An Efficient Synthetic Method and Theoretical Calculations of Olmesartan Methyl Ether. Study of Biological Function of AT1 Antagonism.
Abstract
The dissolution of the antihypertensive AT1 antagonist olmesartan in methanol generates in situ a new highly bioactive methyl ether analogue via SN1 mechanism involving an intramolecular proton transfer from carboxyl to hydroxyl group. Theoretical calculations confirmed the thermodynamic control preference of methyl ether versus the antagonistic product methyl ester. Α facile synthetic method for olmesartan methyl ether from olmesartan or olmesartan medoxomil is also described. Interestingly, the introduction of the methyl group to olmesartan did not alter its pharmacological properties. This obs...
Source: Combinatorial Chemistry and High Throughput Screening - May 29, 2014 Category: Chemistry Authors: Ntountaniotis D, Agelis G, Resvani A, Halabalaki M, Liapakis G, Spyridaki K, Grdadolnik SG, Merzel F, Kostidis S, Potamitis C, Tselios T, Matsoukas J, Skaltsounis LA, Mavromoustakos T Tags: Comb Chem High Throughput Screen Source Type: research
The Randomized Olmesartan and Diabetes Microalbuminuria Prevention (ROADMAP) Observational Follow-Up Study: Benefits of RAS Blockade With Olmesartan Treatment Are Sustained After Study Discontinuation [Hypertension]
Conclusions
Development of microalbuminuria is a valid marker for future CV events. RAS blockade with Olmesartan might cause sustained reduction (legacy effect) of micro- and macrovascular events. (Source: JAHA:Journal of the American Heart Association)
Source: JAHA:Journal of the American Heart Association - April 25, 2014 Category: Cardiology Authors: Menne, J., Ritz, E., Ruilope, L. M., Chatzikyrkou, C., Viberti, G., Haller, H. Tags: Hypertension Source Type: research
High throughput microwell spectrophotometric assay for olmesartan medoxomil in tablets based on its charge-transfer reaction with DDQ.
Abstract
Abstract The study describes the development and validation of a new microwell-based spectrophotometric assay for determination of olmesartan medoxomil (OLM) in tablets. The formation of a colored charge-transfer (CT) complex between OLM as an n-electron donor and 2,3-dichloro- -5,6-dicyano-1,4-benzoquinone (DDQ) as a p-electron acceptor was investigated, and employed as the basis for the development of the new assay. The proposed assay was conducted in 96-microwell plates. The absorbance of the colored-CT complex was measured at 460 nm with a microplate reader. Optimum conditions of the reaction ...
Source: Acta Pharmaceutica - March 1, 2014 Category: Drugs & Pharmacology Authors: Darwish IA, Wani TA, Khalil NY, Abdel-Rahman HM Tags: Acta Pharm Source Type: research
Measurement
and Correlation of Solubility of Olmesartan
Medoxomil in Six Green Solvents at 295.15–330.15 K
Industrial & Engineering Chemistry ResearchDOI: 10.1021/ie404373n (Source: Industrial and Engineering Chemical Research)
Source: Industrial and Engineering Chemical Research - February 5, 2014 Category: Chemistry Authors: Faiyaz Shakeel, Nazrul Haq, Fars K. Alanazi and Ibrahim A. Alsarra Source Type: research
Efficacy and safety of olmesartan/amlodipine/hydrochlorothiazide in patients with hypertension not at goal with mono, dual or triple drug therapy: results of the CHAMPiOn study
Conclusion:
Treatment with OM/AM/HCTZ achieved superior (SBP) ABPM reductions compared with mono, dual or triple drug therapy, resulting in all patients achieving systolic ABPM goal without ABPM documented hypotension. (Source: Therapeutic Advances in Cardiovascular Disease)
Source: Therapeutic Advances in Cardiovascular Disease - February 3, 2014 Category: Cardiology Authors: Punzi, H. A. Tags: Original Research Source Type: research
Effect of olmesartan medoxomil on number and survival of circulating endothelial progenitor cells and calcitonin gene related peptide in hypertensive patients
This study reports in essential hypertensive patients the effect of 6 months treatment with olmesartan on plasma level of CGRP and number and survival of cEPCs.
Methods and results: In 20 essential hypertensive patients treated with olmesartan medoxomil (20 mg per day for 6 months), cEPCs (CD34+KDR+, CD133+KDR+ and CD34+CD133+KDR+) (direct 3-color flow cytometry analysis), apoptosis of cEPCs (CD133+KDR+ cells with Annexin V expression), CGRP determination (ELISA) and HO-1 protein level (western blot) were assessed at baseline and after 3 and 6 months of treatments. Olmesartan normalized blood pressure (P (Source: Journal of Hypertension)
Source: Journal of Hypertension - December 17, 2013 Category: Cardiology Tags: ORIGINAL PAPERS: Therapeutic aspects Source Type: research
Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats.
Abstract
Olmesartan medoxomil (OM) is hydrolyzed to its active metabolite olmesartan by the action of aryl esterase to exert its antihypertensive actions by selectively blocking angiotensin II-AT1 receptor. Poor aqueous solubility and uncontrolled enzymatic conversion of OM to its poorly permeable olmesartan limits its oral bioavailability. The aim of the current study was to formulate a novel nanoemulsion of OM to improve its pharmacokinetics and therapeutic efficacy. The oil-in-water (o/w) nanoemulsion of OM was developed using lipoid purified soybean oil 700, sefsol 218 and solutol HS 15. We have charac...
Source: Colloids and Surfaces - December 16, 2013 Category: Biotechnology Authors: Gorain B, Choudhury H, Kundu A, Sarkar L, Karmakar S, Jaisankar P, Pal TK Tags: Colloids Surf B Biointerfaces Source Type: research
[Severe Enteropathy with Villous Atrophy Olmesartan Medoxomil-associated.]
PMID: 24246126 [PubMed - as supplied by publisher] (Source: Therapie)
Source: Therapie - November 11, 2013 Category: Psychiatry & Psychology Authors: Nunge D, Eoche M, Fumery M, Nguyen-Khac E, Gras V, Andréjak M Tags: Therapie Source Type: research
Olmesartan Linked to Spruelike Enteropathy
* There appears to be a relationship between the antihypertensive drug olmesartan medoxomil and spruelike enteropathy. This condition develops after long-term use of the drug, usually two years or more after the start of therapy.
* Patients who develop diarrhea and weight loss but don't have celiac sprue should be taken off olmesartan. (Source: AJN)
Source: AJN - November 1, 2013 Category: Nursing Tags: Drug Watch Source Type: research
The effects of colesevelam HCl on the single-dose pharmacokinetics of glimepiride, extended-release glipizide, and olmesartan medoxomil.
Abstract
Bile acid sequestrants can potentially bind to concomitant drugs. Single-dose studies evaluated the effects of colesevelam on the pharmacokinetics of glimepiride, glipizide extended-release (ER), and olmesartan medoxomil. Each study enrolled healthy subjects aged 18-45 years. The olmesartan medoxomil study used a randomized adaptive crossover design that initially compared olmesartan medoxomil alone versus simultaneously with colesevelam, then olmesartan medoxomil alone versus 4 hours before colesevelam. The other studies used a three-period crossover design (test drug alone, test drug simultaneou...
Source: The Journal of Clinical Pharmacology - September 10, 2013 Category: Drugs & Pharmacology Authors: He L, Wickremasingha P, Lee J, Tao B, Mendell-Harary J, Walker J, Wight D Tags: J Clin Pharmacol Source Type: research
Effect of the angiotensin II receptor antagonist olmesartan on morning home blood pressure in hypertension: HONEST Study at 16 weeks
hi
& K Shimada (Source: Journal of Human Hypertension)
Source: Journal of Human Hypertension - July 18, 2013 Category: Cardiology Authors: K KarioI SaitoT KushiroS TeramukaiY IshikawaK HiramatsuF KobayashiK Shimada Tags: angiotensin receptor antagonists clinic blood pressure home blood pressure monitoring morning hypertension olmesartan medoxomil Source Type: research
Blood pressure response with fixed-dose combination therapy: comparing hydrochlorothiazide with amlodipine through individual-level meta-analysis
Conclusion:Overall, the combination of olmesartan and HCTZ is as effective as olmesartan and CCB in lowering 24-h, daytime, and night-time ambulatory BP. However, greater lowering is noted with the olmesartan and CCB combination for clinic BP. Thus, out-of-office BP monitoring is necessary to provide better assessment of overall BP and response to treatment. Women and diabetic individuals may have slightly better 24-h ambulatory BP response with the olmesartan and CCB combination therapy. (Source: Journal of Hypertension)
Source: Journal of Hypertension - July 8, 2013 Category: Cardiology Tags: ORIGINAL PAPERS: Therapeutic aspects Source Type: research
Olmesartan/Amlodipine/Hydrochlorothiazide in Obese Participants With Hypertension: A TRINITY Subanalysis
The objective of this prespecified TRINITY study subgroup analysis was to assess the efficacy and safety of triple‐combination treatment with olmesartan medoxomil (OM) 40 mg, amlodipine besylate (AML) 10 mg, and hydrochlorothiazide (HCTZ) 25 mg vs the component dual‐combination treatments in obese (body mass index [BMI] ≥30 kg/m2) and nonobese (BMI <30 kg/m2) hypertensive participants. The double‐blind treatment period primary end point was the least‐squares (LS) mean reduction in seated diastolic BP (SeDBP) at week 12 (end of the double‐blind period). Of the 2492 randomized participants, 1555 (62.4%) h...
Source: The Journal of Clinical Hypertension - June 4, 2013 Category: Cardiology Authors: Eli M. Roth, Suzanne Oparil, Michael Melino, James Lee, Victor Fernandez, Reinilde Heyrman Tags: Original Paper Source Type: research
Clinical effects of combined olmesartan medoxomil and amlodipine on clinic and ambulatory blood pressure in elderly patients with resistant hypertension
In this study, 157 resistant hypertension patients older than 60 years were randomized to 8 weeks double-blind treatment with placebo, AML 10mg/day, OM 40mg/day and AM×L (10mg/day)+OM (40mg/day). Research outcomes suggested that ALM+OM combination therapy had superior efficacy than ALM or OM monotherapies in terms of the clinic blood pressure and 24-h ambulatory blood pressure. In addition, more patients receiving combination therapy (62.5%) achieved BP goal than those treated with placebo (18.4%), AML (37.5) or OM (38.5%) monotherapies. The adverse events in both groups were comparable. Thus, the combination of AML+OM pr...
Source: Archives of Gerontology and Geriatrics - May 13, 2013 Category: Geriatrics Authors: Shunjing Ding, Jin Liu, Qiang Fu, Ying Zheng Source Type: research
