<p>The aim of this work was to study changes in the spectral characteristics of the heart rhythm of experimental animals under the influence of the class I antiarrhythmic drug ethacizine hydrochloride and its supramolecular complexes with glycyrrhizic acid (GA) and its monoammonium salt (MASGA) in various mole ratios (2:1, 4:1, 8:1). It was shown that the complexes GA-ethacizine HCl (2:1) and MASGA-ethacizine HCl (4:1) had stronger negative inotropic effects in which Na<sup>+</sup> channels of cardiomyocytes played an important role as compared to ethacizine and the other complexes. At the same time, these complexes promoted increased excretion of Ca<sup>2+</sup> ions through the Na<sup>+</sup>/Ca<sup>2+</sup> exchanger and a decreased level [Ca<sup>2+</sup>]<sub>i</sub> level by blocking Na<sup>+</sup> channels and reducing the content of Na<sup>+</sup> ions in cardiomyocytes, resulting in a decrease in the contractile activity of the heart muscle. It was determined during the studies that the studied complexes had a more pronounced antiarrhythmic effect than ethacizine, especially the MASGA-ethacizine HCl (4:1) complex, which may become a promising antiarrhythmic drug as a result of further studies.</p>

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Antiarrhythmic Activity of Ethacizine Hydrochloride and its Supramolecular Complexes with Glycyrrhizic Acid and its Monoammonium Salt

  • Yu. I. Oshchepkova,
  • V. V. Uzbekov,
  • I. Z. Jumayev,
  • Sh. Yu. Rustamov,
  • P. B. Usmanov,
  • Sh. I. Salikhov

摘要

The aim of this work was to study changes in the spectral characteristics of the heart rhythm of experimental animals under the influence of the class I antiarrhythmic drug ethacizine hydrochloride and its supramolecular complexes with glycyrrhizic acid (GA) and its monoammonium salt (MASGA) in various mole ratios (2:1, 4:1, 8:1). It was shown that the complexes GA-ethacizine HCl (2:1) and MASGA-ethacizine HCl (4:1) had stronger negative inotropic effects in which Na+ channels of cardiomyocytes played an important role as compared to ethacizine and the other complexes. At the same time, these complexes promoted increased excretion of Ca2+ ions through the Na+/Ca2+ exchanger and a decreased level [Ca2+]i level by blocking Na+ channels and reducing the content of Na+ ions in cardiomyocytes, resulting in a decrease in the contractile activity of the heart muscle. It was determined during the studies that the studied complexes had a more pronounced antiarrhythmic effect than ethacizine, especially the MASGA-ethacizine HCl (4:1) complex, which may become a promising antiarrhythmic drug as a result of further studies.