainamide is an agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Procainamide appears to be similar to that of procaine and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected.

Mechanism of Action

Procainamide is sodium channel blocker. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action.

Absorption

75 to 95%

Toxicity

LD50=95 mg/kg (rat, IV); LD50=312 mg/kg (mouse, oral); LD50=103 mg/kg (mouse, IV); LD50=250 mg/kg (rabbit, IV)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

Complete heart block

Procainamide should not be administered to patients with complete heart block because of its effects in suppressing nodal or ventricular pacemakers and the hazard of asystole. It may be difficult to recognize complete heart block in patients with ventricular tachycardia; but if significant slowing of ventricular rate occurs during procainamide treatment without evidence of A-V conduction appearing procainamide should be stopped. In cases of second degree A-V block or various types of hemiblock, procainamide should be avoided or discontinued because of the possibility of increased severity of block, unless the ventricular rate is controlled by an electrical pacemaker.

Idiosyncratic hypersensitivity

In patients sensitive to procaine or other ester-type local anesthetics, cross sensitivity, to procainamide is unlikely. However, it should be borne in mind, and procainamide should not be used if it produces acute allergic dermatitis, asthma or anaphylactic symptoms.

Lupus Erythematosus

An established diagnosis of systemic lupus erythematosus is a contraindication to procainamide therapy, since aggravation of symptoms is highly likely.

Torsades de Pointes

In the unusual ventricular arrhythmia called "les torsades de pointes" (twistings of the points) characterized by alternation of one or more ventricular premature beats in the directions of the QRS complexes on ECG in persons with prolonged Q-T and often enhanced U waves, Group 1A antiarrhythmic drugs are contraindicated. Administration of procainamide in such cases may aggravate this special type of ventricular extrasystole or tachycardia instead of suppressing it.

Drug Interactions

If other antiarrhythmic drugs are being used additive effects on the heart may occur with procainamide administration, and dosage reduction may be necessary.

Anticholinergic drugs administered concurrently with procainamide may produce additive antivagal effects on A-V nodal conduction, although this is not as well documented for procainamide as for quinidine.

Patients taking procainamide who require neuromuscular blocking agents such as succinylcholine may require less than usual doses of the latter, due to procainamide effects on reducing acetylcholine release.

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