雷米普利通过调节细胞外调节激酶1/2的活性抑制肺动脉高压大鼠肺血管重构

目的探讨雷米普利抑制野百合碱（MCT）诱导的肺动脉高压（PAH）大鼠肺血管重构是否与调节细胞外调节激酶1/2（ERK1/2）活性有关。方法雄性Sprague-Dawley大鼠30只,质量280～320g,随机分为：正常对照组、PAH组、PAH＋雷米普利组。PAH组和PAH＋雷米普利组一次性颈部注射MCT60mg/kg后,PAH＋雷米普利组用雷米普利灌胃,PAH组用生理盐水灌胃。对照组颈部注射生理盐水后,用生理盐水灌胃。4周后,测定大鼠的右室收缩压（RVSP）和右心室肥厚指数（RVHI）,并用图像分析软件,测定肺小动脉管壁厚度（WT）占动脉外径（ED）的百分比（WT,%）及管壁面积（WA）占血管总面积的百分比（WA,%）。放射免疫法检测肺组织中血管紧张素Ⅱ（AngⅡ）浓度。Western免疫印迹分析肺组织中ERK1/2磷酸化水平。结果PAH组的RVSP、RVHI、WT（%）、WA（%）、肺组织AngⅡ浓度和ERK1/2磷酸化水平均显著高于正常对照组;雷米普利组RVSP、RVHI、WT（%）、WA（%）、肺组织AngⅡ浓度和ERK1/2磷酸化水平均明显低于PAH组。结论雷米普利抑制MCT诱导的肺血管重构的机制可能与降低肺组织ERK1/2磷酸化水平有关。     

Ramipril/amlodipine single pill – Effectiveness,tolerance and patient satisfaction with antihypertensive therapy in relation to nutritional status

BackgroundOverweight and obesity decrease the effectiveness of antihypertensive therapy despite the more frequent use of polytherapy. One method for improving therapy effectiveness is by decreasing non-compliance with the use of fixed-dose combinations (FDC).The aim of this study was to assess the effectiveness, tolerance, and satisfaction with ramipril/amlodipine FDC antihypertensive therapy in relation to nutritional status.MethodsThe survey enrolled 24,240 hypertensive patients recently switched to ramipril/amlodipine FDC (EGIRAMLON) at the same doses as previously prescribed separate pills.ResultsThe effectiveness of antihypertensive therapy increased during follow-up from 32.9% to 76.5%. Overweight and obesity were associated with the increased risk of not attaining the recommended BP values [adjusted for age OR = 0.74 (95% CI 0.67–0.83) and 0.70 (0.61–0.81) for overweight; 0.54 (0.47–0.60) and 0.49 (0.42–0.57) for obese, at the first and the second examination, respectively].“Very good” or “good” the FDP tolerance was reported by 98.8%, 97.6% and 96.4%, respectively.Adverse events (AE) were reported in 0.35% of patients regardless of nutritional status.High levels of satisfaction with the FDC were reported by 57.0% of patients with normal weight, 54.5% of overweight, and 50.6% with obesity. Effectiveness and convenience were the most important for patients.ConclusionsThe effectiveness of therapy with ramipril/amlodipine FDC in the study population was high, but slightly lower in overweigh and obese. This FDC was well tolerated and a significant number of patients satisfied with the therapy regardless of nutritional status. Although the perceived tolerance and satisfaction with treatment were lower in obese and overweight than in normal weight patients; the incidence of AE and perceived benefit from the use of a single-pill, compared to multiple tablets, were comparable irrespective of nutritional status.     

贝尼地平与雷米普利治疗原发性高血压的临床对比研究

目的观察贝尼地平和雷米普利治疗轻、中度原发性高血压疗效和不良反应。方法100例高血压患者随机分为两组,贝尼地平组(n=50)及雷米普利组(n=50),观察4周,每周测坐位血压1次,并观察不良反应。结果贝尼地平组和雷米普利组均能有效降低血压,其不良反应发生率贝尼地平明显低于雷米普利。结论贝尼地平和雷米普利相比较治疗高血压有相同的疗效,且不良反应更轻微,是较理想的抗高血压新药。     

雷米普利降低高血压患者心房颤动发生率以及改善左心房内径临床观察

目的观察血管紧张素转换酶抑制剂(ACEI)雷米普利降低高血压患者心房颤动(AF)发生率及对左心房内径的影响。方法将180例原发性高血压患者分为治疗组(90例)和对照组(90例)。治疗组给予雷米普利(2.5～15)mg/d口服,连服50个月。对照组苯磺碳氨氯地平(2.5～10)mg/d口服,连服50个月。结果治疗50个月后治疗组AF发生率3.4%,对照组AF发生率为8.05%;治疗组左心房内径缩小(2.0±1.5)mm,对照组左心房内径缩小(0.0±1.6)mm。2组相比P<0.05,有统计学意义。结论雷米普利可降低高血压患者AF的发生率并缩小左心房内径。     

雷米普利治疗原发性高血压临床疗效

目的：观察雷米普利治疗原发性高血压的临床疗效。方法：选取50例原发性高血压病人，经过1周药物冲洗期后给予雷米普利2．5－10mg/d常规治疗，疗程为8周。结果：治疗8周后收缩压下降24mmHg，舒张压下降25mmHg。与用药前差异有显著意义，无严重不良反应。结论：雷米普利治疗原发性高血压具有疗效好、安全性高及病人的耐受性高的优点。     

雷米普利对老年高血压病患者胰岛素抵抗的影响

目的 探讨雷米普利对老年高血压病患者胰岛素抵抗的的影响。方法 将128例老年高血压痛患者随机分为雷米普利组64例，硝苯地平组64例，雷米普利组口服雷米普利（商品名瑞泰）2．5～10mg每日1次，硝苯地平片10～20mg每日3次，8周为一疗程。观察治疗前后空腹血糖、餐后2h血糖、空腹胰岛素、餐后2小时胰岛素及胰岛素敏感性指数的变化。结果 两组患者治疗前后空腹血糖性差异无统计学意义（P〉0．05），雷米普利组治疗后餐后2h血糖、空腹胰岛素、餐后2小时胰岛素和胰岛素敏感性指数较治疗前差异有统计学意义（P〈0．05）。硝苯地平组治疗前后各项指标差异无统计学意义（P〉0．05）。结论 雷米普利能显著降低老年高血压病患者餐后2h血糖、提高血胰岛素敏感性指标，从而改善胰岛素抵抗。     

Square wave voltammetric determination of the angiotensin-converting enzyme inhibitors cilazapril,quinapril and ramipril in pharmaceutical formulations

The angiotensin-converting enzyme inhibitors cilazapril, quinapril and ramipril are reduced at a hanging mercury drop electrode in the pH range 3.5-13 using Britton-Robinson buffers as supporting electrolyte and KCl as ionic medium. Square wave voltammetry has proved to be the most suitable electroanalytical technique for the quantitative voltammetric determination of these antihypertensive drugs. Optimisation of the chemical and instrumental variables was carried out. Analyses were performed in 0.02 M borate buffer at pH 9.5 and 0.5 M KCl as ionic medium, using a pulse amplitude of 50 mV and a frequency of 150 Hz. A linear relationship between peak current and concentration was found in the interval 0.5-8 microg/ml for cilazapril and up to 6 microg/ml for quinapril and ramipril, allowing the direct determination of their pharmaceutical formulations alone or mixed with hydrochlorothiazide. Good accuracy and repeatativity were obtained.     

雷米普利对慢性心力衰竭患者脑钠肽水平及心功能的影响

目的研究慢性心力衰竭（CHF）患者心力衰竭严重程度与其血浆脑钠肽（BNP）浓度的关系，探讨不同剂量雷米普利对CHF患者BNP的影响和较大剂量雷米普利的可行性与安全性。方法将53例CHF患者在接受基础治疗基础上随机分为小剂量组（雷米普利2．5～5mg／d），大剂量组（雷米普利10mg／d），治疗10周，观察治疗前后两组患者BNP浓度变化及各组间差异。结果CHF患者血浆中BNP浓度随着纽约心脏病协会心功能分级（NYHA）分级增加而升高，大剂量组比小剂量组能更明显降低血浆中BNP浓度。大剂量组患者采用小剂量逐渐递增剂量方式给药．耐受性良好。结论CHF时心力衰竭严重程度与血浆BNP浓度密切相关，血浆BNP浓度是评估CHF诊断、治疗和预后的良好的指标。在CHF患者中采用小剂量逐渐递增剂量的方式给予雷米普利安全可行．患者耐量性良好。     

超声评价血管紧张素转换酶抑制剂及血管紧张素受体拮抗剂对高血压左室肥厚患者冠状动脉血流动力学的影响

目的应用超声技术评价血管紧张素转换酶抑制剂雷米普利和血管紧张素受体拮抗剂氯沙坦及联合用药对高血压左室肥厚患者冠状动脉血流动力学的影响.方法将60例高血压合并左室肥厚的患者随机分入雷米普利、氯沙坦单用和二者联合用药组,治疗6个月后复查,采用多平面经食管超声心动图和动态三维超声心动图评价用药前后左室质量(LVM)和冠状动脉血流动力学的变化.结果最终共50例患者完成了全部检查.治疗6个月后,雷米普利组、氯沙坦组及联合用药组收缩压、舒张压均显著下降,LVM明显减轻(P均《0.01);雷米普利组、氯沙坦组和联合用药组均见冠状动脉前降支近端经LVM校正的舒张期血流流速积分(DVic)较用药前显著增高,收缩期血流流速积分(SVic)降低(P均《0.01);静脉注射双嘧达莫后,经LVM校正后的SVic、DVic在雷米普利组、氯沙坦组和联合用药组均见治疗后较治疗前显著增高(P《0.05～0.01);氯沙坦组和联合用药组冠状动脉血流储备(CFR)指标显著增加(P《0.05),经LVM校正后的上述指标增加程度更为显著(P《0.05～0.01),且联合用药组CFR高于雷米普利组(P《0.05),雷米普利组仅见经LVM校正后的CFR指标较治疗前显著增加(P《0.05).结论雷米普利和氯沙坦联合用药与单一用药在降压、消退LVH方面同样有效,在改善CFR方面联合用药优于雷米普利单用.     

雷米普利对急性心肌梗死患者的长期抗缺血作用

目的　探讨血管紧张素转换酶抑制剂雷米普利减少心肌梗死后患者心肌缺血及缺血事件的作用。方法　对 4 0例雷米普利组 (治疗组 )和 38例一般治疗组 (对照组 )于出院前 ,出院后 0 .5、1.0年行 2 4小时动态心电图心肌缺血总负荷检测 (TIB) ,并观察缺血相关事件。结果　治疗组TIB在出院后 6个月低于对照组 ,但无统计学差异 (P >0 .0 5 )。出院后 1年 ,治疗组TIB显著低于对照组 (P <0 .0 5 ) ,并且治疗组缺血相关事件亦明显少于对照组 (P <0 .0 5 )。结论　雷米普利对心肌梗死后患者具有长期的抗心肌缺血和减少缺血事件的作用。