尼莫地平联合卡维地洛治疗原发性高血压78例临床分析

目的分析尼莫地平联合卡维地洛治疗原发性高血压的临床疗效。方法将150例原发性高血压随机分成两组,对照组给予尼莫地平治疗,治疗组在对照组治疗的基础上,加之卡维地洛。结果治疗组与对照组显效率分别为33.3%和26.4%,总有效率为88.5%和76.4%,两组相比具有显著性差异（P〈0.05）。结论尼莫地平联合卡维地洛治疗原发性高血压疗效更为显著。     

Lack of Major Effects on Mouse Brain Adenosine A1 Receptors of Oral Carbamazepine and Calcium Antagonists

Interaction with adenosine A1 receptors is a possible contributory mechanism to the anticonvulsant effects of carbamazepine (CBZ) and the dihydropyridine calcium antagonists. We measured the binding of [3H]cyclohexyladenosine to adenosine A1 receptors in mouse brain stem, cerebellum, and cortex after oral administration of nifedipine, nimodipine (NMD), and CBZ for 7 days and compared the results with binding in control mice. Equilibrium dissociation constant (Kd) and receptor numbers (Bmax) were calculated using Scatchard and saturation isotherm analyses. Mean Kds (SEM) in control brain stem, cerebellum, and cortex were 2.09 (0.31), 2.39 (0.2), and 3.12 (0.28) nM, respectively. Results of Bmax for the same areas were 188 (26), 280 (24), and 449 (54) fmol/mg protein. Nifedipine (p less than 0.005) and NMD (p less than 0.02) raised the Kd of A1 receptors only in the cerebellum, and CBZ increased cerebellar Bmax (p less than 0.05). These minor effects on A1 receptors in CF1 mice, when given in doses previously shown to have anticonvulsant properties in these animals, do not suggest that alteration in A1 receptor activity is an important mechanism for the anticonvulsant effects of these drugs.     

尼莫地平的合成工艺改进

尼莫地平的合成工艺改进①吴苏敏宋明华峰华维一１（中国药科大学制药有限公司，１药物化学研究室，南京２１０００９）关键词尼莫地平；二氢吡啶合成尼莫地平（１），化学名为（±）１，４二氢２，６二甲基４（３硝基苯基）吡啶３，５二羧酸异丙酯２?..     

急性脑梗死后血浆NO、NOS、ET含量的动态变化及尼莫地平对其影响

目的　观察急性脑梗死 (ACI)后血浆一氧化氮 (NO)、一氧化氮合成酶 (NOS)、内皮素 (ET)含量的动态变化 ,以及尼莫地平治疗后对其影响。方法　ACI患者 110例 ,随机分成尼莫地平组 (5 0例 ) (在常规治疗基础上用尼莫地平 )和常规治疗组 (6 0例 )。在发病后不同时点动态观察血浆NO、NOS、ET含量 ,并设 5 0例脑动脉硬化患者为对照组。结果　脑梗死后血浆ET含量显著升高 ,直至恢复期 ;NO、NOS先增高后下降 ;尼莫地平组和常规组比较ET有显著差异 (P <0 .0 1) ,NO、NOS差别不显著 (P >0 .0 5 )。结论　NO、NOS、ET参与并影响了ACI后复杂的病理生理过程 ;尼莫地平部分通过对ET含量的影响发挥其对脑梗死的治疗作用     

尼莫地平复方丹参注射液治疗新生儿缺氧缺血性脑病疗效观察

目的观察尼莫地平联合复方丹参注射液治疗新生儿缺氧缺血性脑病(HIE)的疗效.方法 128例HIE患儿随机分为复方丹参注射液组32例,尼莫地平组,尼莫地平加复方丹参注射液,与对照组.结果复方丹参注射液组、尼莫地平组、尼莫地平加复方丹参注射液治疗组总有效率分别为81.3%(26/32)、80.0%(24/30)、97.1%(34/35),对照组总有效率为51.6%(16/31),P＜0.05.结论尼莫地平与复方丹参注射液在治疗HIE时有协同作用,疗效显著,未见副作用发生.     

Pretreatment with aldosterone or corticosterone blocks the memory-enhancing effects of nimodipine,captopril, CGP 37 849, and strychnine in mice

Oral pretreatment with aldosterone or corticosterone blocked the memory-enhancing effects of the calcium antagonist nimodipine, the ACE inhibitor captopril, the NMDA blocker CGP 37 849, and the glycine antagonist strychnine in a passive-avoidance test in mice. The memory-disturbing effects of phenobarbitone, diazepam, CGP 37 849 and scopolamine were not influenced by the hormonal pretreatment. These findings could indicate the involvement of a steroid-sensitive mechanism in drug-induced improvement of memory. In the light of clinical observations showing elevated cortisol levels in Alzheimer patients, the results might also explain why only a limited number of these patients respond to therapy with memory enhancers.     

尼莫地平控制性降压对犬血流动力学的影响

在健康杂种犬10只中,分别以15、30、45μg/kg 尼莫地平静注行控制性降压,监测平均动脉压和其它血流动力学指标。结果表明,15μg/kg、30μg/kg 和 45μg/kg 静注后,平均动脉压1min 时分别下降19.44％、29.93％和33.60％,45min 恢复对照水平。降压期间除心输出量指数、每搏量指数和总外周阻力指数外,其它各项指标无显著性改变。因此,我们认为尼莫地平可试用于临床控制性降压,其效果有待临床进一步观察。     

HPLC法测定通脉舒胶囊中尼莫地平的含量

目的建立检测制剂中尼莫地平的专属性方法。方法采用液相色谱法。选用ODSC18柱,以0.01mol/L醋酸铵（用冰醋酸调节pH值为3.5）-乙腈（30：70）为流动相,流速1.0ml/min,检测波长237nm。结果尼莫地平在进样量为0.08～0.8μg范围内线性良好（r=0.9994）,回收率为99.0%（n=6）。结论该方法选择性强,灵敏度高,可作为分析制剂中的尼莫地平。     

尼莫地平联合亚低温疗法治疗SAH后脑血管痉挛的疗效观察

目的探讨尼莫地平联合亚低温疗法治疗蛛网膜下腔出血(SAH)后脑血管痉挛的疗效。方法 93例SAH后脑血管痉挛患者随机分为两组。在常规治疗基础上,对照组采用亚低温疗法治疗,观察组采用尼莫地平联合亚低温疗法治疗。比较两组的治疗效果。结果观察组的总有效率为95.74%,高于对照组的80.43%(P <0.05)。治疗后,观察组的IL-6、 TNF-α、 hs-CRP水平均低于对照组,动脉平均血流速度高于对照组(P <0.05)。结论尼莫地平联合亚低温疗法治疗SAH后脑血管痉挛的效果显著,可有效抑制机体炎性反应,提升动脉平均血流速度。     

尼莫地平固体分散片溶出度比较

以进口尼莫地平薄膜包衣片为参考 ,比较国内两厂家的尼莫地平固体分散片溶出度。以乙醇∶水 (15∶85 )为溶出介质 ,在 (37± 0 5 )℃下 ,浆法 ,进行溶出实验 ,采用紫外分光光度法测定并计算结果。各厂家尼莫地平片 30min内溶出度不低于 70 %。经t检验 ,3种样品组间 4 5min溶出度无显著性差异 (P >0 0 5 )。