非洛地平缓释片对轻中度原发性高血压患者的降压疗效和对脉搏波速度的影响，

目的：探讨非洛地平缓释片对轻中度原发性高血压患者的降压疗效和对脉搏波速度的影响。方法：根据纳入标准选取我院260例原发性高血压患者,按计划方案给予非洛地平缓释片口服治疗。观察患者入院后、治疗2周末、14周末降压疗效及脉搏波传导速度的改变情况,并进行对比分析。结果：本组研究中接受治疗研究者共260例,其所有受检者在治疗2、6、10、14周后血压水平均有不同程度改善,与基线比较差异明显,有统计学意义（P〈0,01）。脉搏波变化分析所有受试者脉搏波速度变化分析,基线脉搏波速度为（10．9±2．4）m／s,经过治疗后2周、14周基线脉搏波速度为（10．3±2．1）m／s,差异明显具有统计学意义（P〈0．01）;心率变化分析表明非洛地平缓释片在降压同时对心率影响不大,安全性评价表示,接受治疗期间曾有68例发生不良事件,占总数26．2％。笔者认为与药物无关,且均为轻度,经过适当处理后均缓解,对本研究无影响。结论：非洛地平缓释片降压效果良好,可同时降低颈动脉．股动脉脉搏波传导速度,改善大动脉僵硬度。     

The effect of felodipine on the uptake and degradation of acetylated LDL in mouse peritoneal cells and on the distribution of acetylated LDL in macrophage-rich organs of the rat

The effect of felodipine on lipoprotein metabolism ex vivo and in vivo was investigated. In the ex vivo studies mice were given felodipine (40–125 μ mol/kg body weight) or vehicle for one week. Peritoneal macrophages from these animals and controls were isolated and used in binding and degradation studies with human iodinated acetylated LDL (Ac-LDL). Macrophages from felodipine-treated mice showed a significant decrease of binding and degradation of Ac-LDL compared to macrophages from control animals (P<0.05). The in vivo studies were performed in rats pretreated with felodipine or vehicle. To determine the distribution and plasma turnover of LDL and Ac-LDL, ¹²⁵I-tyramine cellobiose labelled LDL or Ac-LDL were given i.v. No differences in the removal rate of Ac-LDL or LDL were observed between felodipine-treated or untreated rats. However, an increased uptake of Ac-LDL could be seen in the liver of the felodipine-treated rats. This increased uptake could be ascribed to the parenchymal cells because no differences in uptake could be seen in the liver endothelial cells. However, a significant decreased uptake was seen in the Kuppfer cells and in the spleen, a macrophage-rich organ, of the felodipine-treated rats. The present study suggests a possible mechanism behind the antiatherogenic effects of calcium antagonists, a decreased uptake of atherogenic modified lipoproteins by peripheral macrophages and an increased uptake by the liver.     

Allosteric interactions among drug binding sites on calmodulin

Felodipine is a fluorescent dihydropyridine Ca²⁺-antagonist. It binds to calmodulin in a Ca²⁺-dependent manner, and undergoes a fluorescence increase which allows us to monitor its interaction with calmodulin. Hydrophobic ligands including the calmodulin antagonist, R24571 and Ca²⁺ antagonists, prenylamine and diltiazem, bind to calmodulin and potentiate felodipine binding by as much as 20 fold. These studies suggest that allosteric interactions occur among different drug binding sites on calmodulin. Our results are discussed in terms of the mechanism of action of calmodulin.     

苯扎贝特片联合非洛地平缓释片对高血压合并血脂代谢紊乱患者血脂水平、内皮细胞功能及炎性细胞因子的影响

摘要 目的：探讨苯扎贝特片联合非洛地平缓释片对高血压合并血脂代谢紊乱患者血脂水平、内皮细胞功能及炎性细胞因子的影响。方法：选择2018年1月到2020年1月我院收治的105例高血压合并血脂代谢紊乱患者,按随机表字法随机分为观察组（53例）和对照组（52例）。两组均予以调脂饮食,随后对照组给予非洛地平缓释片治疗,观察组给予苯扎贝特片联合非洛地平缓释片治疗。比较两组收缩压（SBP）、舒张压（DBP）、空腹血糖（GLU）、空腹胰岛素（FINS）、胰岛素抵抗指数（HOMA-IR）、总胆固醇（TC）、甘油三酯（TG）、高密度脂蛋白（HDL-C）、低密度脂蛋白（LDL-C）、白细胞介素-6（IL-6）、超敏C-反应蛋白（hs-CRP）、一氧化氮（NO）、内皮素（ET）、肿瘤坏死因子α（TNF-α）水平。结果：两组治疗后SBP、DBP、GLU、FINS、血清TG、TC、LDL-C、ET、TNF-α、IL-6、hs-CRP水平及HOMA-IR均明显低于治疗前（P<0.05）,血清HDL-C、NO水平均高于治疗前（P<0.05）,同时观察组治疗后SBP、DBP、GLU、FINS、血清TG、TC、LDL-C、ET、TNF-α、IL-6、hs-CRP水平及HOMA-IR低于对照组（P<0.05）,血清HDL-C、NO水平均高于对照组（P<0.05）。结论：苯扎贝特片联合非洛地平缓释片能够更好地调节高血压合并血脂代谢紊乱患者的血压、血脂水平,改善血管内皮功能和胰岛素抵抗,降低血清炎症因子水平。     

非洛地平缓释片对轻中度原发性高血压患者的降压疗效和对脉搏波 速度的影响

目的:探讨非洛地平缓释片对轻中度原发性高血压患者的降压疗效和对脉搏波速度的影响。方法:根据纳入标准选取我院260例原发性高血压患者,按计划方案给予非洛地平缓释片口服治疗。观察患者入院后、治疗2周末、14周末降压疗效及脉搏波传导速度的改变情况,并进行对比分析。结果:本组研究中接受治疗研究者共260例,其所有受检者在治疗2、6、10、14周后血压水平均有不同程度改善,与基线比较差异明显,有统计学意义(P<0.01)。脉搏波变化分析所有受试者脉搏波速度变化分析,基线脉搏波速度为(10.9±2.4)m/s,经过治疗后2周、14周基线脉搏波速度为(10.3±2.1)m/s,差异明显具有统计学意义(P<0.01);心率变化分析表明非洛地平缓释片在降压同时对心率影响不大,安全性评价表示,接受治疗期间曾有68例发生不良事件,占总数26.2%。笔者认为与药物无关,且均为轻度,经过适当处理后均缓解,对本研究无影响。结论:非洛地平缓释片降压效果良好,可同时降低颈动脉-股动脉脉搏波传导速度,改善大动脉僵硬度。