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Azilsartan

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https://www.readbyqxmd.com/read/29710494/novel-angiotensin-receptor-blocker-azilsartan-induces-oxidative-stress-and-nfkb-mediated-apoptosis-in-hepatocellular-carcinoma-cell-line-hepg2
#1
Elham Ahmadian, Ahmad Yari Khosroushahi, Aziz Eftekhari, Safar Farajnia, Hossein Babaei, Mohammad Ali Eghbal
Overexpression of renin angiotensin system (RAS) components and nuclear factor-kappa B (NF-kB) has a key role in various cancers. Blockade of RAS and NF-kB pathway has been suggested to reduce cancer cell proliferation. This study aimed to investigate the role of angiotensin II and NF-kB pathway in liver hepatocellular carcinoma cell line (HepG2) proliferation by using azilsartan (as a novel Ag II antagonist) and Bay 11-7082 (as NF-kB inhibitor). HepG2 cells were treated with different concentrations of azilsartan and Bay 11-7082...
March 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29683146/effects-of-olmesartan-and-azilsartan-on-albuminuria-and-the-intrarenal-renin-angiotensin-system
#2
Takeshi Takami, Sadanori Okada, Yoshihiko Saito, Yoko Nishijima, Hiroyuki Kobori, Akira Nishiyama
Purpose: Olmesartan and azilsartan decrease blood pressure more effectively than other angiotensin receptor blockers (ARBs). ARBs additionally decrease the urinary albumin to creatinine ratio (UACR), a urinary albumin marker, and urinary angiotensinogen (u-AGT), an intrarenal renin-angiotensin system activity marker. We examined the effects of these ARBs on blood pressure, UACR, and u-AGT in patients with uncontrolled hypertension. Methods: Patients with uncontrolled hypertension treated with conventional ARBs, excluding olmesartan and azilsartan, for over 8 weeks were enrolled...
January 2018: World journal of research and review
https://www.readbyqxmd.com/read/29683095/azilsartan-and-chlorthalidone-new-powerful-fixed-dose-antihypertensive-combination
#3
Vasiliki Katsi, Eleni Athanasiadi, Costas Tsioufis, Dimitris Tousoulis
Arterial hypertension is a disease that still affects a major part of the population worldwide, and leads to fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. From the CDC statistical analysis, as regarding to United States, 1 of every 3 adults has high blood pressure, and οnly about half (54%) of them have it under control. Furthermore, all that leads to a nation cost about $46 billion each year. Efforts to find new ways to regulate arterial hypertension are therefore imperative...
April 20, 2018: Current Hypertension Reviews
https://www.readbyqxmd.com/read/29504252/long-term-efficacy-and-tolerability-of-azilsartan-medoxomil-chlorthalidone-vs-olmesartan-medoxomil-hydrochlorothiazide-in-chronic-kidney-disease
#4
George L Bakris, Lin Zhao, Stuart Kupfer, Attila Juhasz, Michie Hisada, Eric Lloyd, Suzanne Oparil
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...
April 2018: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/29504233/treatment-of-hypertension-in-ckd-patients-with-azilsartan-chlorthalidone-vs-olmesartan-hydrochlorothiazide
#5
Walter M van der Merwe
No abstract text is available yet for this article.
April 2018: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/29445520/efficacy-and-safety-of-azilsartan-medoxomil-an-angiotensin-receptor-blocker-in-korean-patients-with-essential-hypertension
#6
Attila Juhasz, Jingtao Wu, Michie Hisada, Tomoka Tsukada, Myung Ho Jeong
Background: This was a phase 3, randomized, double-blind, placebo-controlled study. Methods: Adult Korean patients with essential hypertension and a baseline mean sitting clinic systolic blood pressure (scSBP) ≥150 and ≤180 mmHg were randomized to 6-week treatment with placebo ( n  = 65), azilsartan medoxomil (AZL-M) 40 mg ( n  = 132), or AZL-M 80 mg ( n  = 131). The primary endpoint was the change from baseline to week 6 in trough scSBP. Results: The least-squares mean (standard error) change from baseline in trough scSBP in the placebo, AZL-M 40-mg, and 80-mg groups at week 6 were - 8...
2018: Clinical Hypertension
https://www.readbyqxmd.com/read/29408668/azilsartan-and-its-zn-ii-complex-synthesis-anticancer-mechanisms-of-action-and-binding-to-bovine-serum-albumin
#7
Valeria R Martínez, María V Aguirre, Juan S Todaro, Oscar E Piro, Gustavo A Echeverría, Evelina G Ferrer, Patricia A M Williams
Azilsartan is the eighth approved member of angiotensin II receptor blockers for hypertension treatment. Considering that some drugs have additional effects when administered, we studied its effects and mechanisms of action on a human lung cancer cell line A549. We have also modified the structure of the drug by complexation with Zn(II) cation and assayed the anticancer effect. The crystal structure of the new binuclear Zn(II) complex, for short [Zn2 (azil)2 (H2 O)4 ]·2H2 O (ZnAzil), was determined by X-ray diffraction methods...
April 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/29357704/correction-to-rakugi-et-al-a-phase-iii-open-label-multicenter-study-to-evaluate-the-safety-and-efficacy-of-long-term-triple-combination-therapy-with-azilsartan-amlodipine-and-hydrochlorothiazide-in-patients-with-essential-hypertension
#8
https://www.readbyqxmd.com/read/29334491/a-randomized-titrate-to-target-study-comparing-fixed-dose-combinations-of-azilsartan-medoxomil-and-chlorthalidone-with-olmesartan-and-hydrochlorothiazide-in-stage-2-systolic-hypertension
#9
William C Cushman, George L Bakris, William B White, Michael A Weber, Domenic Sica, Andrew Roberts, Eric Lloyd, Stuart Kupfer
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...
April 2018: Journal of Hypertension
https://www.readbyqxmd.com/read/29276912/-antihypertensive-efficacy-of-fixed-combination-azilsartan-medoxomil-chlorthalidone-in-patients-with-uncontrolled-arterial-hypertension
#10
Z D Kobalava, S V Villevalde, V V Kulakov
AIM: To study effects of a fixed azilsartan medoxomil/chlorthalidone combination (Edarbi Clo) on clinical, ambulatory and central blood pressure (BP) in patients with uncontrolled arterial hypertension (AH)). MATERIALS AND METHODS: Patients (n=25) with uncontrolled AH were given fixed azilsartan medoxomil/chlorthalidone combination (40 / 12.5 mg / day) for 4 weeks. After 4 weeks, in patients who did not achieve target BP levels the dose was increased up to 40 / 25 mg / day...
November 2017: Kardiologiia
https://www.readbyqxmd.com/read/29239867/effects-of-triple-combination-therapy-with-azilsartan-amlodipine-hydrochlorothiazide-on-office-home-blood-pressure-a-randomized-controlled-trial-in-japanese-essential-hypertensive-patients
#11
Hiromi Rakugi, Kohei Shimizu, Yuhei Sano, Yuya Nishiyama, Yoshinobu Kinugawa, Souhei Terashio
OBJECTIVE: The efficacy and safety of triple therapy with azilsartan (AZI), amlodipine besylate (AML), and hydrochlorothiazide (HCTZ) compared with dual therapy with AZI/AML or HCTZ monotherapy were evaluated in Japanese essential hypertensive patients in a double-blinded manner. PATIENTS AND METHODS: A total of 353 patients with office blood pressure (BP) of at least 150/95 mmHg were randomized to a 10-week treatment with AZI/AML/HCTZ 20/5/12.5 mg, AZI/AML/HCTZ 20/5/6...
April 2018: Blood Pressure Monitoring
https://www.readbyqxmd.com/read/29238433/improvement-of-diurnal-blood-pressure-variation-by-azilsartan
#12
Keisuke Okamura, Kazuyuki Shirai, Tetsu Okuda, Hidenori Urata
Background: Azilsartan is an angiotensin II receptor blocker with a potent antihypertensive effect. Methods: In a multicenter, prospective, open-label study, 265 patients with poor blood pressure control despite treatment with other angiotensin II receptor blockers were switched to 20 mg/day of azilsartan (patients on standard dosages) or 40 mg/day of azilsartan (patients on high dosages). Results: Blood pressure was 149/83 mm Hg before switching and was significantly reduced from 1 month after switching until final assessment (132/76 mm Hg, P < 0...
January 2018: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/29235365/a-phase-iii-open-label-multicenter-study-to-evaluate-the-safety-and-efficacy-of-long-term-triple-combination-therapy-with-azilsartan-amlodipine-and-hydrochlorothiazide-in-patients-with-essential-hypertension
#13
Hiromi Rakugi, Kohei Shimizu, Yuya Nishiyama, Yuhei Sano, Yuusuke Umeda
PURPOSE: Patients with essential hypertension who are receiving treatment with an angiotensin II receptor blocker and a calcium channel blocker often develop inadequate blood pressure (BP) control and require the addition of a diuretic. This study aimed to evaluate the long-term safety and efficacy of a triple combination therapy with 20 mg azilsartan (AZL), 5 mg amlodipine (AML) and 12.5 mg hydrochlorothiazide (HCTZ). MATERIALS AND METHODS: The phase III, open-label, multicenter study (NCT02277691) comprised a 4-week run-in period and 52-week treatment period...
December 13, 2017: Blood Pressure
https://www.readbyqxmd.com/read/28974844/effects-of-azilsartan-aliskiren-or-their-combination-on-high-fat-diet-induced-non-alcoholic-liver-disease-model-in-rats
#14
Saad Abdulrahman Hussain, Rabab Mohammed Utba, Ajwad Muhammad Assumaidaee
INTRODUCTION: In addition to its role in regulation of blood pressure, fluid and electrolyte homeostasis, the renin-angiotensin system (RAS) components were expressed in many other tissues suggesting potential roles in their functions. AIM: The present study aims to evaluate the protective effect aliskiren, when used alone or in combination with azilsartan against high fat diet-induced liver disease in rats. MATERIAL AND METHODS: Thirty-two Wistar male rats, weighing 150-200 gm were allocated evenly into four groups and treated as follow: group I, rats were fed a specially formulated high-fat diet for 8 weeks to induce non-alcoholic liver disease and considered as control group; groups II, III and IV, the rats were administered azilsartan (0...
August 2017: Medical Archives
https://www.readbyqxmd.com/read/28966324/association-between-blood-pressure-lowering-and-quality-of-life-by-treatment-of-azilsartan
#15
MULTICENTER STUDY
Nobuharu Fujiwara, Atsushi Tanaka, Atsushi Kawaguchi, Motoko Tago, Jun-Ichi Oyama, Yasufumi Uchida, Kazuo Matsunaga, Kazuo Moroe, Shigeru Toyoda, Teruo Inoue, Hideo Ikeda, Koichi Node
The authors assessed the effects of switching from a conventional angiotensin II receptor blocker (ARB) to azilsartan on blood pressure (BP) and health-related quality of life (HR-QOL) in patients with uncontrolled hypertension. Key eligibility criteria were uncontrolled hypertension treated for ≥ 1 month with an ARB, excluding azilsartan, that did not reach the target BP. We recruited 147 patients (64 males and 83 females; mean ± standard deviation age 73 ± 15 years). Azilsartan reduced both systolic and diastolic BP significantly, from 151 ± 16/82 ± 12 to 134 ± 17/73 ± 12 mm Hg, 3 months after switching...
October 21, 2017: International Heart Journal
https://www.readbyqxmd.com/read/28948575/comparative-pharmaceutical-evaluation-of-candesartan-and-candesartan-cilexetil-physicochemical-properties-in-vitro-dissolution-and-ex-vivo-in-vivo-studies
#16
Ahmed M Amer, Ahmed N Allam, Ossama Y Abdallah
The aim of the present work is to answer the question is it possible to replace the ester prodrug candesartan cilexetil (CC) by its active metabolite candesartan (C) to bypass the in vivo variable effect of esterase enzymes. A comparative physicochemical evaluation was conducted through solubility, dissolution, and stability studies; additionally, ex vivo permeation and in vivo studies were assessed. C demonstrated higher solubility over CC at alkaline pH. Moreover, dissolution testing using the pharmacopeial method showed better release profile of C even in the absence of surfactant in the testing medium...
February 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28789938/azilsartan-ameliorates-diabetic-cardiomyopathy-in-young-db-db-mice-through-the-modulation-of-ace-2-ang-1-7-mas-receptor-cascade
#17
Vijayakumar Sukumaran, Hirotsugu Tsuchimochi, Eisuke Tatsumi, Mikiyasu Shirai, James T Pearson
Hyperglycemia up-regulates intracellular angiotensin II (ANG-II) production in cardiac myocytes. This study investigated the hemodynamic and metabolic effects of azilsartan (AZL) treatment in a mouse model of diabetic cardiomyopathy and whether the cardioprotective effects of AZL are mediated by the angiotensin converting enzyme (ACE)-2/ANG 1-7/Mas receptor (R) cascade. Control db/+ and db/db mice (n=5 per group) were treated with vehicle or AZL (1 or 3mg/kg/d oral gavage) from the age of 8 to 16weeks. Echocardiography was then performed and myocardial protein levels of ACE-2, Mas R, AT1 R, AT2 R, osteopontin, connective tissue growth factor (CTGF), atrial natriuretic peptide (ANP) and nitrotyrosine were measured by Western blotting...
November 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28750149/single-center-evaluation-of-the-pharmacokinetics-and-safety-of-the-angiotensin-ii-receptor-antagonist-azilsartan-medoxomil-in-mild-to-moderate-hepatic-impairment
#18
Caroline Dudkowski, Aziz Karim, Zhen Zhao, Alberto B Alonso, Dyal Garg, Richard A Preston
Azilsartan medoxomil (AZL-M) is a potent angiotensin II receptor blocker that decreases blood pressure in a dose-dependent manner. It is a prodrug that is not detected in blood after its oral administration because of its rapid hydrolysis to the active moiety, azilsartan (AZL). AZL undergoes further metabolism to the major metabolite, M-II, and minor metabolites. The objective of this study was to determine the effect of mild to moderate hepatic impairment on the pharmacokinetics of AZL and its major metabolite...
January 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28681550/comparison-of-long-term-safety-of-fixed-dose-combinations-azilsartan-medoxomil-chlorthalidone-vs-olmesartan-medoxomil-hydrochlorothiazide
#19
Joel M Neutel, William C Cushman, Eric Lloyd, Bruce Barger, Alison Handley
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...
September 2017: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/28611863/effect-of-azilsartan-on-day-to-day-variability-in-home-blood-pressure-a-prospective-multicenter-clinical-trial
#20
Toru Miyoshi, Ryoji Suetsuna, Naoto Tokunaga, Masayasu Kusaka, Ryuichiro Tsuzaki, Kazuya Koten, Kohno Kunihisa, Hiroshi Ito
BACKGROUND: The blood pressure variability (BPV) such as visit-to-visit, day-by-day, and ambulatory BPV has been also shown to be a risk of future cardiovascular events. However, the effects of antihypertensive therapy on BPV remain unclear. The purpose of this study was to evaluate the effect of azilsartan after switching from another angiotensin II receptor blocker (ARB) on day-to-day BPV in home BP monitoring. METHODS: This prospective, multicenter, open-labeled, single-arm study included 28 patients undergoing treatment with an ARB, which was switched to azilsartan after enrollment...
July 2017: Journal of Clinical Medicine Research
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