scholarly journals Blocker, angiotensin II receptor olmesartan to interrupt cardiovascular continuum: vesselsand cardioprotective, anti-atherosclerotic and metabolic pleiotropic effects (part 2)

2015 ◽  
Vol 6 (1) ◽  
pp. 65-74
Author(s):  
M. G Bubnova

The article provides an overview of pleiotropic activity and clinical efficacy of one of the representatives of the class of angiotensin receptor blockers II - olmesartan medoxomil. Analyzed is a wide range of established in experimental and clinical studies and vasoconstriction, cardioprotective, anti-atherogenic, anti-inflammatory and other effects of olmesartan medoxomil. Given clinical studies evaluating anti-atherosclerotic effects of this drug.

2014 ◽  
Vol 11 (4) ◽  
pp. 84-86
Author(s):  
Ye S Minina ◽  
B R Khadzhieva

Sartans are safety and effective class of anti-hypertensives nowadays. Sartans are the most effective inpatients suffering from arterial hypertension. Their efficiency is determined by the association of Angiotensin II type 1 receptor. Candesartan and azilsartan are themost powerful and approved angiotensin receptor blockers. Candesartan in comparison with azilsartan has wide proposed spectrum of clinical use. Azilsartan is indicated for the treatment of arterial hypertension. In terms of efficiency and safety we showed these sartans.


Hypertension ◽  
2019 ◽  
Vol 74 (6) ◽  
pp. 1275-1278 ◽  
Author(s):  
Pradeep Moon Gunasekaran ◽  
Glenn M. Chertow ◽  
Vivek Bhalla ◽  
James Brian Byrd

Losartan was the ninth most prescribed drug in the United States in 2016, and several other angiotensin-II receptor blockers (ARBs) are widely prescribed. Since July 2018, >2 dozen specific ARB products have been recalled owing to the presence of potentially carcinogenic nitrosamine impurities in selected lots. As is the case with all U.S. drug recalls, the ARB recalls have been voluntary on the part of the companies involved. In April 2019, the Food and Drug Administration categorized marketed ARB products with respect to nitrosamine impurities: (1) not present, (2) to be determined with no prior lots removed from the market (TBD), or (3) to be determined in the context of prior lots having been removed from the market (TBD*). The data were structured as hundreds of rows of products. Owing to the complexity of these data, more than a year into the recalls, it remains difficult for clinicians to understand which ARB products are free of impurities.


Synthesis ◽  
2021 ◽  
Author(s):  
Masahiko Seki ◽  
Yusuke Takahashi

Highly convergent synthesis of Angiotensin II receptor blockers has been accomplished by means of late stage C-H arylation using functionalized aryl bromides. C-H arylation of phenyl tetrazole with aryl bromide carrying methyl 2-ethoxy-benzimidazole-7-carboxylate unexpectedly provided coupling product where ethyl group was migrated from oxygen to nitrogen atom. The <i>O</i>- to <i>N</i>-ethyl migration was completely suppressed by the use of <i>N</i>-pivaloyl-L-valine rather than the combined use of triphenyl phosphine and sodium mesitylenesulfonate to result in the preferential formation of a key intermediate of candesartan cilexetil. In contrast, when an aryl bromide having ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate was employed, the C-H arylation proceeded smoothly to provide a late stage intermediate which was rapidly led to olmesartan medoxomil in 3 steps.


Trials ◽  
2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Carinna Hockham ◽  
Sradha Kotwal ◽  
Arlen Wilcox ◽  
Abhinav Bassi ◽  
James McGree ◽  
...  

Abstract Background SARS-CoV-2 binds to membrane-bound angiotensin-converting enzyme 2 (ACE2) which may result in downregulation of membrane-bound ACE2. ACE2 is a key regulator of the renin-angiotensin system (RAS) and is responsible for degrading angiotensin II and thereby counteracting its pro-inflammatory, pro-fibrotic effects mediated through the angiotensin II type 1 receptor (AT1R). As AT1R is directly blocked by angiotensin receptor blockers (ARBs), these agents may offer a safe, low-cost solution for reducing COVID-19 respiratory outcomes. Methods and discussion CLARITY is a pragmatic, adaptive, two-arm, multi-centre, comparative effectiveness phase III randomised controlled trial that examines whether ARBs reduce COVID-19 severity among high-risk patients. Recruiting in India and Australia, the trial will compare treatment with a maximum tolerated daily dose of an ARB to standard of care. Treatment allocation is blinded in India but open-label in Australia due to interruptions to placebo supply in the latter. The primary endpoint is a 7-point ordinal scale of clinical states, ranging from no limitation of activities (category 1) to death (category 7), assessed on day 14. Secondary outcomes include the 7-point scale assessed at day 28 and 28- and 90-day mortality. The design adapts the sample size based on accumulating data via frequent interim analyses and the use of predictive probability to determine whether the current sample size is sufficient or continuing accrual would be futile. The trial commenced recruitment on 18 August 2020. Trial registration ClinicalTrials.gov, NCT04394117. Registered on 19 May 2020. Clinical Trial Registry of India: CTRI/2020/07/026831)


2014 ◽  
Vol 11 (1) ◽  
pp. 34-39
Author(s):  
A I Martynov ◽  
I V Urlaeva ◽  
E V Akatova ◽  
O P Nikolin

The arterial hypertension takes the basic place among the cardiovascular diseases which are a principal cause of death and invalidity. For today the basic group for treatment of an arterial hypertensia remain angiotensin-converting enzyme inhibitors (ACEi). However, according to numerous researches, angiotensin II receptor inhibitors by the efficiency are equal with ACEi, but have the best profile of shipping and provide higher adherence to therapy. One of highly effective, well studied, with considerable demonstrative base of preparations irbesartan.


2014 ◽  
Vol 5 (3-4) ◽  
pp. 32-40
Author(s):  
M. G Bubnova

The article provides an overview of the efficacy and tolerability of one of the representatives of the class angiotensin receptor blockers II - olmesartan medoxomil (Kardosal). Analyzed are the characteristics and pharmacological activity of olmesartan medoxomil antihypertensive monotherapy, in combination with other antihypertensive drugs, in different groups of patients. The article describes the renal protective properties of the drug, its safety profile. It also discusses the reasons for poor adherence therapy in patients with arterial hypertension.


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