LAPPACONITINE HYDROBROMIDE (ALLAPININ): CLINICAL AND EXPERIMENTAL PROSPECTS
Abstract
Despite the widespread use of antiarrhythmic drugs, the optimal therapy for cardiac arrhythmias in patients with coronary artery disease (CAD) remains a subject of debate. Limitations regarding class IC drugs are largely based on the results of the CAST trials conducted over 30 years ago. Current experimental and clinical data suggest that certain representatives of this class may have more complex mechanisms of action and may demonstrate a favorable efficacy and safety profile when used rationally. An experimental study demonstrated that lappaconitine hydrobromide affects not only sodium channels but also alters the expression of genes associated with potassium and calcium channels, as well as increases the expression of the acetylcholine transporter gene. This suggests a more complex mechanism of antiarrhythmic action than traditionally understood for class IC drugs. The clinical trial demonstrated comparability between the study groups in key clinical and surgical characteristics. The use of lappaconitine hydrobromide in combination with beta-blockers was associated with a statistically significant reduction in the incidence of postoperative atrial fibrillation and ventricular extrasystoles compared to beta-blocker monotherapy and demonstrated superiority over amiodarone therapy in several analyzed parameters. Short-term use of the drug in patients with preserved left ventricular systolic function was characterized by high clinical efficacy and a satisfactory safety profile. Current experimental data also demonstrate the potential for developing new lappaconitine hydrobromide derivatives with more pronounced activity at lower active substance concentrations. Conclusion. Lappaconitine hydrobromide exhibits a multifactorial mechanism of antiarrhythmic action that goes beyond the classic characteristics of class IC drugs. Its short-term use in combination with beta-blockers in patients with coronary artery disease after surgical myocardial revascularization and preserved left ventricular ejection fraction is an effective and safe method for preventing postoperative tachyarrhythmias. The obtained results support the rationale for further fundamental and clinical studies of the drug and its derivatives.
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