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Administration of nifedipine CR immediately after awakening prevents a morning surge in hypertensive patients. Case report of three cases. 醒后立即给予硝苯地平CR可防止高血压患者晨涌。三例病例报告。
Pub Date : 2003-05-01 DOI: 10.1080/08038020310000113
Hiroaki Kawano, Naoto Ashizawa, Genji Toda, Shinji Seto, Katsusuke Yano

Although the blood pressure-lowering action of some long-acting calcium antagonists may last more than 24 h, some patients taking this drug still experience a morning surge, i.e. an early morning increase in blood pressure. We evaluated this morning surge in three hypertensive patients with morning surge after administration of antihypertensive drugs including nifedipine CR. Nifedipine CR is one of the once-a-day formulations of nifedipine, which after administration, results in two peaks in the plasma concentration of nifedipine. The first concentration peak of occurs 3 h after administration and the second around 12 h after intake. When the time of intake of nifedipine CR was changed from after breakfast to immediately after awakening, the morning surge was suppressed in these patients without the use of other drugs such as alpha- or beta-blockers. Administration of nifedipine CR immediately after awakening is one option that can be used to prevent morning surge as well as to control blood pressure throughout the day.

虽然一些长效钙拮抗剂的降血压作用可能持续24小时以上,但一些服用此药的患者仍然会出现清晨血压升高的现象。我们评估了3例高血压患者在服用硝苯地平CR等降压药后出现晨起。硝苯地平CR是硝苯地平的一种每日一次的剂型,给药后会导致硝苯地平的血药浓度出现两个高峰。第一个浓度峰出现在给药后3小时,第二次浓度峰出现在服药后12小时左右。当硝苯地平CR的摄入时间由早餐后改为醒来后立即服用时,无需使用α -受体阻滞剂或β -受体阻滞剂等其他药物即可抑制晨起。醒来后立即服用硝苯地平是一种选择,可以用来防止晨起高潮,也可以控制全天的血压。
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引用次数: 6
Effect of doxazosin GITS on blood pressure in hypertensive and normotensive patients: a review of hypertension and BPH studies. doxazosin GITS对高血压和正常患者血压的影响:高血压和BPH研究综述
Pub Date : 2003-05-01 DOI: 10.1080/08038020310000078
Per Lund-Johansen, Roger S Kirby

Doxazosin is an effective treatment for patients with hypertension, benign prostatic hyperplasia (BPH) and the two comorbidly. In its standard formulation, doxazosin requires a multistep titration regimen to minimize a possible first-dose effect. A new extended-release gastrointestinal therapeutic system (GITS) formulation of doxazosin was developed to improve the pharmacokinetic profile of the parent compound and to reduce or eliminate the need for dose titration and the potential risk of overdosing. This review presents an analysis of the effect of doxazosin GITS monotherapy on blood pressure (BP) and tolerability, as evaluated in four clinical trials, two conducted in patients with stage 1 to stage 2 hypertension and two in patients with BPH with different levels of BP. Doxazosin GITS was as effective as doxazosin standard and more effective than placebo was in reducing and controlling BP in patients with hypertension. Among normotensive patients with BPH, no clinically significant effect on BP was observed and no episodes of syncope were recorded. Doxazosin GITS was generally better tolerated than doxazosin standard, based on the proportion of patients with adverse events and those withdrawing due to adverse events. Moreover, the GITS formulation eliminated the need for titration in most patients. Doxazosin GITS is an effective and well-tolerated treatment in patients with hypertension and/or BPH and without heart failure or clinical coronary heart disease and has advantages over doxazosin standard in terms of a simpler dosing regimen and improved tolerability.

多沙唑嗪是治疗高血压、良性前列腺增生(BPH)及两者合并症的有效药物。在其标准配方中,多沙唑嗪需要多步滴定方案,以尽量减少可能的首次剂量效应。为了改善母体化合物的药代动力学特征,减少或消除剂量滴定的需要和潜在的过量风险,开发了一种新的胃肠治疗系统(GITS)制剂doxazosin。这篇综述分析了doxazosin GITS单药治疗对血压(BP)和耐受性的影响,在四项临床试验中进行了评估,其中两项在1至2期高血压患者中进行,两项在血压水平不同的BPH患者中进行。Doxazosin GITS在降低和控制高血压患者血压方面的效果与Doxazosin标准药相同,比安慰剂更有效。在血压正常的BPH患者中,没有观察到对血压的临床显著影响,也没有晕厥发作的记录。从不良事件患者和因不良事件停药患者的比例来看,Doxazosin GITS的耐受性普遍优于Doxazosin标准。此外,GITS配方消除了大多数患者滴定的需要。Doxazosin GITS是一种有效且耐受性良好的治疗方法,适用于高血压和/或BPH且无心力衰竭或临床冠心病的患者,并且在给药方案更简单和耐受性更好方面优于Doxazosin标准。
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引用次数: 12
Evaluation of the efficacy and tolerability of nebivolol versus lisinopril in the treatment of essential arterial hypertension: a randomized, multicentre, double-blind study. 奈比洛尔与赖诺普利治疗原发性动脉高血压的疗效和耐受性评价:一项随机、多中心、双盲研究。
Pub Date : 2003-05-01 DOI: 10.1080/08038020310000104
Enrico Agabiti Rosei, Damiano Rizzoni, Silvia Comini, Gianluca Boari

The main objective of this study was to compare the anti-hypertensive efficacy and safety of nebivolol (5 mg once daily) and lisinopril (20 mg once daily) given for 12 weeks in patients with mild to moderate essential hypertension. Fourteen centres participated in this randomized, double-blind parallel group study. Sixty-eight patients with uncomplicated mild-to-moderate hypertension were randomized, and sixty-five were eligible for the analysis of efficacy (intention-to-treat). Hypertensive patients were newly diagnosed, or previous antihypertensive therapy was withdrawn at least 1 month before active treatment, and were included in the study if their diastolic blood pressure (DBP) was > 95 and < 114 mmHg. The age range was 24-65 years. The primary endpoints of the study were: (i) response rate: patients were defined as "normalized" responders if their blood pressure values were < 140/90 mmHg, or as "non-normalized" responders if the reduction in blood pressure was 10 mmHg or more, compared with baseline; (ii) changes in sitting blood pressure at the end of the study. The secondary endpoints were: standing blood pressure and sitting or standing heart rate (HR). Results showed that baseline sitting DBP was significantly different between groups. Analysis of covariance of the raw data performed with baseline as covariate demonstrated that the DBP and HR values were significantly lower in the nebivolol group at the 8th week. However, when an analysis of variance for repeated measures was performed, a significant reduction in sitting systolic blood pressure (SBP) (p < 0.0001), DBP (p < 0.0001) and HR (p < 0.0001) was observed throughout the study in both groups. No difference was observed between treatments, although for DBP, a significant interaction between treatment-weeks was observed (p = 0.016). There was also a statistically significant difference in favour of the nebivolol group in the distribution of responders and non-responders at week 8. Lisinopril and nebivolol were equally well tolerated. In conclusion, nebivolol was slightly more effective, in comparison with lisinopril, in terms of reduction in DBP. This greater efficacy was obtained without any increase in adverse effects, since both treatments were equally well tolerated.

本研究的主要目的是比较奈比洛尔(5mg每日1次)和赖诺普利(20mg每日1次)治疗轻至中度原发性高血压患者12周的降压疗效和安全性。14个中心参与了这项随机双盲平行组研究。68例无并发症的轻中度高血压患者被随机分组,其中65例符合疗效分析(意向治疗)。新诊断的高血压患者,或在积极治疗前至少1个月停止既往降压治疗的高血压患者,舒张压(DBP) > 95和< 114 mmHg纳入研究。年龄范围为24-65岁。该研究的主要终点是:(i)缓解率:如果患者的血压值< 140/90 mmHg,则定义为“正常化”缓解者,如果与基线相比,血压降低10 mmHg或更高,则定义为“非正常化”缓解者;(ii)研究结束时坐着血压的变化。次要终点是:站立血压和坐着或站立心率(HR)。结果显示,两组患者基线坐位舒张压差异显著。以基线为协变量对原始数据进行协方差分析表明,在第8周时,纳比洛尔组的DBP和HR值显著降低。然而,当对重复测量进行方差分析时,在整个研究过程中,两组的坐位收缩压(SBP) (p < 0.0001)、舒张压(p < 0.0001)和心率(p < 0.0001)均显著降低。治疗组间无差异,但DBP治疗周间有显著的相互作用(p = 0.016)。在第8周,在应答者和无应答者的分布上,纳比洛尔组也有统计学上的显著差异。赖诺普利和奈比洛的耐受性同样良好。总之,奈比洛尔在舒张压降低方面比赖诺普利更有效。这种更大的疗效没有任何不良反应的增加,因为两种治疗都同样耐受良好。
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引用次数: 36
The comparative pharmacology of angiotensin II receptor antagonists. 血管紧张素II受体拮抗剂的比较药理学研究。
Pub Date : 2001-01-01 DOI: 10.1080/080370501750066444
M. Burnier, M. Maillard
Several orally active non-peptide angiotensin II subtype 1 (AT1) receptor antagonists are now available for the treatment of hypertension. These agents have a common mechanism of action--blockade of the binding of angiotensin II to the subtype 1 receptor--and their binding to this receptor is generally insurmountable. There are some pharmacokinetic and pharmacodynamic differences between these antagonists, which may reflect in their clinical efficacy, especially at the end of the dosing interval. Losartan has an active metabolite that prolongs its duration of action, and candesartan cilexetil requires conversion to an active form after administration. Telmisartan has the longest duration of action, with a terminal elimination half-life of around 24 h in comparison with 11-15 h for irbesartan, the agent with the next longest half-life. The long duration of action and insurmountable binding to the receptor may be related to the slow dissociation kinetics of the antagonists from the AT1 receptor. Comparative clinical studies suggest that at the recommended dose losartan, the original drug in this class, has a lower antihypertensive efficacy than the newer agents, such as telmisartan. It is possible that these differences between angiotensin II receptor antagonists are due to variations in the degree and duration of receptor blockade, and may be of clinical significance with regard to the cardioprotective and renoprotective effects of this class of antihypertensive agents.
几种口服活性非肽血管紧张素II亚型1 (AT1)受体拮抗剂现在可用于治疗高血压。这些药物具有共同的作用机制——阻断血管紧张素II与亚型1受体的结合——并且它们与该受体的结合通常是不可克服的。这些拮抗剂之间存在一些药代动力学和药效学差异,这可能反映在它们的临床疗效上,特别是在给药间隔结束时。氯沙坦有一种活性代谢物,可延长其作用时间,坎地沙坦西蕾地酯在给药后需要转化为活性形式。替米沙坦的作用时间最长,终末半衰期约为24小时,而次之的厄贝沙坦为11-15小时。拮抗剂与AT1受体的缓慢解离动力学可能与作用持续时间长和与受体的不可克服的结合有关。比较临床研究表明,在推荐剂量下,这类药物的原始药物氯沙坦的降压效果低于较新的药物,如替米沙坦。血管紧张素II受体拮抗剂之间的这些差异可能是由于受体阻断程度和持续时间的差异,并且可能对这类降压药的心脏保护和肾保护作用具有临床意义。
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引用次数: 37
The problem of hypertension in the elderly. 老年人高血压的问题。
Pub Date : 2000-01-01
T Hedner

Since most developed countries have an ageing population, the prevalence of hypertension is increasing. This age-driven increase in cardiovascular risk is an important factor contributing to the increasing burden of mortality and morbidity associated with cardiovascular disease. Today, there is a strong rationale for an aggressive approach to hypertension since antihypertensive treatment has been shown to reduce cardiovascular mortality and morbidity in the elderly. It is likely that increasing emphasis will be placed on control of isolated and borderline systolic hypertension, which are the predominant forms of hypertension in elderly patients. The recent second Swedish Trial in Old Patients with Hypertension (STOP-Hypertension-2) represents an important contribution to the literature since it shows that newer antihypertensive agents, such as angiotensin converting enzyme (ACE) inhibitors and calcium antagonists, are as effective as older agents in reducing cardiovascular mortality and morbidity in elderly patients.

由于大多数发达国家都存在人口老龄化问题,高血压的患病率正在上升。这种年龄驱动的心血管风险增加是导致与心血管疾病相关的死亡率和发病率负担增加的一个重要因素。今天,由于降压治疗已被证明可以降低老年人心血管疾病的死亡率和发病率,因此有强有力的理由支持积极治疗高血压。孤立性和边缘性收缩期高血压是老年患者高血压的主要形式,因此很可能越来越重视对这两种高血压的控制。最近的瑞典老年高血压患者试验(STOP-Hypertension-2)是对文献的重要贡献,因为它表明新的抗高血压药物,如血管紧张素转换酶(ACE)抑制剂和钙拮抗剂,在降低老年患者心血管死亡率和发病率方面与老年药物一样有效。
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引用次数: 0
The outcome of STOP-Hypertension-2 in relation to the 1999 WHO/ISH hypertension guidelines. 与1999年WHO/ISH高血压指南相关的STOP-Hypertension-2的结果
Pub Date : 2000-01-01
L H Lindholm

The 1999 hypertension management guidelines issued by the World Health Organization and the International Society of Hypertension emphasize the importance of blood pressure reduction in the prevention of cardiovascular events. Furthermore, they conclude that the benefits of treatment are due to blood pressure lowering per se, rather than to any specific antihypertensive therapy. The results of the second Swedish Trial in Old Patients with Hypertension (STOP-Hypertension-2) are consistent with these recommendations, since in this trial angiotensin converting enzyme (ACE) inhibitors and calcium antagonists reduced blood pressure to the same extent as conventional therapy with beta-blockers and diuretics in elderly hypertensive patients, and the three treatments produced similar reductions in the risk of cardiovascular events. Furthermore, a first subgroup analysis of cardiovascular mortality showed that the three treatments seemed equally effective in diabetic patients. The STOP-Hypertension-2 data, therefore, are fully consistent with the 1999 hypertension management guidelines, and underline the advantages offered by both older and newer antihypertensive therapies.

世界卫生组织和国际高血压学会发布的1999年高血压管理指南强调了降低血压对预防心血管事件的重要性。此外,他们得出结论,治疗的好处是由于血压降低本身,而不是任何特定的降压治疗。第二项瑞典老年高血压患者试验(STOP-Hypertension-2)的结果与这些建议一致,因为在该试验中,血管紧张素转换酶(ACE)抑制剂和钙拮抗剂降低老年高血压患者血压的程度与使用β受体阻滞剂和利尿剂的常规治疗相同,并且三种治疗方法在降低心血管事件风险方面效果相似。此外,心血管死亡率的第一亚组分析显示,这三种治疗方法对糖尿病患者似乎同样有效。因此,STOP-Hypertension-2的数据与1999年高血压管理指南完全一致,并强调了旧的和新的抗高血压疗法所提供的优势。
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引用次数: 0
Preserving target-organ function with candesartan cilexetil in patients with hypertension. 坎地沙坦西列地酯对高血压患者靶器官功能的保护作用。
Pub Date : 2000-01-01
F Zannad

Epidemiological evidence suggests that reducing blood pressure alone in hypertensive patients delays the onset of cardiovascular events without necessarily preventing the progression of chronic target-organ disease, such as end-stage renal failure and heart failure. Successful clinical management of hypertensive patients will therefore not be possible unless therapies are aimed both at the effective control of blood pressure and at the preservation of target-organ function. The new angiotensin II type I (AT1) receptor blocker candesartan cilexetil has been shown to be effective in reducing target-organ damage in animal models of hypertension, even at doses that do not produce significant reductions in blood pressure. Protective effects of candesartan cilexetil towards the heart and kidney have also been demonstrated in the clinical studies that have been conducted to date. Thus, candesartan cilexetil has been shown to induce regression of left ventricular hypertrophy within 8-12 weeks of treatment and to improve renal haemodynamics, both acutely and after 6 weeks of treatment in hypertensive patients. Furthermore, in hypertensive patients with co-existent non-insulin-dependent diabetes mellitus and microalbuminuria, 12 weeks of treatment with candesartan cilexetil, 8-16 mg, significantly reduced urinary albumin excretion. Clinical evidence is therefore accumulating that the antihypertensive efficacy and tolerability profile already established for candesartan cilexetil is combined with the renal and cardioprotective effects necessary for optimal management of hypertension.

流行病学证据表明,高血压患者单独降低血压可以延缓心血管事件的发生,而不一定能预防慢性靶器官疾病的进展,如终末期肾衰竭和心力衰竭。因此,除非治疗的目标是有效控制血压和保持靶器官功能,否则不可能成功地对高血压患者进行临床治疗。新型血管紧张素II型I (AT1)受体阻滞剂坎地沙坦西列地酯在高血压动物模型中已被证明可有效减少靶器官损伤,即使剂量不显著降低血压。坎地沙坦西列地酯对心脏和肾脏的保护作用也已在迄今为止进行的临床研究中得到证实。因此,坎地沙坦西列地尔已被证明在治疗8-12周内诱导左心室肥厚消退,并改善高血压患者急性期和治疗6周后的肾脏血流动力学。此外,在同时存在非胰岛素依赖型糖尿病和微量白蛋白尿的高血压患者中,坎地沙坦西列地酯8-16 mg治疗12周后,尿白蛋白排泄明显减少。因此,越来越多的临床证据表明,坎地沙坦西列地酯的降压疗效和耐受性,以及对高血压的最佳管理所必需的肾脏和心脏保护作用,已经建立起来。
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引用次数: 0
Improving prognosis in hypertension: exploring the benefits of angiotensin II type 1 receptor blockade. 改善高血压预后:探索血管紧张素II型1受体阻断的益处。
Pub Date : 2000-01-01
L Ruilope

Prognosis can be improved in hypertensive patients not only by reducing blood pressure, but probably also by effective suppression of adverse neurohormonal influences. Inhibition of the renin-angiotensin system by angiotensin-converting enzyme inhibitors effectively reduces left ventricular hypertrophy and decreases morbidity and mortality due to heart failure, as well as slowing the progression of renal disease. Initial data from studies of angiotensin II type 1 (AT1) receptor blockers indicate that these agents should also be effective in reducing cardiac and renal damage. In this class, candesartan, by virtue of its tight and long-lasting binding to the AT1-receptor, provides pronounced 24-h blood pressure control with effective blockade of all the major negative cardiovascular effects of angiotensin II. Candesartan cilexetil has also been shown to be effective and well tolerated in combination with hydrochlorothiazide in those hypertensive patients who require more than one agent to reach their target blood pressure.

高血压患者的预后不仅可以通过降低血压来改善,还可能通过有效抑制不良神经激素的影响来改善。血管紧张素转换酶抑制剂抑制肾素-血管紧张素系统可有效减少左心室肥厚,降低心力衰竭引起的发病率和死亡率,并减缓肾脏疾病的进展。血管紧张素II型1 (AT1)受体阻滞剂研究的初步数据表明,这些药物也可有效减少心脏和肾脏损害。在这类药物中,坎地沙坦由于其与at1受体紧密而持久的结合,提供了明显的24小时血压控制,有效阻断血管紧张素II的所有主要负面心血管影响。坎地沙坦西列地酯与氢氯噻嗪联合使用对那些需要一种以上药物才能达到目标血压的高血压患者也是有效且耐受性良好的。
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引用次数: 0
The outcome of STOP-Hypertension-2 in relation to the 1999 WHO/ISH hypertension guidelines. 与1999年WHO/ISH高血压指南相关的STOP-Hypertension-2的结果
Pub Date : 2000-01-01 DOI: 10.1080/713782695
L. Lindholm
The 1999 hypertension management guidelines issued by the World Health Organization and the International Society of Hypertension emphasize the importance of blood pressure reduction in the prevention of cardiovascular events. Furthermore, they conclude that the benefits of treatment are due to blood pressure lowering per se, rather than to any specific antihypertensive therapy. The results of the second Swedish Trial in Old Patients with Hypertension (STOP-Hypertension-2) are consistent with these recommendations, since in this trial angiotensin converting enzyme (ACE) inhibitors and calcium antagonists reduced blood pressure to the same extent as conventional therapy with beta-blockers and diuretics in elderly hypertensive patients, and the three treatments produced similar reductions in the risk of cardiovascular events. Furthermore, a first subgroup analysis of cardiovascular mortality showed that the three treatments seemed equally effective in diabetic patients. The STOP-Hypertension-2 data, therefore, are fully consistent with the 1999 hypertension management guidelines, and underline the advantages offered by both older and newer antihypertensive therapies.
世界卫生组织和国际高血压学会发布的1999年高血压管理指南强调了降低血压对预防心血管事件的重要性。此外,他们得出结论,治疗的好处是由于血压降低本身,而不是任何特定的降压治疗。第二项瑞典老年高血压患者试验(STOP-Hypertension-2)的结果与这些建议一致,因为在该试验中,血管紧张素转换酶(ACE)抑制剂和钙拮抗剂降低老年高血压患者血压的程度与使用β受体阻滞剂和利尿剂的常规治疗相同,并且三种治疗方法在降低心血管事件风险方面效果相似。此外,心血管死亡率的第一亚组分析显示,这三种治疗方法对糖尿病患者似乎同样有效。因此,STOP-Hypertension-2的数据与1999年高血压管理指南完全一致,并强调了旧的和新的抗高血压疗法所提供的优势。
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引用次数: 3
Results of the STOP-Hypertension-2 trial. STOP-Hypertension-2试验结果。
Pub Date : 2000-01-01 DOI: 10.1080/713782693
L. Hansson
The second Swedish Trial in Old patients with Hypertension (STOP-Hypertension-2) was conducted to compare the effects of "newer" antihypertensive therapies (angiotensin converting enzyme [ACE] inhibitors and calcium antagonists) and established therapies (beta-blockers and diuretics) on cardiovascular mortality and morbidity in elderly hypertensive patients. A total of 6614 patients were randomized to receive conventional treatment, ACE inhibitors or calcium antagonists, and followed for a mean of 5 years. The primary endpoint was a combination of fatal stroke, fatal myocardial infarction and other fatal cardiovascular disease; secondary endpoints were a combination of fatal or non-fatal stroke or myocardial infarction, and other cardiovascular mortality. The three treatments produced similar reductions in supine systolic blood pressure. There were no significant differences in the risk of cardiovascular events between patients receiving conventional therapy and those receiving newer therapies. All three treatments were well tolerated. The STOP-Hypertension-2 results thus add to the extensive literature showing the benefits of blood pressure reduction in elderly hypertensive patients. Moreover, they are consistent with current management guidelines which emphasise the importance of the achieved blood pressure reduction in the prevention of cardiovascular events.
第二项瑞典老年高血压患者试验(STOP-Hypertension-2)的目的是比较“较新的”降压疗法(血管紧张素转换酶抑制剂和钙拮抗剂)和已有疗法(受体阻滞剂和利尿剂)对老年高血压患者心血管死亡率和发病率的影响。共有6614例患者随机接受常规治疗、ACE抑制剂或钙拮抗剂,平均随访5年。主要终点为致死性卒中、致死性心肌梗死和其他致死性心血管疾病的组合;次要终点是致死性或非致死性卒中或心肌梗死以及其他心血管死亡率的组合。三种治疗方法对仰卧位收缩压的降低效果相似。在接受常规治疗的患者和接受新治疗的患者之间,心血管事件的风险没有显著差异。三种治疗方法均耐受良好。STOP-Hypertension-2的研究结果进一步证实了老年高血压患者降压的益处。此外,它们与当前的管理指南一致,该指南强调实现血压降低对预防心血管事件的重要性。
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引用次数: 21
期刊
Blood pressure. Supplement
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