scholarly journals Morpho-functional indicators changes of rats’ myocardium in experimental doxorubicin-induced chronic heart failure and its pharmacological modulation with new 4-amino-1,2,4-triazole derivative

Pharmacia ◽  
2021 ◽  
Vol 68 (4) ◽  
pp. 919-925
Author(s):  
Pavlo G. Bak ◽  
Igor F. Belenichev ◽  
Liudmyla I. Kucherenko ◽  
Andrei V. Abramov ◽  
Olga V. Khromylоva
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Drug Candidate ◽  
Programming Environment ◽  
Triazole Derivative ◽  
Metoprolol Succinate ◽  
Reference Drug ◽  
Pharmacological Modulation ◽  
Automatic Mode ◽  
Cardioprotective Action

Bromide 1 - (β-phenylethyl)-4-amino-1,2,4-triazolium (Hypertril) has the properties of a beta-blocker and of NO-mimetic, is assigned to the IV class of toxicity. All these effects make Hypertril a promising drug for the treatment of cardiovascular diseases. The aim of this paper was to study the cardioprotective action of Hypertril in terms of the effect on the morpho-functional parameters of the myocardium in rats with experimental chronic heart failure (CHF). CHF was modeled on 80 white outbred rats weighing 190–220g by administering doxorubicin at a cumulative dose of 15 mg/kg. Hypertril and the reference drug metoprolol succinate were administered within 30 days after CHF modeling, intragastrically at doses of 3.5 mg/kg and 15 mg/kg. Morphometric analysis of the cellular structure of the myocardium was carried out on an Axioskop microscope (Zeiss, Germany), in an automatic mode using a macro program developed in a specialized programming environment VIDAS-2.5 (Kontron Elektronik, Germany). The administration of Hypertril to animals with CHF led to an increase in the density of nuclei of cardiomyocytes, the area of myocardiocyte nuclei, an increase in the nuclear cytoplasmic ratio and an increase in the concentration of RNA in the nuclei and cytoplasm of cardiomyocytes compared with the group of untreated animals, which indicated the presence of a pronounced cardioprotective effect in the drug candidate. In terms of such indicators as the density of surviving cardiomyocytes and the content of RNA in them, the nuclear-cytoplasmic ratio of Hypertril is significantly (p < 0.05) superior to metoprolol.

Abstract 3295: De-induction of the Maladaptive Fetal Gene Program During Chronic Monotherapy with Metoprolol Succinate is Retained Following Withdrawal of Therapy in Dogs with Chronic Heart Failure

Circulation ◽  
2007 ◽  
Vol 116 (suppl_16) ◽  
Author(s):  
Rasha Bazari ◽  
Sharad Rastogi ◽  
Valerio Zaca ◽  
Sidney Goldstein ◽  
Hani N Sabbah
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Mrna Expression ◽  
Natriuretic Peptide ◽  
Left Ventricular ◽  
Lv Function ◽  
Metoprolol Succinate ◽  
Myosin Heavy Chain Isoform ◽  
Chronic Therapy ◽  
Lv Remodeling

Background: Chronic therapy with extended release metoprolol succinate (MET), a selective β1 adrenergic receptor blocker, improves left ventricular (LV) function and attenuates global LV remodeling in dogs with chronic heart failure (HF). We previously showed that chronic therapy with β-blockade results in de-induction of the fetal gene program (FGP) in LV myocardium of dogs with HF. In this study, we tested the hypothesis that in dogs with HF withdrawal of chronic MET does not lead to re-induction of FGP. Methods: Studies were performed in 17 intracoronary microembolization-induced HF dogs randomized to 3 months oral therapy with MET (100 mg, once daily, n=11) or no therapy at all (Controls, n=6). In dogs randomized to MET, 6 were sacrificed after 3 months of therapy and in the remaining 5, MET was withdrawn after 3 months of therapy and dogs were observed for 6 weeks after withdrawal of MET (MET-W) and then sacrificed. LV tissue was also obtained from 6 normal (NL) dogs for comparison. mRNA expression of the FGP genes namely, atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), sarcoplasmic reticulum calcium ATPase (CAA), cardiac β-1 adren-ergic receptor (AR) and α-myosin heavy chain isoform (α-MHC) was measured using reverse transcriptase polymerase chain reaction (RT-PCR) and bands were quantified in densitometric units (du). Results: In Controls, mRNA expression of ANP and BNP increased and expression of CAA, β 1-AR and α-MHC decreased. Treatment with MET decreased expression of ANP and BNP and increased expression of CAA, β 1-AR and α-MHC. Except for α-MHC, the improvement in FGP seen during MET treatment was preserved in MET-W dogs. Conclusions: Withdrawal of MET is associated with sustained de-induction of the FGP in LV myocardium of dogs with HF. This observation supports the concept that chronic β-blockade therapy in HF confers lasting reversal of LV remodeling and molecular recovery of the failing myocardium.

Multi-centre Crossover Comparison of Carvedilol, Metoprolol Succinate and Bisoprolol in Patients with Chronic Heart Failure

2009 ◽  
Vol 18 ◽  
pp. S181
Author(s):  
A. Jabbour ◽  
P.S. Macdonald ◽  
A.M. Keogh ◽  
E. Kotlyar ◽  
S. Mellemkjaer ◽  
...  
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Metoprolol Succinate ◽  
Crossover Comparison

scholarly journals A modern view of the place of b-blockers in the treatmentof cardiovascular disease: the choice of drug within a class is crucial

2015 ◽  
Vol 12 (4) ◽  
pp. 69-74
Author(s):  
O D Ostroumova ◽  
V M Fomina ◽  
E A Smolyarchuk
Keyword(s):  
Heart Failure ◽  
Cardiovascular Disease ◽  
Coronary Heart Disease ◽  
Heart Disease ◽  
Cardiovascular Diseases ◽  
Chronic Heart Failure ◽  
Arterial Hypertension ◽  
Clinical Studies ◽  
Metoprolol Succinate ◽  
Selection Of

In the article discusses questions of application of b-blockers (b-AB) for the treatment of arterial hypertension, coronary heart disease, chronic heart failure. The data from modern Russian and European recommendations about the place of b-AB in the treatment of cardiovascular diseases. Analyzed in detail the selection of b-AB inside the class from the standpoint of pharmacokinetics, selectivity, study in clinical studies. Data about efficiency and safety of application of metoprolol succinate for the treatment of arterial hypertension, coronary heart disease, chronic heart failure.

scholarly journals Carvedilol Compared With Metoprolol Succinate in the Treatment and Prognosis of Patients With Stable Chronic Heart Failure

2015 ◽  
Vol 8 (5) ◽  
pp. 887-896 ◽  
Author(s):  
Hanna Fröhlich ◽  
Jingting Zhao ◽  
Tobias Täger ◽  
Rita Cebola ◽  
Dieter Schellberg ◽  
...  
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Metoprolol Succinate

scholarly journals Bisoprolol compared with carvedilol and metoprolol succinate in the treatment of patients with chronic heart failure

2017 ◽  
Vol 106 (9) ◽  
pp. 711-721 ◽  
Author(s):  
Hanna Fröhlich ◽  
Lorella Torres ◽  
Tobias Täger ◽  
Dieter Schellberg ◽  
Anna Corletto ◽  
...  
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Metoprolol Succinate

scholarly journals EFFECT OF FATTY OIL EXTRACT FROM SEEDS OF NIGELLA DAMASCENA L. ON LIPID SPECTRUM IN RATS WITH SIMULATED DYSLIPIDEMIA

2019 ◽  
Vol 7 (2) ◽  
pp. 90-96
Author(s):  
M. P. Efremova
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Blood Serum ◽  
Male Rats ◽  
Laboratory Animals ◽  
Reference Drug ◽  
Fatty Oil ◽  
Oil Extract ◽  
Nigella Damascena ◽  
Lipid Spectrum

The aim of the study is to determine a lipid spectrum of blood plasma and liver in rats in with simulated dyslipidemia against the background of the administration of the fatty oil extract from the seeds of Nigella damascena L.Materials and methods. Laboratory animals – Wistar male rats – were used in the work. To study the hypolipidemic activity, such models as acute Tween, subchronic vitamin-D2 models and a model of chronic heart failure were used. The identifiable parameters were the concentration of cholesterol and triglycerides in the blood serum and liver, as well as the concentration of atherogenic and non-atherogenic lipoproteins in the blood serum, and the atherogenic coefficient.Results. As a result of the study, it was found out that a course administration of the fatty oil extract from the seeds of Nigella damascena L. against the background of simulated chronic heart failure (CHF) by the right ventricular type, normalizes the lipid spectrum of the experimental animals’ blood serum, causing an increase in the concentration of high-density (non-atherogenic) lipoproteins, and reduces the concentration of low-density (atherogenic) lipoproteins. A single administration of the fatty oil extract from the seeds of Nigella damascena L. promotes the correction of lipid metabolism disorders under the conditions of acute Tween lipidopathy, while the direction of the object being studied reduces the concentration of cholesterol and triglycerides in the liver and blood serum under the conditions of subchronic dyslipidemia. At the same time, the effect of the use of the fatty oil extract from the seeds of Nigella damascena L. was not inferior to “Omaсor”, the reference drug.Conclusion. The possibility of using a fatty oil extract from the seeds of Nigella damascena L. for preventive and therapeutic aims in cardiovascular diseases has been established.

scholarly journals Treatment optimisation in patients with functional Class II chronic heart failure and arterial hypertension

2012 ◽  
Vol 11 (2) ◽  
pp. 29-34
Author(s):  
S. G. Kanorskyi ◽  
V. G. Tregubov ◽  
V. M. Pokrovskyi ◽  
N. A. Bulozhenko
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Arterial Hypertension ◽  
Left Ventricular ◽  
Functional Class ◽  
Stage Ii ◽  
Metoprolol Succinate ◽  
Nyha Classification ◽  
Group I ◽  
Group Ii

Aim.To identify the optimal treatment tactics in patients with Functional Class (FC) II chronic heart failure (CHF) (NYHA classification) and essential arterial hypertension (EAH), via investigating the effects of different medication classes on regulatory and adaptive status (RAS). Material and methods.The study included 100 patients with FC II CHF and Stage II EAH, who were randomised into 2 groups. Group I included 53 patients (mean age 52,9±2,3 years) receiving metoprolol succinate (mean dose 97,3±9,5 mg/d). Group II included 47 patients (mean age 57,5±1,3 years) administered quinapril (mean dose 24,7±6,3 mg/d). At baseline and after 6 months of therapy, the following procedures were performed: treadmill test with VO2max assessment; echocardiography; 24-hour blood pressure monitoring; N-terminal pro-brain natriuretic peptide (NT-proBNP) level measurement; and cardio-respiratory synchronism test. Results.While both medications improved left ventricular (LV) diastolic function, only quinapril demonstrated beneficial effects on LV structure, geometry, and systolic function. Only in Group II, exercise capacity and VO2max increased, RAS improved, and NT-proBNP levels decreased to a greater extent. Conclusion.Quinapril was more effective than metoprolol succinate in the treatment of patients with FC II CHF and Stage II EAH.

scholarly journals TREATMENT OF CHRONIC HEART FAILURE: FOCUS ON METOPROLOL SUCCINATE

2012 ◽  
Vol 8 (6) ◽  
pp. 798-803
Author(s):  
O. D. Ostroumova ◽  
G. N. Shchukina ◽  
V. M. Fomina
Keyword(s):  
Heart Failure ◽  
Chronic Heart Failure ◽  
Metoprolol Succinate
Sign in / Sign up

Export Citation Format

Share Document