Combined action of antiarrhythmic agents

Gendenshtein, É. I.; Kostin, Ya. V.; Balashov, V. P.; Олейников, В Э

doi:10.1007/bf00840193

Cited by 3 publications

(3 citation statements)

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“…Bearing in mind that combined administration can provide a reserve for elevation of drug efficiency (potentiation) [2], we examined antiarrhythmic activity of a combination of suphan and lidocaine taken in subthreshold (half-effective) doses equal to 22.5 and 1.4 mg/kg, respectively. In some experiments, suphan injection followed after 1-2 min by lidocaine, while in others, this order was reversed, It was found that the combination suphan+lidocaine exhibited no considerable antiarrhythmic activity (EOA and RPA occurred in 43% of cases), however, it produced a pronounced antifibrillatory effect (VF were noted only in 14% animals).…”

Section: Resultsmentioning

confidence: 99%

“…This system includes phosphatidylcholine hydrolysis to diacylglycerols and phosphorylcholine and activation of pro-V. P. Komissarenko Institute of Endocrinology and Metabolism, Ukrainian Academy of Medical Sciences, Kiev tein kinase C in different cell fractions [2,11,12]. This mechanisms of signal transduction is most typical for proliferative stimuli.…”

Section: Autostimulation Of Prolactinmentioning

confidence: 99%

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Effect of suphan, lidocaine, and their combination on early occlusion and reperfusion arrhythmias in cats

et al. 1997

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It is shown that the nonglycoside cardiotonic drug suphan exhibits antiarrhythmic and antifibfillatory activity, although less pronounced than that of lidocaine. When lidocaine was administered after suphan, the antifibrillatory effects of both preparations increased. Key Words: suphan; #docaine; arrhythmias; treatmentIt is established that the most common variant of ischemic heart disease, angina pectoris, arises from regional transitory insufficiency characterized by consecutive periods of ischemia and restoration of circulation, i.e., reperfusion. The use of intense perfusion and oxygenation of the myocardium (aortocoronary bypass, coronary angioplastics, fibrinolysis, etc.) can also cause postischemic reperfusion syndrome. This is usually accompanied by ominous cardiac rhythm disturbances, reperfusion arrhythmias, such as ventricular fibrillation (VF), acute heart failure, etc. [5].Recent investigation showed that the nonglycoside cardiotonic drug suphan (N-succine-dl-tryptophan dipotassium salt) exerts antihypoxic and antianginal effects in animals [4], and therapeutic effect in patients with ischemic heart disease complicated by congestive circulatory failure.The aim of the present study was to compare antiarrhythmic and antifibrillatory activity of suphan with that of lidocaine and to evaluate the efficiency of their combination in modeled early occlusion (EOA) and reperfusion (RPA) arrhythmia, including VF.Department of Pharmacology, Kuban Medical Academy, Krasnodar MATERIALS AND METHODSExperiments were carried out on 140 male Wistar rats (0.155-0.210 kg) and 75 cats (2.6-3.4 kg).Acute toxicity (mean lethal dose, LDs0 ) was determined by injecting the preparations intravenously to rats as described previously [6].In cats narcotized with Nembutal (40 mg/kg, intraperitoneally) and artificially ventilated, the chest was opened and occlusion (30 rain) and reperfusion (10 min) of the descendent branch of the left coronary artery at the level of lower edge of the auricula was performed [3]. The test preparations and their combinations were slowly injected intravenously in isotoxic doses (5, 10, 15, 20, and 30% of LDs0) 5-7 min prior to occlusion of the coronary artery. For evaluation of antiarrhythmic activity, the occurrences of EOA, RPA, and VF were recorded using an EKIT-04 electrocardiograph.The data were processed statistically using )~2 test [ 1 ]. RESULTSAs seen from Table 1, in the control series coronary occlusion led to EOA in 60% of cases, while RPA

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Section: Resultsmentioning

confidence: 99%

Section: Autostimulation Of Prolactinmentioning

confidence: 99%

Effect of suphan, lidocaine, and their combination on early occlusion and reperfusion arrhythmias in cats

et al. 1997

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“…1-(2-ethoxyethyl)-4-ethynylpiperidin-4-ol was synthesized as hydrochloride by the Favorskii reaction from 1-(2-ethoxyethyl)-4-piperidone according to the well-known procedure [16]. For the purpose of new ionic compounds synthesis it was transferred into the form of a base and then undergone the process of alkylation with alkyl halides.…”

Section: Synthesis Of the Ionic Compounds Based On N-ethoxyethylpmentioning

confidence: 99%

N-ethoxyethylpiperidine, Trimecaine and Piromecaine Based Ionic Compounds: Synthesis and Prediction of Biological Activity

Zolotareva¹,

Basharimova²,

Bayazit³

et al. 2017

IJCEA

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Abstract-Herein we report on the synthesis of new ionic compounds based on N-ethoxyethylpiperidine, trimecaine and piromecaine, obtained via N-alkylation with alkyl halides. The combination of piperidine ring, secondary amine group, trimecaine and piromecaine in form of a base with different alkyl radicals bring to molecule new biological activity and/or reduce toxic effects of parent compounds. The potential pharmacological activity and potential toxic effects of the obtained compounds were predicted with PASS online service (Prediction of Activity Spectra for Substances) showing cardiotonic, antiarrhythmic and spasmolytic potential activities. The dependence of the potential activity on the nature of substituent was compared. These novel ionic compounds can be applied for synthesis of ionic compounds and drug candidates.

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Effect of biotechnological cytochromec on the early postocclusion and reperfusion arrhythmias

et al. 1999

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Biotechnological cytochrome c showed a lower antiarrhythmic activity in cats with acute occlusion and reperfusion arrhythmias than trimecaine, verapamil, and quaternidine but a higher activity than anapriline. Under experimental conditions, cytochrome c potentiated the antiarrhythmic effect of trimecaine and quaternidine. Key Words: cytochrome c; occlusion and reperfusion arrhythmias; antiarrhythmic drugsCytochrome c (Cc) is widely used for correction of tissue hypoxia in cardiology and other fields of clinical medicine [1,8,10]. Biotechnological methods for obtaining Cc developed at the Sintez-Belok Institute [4] cancel the limitations for its application. Biotechnological Cc, like its analog of animal origin, has a favorable effect on acute myocardial ischemia, improves cardiodynamics, and promotes a decrease in the size of necrotic zone [5,10]. Cc possesses an antiarrhythmic activity [2], but its place in combined therapy of heart rhythm disorders complicating the acute stage of myocardial infarction is still unclear.We compared the antiarrhythmic activity of Cc with that of conventional antiarrhythmics of different classes and evaluated the effectiveness of their combinations in cats with occlusion and reperfusion arrhythmias. MATERIALS AND METHODSExperiments were carried out on 140 cats of both sexes weighing 2.5-3.5 kg. The animals were narcotized with sodium thiopental (40 mg/kg intraperitoneally). Acute occlusion and reperfusion arrhythmias were induced as described previously [11]. The duration of coronary artery occlusion was 30 min. The occurrence of occlusion Department ot Pharmacology, Mordovian State University, Saransk and reperfusion arrhythmias (extrasystole and tachycardia) and ventricular fibrillations (VF) were evaluated. Antiarrhythmic activities of Cc, sodium channel blocker lrimecaine, 13-adrenoblocker anapriline (obsidan), polarizing potassium flow blocker quaternidine, and calcium antagonism verapamil (finoptin) were compared. RESULTSIn the control series, all animals developed early occlusion arrhythmias after high ligation of the coronary artery; 28% animals developed lethal VF. During coronary reperfusion the probability of VF markedly increased and reached 65% (Table 1).Cytochrome c in doses of 5-20 mg/kg showed a pronounced antiarrhythmic activity, decreasing the probability of occlusion arrhythmias and reperfusion VF. Its antiarrhythmic effect was virtually dose-independent. Trimecaine (30 mg/kg) and verapamil (0.5-1.0 mg/kg) exerted stronger antiarrhythmic effects than Cc under the experimental conditions, the maximum dose of verapamil impaired cardiac conduction in all experiments. Quaternidine showed the highest antiarrhythmic activity; in a dose of 4 mg/kg it prevented early occlusion and reperfusion arrhythmias in all experiments without causing negative changes_ in the ECG. Anapriline was the lea.st effective and in the studied doses displayed no antifibrillation activity.

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Combined action of antiarrhythmic agents

Cited by 3 publications

References 3 publications

Effect of suphan, lidocaine, and their combination on early occlusion and reperfusion arrhythmias in cats

Effect of suphan, lidocaine, and their combination on early occlusion and reperfusion arrhythmias in cats

N-ethoxyethylpiperidine, Trimecaine and Piromecaine Based Ionic Compounds: Synthesis and Prediction of Biological Activity

Effect of biotechnological cytochromec on the early postocclusion and reperfusion arrhythmias

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