Juliane Bolbrinker, Matthias Huber, Jürgen Scholze, Reinhold Kreutz,
... this study was to investigate any influence on olmesartan plasma pharmacokinetics from amlodipine or atenolol. We analysed pharmacokinetics and safety of olmesartan medoxomil in combination with either amlodipine or atenolol ... received once daily treatment for 7 days with olmesartan medoxomil 20 mg alone or with amlodipine 5 ... daily replaced amlodipine. Concentration vs. time profiles for olmesartan monotherapy were similar to combination therapy. Mean olmesartan AUC ss,τ for olmesartan alone and with ...
Tópico(s): Sodium Intake and Health
2009 - Wiley | Fundamental and Clinical Pharmacology
Yasuo Iwasaki, Yasumitsu Ichikawa, Osamu Igarashi, Masao Kinoshita, Ken Ikeda,
Olmesartan is a novel compound which has been shown to exhibit various neuropharmacological effects. For the purpose of clarifying the effect of Olmesartan on spinal motor neurons, we studied the following tests. We studied the effect in vitro of Olmesartan on neurite outgrowth and choline acetyltransferase (ChAT) activity ... of ventral spinal cord (VSCC) of fetal rats. Olmesartan-treated VSCC, compared with control VSCC, had a ... between activity of ChAT and given doses of Olmesartan. We examined in vivo the effect of Olmesartan ...
Tópico(s): Neurogenetic and Muscular Disorders Research
2002 - Taylor & Francis | Neurological Research
Klaus O. Stumpe, Malte Ludwig,
The therapeutic profile of olmesartan medoxomil, which is a recently developed angiotensin II (A II) receptor blocker, has been compared with four commonly used antihypertensive ... compare the efficacy of individually optimised dosages of olmesartan medoxomil and the comparator agent. The primary efficacy ... in trough mean sitting diastolic blood pressure (DBP). Olmesartan medoxomil (10–20 mg once daily (o.d.)) ... d., in patients with moderate-to-severe hypertension. Olmesartan medoxomil (20–40 mg o.d.) was also ...
Tópico(s): Sodium Intake and Health
2002 - Springer Nature | Journal of Human Hypertension
Joel M. Neutel, W.J. Elliott, Joseph L. Izzo, Chao L. Chen, Harvey N. Masonson,
Olmesartan medoxomil is a new angiotensin II receptor blocker. In this randomized, double‐blind, placebo‐controlled study, the efficacy and safety of olmesartan medoxomil was assessed in 334 patients with moderate ... to receive placebo; 5, 20, or 80 mg olmesartan medoxomil q.d.; or 2.5, 10, or 40 mg olmesartan medoxomil b.i.d. Ambulatory and cuff blood ... and after 8 weeks of treatment. Treatment with olmesartan medoxomil resulted in a significant placebo‐adjusted reduction ... peak ratios of the q.d. doses of olmesartan medoxomil ranged from 57%–70%, indicating 24‐hour ...
Tópico(s): Hormonal Regulation and Hypertension
2002 - Wiley | Journal of Clinical Hypertension
Makoto Mizuno, Toshio Sada, Mikio Kato, Hiroyuki Koike,
... of diabetic nephropathy, we examined the effects of olmesartan medoxomil (olmesartan), an angiotensin II type 1 (AT1) specific ARB, ... type 2 diabetes. We used 2 doses of olmesartan, a sub-antihypertensive dose and an antihypertensive dose, ... effects on the kidney without lowering blood pressure. Olmesartan mixed in the diet at a concentration of ... glucose and insulin concentrations were not affected by olmesartan, and blood pressure was lowered only by the high dose of olmesartan. Progressive proteinuria in ZDF rats was greatly (about ...
Tópico(s): Hormonal Regulation and Hypertension
2002 - Springer Nature | Hypertension Research
Nobuya Kurikawa, Miwa Suga, Shoko Kuroda, Keisuke Yamada, H Ishikawa,
... angiotensin II type 1 (AT 1 ) receptor antagonist, olmesartan medoxomil (olmesartan), on the fibrogenic responses in rat hepatic stellate cells (HSCs) and liver fibrogenesis. Olmesartan (1 mg kg −1 per day) was orally ... 1 (TGF‐ β 1) were significantly reduced by olmesartan treatment, suggesting that olmesartan improved liver fibrosis. Interestingly, AT 1 receptors were ... in bile duct‐ligated rats by immunohistochemical analysis. Olmesartan treatment reduced the number of these cells. In ... tissue growth factor (CTGF), in rat primary HSCs. Olmesartan blocked all these effects of Ang II. Based ...
Tópico(s): Liver Disease Diagnosis and Treatment
2003 - Wiley | British Journal of Pharmacology
Stephanie F. Gardner, Amy M. Franks,
... the pharmacology, pharmacokinetics, efficacy, and adverse effects of olmesartan medoxomil, an angiotensin II receptor antagonist for the ... language medical literature. Search terms included CS-866, olmesartan, olmesartan medoxomil, RNH-6270 (active metabolite of olmesartan), Benicar, angiotensin receptors, and antihypertensive agents. In addition, ... reviewed literature identified in the searches. Studies evaluating olmesartan (i.e., abstracts, clinical trials, data on file ... identified from data sources with pertinent information regarding olmesartan medoxomil were evaluated, and all information deemed relevant ...
Tópico(s): Sodium Intake and Health
2003 - SAGE Publishing | Annals of Pharmacotherapy
Olmesartan medoxomil is a new angiotensin-II receptor antagonist for the treatment of hypertension. Olmesartan medoxomil is a pro-drug that is de-esterified to the active metabolite, olmesartan. Olmesartan has a dual method of elimination, with about ... excretion pathway can compensate for the compromised one. Olmesartan is not metabolized by the cytochrome P450 enzyme ... on multiple drug regimens, such as the elderly. Olmesartan is well tolerated and has an excellent safety ... is comparable to that of placebo. In addition, olmesartan provides 24-h blood pressure control with a ...
Tópico(s): Pharmacogenetics and Drug Metabolism
2003 - Lippincott Williams & Wilkins | Journal of Hypertension
... become important in the management of cardiovascular disease. Olmesartan medoxomil (CS-866) is the newest selective angiotensin ... effect profile, drug-interaction potential, and dosing of olmesartan medoxomil. The results of relevant clinical efficacy and ... EMBASE (1990-2002) were searched using the terms olmesartan medoxomil, CS-866, angiotensin II-receptor blocker, and hypertension.Olmesartan medoxomil has been reported to be an effective ... as early as 2 weeks and persisted when olmesartan medoxomil was administered long term (for 1 year). ...
Tópico(s): Renin-Angiotensin System Studies
2003 - Elsevier BV | Clinical Therapeutics
Shashank Rohatagi, James Lee, Magdy Shenouda, S. J. Haworth, Mohinder S. Bathala, Mark Allison, Igor Rubets, Reinilde Heyrman, Robert J. Noveck, Daniel E. Salazar,
The pharmacokinetics of amlodipine and olmesartan in healthy volunteers after coadministration of amlodipine besylate and olmesartan medoxomil concomitantly as separate dosage forms and together in a fixed‐ ... The mean steady‐state pharmacokinetics of amlodipine and olmesartan were similar when olmesartan medoxomil 40 mg/day and amlodipine 10 mg/ ... The total and maximum exposure to amlodipine and olmesartan after administration of fixed‐dose combination amlodipine/olmesartan medoxomil 10 mg/40 mg was bioequivalent to ...
Tópico(s): Potassium and Related Disorders
2008 - Wiley | The Journal of Clinical Pharmacology
Xian Wu Cheng, Toyoaki Murohara, Masafumi Kuzuya, Hideo Izawa, Takeshi Sasaki, Koji Obata, Kohzo Nagata, Takao Nishizawa, Masakazu Kobayashi, Takashi Yamada, Weon Kim, Kohji Sato, Guo‐Ping Shi, Kenji Okumura, Mitsuhiro Yokota,
... cathepsin inhibitor E64d, or the angiotensin receptor blocker olmesartan from 12 to 19 weeks of age. Cathepsin ... increased in the left ventricle of HF rats; olmesartan inhibited these effects, restored the balance between elastin ... lamina of coronary arteries of HF rats. Furthermore, olmesartan inhibited up-regulation of NADPH oxidase subunits and ... as well as superoxide generation. These effects of olmesartan were mimicked by E64d and were accompanied by amelioration of cardiac fibrosis. Finally, olmesartan and apocynin reduced angiotensin II-induced increases in ...
Tópico(s): Renin-Angiotensin System Studies
2008 - Elsevier BV | American Journal Of Pathology
Roberto Fogari, Annalisa Zoppi, Amedeo Mugellini, Paola Preti, Maurizio Destro, Andrea Rinaldi, Giuseppe Derosa,
... of adding hydrochlorothiazide (HCTZ) 12.5 mg to olmesartan 20 mg or telmisartan 80 mg on blood ... monotherapy. Of these, 35 patients (56%) in the olmesartan group and 33 (52%) in the telmisartan group ... end of monotherapy, the 52 patients in the olmesartan group and the 49 patients in the telmisartan ... py (SBP: 145.3 [6.1] in the olmesartan group and 140.1 [6.4] in the ... 05; DBP: 88.1 [5.1] in the olmesartan group and 84.9 [4.9] in the ... was significantly greater than that observed in the olmesartan/HCTZ-treated patients (18.8 [9.8]/12. ...
Tópico(s): Sodium Intake and Health
2008 - Elsevier BV | Current Therapeutic Research
Riya Nagata, Kiyokazu Kawabe, Ken Ikeda,
We evaluated the effects of olmesartan, an angiotensin II receptor blocker (ARB), on cerebral blood flow (CBF) in elderly and hypertensive subjects. Ten subjects with first- or ... before and after a 24-week course of olmesartan. Mean systolic blood pressure (SBP) was 156.2± ... previous history of stroke or cardiovascular disease. Before olmesartan administration, the hypertensive subjects had approximately 15% less ... in the frontal, parietal, temporal, and posterior lobes. Olmesartan treatment significantly decreased SBP to 130.4±4. ...
Tópico(s): Hormonal Regulation and Hypertension
2010 - Elsevier BV | Journal of Stroke and Cerebrovascular Diseases
Francisco Javier Martínez-Martín, H. Rodriguez-Rosas, Inmaculada Peiró, P. Soriano-Perera, P. Pedrianes-Martin, Cristina Comi-Diaz,
We studied the effects of treatment with olmesartan/amlodipine and olmesartan/hydrochlorothiazide on inflammatory and metabolic parameters (including new-onset diabetes as a secondary endpoint) in non-diabetic hypertensive patients with ... stage I and II hypertension were randomized to olmesartan 20 mg/amlodipine 5 mg or olmesartan 20 mg/hydrochlorothiazide 12.5 mg. If target ... Reductions in albuminuria were also similar (50%). Only olmesartan/amlodipine reduced the insulin resistance index (24%, P< ... of new-onset diabetes was significantly lower with olmesartan/amlodipine (P=0.02). Both olmesartan-based combinations ...
Tópico(s): Sodium Intake and Health
2010 - Springer Nature | Journal of Human Hypertension
Hiromichi Fukushima, Naohiko Kobayashi, Hiroshi Takeshima, Wataru Koguchi, Toshihiko Ishimitsu,
... system. We investigated whether angiotensin II receptor blocker olmesartan could improve cardiac function associated with apelin/APJ ... DS rats were treated with (1) vehicle, (2) olmesartan, and (3) olmesartan plus L-NAME for 7 weeks. Decreased end- ... shortening in failing rats were significantly ameliorated by olmesartan. Increased atherosclerosis and vascular remodeling and fibrosis factors ... fibronectin expression in DS rats were inhibited by olmesartan. Downregulation of apelin and APJ expression and phosphorylation ...
Tópico(s): Nuclear Receptors and Signaling
2010 - Lippincott Williams & Wilkins | Journal of Cardiovascular Pharmacology
Wangde Dai, Sharon L. Hale, Gregory L. Kay, Aarne J. Jyrala, Robert A. Kloner,
We determined the effects of olmesartan on infarct size and cardiac function in a rat ischemia/reperfusion model. Rats underwent 30 min of left coronary artery (CA) ... min after CA occlusion (Group 1, n = 15); olmesartan (0.3 mg/kg) at 10 min after ... before CA reperfusion (Group 3, n = 15); or olmesartan (0.3 mg/kg) 5 min before CA ... before CA reperfusion (Group 5, n = 21); or olmesartan (3 mg/kg) at 5 min before CA ... and infarct size were determined. In protocol 1, olmesartan (0.3 mg/kg) did not affect blood ... no‐reflow or infarct size. In protocol 2, olmesartan (3 mg/kg) significantly reduced infarct size to ...
Tópico(s): Renin-Angiotensin System Studies
2010 - Wiley | Cardiovascular Therapeutics
Mutsumi Iwamoto, Satoshi Hirohata, Hiroko Ogawa, Takashi Ohtsuki, Ryoko Shinohata, Toru Miyoshi, Faruk O Hatipoglu, Shozo Kusachi, Kazuhide Yamamoto, Yoshifumi Ninomiya,
... receptor would reduce CTGF expression. Accordingly, we administered olmesartan and compared its effects with other antihypertensive drugs ... was determined in a rat PO model, and olmesartan, hydralazine or saline was continuously administered. The effects of olmesartan on CTGF induction, myocyte hypertrophy and fibrosis were evaluated. The effect of olmesartan on cardiac function was also examined in CTGF- ... blood pressure was not significantly different in the olmesartan and hydralazine groups, but olmesartan treatment reduced CTGF ...
Tópico(s): Connective tissue disorders research
2010 - Springer Nature | Hypertension Research
Keisuke Shimada, Toshinori Murayama, Masataka Yokode, Tomoko Kita, Masatoshi Fujita, Chiharu Kishimoto,
... hemodynamic actions. Accordingly, we assessed the hypothesis that olmesartan, a novel AT1 receptor antagonist, reduced the severity ... Mice were intraperitoneally treated with an injection of olmesartan (1 mg/kg/day) daily over 8 weeks, ... Blood pressure was not changed significantly by the olmesartan treatment. Fatty streak plaque developed in apo E- ... mice, and was suppressed in mice that received olmesartan. In addition, olmesartan reduced not only superoxide production but the overload ... no significant differences in serum lipid levels between olmesartan-treated and -untreated groups. In vitro study showed ...
Tópico(s): Hormonal Regulation and Hypertension
2010 - Elsevier BV | Nutrition Metabolism and Cardiovascular Diseases
Vijayakumar Sukumaran, Kenichi Watanabe, Punniyakoti T. Veeraveedu, Rajarajan A. Thandavarayan, Narasimman Gurusamy, Meilei Ma, Kenichi Yamaguchi, Kenji Suzuki, Makoto Kodama, Yoshifusa Aizawa,
... remain unknown. Hence, we investigated the effect of olmesartan on myocardial remodeling in a rat model in ... divided into two groups and treated with either olmesartan (10 mg/kg/d) or vehicle. Age-matched ... weeks of treatment, we investigated the effects of olmesartan on cardiac function, inflammatory cytokines and cardiac remodeling ... analyses were significantly improved by the treatment with olmesartan compared with those of vehicle-treated rats. Olmesartan significantly reduced cardiac fibrosis as well as hypertrophy ...
Tópico(s): Cardiac Fibrosis and Remodeling
2010 - SAGE Publishing | Experimental Biology and Medicine
Yoshihiro Kiya, Shin-ichiro Miura, Masahiro Fujino, Satoshi Imaizumi, Sadashiva S. Karnik, Keijiro Saku,
... angiotensin II type 1 (AT1) receptor blocker (ARB) olmesartan has two important interactions to evoke inverse agonism ( ... domain (DCD).” Since the clinical pharmacotherapeutic relevance of olmesartan is still unclear, we examined these effects in ... treatment regimens at age 16 to 21 weeks: olmesartan (2 mg/kg/day) with DCD, a compound related to olmesartan without DCD (6 mg/kg/day, R-239470) ... placebo. We also compared the depressor effects of olmesartan to those of other ARBs in patients with ... outpatients who had been receiving ARBs other than olmesartan were recruited for this study. Our protocol was ...
Tópico(s): Hormonal Regulation and Hypertension
2010 - Informa | Clinical and Experimental Hypertension
Akihiro Yamada, Kazuya Maeda, Emi Kamiyama, Daisuke Sugiyama, Tsunenori Kondo, Yoshiyuki Shiroyanagi, Hayakazu Nakazawa, Teruo Okano, Masashi Adachi, John D. Schuetz, Yasuhisa Adachi, Zhuohan Hu, Hiroyuki Kusuhara, Yuichi Sugiyama,
Olmesartan, a novel angiotensin II AT1-receptor antagonist, is excreted into both bile and urine, with minimal metabolism. Because olmesartan is a hydrophilic anionic compound, some transporters could ... of human drug transporters in the pharmacokinetics of olmesartan and determined the contribution of each transporter to the overall clearance of olmesartan. Olmesartan was significantly taken up into human embryonic kidney ... of OATP1B1 and OATP1B3 to the uptake of olmesartan in human hepatocytes were almost the same, whereas ...
Tópico(s): Pharmacogenetics and Drug Metabolism
2007 - American Society for Pharmacology and Experimental Therapeutics | Drug Metabolism and Disposition
Klaus O. Stumpe, Enrico Agabiti‐Rosei, Tomasz Zieliński, D. Schremmer, Jürgen Scholze, Petra Laeis, P. Schwändt, Malte Ludwig,
Objective The Multicentre Olmesartan atherosclerosis Regression Evaluation (MORE) study was a double-blind trial in patients with hypertension at increased cardiovascular risk with ... of a 2-year treatment based on either olmesartan medoxomil or atenolol on common carotid (CC) intima- ... 90—105 mmHg) were randomized to receive either olmesartan (20—40 mg/day) or atenolol (50—100 ... by 3D US and blood pressure (BP). Results Olmesartan and atenolo produced comparable significant reductions in CC- ... SEM) was -0.090 (0.015) mm for oLmesartan and -0.082 (0.014) mm for atenolol. ...
Tópico(s): Cerebrovascular and Carotid Artery Diseases
2007 - SAGE Publishing | Therapeutic Advances in Cardiovascular Disease
Matthias Barton, Matthias R. Meyer, Eric R. Prossnitz,
... Chappell et al8 found that the AT1 antagonist olmesartan is as effective as 17β-estradiol to suppress ... with atherosclerosis, neither low-dose 17β-estradiol nor olmesartan had an effect on its own on atherosclerotic ... in the protective effects of the AT1 antagonist olmesartan on cerebral infarct size and the cellular changes ... the study by Shimada et al10 were that olmesartan treatment not only reduced infarct size but that these effects of olmesartan were estrogen receptor dependent, that is, olmesartan increased ...
Tópico(s): Nuclear Receptors and Signaling
2011 - Lippincott Williams & Wilkins | Hypertension
... this study was to compare the effects of olmesartan combined with either azelnidipine or amlodipine on central ... mmHg and/or diastolic BP ≥ 90 mmHg received olmesartan monotherapy (20 mg daily) for 12 weeks. The ... in CBP and LVMI were significantly greater with olmesartan/azelnidipine than with olmesartan/amlodipine (CBP, P < 0.001; LVMI, P = 0.002). Conclusions: These findings indicate that olmesartan/azelnidipine had greater effects on CBP and LVMI than did olmesartan/amlodipine, even though the reduction in brachial BP ...
Tópico(s): Heart Rate Variability and Autonomic Control
2011 - Dove Medical Press | Vascular Health and Risk Management
Keiji Kusumoto, Hideki Igata, Mami Ojima, Ayako Tsuboi, Mitsuaki Imanishi, Fuminari Yamaguchi, Hiroki Sakamoto, Takanobu Kuroita, Naohiro Kawaguchi, Nobuhiro Nishigaki, Hideaki Nagaya,
... that of the potent angiotensin II receptor blocker olmesartan medoxomil. Azilsartan, the active metabolite of azilsartan medoxomil, ... h after oral administration. The inhibitory effects of olmesartan medoxomil disappeared within 24 h. ID50 values were ... 0.55 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. In conscious spontaneously hypertensive rats (SHRs), ... Oral administration of 0.1–3 mg/kg olmesartan medoxomil also reduced blood pressure; however, only the ... 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. In renal hypertensive dogs, oral administration ...
Tópico(s): Receptor Mechanisms and Signaling
2011 - Elsevier BV | European Journal of Pharmacology
Yayoi Nishida, Yasuo Takahashi, Tomohiro Nakayama, Masayoshi Soma, Satoshi Asai,
Abstract Background Angiotensin II receptor blockers (ARBs), including olmesartan and candesartan, are widely used antihypertensive agents. Many ... vasculoprotection and renoprotection. However, the effect of prolonged olmesartan monotherapy on lipid metabolism in patients with hypertension ... retrospective observational study to compare the effects of olmesartan with those of candesartan, focusing on lipid metabolism ... Feb 28, 2011, to identify cohorts of new olmesartan users (n = 168) and candesartan users (n = 266). ...
Tópico(s): Sodium Intake and Health
2011 - BioMed Central | Cardiovascular Diabetology
... channel blocker (CCB). Fixed-dose combination formulations of olmesartan medoxomil, an ARB, and the CCB amlodipine are ... European countries for patients with essential hypertension. The olmesartan/amlodipine combination has demonstrated greater efficacy than its ... baseline and after eight weeks of treatment with olmesartan/amlodipine, compared with equivalent doses of olmesartan or amolodipine monotherapy ( P < 0.001), in the factorial Combination of Olmesartan Medoxomil and Amlodipine Besylate in Controlling High Blood ...
Tópico(s): Sodium Intake and Health
2011 - Dove Medical Press | Vascular Health and Risk Management
Jun Agata, Nobuyuki Ura, Hideaki Yoshida, Yasuyuki Shinshi, Haruki Sasaki, Masaya Hyakkoku, Shinya Taniguchi, Kazuaki Shimamoto,
... that long-term treatment of hypertensive patients with olmesartan resulted in a reduction in plasma Ang II ... 1-7). It has recently been reported that olmesartan increases plasma Ang-(1-7) through an increase ... Ang II level and the cardioprotective effect of olmesartan. Administration of 0.5 mg/kg/day of olmesartan for 4 weeks to 12-week-old stroke- ... in SHRSP given a vehicle. Co-administration of olmesartan and (D-Ala7)−Ang-(1-7), a selective ... 1-7) antagonist, partially inhibited the effect of olmesartan on blood pressure and left ventricular weight. Interestingly, ...
Tópico(s): Apelin-related biomedical research
2006 - Springer Nature | Hypertension Research
Shin-ichiro Miura, Masahiro Fujino, Hiroyuki Hanzawa, Yoshihiro Kiya, Satoshi Imaizumi, Yoshino Matsuo, Sayo Tomita, Yoshinari Uehara, Sadashiva S. Karnik, Hiroaki Yanagisawa, Hiroyuki Koike, Issei Komuro, Keijiro Saku,
... molecular mechanism underlying the inverse agonist activity of olmesartan, a potent angiotensin II type 1 (AT1) receptor ... an inositol phosphate production assay. Binding affinity of olmesartan and its related compounds to wild-type and mutant AT1 receptors demonstrated that interactions between olmesartan and Tyr113, Lys199, His256, and Gln257 in the ... were important. The inositol phosphate production assay of olmesartan and related compounds using mutant receptors indicated that ... two interactions, that between the hydroxyl group of olmesartan and Tyr113 in the receptor and that between ...
Tópico(s): Neuropeptides and Animal Physiology
2006 - Elsevier BV | Journal of Biological Chemistry
Eiichiro Yamamoto, Takuro Yamashita, Tomoko Tanaka, Keiichiro Kataoka, Yoshiko Tokutomi, Zhong-Fang Lai, Yi‐Fei Dong, Shinji Matsuba, Hisao Ogawa, Shokei Kim‐Mitsuyama,
... vehicle, (2) hydralazine (5 mg/kg/d), (3) olmesartan (0.5 mg/kg/d), (4) pravastatin (100 mg/kg/d), and (5) combined olmesartan and pravastatin for 4 weeks. Olmesartan or pravastatin significantly and comparably improved vascular endothelium- ... arterial remodeling, and eNOS activity of DS rats. Olmesartan prevented vascular eNOS dimer disruption or the downregulation ... Akt phosphorylation was enhanced by pravastatin but not olmesartan, indicating differential pleiotropic effects between olmesartan and pravastatin. ...
Tópico(s): Lipoproteins and Cardiovascular Health
2006 - Lippincott Williams & Wilkins | Arteriosclerosis Thrombosis and Vascular Biology