Pharmacological profiles and clinical effects of olmesartan medoxomil, a novel angiotensin II receptor blocker

Olmesartan medoxomil is a new angiotensin II receptor blocker (ARB) indicated for the treatment of hypertension. Olmesartan medoxomil is a pro-drug that is converted to the active metabolite olmesartan. Olmesartan does not undergo further metabolism and does not interact with cytochrome P450 enzymes. Olmesartan is a potent ARB with high selectivity for the type 1 (AT(1)) receptor subtype and shows insurmountable antagonism against the AT(1) receptor in vascular tissues. This antagonistic mode, which could be attributed to tight binding of this drug to the receptor, would underlie the potent and persistent action of olmesartan medoxomil in vivo. In fact, oral administration of olmesartan medoxomil produces a potent and long-lasting antihypertensive action without inducing tachycardia. The preventive effects of olmesartan medoxomil on end-organ damage in the kidney, heart, and blood vessels have been demonstrated in various animal models. In clinical studies, olmesartan medoxomil is shown to be well tolerated and have an excellent safety profile that is comparable to that of placebo. Head-to-head comparisons with other ARBs (losartan, valsartan, irbesartan, and candesartan cilexetil) conducted in the United States and Europe have revealed that olmesartan medoxomil is superior to these other ARBs in lowering blood pressure. These facts suggest that olmesartan medoxomil would be beneficial for the treatment of hypertension and other end-organ diseases.     

Clinical and experimental aspects of olmesartan medoxomil, a new angiotensin II receptor antagonist

Olmesartan medoxomil is a new orally active angiotensin II (Ang II) type 1 receptor antagonist. It is a prodrug and is rapidly de-esterified during absorption to form olmesartan, the active metabolite. Olmesartan is a potent, competitive and selective Ang II type 1 receptor antagonist. Olmesartan is not metabolized by the cytochrome P-450 and has a dual route of elimination, by kidneys and liver. In patients with essential hypertension olmesartan medoxomil administered once daily at doses of 10-80 mg dose-dependently reduced diastolic blood pressure (DBP). Troughto-peak ratios for both DBP and systolic blood pressure (SBP) were above 50%. At the recommended once-daily starting doses, olmesartan medoxomil (20 mg) was more effective than losartan (50 mg), valsartan (80 mg) or irbesartan (150 mg) in reducing cuff DBP in patients with essential hypertension. The results of cuff SBP and mean 24-h DBP and SBP were similar to those of cuff DBP measurement. In mild-to-moderate hypertensive patients the recommended starting dose of olmesartan medoxomil was as effective as that of amlodipine besylate (5 mg/day) in reducing both cuff and 24-h blood pressure. In lowering DBP olmesartan medoxomil, at 10-20 mg/day, was as effective as atenolol at 50-100 mg/day. In mild-to-moderate hypertensive patients, olmesartan medoxomil, at 5-20 mg once daily, was more effective than captopril at 12.5-50 mg twice daily. At 20-40 mg once daily olmesartan medoxomil was as effective as felodipine, at 5-10 mg once daily. Olmesartan medoxomil has minimal adverse effects with no clinically important drug interactions. Animal studies have shown that olmesartan medoxomil provides a wide range of organ protection. Olmesartan medoxomil ameliorated atherosclerosis in hyperlipidemic animals and ameliorated cardiac remodeling and improved survival in rats with myocardial infarction. Olmesartan medoxomil has renoprotective effects in a remnant kidney model and type 2 diabetes models. Future investigation should reveal whether these beneficial effects of olmesartan medoxomil are applicable to human diseases.     

The role of olmesartan medoxomil in the management of hypertension

Intensive blood pressure control is a desirable and obtainable goal in patients with hypertension, according to the most recent treatment guidelines from Europe and the US. Achieving target blood pressure depends on the efficacy of antihypertensive treatment and patient compliance. Olmesartan medoxomil, a non-peptidergic angiotensin AT1 receptor antagonist, has been shown to be effective and well tolerated. Continuation of initial treatment is higher with AT1 receptor antagonists than for any other class of antihypertensive drugs. Olmesartan medoxomil may also have end-organ protective effects that provide additional clinical benefit. Optimal blood pressure control may be achieved faster if initial treatment contains the most efficacious and well tolerated antihypertensive drug or drugs. The ongoing European study, known as OLMEBEST (Efficacy and safety of OLMEsartan: reduction of Blood pressure in the treatment of patients suffering from mild to moderate ESsenTial hypertension), will provide important information on the use of olmesartan medoxomil as an initial treatment for hypertension.     

Olmesartan medoxomil

Olmesartan medoxomil is a nonpeptide angiotensin II receptor antagonist which selectively and competitively inhibits the type 1 angiotensin II receptor without affecting other receptors regulating the cardiovascular system. In well designed randomised trials, olmesartan medoxomil was significantly more effective than placebo, and at dosages of 10 to 20 mg/day was at least as effective as atenolol 50 to 100 mg/day in reducing diastolic blood pressure (DBP). At dosages of 5 to 20 mg/day, olmesartan medoxomil was more effective than captopril 12.5 to 50mg twice daily at lowering seated DBP in patients with mild to moderate hypertension in a dose titration study. Reductions in seated DBP were greater with olmesartan medoxomil 10 to 20 mg/day than losartan 50 to 100 mg/day. Olmesartan medoxomil at 20 mg/day was more effective in lowering seated DBP than losartan 50 mg/day, valsartan 80 mg/day or irbesartan 150 mg/day, and was more efficacious than losartan 50 mg/day or valsartan 80 mg/day at reducing 24-hour ambulatory systolic blood pressure. Olmesartan medoxomil has shown no clinically important pharmacokinetic interactions with digoxin, warfarin or antacid (aluminium magnesium hydroxide). Adverse events were infrequent in clinical studies of olmesartan medoxomil and were similar to those attributed to placebo. With olmesartan medoxomil, the frequency of dizziness was higher than with placebo but similar to that occurring with losartan, valsartan and irbesartan.     

Olmesartan medoxomil: a review of its use in the management of hypertension

Olmesartan medoxomil (Olmetec, Benicar) is an angiotensin II type 1 (AT(1)) receptor antagonist (angiotensin receptor blocker [ARB]) that inhibits the actions of angiotensin II on the renin-angiotensin-aldosterone system, which plays a key role in the pathogenesis of hypertension. Oral olmesartan medoxomil 10-40 mg once daily is recommended for the treatment of adult patients with hypertension. In those with inadequate BP control using monotherapy, fixed-dose olmesartan medoxomil/hydrochlorothiazide (HCTZ) [Olmetec plus, Benicar-HCT] combination therapy may be initiated. Extensive clinical evidence from several large well designed trials and the clinical practice setting has confirmed the antihypertensive efficacy and good tolerability profile of oral olmesartan medoxomil, as monotherapy or in combination with HCTZ, in patients with hypertension, including elderly patients with isolated systolic hypertension (ISH). Notably, BP control is sustained throughout the 24-hour dosage interval, including during the last 4 hours of this period. In clinical trials, olmesartan medoxomil monotherapy provided better antihypertensive efficacy than losartan, candesartan cilexetil or irbesartan monotherapy, and was at least as effective as valsartan treatment, with a faster onset of action than other ARBs in terms of reductions from baseline in diastolic BP (DBP) and, in most instances, systolic BP (SBP). Combination therapy with olmesartan medoxomil plus HCTZ was superior to that with benazepril plus amlodipine, as effective as that with losartan plus HCTZ, noninferior to that with atenolol plus HCTZ, but less effective than that with telmisartan plus HCTZ, in individual trials. Data from ongoing clinical outcome trials are required to more fully determine the relative position of olmesartan medoxomil therapy in the management of hypertension. In the meantime, the consistent antihypertensive efficacy during the entire 24-hour dosage interval and good tolerability profile of olmesartan medoxomil, with or without HCTZ, make it a valuable option for the treatment of adult patients with hypertension, including the elderly.     

奥美沙坦酯治疗轻中度原发性高血压的疗效和安全性

目的评价奥美沙坦酯治疗轻中度原发性高血压的疗效和安全性。方法随机、双盲、双模拟、阳性药物(氯沙坦钾)平行对照。40例轻中度原发性高血压患者随机分为奥美沙坦酯或氯沙坦钾组,均治疗8周,观察两组治疗前后的血压、心率、心电图和血、尿常规等实验室检查结果的变化。结果奥美沙坦酯组与氯沙坦钾组比较,患者平均坐位收缩压和舒张压的降低程度均有显著性差异,分别为(18.9±8.7)mmHg和(12.6±7.6)mmHg(P<0.01);(13.8±3.5)mmHg和(11.7±3.3)mmHg(P<0.05)。治疗前后两组血压降低幅度均有显著差异,心率无明显变化。奥美沙坦酯和氯沙坦钾组降压显效率分别为63.2%和57.9%,总有效率分别为84.2%和68.4%,组间无显著差异。两组共出现3例头晕,实验室检查无异常改变。结论奥美沙坦酯治疗轻中度原发性高血压的疗效良好,不良反应发生率低。     

Olmesartan medoxomil-based therapy for the management of hypertension

Contemporary practice guidelines for hypertension recommend a goal systolic/diastolic blood pressure (BP) of less than 140/90 mmHg for patients with hypertension and less than 130/80 mmHg for patients with diabetes mellitus or chronic kidney disease. Current guidelines recognize that most patients will require combination therapy to achieve these BP goals and recommend that the agents used in such therapy should have complementary mechanisms of action. Olmesartan medoxomil is an angiotensin receptor blocker approved for the treatment of hypertension as monotherapy or in combination with antihypertensive agents. It is also approved in a fixed-dose combination with hydrochlorothiazide or amlodipine. Olmesartan medoxomil-based therapy can manage hypertension across a range of patient types and has demonstrated good BP-lowering efficacy and goal attainment in individuals with stage 1 or stage 2 hypertension. The comparative antihypertensive efficacy and safety of olmesartan medoxomil, as monotherapy and as part of combination therapy, has been established in several large, randomized clinical trials. This review evaluates the chemistry, efficacy and safety of olmesartan medoxomil-based therapy and its expanding role in hypertension management.     

Olmesartan medoxomil: in children and adolescents with hypertension

Olmesartan medoxomil is an orally administered angiotensin II receptor antagonist, selective for the angiotensin II type 1 receptor, which has established antihypertensive efficacy in adults. In children and adolescents with hypertension (n?=?302), oral olmesartan medoxomil significantly and dose-dependently reduced seated systolic blood pressure (BP) and seated dystolic BP from baseline (the primary endpoint) in a 3-week, dose-response period in a well designed phase II/III clinical trial. Patients received olmesartan medoxomil high dose (20 or 40?mg once daily depending on bodyweight) or low dose (2.5 or 5.0?mg once daily depending on bodyweight). The response was significant for both cohorts, which were stratified by race (cohort A was mixed race [62% White] and cohort B was 100% Black). In addition, BP control was maintained in olmesartan recipients relative to placebo recipients in cohort A and the combined cohort A?+?B, but not for patients in cohort B, during a placebo-controlled withdrawal period of this trial. Oral olmesartan medoxomil was generally well tolerated in children and adolescents with hypertension. The majority of adverse events were of mild to moderate intensity.     

Blood pressure reduction with olmesartan in mild-to-moderate essential hypertension: a planned interim analysis of an open label sub-study in German patients

OBJECTIVE: To present the baseline characteristics and open-label treatment phase results for German patients in OLMEBEST, a European, multinational, partially randomized, partially double-blind study in patients with mild-to-moderate essential hypertension. RESEARCH DESIGN AND METHODS: After a 2-week placebo run-in, patients received olmesartan 20 mg for 8 weeks. Controlled patients (mean sitting diastolic blood pressure [sDBP] < 90 mmHg) continued on olmesartan 20 mg/day for a further 4 weeks. Non-controlled patients (sDBP > 90 mmHg) were randomized to olmesartan 40 mg/day or olmesartan 20 mg/day plus 12.5 mg hydrochlorothiazide for 4 weeks. Of 823 patients included, 558 continued olmesartan 20 mg treatment and 228 patients were randomized to olmesartan 40 mg/day or combination therapy. Efficacy variables included the change from baseline in mean sitting DBP and systolic blood pressure [sSBP] at Week 8 (and Week 12 for controlled patients), and the proportion of controlled patients and responders (mean sDBP < 90 mmHg or improvement of > 10 mmHg from baseline at Week 8). RESULTS: After 8 weeks of olmesartan medoxomil 20 mg, mean reduction from baseline in sDBP was 11.8 mmHg and in sSBP was 17.1 mmHg. In controlled patients continuing open-label olmesartan medoxomil 20 mg, mean reduction from baseline at 12 weeks in sDBP was 14.9 mmHg and in sSBP was 20.1 mmHg. At Week 8, the response rate was 76% and the control rate was 70%. Olmesartan medoxomil 20 mg/day was well tolerated; 30.9% of patients experienced an adverse event, and the majority of these events were judged by the investigators to be mild. CONCLUSION: Olmesartan medoxomil monotherapy at the recommended dosage of 20 mg once daily is effective and well tolerated in patients with mild-to-moderate hypertension.     

奥美沙坦:一种新的血管紧张肽Ⅱ受体拮抗剂

奥美沙坦 (olmesartan)是最新的血管紧张肽Ⅱ受体 (AT1)拮抗剂 ,对不同程度的高血压均有很好的降压作用 ,病人对其亦有很好的耐受性。本文对该药的药效学、药动学和临床应用等研究作一综述     

奥美沙坦酯片治疗轻中度原发性高血压的疗效和安全性

目的评价国产奥美沙坦酯片治疗轻中度原发性高血压的疗效和安全性。方法用随机双盲双模拟多中心活性药对照的试验设计,符合入选条件的221例轻中度原发性高血压患者随机分为奥美沙坦酯组和氯沙坦组,治疗8周,观察2组治疗前后的血压、心率、心电图和血尿实验室检查的变化。动态血压用开放试验方法,分别在安慰剂末期和治疗期结束时(未停药),做24h动态血压监测。结果奥美沙坦组与氯沙坦组比较,平均坐位收缩压和舒张压降低程度都有显著性差异,分别为17.22vs11.02mmHg,(P<0.01);13.41vs11.18mmHg(P<0.05)。奥美沙坦组降压总有效率为82.41%;每日1次服用奥美沙坦酯片作用可持续24h,药物降低收缩压和舒张压的谷峰比值均>50%。2组药物不良反应发生率分别为3.5%,5.4%,2组比较无显著性差别。结论国产奥美沙坦酯片治疗轻中度原发性高血压患者,能24h平稳降压,谷峰比满意,且耐受性较好。     

奥美沙坦酯与氨氯地平或氢氯噻嗪联合治疗原发性高血压的疗效比较

目的比较奥美沙坦酯联合氨氯地平与奥美沙坦酯联合氢氯噻嗪治疗原发性高血压的疗效。方法将206例2—3级原发性高血压患者完全随机分为观察组（奥美沙坦酯联合氨氯地平）和对照组（奥美沙坦酯联合氢氯噻嗪）,每组103例,监测2组治疗前和治疗8周后24h动态血压,分析2组间降压效果及血压变异的差异,并观察治疗期间药物不良反应。结果治疗后2组患者24h平均收缩压及舒张压、白昼收缩压及舒张压、夜间收缩压及舒张压均较治疗前明显降低[观察组：（133±9）mmHg（1mmHg=0．133kPa）比（166±10）mmHg,（73±8）mmHg比（96±9）mmHg;（134±9）mmHg比（164±9）mmHg,（76±8）mmHg比（100±8）mmHg;（120±9）mmHg比（158±11）mrllHg;（72±7）mmHg比（94±8）mmHg。对照组：（130±7）mmHg比（164±11）mmHg,（75±7）mmHg比（97±8）mmHg;（131±8）mmHgI;L（164±10）mmHg,（79±7）mmHg比（101±8）mmHg;（129±8）mmHg比（160±9）mmHg,（80±8）mmHg比（102±8）InlllHg],差异有统计学意义（P〈0．05）,组间比较差异无统计学意义（P〉0．05）。白昼和夜间血压变异性2组差异有统计学意义（P〈0．05）。观察组和对照组降压总有效率分别为97．1％（100／103）和96．1％（99／103）,差异无统计学意义（P〉0．05）。治疗期间2组不良反应发生率差异无统计学意义（P〉0．05）。结论奥美沙坦酯联合氨氯地平与氢氯噻嗪对原发性高血压患者降压效果较好,疗效相当且安全,奥美沙坦酯联用氨氯地平在血压变异性上控制较好。     

Improvement of stunned myocardium in dogs with olmesartan, an angiotensin II type 1 receptor antagonist, is independent of type 2 receptors

Olmesartan is a selective angiotensin II type 1 receptor (AT1) antagonist. In pentobarbital-anesthetized open-chest dogs, ischemia/reperfusion was induced by ligating the left anterior descending coronary artery for 20 min and releasing it for 60 min, respectively. The myocardial contraction in the ischemic area decreased and returned towards its pre-ischemic level during reperfusion but incompletely. Olmesartan improved the recovery of myocardial contraction during reperfusion associated with restoration of myocardial ATP. Angiotensin II repelled by AT1 receptors occupied by olmesartan can reach and stimulate the angiotensin II type 2 (AT2) receptors, resulting in some beneficial effects on the ischemic myocardium. In fact, AT2 receptor mRNA was found in the adult dog myocardium. In addition, the plasma level of angiotensin II was significantly increased by olmesartan. PD123319, a selective AT2 receptor antagonist, however, did not modify the effect of olmesartan on the cardiac contraction. The hypertensive response to exogenous angiotensin II was completely inhibited by olmesartan, whereas PD123319 did not abolish the effect of olmesartan. In conclusion, olmesartan protects the ischemic/reperfused heart against ischemic injury through inhibition of AT1 receptors but not indirect activation of AT2 receptors.     

Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models

The pharmacological profile of a novel angiotensin II type 1 receptor blocker, azilsartan medoxomil, was compared with that of the potent angiotensin II receptor blocker olmesartan medoxomil. Azilsartan, the active metabolite of azilsartan medoxomil, inhibited the binding of [(125)I]-Sar(1)-I1e(8)-angiotensin II to angiotensin II type 1 receptors. Azilsartan medoxomil inhibited angiotensin II-induced pressor responses in rats, and its inhibitory effects lasted 24h after oral administration. The inhibitory effects of olmesartan medoxomil disappeared within 24h. ID(50) values were 0.12 and 0.55 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. In conscious spontaneously hypertensive rats (SHRs), oral administration of 0.1-1mg/kg azilsartan medoxomil significantly reduced blood pressure at all doses even 24h after dosing. Oral administration of 0.1-3mg/kg olmesartan medoxomil also reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24h after dosing. ED(25) values were 0.41 and 1.3mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. In renal hypertensive dogs, oral administration of 0.1-1mg/kg azilsartan medoxomil reduced blood pressure more potently and persistently than that of 0.3-3mg/kg olmesartan medoxomil. In a 2-week study in SHRs, azilsartan medoxomil showed more stable antihypertensive effects than olmesartan medoxomil and improved the glucose infusion rate, an indicator of insulin sensitivity, more potently (≥ 10 times) than olmesartan medoxomil. Azilsartan medoxomil also exerted more potent antiproteinuric effects than olmesartan medoxomil in Wistar fatty rats. These results suggest that azilsartan medoxomil is a potent angiotensin II receptor blocker that has an attractive pharmacological profile as an antihypertensive agent.     

奥美沙坦酯片治疗轻、中度原发性高血压的疗效和安全性

目的观察奥美沙坦酯片治疗轻、中度原发性高血压的疗效和安全性。方法61例轻、中度原发性高血压患者随机分为奥美沙坦酯组(n=30)和氯沙坦组(n=31),治疗8wk,观察2组治疗前后的血压、心率、心电图和血、尿实验室检查的变化。结果奥美沙坦酯组与氯沙坦组比较,坐位收缩压和舒张压降低程度都有显著差异,分别为(132±13 vs 139±13)mmHg(P<0.01)和(85±9 vs 87±9)mmHg(P<0.05)。奥美沙坦酯组降压有效率为83%;每日1次服用奥美沙坦酯作用可持续24h,药物降低收缩压和舒张压的谷峰比值均>50%。2组药物不良反应发生分别为1例和3例,2组比较无显著差别。结论奥美沙坦酯治疗轻、中度原发性高血压患者,能24h平稳降压,谷峰比满意,且耐受性较好。     

奥美沙坦酯对轻中度高血压的降压疗效及对踝臂指数的影响

目的探讨奥美沙坦酯对轻中度高血压降压疗效及对踝臂指数的影响。方法 2011年7-11月我院收治的高血压患者120例,将其随机分为奥美沙坦组和氨氯地平组,治疗8周,检测血常规、尿常规、生化、心电图,记录血压、心率变化,并在治疗开始及结束后检测24 h动态血压和踝臂指数。结果 8周末,两组治疗前后随机血压及24 h、白昼、夜间平均收缩压及舒张压均显著下降(P<0.05),心率无明显变化。两组降压有效率均为85%,奥美沙坦酯降压可持续24 h,收缩压及舒张压的降压谷峰比均>50%。两组治疗8周ABI较前分别有所升高(P<0.05),两组间比较差异无统计学意义(P>0.05)。结论奥美沙坦酯治疗轻中度高血压安全有效,谷峰比满意,能够24 h平稳降压,且长期应用可改善动脉硬化。     

An angiotensin II type 1 receptor antagonist,olmesartan medoxomil,improves experimental liver fibrosis by suppression of proliferation and collagen synthesis in activated hepatic stellate cells

1. We studied the effect of a new angiotensin II type 1 (AT(1)) receptor antagonist, olmesartan medoxomil (olmesartan), on the fibrogenic responses in rat hepatic stellate cells (HSCs) and liver fibrogenesis. 2. Olmesartan (1 mg kg(-1) per day) was orally administered to fibrotic rats, induced by bile duct ligation. Liver hydroxyproline content, the mRNA expression of collagen alpha1(I) and alpha-smooth muscle actin (alpha-SMA), and plasma levels of transforming growth factor-beta1 (TGF-beta1) were significantly reduced by olmesartan treatment, suggesting that olmesartan improved liver fibrosis. Interestingly, AT(1) receptors were found to be expressed in alpha-SMA-positive cells in the fibrotic area of livers in bile duct-ligated rats by immunohistochemical analysis. Olmesartan treatment reduced the number of these cells. 3. In vitro experiments showed that angiotensin II (Ang II) treatment induced proliferation and collagen synthesis, and upregulated the profibrogenic cytokines, TGF-beta1 and connective tissue growth factor (CTGF), in rat primary HSCs. Olmesartan blocked all these effects of Ang II. 4. Based on these results, since activated HSCs were found to express AT(1) receptors and Ang II is thought to play an important role in the pathogenesis of liver fibrosis by binding to these receptors, olmesartan may act as a potent antifibrotic drug to suppress the proliferation, collagen synthesis and the expression of profibrogenic cytokines in activated HSCs by blocking these receptors.     

不同剂量奥美沙坦对原发性高血压患者血压及胰岛素抵抗的影响

目的研究不同剂量奥美沙坦对原发性高血压(Essential hypertension,EH)患者血压及胰岛素抵抗(insulin resistance,IR)的影响。方法 EH患者65例随机分成A组(奥美沙坦20mg)33例,B组(奥美沙坦40mg)32例,治疗12周。观察两组治疗前后的动态血压(ABPM)、空腹血糖(FPG)和胰岛素(FINS)、胰岛素敏感指数(ISI)和胰岛素抵抗指数(HOMA-IR)水平的变化。结果①治疗后两组EH患者血压水平均较治疗前明显降低,B组较A组更为明显,差异有统计学意义(P<0.05)。②治疗后两组ISI均明显高于治疗前,B组升高更为明显,差异有统计学意义(P<0.05);治疗后两组HOMA-IR均明显低于治疗前,B组降低更为明显,差异有统计学意义(P<0.05)。结论奥美沙坦可有效降压及改善胰岛素抵抗,且存在剂量相关性。     

阿齐沙坦与奥美沙坦酯治疗轻中度原发性高血压的疗效比较

目的 比较阿齐沙坦与奥美沙坦酯治疗轻中度原发性高血压的临床疗效。方法 2015年9月—2017年2月从全国多家研究中心筛选轻、中度原发性高血压304例,随机分为奥美沙坦酯组和阿齐沙坦组。受试者从起始剂量开始,阿齐沙坦片20 mg/次和奥美沙坦酯片模拟剂,1次/d,或奥美沙坦酯片20 mg/次和阿齐沙坦片模拟剂,1次/d,开始治疗。用药后第8周末对受试者进行血压评价,如果服药前（药物浓度谷值时）坐位收缩压≥140 mmHg（1 mmHg=133 Pa）和/或舒张压≥90 mmHg则试验药物剂量加倍（阿齐沙坦片40 mg/次口服或奥美沙坦酯片40 mg/次,1次/d）继续治疗8周,如果服药前（药物浓度谷值时）坐位收缩压<140 mmHg且舒张压<90 mmHg则维持原剂量继续治疗8周。治疗总周期16周。观察两组的有效率和达标率。比较两组治疗前,治疗8、12、16周收缩压、舒张压,血压与治疗前差值的变化情况。结果 用药8、16周,奥美沙坦酯组有效率分别是66.89%、69.59%;阿齐沙坦组有效率分别是59.60%、58.94%,两组有效率比较差异没有统计学意义。用药8、16周,奥美沙坦酯组达标率分别是62.16%、61.49%;阿齐沙坦组达标率分别是56.95%、56.29%,两组达标率比较差异均没有统计学意义。治疗8、12、16周,两组受试者的坐位收缩压、舒张压逐渐降低,与同组治疗前比较差异均有统计学意义（P<0.05）;治疗后,两组血压比较差异无统计学意义。用药后两组受试者的坐位收缩压和舒张压均逐渐降低,至16周末时,两组间坐位舒张压下降值比较差异具有统计学意义（P<0.05）;16周末时两组收缩压下降值差异均没有统计学意义。结论 有效性方面,阿齐沙坦组疗效未达非劣效于奥美沙坦酯组,但阿齐沙坦自身的降压效果显著并具临床意义;安全性方面,阿齐沙坦组与奥美沙坦酯组不良事件、严重不良事件、不良反应发生率相当,安全性良好。