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Azilsartan

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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
#1
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...
January 13, 2018: Journal of Hypertension
https://www.readbyqxmd.com/read/29276912/-antihypertensive-efficacy-of-fixed-combination-azilsartan-medoxomil-chlorthalidone-in-patients-with-uncontrolled-arterial-hypertension
#2
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
#3
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...
December 12, 2017: Blood Pressure Monitoring
https://www.readbyqxmd.com/read/29238433/improvement-of-diurnal-blood-pressure-variation-by-azilsartan
#4
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
#5
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
#6
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
#7
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
#8
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...
September 25, 2017: 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
#9
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, AT1R, AT2R, 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
#10
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...
July 27, 2017: 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
#11
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
#12
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
https://www.readbyqxmd.com/read/28576855/sodium-balance-circadian-bp-rhythm-heart-rate-variability-and-intrarenal-renin-angiotensin-aldosterone-and-dopaminergic-systems-in-acute-phase-of-arb-therapy
#13
Yukako Isobe-Sasaki, Michio Fukuda, Yoshiaki Ogiyama, Ryo Sato, Toshiyuki Miura, Daisuke Fuwa, Masashi Mizuno, Tetsuhei Matsuoka, Hiroko Shibata, Hiroyuki Ito, Minamo Ono, Sumiko Abe-Dohmae, Ken Kiyono, Yoshiharu Yamamoto, Hiroyuki Kobori, Makoto Michikawa, Junichiro Hayano, Nobuyuki Ohte
We have revealed that even in humans, activated intrarenal renin-angiotensin-aldosterone system (RAAS) enhances tubular sodium reabsorption to facilitate salt sensitivity and nondipper rhythm of blood pressure (BP), and that angiotensin receptor blocker (ARB) could increase daytime urinary sodium excretion rate (UNaV) to produce lower sodium balance and restore nondipper rhythm. However, the sympathetic nervous system and intrarenal dopaminergic system can also contribute to renal sodium handling. A total of 20 patients with chronic kidney disease (61 ± 15 years) underwent 24-h ambulatory BP monitoring before and during two-day treatment with ARB, azilsartan...
June 2017: Physiological Reports
https://www.readbyqxmd.com/read/28496022/comparison-of-efficacy-and-safety-of-azilsartan-and-olmesartan-in-patients-with-essential-hypertension
#14
RANDOMIZED CONTROLLED TRIAL
Yuhei Shiga, Shin-Ichiro Miura, Kota Motozato, Kenji Norimatsu, Masaya Yano, Yuka Hitaka, Sen Adachi, Takashi Kuwano, Ken Inoue, Asao Inoue, Kazuaki Fujisawa, Tetsuro Shirotani, Takaaki Kusumoto, Munehito Ideishi, Keijiro Saku
Many patients still have high blood pressure (BP) after treatment with angiotensin II type 1 (AT1) receptor blockers (ARBs). We compared the efficacy and safety of azilsartan to those of olmesartan in a prospective randomized clinical trial. Sixty-four hypertensive patients who were treated with ARBs other than azilsartan and olmesartan were enrolled in this study. We randomly assigned patients to changeover from their prior ARBs to either azilsartan or olmesartan, and followed the patients for 3 months. Systolic BP (SBP) in the azilsartan group was significantly decreased at 3 months, and diastolic BP (DBP) and pulse rate (PR) in the olmesartan group showed significant reductions after 3 months...
May 31, 2017: International Heart Journal
https://www.readbyqxmd.com/read/28493376/evaluation-of-the-angiotensin-ii-receptor-blocker-azilsartan-medoxomil-in-african-american-patients-with-hypertension
#15
Wallace Johnson, William B White, Domenic Sica, George L Bakris, Michael A Weber, Alison Handley, Alfonso Perez, Charlie Cao, Stuart Kupfer, Elijah B Saunders
The efficacy and safety of azilsartan medoxomil (AZL-M) were evaluated in African-American patients with hypertension in a 6-week, double-blind, randomized, placebo-controlled trial, for which the primary end point was change from baseline in 24-hour mean systolic blood pressure (BP). There were 413 patients, with a mean age of 52 years, 57% women, and baseline 24-hour BP of 146/91 mm Hg. Treatment differences in 24-hour systolic BP between AZL-M 40 mg and placebo (-5.0 mm Hg; 95% confidence interval, -8...
May 11, 2017: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/28445961/azilsartan-ameliorates-apoptosis-of-dopaminergic%C3%A2-neurons-and-rescues-characteristic-parkinsonian-behaviors-in-a-rat-model-of-parkinson-s-disease
#16
Qing Gao, Zhou Ou, Teng Jiang, You-Yong Tian, Jun-Shan Zhou, Liang Wu, Jian-Quan Shi, Ying-Dong Zhang
Loss of dopaminergic neurons within the substantia nigra (SN) is a pathological hallmark of Parkinson's disease (PD), which leads to the onset of motor symptoms. Previously, our in vitro studies revealed that Angiotensin II (Ang II) induced apoptosis of dopaminergic neurons through its type 1 receptor (AT1R), but these findings needed to be confirmed via animal experiments. Here, using a rotenone-induced rat model of PD, we observed an overactivation of Ang II/AT1R axis in the SN, since Ang II level and AT1R expression were markedly increased...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28444983/azilsartan-medoxomil-an-angiotensin-ii-receptor-antagonist-for-the-treatment-of-hypertension
#17
REVIEW
Marie Hjermitslev, Daniela G Grimm, Markus Wehland, Ulf Simonsen, Marcus Krüger
Azilsartan (AZL) medoxomil was approved by the United States Food and Drug Administration in 2011 for the treatment of hypertension and has shown promising results both in blood pressure (BP) reduction and in tolerability, but has not yet been taken into practice to the same extent as other angiotensin II receptor blockers (ARBs) that have been on the market for a longer period. AZL antagonizes the AT1 receptor for angiotensin II (ANG II), whereas angiotensin-converting enzyme inhibitors block the conversion of angiotensin I to ANG II, but not alternative routes of formation of ANG II...
October 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28382073/at1-receptor-modulator-attenuates-the-hypercholesterolemia-induced-impairment-of-the-myocardial-ischemic-post-conditioning-benefits
#18
Yun-Wei Li, Yan-Ming Li, Yan Hon, Qi-Lin Wan, Rui-Li He, Zhi-Zhong Wang, Cui-Hua Zhao
BACKGROUND AND OBJECTIVES: Ischemic post-conditioning (PostC) has been demonstrated as a novel strategy to harness nature's protection against myocardial ischemia-reperfusion (I/R). Hypercholesterolemia (HC) has been reported to block the effect of PostC on the heart. Angiotensin II type-1 (AT1) modulators have shown benefits in myocardial ischemia. The present study investigates the effect of a novel inhibitor of AT1, azilsartan in PostC of the heart of normocholesterolemic (NC) and HC rats...
March 2017: Korean Circulation Journal
https://www.readbyqxmd.com/read/28290893/-hronotherapy-aspects-of-efficiency-azilsartan-medoxomil-in-combination-therapy-in-patients-with-hypertension-and-metabolic-syndrome
#19
V V Skibitskiy, A V Fendrikova, D V Sirotenko, A V Skibitskiy
OBJECTIVE: Determination of the effectiveness and safety of different dosing regimens during the day (in the morning or at bedtime) combination therapy including azilsartan medoxomil in patients with essential hypertension and metabolic syndrome (MS). DESIGN AND METHODS: The study included 60 patients with uncontrolled hypertension and MS (age median - 59 (54-65) years). Patients were randomized in two groups: group 1 (n=30) received azilsartan medoxomil 40 mg/day, and indapamide retard 1,5 mg/day in the morning; group 2 (n=30)- azilsartan medoxomoil 40 mg at bedtime and indapamide retard 1,5 mg in the morning...
October 2016: Kardiologiia
https://www.readbyqxmd.com/read/28290827/-azilsartan-medoxomil-capabilities-in-arterial-hypertension-and-obesity
#20
Y A Vasyuk, E Y Shupenina, V V Nesvetov, E A Nesterova, E I Golubkova
Arterial hypertension (AH) is one of the most common cardiovascular disease. Angiotensin II (AT II), the hormone of renin-angiotensin-aldosterone system, realizes its negative effects through AT 1 receptors - application point of angiotensin receptor blockers (ARB). Due to different dissociation AT 1 receptors properties some ARBs are more effective than others. Multiply multicenter randomized and observational studies approve the effectiveness and safety of azilsartan medoxomil in patients with AH 1-2 grade...
December 2016: Kardiologiia
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