How to deal with the occurrence of rare drug-induced adverse events: the example of sprue-like enteropathy induced by olmesartan medoxomil and other angiotensin-receptor blockers.
Authors: Burnier M, Kjeldsen SE, Narkiewicz K, Oparil S PMID: 32049554 [PubMed - as supplied by publisher] (Source: Blood Pressure)
Source: Blood Pressure - February 14, 2020 Category: Hematology Tags: Blood Press Source Type: research

Severe intoxication caused by sodium-glucose cotransporter 2 inhibitor overdose: a case report.
CONCLUSIONS: Our case showed that an overdose of an SGLT2 inhibitor caused toxic effects on renal function, but severe hypoglycemia was not observed. Additional cases of intoxication from SGLT2 inhibitors alone would be helpful to clarify the mechanism of intoxication. PMID: 31918741 [PubMed - in process] (Source: BMC Pharmacology and Toxicology)
Source: BMC Pharmacology and Toxicology - January 11, 2020 Category: Drugs & Pharmacology Tags: BMC Pharmacol Toxicol Source Type: research

Method Validation for Simultaneous Quantification of Olmesartan and Hydrochlorothiazide in Human Plasma Using LC-MS/MS and Its Application Through Bioequivalence Study in Healthy Volunteers
A new, simple, sensitive, selective, rapid and high throughput liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for simultaneous quantification of Olmesartan and Hydrochlorothiazide in human plasma. Simple liquid–liquid extraction procedure was applied for plasma sample pretreatment using a mixture of diethyl ether and dichloromethane, as an extraction solution. Analytes were separated on Unisol C18 150*4.6 mm, 5 µm column using methanol and 2 mM ammonium acetate pH 5.5 (80:20, v/v) as a mobile phase and detected by electrospray ionization in the multiple reactio...
Source: Frontiers in Pharmacology - July 23, 2019 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo evaluation of Olmesartan Medoxomil microcrystals and nanocrystals: Preparation, characterization, and pharmacokinetic comparison in Beagle Dogs.
Conclusion:Particles size reduction to nano-scale by means of nanocrystals technology significantly increased in vitro dissolution rate and in vivo oral bioavailability of OLM. PMID: 31244438 [PubMed - as supplied by publisher] (Source: Current Drug Delivery)
Source: Current Drug Delivery - June 27, 2019 Category: Drugs & Pharmacology Authors: Chai R, Gao H, Ma Z, Guo M, Fu Q, Liu H, He Z Tags: Curr Drug Deliv Source Type: research

Design and development of a self-microemulsifying drug delivery system of Olmesartan Medoxomil for enhanced bioavailability.
Authors: Komesli Y, Ozkaya AB, Ergur BU, Kirilmaz L, Karasulu E Abstract Olmesartan Medoxomil (OM) is a hydrophobic antihypertensive drug with low bioavailability (26%) and is known to have adverse effects such as celiac disease and enteropathy. The purpose of this study was to develop SMEDDS to increase bioavailability and decrease potential side effects of OM. Hydrophilic lipophilic balance was calculated by testing solubility of OM in different oils, surfactants and cosurfactants to obtain the most suitable combination of SMEDDS. Pseudoternary phase diagram was used to select the better oil/water formulation of ...
Source: Drug Development and Industrial Pharmacy - April 17, 2019 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Olmesartan medoxomil
(Source: Reactions Weekly)
Source: Reactions Weekly - February 1, 2019 Category: Drugs & Pharmacology Source Type: research

Effect of block sequence of hyperbranched block copolymers on the aggregation behavior, drug solubilization and release property
Publication date: Available online 15 January 2019Source: Journal of Molecular LiquidsAuthor(s): Yutao Xue, Jie Sun, Shan Xiong, Huining Chai, Xia Xin, Guiying Xu, Teng LiuAbstractTwo hyperbranched block copolymers H904 and H90R4 which were the same in chemical composition but different in block sequence were synthesized by anionic polymerization. Commercially X shaped Tetronic block copolymers T904 and T90R4 were selected for comparison. The effect of block sequence on the aggregation behaviors of these four copolymers were studied by surface tension, transmission electron microscopy, steady-state fluorescence and dynamic...
Source: Journal of Molecular Liquids - January 15, 2019 Category: Molecular Biology Source Type: research

Inhibition of Co-Crystallization of Olmesartan Medoxomil and Hydrochlorothiazide for Enhanced Dissolution Rate in Their Fixed Dose Combination.
This study investigated the possibility of this interaction during co-processing. The research was extended to inhibit deleterious interactions. The drugs were co-evaporated from ethanolic solution to maximize the chance of interaction. This was performed in the absence and presence of hydroxypropyl methylcellulose (HPMC) and/or aerosil. The products were characterized using Fourier transform infrared spectroscopy (FTIR), differential thermal analysis, and powder X-ray diffraction (PXRD) in addition to dissolution studies. Co-evaporation of Olm with HCTZ in the absence of excipients produced crystalline material with FTIR ...
Source: AAPS PharmSciTech - December 17, 2018 Category: Drugs & Pharmacology Authors: Abdelquader MM, Essa EA, El Maghraby GM Tags: AAPS PharmSciTech Source Type: research

Nanocolloidal lipidic carriers of olmesartan medoxomil surface-tailored with Concavalin-A for lectin receptor targeting
Nanomedicine, Ahead of Print. (Source: Future Medicine: Nanomedicine)
Source: Future Medicine: Nanomedicine - November 26, 2018 Category: Nanotechnology Authors: Sarwar Beg Hani Choudhry Mazin A Zamzami Khalid S Alharbi Mahfoozur Rahman Bhupinder Singh Source Type: research

Nanocolloidal lipidic carriers of olmesartan medoxomil surface-tailored with Concavalin-A for lectin receptor targeting
Nanomedicine, Ahead of Print. (Source: Nanomedicine)
Source: Nanomedicine - November 26, 2018 Category: Nanotechnology Authors: Sarwar Beg Hani Choudhry Mazin A Zamzami Khalid S Alharbi Mahfoozur Rahman Bhupinder Singh Source Type: research

Characterization of the binding and conformational changes of bovine serum albumin upon interaction with antihypertensive olmesartan medoxomil
Publication date: Available online 1 November 2018Source: Journal of Molecular StructureAuthor(s): Atmanand M. Bagoji, Arunkumar T. Buddanavar, Naveen M. Gokavi, Sharanappa T. NandibewoorAbstractThe interaction of bovine serum albumin (BSA) with the olmesartan medoxomil (OLM) was investigated by different spectroscopic and linear sweep voltammetric techniques under experimentally optimised physiological conditions. The alteration of functional properties of BSA when quenched by OLM was illustrated by the continuous decrease of the fluorescence intensity of BSA upon addition of OLM. The quenching constants (Ksv) obtained we...
Source: Journal of Molecular Structure - November 6, 2018 Category: Molecular Biology Source Type: research

Olmesartan medoxomil
(Source: Reactions Weekly)
Source: Reactions Weekly - November 1, 2018 Category: Drugs & Pharmacology Source Type: research

Correction to: Olmesartan medoxomil/amlodipine/hydrochlorothiazide 20  mg/5 mg/12.5 mg fixed-dose combination in hypertension: a profile of its use
Page 2, column 2, section “What is the clinical efficacy of OLM/AMT/HCT 20 mg/5 mg/12.5 mg?”, paragraph 1, lines 5–8: The following text, which previously read. (Source: Drugs and Therapy Perspectives)
Source: Drugs and Therapy Perspectives - June 8, 2018 Category: Drugs & Pharmacology Source Type: research

Fabrication of Nanosuspension Directly Loaded Fast-Dissolving Films for Enhanced Oral Bioavailability of Olmesartan Medoxomil: In Vitro Characterization and Pharmacokinetic Evaluation in Healthy Human Volunteers.
Abstract Olmesartan medoxomil (OM) is an antihypertensive drug with poor water solubility and low oral bioavailability (28.6%). Accordingly, this study aimed to formulate and evaluate OM nanosuspension incorporated into oral fast-dissolving films (FDFs) for bioavailability enhancement. OM nanosuspension was prepared by antisolvent-precipitation-ultrasonication method and characterized regarding particle size (122.67 ± 5.03 nm), span value (1.40 ± 0.51), and zeta potential (- 46.56 ± 1.20 mV). Transmission electron microscopy (TEM) of t...
Source: AAPS PharmSciTech - April 26, 2018 Category: Drugs & Pharmacology Authors: Alsofany JM, Hamza MY, Abdelbary AA Tags: AAPS PharmSciTech Source Type: research

Case of photosensitivity after the administration of olmesartan medoxomil
The Journal of Dermatology, EarlyView. (Source: The Journal of Dermatology)
Source: The Journal of Dermatology - March 31, 2018 Category: Dermatology Source Type: research

Long ‐term efficacy and tolerability of azilsartan medoxomil/chlorthalidone vs olmesartan medoxomil/hydrochlorothiazide in chronic kidney disease
The Journal of Clinical Hypertension, EarlyView. (Source: The Journal of Clinical Hypertension)
Source: The Journal of Clinical Hypertension - March 4, 2018 Category: Cardiology Source Type: research

A randomized titrate-to-target study comparing fixed-dose combinations of azilsartan medoxomil and chlorthalidone with olmesartan and hydrochlorothiazide in stage-2 systolic hypertension
Background: Azilsartan medoxomil (AZL-M), an angiotensin II receptor blocker, has been developed in fixed-dose combinations (FDCs) with chlorthalidone (CTD). Objective/methods: We compared FDCs of AZL-M/CTD 20/12.5 mg once daily titrated to 40/25 mg if needed or AZL-M/CTD 40/12.5 mg once daily titrated to 80/25 mg if needed with an olmesartan medoxomil (OLM)-hydrochlorothiazide (HCTZ) 20/12.5 mg FDC once daily titrated to 40/25 mg if needed in a randomized, double-blind, 8-week study of 1085 participants with clinic SBP 160–190 mmHg and DBP 119 mmHg or less. Titration to higher doses occurred at ...
Source: Journal of Hypertension - March 1, 2018 Category: Cardiology Tags: ORIGINAL PAPERS: Therapeutic aspects Source Type: research

Identification and characterization of the druggable kinase targets of olmesartan and its analogues from a systematic kinase –chemical interaction profile in atherosclerosis
Publication date: March 2018 Source:Journal of Molecular Graphics and Modelling, Volume 80 Author(s): Rui-Juan Zhuang, Wei-Dong Jin, Xiao-Yan Wang, Xue-Ming Wu Olmesartan (OL) is the pharmacologically active metabolite of Olmesartan medoxomil (OM), an FDA-approved angiotensin II receptor antagonist for administrating cardiovascular diseases. The drug has been found to have potential effects on diverse protein kinase signaling involved in the pathogenesis of atherosclerosis, either by directly inhibiting the hub kinases or by indirectly modulating marginal members in the signaling pathways. In the present study, we computa...
Source: Journal of Molecular Graphics and Modelling - March 1, 2018 Category: Molecular Biology Source Type: research

Solid lipid nanoparticles as an efficient drug delivery system of olmesartan medoxomil for the treatment of hypertension
Publication date: 1 May 2018 Source:Colloids and Surfaces B: Biointerfaces, Volume 165 Author(s): Nilima T. Pandya, Parva Jani, Jigar Vanza, Hemal Tandel The aim of the current investigation was to develop solid lipid nanoparticles of olmesartan medoxomil using hot homogenization method to improve its oral bioavailability. Central composite design was applied to optimize the formulation variables; lipid X1 (Glyceryl monostearate) and surfactant X2 (Poloxamer: Tween 80). The particle sizes were in the nanometer range and spherical shaped for all prepared solid lipid nanoparticles formulations and the zeta potential absolut...
Source: Colloids and Surfaces B: Biointerfaces - February 23, 2018 Category: Biochemistry Source Type: research

Comparative effectiveness of an angiotensin receptor blocker, olmesartan medoxomil, in older hypertensive patients
The efficacy and safety of olmesartan medoxomil (OM) vs active control (AC) monotherapy among elderly patients aged 60‐79 years (N = 4487) was evaluated by meta‐analysis (25 studies). In all patients, change from baseline to end point in blood pressure (BP) was significantly greater with OM vs AC (−19.5/−11.9 vs −16.8/−10.7 mm Hg). Greater proportions of OM‐ vs AC‐treated patients achieved BP goals. In patients with impaired renal function (estimated glomerular filtration rate
Source: The Journal of Clinical Hypertension - February 20, 2018 Category: Cardiology Authors: Josep Redon, Michael A. Weber, Paul ‐Egbert Reimitz, Ji‐Guang Wang Tags: ORIGINAL PAPER Source Type: research

Solid lipid nanoparticles as an efficient drug delivery system of olmesartan medoxomil for the treatment of hypertension.
Abstract The aim of the current investigation was to develop solid lipid nanoparticles of olmesartan medoxomil using hot homogenization method to improve its oral bioavailability. Central composite design was applied to optimize the formulation variables; lipid X1 (Glyceryl monostearate) and surfactant X2 (Poloxamer: Tween 80). The particle sizes were in the nanometer range and spherical shaped for all prepared solid lipid nanoparticles formulations and the zeta potential absolute values were high, predicting good long-term stability. In vitro study of olmesartan loaded solid lipid nanoparticle exhibited controlle...
Source: Colloids and Surfaces - February 9, 2018 Category: Biotechnology Authors: Pandya NT, Jani P, Vanza J, Tandel H Tags: Colloids Surf B Biointerfaces Source Type: research

Long ‐term efficacy and tolerability of azilsartan medoxomil/chlorthalidone vs olmesartan medoxomil/hydrochlorothiazide in chronic kidney disease
An open‐label, long‐term study evaluated safety and tolerability of azilsartan medoxomil/chlorthalidone (AZL‐M/CLD) vs olmesartan/hydrochlorothiazide (OLM/HCTZ) in hypertensive participants with stage 3 chronic kidney disease. Initial therapy was AZL‐M/CLD 20/12.5 mg (n = 77) or OLM/HCTZ 20/12.5 mg (n = 76), but could be up‐titrated (AZL‐M/CLD to 40/25 mg; OLM/HCTZ to 40/25 mg [US] or 20/25 mg [Europe]) with other agents added during weeks 4‐52. Primary endpoint was proportion of participants with ≥ 1 adverse event (AE) through week 52. Baseline demograph...
Source: The Journal of Clinical Hypertension - February 1, 2018 Category: Cardiology Authors: George L. Bakris, Lin Zhao, Stuart Kupfer, Attila Juhasz, Michie Hisada, Eric Lloyd, Suzanne Oparil Tags: ORIGINAL PAPER Source Type: research

In Brief: Olmesartan and Sprue-Like Enteropathy
Date: January 29, 2018 Issue #:  1539Summary:  A reader asked whether healthcare providers should avoid prescribing the angiotensin receptor blocker (ARB) olmesartan medoxomil (Benicar, and others) because it can cause severe GI adverse effects.In 2013, the FDA warned that olmesartan can cause sprue-like enteropathy, a condition characterized by intestinal villous atrophy, severe chronic diarrhea, and significant unintended weight loss. The warning was based on 23 cases of serious sprue-like enteropathy associated with use of olmesartan, some occurring years after starting the drug. All patient...
Source: The Medical Letter - December 27, 2017 Category: Drugs & Pharmacology Authors: admin Source Type: research

Olmesartan medoxomil/amlodipine/hydrochlorothiazide 20  mg/5 mg/12.5 mg fixed-dose combination in hypertension: a profile of its use
AbstractThe triple-component fixed-dose combination of olmesartan medoxomil (OLM)/amlodipine (AML)/hydrochlorothiazide (HCT) is a rational choice for patients who require treatment with three or more antihypertensives. The three drugs in the FDC have complementary mechanisms of action, with OLM, AML and HCT being an angiotensin II receptor blocker, calcium channel blocker and diuretic, respectively. Once-daily OLM/AML/HCT 20  mg/5 mg/12.5 mg reduced systolic and diastolic blood pressure, thereby enabling patients to achieve blood pressure goals, and was generally well tolerated in clinical trials. Moreover, ...
Source: Drugs and Therapy Perspectives - December 4, 2017 Category: Drugs & Pharmacology Source Type: research

The Effect of Ethanol on the Hydrolysis of Ester-type Drugs by Human Serum Albumin.
Abstract Human serum albumin (HSA) has two major ligand-binding sites, sites I and II, and hydrolyzes compounds at both sites. Although the hydrolytic interaction of ester-type drugs with other drugs by HSA has been reported, there are only a few studies concerning the effect of pharmaceutical excipients on the hydrolysis of ester-type drugs by HSA. In the present study, we investigated the effect of ethanol (2 vol%; 345 mM) on the hydrolysis of aspirin, p-nitrophenyl acetate, and olmesartan medoxomil, which are ester-type drugs, with 4 different lots of HSA preparations. The hydrolysis activities of HSA toward as...
Source: Biological and Pharmaceutical Bulletin - November 27, 2017 Category: Drugs & Pharmacology Authors: Tatsumi A, Inoue S, Hamaguchi T, Iwakawa S Tags: Biol Pharm Bull Source Type: research

A Case of Moderate Sprue-Like Enteropathy Associated With Telmisartan.
We report a case of sprue-like enteropathy associated with telmisartan. A 52-year-old man presented with chronic diarrhea, abdominal discomfort and significant weight loss. In the last 3 years, he had been treated with telmisartan 40 mg/day for hypertension after right adrenalectomy for an aldosterone-producing adenoma. Laboratory investigations showed no significant abnormalities: Hb 13.6 g/dL, serum albumin 3.9 g/dL, total cholesterol 193 mg/dL, serum creatinine 0.99 mg/dL, sodium 143.6 mmol/L, K(+) 4.3 mmol/L, calcium 9.3 mg/dL, phosphorus 3.9 mg/dL and 25-OH-D3 27.7 ng/mL. Duodenal histology showed subtotal VA and infl...
Source: Clin Med Res - November 24, 2017 Category: Research Authors: Negro A, De Marco L, Cesario V, Santi R, Boni MC, Zanelli M Tags: J Clin Med Res Source Type: research

Olmesartan ‐based monotherapy vs combination therapy in hypertension: A meta‐analysis based on age and chronic kidney disease status
Antihypertensive monotherapy is often insufficient to control blood pressure (BP). Several recent guidelines advocate for initial combination drug therapy in many patients. This meta‐analysis of seven randomized, double‐blind studies (N = 5888) evaluated 8 weeks of olmesartan medoxomil (OM)–based single‐pill dual‐combination therapy (OM+amlodipine/azelnidipine or hydrochlorothiazide) vs OM monotherapy in adults with hypertension. BP‐lowering efficacy, goal achievement, and adverse events were assessed in the full cohort and subgroups (elderly/nonelderly and patients with and without chronic k...
Source: The Journal of Clinical Hypertension - October 25, 2017 Category: Cardiology Authors: Prakash Deedwania, Michael Weber, Paul ‐Egbert Reimitz, George Bakris Tags: ORIGINAL PAPER Source Type: research

QbD-Driven Development and Evaluation of Nanostructured Lipid Carriers (NLCs) of Olmesartan Medoxomil employing Multivariate Statistical Techniques.
CONCLUSIONS: Overall, the presented studies indicated successful development of NLCs using multivariate statistical approaches for improved product and process understanding. PMID: 29048242 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - October 21, 2017 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Comments on: “Population Pharmacokinetic Modeling of Olmesartan, the Active Metabolite of Olmesartan Medoxomil, in Patients with Hypertension”
(Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Comparison of long ‐term safety of fixed‐dose combinations azilsartan medoxomil/chlorthalidone vs olmesartan medoxomil/hydrochlorothiazide
This 52‐week, randomized, open‐label study evaluated long‐term safety/tolerability of fixed‐dose combination azilsartan medoxomil/chlorthalidone (AZL‐M/CLD) vs fixed‐dose combination olmesartan medoxomil/hydrochlorothiazide (OLM/HCTZ) in patients with essential hypertension (stage 2; clinic systolic blood pressure 160–190 mm Hg). Initial AZL‐M/CLD 40/12.5 mg/d (n=418) or OLM/HCTZ 20/12.5 mg/d (n=419) could be uptitrated during weeks 4 to 52 (AZL‐M/CLD to 80/25 mg; OLM/HCTZ to 40/25 mg [United States] or 20/25 mg [Europe]) to meet blood pressure targets. Treatment‐emerge...
Source: The Journal of Clinical Hypertension - July 6, 2017 Category: Cardiology Authors: Joel M. Neutel, William C. Cushman, Eric Lloyd, Bruce Barger, Alison Handley Tags: ORIGINAL PAPER Source Type: research

Bioequivalence Study of a New Fixed-Dose Combination Tablet Containing S-Amlodipine Nicotinate and Olmesartan Medoxomil in Healthy Korean Male Subjects.
Abstract PURPOSE: A fixed-dose combination (FDC) pill of amlodipine (relatively old calcium channel blocker as dihydropyridine) and olmesartan (relatively new angiotensin II receptor blocker) is used for hypertension that is not adequately controlled with a single-formulation drug. Because the FDC is a one-pill formulation, and amlodipine and olmesartan have different mechanisms of action, it is expected to improve patients' medication compliance and have an increased blood pressure-lowering efficacy. The purpose of this study was to assess the safety profile and the bioequivalence of two different FDC formulation...
Source: Clinical Therapeutics - June 15, 2017 Category: Drugs & Pharmacology Authors: Oh MJ, Hwang HH, Kim HG, Lee GH, Cho YS, Lee SY, Kang SY, Cho KH, Lee YY, Lee YJ, Jang CG, Lee SY Tags: Clin Ther Source Type: research

Triple Combination Therapies Based on Olmesartan: A Personalized Therapeutic Approach to Improve Blood Pressure Control
AbstractRecent epidemiological surveys have demonstrated that effective and sustained blood pressure (BP) control is achieved in a relatively small proportion of treated hypertensive patients. Indeed, treatment of hypertension represents a key strategy for preventing coronary artery disease, stroke, congestive heart failure and cardiovascular death. Several interventions have been proposed by international guidelines for ameliorating hypertension management and control, mostly including integrated and multi-dimensional pharmacological and non-pharmacological strategies. In particular, numerous evidence demonstrated that a ...
Source: High Blood Pressure and Cardiovascular Prevention - June 12, 2017 Category: Cardiology Source Type: research

Autoimmune ‐like chronic hepatitis induced by olmesartan
This article is protected by copyright. All rights reserved. (Source: Hepatology)
Source: Hepatology - April 24, 2017 Category: Internal Medicine Authors: Sandrine Barge, Marianne Ziol, Jean ‐Charles Nault Tags: Clinical Observations in Hepatology Source Type: research

Olmesartan medoxomil
(Source: Reactions Weekly)
Source: Reactions Weekly - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Development of olmesartan medoxomil lipid-based nanoparticles and nanosuspension: preparation, characterization and comparative pharmacokinetic evaluation.
Authors: B A, D N, Veerabrahma K Abstract The aim was to enhance the oral bioavailability of olmesartan medoxomil (OM) by preparing solid lipid nanoparticles (SLNs) and comparing with nanosuspension (OM-NS). OM-SLNs and OM-NS were prepared by known methods. Prepared SLNs were evaluated for physical characters and in vivo pharmacokinetic (PK) performance in rats. OM-NS showed more than four-fold increase in the solubility. During DSC and XRD studies, drug incorporated in SLNs was found to be in amorphous form. The relative bioavailability of OM-SLN and OM-NS was 7.21- and 3.52-fold when compared with that of coarse ...
Source: Artificial Cells, Nanomedicine and Biotechnology - March 17, 2017 Category: Biotechnology Tags: Artif Cells Nanomed Biotechnol Source Type: research

Development of olmesartan medoxomil lipid-based nanoparticles and nanosuspension: preparation, characterization and comparative pharmacokinetic evaluation
. (Source: Artificial Cells, Blood Substitutes, and Biotechnology)
Source: Artificial Cells, Blood Substitutes, and Biotechnology - March 14, 2017 Category: Biotechnology Authors: Arun B. Narendar D. Kishan Veerabrahma Source Type: research

Practical efficacy of olmesartan versus azilsartan in patients with hypertension: a multicenter randomized-controlled trial (MUSCAT-4 study)
Background: Olmesartan and azilsartan, angiotensin II receptor blockers (ARBs), are expected to decrease blood pressure more than the other ARBs. We conducted randomized-controlled trials to compare the practical efficacy of olmesartan with azilsartan. Methods: Eighty-four patients treated with the conventional ARBs for more than 3 months were assigned randomly to receive either 20 mg of olmesartan (olmesartan medoxomil, OL group) or 20 mg of azilsartan (azilsartan, not azilsartan medoxomil, AZ group) once daily for 16 weeks. The practical efficacy on blood pressure was compared between the OL and AZ groups....
Source: Blood Pressure Monitoring - March 11, 2017 Category: Cardiology Tags: Clinical Trial Source Type: research

Development of olmesartan medoxomil optimized nanosuspension using Box-Behnken design to improve oral bioavailability.
Authors: K N, D N, V K Abstract The aim of present investigation was to enhance the oral bioavailability of olmesartan medoxomil by improving its solubility and dissolution rate by preparing nanosuspension (OM-NS), using Box-Behnken design. In this, four factors were evaluated at three levels. Independent variables include: concentration of drug (X1), concentration of surfactant (X2), concentration of polymer (X3) and number of homogenization cycles (X4). Based on preliminary studies the size (Y1), zeta potential (Y2) and % drug release at 5min (Y3) were chosen as dependent responses. OM-NS were prepared by high pr...
Source: Drug Development and Industrial Pharmacy - March 10, 2017 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Nanostructured lipid carriers of olmesartan medoxomil with enhanced oral bioavailability
Publication date: 1 June 2017 Source:Colloids and Surfaces B: Biointerfaces, Volume 154 Author(s): Vikram Kaithwas, Chander Parkash Dora, Varun Kushwah, Sanyog Jain The current study explores the potential of nanostructured lipid carriers (NLCs) for oral bioavailability enhancement of olmesartan medoxomil (OLM) by systemic design approach. OLM-NLC was successfully prepared with optimized process parameters (i.e. amount of liquid lipid, total amount of lipid, drug content and surfactant concentration) using the Box-Behnken design of experiments for different response parameters (i.e. particle size, Polydispersity index and...
Source: Colloids and Surfaces B: Biointerfaces - March 9, 2017 Category: Biochemistry Source Type: research

Nanostructured lipid carriers of olmesartan medoxomil with enhanced oral bioavailability.
Abstract The current study explores the potential of nanostructured lipid carriers (NLCs) for oral bioavailability enhancement of olmesartan medoxomil (OLM) by systemic design approach. OLM-NLC was successfully prepared with optimized process parameters (i.e. amount of liquid lipid, total amount of lipid, drug content and surfactant concentration) using the Box-Behnken design of experiments for different response parameters (i.e. particle size, Polydispersity index and entrapment efficiency). Further, optimized formulation was validated which depicted nano size, homogenous distribution with optimum entrapment effi...
Source: Colloids and Surfaces - March 6, 2017 Category: Biotechnology Authors: Kaithwas V, Dora CP, Kushwah V, Jain S Tags: Colloids Surf B Biointerfaces Source Type: research

Management of Hypertension Using Olmesartan Alone or in Combination
In conclusion, olmesartan medoxomil, is an angiotensin II receptor blocker with an excellent efficacy in the reduction and stabilization of blood pressure. When combined with calcium channel blockers (CCBs) and diuretics, olmesartan medoxomil has a better effect on controlling BP and reducing AEs in patients. (Source: Cardiology and Therapy)
Source: Cardiology and Therapy - March 3, 2017 Category: Cardiology Source Type: research

Solid lipid nanoparticles as vesicles for oral delivery of Olmesartan Medoxomil: Formulation, optimization and in vivo evaluation.
CONCLUSION: In conclusion, SLN show promising approaches as a vehicle for oral delivery of drugs like OLM. PMID: 28005442 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - December 24, 2016 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion
Publication date: December 2016 Source:Regulatory Toxicology and Pharmacology, Volume 82 Author(s): Bapi Gorain, Hira Choudhury, Rakesh Kumar Tekade, Saumen Karan, P. Jaisankar, Tapan Kumar Pal Poor aqueous solubility and unfavourable de-esterification of olmesartan medoxomil (a selective angiotensin II receptor blocker), results in low oral bioavailability of less than 26%. Improvement of oral bioavailability with prolonged pharmacodynamics activity of olmesartan in Wistar rats had been approached by nanoemulsification strategy in our previous article [Colloid Surface B, 115, 2014: 286]. In continuation to that work, we ...
Source: Regulatory Toxicology and Pharmacology - November 7, 2016 Category: Toxicology Source Type: research

Olmesartan Prevented Intra-articular Inflammation Induced by Zymosan in Rats.
The objective of this study was to study the effect of olmesartan medoxomil (OLM), an antihypertensive drug, on intra-articular inflammation induced by zymosan (Zy) in Wistar rats. Intra-articular inflammation was induced in the right knees of rats by 1 mg Zy dissolved in saline. The animals were divided into the following groups: saline only (oral saline and intra-articular saline); Zy only (intra-articular Zy and oral saline), and intra-articular Zy and oral OLM (5, 15, or 30 mg/kg) or diclofenac sodium (SD; 100 mg/kg). Twenty-four hours after Zy injection, synovial fluid was collected for total leuk...
Source: Biological and Pharmaceutical Bulletin - November 4, 2016 Category: Drugs & Pharmacology Authors: Guerra GC, de Menezes MS, de Araújo AA, de Araújo Júnior RF, de Medeiros CA Tags: Biol Pharm Bull Source Type: research

Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion.
Abstract Poor aqueous solubility and unfavourable de-esterification of olmesartan medoxomil (a selective angiotensin II receptor blocker), results in low oral bioavailability of less than 26%. Improvement of oral bioavailability with prolonged pharmacodynamics activity of olmesartan in Wistar rats had been approached by nanoemulsification strategy in our previous article [Colloid Surface B, 115, 2014: 286]. In continuation to this work, we herewith report the biodistribution behaviour and 28-day repeated dose subchronic toxicity of olmesartan medoxomil nanoemulsion in Wistar rats following oral administration. The...
Source: Regulatory Toxicology and Pharmacology : RTP - November 1, 2016 Category: Toxicology Authors: Gorain B, Choudhury H, Tekade RK, Karan S, Jaisankar P, Pal TK Tags: Regul Toxicol Pharmacol Source Type: research

Assessment of the Cardiovascular Risk of Olmesartan Medoxomil-Based Treatment: Meta-Analysis of Individual Patient Data
AbstractIntroductionResults from two long-term studies (ROADMAP and ORIENT) indicated a numerical imbalance in the number of cardiovascular deaths between the olmesartan medoxomil (OM) and placebo groups.ObjectiveOur objective was to conduct an individual patient data meta-analysis to provide more complete information regarding OM-associated cardiovascular risks and/or benefits.MethodsWe created an integrated database based on 191 clinical trials from the OM development program. Events were identified and adjudicated by an independent, blinded clinical events committee. The incidence of major cardiovascular events and tota...
Source: American Journal of Cardiovascular Drugs - August 26, 2016 Category: Cardiology Source Type: research

Byvalson - A Beta Blocker/ARB Combination for Hypertension
Date: September 12, 2016 Issue #:  1503Summary:  The FDA has approvedByvalson (Allergan), a fixed-dose combination of the beta blocker nebivolol(Bystolic) and the angiotensin receptor blocker (ARB) valsartan (Diovan, and generics), for treatment of hypertension. It is the only combination product that contains nebivolol, and the first to combine a beta blocker with an ARB. (Source: The Medical Letter)
Source: The Medical Letter - August 24, 2016 Category: Drugs & Pharmacology Authors: admin Tags: ACE inhibitors Amlodipine Angiotensin receptor blockers Atacand Atenolol Avalide azilsartan Azor Bendroflumethiazide Benicar Beta blockers Bisoprolol Bystolic Byvalson Chlorthalidone Corzide Diovan Diuretics Edarbyclor Source Type: research

Population Pharmacokinetic Modeling of Olmesartan, the Active Metabolite of Olmesartan Medoxomil, in Patients with Hypertension
ConclusionThe final population pharmacokinetic model was demonstrated to be appropriate and effective and it can be used to assess the pharmacokinetic parameters of olmesartan in Indian patients with hypertension. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - August 17, 2016 Category: Drugs & Pharmacology Source Type: research

Olmesartan medoxomil: a guide to its use as monotherapy or in fixed-dose combinations with amlodipine and/or hydrochlorothiazide
AbstractOlmesartan medoxomil (OLM)-based antihypertensive treatment is a valuable option in the treatment of patients with mild to severe hypertension, including those with difficult-to-treat disease. Once-daily OLM, as monotherapy or in combination with hydrochlorothiazide (HCT) and/or amlopidine (AML), provides blood pressure (BP) control over the entire 24-h dosing interval, reduces systolic and diastolic BP, enables patients to achieve BP goals and is generally well tolerated. In patients who require treatment with two or more antihypertensives, treatment with fixed-dose combinations (FDC) of OLM (an angiotensin II rec...
Source: Drugs and Therapy Perspectives - August 12, 2016 Category: Drugs & Pharmacology Source Type: research