Hypertension: Focus on Olmesartan Medoxomil

2009 ◽  
Vol 1 ◽  
pp. CMT.S2206 ◽  
Author(s):  
Allison M. Bell ◽  
Diane Nykamp

Hypertension is the leading cause of stroke, heart failure, and ischemic heart disease. One of the key regulators of blood pressure is the renin-angiotensin aldosterone system (RAAS). Olmesartan medoxomil, an angiotensin receptor blocker (ARB), counteracts some of the primary effects of the RAAS by selectively and irreversibly binding to the type 1 angiotensin II receptor (AT1-R). The pharmacokinetic profile of this ARB allows for the convenience of one a day dosing. The pharmacodynamic profile of olmesartan is favorable because it is neither metabolized by, induces, nor inhibits the CYP450 isozyme system. The metabolism of the prodrug to the active form occurs in the gut by the enzyme arylesterase. No further metabolism and a lack of interaction with the CYP450 isozyme system leads to very few drug interactions with olmesartan medoxomil. Numerous studies have been conducted to evaluate the efficacy, safety, and tolerability of olmesartan medoxomil. Studies have been conducted to compare olmesartan medoxomil to other angiotensin receptor blockers. The efficacy of olmesartan medoxomil has been compared to other classes of antihypertensive agents. Results of all trials have proven non-inferiority of olmesartan medoxomil to other antihypertensive agents; some studies have shown superior blood pressure control provided by olmesartan medoxomil when starting dosages are evaluated. Overall, olmesartan medoxomil has the potential to facilitate the achievement of blood pressure goals, enhance compliance with a once daily dosing regimen, and is associated with minimal side effects. Olmesartan medoxomil has been proven to be a safe and effective antihypertensive drug when compared to other ARBs and other antihypertensive agents.

2005 ◽  
Vol 6 (1_suppl) ◽  
pp. S8-S11
Author(s):  
Hans-Christoph Diener

Hypertension is the most important modifiable risk factor for primary and secondary stroke prevention. All antihypertensive drugs are effective in primary prevention: the risk reduction for stroke is 30—42%. However, not all classes of drugs have the same effects: there is some indication that angiotensin receptor blockers may be superior to other classes of antihypertensive drugs in stroke prevention. Seventy-five percent of patients who present to hospital with acute stroke have elevated blood pressure within the first 24—48 hours. Extremes of systolic blood pressure (SBP) increase the risk of death or dependency. The aim of treatment should be to achieve and maintain the SBP in the range 140—160 mmHg. However, fast and drastic blood pressure lowering can have adverse consequences. The PROGRESS trial of secondary prevention with perindopril + indapamide versus placebo + placebo showed a decrease in numbers of stroke recurrences in patients given both active antihypertensive agents, more impressive for cerebral haemorrhage.There were also indications that active treatment might decrease the development of post-stroke dementia.


2015 ◽  
Author(s):  
Jacek Musijowski ◽  
Edyta Piórkowska ◽  
Katarzyna Buś - Kwaśnik ◽  
Agnieszka Tycz ◽  
Piotr J. Rudzki

Olmesartan belongs to a class of drugs called angiotensin II receptor blockers (ARBs). It works by relaxing blood vessels so that blood can flow more easily and is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Olmesartan medoxomil is an ester prodrug that is hydrolysed during absorption from gastrointestinal tract to the active form olmesartan. Due to rapid metabolism determination of the concentration of the prodrug in plasma is impossible. Previous human pharmacokinetic studies indicated that olmesartan is the only metabolite of olmesartan medoxomil. The aim of the study was to develop a method for the determination of olmesartan in human plasma. The developed LC-MS method is linear within the range of 5.00-2500.00 ng/mL which is suitable for pharmacokinetic studies after administration of 40 mg olmesartan medoxomil single oral dose. The sample preparation procedure is fast and allows examination of large numbers of samples in a short time. The method was validated according to European Medicines Agency (EMA) and Food and Drug Administration (FDA) guidelines, in compliance with the principles of Good Laboratory Practice (GLP). All of the validation parameters met acceptance criteria and the method was successfully applied in the pharmacokinetic study in humans.


2003 ◽  
Vol 37 (1) ◽  
pp. 99-105 ◽  
Author(s):  
Stephanie F Gardner ◽  
Amy M Franks

OBJECTIVE To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of olmesartan medoxomil, an angiotensin II receptor antagonist for the treatment of hypertension. DATA SOURCES Information was obtained from MEDLINE searches (1996–April 2002) of English-language medical literature. Search terms included CS-866, olmesartan, olmesartan medoxomil, RNH-6270 (active metabolite of olmesartan), Benicar, angiotensin receptors, and antihypertensive agents. In addition, references from relevant articles were reviewed for additional citations. The authors independently reviewed literature identified in the searches. Studies evaluating olmesartan (i.e., abstracts, clinical trials, data on file with manufacturer) were considered for inclusion. STUDY SELECTION All articles identified from data sources with pertinent information regarding olmesartan medoxomil were evaluated, and all information deemed relevant was included in this review. DATA SYNTHESIS Olmesartan medoxomil is a competitively priced addition to the class of angiotensin II receptor antagonists. Monotherapy with olmesartan medoxomil in once-daily doses of 20–40 mg has produced significant reductions in systolic and diastolic blood pressure in hypertensive patients. Adverse effects have been minimal with olmesartan medoxomil, with dizziness being the only adverse effect occurring more often than with placebo in clinical trials. Additionally, animal studies indicate that olmesartan medoxomil may prove to be useful treatment for diabetic nephropathy, as well as atherosclerosis. CONCLUSIONS Olmesartan medoxomil has a favorable safety and efficacy profile, with blood pressure–lowering effects comparable to those of other angiotensin receptor blockers (i.e., losartan, valsartan, irbesartan). At this time, formulary decisions will be driven primarily by economic issues. Theoretical benefits of olmesartan medoxomil in reducing atherogenesis and lowering angiotensin II concentrations better than the alternative agents will be determined only with more extensive research. THIS ARTICLE IS APPROVED FOR CONTINUING EDUCATION CREDIT ACPE UNIVERSAL PROGRAM NUMBER: 407-000-03-002-H01


2015 ◽  
Author(s):  
Jacek Musijowski ◽  
Edyta Piórkowska ◽  
Katarzyna Buś - Kwaśnik ◽  
Agnieszka Tycz ◽  
Piotr J. Rudzki

Olmesartan belongs to a class of drugs called angiotensin II receptor blockers (ARBs). It works by relaxing blood vessels so that blood can flow more easily and is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Olmesartan medoxomil is an ester prodrug that is hydrolysed during absorption from gastrointestinal tract to the active form olmesartan. Due to rapid metabolism determination of the concentration of the prodrug in plasma is impossible. Previous human pharmacokinetic studies indicated that olmesartan is the only metabolite of olmesartan medoxomil. The aim of the study was to develop a method for the determination of olmesartan in human plasma. The developed LC-MS method is linear within the range of 5.00-2500.00 ng/mL which is suitable for pharmacokinetic studies after administration of 40 mg olmesartan medoxomil single oral dose. The sample preparation procedure is fast and allows examination of large numbers of samples in a short time. The method was validated according to European Medicines Agency (EMA) and Food and Drug Administration (FDA) guidelines, in compliance with the principles of Good Laboratory Practice (GLP). All of the validation parameters met acceptance criteria and the method was successfully applied in the pharmacokinetic study in humans.


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.


2013 ◽  
Vol 4 (3) ◽  
Author(s):  
Renny M. Toreh ◽  
Sonny J.R. Kalangi ◽  
Sunny Wangko

Abstract: As the main structural component of the renin-angiotensin-aldosterone system (RAAS), the juxtaglomerular complex plays a very important role in the regulation of vascular resistance. The synthesis and release of renin into the circulation occurs due to the decrease of blood pressure, loss of body fluid, and a decrease of sodium intake. Renin converts angiotensinogen into angiotensin I, which is further converted by the angiotensin converting enzyme (ACE) into angiotensin II. This angiotensin II causes vasoconstriction of blood vessels, resulting in an increase of vascular resistance and blood pressure. The ACE inhibitors and the angiotensin receptor blockers (ARBs) do not inhibit the RAAS completely since they cause an increase of renin activity. The renin blockers are more effective in inhibiting RAAS activity; therefore, these renin blockers can be applied as antihypertensive agents with fewer side effects. The RAAS activity can be inhibited by a decrease of renin synthesis in the juxtaglomerular complex by blocking the signals in the juxtaglomerular complex that stimulate renin synthesis, and by blocking the gap junctions in the juxtaglomerular complex. Keywords: juxtaglomerular complex, vascular resistance, RAAS.   Abstrak: Kompleks jukstaglomerulus sebagai komponen struktural utama sistem renin angiotensin berperan penting dalam pengaturan resistensi pembuluh darah. Sintesis dan pelepasan renin ke sirkulasi terjadi karena tekanan darah yang rendah, kehilangan cairan tubuh, dan kurangnya intake natrium. Renin akan memecah angiotensinogen menjadi angiotesin I yang kemudian secara cepat dikonversi oleh enzim pengonversi angiotensin  menjadi angiotensin II. Angiotensin II menyebabkan vasokontriksi pembuluh darah sehingga meningkatkan resistensi pembuluh darah yang pada akhirnya akan meningkatkan tekanan darah. ACEinhibitor dan ARB kurang sempurna dalam menghambat kerja SRAA oleh karena keduanya memutuskan rantai mekanisme timbal balik sehingga meningkatkan aktifitas renin. Penghambat renin lebih efektif digunakan untuk menghambat aktifitas SRAA sehingga penghambat renin dapat digunakan sebagai obat anti-hipertensi dan memiliki efek samping yang rendah. Metode penghambatan SRAA yang juga dapat dikembangkan ialah penghambatan sintesis renin dalam kompleks jukstaglomerulus dengan cara menekan sinyal-sinyal dalam kompleks jukstaglomerulus yang merangsang sintesis renin dan menghambat fungsi taut kedap yang terdapat dalam kompleks jukstaglomerulus. Kata kunci: kompleks juksta glomerulus, resistensi vaskular, SRAA.


2021 ◽  
Vol 54 (3) ◽  
pp. 275-276
Author(s):  
Kanwal Ashiq ◽  
Sana Ashiq

Dear Editor, In December 2019, a new virus which is known as SARS-COV-2 (COVID-19) was identified. In a short period, this virus spread rapidly and caused significant morbidities and mortalities across the earth. On March 11, 2020, the World Health Organization (WHO) declared a pandemic due to the logarithmic expansion of COVID-19 cases globally.1 Various guidelines were issued, and a complete lockdown has been observed on a large scale to stop the spread of the virus. Currently, there is no specific treatment for COVID-19 is available. Throughout the year 2020, scientists struggled a lot to find the COVID-19 cure, and many vaccines are successfully developed which would be helpful in the prevention of disease. Nevertheless, the emergence of virus variants remains an issue. The epidemiological trends and clinical features of this disease have been reported in several publications.2 Due to comorbidities, COVID-19 disease can exacerbate and may result in increased severity and deadly consequences. In a study, the most common comorbidities in COVID-19 patients were reported as following; diabetes (19%), hypertension (30%), and coronary heart disease (8%). In hypertension, blood pressure elevates from the threshold level. The occurrence of hypertension is not necessarily to be associated with COVID-19 as hypertension is quite frequent in geriatric patients, and these patients are at higher risk of being infected with COVID-19.3,4 Angiotensin receptor blockers (ARBs) and angiotensin-converting enzyme (ACE) inhibitors are widely prescribed for the cure of hypertension and other cardiovascular-related diseases. On the other hand, the COVID-19 virus binds with ACE2 to gain entry into the lung cells. ACE inhibitors and ARBs escalate ACE2 that could hypothetically increase the chance of COVID-19 binding to lung cells and could headway to more damage. Conversely, in experimental studies, ACE2 showed a protective effect against lung injury. Due to the anti-inflammatory potential of ACE inhibitors and ARBs, these agents can reduce the incidence of developing myocarditis and acute respiratory distress syndrome in COVID-19 patients. There is no evidence that hypertension is linked with the COVID-19 and anti-hypertensive medicines (ACE inhibitors and ARBs) are either harmful or beneficial during the COVID-19 pandemic.5 During this unprecedented situation, the Council on Hypertension of the European Society of Cardiology released a statement that “The Council on Hypertension strongly recommends that physicians and patients should continue treatment with their usual anti-hypertensive therapy because there is no clinical or scientific evidence to suggest that treatment with ACEIs or ARBs should be discontinued because of the COVID-19 infection.” After this announcement, many other societies also recommend that patients should continue using their current hypertensive therapy and if necessary, after careful assessment, changes can be made in the hypertensive regimen.6 According to estimation, globally, 1.5 billion people can suffer from hypertension by 2025 which may contribute approximately 75% of stroke risk and 50% of heart disease risk. CVDs accounts almost 38% of deaths related to the non-communicated disease (NCDs). In Pakistan, hypertension is a chief health concern that leads to significant morbidity and mortality. Blood pressure can be control with medications and lifestyle modifications. One of the best approaches to control and improve blood pressure is team-based care consisting of doctors, pharmacists, and nurses. During COVID-19, collaborative efforts are required to improve patient’s quality of life and to reduce the healthcare burden.7,8 Keywords: COVID-19, Hypertension, Pandemic, ACE inhibitors References Ashiq K, Bajwa MA, Ashiq S. COVID-19 Pandemic and its Impact on Pharmacy Education. Turkish J Pharma Sci. 2021;18(2):122. Ashiq K, Ashiq S, Bajwa MA, Tanveer S, Qayyum M. Knowledge, attitude and practices among the inhabitants of Lahore, Pakistan towards the COVID-19 pandemic: an immediate online based cross-sectional survey while people are under the lockdown. Bangladesh J Med Sci. 2020:69-S 76. Zhou F, Yu T, Du R, Fan G, Liu Y, Liu Z, et al. Clinical course and risk factors for mortality of adult inpatients with COVID-19 in Wuhan, China: a retrospective cohort study. Lancet. 2020;395(10229):1054-62. Ashiq S, Ashiq K. The Role of Paraoxonase 1 (PON1) Gene Polymorphisms in Coronary Artery Disease: A Systematic Review and Meta-Analysis. Biochem Genet. 2021:1-21. Schiffrin EL, Flack JM, Ito S, Muntner P, Webb RC. Hypertension and COVID-19. Am J Hypertens. 2020;33(5):373–374. Patel AB, Verma A. COVID-19 and angiotensin-converting enzyme inhibitors and angiotensin receptor blockers: what is the evidence? JAMA. 2020;323(18):1769-70. Riaz M, Shah G, Asif M, Shah A, Adhikari K, Abu-Shaheen A. Factors associated with hypertension in Pakistan: A systematic review and meta-analysis. PLoS One. 2021;16(1):e0246085. Zarei L, Karimzadeh I, Moradi N, Peymani P, Asadi S, Babar Z-U-D. Affordability assessment from a static to dynamic concept: a scenario-based assessment of cardiovascular medicines. Int J Environ Res Public Health. 2020;17(5):1710.


Sign in / Sign up

Export Citation Format

Share Document