钙通道阻滞剂在联合降压中的作用

钙通道阻滞剂(CCB)已经成为最广泛使用的降压药物,并可以很好地与其他各类降压药物联合应用。二氢吡啶类CCB与血管紧张素转换酶(ACE)抑制剂或血管紧张素受体拮抗剂(ARB)的联合在多项大型临床研究中显示出优越性。氨氯地平和拉西地平等第三代CCB半衰期更长、副反应更少、抗动脉粥样硬化等心血管保护作用证据更多,特别适合于老年单纯收缩期高血压、伴冠心病或颈动脉粥样硬化的高血压患者。     

拉西地平治疗原发性高血压的临床观察

应用国产拉西地平对40例外高血压患进行了临床研究。病人口服拉西地平2-6mg·d^-1,1次/日,共服6周。结果：该药降压效果显,显效率为75.19%,总有效率为92.86%。降压幅度：收缩压为15.11%;舒张压为14.18%,与治疗前相比,差异显（P<0.01）。而且对心率及肝肾功能、血糖、血酯、电解质无影响。     

Lacidipine, thiamine pyrophosphate and their combination on the ocular ischemic syndrome induced by bilateral common carotid artery ligation

AIM: To investigate the effect of lacidipine, thiamine pyrophosphate (TPP) and the combination of lacidipine and TPP against oxidative and inflammatory eye damage induced by bilateral common carotid artery ligation in rats. METHODS: Male albino Wistar rats were categorized as those who underwent sham surgery (SG), right and left common carotid cross-clamping and unclamping procedure (CCU), lacidipine+CCU (LCCU), TPP+CCU (TCCU), and combination of lacidipine and TPP (LTC)+CCU (LTCCU). One hour before anesthesia, the LCCU (n=6) received lacidipine (4 mg/kg, orally) and the TCCU (n=6) received TPP (20 mg/kg, intraperitoneally). The SG (n=6) and CCU (n=6) received the same volume of distilled water from the same route. After anesthesia (60 mg/kg ketamine, intraperitoneally), the necks of the rats were opened in the midline. Ischemia was created for 10min by placing clips on the right and left common carotid arteries. Rats in the SG only underwent subcutaneous incision. After 10min, the clips were removed and reperfusion was achieved for six days. Then, the animals were euthanized (120 mg/kg ketamine, intraperitoneally) and the levels of oxidant, antioxidant and proinflammatory cytokines in the eye tissues were determined. The retinal tissue of the eye was also examined histopathologically. RESULTS: Lacidipine, TPP, and LTC significantly prevent the increase in malondialdehyde, tumor necrosis factor-alpha, interleukin-1β (IL-1β), and IL-6 levels, decrease in total glutathione levels, superoxide dismutase and catalase activities and histopathological retinal damage in eye tissue induced by bilateral common carotid artery ligation in rats. The impact of these drugs on protection is determined to be LTC>lacidipine>TPP. CONCLUSION: As a result of the study, it is concluded that LTC may be more effective than lacidipine and TPP alone in treating ocular ischemic syndrome.     

拉西地平合用阿托伐他汀对原发性高血压左室肥厚及舒张功能的影响

目的 评价拉西地平合用阿托伐他汀对原发性原发性高血压左室肥厚及舒张功能的影响.方法 将90例原发性原发性高血压左室肥厚患者随机分为A、B两组,A组给予拉西地平4mg/d;B组给予拉西地平4mg/d+阿托伐他汀10 mg/d.疗程6个月.分别在用药前、用药后6个月应用超声心动图检查评价心肌肥厚和左室舒张功能.结果 两组治疗6个月后左室肥厚的逆转及舒张功能指标(E、A、E/A、IVRT)改善程度与用药前比较差异有统计学意义(P<0.05).两组间比较B组明显优于A组(P<0.01).结论 拉西地平合用阿托伐他汀对原发性高血压左室肥厚逆转及舒张功能改善有协同作用,较单一用药疗效显著.     

拉西地平和卡托普利治疗老年人轻中度原发性高血压的比较

目的比较拉西地平和卡托普利治疗老年人轻中度原发性高血压的疗效和安全性。方法经２周安慰剂导入期，５１例患者参加为期１４周随机服用拉西地平或卡托普利开放性对照试验。结果两种药物均能明显降压（Ｐ＜０．００１），拉西地平具有平稳降压效应，谷峰值比率达７６．９％。不良反应发生率，拉西地组为２６．９％（７／２６），卡托普利组为２８．０％（７／２５），差异无显著性。结论对老年高血压患者拉西地平是一种有效、安全且易耐受的降压药，每天１次（４～６ｍｇ）能维持２４小时降压效应。     

拉西地平合用阿托伐他汀治疗原发性高血压90例疗效观察

目的观察拉西地平合用阿托伐他汀治疗原发性高血压病的疗效和不良反应。方法原发性高血压病90例,随机分为A组（应用拉西地平）和B组（应用拉西地平＋阿托伐他汀）,疗程为6个月。分别在用药前后动态监测血压和不良反应。结果治疗6个月后两组患者血压均显著下降,B组降压更明显,两组降压幅度比较差异有统计学意义（P〈0．05）。降压疗效总有效率A组为77．7％,B组为88．9％,两组比较差异有统计学意义（P〈0．05）。结论拉西地平合用阿托伐他汀有协同降压作用,降压幅度较单用拉西地平高。     

北京降压0号治疗原发性高血压75例临床研究

目的 探讨北京降压0号治疗原发性高血压的降压效果及安全性。方法 将150例在门诊就诊的轻、中度高血压患者随机分为两组,每组75例。北京降压0号治疗组用北京降压0号,1片／d;对照组用长效降压药拉西地平4mg／d。两组服药时间均为晨服。每周随访1次,追踪观察6个月,了解其降压效果及不良反应发生情况;并在治疗前后分别检测血糖、血脂、电解质及肝、肾功能变化。结果 用北京降压0号治疗1周、4周和8周后达到正常血压值（〈140／90mmHg）者分别为52例（69．33％）、64例（85．33％）和70例（94．66％）。用拉西地平片治疗1周、4周和8周后达到正常血压值者分别为56例（74．67％）、62例（82．67％）和69例（92．67％）。两组降压幅度与疗效无明显差异（P〉0．05）。用北京降压0号治疗出现不良反应5例（6．7％）,主要为轻度头晕、鼻塞、乏力,继续治疗可自行缓解。对照组出现不良反应6例（8．0％）,为头痛、面红、心悸和轻度浮肿。结论 应用北京降压0号可显著降低轻、中度高血压患者血压,安全性好,可作为临床推荐使用的高血压一线药物。     

Potassium Magnesium Supplementation for Four Weeks Improves Small Distal Artery Compliance and Reduces Blood Pressure in Patients with Essential Hypertension

It has been postulated that the loss of arterial compliance may precede cardiovascular diseases, and that arterial compliance is an important parameter to consider when evaluating arterial diseases such as essential hypertension (EH) and the effects of antihypertensive treatment. In all, 133 EH patients and 147 healthy subjects were enrolled in this study. Large arterial compliance (C1) and small arterial compliance (C2) were measured by the CVProfilor? DO-2020 CardioVascular Profiling System. Thirty-five patients randomly received magnesium potassium supplementation (magnesium, 70.8 mg/d; potassium, 217.2 mg/d) for four weeks, and 32 patients received lacidipin (4mg/d) as a control. Before and after the four weeks, blood pressure, C1, and C2 were measured. It was found that arterial compliance was significantly lower in EH patients compared with healthy subjects (C1: 12.53 ± 0.33 vs. 15.63 ± 0.30 ml/mmHg × 10, p < 0.01;C2: 3.79 ± 0.17 vs. 5.69 ± 0.25 ml/mmHg × 100,p < 0.01). On lacidipine, systolic and diastolic BP decreased 13.27 ± 1.76 mm Hg and 6.33 ± 1.55 mm Hg, and C1 and C2 compliance values increased 25.05% ± 4.49% and 34.50% ± 7.40%, respectively. On K⁺ and Mg²⁺ supplementation, systolic and diastolic BP decreased 7.83 ± 1.87 mm Hg and 3.67 ± 1.03 mm Hg, and C1 and C2 compliance values increased 12.44% ± 4.43% and 45.25% ± 6.67%, respectively. Decreases in systemic vascular resistance (mean arterial pressure divided by cardiac output) by 11.9% and 16.6 % (p < 0.01) were seen between the drug-induced changes, respectively. Both large arterial compliance and small arterial compliance were decreased in essential hypertension patients. In essential hypertension patients, magnesium and potassium supplementation could improve small arterial compliance, while lacidipine improved large arterial compliance significantly.     

拉西地平对原发性高血压患者血粘度和血小板聚集的影响

目的:研究原发性高血压(essential hypertension,EH)患者血粘度和血小板聚集情况及拉西地平对其影响。方法:采用前瞻性自身对照研究近年门诊EH和正常血压各40例,EH患者服用拉西地平6周,分别检测治疗前后全血粘度(WBV)、血浆粘度(PV)、血小板一分钟聚集率(PAG1)、血小板五分钟聚集率(PAG5)、血小板最大聚集率(PAGm),并与正常血压组对照分析。结果:高血压组WBV、PV、PAG1、PAG5和PAGm均明显高于血压正常组(P0.05)。结论:EH患者的血粘度和血小板聚集性增高,拉西地平能降低EH患者的WBV、PAG,从而降低EH患者并发血栓病的潜力。     

The effects of lacidipine on the steady/state plasma concentrations of simvastatin in healthy subjects

AIMS: Lacidipine, a long acting 2, 4-dihydropyridine calcium channel antagonist is frequently administered with cholesterol lowering agents, particularly in elderly populations. The effects of lacidipine on the pharmacokinetics of simvastatin were investigated, since they share the CYP3A4 pathway for metabolism. METHODS: The study was an open, randomised, two-way crossover design, with at least 7 days washout. Eighteen healthy subjects received simvastatin, 40 mg once daily, alone and together with lacidipine, 4 mg once daily, for 8 days. The pharmacokinetics of simvastatin were studied on the eighth day. Analysis was made of total simvastatin acid concentrations (naive simvastatin acid plus that derived from alkaline hydrolysis of the lactone). RESULTS: Lacidipine increased the maximum concentration of simvastatin (Cmax) by approximately 70% (P=0.016) and the area under the plasma concentration-time curve AUC(0,24 h) by approximately 35% (P=0.001). The mean Cmax and AUC(0,24 h) of simvastatin (95% confidence interval) when given alone were 8.76 (6.72-11.41) ng ml(-1) and 60.36 (47.15-77.28) ng ml(-1) h. During treatment with lacidipine they were, respectively, 14.89 (10.77-20.58) ng ml(-1) and 80.96 (64.62-101.44) ng ml(-1) h. No significant differences were observed in either time to peak concentration (tmax was 1.0 h for simvastatin alone and 1.5 h for the combination) or in the half-life (t1/2,z was 8.5 h in both cases). The combination was safe and well tolerated. CONCLUSIONS: The observed increased exposure to simvastatin 40 mg following coadministration of lacidipine is unlikely to be of clinical relevance.