培哚普利和贝那普利降压疗效的观察

目的：研究比较培哚普利及贝那普利的降压疗效及安全性。方法本研究共收集112例未治疗的新诊断或以往单药治疗而血压未控制的1、2级高血压病患者,分两组比较：一组服用培哚普利1日8mg,另一组为贝那普利1日10mg,观察时间8周,观察24h平均血压和清晨血压的降压疗效和安全性,进行统计分析。结果培哚普利和贝那普利均能明显降低24 h平均血压和清晨血压（ P＜0.05）,1日8 mg培哚普利较贝那普利1日10mg疗效更显著（P＜0.05）。结论培哚普利和贝那普利均是有效而且安全性良好的降压药物,且足量的培哚普利（1日8mg）疗效更佳。     

左旋氨氯地平联合培哚普利治疗糖尿病并发高血压与肾功能损害17例

目的探讨左旋氨氯地平和培哚普利联合应用对2型糖尿病并发高血压及新发肾功能损害患者的疗效。方法2型糖尿病并发高血压、微量蛋白尿患者51例，随机分3组：左旋氨氯地平组、培哚普利组、联合治疗组各17例；3组分别给予左旋氨氯地平2.5 mg，培哚普利4 mg，培哚普利4 mg和左旋氨氯地平2.5 mg，均qd，po，疗程12周。观察治疗前后血压和肾功能变化。结果两药单独治疗及两药联合应用均明显降低高血压（P＜0.01），降低微量尿蛋白（P＜0.05），联合治疗降血压和降低尿蛋白的幅度优于单独治疗（P＜0.01）。结论左旋氨氯地平、培哚普利治疗糖尿病高血压均有较好的降血压作用，且能降低微量尿蛋白，降低新发肾功能损害，两药联合治疗可起到协同作用。     

应用动态血压监测评价培哚普利治疗原发性高血压的降压疗效

目的：应用动态血压监测（ABPM）评估培哚普利（Perindopril）对轻、中度原发性高血压（EH）病人的24h降压效果。方法：轻、中度EH病人36例,服用2周安慰剂,坐位舒张压仍在95ˉ114mmHg者给与培哚普利4mg/d治疗8周。及治疗2、4、6、8周末测诊室血压,于服安慰剂末及治疗8周末应用ABPM。结果：培哚普利治疗8周,降压总有效率为83.3%;24h各时点血压均较治疗前显著下降（P＜0.01）不伴有心率及血压昼夜节律的改变;降低收缩压和舒张压的谷／峰值分别为80.6%和86.7%。结论：培哚普利能平稳、有效的控制EH病人24h血压,且病人总体耐受良好。     

培哚普利与吲哒帕胺联用对高血压左室肥厚的逆转作用

目的：观察培哚普利与吲哒帕胺联用对原发性高血压（EH）左室肥厚（LVH）的逆转作用。方法：将78例EH伴LVH病人随机分为A组（单用培哚普利）38例，B组（培哚普利与吲达帕胺联用）40例。观察两组治疗前后及两组间血压及LVH指标的变化。结果：6个月后两组血压均较治疗前明显下降（P＜0．01），组间降压幅度差异无显著意义（P＞0．05）。两组左室重量指数均较治疗前明显降低（P＜0．01），B组较A组明显（P＜0．05）。结论：两药联用对LVH逆转有协同作用。     

乐卡地平与培哚普利联合治疗轻中度高血压疗效及安全性观察

目的评价乐卡地平与培哚普利小剂量单独治疗和联合治疗轻度原发性高血压的疗效及安全性。方法 180例轻度原发性高血压患者随机分成联合治疗组（A组）和单用乐卡地平组（B组）和单用培哚普利组（C组）。A组服用培哚普利2 mg·d^-1＋乐卡地平5 mg·d^-1;B组服用乐卡地平10 mg·d^-1;C组服用培哚普利4 mg·d^-1。分别观察三组治疗后4、8、12周后降压效果及安全性。结果联合治疗组第4周开始,血压达标率及血压下降幅度均优于单药治疗组,三组间差异有统计学意义（P〈0.05）。联合治疗组治疗期间不良事件发生4例,明显低于单药治疗组（乐卡地平组7例,培哚普利组19例）,差异有显著性（P〈0.05）。结论乐卡地平与培哚普利联合应用可明显增加降压幅度和降压速度、提高降压有效率,两药小剂量联合可减少药物不良反应发生率。     

培哚痹利对原发性高血压合并外周动脉病变的影响

目的：探索培哚痹利对原发性高血压（ＥＨ）合并外周动脉病变（ＰＡＤ）的影响。方法：将４３例Ⅱ期ＥＨ合并ＰＡＤ的男性病人随机分为２组。治疗组２２例（年龄５４±ｓ９ａ）采用培哚普利４￣８ｍｇ，ｐｏ，ｑｄ，共４ｗｋ。对照组２１例（年龄５４±１０ａ）其中１４例采用卡托普利２５ｍｇ，ｐｏ，ｂｉｄ或ｔｉｄ治疗，共４ｗｋ。结果：２组均有显的降压疗效，Ｐ值均〈０．０１；培哚普利对２４ｈ动态血压趋于正常治疗后降压疗     

小剂量培哚普利吲达帕胺片治疗原发性高血压疗效观察

目的：探讨小剂量培哚普利吲达帕胺片治疗原发性高血压的疗效与安全性。方法：原发性轻中度高血压患者106例分为两组,观察组54例给予培哚普利吲哒帕胺片1片（培哚普利2 mg,吲哒帕胺0.625 mg）,qd,对照组52例给予培哚普利片4 mg,qd。治疗8周后,比较两组血压达标率、临床疗效,以及两组不良反应发生情况。结果：治疗后,观察组总有效率88.8%,对照组总有效率80.7%,两组比较差异无统计学意义（P〉0.05）。两组治疗后SBP和DSP均较治疗前明显下降（P〈0.05）,且观察组改善效果优于对照组（P〈0.05）。观察组不良反应发生率比较,明显低于对照组（P〈0.05）。结论：小剂量培哚普利吲达帕胺片治疗原发性高血压可提高血压达标率,降压效果较好,且不良反应少,值得临床推广应用。     

培哚普利、氨氯地平降压治疗对原发性高血压患者大动脉弹性的影响

目的 比较培哚普利、氨氯地平改善原发性高血压患者动脉弹性的作用.方法 78例轻中度原发性高血压患者随机均分成培哚普利组和氨氯地平组,以血压＜140/90 mm Hg为降压达标,检测用药前和降压达标后4、12周的颈股脉搏波传导速度(cfPWV).结果 与治疗前比较,培哚普利组和氨氯地平组治疗后4、12周的cfPWV均明显下降[(12.9±2.3)m/s vs.(11.1±2.1) m/s、(9.6±1.7) m/s和(13.3±2.6)m/s vs.(11.4±2.2)m/s、(9.4±1.6)m/s](P＜0.01).结论 运用培哚普利、氨氯地平降压达标,均能改善原发性高血压患者大动脉弹性.     

培哚普利联合依贝沙坦治疗高血压病的临床观察

目的：观察培哚普利联合依贝沙坦对高血压患者血压、血肌酐、血钾、尿蛋白的影响。方法：将60例高血压病患者用数字随机法分为两组,每组各30例。对照组使用培哚普利降压,必要时加用吲达帕胺;观察组在此基础上加用依贝沙坦。疗程均为4周。检测两组治疗前后血压、24h尿蛋白、血肌酐、血钾。结果：两组治疗前后组内比较,血压和24h尿蛋白定量下降明显（P〈0.01）,血肌酐及血钾水平无明显改变（P〉0.05）。治疗后两组间血压比较差异不明显（P〉0.05）,观察组24h尿蛋白定量较对照组下降明显（P〈0.01）。结论：培哚普利联合依贝沙坦对降低高血压病患者尿蛋白排出量较单独应用培哚普利疗效更佳。     

倍哚普利和非洛地平治疗高血压的比较

比较30例倍哚普利与30例非洛地平治疗的降压效果。两组剂量分别为4mg／日和5mg／日2次。4周后未达目标血压（≤140／90mmHg）者，加倍剂量。8周后倍哚普利组未达目标血压者，加用小剂量氯噻嗪。结果：8周后非洛地平组血压下降23／20mmHg，80％达到目标血压；倍哚普利组分别为11／10mmHg及36．3％（P值均＜0．01）。倍哚普利加氯噻嗪（12．5mg／日）后，血压进一步下降14／gmmHg，70．0％达到目标血压。非洛地平、倍哚普利及加用氯噻嗪三组的显效率和总有效率分别为93．3％，100．0％；43，3％，63．3％；86．7％，96．7％。非洛地平和倍哚普利均具有降压效果，非洛地平优于信哚普利。倍哚普利和小剂量氯噻嗪联合应用可达到满意的血压下降。     

Persistent effects on blood pressure and renal haemodynamics following chronic angiotensin converting enzyme inhibition with perindopril

Spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats aged 4 and 16 weeks were given an acute oral dose of either Perindopril (3 mg/kg) or vehicle. Direct blood pressure (BP), glomerular filtration rate (GFR) and renal blood flow (RBF) were measured, and renal vascular resistance (RVR) calculated. GFR and RBF were lower in vehicle-treated SHR than WKY at 4 weeks of age, but were not different at 16 weeks. Acute Perindopril increased GFR and RBF and reduced RVR in both strains at both 4 and 16 weeks. Total body sodium, sodium intake and blood pressure were measured in SHR and WKY from 1 to 28 weeks of age. Rats of both strains were treated daily between 4 and 16 weeks of age with either Perindopril (3 mg/kg per day) or vehicle. Chronic Perindopril treatment prevented the development of hypertension in the SHR. From 16 to 28 weeks of age, after stopping Perindopril, BP rose slowly in SHR, but remained lower than vehicle-treated SHR. No changes in total body sodium occurred during Perindopril treatment. GFR and RBF were measured in SHR and WKY chronically treated with either Perindopril or vehicle, 3 days or 12 weeks after stopping treatment. In WKY, GFR and RBF were not different between Perindopril-treated and untreated rats at either measurement. In SHR, GFR and RBF remained significantly higher in rats previously treated with Perindopril at both ages. These findings suggest that renal haemodynamic abnormalities may be important in the initiation of hypertension in the SHR. These renal circulatory abnormalities and the hypertension of the SHR depend, at least in part, on intact converting enzyme activity, yet appear to be independent of abnormalities of total body sodium. At a later age, hypertension seems to develop independently of renal vascular abnormalities.     

Effects of beta-adrenoreceptor antagonists on cerebral blood flow of cirrhotic patients with portal hypertension.

The current study evaluated the effect of two beta adrenergic-blocking agents, propranolol (PRP) and atenolol (ATN), versus placebo on cerebral blood flow (CBF) of three homogeneous groups of cirrhotic patients with portal hypertension. CBF was measured by the noninvasive 133-Xenon inhalation method at rest and 1 hour after a single oral dose of PRP (40 mg), or ATN (100 mg), or placebo. Blood pressure and heart rate (HR) were measured at the beginning of each examination, and end-tidal pCO2(PeCO2) was monitored. The HR decreased significantly in both the PRP and ATN groups (P less than .01), whereas no changes were recorded for both PeCO2 and mean arterial blood pressure (MABP). The comparisons of the CBF differences among groups (ANOVA with the significance levels adjusted by the Bonferroni's correction) showed a significant increase in CBF after ATN as compared with both placebo (P less than .02) and PRP (P less than .01), whereas no significant differences were seen after PRP as compared with placebo. Our results confirm that PRP does not significantly affect CBF, whereas ATN induces an increase in CBF, although the underlying mechanism is difficult to explain.     

Effects of mergocriptine on cerebral circulation and metabolism in cats.

Mergocriptine (CBM 36-733, CAS 81968-16-3) is an ergot alkaloid derivative and a dopaminergic agonist. Effects of mergocriptine on cerebral circulation and metabolism were examined by monitoring cerebral tissue oxygen and carbon dioxide tension (BrPO2, BrPCO2), cerebral blood flow (CBF) and blood pressure (BP) in 10 cats. Mergocriptine (10 micrograms/kg) infused into the carotid artery produced a significant increase in CBF during the administration followed by a decrease in BrPO2 in parallel with a significant decrease in BP.     

Effects of VA-045 on peripheral and central circulation in anesthetized dogs

• 1.1. The effects of VA-045, a novel apovincaminic acid derivative, vinpocetine, apovincaminic acid, brovincamine and nicergoline on peripheral and cerebral circulation were examined in anesthetized dogs.
• 2.2. Peripheral circulation: VA-045 induced a transient decrease in both blood pressure (BP) and heart rate (HR) and an increase in vertebral arterial blood flow (VBF) without affecting femoral arterial blood flow (FBF) or carotid arterial blood flow (CBF). Vinpocetine had no effect on BP, HR, VBF, FBF or CBF. Apovincaminic acid decreased HR and increased VBF without affecting FBF, CBF or BP. Brovincamine increased VBF and decreased CBF without affecting BP or FBF. Nicergoline decreased BP without affecting VBF, FBA or CBF.
• 3.3. Cerebral circulation: VA-045 increased cerebral blood flow (CerBF) without affecting BP. Brovincamine also increased CerBF and decreased BP. The potency of VA-045 in increasing CerBF was stronger than that of brovincamine. Vinpocetine and apovincaminic acid had no effect on BP or CerBF. Nicergoline decreased BP but did not affect CerBF.
• 4.4. These findings indicate that VA-045 has a more selective vasodilative effect on the vertebral and cerebral arteries than the other reference drugs.

     

Perindopril: an updated review of its use in hypertension

Perindopril erbumine (perindopril) is a prodrug ester of perindoprilat, an angiotensin converting enzyme (ACE) inhibitor. Perindopril 4 to 8 mg once daily significantly reduces supine systolic blood pressure (SBP) and diastolic blood pressure (DBP) from baseline values in hypertensive patients. These reductions are maintained for at least 24 hours, as evidenced by trough/peak ratios of >50%. Vascular abnormalities associated with hypertension were improved or normalised during perindopril treatment. Perindopril 4 to 8 mg once daily significantly decreased carotid-femoral aortic pulse wave velocity (PWV), improved arterial compliance, reduced left ventricular mass index and, in patients with recent cerebral ischaemia and/or stroke, preserved cerebral blood flow despite significantly reducing SBP and DBP. Further research is needed to establish the significance of promising results showing that reductions in aortic PWV were associated with reduced mortality in patients with end-stage renal failure, a third of whom received perindopril. Response rates (numbers of patients with supine DBP < or = 90 mm Hg) were significantly higher with perindopril 4 to 8 mg once daily (67 to 80%) than with captopril 25 to 50 mg twice daily (44 to 57%) in 3 randomised double-blind trials. In other clinical trials, the antihypertensive effects of perindopril were similar to those of other ACE inhibitors (including enalapril) and calcium-channel antagonists. Combination treatment with perindopril and an antihypertensive agent from another treatment class provided additional benefits, either as first-line treatment or in patients failing to respond to monotherapy. Perindopril monotherapy was also effective in the elderly and in patients with hypertension and concomitant disease. Perindopril has a similar adverse event profile to that of other ACE inhibitors; cough is the most common event reported during treatment, and is also the most common adverse event responsible for treatment withdrawal. Conclusions: Perindopril is a well tolerated ACE inhibitor that is significantly better than captopril (in terms of response rates) in the treatment of hypertension, and as effective as other ACE inhibitors. Perindopril appears to reverse some of the vascular abnormalities associated with hypertension, including arterial stiffness and left ventricular hypertrophy, although further research is needed to confirm promising results regarding its ability to decrease associated cardiovascular morbidity and mortality. Results from ongoing studies will help confirm the place of perindopril in the treatment of hypertension; currently, it is an effective and well tolerated treatment for patients with mild to moderate essential hypertension.     

豨莶草胶囊对麻醉犬脑血流量及脑血管阻力影响的研究

目的:研究豨莶草胶囊对麻醉犬脑血流量(CBF)、脑血管阻力(CVR)、血压、心电图及心率的影响。方法:将犬结扎一侧颈外动脉及椎动脉,以电磁流量计测颈动脉血流量,以多道生理记录仪记录血压、心电图及心率的变化。结果:豨莶草胶囊可显著增加麻醉犬的CBF,降低CVR,但对麻醉犬的血压、心电图及心率无显著影响。结论:豨莶草胶囊可通过增加CBF及降低CVR,改善脑血液循环。     

ANGIOTENSIN-CONVERTING ENZYME INHIBITION AS FIRST-LINE TREATMENT FOR HYPERTENSION

1. Perindopril (4 mg) was compared with atenolol (50 mg), captopril (25 mg b. d.) or a diuretic (hydrochlorothiazide 50 mg and amiloride 5 mg) in three studies involving a total of 503 hypertensive patients with a diastolic blood pressure (DBP) of 95–125 mmHg.
2. A 4 week single-blind placebo period preceded 12 weeks of active treatment. Dose titration was at weeks 4 and 8 if supine DBP >90 mmHg. The dose was doubled and if necessary a diuretic was added in the atenolol or captopril comparisons, and atenolol was added in the diuretic study.
3. The fall in supine blood pressure (BP) was 27/17 mmHg with perindopril and 21/16 mmHg for atenolol. Monotherapy controlled 55% of patients on perindopril and 48% on atenolol, increasing to 78% and 58% with the addition of hydrochlorothiazide, respectively. Captopril caused a BP fall of 19/12 mmHg compared with 27/18 mmHg for perindopril, with 49% of both groups being controlled on monotherapy.
4. Diuretic addition produced a greater antihypertensive effect with perindopril (75%) compared with 57% for captopril in achieving control. Perindopril caused a comparable fall in supine BP to the diuretic combination 27/19 mmHg and 31/18 mmHg, but the fall in erect systolic BP was significantly greater for the diuretic. At 3 months, 85% of the diuretic group and 78% of the perindopril group achieved the target BP.
5. A multicentre trial of 856 patients treated with perindopril (690 patients treated for 1 year or more) has shown that BP control is maintained in the long term with a low incidence of side-effects (7.9%) causing withdrawal from treatment. These studies demonstrate that perindopril compares favourably with standard first-line therapy for mild to moderate hypertension.     

Selective effects of lomerizine, a novel diphenylmethylpiperazine Ca2+ channel blocker, on cerebral blood flow in rats and dogs

1. In the present study we examined the effects of a new Ca2+ channel blocker (lomerizine), an antimigraine drug, on cerebral cortical blood flow (CBF) in anaesthetized rats (laser Doppler flowmetry) and on vertebral blood flow in anaesthetized beagle dogs (electromagnetic flowmeter). 2. Lomerizine (1.25-10 mg/kg, p.o.) dose-dependently increased CBF in rats without affecting blood pressure (BP) or heart rate (HR). 3. The plasma concentration of lomerizine (free base) in anaesthetized rats at 30 and 60 min after the initial administration of 5 mg/kg, p.o., time at which there was a significant increase in CBF, was similar to that reported in healthy subjects receiving lomerizine at 10 mg (2 x 5 mg)/day, p.o., a dose that significantly reduces the frequency and mean duration of headache attacks. 4. Flunarizine (10 mg/kg, p.o.) did not increase CBF significantly. Flunarizine (20 mg/kg, p.o.) did not increase CBF, but did decrease BP 30-120 min after its administration. 5. Lomerizine (2.5 and 5 mg/kg, intraduodenally) dose-dependently increased vertebral blood flow in dogs without significantly changing BP or HR. With 10 mg/kg intraduodenal lomerazine, vertebral blood flow remained elevated from 20 to 240 min after administration and BP was decreased from 20 to 120 min. 6. Thus, lomerizine had a greater effect on CBF than on BP and HR and, therefore, it may be clinically effective in conditions associated with circulatory disturbances in the brain, such as migraine, without producing systemic effects (e.g. hypotension) generally seen with other Ca2+ channel blockers.     

川芎、当归超临界CO2萃取液对犬血液动力学的影响

目的：观察不同剂量的CO2超临界川芎、当归萃取液犬脑血流动力学的影响。方法：各实验组十二指肠给药（5ml.mg^-1）后记录其脑血流量及血压的改变，并将同组各动物对应的脑血流量、血压进行统计学处理。结果：给川芎、当归萃取液及阳性药物（脑安胶囊），脑血流平均变动幅度与溶剂对照组相比，具有显著性差异，而平均血压变动无显著性差异。结论：川芎、当归萃取液对及血液动力学有影响，可使犬脑的血流量显著增加，而对血压没有明显的作用。