Procainamide HCl

Procainamide hydrochloride (CAS No. 614-39-1) is a classic sodium channel blocker, with the cardiac sodium channel (Nav1.5) as its primary target, exhibiting an IC₅₀ of approximately 3~10 μM. It exerts antiarrhythmic effects by inhibiting the conduction of action potentials in cardiomyocytes; simultaneously, it possesses anti-inflammatory and immunomodulatory properties, capable of suppressing neutrophil activation and cytokine release. Clinically, it is primarily indicated for the treatment of ventricular arrhythmias (e.g., ventricular premature beats, ventricular tachycardia). The intravenous loading dose is 10~15 mg/kg (infusion time ≥ 30 minutes) with a maintenance dose of 2~6 mg/min, while the oral maintenance dose is 500~1000 mg per dose administered every 6 hours. Therapeutic drug monitoring is required (therapeutic window: 4~10 μg/ml), and long-term administration may lead to adverse reactions such as lupus-like syndrome. Moreover, procainamide hydrochloride demonstrates inhibitory activity against DNA methyltransferase 1 (DNMT1), which allows it to regulate DNA methylation status, restore the expression of tumor suppressor genes, and inhibit cell proliferation and migration. Additionally, this compound exerts the biological effect of inducing cellular vacuolization.