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Azilsartan

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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
#1
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...
August 5, 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
#2
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
#3
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...
July 6, 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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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...
April 26, 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
#10
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
#11
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
#12
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
https://www.readbyqxmd.com/read/28079534/practical-efficacy-of-olmesartan-versus-azilsartan-in-patients-with-hypertension-a-multicenter-randomized-controlled-trial-muscat-4-study
#13
RANDOMIZED CONTROLLED TRIAL
Yuki Kakio, Haruhito A Uchida, Ryoko Umebayashi, Hidemi Takeuchi, Yuka Okuyama, Yoshihisa Hanayama, Jun Wada
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...
April 2017: Blood Pressure Monitoring
https://www.readbyqxmd.com/read/28013242/development-and-validation-of-a-gas-chromatography-method-for-quality-control-of-residual-solvents-in-azilsartan-bulk-drugs
#14
Jin Guan, Jie Min, Feng Yan, Wen-Ya Xu, Shuang Shi, Si-Lin Wang
A new gas chromatographic method for the simultaneous determination of six organic residual solvents (acetonitrile, tetrahydrofuran, ethanol, acetone, 2-propanol and ethyl acetate) in azilsartan bulk drug is described. The chromatographic determination was achieved on an OV-624 capillary column employing programmed temperature within 21 min. The validation was carried out according to International Conference on Harmonization validation guidelines. The method was shown to be specific (no interference in the blank solution), sensitive (Limit of detection can achieve 1...
April 1, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27829955/efficacy-and-safety-of-a-single-pill-fixed-dose-combination-of-azilsartan-and-amlodipine
#15
Kota Motozato, Shin-Ichiro Miura, Yuhei Shiga, Takaaki Kusumoto, Keijiro Saku
BACKGROUND: Guidelines for the management of hypertension recommend the use of drugs with different mechanisms of action in antihypertensive regimens that include single-pill fixed-dose combinations of medications. There is some controversy regarding which single-pill fixed-dose combinations of angiotensin II type 1 receptor blockers (ARBs) and calcium channel blockers (CCBs) are effective at reducing blood pressure (BP). METHODS: Forty hypertensive patients who were receiving a single-pill fixed-dose combination of valsartan 80 mg/day and amlodipine 5 mg/day or irbesartan 100 mg/day and amlodipine 5 mg/day were enrolled...
December 2016: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/27824680/angiotensin-ii-receptor-blockers-following-intravenous-nicardipine-administration-to-lower-blood-pressure-in-patients-with-hypertensive-intracerebral-hemorrhage-a-prospective-randomized-study
#16
RANDOMIZED CONTROLLED TRIAL
Joji Inamasu, Shunsuke Nakae, Kazuhide Adachi, Yuichi Hirose
BACKGROUND AND OBJECTIVE: In patients with hypertensive intracerebral hemorrhage (HICH), intravenous nicardipine is primarily used to lower blood pressure (BP). However, there are few studies investigating the role of oral antihypertensives administered after intravenous nicardipine to prevent BP from rising. Angiotensin II receptor blockers (ARBs) may be beneficial in HICH patients not only as antihypertensives but also by lowering plasma catecholamine levels. A prospective randomized study was conducted between January 2015 and March 2016 to comparatively evaluate the efficacy of two ARBs (azilsartan vs...
February 2017: Blood Pressure Monitoring
https://www.readbyqxmd.com/read/27731574/azilsartan-novel-angiotensin-receptor-blocker
#17
Ramesh R Dargad, Jai D Parekh, Rohit R Dargad, Shweta Kukrety
OBJECTIVE: To describe the efficacy and safety profile of the new angiotensin receptor blocker (ARB), "Azilsartan Medoxomil", reviewing data available from both clinical and pre-clinical studies. MATERIAL: We completed a review of the English literature from PubMed using the keywords- azilsartan medoxomil, angiotensin receptor blockers (ARB), angiotensin converting enzyme inhibitors (ACEi) and hypertension. DATA EVALUATION: Many clinical trials have been conducted comparing the efficacy of azilsartan with other ARB's and also with the ACEi ramipril...
March 2016: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/27635180/depressor-and-anti-inflammatory-effects-of-angiotensin-ii-receptor-blockers-in-metabolic-and-or-hypertensive-patients-with-coronary-artery-disease-a-randomized-prospective-study-diamond-study
#18
Sen Adachi, Shin-Ichiro Miura, Yuhei Shiga, Tadaaki Arimura, Takashi Kuwano, Ken Kitajima, Amane Ike, Makoto Sugihara, Atsushi Iwata, Hiroaki Nishikawa, Natsumi Morito, Keijiro Saku
BACKGROUND: We compared the efficacy and safety of azilsartan to those of olmesartan in a prospective, randomized clinical trial. METHODS: Forty-four hypertensive patients who had coronary artery disease (CAD) were enrolled. We randomly assigned patients to changeover from their prior angiotensin II receptor blockers (ARBs) to either azilsartan or olmesartan, and followed the patients for 12 weeks. RESULTS: Office systolic blood pressure (SBP) in the azilsartan group was significantly decreased after 12 weeks...
October 2016: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/27558280/the-impact-of-azilsartan-medoxomil-treatment-capsule-formulation-at-doses-ranging-from-10-to-80%C3%A2-mg-significant-rapid-reductions-in-clinic-diastolic-and-systolic-blood-pressure
#19
Alfonso Perez, Charlie Cao
In this phase 2, multicenter, parallel-group, double-blind, dose-ranging study, hypertensive adults (n=449) were randomized to receive one of five doses of a capsule formulation of azilsartan medoxomil (AZL-M; 5, 10, 20, 40, 80 mg), olmesartan medoxomil (OLM) 20 mg, or placebo once daily. The primary endpoint was change in trough clinic diastolic blood pressure (DBP) at week 8. AZL-M provided rapid statistically and clinically significant reductions in DBP and systolic blood pressure (SBP) vs placebo at all doses except 5 mg...
March 2017: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/27536242/azilsartan-as-a-potent-antihypertensive-drug-with-possible-pleiotropic-cardiometabolic-effects-a-review-study
#20
REVIEW
Georgios Georgiopoulos, Vasiliki Katsi, Dimitrios Oikonomou, Georgia Vamvakou, Evangelia Koutli, Aggeliki Laina, Constantinos Tsioufis, Petros Nihoyannopoulos, Dimitrios Tousoulis
BACKGROUND: Hypertension related cardiovascular (CV) complications could be amplified by the presence of metabolic co-morbidities. Azilsartan medoxomil (AZL-M) is the eighth approved member of angiotensin II receptor blockers (ARBs), a drug class of high priority in the management of hypertensive subjects with diabetes mellitus type II (DMII). METHODS: Under this prism, we performed a systematic review of the literature for all relevant articles in order to evaluate the efficacy, safety, and possible clinical role of AZL-M in hypertensive diabetic patients...
2016: Frontiers in Pharmacology
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