硝苯地平缓释片单用及与双氢克尿噻小剂量联用治疗高血压疗效分析

目的：比较硝苯地平缓释片（NF）单用及与双氢克尿噻（DHCT）小剂量联用的降压疗效。方法：将轻、中度原发性高血压患者140例．随机分为治疗组（A组）71例和对照组（B组）69例。A组：口服NF、DHCT（小剂量）；B组：单服NF，疗程均为4周。结果：A组总有效率为93．00%，B组总有效率为86．96%，两组比较有显著性差异（P〈0.05）。结论：NF与DHCT小剂量联用治疗轻、中度高血压痛．疗效优于单用NF。     

硝苯地平制剂的溶出度测定方法

目的测定硝苯地平制剂的溶出度。方法在溶出介质中加入非离子表面活性剂吐温-80,使硝苯地平的溶解度增加至86μg·ml-1。结果及结论此方法完全符合溶出度测定的漏槽条件。     

硝苯地平推拉式渗透泵片体外释放影响因素的研究

目的：本实验的目的是以难溶性药物硝苯地平为模型药物来研究推拉式渗透泵片剂中药物层和推动层的配方中聚合物聚氧乙烯的用量、氯化钠的用量、控释层包衣增重以及药物层和推动层的比例对药物释放的影响。方法：采用推拉式渗透泵设计,分别考察聚氧乙烯-N80在药物层中的不同用量、聚氧乙烯Coagulant在推动层中的不同用量以及氯化钠在推动层中不同用量的7个配方,7个配方片芯同时采用欧巴代CA包衣进行半透膜控释包衣,因片重大小不同,无法同时得到相同的包衣增重,所以结合实际包衣增重的数据,采用统计分析软件对包衣片在不同时间的药物释放数据进行建模分析。结果：统计结果表明欧巴代CA的包衣增重对药物释放有显著影响（P〈0.05）,随着包衣增重的增加,药物的释放变慢。聚氧乙烯N-80在药物层中的用量对药物释放也有显著影响（P〈0.05）,随着聚氧乙烯N-80在药物层中用量的增加,药物的释放变慢。而聚氧乙烯Coagulant和氯化钠在推动层的用量变化,在配方考察的比例范围内对药物的释放的影响不显著。对20小时的药物释放分析结果表明,药物层与推动层的比例对药物的后期释放有显著影响（P〈0.05）。药物层与推动层的比例越高,药物后期释放得越慢。     

Effect of nifedipine and mefruside on renal function and platelet function in hypertensive patients

Summary

A study was carried out in 16 patients with moderately severe hypertension to investigate the effects of nifedipine, given alone or combined with a diuretic, on blood pressure and on renal and platelet function. After 4 weeks on placebo, patients were randomized to receive treatment for 6 weeks with either 20?mg nifedipine twice daily or 25?mg mefruside once daily on a double-blind, double-dummy basis. All patients then received treatment for a further 6 weeks with a combination of the two drugs in the same dosage as before. The results of blood pressure measurements and laboratory investigations during the three phases of the study showed that significantly better blood pressure control was achieved with nifedipine alone than with mefruside alone. Mefruside had an additional hypotensive effect when added to nifedipine. There was no significant change in the renal blood flow or glomerular filtration rate, with a satisfactory control of blood pressure. There was also no detectable change in platelet aggregation with increasing concentrations of ADP and ristocetin. An adaptive mechanism could be responsible for the apparent lack of change compared with single dose studies.     

硝苯地平与硫酸镁联用治疗妊娠期高血压疾病的分析

目的：探讨硝苯地平联合硫酸镁用于妊娠期高血压疾病治疗的临床效果。方法将我院收治的妊娠期高血压疾病患者96例随机分成观察组48例（硝苯地平联合硫酸镁治疗）和对照组48例（硫酸镁治疗），对比2组的治疗效果。结果2组治疗有效率相比差异具有显著性（P<0.05）。结论硫酸镁和硝苯地平联合治疗能够在改善患者心肌血氧的同时保护心肌功能，避免并发症的出现，减少高血压发病率，保障孕妇和婴儿的生命健康。     

服用硝苯地平后牙龈增生以及未增生患者牙龈成纤维细胞生物特性比较

目的：观察服用硝苯地平后牙龈增生和未增生患者牙龈成纤维细胞（nifedipine responders gingival fibro-blasts NIFr-HGF,nifedipine non-responders gingival fibroblasts NIFn-HGF）超微结构、细胞周期变化以及增殖能力的差异性,以探讨该药导致牙龈增生的可能作用机理。方法：采用透射电镜观察NIFr-HGF、NIFn-HGF的超微结构,利用流式细胞仪、MTT法检测和比较2种细胞经硝苯地平诱导后其细胞周期以及增殖能力的差异性。结果：与NIFn-HGF相比较,NIFr-HGF内粗面内质网扩张;受硝苯地平诱导后其增殖明显加强。结论：NIFr-HGF合成蛋白质的能力可能较NIFn-HGF强,且前者对于硝苯地平的反应也明显强于后者,这提示两类细胞的细胞生物学特性以及对钙离子拮抗剂的反应能力存在差异,药物性牙龈增生的发生可能存在细胞异质性。     

Angiotensin - Forming Enzyme Active at the Physiological PH in the Brain of Normal and Nephrectomized Rats

Enzymatic activity generating angiotensin at pH 5.5 and 7.2 has been detected in different areas of the central nervous system (CNS) of the rat. Control animals and those subjected to bilateral nephrectomy 48 h before the experiment (Nx) were analyzed. The different areas of the CNS were studied by the incubation of tissue homogenates in the presence (enzyme concentration) or not (enzyme activity) of an excess of added angiotensinogen. Concentration was determined by incubation at pH 7.2 and 5.5 while activity was evaluated only at pH 7.2. The enzymatic renin-like concentration at both pHs did not change after Nx thus showing they do not depend on plasma and vascular renin. On the other hand the activity of the enzyme showed a significant increase in the cerebral cortex and cerebellum after Nx suggesting an increased concentrations of renin substrate and/or different concentrations of inhibitors or activators of the enzymatic system in those areas.     

A Combination of Nifedipine and OctreotideTreatment in an HyperinsulinemicHypoglycemic Infant

Hyperinsulinemic hypoglycemia (HH) is the commonest cause of persistent hypoglycemia in the neonatal and infancy periods. Mutations in the ABCC8 and KCNJ11 genes, which encode subunits of the ATP-sensitive potassium channel in the pancreatic beta cell, are identified in approximately 50% of these patients. The first-line drug in the treatment of HH is diazoxide. Octreotide and glucagon can be used in patients who show no response to diazoxide. Nifedipine, a calcium-channel blocker, has been shown to be an effective treatment in a small number of patients with diazoxide-unresponsive HH. We report a HH patient with a homozygous ABCC8 mutation (p.W1339X) who underwent a near-total pancreatectomy at 2 months of age due to a lack of response to diazoxide and octreotide treatment. Severe hypoglycemic attacks continued following surgery, while the patient was being treated with octreotide. These attacks resolved when nifedipine was introduced. Whilst our patient responded well to nifedipine, the dosage could not be increased to 0.75 mg/kg/day due to development of hypotension, a reported side effect of this drug. Currently, our patient, now aged 4 years, is receiving a combination of nifedipine and octreotide treatment. He is under good control and shows no side effects. In conclusion, nifedipine treatment can be started in patients with HH who show a poor response to diazoxide and octreotide treatment.     

Nifedipine in Hypertensive Crises of Infants and Children

Nifedipine given by the sublingual route has been used in the treatment of 30 hypertensive emergencies in 20 children suffering from renal disease. The mean dosage of nifedipine was 0.33 mg/kg body weight. In 20 hypertensive crises occurring in 16 patients a single dose of nifedipine was sufficient to lower systolic as well as diastolic blood pressure significantly within 90 min. for a period of 4 to 12 hours. No side effects were noted with the exception of a transient flush in one patient. Nifedipine proved to be suitable for the primary treatment of hypertensive emergencies in children suffering from renal hypertension. The advantages of nifedipine compared to other drugs used for treating hypertensive crises is the rapid onset of the antihypertensive action without need for an intravenous form of administration.     

Antireproductive effect of calcium channel blockers on male rats

Introduction  Drugs have been shown to adversely affect male fertility and recently anti-hypertensive drugs were added to the list. The anti-fertility effects of nifedipine and similar calcium channel blockers are well-illustrated in in vitro experiments but not in vivo. Purpose  The present study was designed to experimentally elucidate the sub-chronic effect of nifedipine, verapamil and diltiazem on sperm functions and reproductive hormone levels in vivo. Methods  Male rats (150–200 g) were divided into four groups of ten rats each. Group 1 (control) received distilled water; Group 2 received nifedipine 0.57 mg/kg BW; Group 3 were given verapamil 3.40 mg/kg BW and Group 4 were given diltiazem 2.57 mg/kg BW. Each drug-treated group had its own recovery group from which treatment was discontinued for 30 days before the animals were sacrificed. Blood samples were collected for hormonal assay of FSH, LH and testosterone. Semen evaluation was done and the testes, seminal vesicle, epididymis and prostate were removed, and weighed immediately. Results  Nifedipine, verapamil and diltiazem significantly decreased (P < 0.05) sperm count and motility in drug treated groups. The weight of the epididymis was significantly reduced (P < 0.05) in the drug treated rats. Semen parameters and other associated changes were restored after 30 days of drug withdrawal. Conclusion  Calcium channel blockers appear to have a reversible anti-fertility effect on male rats which does not occur through inhibition of the pituitary-gonadal axis.