• 【依那普利引起的持续性干咳:发病率取决于所使用的方法。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:Yeo WW,Ramsay LE
    BACKGROUND & AIMS: :In a cohort of 136 hypertensive patients started consecutively on enalapril the incidence of persistent dry cough by life-table analysis was 14.6% (95% CI 10.2-19.0%). The incidence in women (19.2%; 95% CI 11.3-27.1%) was twice that in men (9.7%; 95% CI 6.6-12.8%). Dry cough was unrelated to age, smoking habit, renal function, or the dose and duration of enalapril treatment. In one half of patients who developed cough enalapril had to be stopped. The incidence of withdrawal due to cough was 6.0% (95% CI 4.5-7.5%), and cough was by far the most common reason for discontinuing enalapril treatment. Reviewing previous studies of enalapril-induced cough, it is evident that postmarketing surveillance studies have grossly underestimated the incidence and importance of this side-effect. Surveys in hospital clinics have slightly underestimated the true incidence through failure to use life-table methods of analysis.
    背景与目标: :在136名依那普利连续开始的高血压患者队列中,根据生命表分析,持续性干咳的发生率为14.6%(95%CI 10.2-19.0%)。女性(19.2%; 95%CI 11.3-27.1%)的发病率是男性(9.7%; 95%CI 6.6-12.8%)的两倍。干咳与年龄,吸烟习惯,肾功能或依那普利治疗的剂量和持续时间无关。在发生咳嗽的依那普利患者中,有一半必须停止治疗。咳嗽引起的戒断发生率为6.0%(95%CI为4.5-7.5%),而咳嗽是迄今为止停用依那普利治疗的最常见原因。回顾以前对依那普利引起的咳嗽的研究,很明显,上市后的监测研究严重低估了这种副作用的发生率和重要性。医院诊所的调查由于未使用生命表分析方法而略低了真实发生率。
  • 【依那普利对首次急性心肌梗塞后左心室功能和运动表现的影响。 EDEN研究调查员。】 复制标题 收藏 收藏
    DOI:10.1016/s0167-5273(97)02960-4 复制DOI
    作者列表:
    BACKGROUND & AIMS: AIMS:To study the effects of early use of enalapril on left ventricular function and exercise capacity after a first acute myocardial infarction, 356 patients without overt signs of congestive heart failure were randomly allocated to receive placebo or enalapril between days 7 and 14 after a first myocardial infarction. The study was conducted double-blind in 40 hospitals throughout Spain.

    METHODS AND RESULTS:At baseline and after 26 weeks of follow-up exercise stress tests, Doppler-echocardiograms and isotopic ventriculography were performed in study participants. At the end of follow-up, patients in the enalapril group had lower end-systolic volume compared to those in the placebo group (55 vs. 62 ml; P=0.05). No difference in exercise capacity was evident between both groups.

    CONCLUSION:The present study shows that enalapril therapy administered between 7 and 14 days after a first acute myocardial infarction decreases end-systolic volume and may inhibit the remodeling process of the left ventricle.

    背景与目标: AIMS :为了研究早期使用依那普利对首次急性心肌梗塞后左心室功能和运动能力的影响,随机分配356例无明显充血性心力衰竭迹象的患者接受安慰剂或依那普利第一次心肌梗塞后的第7天和第14天。该研究在西班牙的40所医院中进行了双盲研究。

    方法和结果:在基线以及随访运动压力测试26周,多普勒超声心动图和同位素心室造影后在研究参与者中进行。随访结束时,依那普利组患者的收缩末期容积较安慰剂组低(55 vs. 62 ml; P = 0.05)。两组之间的运动能力无明显差异。

    结论:本研究表明,在首次急性心肌梗死后7到14天之间服用依那普利治疗可减少收缩末期容积并可能抑制左心室的重塑过程。

  • 【依普利农,依那普利及其联合治疗对Ⅱ型糖尿病大鼠糖尿病肾病的影响。】 复制标题 收藏 收藏
    DOI:10.1093/ndt/gfn448 复制DOI
    作者列表:Kang YS,Ko GJ,Lee MH,Song HK,Han SY,Han KH,Kim HK,Han JY,Cha DR
    BACKGROUND & AIMS: BACKGROUND:Recent data suggest that aldosterone antagonists have beneficial effects on diabetic nephropathy. In this study, we investigated the dose-dependent effect of eplerenone and a combined treatment with eplerenone and enalapril compared with each drug alone on renal function in type II diabetic rats. To further explore the molecular mechanism of action of combination therapy, we also performed in vitro study. METHODS:The animals were divided into six groups as follows: normal control Long-Evans Tokushima Otsuka (LETO) rats, Otsuka Long-Evans Tokushima Fatty (OLETF) rats, OLETF rats treated with low dose of eplerenone (50 mg/kg/day), OLETF rats treated with high dose of eplerenone (200 mg/kg/day), OLETF rats treated with enalapril (10 mg/kg/day) and OLETF rats treated with a combination of both drugs (eplerenone 200 mg/kg/day and enalapril 10 mg/kg/day) for 6 months. RESULTS:Treatment of OLETF rats had no significant effect on body weight, kidney weight and blood glucose levels. However, urinary albumin excretion, glomerular filtration rate and glomerulosclerosis were significantly improved in the enalapril group and improvement was observed in a dose-dependent manner in the eplerenone groups; the most dramatic decreases were observed in the combination group. In accordance with these findings, renal expressions of TGF-beta1, type IV collagen and PAI-1 were also markedly decreased in the treatment groups, with the combined treatment providing the most significant level of improvement. In cultured mesangial cells, combined treatment resulted in an additive decrease in TGF-beta1, PAI-1 and collagen gene expressions and protein production induced by high glucose and aldosterone stimulation. CONCLUSIONS:Aldosterone receptor antagonism provided additional benefits beyond blockade of the renin-angiotensin system in type II diabetic nephropathy.
    背景与目标: 背景:最近的数据表明,醛固酮拮抗剂对糖尿病肾病具有有益的作用。在这项研究中,我们调查了依普利农以及依普利农和依那普利联合治疗与每种药物单独治疗对II型糖尿病大鼠肾功能的剂量依赖性作用。为了进一步探讨联合治疗的分子机制,我们还进行了体外研究。
    方法:将动物分为六组:正常对照组长埃文斯德岛大冢(LETO)大鼠,大冢长埃文斯德岛胖子(OLETF)大鼠,低剂量依普利农(50 mg / kg /天)治疗的OLETF大鼠),接受高剂量依普利农(200 mg / kg /天)治疗的OLETF大鼠,接受依那普利(10 mg / kg /天)治疗的OLETF大鼠和接受两种药物联合治疗(依普利酮200 mg / kg /天)的OLETF大鼠和依那普利10毫克/公斤/天)服用6个月。
    结果:OLETF大鼠的治疗对体重,肾脏重量和血糖水平无明显影响。但是依那普利组尿白蛋白排泄,肾小球滤过率和肾小球硬化明显改善,依普利农组剂量依赖性。在组合组中观察到最大的下降。根据这些发现,在治疗组中,TGF-β1,IV型胶原和PAI-1的肾表达也显着降低,联合治疗提供了最显着的改善水平。在培养的肾小球系膜细胞中,联合处理导致高葡萄糖和醛固酮刺激诱导的TGF-β1,PAI-1和胶原基因表达以及蛋白质产生的累加减少。
    结论:醛固酮受体拮抗剂在II型糖尿病肾病中除了阻断肾素-血管紧张素系统外,还提供了其他益处。
  • 【卡托普利和依那普利清除自由基的活性比较:高血压糖尿病患者体内研究三个月。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:Bain SC,Le Guen CA,Lunec J,Barnett AH
    BACKGROUND & AIMS: :Lipid peroxides and fluorescent serum proteins, possible markers of free radical activity, are increased in diabetic patients, particularly those with angiopathy. Captopril, an angiotensin converting enzyme (ACE) inhibitor, scavenges free radicals in vitro independently of ACE inhibition. This is probably due to the presence of a sulphydryl group which is not present in other ACE inhibitor drugs. We have compared the effects of captopril and enalapril on free radical activity in thirty-two diabetic subjects with hypertension (BP greater than 160/95 mmHg). After a three week run-in period on no antihypertensive therapy, patients were randomly allocated to receive captopril or enalapril, the dose titrated according to BP response. After three months, BP was well controlled in both groups and glycaemic control unchanged. Both drugs were associated with a reduction of fluorescent IgG (captopril:Baseline [BL] 0.564 vs. 12 weeks [w] 0.428, P less than 0.05, enalapril:BL 0.603 vs. 12w 0.422 P less than 0.05) and thiobarbituric acid reactive material (captopril:BL 2.35 nmol MDA vs. 12w 1.46 nmol, P less than 0.05, enalapril:BL 2.44 nmol vs. 12w 1.72 nmol, P less than 0.01). In contrast to in vitro studies, there was no significant difference between the drugs when used in therapeutic doses, questioning a hypothesised advantage of captopril over enalapril.
    背景与目标: :脂质过氧化物和荧光血清蛋白,可能是自由基活性的标志物,在糖尿病患者,特别是患有血管病的患者中增加。卡托普利是一种血管紧张素转化酶(ACE)抑制剂,可在体外独立于ACE抑制清除自由基。这可能是由于存在其他ACE抑制剂药物中不存在的巯基。我们已经比较了卡托普利和依那普利对32例高血压糖尿病患者的自由基活性的影响(血压大于160/95 mmHg)。经过三周的不使用降压疗法的磨合期后,患者被随机分配接受卡托普利或依那普利治疗,剂量根据BP反应而调整。三个月后,两组血压均得到良好控制,血糖控制未改变。两种药物均与荧光IgG(卡托普利:基线[BL] 0.564比12周[w] 0.428,P小于0.05,依那普利:BL 0.603与12w 0.422 P小于0.05)降低有关,并且硫代巴比妥酸反应性物质减少(卡托普利:BL 2.35 nmol MDA与12w 1.46 nmol,P小于0.05,依那普利:BL 2.44 nmol与12w 1.72 nmol,P小于0.01)。与体外研究相反,当以治疗剂量使用时,两种药物之间没有显着差异,这质疑了卡托普利相对于依那普利的假设优势。
  • 【直接压缩的儿科患者新的马来酸依那普利口服分散剂微型片剂。】 复制标题 收藏 收藏
    DOI:10.2174/1567201817666200508093442 复制DOI
    作者列表:Ortega CA,Favier LS,Cianchino VA,Cifuente DA
    BACKGROUND & AIMS: BACKGROUND:In many countries, hypertension in the pediatric population is considered a serious risk of mortality and morbidity. In this respect, it is central to design and develop new pharmaceutical forms for pediatric patients with hypertension. The development of Orodispersible Mini-Tablets (ODMTs) for pediatric use has gained importance in recent years. Therefore, regulations for developing suitable and palatable dosage forms for pediatric patients have been established by WHO authorities. OBJECTIVE:This study aimed to design and develop orodispersible mini tablets of enalapril maleate (EnM ODMTs) for pediatric use. METHODS:Five pharmaceutical formulations (A, B, C, D and E, shown in Table 1) were designed. The effects of different co-processed excipients and active pharmaceutical ingredients at different doses were studied. Lactose co-processed excipients selected were the following: Tablettose® 80, Microce- Lac® 100 and StarLac®. The micromeritic properties for all the physical mixtures were examined. The mini tablets were obtained by direct compression. Quality control parameters were determined in accordance with US Pharmacopeia. RESULTS:Three OMDTs with StarLac® showed good results of hardness, flow ability and fast disintegration. The formulation with 0.1 mg of enalapril maleate presented the best results for the official parameters of hardness (4.0 kp), friability (< 1%), disintegration time (28 s), drug content uniformity (103.6 %), and wetting time (23 s). CONCLUSION:The three OMDTs with StarLac® showed good quality parameters, according to official requirements. Formulation A exhibited the best wetting time, complying with the dose recommended for pediatric patients. This formulation could be considered eligible for being manufactured at industrial scale.
    背景与目标: 背景:在许多国家,小儿人群的高血压被认为具有严重的死亡和发病风险。在这方面,为小儿高血压患者设计和开发新的药物形式是至关重要的。近年来,用于儿童的可口分散小片剂(ODMT)的开发变得越来越重要。因此,世卫组织当局已经制定了开发适用于儿科患者的合适且可口的剂型的法规。
    目的:本研究旨在设计和开发用于儿科的马来酸依那普利口服分散微型片剂(EnM ODMTs)。
    方法:设计了五种药物制剂(表1所示为A,B,C,D和E)。研究了不同剂量的不同共处理的赋形剂和活性药物成分的作用。选择的乳糖共加工的赋形剂如下:Tablettose®80,Microce-Lac®100和StarLac®。检查了所有物理混合物的微链性能。通过直接压制获得小片剂。根据美国药典确定质量控制参数。
    结果:三种采用StarLac®的OMDT显示出良好的硬度,流动性和快速崩解效果。含有0.1 mg马来酸依那普利的配方在以下各项的官方参数中表现出最好的结果:硬度(4.0 kp),脆碎度(<1%),崩解时间(28 s),药物含量均匀性(103.6%)和润湿时间(23) s)。
    结论:根据官方要求,采用StarLac®的三种OMDT显示出良好的质量参数。配方A表现出最佳的润湿时间,符合儿科患者推荐的剂量。可以认为该制剂符合工业规模生产的条件。
  • 【比索洛尔和依那普利最初6个月单药治疗轻度至中度慢性心力衰竭的临床效果。来自CIBIS III试验的数据。】 复制标题 收藏 收藏
    DOI:10.1007/s10557-008-6116-9 复制DOI
    作者列表:Dobre D,van Veldhuisen DJ,Goulder MA,Krum H,Willenheimer R
    BACKGROUND & AIMS: PURPOSE:To assess the clinical effects and safety profile of initial monotherapy with either bisoprolol or enalapril in elderly patients with heart failure (HF). METHODS:In CIBIS III, 1010 patients with mild to moderate HF and age>or=65 years were randomized to monotherapy with either bisoprolol or enalapril for 6 months. RESULTS:Bisoprolol had a similar effect as enalapril on the combined end-point of all-cause mortality or hospitalization (HR 1.02; p=0.90), as well as on each of the individual end-points. A trend towards fewer sudden deaths was observed with bisoprolol (NS). On the other hand, more cases of worsening HF requiring hospitalization or occurring while in hospital were observed in the bisoprolol group (HR 1.67; p=0.03). The two groups were similar with regard to treatment cessations and early introduction of the second drug. CONCLUSIONS:Bisoprolol and enalapril had a similar effect on the combined end-point of mortality or hospitalization during 6 months monotherapy. However, more worsening HF events were observed in the bisoprolol group.
    背景与目标: 目的:评估比索洛尔或依那普利初次单药治疗老年心力衰竭(HF)的临床效果和安全性。
    方法:在CIBIS III中,将1010例轻度至中度HF且年龄≥65岁的患者随机分为比索洛尔或依那普利单药治疗6个月。
    结果:比索洛尔在全因死亡率或住院综合终点(HR 1.02; p = 0.90)以及各个终点上具有与依那普利相似的作用。比索洛尔(NS)观察到突然死亡的趋势有所减少。另一方面,在比索洛尔组中观察到更多需要住院治疗或在住院期间发生的心衰恶化病例(HR 1.67; p = 0.03)。两组在停止治疗和早期引入第二种药物方面相似。
    结论:比索洛尔和依那普利对6个月单药治疗死亡率或住院综合终点的影响相似。但是,在比索洛尔组中观察到更严重的HF事件。
  • 【在心脏疾病的实验模型中,Serelaxin比依那普利更有效的抗纤维化作用。】 复制标题 收藏 收藏
    DOI:10.1161/HYPERTENSIONAHA.114.03594 复制DOI
    作者列表:Samuel CS,Bodaragama H,Chew JY,Widdop RE,Royce SG,Hewitson TD
    BACKGROUND & AIMS: :Relaxin is a naturally occurring peptide hormone that mediates systemic hemodynamic and renal adaptive changes during pregnancy and abrogates aberrant scar tissue formation (fibrosis) in diverse pathogeneses. However, its efficacy relative to renin–angiotensin system blockade, the most effective antifibrotic strategy currently available, is not known. We compared the individual versus combined antifibrotic effects of serelaxin (a recombinant form of human gene-2 relaxin) and the angiotensin-converting enzyme inhibitor enalapril, in preventative (started before injury) and therapeutic (treatment of established fibrosis) strategies, in a mouse model of isoprenaline-induced cardiac injury (at 17 days). Changes in systolic blood pressure, organ hypertrophy, and tissue remodeling/fibrosis were assessed. Pretreatment with serelaxin (0.5 mg/kg per day via subcutaneous administration) alone reduced cardiac fibrosis to a greater extent than enalapril (200 mg/L via drinking water; equivalent to 48 mg/kg per day) alone (P<0.05 versus enalapril alone). Additionally, the combined effects of serelaxin and enalapril reduced cardiac fibrosis by at least 2-fold compared with enalapril alone, when administered preventatively or therapeutically; by suppressing transforming growth factor-β1 expression and phosphorylation of Smad2 (an intracellular regulator of transforming growth factor-β1 activity; both P<0.05 versus enalapril alone) to a greater extent. The effects of serelaxin were independent of blood pressure, while enalapril lowered systolic blood pressure in the model studied. These findings suggest that serelaxin alone and in combination with an angiotensin-converting enzyme inhibitor more effectively ameliorates fibrosis than angiotensin-converting enzyme inhibition alone in the diseased heart, in a clinically relevant experimental scenario.
    背景与目标: :松弛素是一种天然存在的肽激素,可在妊娠期间介导全身血液动力学和肾脏适应性变化,并消除多种病原体中异常的疤痕组织形成(纤维化)。但是,相对于肾素-血管紧张素系统阻滞剂(目前可用的最有效的抗纤维化策略)的疗效尚不清楚。我们在小鼠的预防(从受伤前开始)和治疗(已确立的纤维化治疗)策略中比较了Serelaxin(人类基因2松弛素的重组形式)和血管紧张素转化酶抑制剂依那普利的个体与联合抗纤维化作用。异丙肾上腺素诱发的心脏损伤模型(第17天)。评估收缩压,器官肥大和组织重塑/纤维化的变化。与单独使用依那普利(200 mg / L,通过饮用水;相当于每天48 mg / kg)相比,单独使用serelaxin(经皮下给药每天0.5 mg / kg)进行预处理可减少更大程度的心脏纤维化(与单独使用enalapril相比,P <0.05 )。此外,当预防性或治疗性给药时,与单独的依那普利相比,塞拉辛和依那普利的联合作用可使心脏纤维化减少至少两倍。通过更大程度地抑制转化生长因子-β1的表达和Smad2(转化生长因子-β1活性的细胞内调节剂; P <0.05与依那普利单独使用)的磷酸化来实现。 Serelaxin的作用与血压无关,而依那普利可降低所研究模型的收缩压。这些发现表明,在临床相关的实验情况下,与单独的血管紧张素转化酶抑制相比,单独的Serelaxin以及与血管紧张素转化酶抑制剂联合使用在患病心脏中比单独的血管紧张素转化酶抑制更有效地改善了纤维化。
  • 【依那普利的上市后监督。 I:处方事件监控的结果。】 复制标题 收藏 收藏
    影响因子 :
    发表时间:1988-10-01
    来源期刊:BMJ
    DOI:10.1136/bmj.297.6652.826 复制DOI
    作者列表:Inman WH,Rawson NS,Wilton LV,Pearce GL,Speirs CJ
    BACKGROUND & AIMS: :To identify and measure the incidence of adverse effects of the angiotensin converting enzyme inhibitor enalapril 13,713 patients were studied for one year by prescription-event monitoring. Precise information about the duration of treatment was available for 12,543 patients. The frequency of many events was calculated, including dizziness (483 patients; 3.9%), persistent dry cough (360; 2.9%), headache (310; 2.5%) hypotension (218; 1.7%), and syncope (155; 1.2%). Less common reactions included angioedema, urticaria, and muscle cramps. Altogether 1098 (8%) patients died and the notes of 913 of them (83%) were obtained for detailed scrutiny. With the exception of a few patients with renal failure who deteriorated during treatment (reported on separately), no death was attributed to enalapril. Enalapril was considered to be effective, even in patients with advanced cardiac failure. These results for enalapril are reassuring and provide further evidence of the value of prescription-event monitoring.
    背景与目标: :为了鉴定和测量血管紧张素转化酶抑制剂依那普利的不良反应发生率,通过处方事件监测对13713例患者进行了为期一年的研究。有关治疗持续时间的准确信息可供12543名患者使用。计算了许多事件的发生频率,包括头晕(483例; 3.9%),持续干咳(360; 2.9%),头痛(310; 2.5%),低血压(218; 1.7%)和晕厥(155; 1.2%)。 )。较不常见的反应包括血管性水肿,荨麻疹和肌肉痉挛。共有1098名患者(8%)死亡,其中913名患者(83%)的病历得到了详细的检查。除少数在治疗期间恶化的肾衰竭患者(单独报告)外,依那普利没有死亡。依那普利被认为是有效的,即使在晚期心力衰竭患者中也是如此。依那普利的这些结果令人放心,并为处方事件监测的价值提供了进一步的证据。
  • 【依那普利引起的咳嗽与非严重心力衰竭有关。】 复制标题 收藏 收藏
    DOI:10.1016/j.ijcard.2008.03.063 复制DOI
    作者列表:Sadanaga T,Yoshimura M,Sakamoto T,Sumida H,Ogawa H
    BACKGROUND & AIMS: :The incidence of enalapril-induced cough was evaluated in 199 patients with congestive heart failure. Cough was more frequent in class I or II patients (28%) than in class III (4.1%, p<0.01) and class IV (0%, p<0.01) patients. Brain natriuretic peptide level was lower in patients in the cough (+) group than in the cough (-) group (170+/-107 vs. 538+/-637 pg/ml, p<0.01). The incidence of enalapril-induced cough is low in patients with severe congestive heart failure and a cough can be a marker of non-severe heart failure.
    背景与目标: :对199例充血性心力衰竭患者进行了依那普利引起的咳嗽的发生率评估。 I级或II级患者(28%)比III级(4.1%,p <0.01)和IV级(0%,p <0.01)患者咳嗽更为频繁。咳嗽()组患者的脑钠肽水平低于咳嗽(-)组(170 / -107 vs. 538 / -637 pg / ml,p <0.01)。依那普利引起的咳嗽在严重充血性心力衰竭患者中的​​发生率较低,咳嗽可能是非严重心力衰竭的标志。
  • 【替米沙坦和依那普利对冠心病合并糖尿病肾病患者心室重构和肾脏预后的影响。】 复制标题 收藏 收藏
    DOI:10.3892/etm.2016.3933 复制DOI
    作者列表:Hou Y,Zhang F,Liu Z,Su S,Wu X,Wang Z
    BACKGROUND & AIMS: :The aim of the present study was to compare the value of telmisartan and enalapril on ventricular remodeling and kidney prognosis of patients with coronary artery disease complicated with diabetic nephropathy, and provide discussion on clinical reasonably chosen medicine. A total of 60 cases of coronary artery disease complicated with diabetic nephropathy were randomly divided for telmisartan (80 mg/day) treatment (n=32), enalapril (10 mg/day) treatment (n=28), while the rest of the therapy was kept the same. After 12 weeks, the clinical effects were compared between different groups. It was found that in comparison with enalapril group, the left ventricular ejection fraction of telmisartan group was significantly higher, and left ventricular end-diastolic diameter was significantly lower (P<0.05). The serum creatinine level and 24-h protein of telmisartan group were significantly lower than that for the enalapril group (P<0.05). In conclusion, the regular telmisartan treatment for patients with coronary artery disease complicated with diabetic nephropathy is better than enalapril on ventricular remodeling and kidney prognosis.
    背景与目标: :本研究的目的是比较替米沙坦和依那普利在冠心病合并糖尿病肾病患者心室重构和肾脏预后中的价值,并为临床合理选择药物提供讨论。随机将60例合并糖尿病肾病的冠心病患者随机分为替米沙坦(80 mg /天)治疗(n = 32),依那普利(10 mg / day)治疗(n = 28)。疗法保持不变。 12周后,比较不同组之间的临床效果。结果发现,与依那普利组相比,替米沙坦组左心室射血分数明显升高,而舒张末期左心室直径明显降低(P <0.05)。替米沙坦组的血清肌酐水平和24-h蛋白水平明显低于依那普利组(P <0.05)。综上所述,常规替米沙坦治疗冠心病合并糖尿病肾病的患者在心室重构和肾脏预后方面优于依那普利。
  • 【依那普利和肾脏:由于抑制血管紧张素II的形成,导致肾血管舒张和钠尿。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:Navis GJ,de Zeeuw D,de Jong PE
    BACKGROUND & AIMS: :Essential hypertension is characterized by increased renal vascular resistance, which also has definite implications for renal sodium handling. We studied the possibility of correcting these abnormalities by inhibiting angiotensin-converting enzyme with enalapril. Enalaprilic acid produced renal vasodilation. This, particularly postglomerular, vasodilation was accompanied with an increase in sodium excretion. The natriuresis was positively correlated to initial plasma renin activity. During continuous treatment with enalapril up to 12 weeks, this vasodilation persisted in 22 patients with essential hypertension. We also showed that orally administered enalapril induces natriuresis, both during a 50-mmol and during a 200-mmol sodium intake a day. This natriuresis caused a net negative sodium balance of approximately 120-140 mmol Na after 1 week of enalapril therapy. This was accompanied with a fall in body weight. We conclude that enalapril in essential hypertension alleviates the angiotensin-II-mediated abnormalities in renal hemodynamics and sodium excretion.
    背景与目标: :原发性高血压的特征是肾血管阻力增加,这对肾钠处理也具有一定意义。我们研究了通过用依那普利抑制血管紧张素转化酶来纠正这些异常的可能性。依那普利酸产生肾血管舒张。这尤其是肾小球后血管舒张伴随着钠排泄的增加。钠尿与初始血浆肾素活性呈正相关。在依那普利连续治疗长达12周的过程中,这种血管扩张在22例原发性高血压患者中持续存在。我们还表明,口服依那普利每天钠摄入量为50毫摩尔和200毫摩尔时均诱发利尿。利尿钠治疗1周后,这种钠尿导致钠的净负平衡约为120-140 mmol Na。这伴随着体重的下降。我们得出的结论是,依那普利在原发性高血压中缓解了血管紧张素II介导的肾脏血液动力学和钠排泄异常。
  • 【依那普利和GLP类似物(艾塞那肽)在糖尿病肾病中的肾保护作用比较。】 复制标题 收藏 收藏
    DOI:10.1055/s-0034-1372584 复制DOI
    作者列表:Çavusoglu T,Erbas O,Karadeniz T,Akdemir O,Acikgoz E,Karadeniz M,Tuglu MI,Ates U
    BACKGROUND & AIMS: BACKGROUND:One of the major concerns is a nephropathy in diabetes, which applies many different kinds of medicines. However, required level of the treatment of renal disease has not been achieved. AIM:To investigate and compare the effect of the enalapril and the exenatide on diabetic nephropathy in rats developed diabetes by streptozosin. MATERIAL AND METHODS:32 male Sprague Dawley rats were divided into 4 groups: (1) Control, (2) Diabetic (DM), (3) DM+ Enalapril, and (4) DM+ exenatide groups. Then, the animals were euthanized and their blood samples were collected by cardiac puncture for blood glucose; blood urea nitrogen (BUN), creatinin, and nephrectomy were performed for histopathologic examination, and urine samples were taken on stick for proteinuria. RESULTS:Administration of the enalapril or the exenatide in diabetic rats resulted in a significant reduction both fibronectin, induced nitric oxide synthase (i-NOS) expression in glomerular area and urine protein levels. It was shown that both of enalapril and exenatide protected the renal glomerulus more than diabetic group in the nephropathy histopathologically. CONCLUSION:The beneficial effects of enalapril and exenatide which reduces fibronectin, i-NOS expression and urine protein levels or increases recovery of glomerules, might be used for preventing the harmful effects of diabetic nephropathy.
    背景与目标: 背景:主要关注的问题之一是糖尿病肾病,它应用了许多不同种类的药物。但是,尚未达到所需的肾脏疾病治疗水平。
    目的:研究和比较依那普利和艾塞那肽对链脲佐菌素开发的糖尿病大鼠糖尿病肾病的作用。
    材料与方法:将32只Sprague Dawley雄性大鼠分为4组:(1)对照组,(2)糖尿病(DM),(3)DM依那普利和(4)DM艾塞那肽组。然后,对动物实施安乐死,并通过心脏穿刺收集其血液样本中的血糖;进行血液尿素氮(BUN),肌酐和肾切除术以进行组织病理学检查,并在棒上采集尿液样本中的蛋白尿。
    结果:在糖尿病大鼠中服用依那普利或艾塞那肽可显着降低纤连蛋白,诱导的肾小球区域一氧化氮合酶(i-NOS)表达和尿蛋白水平。从组织病理学上来看,依那普利和艾塞那肽对肾小球的保护作用均大于糖尿病组。
    结论:依那普利和艾塞那肽的有益作用可降低纤维连接蛋白,i-NOS表达和尿蛋白水平或增加肾小球的回收率,可用于预防糖尿病肾病的有害作用。
  • 【依那普利,美托洛尔和地高辛长期单药治疗对射血分数降低的犬左室功能障碍和扩张的影响。】 复制标题 收藏 收藏
    DOI:10.1161/01.cir.89.6.2852 复制DOI
    作者列表:Sabbah HN,Shimoyama H,Kono T,Gupta RC,Sharov VG,Scicli G,Levine TB,Goldstein S
    BACKGROUND & AIMS: BACKGROUND:Recent clinical trials have suggested that therapy with angiotensin-converting enzyme inhibitors in asymptomatic patients with reduced left ventricular (LV) function can significantly reduce the incidence of congestive heart failure compared with patients receiving placebo. In the present study, we examined the effects of long-term monotherapy with enalapril, metoprolol, and digoxin on the progression of LV systolic dysfunction and LV chamber enlargement in dogs with reduced LV ejection fraction (EF). METHODS AND RESULTS:LV dysfunction was produced in 28 dogs by multiple sequential intracoronary microembolizations. Embolizations were discontinued when LVEF was 30% to 40%. Three weeks after the last embolization, dogs were randomized to 3 months of oral therapy with enalapril (10 mg twice daily, n = 7), metoprolol (25 mg twice daily, n = 7), digoxin (0.25 mg once daily, n = 7), or no treatment (control, n = 7). As expected, in untreated dogs, LVEF decreased (36 +/- 1% versus 26 +/- 1%, P < .001) and LV end-systolic volume (ESV) and end-diastolic volume (EDV) increased during the 3-month follow-up period (39 +/- 4 versus 57 +/- 6 mL, P < .001, and 61 +/- 6 versus 78 +/- 8 mL, P < .002, respectively). In dogs treated with enalapril or metoprolol, LVEF remained unchanged or increased after therapy compared with before therapy (35 +/- 1% versus 38 +/- 3% and 35 +/- 1% versus 40 +/- 3%, respectively, P < .05), whereas ESV and EDV remained essentially unchanged. In dogs treated with digoxin, EF remained unchanged but ESV and EDV increased significantly. CONCLUSIONS:In dogs with reduced LVEF, long-term therapy with enalapril or metoprolol prevents the progression of LV systolic dysfunction and LV chamber dilation. Therapy with digoxin maintains LV systolic function but does not prevent progressive LV enlargement.
    背景与目标: 背景:最近的临床试验表明,与接受安慰剂的患者相比,对无症状的左心室(LV)功能降低的无症状患者进行血管紧张素转换酶抑制剂治疗可以显着降低充血性心力衰竭的发生率。在本研究中,我们检查了依那普利,美托洛尔和地高辛长期单药治疗对左室射血分数(EF)降低的犬左室收缩功能障碍和左室扩大的影响。
    方法与结果:28例犬经多次冠状动脉内微栓塞术后产生LV功能障碍。当LVEF为30%至40%时,栓塞停止。最后一次栓塞后三周,将狗随机分为3个月口服依那普利(每天两次10毫克,n = 7),美托洛尔(每天两次25mg,n = 7),地高辛(0.25毫克每天一次,n = 7)口服治疗7)或不进行任何治疗(对照组,n = 7)。正如预期的那样,在未经治疗的狗中,LVEF在3个月内下降了(36 /-1%比26 /-1%,P <.001),LV收缩末期容积(ESV)和舒张末期容积(EDV)增加了随访期(分别为39 /-4对57 /-6 mL,P <.001和61 /-6对78 /-8 mL,P <.002)。在接受依那普利或美托洛尔治疗的狗中,与治疗前相比,LVEF在治疗后保持不变或升高(分别为35 /-1%对38 /-3%和35 /-1%对40 /-3%,P <.05 ),而ESV和EDV基本上保持不变。在用地高辛治疗的狗中,EF保持不变,但ESV和EDV显着增加。
    结论:对于LVEF降低的犬,依那普利或美托洛尔的长期治疗可防止LV收缩功能障碍和LV腔扩张。地高辛的治疗可维持左心室收缩功能,但不能防止进行性左心室肥大。
  • 【第三项血管扩张剂-心力衰竭试验(V-HeFT III)的原理和设计:非洛地平作为依那普利和loop利尿剂联合或不联合地高辛治疗慢性充血性心力衰竭的辅助治疗。 V-HeFT III调查员。】 复制标题 收藏 收藏
    DOI:10.1016/s0002-9149(96)00136-1 复制DOI
    作者列表:Boden WE,Ziesche S,Carson PE,Conrad CH,Syat D,Cohn JN
    BACKGROUND & AIMS: Therapy with angiotensin-converting enzyme inhibitors and nonselective vasodilators (hydralazine and isosorbide dinitrate) has become accepted treatment in patients with symptomatic, chronic congestive heart failure (CHF), and has been demonstrated in large clinical trials to ameliorate symptoms, improve exercise performance, and reduce cardiac mortality. Nevertheless, the management of patients with CHF remains a therapeutic challenge. The second Vasodilator-Heart Failure Trial (V-HeFT II) showed that the average 2-year mortality with enalapril (18%) was significantly lower than that with hydralazine-isosorbide dinitrate (25%) but, somewhat surprisingly, the nonspecific vasodilators produced significantly more improvement in exercise performance and left ventricular function. Such data suggest that improvement in symptoms, hemodynamics, and survival may not be afforded by the use of a single class of vasodilator therapy, but might be optimized by the combined use of different agents. This report describes the rationale and design of V-HeFT III, a multicenter, prospective, randomized, double-blind, placebo-controlled trial comparing the effects of chronic oral extended-release felodipine (felodipine ER) 2.5 to 5 mg twice daily, when added to a stable regimen of enalapril and loop diuretics, with or without digoxin, on exercise performance, morbidity, and mortality in patients with New York Heart Association functional class II to III CHF followed for a minimum of 12 weeks. Felodipine is a second-generation dihydropyridine calcium antagonist with a high degree of vascular selectivity which, in the doses used in this study, exerts its systemic arterial effect by decreasing peripheral vascular resistance without producing negative inotropic effects. The results of V-HeFT III may shed important light on the role of additive vasodilator therapy in the management of patients with CHF.

    背景与目标: 血管紧张素转换酶抑制剂和非选择性血管扩张剂(肼苯哒嗪和硝酸异山梨酯)的治疗已成为有症状,慢性充血性心力衰竭(CHF)患者的公认治疗方法,并且已在大型临床试验中证明其可改善症状,改善运动表现并降低心脏死亡率。然而,CHF患者的治疗仍然是治疗上的挑战。第二项血管扩张剂心脏衰竭试验(V-HeFT II)表明,依那普利(2%)的平均2年死亡率显着低于二氢肼屈嗪-异山梨醇酯(25%),但令人惊讶的是,产生了非特异性血管扩张剂显着改善运动表现和左心室功能。这些数据表明,使用单类血管扩张剂治疗可能无法改善症状,血液动力学和存活率,但可以通过组合使用不同的药物来优化症状,血液动力学和存活率。本报告介绍了V-HeFT III的原理和设计,该研究是一项多中心,前瞻性,随机,双盲,安慰剂对照试验,比较了慢性口服缓释非洛地平(非洛地平ER)2.5至5 mg每天两次的效果,当时在有心脏心脏功能衰竭的纽约心脏协会II级至III级CHF患者中,将其加入稳定的依那普利和loop利尿剂治疗方案(有或没有地高辛)对运动表现,发病率和死亡率的影响,持续至少12周。非洛地平是第二代二氢吡啶类钙拮抗剂,具有高度的血管选择性,在本研究中使用的剂量,可通过降低周围血管阻力而发挥系统性动脉效应,而不会产生负性变力作用。 V-HeFT III的结果可能会进一步阐明加性血管扩张剂治疗在CHF患者治疗中的作用。

  • 【乐卡地平,依那普利及其组合在老年高血压患者中的治疗:安慰剂对照,随机,交叉研究与四种ABPM。】 复制标题 收藏 收藏
    DOI:10.1038/sj.jhh.1002248 复制DOI
    作者列表:Puig JG,Calvo C,Luurila O,Luurila H,Sulosaari S,Strandberg A,Ghezzi C
    BACKGROUND & AIMS: :This double-blind, placebo-controlled, four-way balanced design crossover study included hypertensive patients aged 60-85 years with mean office-measured sitting systolic blood pressure (SBP) 160-179 mm Hg and daytime SBP > or =135 mm Hg. After a 2-week run-in period, during which previous medications were discontinued, each patient received the following four treatments in randomized order for 4 weeks each: lercanidipine 10 mg (L), enalapril 20 mg (E), lercanidipine 10 mg plus enalapril 20 mg (L/E) and placebo (P). At the end of each treatment period, office trough blood pressure (BP) was measured and a 24-h Ambulatory Blood Pressure Monitoring (ABPM) was performed. Seventy-five patients (mean age 66 years, office BP 168/92 mm Hg, daytime SBP 151 mm Hg) were randomized and 62 completed the study with four valid post-baseline ABPMs. The administration of P, L, E and L/E was associated with a mean 24-h SBP of 144, 137, 133 and 127 mm Hg, respectively. All active treatments significantly reduced the mean 24-h SBP in comparison with placebo, but L/E was significantly more effective than L and E alone. Similarly, office SBP was significantly more reduced with L/E (-16.9 mm Hg) than with L (-5.0 mm Hg) or E (-5.9 mm Hg). A BP <140/90 mm Hg was recorded in 18% of patients with L, 19% with E and 45% with L/E. Two patients on P and two on L/E were withdrawn from the study due to adverse events. In conclusion, combination therapy with L/E has additive antihypertensive effects on both ambulatory and office BP in elderly patients and is well tolerated.
    背景与目标: :这项双盲,安慰剂对照,四向平衡设计交叉研究纳入了60-85岁,平均办公室测量的坐位收缩压(SBP)160-179 mm Hg和白天SBP>或= 135 mm的高血压患者汞经过2周的磨合期(在此期间以前的药物已停止使用),每位患者随机接受以下4种治疗,每组4周:乐卡地平10 mg(L),依那普利20 mg(E),乐卡地平10 mg加依那普利20毫克(L / E)和安慰剂(P)。在每个治疗期结束时,测量办公室低谷血压(BP)并进行24小时动态血压监测(ABPM)。将75名患者(平均年龄66岁,办公室BP 168/92毫米汞柱,白天SBP 151毫米汞柱)随机分组,其中62名患者接受了四个有效的基线后ABPM来完成研究。施用P,L,E和L / E的平均24小时SBP分别为144、137、133和127 mm Hg。与安慰剂相比,所有积极治疗均显着降低了平均24小时SBP,但L / E比单独使用L和E更有效。同样,使用L / E(-16.9 mm Hg)的办公室SBP明显比使用L(-5.0 mm Hg)或E(-5.9 mm Hg)的办公室SBP减少更多。在18%的L患者,19%的E患者和45%的L​​ / E患者中记录到BP <140/90 mm Hg。由于不良事件,两名P病人和L / E病人两名退出研究。总之,L / E联合疗法对老年患者的门诊和办公室BP都有加成的降压作用,并且耐受性良好。

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