Felodipine. A review of the pharmacology and therapeutic use of the extended release formulation in cardiovascular disorders.

Felodipine is a vascular-selective, dihydropyridine calcium antagonist previously investigated as a conventional tablet formulation administered twice daily. More recently considerable experience has been gained with an extended release (ER) formulation which has the convenience of once daily administration. Felodipine ER has been well studied in patients with essential hypertension. As monotherapy in mild to moderate essential hypertension, felodipine ER is at least as effective in reducing blood pressure as other calcium antagonists, beta-blockers, diuretics and ACE inhibitors, with some results favouring felodipine ER at a statistically significant level at the dosages used. It is also effective combined with controlled release metoprolol or enalapril in patients with mild to moderate essential hypertension. In patients with more severe forms of essential hypertension uncontrolled by beta-blocker and/or diuretic therapy, felodipine ER was effective as an 'add-on' therapy in placebo-controlled trials, and, at the dosages used, more effective than either sustained release nifedipine or nitrendipine. Felodipine produces effective control of blood pressure without negative effects on cardiac performance. In addition to its antihypertensive action, results suggest that felodipine therapy is associated with significant regression of left ventricular hypertrophy. Furthermore, it appears suitable for use in patients with concomitant diabetes, renal dysfunction or asthma, and is also being investigated for use in patients with congestive heart failure or angina pectoris. Felodipine ER is an effective drug for the treatment of all grades of essential hypertension, and can be used both as monotherapy and in combination with other antihypertensive agents. Further clinical experience should fully establish the long term tolerability of felodipine ER and consequently its place in therapy relative to other accepted antihypertensive drugs. However, with the convenience of once daily administration, felodipine ER is a worthwhile innovation in the treatment of hypertension.     

Diuretics as a basis of antihypertensive therapy. An overview

Diuretics have been, except for during a few recent years, the most commonly used therapy for hypertension. Although use of these agents fell significantly in the early 1990s, since then it has begun to increase again. Their recent return to popularity reflects 3 major factors: (i) recognition of the effectiveness of much lower dosages than previously used, thereby providing good antihypertensive activity with fewer adverse effects; (ii) the excellent reductions in morbidity and mortality achieved by low dosage diuretic-based therapy in multiple randomised controlled trials in elderly patients with hypertension; and (iii) the increasing recognition that some diuretic-induced shrinkage of effective blood volume is essential for the adequate treatment of many, if not most, patients with hypertension. Therefore, diuretics will probably continue to be the basis for antihypertensive therapy, and the indapamide sustained release 1.5 mg formulation provides all the essential characteristics of diuretic therapy.     

Perception of symptoms in hypertensive patients and the relevance to the application of anti- hypertensive drug therapy

While symptoms are common during the detection and treatment of hypertensive patients it is rarely the case that either uncomplicated essential hypertension (of whatever severity) or treatment presents insurmountable problems. Unfortunately they frequently result in changes in effective therapy or encourage clinicians and prescribers to settle with altered and inadequate treatment goals. This review considers the association of patients' symptoms in the management of hypertension. It considers the relationship of symptoms at the time of diagnosis and the impact of symptoms voiced during active drug treatment. The data relating antihypertensive therapy to adverse symptoms during chronic therapy and the consequences of this on treatment goals are summarised.     

步长脑心通在原发性高血压病中的运用及对C反应蛋白、一氧化氮的影响

目的观察步长脑心通在原发性高血压病中的运用及对C反应蛋白（CRP）和一氧化氮（NO）的影响,探讨脑心通的作用机制。方法 120例原发性高血压病患者随机分为常规治疗组（n=60）及脑心通组（n=60）。常规治疗组应用降压药物治疗使血压控制在140/90 mmHg以下。不使用其他调脂、抗氧化药物、非类固醇类消炎镇痛药物;脑心通组在常规治疗基础上加用步长脑心通胶囊,疗程为4周。治疗前后测定CRP、NO。结果经治疗后CRP均有下降,NO均明显升高,脑心通组与常规治疗组比较,变化更明显（P〈0.05）。结论步长脑心通胶囊治疗原发性高血压通过降低CRP水平,提高NO水平而起到抑制炎症,改善内皮功能等作用,对预防脑血栓形成是有效、安全的治疗手段。     

THE EFFECT OF PRAZOSIN THERAPY ON PLATELET ACTIVATION IN ESSENTIAL HYPERTENSION

1. Plasma levels of beta-thromboglobulin, initial and total platelet aggregation (induced by adrenaline or adenosine diphosphate [ADP]) were determined in 26 normotensive subjects and 26 patients with untreated essential hypertension. Groups of 18 essential hypertensive patients and 18 age- and sex-matched normotensives were compared. 2. After 7 days of treatment with prazosin in a dose of 2-8 mg daily the above measures were repeated in 18 essential hypertensive patients. A significant increase in plasma levels of beta-thromboglobulin, initial and total adrenaline-induced as well as ADP-induced platelet aggregation was found in hypertensives. Prazosin restored the mean arterial blood pressure in hypertensives to normal, but it had no significant influence either on increased beta-thromboglobulin levels or on initial and total aggregability. 3. The results confirm increased platelet aggregation and in vivo platelet activation in patients with essential hypertension; however there is a discrepancy with previous reports about those results obtained after prazosin therapy. The results suggest that increased platelet aggregation and in vivo activation need not be restored to normal after effective antihypertensive therapy alone. They give reason for the combination of antihypertensive together with anti-aggregatory therapy in essential hypertension.     

固定复方降压药物对高血压病患者依从性及疗效的影响

目的 探讨用药形式对高血压病患者依从性的影响,寻求提高血压控制率的方法.方法 将160例初发轻中度高血压病患者随机分成固定复方组和简单合用组.固定复方组服用固定复方制剂(成分为厄贝沙坦150 mg/氢氯噻嗪12.5 mg)1 次/d;简单合用组分别服用厄贝沙坦150 mg及氢氯噻嗪12.5 mg.1次/d.观察3个月内2组依从性和临床疗效差别.结果 1个月时固定复方组和简单合用组收缩压分别为(139.4±3.6)和(141.3±5.7)mm Hg,舒张压分别是(83.2±2.1)和(85.5±3.8)mm Hg,2组差异无统计学意义(P>0.05).3个月时固定复方降压药物组依从性达61.5%(48例),收缩压(138.4±2.2)mm Hg,血压达标率56.4%(44例),均明显好于简单合用组[依从性45.6%(36例),收缩压(146.3±2.7)mm Hg,血压达标率46.8%(37例),差异有统计学意义(P<0.05)].结论 固定复方制剂降压药物使高血压病患者依从性更好,降压疗效更佳.

Abstract：

Objecfive To compare the effects of fix-combination with simple combination on the antihypertensive activity and compliance.Methods Totally 160 patients with initial mild-moderate essential hypertension were randomized into two groups:fix-combination or simple combination with irbesartan and hydrochlorothiazide groups.The antihypertensive activity and tolerability within three months were monitored.Results Compared with simple combination(141.3±5.7)mm Hg and(85.5±3.8)mm Hg,fix-combination(139.4±3.6)mm Hg and (83.2±2.1)mm Hg did not further decrease the systolic and diastolic blood pressure within 1 month's treatment (P>0.05).However,3 months later,the systolic blood pressure,the rate of reaching blood pressure target and tolerability were improved more in fix-combination group than that in simple combination group(all P<0.05).Conclusion Fix-combination antihypertensive therapy can increase antihypertensive activity and tolerability in patients with initial mild-moderate essential hypertension.     

阿托伐他汀联合应用左旋氨氯地平治疗原发性高血压临床研究

目的探讨联合应用阿托伐他汀与左旋氨氯地平治疗原发性高血压的临床疗效。方法将95例原发性高血压患者随机分为治疗组和对照组。治疗组采用阿托伐他汀联合左旋氨氯地平治疗,对照组单独采用左旋氨氯地平治疗,观察期为3个月,分别于治疗前后测定两组血压及血脂水平,并进行统计学分析。结果两组治疗前血压和血脂差异均无统计学意义(均P0.05);治疗3个月后,治疗组血脂指标和收缩压的下降幅度大于对照组,而舒张压及脉压差的下降幅度对照组大于治疗组,差异均有统计学意义(P0.05)。治疗期间所有患者均无其他严重不良反应。结论阿托伐他汀与左旋氨氯地平联合应用可更显著地降低高血压病患者的收缩压、脉压差和血脂,临床疗效显著优于单一用药,不良反应少,患者耐受性好,是一种较理想的降压治疗方案。     

Biodegradable synthetic polyesters in the technology of controlled dosage forms of antihypertensive drugs – the overview

ABSTRACT

Introduction: Arterial hypertension is a disease of civilization that requires long-term treatment. Recently, growing interest in natural and synthetic polymers as drug delivery vehicles in controlled release dosage forms for improving the efficacy of treatment has been observed.

Areas covered: This review introduces biodegradable synthetic polyesters as macromolecular carriers of antihypertensive drugs. Although various, synthetic and natural polymer-drug conjugates and/or polymeric carriers of anticancer drugs are currently under preclinical and clinical studies, there is no such data for antihypertensive drugs. Therefore, it seems appropriate to use such materials for the treatment of hypertension.

Expert opinion: There are currently only a few studies describing the use of synthetic polyesters in the arterial hypertension therapy. In order to the fact that there is a high demand for new, effective antihypertensive dosage forms, further studies for such drug carriers are certainly expected. Synthetic polyester carriers could improve the drug bioavailability and its pharmacokinetic properties by altering the pharmaceutical dosage form. This property is particularly useful for drugs with proven pharmacological action, but with limited application due to their inappropriate pharmacological properties. The development of new polymeric materials and technologies affords the opportunity to produce novel synthetic polyester DDSs.     

辛伐他汀调脂治疗对高血压病人降压平滑性的影响

目的：观察辛伐他汀调脂治疗对原发性高血压病人降压平滑性的影响。方法：入选86例血脂正常或略高（LDL—C〈3．1mmol／L）的原发性高血压患者随机分为辛伐他汀调脂治疗组和对照组两组。两组降压治疗无差异,降压药物剂量调整直至目标血压〈140／90mmHg,调脂治疗组采用辛伐他汀20mg每晚1次口服调脂治疗,所有病人均于治疗前及治疗8周后行24h动态血压检测,比较两组患者治疗后血压变化及对降压平滑性指数（smoothness index,SI）的影响。结果：两组治疗后血压无明显差异（P〉0．05）,辛伐他汀调脂治疗组SI（6．2）高于对照组SI（2．8）（P〈0．05）。结论：辛伐他汀调脂治疗能够提高原发性高血压病人的降压平滑性。     

依那普利联合氢氯噻嗪治疗原发性高血压31例疗效观察

目的探讨依那普利联合氢氯噻嗪治疗原发性高血压的临床疗效。方法将2008年12月至2010年12月我院住院原发性高血压患者62例随机分为治疗组和对照组,两组治疗前2周停服其他降压药物,并监测血压。对照组给予依那普利10mg/次,每日2次;治疗组在对照组基础上给予氢氯噻嗪l2.5mg/次,每日1次,连服8周,观察比较两组的治疗疗效。结果疗程结束后,治疗组显效率和总有效率与对照组相比,均有显著性差异(P<0.05)。治疗组和对照组的收缩压、舒张压均较治疗前明显降低,且治疗组血压降低较对照组更明显(P<0.05)。两组不良反应发生率比较差异显著(P<0.05)。结论依那普利联合氢氯噻嗪治疗原发性高血压具有协同降压作用,优于单纯用药,同时两种药物的某些不良反应可相互抵消,安全性好,值得推广。     

常用降压药物的相互作用

高血压是心脑血管疾病的主要危险因素之一,安全和有效的控制血压是降低心脑血管疾病风险必不可少的措施。本文简单介绍了常用的5种降压药物（利尿剂、钙拮抗剂、β肾上腺素受体阻滞剂、血管紧张素转换酶抑制剂、血管紧张素Ⅱ受体阻滞剂）联合应用的原则,重点介绍这5种降压药物联合应用时可能产生的药物相互作用,以及与其它非降压药物联合应用时可能产生的药物相互作用。旨在引起临床关注联合治疗中药物的相互作用和对用药安全产生的影响。     

比索洛尔/氢氯噻嗪与比索洛尔治疗高血压临床试验

目的：评价比索洛尔／氢氯噻嗪复方片治疗轻中度原发性高血压的疗效和安全性。方法：选择73例轻中度原发性高血压患者，按随机、双盲双模拟及平行对照原则分为比索洛尔／氢氯噻嗪复方片组（A组）41例，比索洛尔组（B组）32例，分别观察两组降压疗效、不良反应及对血生化的影响。结果：服药8周后，A、B两组总有效率分别为75．6％和37．5％（P〈0．01）。A组及B组患者血脂、尿酸、血糖及血钾无不良影响。结论：比索洛尔／氢氯噻嗪复方片降压作用显著优于比索洛尔，可作为治疗轻中度原发性高血压的一线药物。     

左旋氨氯地平联合依拉普利在原发性高血压中的应用效果

目的 针对左旋氨氯地平联合依拉普利在原发性高血压中的应用效果进行分析研究.方法 随机选择2014年1月至2015年2月我院收治120例原发性高血压患者,将其平均分为对照组和观察组,作为本次研究的对象.对照组患者实施左旋氨氯地平治疗,观察组患者实施左旋氨氯地平联合依拉普利治疗.针对观察组和对照组患者的临床治疗有效率,以及治疗的过程中患者发生的不良反应和血压等指标,进行对比分析.结果 在本次研究中,治疗后观察组患者的血压与治疗前比较,差异有统计学意义(P＜0.05);观察组患者治疗后的血压与对照组比较,差异有统计学意义(P＜0.05).本次研究中观察组和对照组患者的临床治疗总有效率分别为96.67％、83.33％,差异有统计学意义(P＜0.05).观察组与对照组患者在治疗过程中总不良反应发生率分别为5.00％、21.67％,差异有统计学意义(P＜0.05).结论 在原发性高血压患者的治疗中,使用左旋氨氯地平联合依拉普利治疗,其降压效果较好,且在治疗的过程中,患者产生的不良反应少,总体临床治疗效果显著,安全性较高.     

肝移植术后高血压患者的药学监护

目的：加强对肝移植术后高血压药物治疗的合理性和安全性。方法：阐述肝移植后高血压的特点及影响因素,确定肝移植术后高血压药物的选择及监护要点。结果与结论：肝移植患者高血压药物的选择,应在治疗原发性高血压的基础上,充分考虑其可能的禁忌证、不良反应及与免疫抑制药物的相互作用,进行个体化给药。目前,CCB类药常被作为首选药使用。     

Economics of antihypertensive therapy in the elderly

Because of the high incidence of morbidity and mortality associated with hypertension in the elderly, the treatment of hypertension in this patient group must involve consideration of clinical, humanistic and economic outcomes. The most frequently used method of pharmacoeconomic analysis for antihypertensive therapy involves cost-effectiveness analysis, although several other methods are available. Current evidence reveals a trend toward cost effectiveness of antihypertensive treatment in elderly patients. However, these formal analyses are limited by the need for extrapolation of data regarding efficacy and level of risk from epidemiological and randomised trials, information which is often lacking. To incorporate economic factors into clinical decision making, other measures of economic impact should be explored. The economic impact of antihypertensive therapy is affected by the level of risk for the patient and the efficacy of the treatment. Data indicate that the risk of morbidity and mortality related to hypertension increases with age and that current antihypertensive drugs reduce this risk. When choosing an antihypertensive agent, the following parameters should be considered: acquisition cost, likelihood of adverse effects and other determinants of treatment adherence, and individual predictors of response. The economic outcomes will be maximised if prudent drug selection is supplemented by appropriate diagnostic and classification procedures and reduction of cardiovascular risk factors other than hypertension. The accumulation of data addressing the risks and benefits of therapy for the very old and the comparative efficacy of newer antihypertensive therapies will further clarify the decision-making process.     

Calcium metabolism, calcium-channel blocking agents, and hypertension management

Increasing evidence has suggested that a disturbance of cellular calcium metabolism may have a role in initiating and maintaining elevated systemic vascular resistance in essential hypertension. Controversy exists over whether calcium can alleviate or exacerbate the hypertensive process, and diversity of calcium metabolism in hypertensive patients has been proposed. Calcium-channel blocking agents are potent vasodilators capable of correcting the elevated systemic vascular resistance. Clinical studies have shown that these drugs have antihypertensive efficacy comparable to established agents. The elderly, blacks, and patients with low renin activity respond well to calcium-channel blockers. These drugs may also offer potential advantages over established antihypertensive agents in patients with other coexisting diseases. Sustained release formulations have been developed, and initial experience with long-term efficacy and tolerability is encouraging. The calcium-channel blockers may become first-line therapy for treatment of hypertension in selected patients.     

贝那普利与卡托普利降压效果的对比研究

目的 对比观察贝那普利与卡托普利治疗轻、中度高血压患者的临床疗效与安全性.方法 将120例高血压患者随机平分为两组,分别给予贝那普利和卡托普利治疗,均加用小剂量氢氯噻嗪, 治疗8周, 于治疗前及治疗8周末行血压监测, 评定各组降压效果.结果 贝那普利组患者降压有效率高于卡托普利组,组间比较差异有统计学意义(P<0.05);不良反应发生率两组间差异无统计学意义(P>0.05).结论 贝那普利对轻、中度原发性高血压病有较好的降压效果,联合应用小剂量利尿剂可提高疗效.     

Comparison of two slow-release formulations of metoprolol with conventional metoprolol and atenolol in hypertensive patients

We have compared the beta-adrenoceptor blocking and antihypertensive effects of chronic once daily treatment with conventional metoprolol 200 mg, two 'long-acting' formulations of metoprolol 200 mg and atenolol 100 mg in a cross-over study in 12 hypertensive patients concurrently receiving diuretic therapy. The peak effects of all compounds were similar, with significant reductions in exercise heart rate and blood pressure. Twenty-four hours after dosing only atenolol treatment was consistently associated with a reduction in both exercise heart rate (P less than 0.001) and blood pressure (P less than 0.02) when compared with placebo. Once daily treatment of hypertension with metoprolol, even in 'long-acting' formulations, cannot be recommended because of waning antihypertensive effect which would be missed at routine clinic attendance. Metoprolol should be prescribed twice daily in hypertension. So-called long-acting formulations do not always confer benefits over conventional dose forms.     

厄贝沙坦治疗原发性高血压的临床疗效和靶器官保护

目的评价厄贝沙坦治疗原发性高血压的临床疗效及其对原发性高血压左心室肥厚(LVH)的逆转作用以及对肾功能的保护作用。方法 100例确诊为高血压病患者服用厄贝沙坦150 mg,每天1次,每周随访1次,治疗12周,监测治疗前及治疗中24 h动态血压水平及肾功能指标。用超声心动图测量LVH患者左心室肥厚的改善情况。结果厄贝沙坦治疗后,患者24 h平均收缩压及舒张压、日间及夜间收缩压及舒张压均有明显下降(P<0.01),血及尿β2-MG明显减少(P<0.01)。经厄贝沙坦治疗后左心室重量(left ventricular hypertraphy,LVMI)明显下降(P<0.01)。结论厄贝沙坦对原发性高血压患者有良好的平稳降压效果,对原发性高血压患者的LVH有逆转作用,且对其肾功能有良好的保护作用。     

实施国家基本药物制度对社区居民高血压管理影响的调查分析

目的:了解国家基本药物制度实施后社区居民高血压管理情况,为进一步推广国家基本药物制度、完善社区居民高血压管理、减轻高血压患者的用药负担提供参考。方法:以基层医疗卫生机构工作人员、社区(镇、村)居民为对象,就国家基本药物制度和高血压相关知识了解情况、降压药品费用、高血压管理需求等进行问卷调查,并对调查结果进行统计分析。结果:受访的全部基层医疗卫生机构工作人员和83.75%的社区居民了解国家基本药物制度;受访的社区高血压患者国家基本药物制度实施后的人均降压药品费用下降了36.76%;社区居民高血压诊断标准的掌握率提高了24.50%,且受访的社区居民对高血压相关危险因素更加了解;受访的社区高血压患者用药依从性提高;受访者的高血压管理需求有所增加;受访者也反映存在国家基本药物目录中降压药物品种少等问题。结论:国家基本药物制度实施有利于促进社区居民高血压管理的完善,应进一步加强国家基本药物制度和高血压知识的公众教育,以利2012年版《国家基本药物目录》的顺利实施并为社区居民高血压治疗带来更大的受益。