动态血压监测的临床应用

目的本文主要探讨动态血压监测在高血压诊断中的应用价值及对药物疗效的评价。方法选用德国产动态血压监测仪对临床上的高血压患者及高度怀疑高血压的患者进行24h监测。结果以高血压诊断标准为依据,动态血压监测对引起高血压的各种病因分析及药物疗效的评价方面,具有指导意义,可以通过对统计结果的分析加以区分,评价药物疗效。结论动态血压监测能明显提高高血压诊断的正确率,可以对高血压患者进行监测和评价,是诊断高血压的可靠方法 。     

抗高血压药物与生命质量

本文从评价抗高血压药物疗效的传统指标的局限性出发,引入生命质量的概念及其作为评价药物疗效的新指标的价值,并概述了生命质量评价在四种主要抗高血压药物疗效评价中的应用.     

某医院抗高血压药物利用评价

目的 开展药物利用研究,促进临床合理用药.方法 采用药物利用评价(DUR)方法,对某大学附属医院2008年1～8月期间,以冠心病为出院诊断,合并高血压的132例患者进行抗高血压药物利用评价.结果 与结论 从评价结果看,该院医生选择和应用抗高血压药物基本遵从了科学、安全、有效、适用、经济的原则,但有4种药物存在用药过量现象,提示临床医师加以注意.     

我院门诊抗高血压药物应用分析

目的分析该院门诊抗高血压药物的应用情况。方法选择2012年1～3月门诊抗高血压处方615张,分别对用药品种、用药频度（DDDs）、药物利用指数（DUI）等进行分析,并以DUI为指标评价抗高血压药物应用的合理性。结果该院抗高血压药物除替米沙坦、缬沙坦、左旋氨氯地平、吲达帕胺外,其余药物DUI均≤1。结论该院抗高血压药使用基本合理,基本符合我国和欧洲高血压防治指南的原则。     

复方抗高血压药物在我国的应用

近几年,高血压的患病率呈逐年上升,而药物治疗是高血压治疗中的一项重要措施。本文对我国多年来广泛应用的几种复方抗高血压药物的药物组分和疗效进行分析和评价。     

抗高血压药物使用情况与不合理用药的干预措施研究

目的:分析我院心内科抗高血压药物使用情况,探讨不合理用药的原因,确保抗高血压用药的合理性.方法:连续入选2018年6月—2020年6月期间在我院心内科治疗的699例高血压患者,利用EXCEL表格对入选病历进行统计,评价其不同性别、年龄段患者抗高血压药物处方占比情况,分析不同种类抗高血压药物使用情况、抗高血压药物占处方比...     

合肥地区基层医疗机构基本药物中抗高血压药物利用评价

目的评价合肥地区基层医疗机构抗高血压基本药物的使用情况及其在基层医疗机构应用的合理性。方法收集2012年合肥地区45家基层医疗机构抗高血压基本药物的使用数据,采用药物利用评价方法,对销售金额、用药频度(DDDs)、日均费用、序号比等参数进行统计分析。结果 45家基层医疗机构抗高血压基本药物销售金额占全部药品销售总金额的1.50%,其中复方制剂占此类药物销售总金额的47.65%、血管紧张素转化酶抑制药占17.82%、钙通道阻滞药占17.71%、利尿药占13.38%,此四类为本区基层医疗机构应用的主要治疗药物;尼群地平DDDs为836 773、复方利血平DDDs为654 000,分别排名前两位。结论本区抗高血压药的使用在药物选择方面基本符合中国高血压防治指南,但在联合用药和药物剂型选择等方面尚有待加强。     

复方抗高血压药物在我国的应用

近几年,高血压的患病率呈逐年上升,而药物治疗是高血压治疗中的一项重要措施.本文对我国多年来广泛应用的几种复方抗高血压药物的药物组分和疗效进行分析和评价.     

我院2008-2010年抗高血压药物应用分析

目的了解并评价该院抗高血压药物的使用情况。方法调取2008—2010年抗高血压药物消耗的相关数据信息,对年药品消耗金额、用药频度（DDDs）与日用药费用（DDC）进行统计。结果抗高血压药物品种逐渐增加、销售金额持续增长。钙通道阻滞剂（CCB）的销售金额和用药频度都居于首位,单品种CCB的长效制剂和中效能利尿剂用药频度位于前2位。结论该院使用的抗高血压药物与中国高血压防治指南推荐的基本一致,抗高血压药物的使用较为合理。     

复方抗高血压药物在我国的应用

近几年,高血压的患病率呈逐年上升.而药物治疗是高血压治疗中的一项重要措施.本文对我国多年来广泛应用的几种复方抗高血压药物的药物组分和疗效进行分析和评价.     

Azilsartan medoxomil: a review of its use in hypertension

Azilsartan medoxomil (Edarbi?; Ipreziv?) is an orally administered angiotensin II receptor type 1 antagonist (blocker) used in the treatment of adults with essential hypertension. This article reviews data on the clinical efficacy and tolerability of azilsartan medoxomil in adults with essential hypertension and provides a summary of its pharmacological properties. Azilsartan medoxomil is a prodrug that undergoes rapid hydrolysis in the gastrointestinal tract after oral administration to the bioactive moiety azilsartan, before systemic absorption. Azilsartan medoxomil produces antihypertensive effects by selectively blocking the binding of angiotensin II to the angiotensin type 1 (AT(1)) receptor, thereby antagonizing the pressor response activity of angiotensin II. In vitro, azilsartan produced greater and more sustained AT(1) receptor binding/blockade activity than several comparator angiotensin II receptor antagonists. Azilsartan medoxomil reduces blood pressure (BP) in hypertensive adults. In addition, the drug has been shown to have pleiotropic effects (i.e. effects beyond AT(1) receptor blockade). In adults with essential hypertension, azilsartan medoxomil 20, 40 or 80?mg effectively reduced BP over a 24-hour period with once-daily administration in three major, randomized, controlled trials in which the primary endpoints were changes from baseline in 24-hour mean systolic BP (SBP) at week 6 (two trials) or week 24, assessed by ambulatory BP monitoring (ABPM). In the two 6-week trials, azilsartan medoxomil showed dose-dependent efficacy over all evaluated dosages and was more effective than placebo in lowering SBP. At the maximum approved dosage of 80?mg once daily, azilsartan medoxomil was significantly more effective than maximum dosages of olmesartan medoxomil (40?mg once daily) or valsartan (320?mg once daily), based on primary endpoint assessments. Mean reductions in clinic measurements of SBP and diastolic BP (DBP) measurements were also generally greater with azilsartan medoxomil 80?mg once daily than with the comparator drugs in these 6-week studies. Over a longer treatment period of 24 weeks, azilsartan medoxomil showed sustained BP-lowering efficacy, with the reduction in 24-hour mean SBP at week 24 significantly greater with azilsartan medoxomil 40 or 80?mg once daily than with valsartan 320?mg once daily. Mean reductions from baseline in mean clinic SBP and DBP as well as DBP by ABPM were also significantly greater with azilsartan medoxomil 40 or 80?mg once daily than with valsartan. Azilsartan medoxomil was generally well tolerated, with a tolerability profile similar to that of placebo in the 6-week trials. Across the three major trials, headache and dizziness were among the most common adverse events. Overall, rates of treatment discontinuation as a result of adverse events were low in the 6-week and 24-week trials. In conclusion, once-daily azilsartan medoxomil effectively lowers BP in adults with essential hypertension and has shown better antihypertensive efficacy than maximum therapeutic dosages of olmesartan medoxomil or valsartan in major trials of up to 24 weeks' duration. Azilsartan medoxomil is generally well tolerated and the low rates of discontinuation due to adverse events suggest that patients are likely to persist with long-term treatment. Azilsartan medoxomil is therefore a useful and attractive new option for lowering BP in patients with essential hypertension, particularly for those not able to tolerate other antihypertensive drugs. Further studies are required to evaluate the effects of azilsartan medoxomil on cardiovascular morbidity and mortality.     

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.     

抗高血压新药选择性AT1亚型血管紧张素II受体拮抗剂——阿齐沙坦酯

阿齐沙坦酯为新一代选择性AT1血管紧张素II亚型1受体拮抗剂,临床前和临床研究证实其具有平稳持久的抗高血压作用。2011年2月25日,FDA批准阿齐沙坦酯(商品名为Edarbi)用于治疗成人高血压。本综述主要介绍其药物作用机制,药物代谢动力学、疗效、安全性及临床研究进展。     

Azilsartan medoxomil for the treatment of hypertension

The use of angiotensin receptor blockers (ARBs) represents a favorable approach for the control of blood pressure in patients with hypertension. Azilsartan medoxomil, a prodrug that undergoes rapid hydrolysis to its active moiety azilsartan, is an angiotensin AT(1) receptor antagonist with promising antihypertensive activity and a good safety profile. The agent has been evaluated as monotherapy and in combination with amlodipine or chlorthalidone in phase III trials in patients with essential hypertension. In 2011, azilsartan medoxomil was approved in the U.S. for the treatment of hypertension.     

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。     

Azilsartan medoxomil in the treatment of hypertension: the definitive angiotensin receptor blocker?

Introduction: Azilsartan medoxomil is the newest angiotensin receptor blocker marketed for the treatment of arterial hypertension. The aim of this article was to review the available evidence about this drug alone or combined with other antihypertensive agents in the treatment of hypertensive population.

Areas covered: For this purpose, a search on MEDLINE and EMBASE databases was performed. The MEDLINE and EMBASE search included both medical subject headings (MeSHs) and keywords including azilsartan or azilsartan medoxomil or angiotensin receptor blockers or renin angiotensin system or chlorthalidone and hypertension. References of the retrieved articles were also screened for additional studies. There were no language restrictions.

Expert opinion: Azilsartan medoxomil has a potent and persistent ability to inhibit binding of angiotensin II to AT1 receptors, which may play a role in its superior blood pressure (BP) -lowering efficacy compared with other drugs, including ramipril, candesartan, valsartan or olmesartan, without an increase of side effects. Chlortalidone is a diuretic which significantly differs from other classic thiazides and has largely demonstrated clinical benefits in outcome trials. The fixed-dose combination of azilsartan and chlorthalidone has been shown to be more effective than other potent combinations of angiotensin receptor blockers plus hydrochlorothiazide, with a good tolerability profile.     

Pharmacokinetics of amlodipine and olmesartan after administration of amlodipine besylate and olmesartan medoxomil in separate dosage forms and as a fixed-dose combination

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-dose combination tablet were characterized in 5 phase I, randomized, crossover studies. The mean steady-state pharmacokinetics of amlodipine and olmesartan were similar when olmesartan medoxomil 40 mg/day and amlodipine 10 mg/day were administered separately or concomitantly for 10 days. 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 amlodipine 10 mg plus olmesartan medoxomil 40 mg. The ratio of least squares mean and 90% confidence intervals for the area under the drug concentration-time curve from time zero to time t, from time zero to infinity, and the maximum observed plasma drug concentration of amlodipine and olmesartan fell within the prespecified range for bioequivalence (80.0% - 125.0%). The area under the drug concentration-time curve from time zero to time t, from time zero to infinity, and the maximum observed plasma drug concentration of both drugs also met the prespecified criterion for bioequivalence when the fixed-dose combination tablet was taken 30 minutes after a high-fat breakfast. Total exposure to amlodipine and olmesartan was dose-proportional after administration of olmesartan medoxomil 10 mg to 40 mg in the fixed-dose combination formulation with amlodipine 5 mg to 10 mg. From a pharmacokinetic perspective, the 2 drugs are well suited to coadministration in a fixed-dose combination.     

Gateways to clinical trials

Aclidinium bromide, AE-37, Alemtuzumab, AMA1-C1/ISA 720, Amlodipine besylate/atorvastatin calcium, Arachidonic acid, Arbaclofen placarbil, Aripiprazole, ARQ-621, Azelnidipine, Azilsartan medoxomil potassium; Bevacizumab, Biphasic insulin aspart, Bortezomib; Choriogonadotropin alfa, CTS-1027; Dapagliflozin, Dasatinib, Deforolimus, Degarelix acetate, Denufosol tetrasodium, Desvenlafaxine succinate, Dronedarone hydrochloride, Duloxetine hydrochloride, Dutasteride; Enfuvirtide, Entecavir, Etaracizumab, Everolimus, Exenatide, Ezetimibe; Ferric carboxymaltose, Fludarabine, Foretinib; Gefitinib, GFT-505, GSK-256066; HPV-6/11/16/18, HuM195/rGel, HyperAcute-Lung cancer vaccine; I5NP, Imatinib mesylate, Imexon, Insulin detemir, Insulin glargine, Ivabradine hydrochloride; L2G7, Lacosamide, Lapatinib ditosylate, Lenalidomide, Lidocaine/prilocaine, Liposomal vincristine, Liraglutide, Lixivaptan; Meningococcal (groups A, C, Y and W-135) oligosaccharide diphtheria CRM197 conjugate vaccine, Methoxy polyethylene glycol-epoetin-β, Mirabegron, Morphine/oxycodone, MR Vaccine, MSC-1936369B, Mycophenolic acid sodium salt; Narlaprevir, N-Desmethylclozapine; Ocriplasmin, Olaparib, Olmesartan medoxomil, Olmesartan medoxomil/azelnidipine, ONO-5334, ONO-8539; Palifermin, Panitumumab, Pardoprunox hydrochloride, PCV7, Peginterferon alfa-2a, Peginterferon alfa-2b, Pemetrexed disodium, Pexelizumab, PF-337210, Pitavastatin calcium; Raltegravir potassium, Recombinant interleukin-7, Regadenoson, Reniale, Roflumilast, Rosuvastatin calcium; Safinamide mesilate, SB-1518, SCH-527123, Selumetinib, Sipuleucel-T, Solifenacin succinate, Sorafenib, Sunitinib malate; Tadalafil, Talaporfin sodium, Tanespimycin, Technosphere/Insulin, Telaprevir, Telatinib, Telcagepant, Telmisartan/hydrochlorothiazide, Teriparatide, Testosterone transdermal gel, TH-302, Tiotropium bromide, Tocilizumab, Trabedersen, Tremelimumab; Valsartan/amlodipine besylate, Vernakalant hydrochloride, Visilizumab, Voreloxin, Vorinostat.     

奥美沙坦酯治疗老年高血压的疗效及安全性观察

目的：评价奥美沙坦酯治疗老年高血压的疗效和安全性。方法：选取2009年1-8月我院42例老年高血压患者,随机分为两组。治疗组（21例）服用奥美沙坦酯每次20mg,每日1次;对照组（21例）服用氯沙坦每次50mg,每日1次。总疗程均为8周。结果：奥美沙坦酯组和氯沙坦组治疗前后血压下降幅度差异均有统计学意义（P〈0.01）。奥美沙坦酯组和氯沙坦组降压显效率分别为69.0%和68.4%,总有效率分别为90.4%和89.7%,两组间差异无统计学意义（P〉0.05）。奥美沙坦酯组和氯沙坦组均未出现药品不良反应。结论：奥美沙坦酯治疗老年高血压效果明显,安全性好。     

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.