scholarly journals Imidazoline receptors agonists: possible mechanisms of endothelioprotection

2018 ◽  
Vol 4 (2) ◽  
pp. 11-19 ◽  
Author(s):  
Vladislav O. Soldatov ◽  
Elena A. Shmykova ◽  
Marina A. Pershina ◽  
Andrey O. Ksenofontov ◽  
Yaroslav M. Zamitsky ◽  
...  

Imidazoline receptor agonists are one of the groups of contemporary antihypertensive drugs with the pleiotropic cardiovascular effects. In this review, the historical, physiological, pathophysiological aspects concerning imidazoline receptor agonists and possible mechanisms for their participation in endothelioprotection were considered. Illuminated the molecular biology of each subtype of imidazoline receptors and their significance in the pharmacological correction of cardiovascular disease. IR type 1 are localized in the brain nucleus, carrying out the descending tonic control of sympathetic activation, as well as in the endothelial cells of the vessels and kidneys. Their activation leads to a decrease in blood pressure, slowing the remodeling of the vascular wall and increasing sodium nares. IR type 2 is expressed predominantly in the adrenal gland, fat and muscle tissues. The physiological effects of their stimulation are associated with an increase in glucose utilization by peripheral tissues. IR type 3 are mainly present in pancreatic cells and are associated with the regulation of insulin secretion. Their stimulation leads to an increase in insulin liberation. Thus, IR agonists are able to improve endothelial function through various mechanisms, including blood pressure reduction, improvement in metabolic profile, and direct positive effects on the vascular wall. Current information on the pharmacological effects of this group compounds allows us to conclude that they are a promising group for correcting endothelial dysfunction and complications associated with it.

2019 ◽  
Vol 6 (5) ◽  
pp. 1688
Author(s):  
Sadanand Shetty ◽  
Anil Bhoraskar ◽  
J. C. Mohan ◽  
Deodatta Chafekar ◽  
K. Tripathi ◽  
...  

Hypertension, often referred to as ‘The silent killer’, is christened so, as it is seldom preceded by any warning signs or symptoms. With the new ACC/AHA guidelines lowering the Blood Pressure (BP) threshold values, it has resulted in a 140% relative increase in the hypertension prevalence in India, which is 3 times higher than that of in United States. Imidazoline receptor agonists control BP effectively with minimal adverse effects of sedation and mental depression that are usually associated with centrally acting antihypertensives. While having a low affinity to the α2-adrenergic receptors, these new generation centrally acting antihypertensive agents are highly selective for imidazoline receptor. Moxonidine, a second-generation centrally acting antihypertensive drug having selective agonist activity on imidazoline I1 receptors and minor activity on imidazoline α2 adrenoceptors, reduces the activity of Sympathetic Nervous System (SNS) by activating I1 imidazoline receptors in Rostral Ventrolateral Medulla (RVLM). Studies of moxonidine have shown equal effectiveness in lowering BP like other well-established antihypertensive drugs such as nifedipine, atenolol or angiotensin-converting enzyme inhibitors, with minimal adverse events. At doses of 0.2-0.6 mg, moxonidine induces satisfactory BP reduction in patients with mild-to-moderate essential hypertension. In patients with mild-to-moderate hypertension, moxonidine (0.2-0.4 mg o.d.) significantly decreased Systolic Blood Pressure/Diastolic Blood Pressure (SBP/DBP), respectively, by 19.5/11.6 mmHg. In obese, non-controlled hypertensive patients, there is a 14% and 13.5% reduction in the mean SBP and DBP, respectively, from the baseline value after moxonidine treatment and during the follow-up with an additional reduction in body weight, plasma leptin levels and Body Mass Index (BMI) (p<0.01). Thus, moxonidine could be considered as a therapeutic option in obese patients with metabolic syndrome.


2016 ◽  
pp. 76-84
Author(s):  
Khoa Bao Chau Thai ◽  
Thi Hong Phuong Vo

Background: Hypertension is a common condition in the world as well as in Viet Nam. If hypertension isn’t treated well, it can cause many serious complications. Controlling target blood pressure will bring positive effects on reducing mortality rate and also disabilities caused by diseases related to hypertension. Objectives: (1) Analyzing the use of medicines in treating hypertension. (2) Evaluating the effects of medicine usage in treating hypertension at the hospital of Hue University of Medicine and Pharmacy. Materials and methods: 388 patients were diagnosed as having hypertension with inpatient care at the Cardiovascular Department of Hue University of Medicine and Pharmacy’s hospital, using cross-sectional descriptive study methods. Results: All antihypertensive drugs in the research were contained in the antihypertensive list recommended by Vietnamese Society of Cardiology. Angiotensin converting enzyme inhibitor and calcium channel blocker were the two most popular drug groups (96.6% and 71.4%, respectively). The rate of using multi-therapy regimens was higher than the rate of using uni-therapy regimens in both initial therapies (64.7%>35.3%) and final therapies (61.9%>38.1%). The rate of patients having interactions between antihypertensive drugs and the other kinds of drugs was 7.5%. The rate of patients having reasonable prescriptions was 84.3%. Evaluating the effects of medicine usage in treatments showed that the rate of patients reaching target blood pressure before leaving the hospital was 67.3%. Most patients were evaluated as having good prognosis after treatment, up to 81.7%. Conclusions: All antihypertensive drugs in the research were contained in the antihypertensive list recommended by Vietnamese Society of Cardiology. The rate of using multi-therapy regimens was higher than the rate of using uni-therapy regimens. The rate of drug interactions was quite low; most patients were evaluated as having good prognosis after treatment. Key words: hypertension, antihypertensive drugs.


2016 ◽  
Vol 13 (2) ◽  
pp. 17-23
Author(s):  
O D Ostroumova ◽  
A I Kochetkov ◽  
M V Lopukhina

The article discusses the factors that increase the arterial stiffness: the blood pressure, atherosclerosis, smoking, diabetes, age. Given evidence that pulse wave velocity and a number of other indicators that reflect the state of the vascular wall, are markers for increased risk of cardiovascular complications and mortality. The influence of antihypertensive drugs of different groups on the stiffness of the vascular wall, with particular attention paid to the effects of drugs from group of diuretics. We discuss possible mechanisms of the influence of indapamide retard on the elastic properties of vessels. It is emphasized that the influence on the stiffness of the arteries of different antigipertenzivny medicines, even belong to the same class, is different, due to differences in pharmacokinetic properties.


2021 ◽  
Vol 29 (1) ◽  
pp. 62-66
Author(s):  
D.S. Tratsiak ◽  
◽  
K.A. Abdin ◽  
A.A. Makarov ◽  
A.P. Trukhan ◽  
...  

Objective. To determine the possibility of using automatic plasmapheresis in patients with COVID-19- associated bilateral polysegmental pneumonia. Methods. The treatment of three patients with COVID-19-associated pneumonia with application of the Autopheresis-C™ automatic plasmapheresis machine (the USA) has been analyzed. The patients’ age was 47. 49 and 55 years. The patients’ case histories included factors aggravating the course of pneumonia (diabetes mellitus, chronic cardiovascular pathology with heart failure, obesity). The condition of all patients was severe. The effectiveness estimation of the given technique was carried out 6 hours after the manipulation and included a general clinical blood test, a biochemical blood test, hemodynamic parameters, and objective data. Results. After the first application of automatic plasmapheresis, all patients occurred a decrease in temperature and the level of respiratory failure, which was accompanied by an increase in hemoglobin saturation; a decrease in the severity of dyspnea was also reported, which was the reason for the changing patient position from prone to supine. All patients had a blood pressure reduction. Positive changes in the hemodynamic situation were the basis for reducing the dosage of antihypertensive drugs. Along with this, in the course of manipulation, a gradual decrease in the severity of tachycardia was noted in all patients: a reduction of heart rate was recorded. On the second day after the manipulation, the main blood parameters (leukocytosis, c-reactive protein) decreased. The observed positive effects contributed to the early transfer (by 10-15 days) of patients from the intensive care unit to the general somatic departments. Conclusion. The early inclusion of automatic plasmapheresis in the complex therapy of patients with COVID-19- associated bilateral polysegmental pneumonia leads to the stabilization of hemodynamic parameters, decline of the severity of respiratory failure, which made it possible to avoid the mechanical ventilation. What this paper adds For the first time, the clinical effectiveness of the method of automatic plasmapheresis in the framework of the complex therapy of COVID-19- associated polysegmental pneumonia is shown, which is expressed in a decrease in the manifestations of functional and metabolic disorders of vital systems for maintaining homeostasis. It was found that the inclusion of this technology in the complex therapy contributed to the stabilization of respiratory and hemodynamic parameters, which made it possible to avoid the mechanical ventilation.


2015 ◽  
Vol 38 (6) ◽  
pp. 394 ◽  
Author(s):  
Ernesto L Schiffrin

This review summarizes my lecture for the 2015 Distinguished Scientist Award from the Canadian Society of Clinical Investigation, and is based mainly on studies in my laboratory on the mechanisms of remodelling of small arteries in experimental animal and human hypertension and on treatments that lower blood pressure and improve structure and function of resistance vessels. Small resistance arteries undergo either inward eutrophic or hypertrophic remodelling, which raises blood pressure and impairs tissue perfusion. These vascular changes are corrected by some antihypertensive drugs, which may lead to improved outcomes. Vasoconstriction, growth, oxidative stress and inflammation are some of the mechanisms, within the vascular wall, that can be beneficially affected by antihypertensive agents. These antihypertensive-sensitive mechanisms are reviewed in this review, together with the inflammatory and immune mechanisms that may participate in hypertension and associated cardiovascular injury. Molecular studies, based on this research, will hopefully identify novel diagnostic and therapeutic targets, which will improve our ability to prevent and treat hypertension and cardiovascular disease.


INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (05) ◽  
pp. 5-19
Author(s):  
S. R Pattan ◽  
◽  
A. O. Zanwar ◽  
N. B Wabale ◽  
U. B. Shetkar

The recommendation for first-line therapy for hypertension remains a beta blocker or diuretic given in a low dosage. A target blood pressure of less than 140/90 mm Hg is achieved in about 50 percent of patients treated with monotherapy; two or more agents from different pharmacological classes are often needed to achieve adequate blood pressure control. Single-dose combination antihypertension therapyis an important option that combines efficacy of blood pressure reduction and a low side effect profilewith convenient once-daily dosing to enhance compliance. Combination antihypertensives include combined agents from the following pharmacological classes: diuretics and potassium-sparing diuretics,beta blockers and diuretics, angiotensin-converting enzyme (ACE) inhibitors and diuretics, angiotensin-II antagonists and diuretics and calcium channel blockers and ACE inhibitors.


Author(s):  
Athanasia K. Papazafiropoulou ◽  
Elias Georgopoulos ◽  
Stavros Antonopoulos

Chronic kidney disease is a major problem of public health and is associated with increased cardiovascular mortality and morbidity. Its treatment includes multifactorial intervention: optimal blood pressure and intensive glycaemic control. There are many studies – clinical and experimental – demonstrating that classic and newer antidiabetic agents delay the progression of diabetic nephropathy. Glucagon-like-peptide-1 (GLP-1) receptor agonists and sodium-glucose co-transporters-2 (SGLT-2) inhibitors have renoprotective action. Furthermore, these antidiabetic agents have beneficial effects to the cardiovascular system, including weight loss and blood pressure reduction. Large, randomized, placebo-controlled outcome trials have showed that SGLT-2 inhibitors and GLP-1 receptor agonists are able to reduce cardiovascular events. Therefore, the present review aims to summarize the existing data regarding the effect of newer antidiabetic agents on kidney function and cardiovascular system.


2020 ◽  
Vol 16 (1) ◽  
pp. 30-36 ◽  
Author(s):  
Michail Natsis ◽  
Christina Antza ◽  
Ioannis Doundoulakis ◽  
Stella Stabouli ◽  
Vasilios Kotsis

Backround: The relationship between obesity and hypertension has been established in both adults and children. The combination of obesity, hypertension and other cardiovascular risk factors significantly increases the likelihood of adverse cardiovascular effects and raises concerns about aggressive treatment strategies. Objective: Despite the impressive elements which indicate an important role for excessive weight gain in increasing blood pressure, not all obese patients are hypertensive. A subgroup of obese people may not develop hypertension. Furthermore, masked hypertension occurs more common among obese patients, and body fat distribution has a major role in the development of hypertension. Methods: We conducted a research of the relevant literature regarding obesity-induced hypertension and possible treatment strategies. Results: Successful weight loss is correlated with blood pressure reduction and requires a multidisciplinary approach that includes personalized dietary interventions combined with regular exercise and cognitive behavioral therapy. Conclusion: Pharmacological therapy may be considered as part of a comprehensive obesity management strategy. More research and new treatment therapies are required in this field.


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