Hypertension: Focus on Olmesartan Medoxomil

Bell, Allison; Nykamp, Diane

doi:10.4137/cmt.s2206

Cited by 2 publications

(4 citation statements)

References 26 publications

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“…Olmesartan also has good plasma protein binding (99%) with a high volume distribution rate of around 17 Liters. 13 In general, Olmesartan works by inhibiting AT 1 -R. Inhibition of AT 1 -R can inhibit the effect of vasoconstriction, reduce sodium and water retention, and reduce cell proliferation and hypertrophy. Inhibition of AT 1 -R provides an opportunity for AT 2 -R receptors with the opposite system of action.…”

Section: Mechanism Of Action Of Olmesartan and Amlodipinementioning

confidence: 99%

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The efficacy of olmesartan/amlodipine combination in hypertension treatment – a systematic review

Praptika¹,

Ryantama²,

Bhuwana³

2022

Intisari Sains Medis

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Introduction: Hypertension is the most common non-communicable disease, which persists as a major risk factor of cardiovascular diseases such as stroke, myocardial infection, and heart failure. Another major problem in clinical practice was the patients' adherence to treatment, directly related to the number of hypertension pills to be taken. Thus, determining the appropriate time duration and action of a hypertensive drug to maintain the blood pressure is needed. Olmesartan is one of the drug compounds frequently used for long-acting anti-hypertensive treatment. It is often combined with amlodipine; however, their combination remains unclear to provide equal efficacy and safety. Thus, in this article, we systematically summarize the combination of Olmesartan with amlodipine.Methods: This systematic literature review was extracted from Science Direct and Pubmed to identify randomized clinical trials (RCT) of the outcome of the Olmesartan/amlodipine effect compared with other hypertension regimens by using PRISMA guideline 2009. The methodological quality of the included studies was assessed independently by two reviewers using The Cochrane Collaboration's RoB 2 tool.Results: We evaluated twelve studies in the last ten years, and there were four studies with an intention-to-treat protocol (25% of articles had some concern, and 75% had a low risk of bias.) and eight studies with per-protocol analysis (37,5% of articles were concerned, and the rest had a low risk of overall bias). We also presented the efficacy and safety outcomes of the study reviewed.Conclusion: Hypertension is a common non-communicable disease, and treatment approaches for hypertension vary widely. Administration of combination drugs is a good approach in reducing the dose of drug administration and reducing the incidence of side effects in monotherapy. Inhibiting the RAA system by olmesartan and reducing vascular smooth muscle tone by amlodipine gives better results and can be a safe and effective option for lowering blood pressure in hypertensive patients. The side effects observed were not severe and only observed in a few cases, making it an option to treat hypertension.

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Section: Mechanism Of Action Of Olmesartan and Amlodipinementioning

confidence: 99%

“…This mechanism causes a decrease in blood pressure. [12][13][14] On the other hand, Amlodipine is a calcium channel blocker (CCB) dihydropyridine type hypertension drug. Amlodipine has good bioavailability (80%) and a long half-life that allows administration in a single daily dose.…”

Section: Mechanism Of Action Of Olmesartan and Amlodipinementioning

confidence: 99%

The efficacy of olmesartan/amlodipine combination in hypertension treatment – a systematic review

Praptika¹,

Ryantama²,

Bhuwana³

2022

Intisari Sains Medis

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“…The next intermediate in the synthesis of OM, N-tritylolmesartan medoxomil (6), is obtained in two steps from 3 (Scheme 1). Alkaline hydrolysis of 3 generates the potassium salt 4.…”

Section: Determination Of the Structure Of The Bromide 2 And The Intementioning

confidence: 99%

“…In April 2002, the U.S. Food and Drug Administration (FDA) approved OM (7, Scheme 1) for the treatment of www.mdpi.com/journal/molecules hypertension. The seventh in a growing class of antihypertensive agents known as the angiotensin II receptor blockers (Figure 1), the drug works by inhibiting effects of angiotensin II, a potent vasoconstrictor and one of the key contributors to cardiovascular and renal disease [4][5][6][7][8]. OM is a prodrug containing an ester moiety, which is rapidly and completely cleaved to release the active metabolite olmesartan (8) during absorption from the gastrointestinal tract.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Physicochemical Characterization of the Process-Related Impurities of Olmesartan Medoxomil. Do 5-(Biphenyl-2-yl)-1-triphenylmethyltetrazole Intermediates in Sartan Syntheses Exist?

et al. 2015

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During the process development for multigram-scale synthesis of olmesartan medoxomil (OM), two principal regioisomeric process-related impurities were observed along with the final active pharmaceutical ingredient (API). The impurities were identified as N-1-and N-2-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl derivatives of OM. Both compounds, of which N-2 isomer of olmesartan dimedoxomil is a novel impurity of OM, were synthesized and fully characterized by differential scanning calorimetry (DSC), infrared spectroscopy (IR), nuclear magnetic resonance spectroscopy (NMR) and high-resolution mass spectrometry/electrospray ionization (HRMS/ESI). Their 1 H, 13 C and 15 N nuclear magnetic resonance signals were fully assigned. The molecular structures of N-triphenylmethylolmesartan ethyl (N-tritylolmesartan ethyl) and N-tritylolmesartan medoxomil, the key intermediates in OM synthesis, were solved and refined using single-crystal X-ray diffraction (SCXRD). The SCXRD study revealed that N-tritylated intermediates of OM exist exclusively as one of the two possible regioisomers. In molecular structures of these regioisomers, the trityl substituent is attached to the N-2 nitrogen atom of the tetrazole ring, and not to the N-1 nitrogen, as has been widely reported up to the present. This finding indicates that the reported structural formula of N-tritylolmesartan ethyl and N-tritylolmesartan medoxomil, as well as their systematic chemical names, must be revised. The careful analysis of literature spectroscopic data for other sartan intermediates and their analogs with 5-(biphenyl-2-yl)tetrazole moiety showed that they also exist exclusively as N-2-trityl regioisomers.

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Hypertension: Focus on Olmesartan Medoxomil

Cited by 2 publications

References 26 publications

The efficacy of olmesartan/amlodipine combination in hypertension treatment – a systematic review

The efficacy of olmesartan/amlodipine combination in hypertension treatment – a systematic review

Synthesis and Physicochemical Characterization of the Process-Related Impurities of Olmesartan Medoxomil. Do 5-(Biphenyl-2-yl)-1-triphenylmethyltetrazole Intermediates in Sartan Syntheses Exist?

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