Determination of felodipine in plasma by capillary gas chromatography with electron capture detection

Felodipine in plasma was extracted with toluene and determined by automated capillary gas chromatography with electron capture detection. Undesirable oxidation of the dihydropyridine derivative in the injector and in the column was avoided by the use of glass materials with the inner surfaces treated by high-temperature silylation. The day-to-day reproducibility of the method was represented by a relative standard deviation (RSD) of 5% for a felodipine concentration of 25 nmol/l. The minimum determinable concentration (giving better than 15% RSD) was 1–2 nmol/l (0.4–0.8 ng/ml).     

波依定治疗老年单纯收缩期高血压的疗效观察

目的：观察波依定对老年单纯收缩期高血压的疗效。方法：42例老年单纯收缩期高血压患者波依定5－10mg,每天早晨口服1次,疗程3个月,治疗前后对患者的动态血压,血糖、血脂和血尿酸进行监测,并进行统计分析,结果：波依定治疗后24小时平均收缩压、日间及平均收缩压均明显下降（P＜0．05）;24小时平均舒张压、日间及夜间舒张压亦有所下降（P＜0．05）24小时平均心率、血糖、血脂、血尿酸未见明显改变。结论：波依定治疗老年单纯收缩期高血压是有效而安全的。     

非络地平对原发性高血压患者心肌保护的影响

目的;研究原发性高血压患者服用非络地平,其心肌缺血改善的情况。方法：将47例原发性高血压患者经过6周的观察期后分为2组,氢氯噻嗪＋非络地平组（A组,n=25),氢氯噻嗪＋安慰剂组（B组,n=22)。接受治疗12周,治疗前后做12导联心电图,测定QT离散度（QTd)、ST段及T波的变化情况。结果：经过非络地平和安慰剂治疗12周后,非络地平组QTd明显缩短（P＜0．001）,ST段下降导联数及异常T波导联数均显著减少（P均＜0．001）,安慰剂组各指标无明显变化。结论：非络地平能够明显改善原发性高血压病心肌缺血,对心脏起保护作用。     

Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics on felodipine — and its potential clinical relevance

Summary The effect of drinking grapefruit juice on the acute pharmacokinetic and haemodynamic actions of the dihydropyridine calcium antagonist felodipine given as a 5 mg plain tablet has been studied in nine, healthy, middle-aged males.Compared to water, grapefruit juice caused an increase in C_max from mean 6 to 16 nmol · l^–1, and in the AUC from 23 to 65 nmol · h · l^–1. The change in AUC corresponded to an increase in the systemic availability of felodipine from 15 to 45%, assuming no change in its clearance. This change was probably caused by inhibition of the oxidation of felodipine to the inactive dehydrofelodipine by flavonoids in grapefruit juice. The interaction with grapefruit juice is believed to be a class effect for the dihydropyridines, as oxidation of the dihydropyridine ring to the corresponding pyridine derivative is a major metabolic route for all these drugs.The higher plasma concentrations of felodipine taken with grapefruit juice resulted in a greater change in blood pressure measured in the morning 3 h after dosing (–9%) than did water (0%).     

非洛地平降低心、脑血管并发症的临床评价

4 背景 我国曾进行的两项钙离子拮抗剂治疗高血压的对照试验（Syst-China，STONE）显示，与安慰剂对照，使用钙拮抗剂治疗可以显著降低脑卒中和其他主要心血管事件的发生。在前述的两个试验中，收缩压（systolic blood pressure，SBP）的降压目标为〈160mmHg（STONE）或〈150mmHg（Syst-China），且治疗后的SBP在150mmHg左右，远高于目前推荐的目标值SBP〈140mmHg。目前研究的证据显示，仅在有糖尿病或既往心血管疾病史的患者中SBP〈140mmHg有利，但是在所有高血压患者中血压进一步降低能否获益尚缺乏证据。     

非洛地平减轻造影剂诱导的肾小管上皮细胞损伤

目的 探讨钙通道拮抗药非洛地平是否对造影剂诱导的肾小管上皮细胞损伤具有保护作用及其机制. 方法 培养大鼠肾小管上皮细胞（NRK52E）与非洛地平（10^-5 mol•L^-1）作用12 h后, 加入造影剂（110 mgI•L^-1）作用0.5, 1.0 h, 采用乳酸脱氢酶（LDH）检测细胞损伤, 倒置显微镜观察细胞形态变化, 流式细胞仪检测细胞凋亡, 共聚焦显微镜测定细胞内钙和反应氧产物水平. 相同渗透压甘露醇作对照. 结果 泛影葡胺作用0.5, 1.0 h明显诱导细胞损伤或细胞凋亡, 造影剂组细胞内钙和反应氧产物随时间进行性增加, 显著高于相同渗透压甘露醇组和对照组; 非洛地平降低细胞内钙和反应氧产物水平, 同时降低细胞损伤和细胞凋亡. 结论 非洛地平通过降低细胞内钙超载和氧化应激对造影剂诱导的肾小管上皮细胞损伤发挥保护作用.     

非洛地平缓释片合用卡托普利治疗老年高血压病58例疗效观察

目的：观察非洛地平缓释片合用卡托普利治疗老年高血压病的临床疗效。方法：116例高血压痛患者随机分为两组。A组：非洛地平缓释片、卡托普利合用组58例；B组：单用卡托普利组58例。观察降压疗效及对心率、血脂、血糖、肾功能的影响。结果：A组显效43例，有效10例，无效5例，总有效率为91．38％；B组显效28例，有效20例，无效10例，总有效率为82．75％。两组比较有显著性差异，两组治疗前后心率、血脂、血糖、肾功能无明显变化。结论：非洛地平缓释片、卡托普利合用降压效果明显，同时对心率、血脂、血糖、肾功能无明显影响，是治疗老年高血压痛的适宜药物．     

The systemic and coronary haemodynamic effects of felodipine in patients with coronary heart disease

The cardiovascular effects of felodipine, a new arteriolar vasodilator,were studied in 22 patients with coronary heart disease. Therewere significant falls in blood pressure and systemic vascularresistance of 16 and 38% respectively (P = 0.001), thus affectingafter-load. Cardiac index and stroke index increased by 35 and12% respectively. There was reflex tachycardia-from 75 ±3to 85 ±3 b.p.m. (P =0.005). Coronary sinus blood /lowincreased from 134±9 to 191 ±17 ml/min (P<0.005)and myocardial arterio- venous oxygen difference narrowed from12.l±0.5 to 9.0±0.4 vols% (P<0.001) indicatingless oxygen usage. With the heart rate held constant by atrialpacing, cardiac index and stroke index increased by 30 and 26%(P<0.001), whilst systolic blood pressure and systemic vascularresistance fell by 20 and 29% (P<0.001). This would suggestthat the improved haemodynamics were largely secondary to after-loadreduction.     

非洛地平缓释片对原发性高血压患者动态血压的影响及与细胞内胞浆游离钙浓度的关系

目的 观察非洛地平对高血压患者动态血压的影响及与细胞内胞浆游离钙浓度的关系。方法 检测28例原发性高血压患者及相应对照组之血压及淋巴细胞胞浆游离钙浓度及非洛地平缓释片治疗四周后血压及淋巴细胞胞浆游离钙浓度的变化,并观察其治疗前后24h动态血压的变化。结果 原发性高血压患者淋巴细胞胞浆游离钙浓度显著高于对照组,非洛地平缓释片治疗后淋巴细胞胞浆游离钙浓度和血压显著下降(P<0.01),淋巴细胞胞浆游离钙浓度的下降幅度与收缩压及舒张压下降幅度呈正相关(r=O.866,P<0.001及r=0.734,P<0.001)。治疗后24h平均收缩压、24h平均舒张压、日间平均收缩压、日间平均舒张压、夜间平均收缩压、夜间平均舒张压、日间收缩压负荷、日间舒张压负荷、夜间收缩压负荷、夜间舒张压负荷均较治疗前明显降低(P<0.05-P<0.01)。结论非洛地平是平稳有效的抗高血压药物,其降压作用可能是通过降低细胞内胞浆游离钙浓度而发挥作用。     

珍菊降压片与其他一线降压药治疗原发性高血压临床研究

目的：比较珍菊降压片与其他一线降压药小剂量单用及联用对原发性高血压的有效治疗率。方法：原发性高血压466例分别给予珍菊降压片、CCB(非洛地平或硝苯地平）、ACEI（苯那普利或卡托普利）、美托洛尔或吲达帕胺治疗,未达治疗目标者二药、三药乃至四药合用,直至达到目标血压（＜140／90mmHg)为止。结果：珍菊降压片单用的有效治疗率72．8％,高压其他4类一线降压药（46．2％－54．0％）（P＜0．05）;与ACEI与CCB合用可进一步提高有效控制率（92．9％、97．1％）,且耐受性良好。结论：珍菊降压片价廉效好,可作为一线降压药。