scholarly journals Complete Characterization of Degradation Byproducts of Olmesartan Acid, Degradation Pathway, and Ecotoxicity Assessment

2021 ◽  
Vol 11 (12) ◽  
pp. 5393
Author(s):  
Giovanni Luongo ◽  
Antonietta Siciliano ◽  
Giovanni Libralato ◽  
Marco Guida ◽  
Lorenzo Saviano ◽  
...  

Antihypertensive drugs are among the most prescribed drugs. Olmesartan acid, of the sartan class, belongs to a relatively new generation of antihypertensive drugs called angiotensin II receptor blockers. There are very few studies on the presence and fate of sartans in the environment, despite them being marketed in huge quantities, metabolized in low percentages, and detected in wastewater and water bodies. This paper presents a study on the less abundant and more polar fractions that have been neglected in previous studies, which led to the isolation by chromatographic methods of thirteen degradation byproducts (DPs), six of which are new, identified by nuclear magnetic resonance and mass spectrometry. A mechanism of degradation from the parent drug was proposed. The ecotoxicity of olmesartan acid and identified compounds was evaluated in Aliivibrio fischeri bacteria and Raphidocelis subcapitata algae to assess acute and chronic toxicity. For 75% of the DPs, acute and chronic exposure to the compounds, at concentrations of 5 mg/L, inhibited population growth in the algae and decreased bioluminescence in the bacteria.

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1769
Author(s):  
Giovanni Luongo ◽  
Antonietta Siciliano ◽  
Giovanni Libralato ◽  
Sara Serafini ◽  
Lorenzo Saviano ◽  
...  

The discovery of various sartans, which are among the most used antihypertensive drugs in the world, is increasingly frequent not only in wastewater but also in surface water and, in some cases, even in drinking or groundwater. In this paper, the degradation pathway of olmesartan acid, one of the most used sartans, was investigated by simulating the chlorination process normally used in a wastewater treatment plant to reduce similar emerging pollutants. The structures of nine isolated degradation byproducts (DPs), eight of which were isolated for the first time, were separated via chromatography column and HPLC methods, identified by combining nuclear magnetic resonance and mass spectrometry, and justified by a proposed mechanism of formation beginning from the parent drug. Ecotoxicity tests on olmesartan acid and its nine DPs showed that 50% of the investigated byproducts inhibited the target species Aliivibrio fischeri and Raphidocelis subcapitata, causing functional decreases of 18% and 53%, respectively.


2010 ◽  
Vol 6 (3) ◽  
pp. 33
Author(s):  
Robert J Petrella ◽  

It is widely recognised that hypertension is a major risk factor for the development of future cardiovascular (CV) events, which in turn are a major cause of morbidity and mortality. Blood pressure (BP) control with antihypertensive drugs has been shown to reduce the risk of CV events. Angiotensin-II receptor blockers (ARBs) are one such class of antihypertensive drugs and randomised controlled trials (RCTs) have shown ARB-based therapies to have effective BP-lowering properties. However, data obtained under these tightly controlled settings do not necessarily reflect actual experience in clinical practice. Real-life databases may offer alternative information that reflects an uncontrolled real-world setting and complements and expands on the findings of clinical trials. Recent analyses of practice-based real-life databases have shown ARB-based therapies to be associated with better persistence and adherence rates and with superior BP control than non-ARB-based therapies. Analyses of real-life databases also suggest that ARB-based therapies may be associated with a lower risk of CV events than other antihypertensive-drug-based therapies.


2022 ◽  
Vol 12 ◽  
Author(s):  
Yujiao Deng ◽  
Yuxiu Xie ◽  
Meng Wang ◽  
Peng Xu ◽  
Bajin Wei ◽  
...  

Background: Antihypertensive drugs might play a key role in the risk and poor prognosis of colorectal cancer. However, current epidemiologic evidence remains inconsistent. The aim of this study is to quantify the association between antihypertensive drugs and colorectal cancer.Methods: To identify available studies, we systematically searched electronic databases: PubMed, Web of Science, Embase, Cochrane Library. The risk estimates and their corresponding 95% confidence intervals (CIs) were collected and analyzed by using random-effects models. Heterogeneity test and sensitivity analysis were also performed.Results: Overall, 37 observational studies were included in this analysis (26 studies with cohort design, three studies with nested case-control design, and 8 studies with case-control design). Antihypertensive drugs did not present a significant effect on the risk or overall survival of patients with colorectal cancer [Risk ratio (RR) = 1.00, 95% CI: 0.95–1.04; Hazard ratio (HR) = 0.93, 95% CI: 0.84–1.02]. In the subgroup analysis, diuretics use was significantly associated with a worse overall survival of patients with colorectal cancer (HR = 1.27; 95% CI: 1.14–1.40). However, use of angiotensin-converting enzyme inhibitors/angiotensin II receptor blockers was associated with improved progression-free survival of patients who suffered from colorectal cancer (HR = 0.83; 95% CI: 0.72–0.95).Conclusion: Antihypertensive drug usage did not influence the risk and overall survival of patients with colorectal cancer in general. Further investigation reminded us that diuretics use might reduce the overall survival time in colorectal cancer patients, whereas those who took Angiotensin-converting enzyme inhibitors/angiotensin II receptor blockers had a longer progression-free survival.


2016 ◽  
Vol 13 (4) ◽  
pp. 47-55
Author(s):  
O D Ostroumova ◽  
I A Garelik ◽  
E A Karavashkina

This article discusses the definition, classification and pathogenetic mechanisms of cognitive functions in arterial hypertension. The authors discuss the capabilities of the different classes of antihypertensive drugs in correction of cognitive impairments and prevention of dementia. The authors also discuss the advantages of the angiotensin II receptor blockers in prevention of dementia and in their potential mechanisms of cerebral protection. The article describes in detail the possibilities of valsartan in correction of cognitive impairments associated with arterial hypertension, the advantages of valsartan in comparison with calcium antagonists and its unique neuroprotective mechanisms. We show our own results of the study concerning fixed-dose combination of valsartan and hydrochlorothiazide, and find out that this combination has high antihypertensive and cerebral protection (capacity to improve cognitive function) and effectiveness.


2018 ◽  
Vol 25 (3) ◽  
pp. 218-219
Author(s):  
Vitalina Petrenko ◽  
Anatoliy Kubyshkin ◽  
Irina Fomochkina ◽  
Natalia Kornienko ◽  
Alexander Kucherenko

2018 ◽  
Vol 25 (3) ◽  
pp. 213
Author(s):  
Vitalina Petrenko ◽  
Anatoliy Kubyshkin ◽  
Irina Fomochkina ◽  
Natalia Kornienko ◽  
Alexander Kucherenko

2017 ◽  
Vol 8 (2) ◽  
pp. 70
Author(s):  
Dimas Pramita Nugraha ◽  
Iwan Dwiprahasto ◽  
Jarir At Thobari

Hypertension is the second largest of the 10 diseases on an outpatient at a hospital in Indonesia. The poor complianceto therapy of hypertension is a major cause of uncontrolled blood pressure. The aim of this study is to determinecompliance antihypertension on patient at DR. Sardjito hospital Yogyakarta. This study was designed with aretrospective cohort study design using a database of participants claimed prescribing health insurance (ASKES) inthe DR. Sardjito hospital using antihypertensive drugs. Compliance measured with medication possession ratio (MPR).Data was analysed by chi- square and logistic regression statistic. From 8.011 patients, compliance of antihypertensivedrugs during the first year is 7,6%. Analysis for compliance showed that the type of antihypertensive diuretics aremore compliance compare with angiotensin II receptor blockers, ACE inhibitors, calcium channel blockers and betablockers. Combination therapy (20,7%) is more compliance than monotherapy ( 4,1%), as well as drugs administration1 time a day (8,2%) is more compliance than drug administration 2 times (2,5%) and 3 times a day (3%). Theproportion of compliance in antihypertensive users at DR. Sardjito hospital classified as less good. Compliancepattern indicates that therapy is not continuous, the longer the use of antihypertensive therapy, the higher thediscontinuous therapy.


2013 ◽  
Vol 10 (2) ◽  
pp. 53-56
Author(s):  
O D Ostroumova ◽  
A A Zykova ◽  
T A Polosova ◽  
O V Bondarets

The paper gives the data of Russian guidelines for the diagnosis and approaches to treating metabolic syndrome. It considers the choice of antihypertensive drugs in the treatment of hypertensive patients with metabolic syndrome. The benefits of angiotensin II receptor blockers are shown. The results of a number of trials evaluating the efficacy and safety of irbesartan used to manage arterial hypertension in metabolic syndrome are analyzed.


2015 ◽  
Vol 6 (2) ◽  
pp. 69-80
Author(s):  
M. G Bubnova

This article deals withthe overview of the pharmacological characteristics of one class of antihypertensive drugs - angiotensin II receptor antagonists (ARA II) and new member of this class - azilsartan medoxomil (Edarbi®).We have analyzed the antihypertensive efficacy of different ARA, as well as azilsartan medoxomil efficacyin case of monotherapy and in comparison with other ARA and angiotensin-converting enzyme inhibitorsamong different groups of patients.The article describes the pleiotropic effects of azilsartan medoxomil, discovered nowadays.


2015 ◽  
Vol 12 (3) ◽  
pp. 11-18
Author(s):  
M V Leonova ◽  
Yu B Belousov ◽  
L L Shteinberg ◽  
E E Alimova ◽  
E P Smirnova ◽  
...  

Group of researchers analytical group of PIFAGOR IV study The aim is to study the next step of pharmacoepidemiology of arterial hypertension (AH) in Russia to evaluate the structure and frequency of different classes of antihypertensive drugs (AHD) usage in clinical practice.Material and methods. The prospective pharmacoepidemiological multicenter study (PIFAGOR IV). We interrogated AH patients using special prepared questionnaires. The collection of questionnaires took place from February to July, 2013. The study included 2533 valid questionnaires from 52 cities and towns of Russia.Results. 80% of the patients regularly take AHD; 32.8% of patients receive monotherapy, 38.6% receive two AHD combinations, 28.4% - 3 or more AHD combinations. The average number of AHD was 2.02 per patient. The structure of AHD consisted of 5 recommended classes: ACE inhibitors (27.8%), -adrenergic receptor blocking agents (21.7%), diuretics (15.7%), calcium antagonists (11.3%) and angiotensin II receptor blockers (10.7%), fixed combination - 10.8%. Additional proportion of classes: central-acting agents - 2.3% and b-adrenoceptor blocking agents - 0.1%. Among the ACE inhibitors the main share had 3 drugs: enalapril (33.6%), perindopril (16%), and lisinopril (13%). In b-blockers class the main share had 2 drugs - bisoprolol (64.4%), and usual form of release and modified release dosage form of metoprolol (the total share 21,4%). Indapamide of standard and retard form took the first place in the structure of diuretics (the total share 75%). In calcium antagonists class the main share had amlodipine (55.8%). The main drug in ARBs II was losartan (55.4%). Central-acting agent class was consisted of moxonidine (66%), methyldopa (17%) and clonidine (5%). For about 76% of cases were presented by combinations containing diuretics and 24% - by combinations containing calcium antagonists among the fixed combinations. The proportion of original drugs in the structure of AHD was 38.3%. The average BP level in patients was 140.4/86.4 mm Hg and the blood pressure targets were determined in 50.2% of cases. A high degree of compliance according to the Morisky-Green test indicated in 32%, low compliance - in 49% of cases.Conclusions. We noted the reduction of ACE inhibitors proportion and increase of ARBs II proportion, increase of fixed combinations in the structure of AHD. However, we noticed the decrease of the treatment efficacy in patients with AH using average BP level and achievement of the target BP, as well as the average number of AHD.


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