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Hiroyuki Koshiyama - One of the best experts on this subject based on the ideXlab platform.
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Olmesartan reduced microalbuminuria in Japanese subjects with type 2 diabetes
Diabetes research and clinical practice, 2008Co-Authors: Hiroki Ikeda, Yoshiyuki Hamamoto, Sachiko Honjo, Koichiro Nabe, Yoshiharu Wada, Hiroyuki KoshiyamaAbstract:We investigated the effect of Olmesartan on early diabetic nephropathy in hypertensive patients with type 2 diabetes by its replacement of other angiotensin II type 1 receptor blockers (ARBs) by Olmesartan. The urinary albumin/creatinine ratio significantly decreased. The present result suggests a possibility that Olmesartan may have more effect on early nephropathy than other ARBs.
Pamela Maffioli - One of the best experts on this subject based on the ideXlab platform.
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Results from a 12 months, randomized, clinical trial comparing an Olmesartan/amlodipine single pill combination to Olmesartan and amlodipine monotherapies on blood pressure and inflammation
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2013Co-Authors: Giuseppe Derosa, Arrigo F.g. Cicero, Anna Carbone, Fabrizio Querci, Elena Fogari, Angela D'angelo, Pamela MaffioliAbstract:AIM Hypertension affects nearly 1 in 3 adults in the United States, and it is an important modifiable risk factor for coronary artery disease, heart failure, renal failure, and stroke. The aim of this study was to evaluate the effects of a fixed-dose Olmesartan/amlodipine combination on blood pressure control, lipid profile, insulin sensitivity, and inflammation compared to singles monotherapies. METHODS We randomized 276 hypertensive patients to Olmesartan 20 mg, amlodipine 10mg or a single pill containing a fixed-dose Olmesartan/amlodipine combination 20/5mg for 12 months. We evaluated: body weight, body mass index (BMI), systolic and diastolic blood pressure (SBP and DBP), fasting plasma glucose (FPG), fasting plasma insulin (FPI), lipid profile, omentin, chemerin, high sensitivity C-reactive protein (Hs-CRP). At baseline, and after 6 and 12 months, patients underwent an euglycemic, hyperinsulinemic clamp to assess insulin sensitivity (M value). RESULTS Olmesartan/amlodipine combination was more effective than amlodipine or Olmesartan in reducing blood pressure. Olmesartan/amlodipine combination, but not amlodipine, decreased FPG after 12 months. Olmesartan/amlodipine combination better decreased FPI and HOMA index and increased M value compared to Olmesartan and amlodipine monotherapies. Olmesartan/amlodipine significantly decreased chemerin and omentin compared to Olmesartan and amlodipine. CONCLUSION Other than to be more effective in reducing blood pressure, Olmesartan/amlodipine single pill combination gave also a major increase of insulin sensitivity and a decrease of inflammatory markers compared to single monotherapies.
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Effects of an Olmesartan/amlodipine combination compared to Olmesartan or amlodipine monotherapies on some insulin resistance parameters in hypertensive patients
European Heart Journal, 2013Co-Authors: Giuseppe Derosa, Arrigo F.g. Cicero, Angela D'angelo, Aldo Bonaventura, Lucio Bianchi, Davide Romano, Pamela MaffioliAbstract:Purpose: To evaluate the effects of a fixed Olmesartan/amlodipine combination on blood pressure control, lipid profile, and some insulin resistance parameters compared to single monotherapies. Methods: After a 2 week wash-out period, 276 hypertensive patients were randomly assigned to Olmesartan 20 mg, amlodipine 10 mg or to a single pill containing a fixed dose of Olmesartan/amlodipine 20/5 mg for 12 months. We evaluated at baseline, after 6, and 12 months: body weight, body mass index (BMI), systolic and diastolic blood pressure (SBP and DBP, respectively), fasting plasma glucose (FPG), fasting plasma insulin (FPI), HOMA index, lipid profile, adiponectin (ADN), resistin (r), retinol binding protein-4 (RBP-4), vaspin, visfatin, omentin, and chemerin. Furthermore, at the baseline, and after 6 and 12 months, patients underwent an euglycemic, hyperinsulinemic clamp to assess M value. Results: SBP and DPB were better decreased by Olmesartan/amlodipine combination compared to amlodipine and Olmesartan monotherapies (p< 0.01 for both). No variations of lipid profile were recorded in neither of the three groups. There was a decrease of FGP with Olmesartan/amlodipine combination after 12 months compared to amlodipine monotherapy (p< 0.05). Olmesartan/amlodipine combination decreased FPI and HOMA index both compared to baseline (p< 0.05), and compared to Olmesartan and amlodipine monotherapies (p< 0.05 for both), that did not alter these parameters. The Olmesartan/amlodipine combination gave an increase of M value after 12 months, both compared to baseline (p< 0.01), to Olmesartan monotherapy (p< 0.05), and to amlodipine monotherapy (p< 0.01). Both Olmesartan, and Olmesartan/amlodipine increased ADN and reduced r (p< 0.01 vs baseline, for both), without significant differences between the two groups. Olmesartan/amlodipine gave a decrease of both visfatin and vaspin after 12 months (p< 0.05, and p< 0.01 respectively), even if no differences in group to group comparison were observed. None of treatments influenced RBP-4 levels. Finally, Olmesartan/amlodipine significantly decreased chemerin and omentin compared to single therapies (p< 0.05 for both). Conclusions: Other than to be more effective in reducing blood pressure, Olmesartan/amlodipine single pill combination gave also a major increase of insulin sensitivity and a decrease of insulin resistance parameters compared to single monotherapies.
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Variation of some inflammatory markers in hypertensive patients after 1 year of Olmesartan/amlodipine single-pill combination compared with Olmesartan or amlodipine monotherapies.
Journal of the American Society of Hypertension : JASH, 2013Co-Authors: Giuseppe Derosa, Arrigo F.g. Cicero, Anna Carbone, Fabrizio Querci, Elena Fogari, Angela D'angelo, Pamela MaffioliAbstract:The purpose of this study was to evaluate a fixed Olmesartan/amlodipine combination on blood pressure control, lipid profile, insulin sensitivity, and some inflammatory markers compared with single-drug monotherapy. A total of 276 hypertensive patients were randomly assigned to Olmesartan 20 mg, amlodipine 10 mg, or a single pill containing Olmesartan/amlodipine combination 20/5 mg for 12 months. We evaluated the following at baseline and after 6 and 12 months: body weight, body mass index, systolic (SBP) and diastolic blood pressures (DBP), fasting plasma glucose (FPG), fasting plasma insulin (FPI), lipid profile, tumor necrosis factor-a (TNF-a), retinol binding protein-4 (RBP-4), and interleukins 6 and 7 (IL-6 and IL-7). At baseline, and after 6 and 12 months, patients underwent an euglycemic, hyperinsulinemic clamp. The Olmesartan/amlodipine combination provided a greater decrease of SBP and DPB compared with amlodipine and Olmesartan monotherapies. The Olmesartan/amlodipine combination decreased FPG after 12 months compared with amlodipine monotherapy. The combination decreased FPI and homeostasis model assessment index and increased M value both compared with baseline and with Olmesartan and amlodipine monotherapies. Olmesartan/amlodipine decreased IL-7, but not IL-6, compared with single drug components. The Olmesartan/amlodipine combination is effective and safe in reducing blood pressure and has some additive effects not shown by single drugs, such as an improvement of IL-7. J Am Soc Hypertens 2013;7(1):32‐39. 2013 American
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Effects of an Olmesartan/amlodipine fixed dose on blood pressure control, some adipocytokines and interleukins levels compared with Olmesartan or amlodipine monotherapies.
Journal of clinical pharmacy and therapeutics, 2012Co-Authors: Giuseppe Derosa, Arrigo F.g. Cicero, Anna Carbone, Fabrizio Querci, Elena Fogari, Angela D'angelo, Pamela MaffioliAbstract:Summary What is known and Objective: To evaluate the effects of an Olmesartan/amlodipine single pill combination compared with Olmesartan or amlodipine monotherapies on blood pressure control, lipid profile, insulin sensitivity and some adipocytokines levels. Methods: Two hundred and seventy-six patients were enroled in the study and were randomly assigned to take Olmesartan 20 mg, amlodipine 10 mg, or a single pill containing an Olmesartan/amlodipine combination 20 mg/5 mg for 12 months. We evaluated at the baseline, and after 6 and 12 months: body weight, body mass index, systolic and diastolic blood pressure (SBP and DBP), fasting plasma glucose (FPG), fasting plasma insulin (FPI), lipid profile, adiponectin (ADN), resistin (r), interleukin-1β (IL-1β) and interleukin-5 (IL-5). At the baseline, and after 6 and 12 months, patients underwent an euglycemic, hyperinsulinemic clamp to assess insulin sensitivity (M value). Results and Discussion: There was a similar decrease in SBP and DBP after 6 and 12 months in all groups, even if Olmesartan/amlodipine combination gave a major decrease in SBP and DPB compared with amlodipine and Olmesartan monotherapies. Olmesartan/amlodipine combination decreased FPG after 12 months compared with amlodipine monotherapy. Olmesartan/amlodipine combination decreased FPI and HOMA index and increased M value both compared with baseline and compared with Olmesartan and amlodipine monotherapies. Both Olmesartan and Olmesartan/amlodipine increased ADN and reduced r, without significant differences between the two groups. Regarding interleukins, no differences emerged in group to group comparison. What is new and Conclusion: Olmesartan/amlodipine combination resulted more effective than Olmesartan and amlodipine monotherapies in reducing blood pressure, and in increasing insulin sensitivity parameters, but not resulted more effective in improving adipocytokines and interleukins levels analysed, compared with amlodipine or Olmesartan monotherapy in hypertensive patients in this double-blind, randomized clinical trial.
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Olmesartan/amlodipine combination versus Olmesartan or amlodipine monotherapies on blood pressure and insulin resistance in a sample of hypertensive patients
Clinical and experimental hypertension (New York N.Y. : 1993), 2012Co-Authors: Giuseppe Derosa, Arrigo F.g. Cicero, Anna Carbone, Fabrizio Querci, Elena Fogari, Angela D'angelo, Pamela MaffioliAbstract:Despite the wide range of antihypertensive medications, about 45.5% of treated patients fail to achieve the desired blood pressure (BP) target. This study evaluated the effects of an Olmesartan/amlodipine single pill combination compared to Olmesartan or amlodipine monotherapies on BP, lipid profile, insulin resistance, and insulin sensitivity parameters. Two hundred and seventy-six patients were randomly assigned to Olmesartan (20 mg), amlodipine (10 mg), or a single pill containing Olmesartan/amlodipine (5/20 mg) for 12 months. We evaluated the following parameters at the baseline, and after 6 and 12 months: body weight, body mass index (BMI), systolic and diastolic blood pressure (SBP and DBP), fasting plasma glucose (FPG), fasting plasma insulin (FPI), and lipid profile. At the baseline, and after 6 and 12 months, patients underwent an euglycemic, hyperinsulinemic clamp to assess M value. Olmesartan/amlodipine gave a greater decrease in SBP and DPB compared to amlodipine and Olmesartan at 6 (P < .05) ...
Hans R. Brunner - One of the best experts on this subject based on the ideXlab platform.
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Olmesartan medoxomil: current status of its use in monotherapy
Vascular health and risk management, 2006Co-Authors: Hans R. BrunnerAbstract:Olmesartan medoxomil is an angiotensin II receptor antagonist. In pooled analyses of seven randomized, double-blind trials, 8 weeks' treatment with Olmesartan medoxomil was significantly more effective than placebo in terms of the response rate, proportion of patients achieving target blood pressure (BP) and mean change from baseline in diastolic (DBP) and systolic blood pressure (SBP). Olmesartan medoxomil had a fast onset of action, with significant between-group differences evident from 2 weeks onwards. The drug was well tolerated with a similar adverse event profile to placebo. In patients with type 2 diabetes, Olmesartan medoxomil reduced renal vascular resistance, increased renal perfusion, and reduced oxidative stress. In several large, randomized, double-blind trials, Olmesartan medoxomil 20 mg has been shown to be significantly more effective, in terms of primary endpoints, than recommended doses of losartan, valsartan, irbesartan, or candesartan cilexetil, and to provide better 24 h BP protection. Olmesartan medoxomil was at least as effective as amlodipine, felodipine and atenolol, and significantly more effective than captopril. The efficacy of Olmesartan medoxomil in reducing cardiovascular risk beyond BP reduction is currently being investigated in trials involving patients at high risk due to atherosclerosis or type 2 diabetes.
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Clinical efficacy and tolerability of Olmesartan.
Clinical therapeutics, 2004Co-Authors: Hans R. BrunnerAbstract:Olmesartan medoxomil is an angiotensin II receptor antagonist that selectively and competitively inhibits the angiotensin II type 1 receptor. This article reviews the results of some key studies that assessed the efficacy and tolerability of Olmesartan in patients with hypertension. Olmesartan has been investigated in several clinical studies. This article reports on data from 1 such study with a prospective, randomized, double-blind, placebo-controlled, parallel-group, dose-finding design in patients with mild to moderate hypertension (baseline mean sitting diastolic blood pressure, 100-114 mm Hg). The results from a meta-analysis of 7 randomized, double-blind, placebo-controlled studies are also presented. In the dose-finding study, 792 patients were randomized to Olmesartan (2.5-80 mg) or placebo once daily, and changes were recorded in trough mean sitting diastolic and systolic blood pressures from baseline to the end of a 12-week treatment period. For the meta-analysis, 3055 patients were randomized to treatment; 2511 received Olmesartan. In the dose-finding study as well as in the meta-analysis, Olmesartan (2.5-80 mg once daily) produced a dose-dependent decrease in diastolic and systolic blood pressures, and at a dose of 10 to 80 mg showed significant superiority in reducing diastolic blood pressure over placebo (P < 0.05). The 20-mg dose was considered optimal, with a responder rate of 70%. Furthermore, in a 2-year study with 462 patients, Olmesartan had a good safety profile and was well tolerated. The results of the clinical studies in >3000 patients receiving Olmesartan showed that the frequency and profile of adverse events with Olmesartan were generally similar to those with placebo; the frequency of adverse events was not dose related. Olmesartan, with or without hydrochlorothiazide, was well tolerated over 2 years of treatment.
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Clinical Efficacy and Tolerability of Olmesartan
Clinical Therapeutics, 2004Co-Authors: Hans R. BrunnerAbstract:Abstract Background: Olmesartan medoxomil is an angiotensin II receptor antagonist that selectively and competitively inhibits the angiotensin 11 type 1 receptor. Objective: This article reviews the results of some key studies that assessed the efficacy and tolerability of Olmesartan in patients with hypertension. Methods: Olmesartan has been investigated in several clinical studies. This article reports on data from 1 such study with a prospective, randomized, double-blind, placebo-controlled, parallel-group, dose-finding design in patients with mild to moderate hypertension (baseline mean sitting diastolic blood pressure, 100–114 mm Hg). The results from a meta-analysis of 7 randomized, double-blind, placebo-controlled studies are also presented. Results: In the dose-finding study, 792 patients were randomized to Olmesartan (2.5–80 mg) or placebo once daily, and changes were recorded in trough mean sitting diastolic and systolic blood pressures from baseline to the end of a 12-week treatment period. For the meta-analysis, 3055 patients were randomized to treatment; 2511 received Olmesartan. In the dose-finding study as well as in the meta-analysis, Olmesartan (2.5–80 mg once daily) produced a dose-dependent decrease in diastolic and systolic blood pressures, and at a dose of 10 to 80 mg showed significant superiority in reducing diastolic blood pressure over placebo ( P 3000 patients receiving Olmesartan showed that the frequency and profile of adverse events with Olmesartan were generally similar to those with placebo; the frequency of adverse events was not dose related. Olmesartan, with or without hydrochlorothiazide, was well tolerated over 2 years of treatment.
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Clinical efficacy of Olmesartan medoxomil.
Journal of hypertension. Supplement : official journal of the International Society of Hypertension, 2003Co-Authors: Hans R. Brunner, Petra LaeisAbstract: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 60% eliminated by the liver and the remainder by the kidney. In situations of impaired renal or hepatic function, the alternative excretion pathway can compensate for the compromised one. Olmesartan is not metabolized by the cytochrome P450 enzyme system and therefore has a low potential for metabolic drug interactions, a feature that may be of importance when treating patients on multiple drug regimens, such as the elderly. Olmesartan is well tolerated and has an excellent safety profile that is comparable to that of placebo. In addition, Olmesartan provides 24-h blood pressure control with a once-daily dosing. In head-to-head studies, Olmesartan delivered superior blood pressure reduction when compared with other angiotensin-II receptor antagonists at their recommended doses.
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The new oral angiotensin II antagonist Olmesartan medoxomil: a concise overview
Journal of Human Hypertension, 2002Co-Authors: Hans R. BrunnerAbstract:The new orally active angiotensin II (A II) type-1 receptor antagonist Olmesartan medoxomil is a prodrug, which is rapidly converted in vivo to the active metabolite, Olmesartan. The pharmacology, antihypertensive efficacy and safety of Olmesartan medoxomil and/or the pharmacologically active metabolite, Olmesartan, have been evaluated in both non-clinical and clinical models. Orally administered Olmesartan medoxomil is rapidly absorbed from the gastrointestinal tract and converted during absorption to Olmesartan, which is subsequently excreted without further metabolism. Peak plasma concentrations of Olmesartan occur 1–3 h after administration, after which concentrations decrease with an elimination half-life of 10–15 h. The absolute bioavailability of Olmesartan from Olmesartan medoxomil tablets is 28.6%. In a single-dose crossover study in 16 patients with mild-to-moderate hypertension receiving a sodium-restricted diet, statistically significant lowering of mean 24-h blood pressure was seen at doses of 10–80 mg. Evaluation of 14 phase II/III studies has confirmed the antihypertensive efficacy of Olmesartan medoxomil in over 3500 patients who received the drug for up to 2 years. Frequencies of adverse events during treatment with Olmesartan medoxomil and placebo are similar, with no evidence of a dose response. There are no clinically significant effects on laboratory parameters, and the drug-interaction potential of Olmesartan medoxomil is low. Current indications are that Olmesartan medoxomil is a true once-daily, orally active A II antagonist with good antihypertensive efficacy and a favourable adverse-event profile. Clinical pharmaco- dynamic and efficacy studies support a usual dose of 20 mg once daily, increasing to 40 mg if needed.
John D Schuetz - One of the best experts on this subject based on the ideXlab platform.
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multiple human isoforms of drug transporters contribute to the hepatic and renal transport of Olmesartan a selective antagonist of the angiotensin ii at1 receptor
Drug Metabolism and Disposition, 2007Co-Authors: Akihiro Yamada, Kazuya Maeda, Emi Kamiyama, Daisuke Sugiyama, Tsunenori Kondo, Yoshiyuki Shiroyanagi, Hayakazu Nakazawa, Teruo Okano, Masashi Adachi, John D SchuetzAbstract: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 be involved in its hepatic and renal clearance. In this study, we characterized the role 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 293 cells expressing organic anion-transporting polypeptide (OATP) 1B1, OATP1B3, organic anion transporter (OAT) 1, and OAT3. We also observed its saturable uptake into human hepatocytes and kidney slices. Estimated from the relative activity factor method and application of specific inhibitors, the relative contributions of OATP1B1 and OATP1B3 to the uptake of Olmesartan in human hepatocytes were almost the same, whereas OAT3 was predominantly involved in its uptake in kidney slices. The vectorial transport of Olmesartan was observed in OATP1B1/multidrug resistance-associated protein (MRP) 2 double transfectants, but not in OATP1B1/multidrug resistance (MDR) 1 and OATP1B1/breast cancer resistance protein (BCRP) transfectants. ATP-dependent transport into membrane vesicles expressing human MRP2 and MRP4 was clearly observed, with K(m) values of 14.9 and 26.2 microM, respectively, whereas the urinary excretion of Olmesartan in Mrp4-knockout mice was not different from that of control mice. We also investigated the transcellular transport of Olmesartan medoxomil, a prodrug of Olmesartan. Vectorial basal-to-apical transport was observed in OATP1B1/MRP2, OATP1B1/MDR1 double, and OATP1B1/BCRP double transfectants, suggesting the possible involvement of MRP2, MDR1, and BCRP in the limit of intestinal absorption of Olmesartan medoxomil. From these results, we suggest that multiple transporters make a significant contribution to the pharmacokinetics of Olmesartan and its prodrug.
Hiroki Ikeda - One of the best experts on this subject based on the ideXlab platform.
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Olmesartan reduced microalbuminuria in Japanese subjects with type 2 diabetes
Diabetes research and clinical practice, 2008Co-Authors: Hiroki Ikeda, Yoshiyuki Hamamoto, Sachiko Honjo, Koichiro Nabe, Yoshiharu Wada, Hiroyuki KoshiyamaAbstract:We investigated the effect of Olmesartan on early diabetic nephropathy in hypertensive patients with type 2 diabetes by its replacement of other angiotensin II type 1 receptor blockers (ARBs) by Olmesartan. The urinary albumin/creatinine ratio significantly decreased. The present result suggests a possibility that Olmesartan may have more effect on early nephropathy than other ARBs.
