Anticholinergic activity and pharmacokinetic parameters of agent SS-68 with properties of class iii antiarrhythmic drugs

Авторы

  • Saida Kazbekovna Bogus Kuban State Medical University
  • Alexandr Kulikov Belgorod State University
  • Dmitry V. Vinakov Belgorod State University
  • Konstantin Suzdalev Southern Federal University
  • Pavel Alexandrovich Galenko-Yaroshevsky Kuban State Medical University

Аннотация

It was shown that the indole derivate SS-68 (50 and 250 µg/kg intravenous) in acute experiments on cats with neurogenic atrial fibrillation (AF) has a dose-dependent antiarrhythmic action which is associated with the neurotropic influence of this substance, since the suppression of the AF coincides with its anticholinergic effect observed for more than 2 hours, but cardiotropic action at this time was not observed. High antiarrhythmic activity of SS-68 to neurogenic AF may be due to the IKAch inhibition and blockade of M2-cholinergic receptors. SS-68 (50 µg/kg intravenous) in experiments on rabbits is characterized by the following pharmacokinetic parameters: Cmax = 14.5 ng/ml of blood plasma (duration of plasma exposure of SS-68 is 4 hours), T1/2 = 1,1 ± 0.06 hours, MRT(0 – t) = 1.6 ± 0.08 hours, AUC(0 – 1440) = 1006.1 ± 147.7 ng/ml×min, Vss = 4.8 ± 0.8 l/kg and CL = 0.051 l/h. Based on pharmacodynamic and pharmacokinetic parameters it was suggested that anticholinergic action of SS-68 in neurogenic AF will occur in a much lower dose than 50 mg/kg.

Ключевые слова:

vagus nerve, neurogenic atrial fibrillation, indole derivate SS-68, antiarrhythmic action, pharmacokinetics

Вклад авторов

Saida Kazbekovna Bogus, Kuban State Medical University

PhD of Medical Sciences, Assistant of the Department of Pharmacology of Kuban State Medical University, Krasnodar, Russia

Alexandr Kulikov, Belgorod State University

Postgraduate student of the Department of Pharmacology of Medical institute of Belgorod State University,
Belgorod, Russia

Dmitry V. Vinakov, Belgorod State University

Postgraduate student of the Department of Pharmacology of Medical institute of Belgorod State University, Belgorod, Russia

Konstantin Suzdalev, Southern Federal University

PhD of Chemical Sciences, assistant professor of the Department of chemistry of natural and macromolecular compounds, Southern Federal University, Rostov-on-Don, Russia

Pavel Alexandrovich Galenko-Yaroshevsky, Kuban State Medical University

Corresponding member of Russian Academy of Sciences, Doctor of Medicine, Prof. of of Kuban State Medical University, Krasnodar, Russia 

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Опубликован

10.08.2016

Как цитировать

Bogus SK, Kulikov A, Vinakov DV, Suzdalev K, Galenko-Yaroshevsky PA (2016) Anticholinergic activity and pharmacokinetic parameters of agent SS-68 with properties of class iii antiarrhythmic drugs. Research Results in Pharmacology: 3–10

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