氨氯地平与尼群地平治疗高血压的多中心平行对照研究

采用多中心、随机、单盲、组间、平行对照的方法对488例原发性高血压患者进行氨氯地平或尼群地平4周治疗观察，显示氨氯地平的降压有效率为90．4％，较尼群地平显著为高。不良反应较少，安全性好。每日只需服药1次，剂量5～10mg，方便病人。     

氨氯地平与非洛地平缓释剂治疗原发性轻、中度高血压的随机、双盲平行对照研究

目的:对比氨氯地平与非洛地平缓释剂治疗轻中度原发性高血压的疗效和安全性;每日1次服药对24小时动态血压的影响;并对比药物漏服对血压控制的影响。方法:76例轻、中度高血压患者被随机、双盲分成两组,分别每日口服1次氨氯地平5～10mg(Ⅰ组)或非洛地平缓释剂5～10mg(Ⅱ组),治疗12周,并用24小时动态血压监测评价用药前后24小时血压变化情况及漏服48小时的血压变化。结果:氨氯地平治疗组舒张压降低15.1mmHg(治疗末为84.8mmHg),非洛地平缓释剂治疗组舒张压降低15.3mmHg(治疗末为85.0mmHg)。总有效率Ⅰ组病人为83.8％,Ⅱ组为87.9％(P=NS)。在药物的初始剂量下即能达到有效血压控制的病人数Ⅰ组为76％,Ⅱ组为52％(P<0.01)。药物漏服24和48h后,Ⅰ组临床血压仍低于140/90mmHg,24小时动态血压与漏服前相比无显著性差异,而Ⅱ组的临床血压高于140/90mmHg,临床血压和24小时动态血压与漏服前相比具有显著性差异。两治疗组的副作用发生率均较低。结论:氨氯地平与非洛地平缓释剂均能有效降低轻、中度高血压病人的血压,安全、疗效可靠,病人耐受性好,但漏服试验表明漏服24与48h氨氯地平仍能较好的控制血压。Ⅰ组的血压波动明显低于Ⅱ组。     

西拉普利和氨氯地平治疗原发性高血压的临床对照研究

目的探讨西拉普利治疗原发性高血压的临床疗效和安全性。方法采用随机对照的方法,分别用西拉普利和氨氯地平治疗92例原发性高血压患者。观察药物治疗后8周内血压、心率的变化。结果服药8周后西拉普利组总有效率85．4％,收缩压和舒张压分别由治疗前的(20．4±1．8)kPa和(13．7±1．3)kPa降至治疗后的(17．4±1．7)kPa和(11．9±1．1)kPa;氨氯地平组总有效率为88．6％,收缩压和舒张压分别由治疗前的(20．5±1．7)kPa和(13．5±1．6)kPa降至治疗后的(17．3±1．7)kPa和(11．8±1．2)kPa,两组比较无统计学意义。患者用药后无严重的不良反应。结论西拉普利是一种安全和有效的治疗轻中度原发性高血压的药物。     

氨氯地平对巨噬细胞基质金属蛋白酶-2,9 mRNA表达及分泌的影响

目的 :观察氨氯地平对巨噬细胞基质金属蛋白酶 2 ,9(MMP 2 ,MMP 9)的mRNA表达及分泌影响 ,探讨氨氯地平是否具有稳定动脉粥样硬化斑块 ,减少其破裂的功能。方法 :收集小鼠腹腔巨噬细胞与不同浓度的氨氯地平进行培养 ,采用RT PCR方法检测细胞MMP 2 ,MMP 9mRNA的表达 ;用明胶酶谱法检测细胞培养上清液中MMP 2 ,MMP 9的活性 ,在蛋白分泌水平观察氨氯地平对MMP 2 ,MMP 9分泌影响。结果 :5 μg·L- 1浓度的氨氯地平对MMP 2 ,MMP 9的mRNA表达和分泌几乎没有影响 (P >0 .0 5 ) ;15 μg·L- 1浓度可以完全抑制MMP 2 ,MMP 9的mRNA表达 ,对MMP 9分泌有明显的抑制作用 (P <0 .0 5 ) ,对MMP 2的抑制作用较轻 (P >0 .0 5 ) ;浓度为 30 μg·L- 1时 ,完全抑制MMP 2 ,MMP 9的mRNA表达 ,对MMP 2 ,MMP 9分泌的影响由于细胞破裂的影响而不能定论。结论 :中等浓度的氨氯地平可能具有稳定动脉粥样硬化斑块 ,减少其破裂的功能。     

Evaluation of amlodipine, lisinopril, and a combination in the treatment of essential hypertension

Angiotensin converting enzyme (ACE) inhibitors and dihydropyridine calcium antagonists are well established and widely used as monotherapy in patients with mild to moderate essential hypertension. Earlier studies combining short acting drugs from these classes require multiple dosing and were associated with poor compliance. Availability of longer acting compounds allows once daily administration to avoid the inconvenience of a multiple daily dose. It was decided to perform a randomised double blind, crossover study with the long acting calcium channel blocker amlodipine and the long acting ACE inhibitor lisinopril, given either alone or in combination in essential hypertension. Twenty four patients with diastolic blood pressure (DBP) between 95 and 104 mm Hg received amlodipine 2.5 mg and 5 mg, lisinopril 5 mg and 10 mg, and their combination as per a prior randomisation schedule. Supine and standing blood pressure and heart rate were recorded at weekly intervals. Higher doses of both the drugs individually or in combination were used if the target supine DBP below 90 mm Hg was not achieved. There was a significant additional blood pressure lowering effect with the combination when compared either with amlodipine or lisinopril alone. Five mg amlodipine and 10 mg lisinopril monotherapy achieved the target blood pressure in 71% and 72% patients respectively. The combination of 2.5 mg amlodipine with 5 mg lisinopril produced a much more significant lowering of blood pressure in a higher percentage of patients than that with an individual low dose.     

西尼地平片治疗轻中度高血压的有效性和安全性

目的评价西尼地平治疗轻中度原发性高血压的有效性和安全性。方法用随机双盲对照试验设计,入选病人共48例,西尼地平(试验组)24例,氨氯地平(对照组)24例。结果与治疗前相比,治疗8周后试验组收缩压和舒张压分别下降19.26和14.68mmHg(P<0.01),对照组分别下降为18.22和12.91mmHg(P<0.01),均有统计学意义。试验组和对照组药物不良反应的例数分别为0和2例,2组比较无统计学差异(P>0.05),均无严重不良反应发生。结论西尼地平片每日服用1次,降低血压,安全有效。     

氨氯地平复方丹参滴丸对高血压大鼠血管壁重塑的干预

目的：探讨氨氯地平片（络活喜）加复方丹参滴丸对自发性高血压大鼠（SHR）血管壁重塑的干预。方法：将32只10周龄雄性SHR随机分成空白对照组（SHRc）、阴性对照组（SHRNs）、阳性对照组（SHRA）和治疗组（SHRA＋D）四组，每组8只。空白对照组未作治疗即测定各指标，并与8只同周龄Wistar鼠比较。除空白对照组外，后三组分别经生理盐水、络活喜、络活喜加复方丹参滴丸治疗8周后处死，测定各项指标。结果：与wistar组比较，空白对照组及阴性对照组血压明显增高、管腔增大、血管壁明显增厚，尤以血管中层平滑肌细胞（VSMC）肥大为主；经治疗后，阳性对照组及治疗组血压明显降低，血管壁增厚得到遏制；阳性对照组与治疗组之间比较，治疗组血管壁变薄更明显，但无统计学意义。结论：络活喜通过降低血压遏制SHR血管壁重塑，加复方丹参滴丸治疗能进一步遏制血管壁重塑，但可能表现为时效关系。     

健康志愿者口服氨氯地平片的药代动力学和生物等效性研究

目的:研究氨氯地平进口片和国产片在健康志愿者体内的药代动力学及相对生物利用度.方法:单次口服10mg氨氯地平片,用高效液相色谱法测定血药浓度,3p97程序处理数据.结果:两种制剂降压平稳,72 h内均有降压作用.受试制剂和参比制剂的主要药代动力学参数,峰时间(Tmax)分别为(5.22±1.70),(5.89±1.28)h;峰浓度(Cmax)分别为(6.98±1.30),(6.95±1.15)ng/mL;消除半衰期[T1/2(he)]分别为(38.02±7.30),(41.03±11.62)h;药时曲线下面积(AUC0-72)分别为(244.96±55.80),(243.68±46.87)ng·h/mL;氨氯地平国产片的相对生物利用度平均为(100.7±12.5)%.结论:两种制剂生物等效.     

(S)-(—)-氨氯地平苯磺酸盐二水合物的制备

氨氯地平消旋体经D-(—)-酒石酸拆分,得到(S)-(—)-氨氯地平,再与苯磺酸成盐制得钙通道阻滞剂(S)-(—)-氨氯地平苯磺酸盐二水合物,收率67%,光学纯度近100%.     

Efficacy of Initiating Therapy with Amlodipine and Hydrochlorothiazide or Their Combination in Hypertensive Nigerians

In order to evaluate whether amlodipine or hydrochlorothiazide would be preferable to initiate therapy, 90 untreated hypertensive Nigerians of both genders aged 31–86 years with blood pressure >160/90 and ≤180/120 mm Hg were recruited into a randomized 48-week study. Patients, 30 each in amlodipine, hydrochlorothiazide, and amlodipine–hydrochlorothiazide groups, were treated, respectively, with amlodipine 5 mg for 6 weeks and the dose increased to 10 mg till week 12, after which hydrochlorothiazide 25 mg was added; hydrochlorothiazide 25 mg till week 6, after which amlodipine 5–10 mg was added; and amlodipine 5–10 mg + hydrochlorothiazide 25 mg. Body mass index, blood pressure, heart rate, and 24-hour urine volume were evaluated at baseline and at the end of weeks 1, 3, 6, 12, 24, 36, and 48. The primary efficacy variables were decreased in mean trough sitting diastolic and systolic blood pressure such that blood pressure < 140/90 mm Hg was regarded as normalized. At week 48 in the amlodipine group, 27 patients versus 25 patients in the hydrochlorothiazide group had diastolic blood pressure <90 mm Hg (90% vs. 83.3%; P <.03). In the amlodipine group, 23 patients versus 20 patients in the hydrochlorothiazide group had blood pressure < 140/90 mm Hg (76.7% vs. 66.7%; P <.01). In the amlodipine–hydrochlorothiazide group, 27 patients (90%) and 15 patients (50%) had diastolic blood pressure <90 mm Hg and blood pressure < 140/90 mm Hg, respectively. This study has demonstrated that a regimen of amlodipine to which hydrochlorothiazide is subsequently added provides superior efficacy on blood pressure control when compared with a regimen of hydrochlorothiazide to which amlodipine is subsequently added or with ab initio amlodipine–hydrochlorothiazide combination therapy.