依普罗沙坦与氯沙坦在轻中度原发性高血压病人中的降压疗效比较

目的:以氯沙坦为对照,观察依普罗沙坦治疗轻、中度原发性高血压(EH)病人的疗效与安全性。方法:采用前瞻性、随机、双盲、阳性药对照研究。符合方案的50例轻、中度EH病人经筛选期(2 wk)、安慰剂导入期(2 wk)后,随机分为依普罗沙坦组(n=24)与氯沙坦组(n=26)。在治疗期,2组病人分别每日1次口服依普罗沙坦600 mg或氯沙坦50 mg。若4 wk血压不达标,即坐位舒张压(DBP)≥90 mmHg (1 mmHg=0．133 3 kPa),加氢氯噻嗪12．5 mg,每日1次口服至8 wk。观察治疗前、治疗后4 wk与8 wk血压、心率以及治疗前后血、尿常规,血生化及心电图改变。结果:在治疗后8 wk,依普罗沙坦组的收缩压(SBP)与DBP分别下降了(12±s 10)mmHg与(12±5)mmHg,氯沙坦组的降压幅度分别为(14±9)mmHg与(10±6)mmHg,治疗前后比较有非常显著差异(P<0．01);但2组间血压下降的幅度无显著差异(P>0．05)。依普罗沙坦组与氯沙坦组的降压总有效率分别为100％和8l％,2组疗效无显著差异(P>0．05)。依普罗沙坦组加用氢氯噻嗪病例为9例(38％),而氯沙坦组为6例(23％),p> 0．05。2组心率及血液生化检查结果,治疗前后变化均无显著意义(P>0．05),均无严重不良反应发生。结论:依普罗沙坦与氯沙坦均能有效降低轻、中度EH病人的血压,疗效相似,都具有良好的安全性。     

Comparison of atenolol 50 mg and 100 mg as initial treatment in uncomplicated mild to moderate hypertension

Summary After screening a local population in the northern part of The Netherlands for hypertension, 59 patients with a diastolic pressure (DP) between 95 and 130 mmHg were randomized and treated either with 50 mg atenolol (n=29) or 100 mg atenolol (n=30) for 1 month. There was no significant difference between the two treatments, neither in the fall in systolic and diastolic pressures nor in the number of complaints reported. It is concluded that in the initial treatment of uncomplicated mild to moderate hypertension, 100 mg atenolol has no advantage over a 50 mg dose.     

Antihypertensive effect of low-dose hydrochlorothiazide alone or in combination with quinapril in black patients with mild to moderate hypertension

In this study, using 24-hour ambulatory blood pressure (BP) monitoring, the authors assessed the potential for BP control using hydrochlorothiazide (HCTZ, 12.5 mg daily), given as a monotherapy over 12 months to 49 black South African patients with mild to moderate hypertension (mean day diastolic blood pressure [DBP] > or = 90 and < 115 mmHg). Uncontrolled patients received fixed combination of quinapril/HCTZ 10/12.5, 20/12.5, and 20/25 mg, with dose titration at 3 monthly intervals if BP control was not achieved (day DBP < 90 mmHg). Overall, profound and sustained BP reduction was observed at the end of the study. The 24-hour BP decreased from 151 +/- 14/98 +/- 7 to 136 +/- 15/87 +/- 9 mmHg (p < 0.0001 at end of study vs. baseline); the mean day BP decreased from 155 +/- 14/104 +/- 7 to 140 +/- 15/91 +/- 10 mmHg (p < 0.0001 at end of study vs. baseline). The overall control (mean day DBP < 90 mmHg) and response (decrease in day DBP > or = 10 mmHg) rates were 49% and 61%, respectively. At the end of the study, only 2 patients (4%) remained on treatment with HCTZ. Out of the initial 12 patients controlled on HCTZ at 3 months (12/49, 24%), 5 patients remained controlled at 6 months and only 1 patient at 12 months. In contrast, quinapril/HCTZ combinations maintained their antihypertensive effect up to 9 months, with a significant number of patients (22/49, 45%) requiring the highest dose of the combination (20/25 mg daily). In conclusion, low-dose HCTZ should not be recommended as monotherapy in black patients with mild to moderate hypertension due to the fact that the BP-lowering effect is attenuated already at 6 months of treatment, with most patients requiring the addition of the ACE inhibitor.     

硝苯地平控释片与普通片治疗老年高血压病比较

目的 比较硝苯地平控释片与普通片对老年高血压患者的降压疗效。方法 采用随机、单盲的方法，对８４例老年高血压患者进行２４ｈ动态血压监测，比较其疗效及副反应。结果 两药均能显著降低老年高血压患者的偶测血压及２４ｈ平均血压（Ｐ〈０．０１）。两药在降低偶测压缩压、２４ｈ平均收缩压及白天平均血压幅度方面差异无显著性（Ｐ〉０．０５），硝苯地平控释片能明显降低患者的偶测舒张压（Ｐ〈０．０５）、２４ｈ平均舒张压（     

依那普利和氯沙坦治疗中重度高血压的疗效观察

目的：评价依那普利和氯沙坦联用对中度重度高血压患者的降压效果和左心室肥厚的逆转作用。方法：对36例中重度高血压患者给予口服依那普利5－10mg/日和氯沙坦25－50mg/日,监测血压、心率及行超声心动图检查。结果：经治疗患者血压、心率明显下降,IVST、LVPWT和LVMI明显减少（P＜0．01）。结论：依那普利和氯沙坦联用能有效降低血压及逆转心室肥厚,且两药单独用量少,副作用少。     

氯沙坦与缬沙坦治疗轻、中度老年高血压疗效与成本分析

目的比较两种AT1拮抗剂治疗轻、中度原发性高血压病人的成本-效果。方法运用药物经济学成本-效果分析方法对两种口服AT1拮抗剂(A组:氯沙坦;B组:缬沙坦)进行比较。结果两组均有效降压(P<0.05),组间对照无显著性差异(P>0.05),但B组的成本-效果值低与A组。结论两种方案都能将血压控制在理想范围,疗效确切,不良反应少,缬沙坦更理想、经济。     

替米沙坦联用氢氯噻嗪治疗轻中度高血压的临床研究

目的:评估国产替米沙坦片联用氢氯噻嗪片治疗轻中度高血压的有效性和安全性。方法:152例轻中度原发性高血压患者经2周安慰剂洗脱期后,用替米沙坦40mg治疗4周,4周末单剂治疗无效的72例患者接受替米沙坦40mg和氢氯噻嗪12．5mg治疗8周。在洗脱期末(0周)、替米沙坦单剂治疗末(4周末)和替米沙坦联用氢氯噻嗪8周末(12周末),进行诊室血压(CBP)、心电图、血生化指标、24h动态血压监测(ABPM)、脉搏波传导速度(PWV)和超声心动图检测。结果:12周末与4周末比较,诊室收缩压(CSBP)和诊室舒张压(CDBP)均显著降低(P＜0．001),降压幅度达16．70/15．28mmHg,总有效率91．67%,不良事件发生率9．7%;24h平均收缩压和舒张压均显著降低(P＜0．001),降幅为8．41/6．21mmHg,24h平均脉压(PP)也显著降低,降幅为4．60 mmHg,白昼及夜间血压及血压负荷值均显著降低(P＜0．05),12周末收缩压谷峰比为72．66%,舒张压谷峰比为76．21%。4周末, PWV显著降低[(11．17±1．83)vs(10．19±1．44)m·s~(-1),P＜0．05],舒张早期血流峰值流速(E峰)与舒张晚期血流峰值流速(A峰)的比值(E/A)显著增加、左室等容舒张时间(IVRT)显著缩短,左室重量指数(LVMI)也显著改善(P＜0．05)。12周末,PWV进一步降低至(9．24±1．01)m·s~(-1)(P＜0．001),舒张功能显著改善(P＜0,01), LVMI也显著降低(P＜0．001)。结论:国产替米沙坦片40mg联用氢氯噻嗪片12．5mg对于替米沙坦40mg单剂治疗4周无效的轻中度高血压患者安全有效。     

A comparison of lisinopril and nifedipine in the treatment of mild to moderate hypertension

Lisinopril has been compared with slow-release nifedipine in a 16-week double-blind, randomized, parallel-group study involving 102 patients with mild to moderate hypertension. Sitting systolic and diastolic blood pressures were reduced 6 and 5 mm Hg more by lisinopril than by nifedipine over 12 weeks monotherapy.After 12 weeks a greater proportion of patients taking lisinopril was controlled (sitting diastolic blood pressure below 95 mm Hg) than in those taking nifedipine. As a result, 17% of those taking lisinopril and 38% of those taking nifedipine required additional therapy with hydrochlorothiazide. The addition of hydrochlorothiazide resulted in similar response rates in the lisinopril and nifedipine groups (89% and 75% respectively).The rate of reporting of adverse events considered to be drug-related and the rate of withdrawals were similar for both treatments. Cough was more often reported with lisinopril and headache, sweating, and hot flushes with nifedipine.We conclude that once-daily titrated doses of lisinopril produced better control of blood pressure than twicedaily titrated doses of nifedipine.     

地尔硫和氯沙坦联合应用治疗轻、中度原发性高血压

目的 :探索地尔硫和氯沙坦联合应用治疗原发性高血压的疗效和安全性。方法 :采用随机、单盲、平行对照研究 ,5 9例病人分为 2组 :一组给予地尔硫 90mg +氯沙坦 5 0mg ,另一组给予地尔硫 90mg +福辛普利 10mg ,观察降压效果、改善左室重构的作用和不良反应。结果 :治疗后 4wk起 ,血压即显著下降。wk 12时 ,地尔硫 +氯沙坦组和地尔硫 +福辛普利组收缩压 /舒张压平均下降幅度分别为 (2 .1± 0 .3) /(2 .1± 0 .4 )kPa和 (2 .1± 0 .3) /(1.7± 0 .3)kPa ,血压达标率分别为 83%(2 5 /30 )和 86% (2 5 /2 9) ,左室重量指数均显著下降。 2组之间各项指标均无统计学差异 (P >0 .0 5 )。病人均能很好耐受。结论 :与地尔硫 +福辛普利一样 ,地尔硫和氯沙坦联合应用是治疗轻、中度原发性高血压的有效而安全的方案。     

A multi-centre, placebo controlled comparative study between 200 mg and 400 mg celiprolol in patients with mild to moderate essential hypertension

A two-centre, double-blind, placebo controlled, randomized 3-way crossover study was undertaken to assess the efficacy, tolerability and safety of celiprolol in mild to moderate essential hypertension. A 4-week single-blind placebo run-in/screening period, during which no antihypertensive medication was given, was followed by 3 consecutive 4-week treatment periods with placebo or celiprolol (200 mg or 400 mg daily). At the end of the 4-week placebo run-in/screening period, 26 hospital out-patients with a seated mean blood pressure (systolic/diastolic) of 161.4/101.7 mmHg and a mean pulse rate of 75 beats/min entered the double-blind crossover phase of the study. Results showed that there was no significant difference in seated mean systolic or diastolic blood pressure between 200 mg celiprolol daily (149.2/92.3 mmHg) and 400 mg celiprolol daily (149.1/92.5 mmHg). However, mean seated systolic and diastolic blood pressures were significantly (p less than 0.05) lower on celiprolol than on placebo (157.1/98.2 mmHg). Neither dose of celiprolol had a significant effect on seated pulse rate. No patient was withdrawn due to an adverse event and no laboratory assessment outside the normal range was reported to be of any clinical significance. It is concluded that oral celiprolol, 200 mg or 400 mg daily, is effective and well tolerated for controlling mild to moderate essential hypertension. Since both doses had very similar effects on blood pressure there is no advantage in this group of patients for the 400 mg daily dose of celiprolol.     

Efficacy of a fixed-dose combination of 40 mg penbutolol with 6 mg piretanide in the treatment of mild to moderate hypertension: a double-blind study against placebo

The antihypertensive efficacy and tolerability of a fixed-dose combination containing 40 mg penbutolol (a beta-blocking agent) and 6 mg piretanide (a diuretic) in comparison to placebo was investigated in a double-blind, crossover study in 20 patients with mild to moderate essential hypertension. After a 1-week period on placebo, patients were allocated at random to receive 1 tablet daily for 4 weeks of either the combination preparation or placebo and were then crossed over to the alternative medication for a further 4 weeks. The reduction in systolic and diastolic blood pressure both at rest, during maximal ergometric exercise and isometric word load, and also in the diurnal blood pressure profile over 24 hours was significantly greater in the group treated with the fixed-dose combination than in the placebo group. Pulse rate was also decreased to a greater extent. Mean diastolic blood pressure before exercise was reduced to normal (85.5 mmHg) after 4-weeks' treatment with the fixed-dose combination. Biochemical, haematological and urinary parameters showed no clinically relevant changes after either treatment. One patient complained of transient dizziness during treatment with the fixed-dose combination. No patient withdrew prematurely from the study because of side-effects.     

Comparison of once daily felodipine 10 mg ER and hydrochlorothiazide 25 mg in the treatment of mild to moderate hypertension

Summary The efficacy of extended release felodipine 10 mg (ER) o.d., a new dihydropyridine calcium antagonist, and 25 mg hydrochlorothiazide (HCTZ) o.d. have been compared in a randomized, double-blind, crossover trial in 28 mildly to moderately hypertensive subjects (supine diastolic blood pressure, BP, 95 mm Hg and 110 mm Hg on three separate occasions).Both drugs significantly reduced systolic and diastolic BP in the sitting position felodipine from 157.1/93.8 mm Hg at baseline to 133/78.9 mm Hg 2.5 h after medication and to 138/82.7 mm Hg after 2 weeks of treatment, and HCTZ from 156/95.6 mm Hg to 147/88.4 mm Hg 2.5 h after medication and to 149/89.5 mm Hg also after 2 weeks.A decrease of the same magnitude in standing systolic and diastolic BP was observed after both treatment regimens with the exception of diastolic BP 2.5 h after dosing with HCTZ, which was not significantly lower. At all times (2.5 h and 2 weeks), the reduction in systolic and diastolic BP was greater after felodipine compared to HCTZ. Heart rate was significantly increased after felodipine in both the sitting and standing positions, and both 2.5 h following medication and after 2 weeks of treatment. The difference between the regimens was significant only 2.5 h after dosing. Overall, felodipine 10 mg ER o.d. was superior to 25 mg HCTZ o.d. in lowering BP.Presented in part at the Vth Scientific Meeting of the American Society of Hypertension, 17–20 May 1990, New York     

吲达帕胺与硝苯地平对轻、中度高血压病人生活质量影响的比较

目的 :探讨吲达帕胺与硝苯地平对轻、中度高血压病人的治疗效果和对生活质量的影响。方法 :12 7例轻、中度高血压病人分为 2组 ,吲达帕胺组 6 7例 ,给 2 .5mg ,po ,qd× 2mo ;硝苯地平组 6 0例 ,给硝苯地平 10mg ,po ,tid× 2mo。结果 :2药均能有效降低血压 (P <0 .0 1) ,对血脂、肾功能、尿酸、电解质等生化指标均无明显影响。吲达帕胺组可使各项生活质量指标均获好转 ,而硝苯地平组自觉症状增多 ,生活质量下降。结论 :2药降压作用均肯定 ,但吲达帕胺不良反应少、在全面改善生活质量方面优于硝苯地平。     

Reproducibility of nifedipine absorption from GITS tablets: comparison of single-dose pharmacokinetics using 10, 20, 40 and 60 mg nifedipine

OBJECTIVE: To examine the reproducibility of nifedipine absorption from gastrointestinal therapeutic system (GITS) tablets by comparing the single-dose pharmacokinetic profiles of 4 different dosages administered orally. METHODS: Twelve healthy male volunteers, aged between 22 and 29 years were enrolled in the open, 4-way, dose escalation study with single oral doses of 10, 20, 40 and 60 mg (two 30 mg) nifedipine GITS tablets. Each administration was separated by a 1-week washout period. Coefficients of variation (CV) of dose-corrected area under the concentration-time curve (AUC) and peak plasma drug concentrations (Cmax) were calculated from the pharmacokinetic profiles. RESULTS: Mean AUC and mean Cmax were dose-proportional from 10 to 60 mg. Although the CV of 4 mean dose-corrected AUC and Cmax were 5.5% and 17.5%, respectively, CV of dose-corrected AUC and Cmax in each subject varied from 5.1 to 37.4% (mean 11.0%) and from 14.1% to 46.4% (mean 25.8%), respectively. CONCLUSIONS: Whereas mean plasma nifedipine concentration remained markedly stable over a 16- to 24-hour interval and mean dose-corrected AUC showed good reproducibility with nifedipine GITS, the CV of dose-corrected AUC of the nifedipine GITS tablets in each subject showed large variability.     

Effects of amlodipine and enalapril on platelet function in patients with mild to moderate hypertension.

OBJECTIVE: The aim of this study was to compare the effect of amlodipine and enalapril on platelet aggregation, and platelet production of malondialdehyde in patients with mild to moderate arterial hypertension. PATIENTS AND METHODS: A parallel, double-blind, placebo-controlled study was carried out in 24 patients (2 groups of 12 patients each). Initially all patients received placebo for four weeks; then amlodipine, 5 mg daily or enalapril 20 mg daily taken once a day at 7 am. Dosage was doubled after 4 weeks when diastolic blood pressure was > 90 mmHg in sitting position, the treatment was continued for 12 weeks. At the end of placebo and active phases a platelet aggregation test, using adenosine diphosphate, collagen and adrenaline, and a platelet malondialdehyde production test, either in basal conditions (MDA-basal) and after the stimulation of arachidonic acid pathway by adding ethylmaleimide (MDA-activated) were carried out. RESULTS: Blood pressure was reduced by both agents, enalapril and amlodipine. Enalapril controlled 58.3% of hypertensive patients with an average dosage of 31.7 mg/daily. Amlodipine controlled 75% of patients with a dosage of 7.1 mg/daily. Platelet aggregation was reduced by amlodipine in 15.9% for ADP (10 microM); 17.4% for collagen (2 microg/ml) and 19.9% for adrenaline (2 microM) (p < 0.025). Meanwhile enalapril slightly increased platelet aggregation by 6.7%, 1.3% and 5.6% for the three agents, respectively (p > 0.05, ns). Malondialdehyde was reduced by amlodipine in 45.33% (p < 0.05) for MDA-basal; 3.76% (p > 0.05) for MDA-activated; and the ratio MDA-basal:MDA-activated in 36.79% (p < 0.005). Meanwhile enalapril increased MDA-basal in 2.89%; MDA-activated in 3.58% and reduced the ratio MDA-basal:MDA-activated, in 10.34% (p > 0.05). CONCLUSION: Both agents, enalapril and amlodipine, reduced blood pressure, but only amlodipine reduced platelet aggregation and platelet production of malondialdehyde, indicating its action on the arachidonic acid metabolic pathway.     

Efficacy and safety of sumatriptan 50 mg in patients not responding to standard care, in the treatment of mild to moderate migraine. The Sumatriptan 50 mg Italian Study Group

The tolerability and efficacy of oral sumatriptan 50 mg for the treatment of mild to moderate migraine attacks were assessed in a double-blind, multicenter placebo-controlled study on a group of patients who had not responded sufficiently to analgesic preparations. Three-hundred-and-twenty-eight migraine sufferers treated a first migraine attack with a nontriptan standard care medication: a mixture containing phenazone, butalbital and caffeine (optalidon) or indomethacin plus prochlorperazine plus caffeine (difmetre) or paracetamol 100 mg (tachipirine), depending on their habits. Of these patients, 32.6% reported headache relief with this treatment and were not included in phase II of the study. The 219 patients not reporting relief during the first phase of the study entered the second phase and were randomized to sumatriptan 50 mg or to placebo; 167 of these patients treated a second attack according to the protocol and were evaluated for efficacy. Of the patients with migraine taking sumatriptan, 58% reported headache relief compared with 35% of placebo-treated patients (p = 0.008). The reduction of nausea and vomiting was significantly better in the sumatriptan group. No differences were detected for the recurrence rate, while rescue medication was used more by the placebo group. The safety profile of sumatriptan 50 mg was confirmed. This study demonstrates the usefulness of this dose of oral sumatriptan against the pain and the accompanying symptoms of mild and moderate migraine.     

依那普利联合硝苯地平控释片治疗高血压疗效观察

目的观察依那普利联合硝苯地平控释片治疗高血压病的临床疗效。方法将120例高血压患者随机分为治疗组和对照组各60例。对照组给予依那普利口服治疗;治疗组在对照组基础上给予硝苯地平控释片口服治疗。观察2组临床疗效和血压改善情况。结果治疗组总有效率为95．0％高于对照组的81．7％,差异有统计学意义（P〈0．05）。治疗后2组血压均低于治疗前,且治疗组低于对照组,差异均有统计学意义（P〈0．05）。结论依那普利联合硝苯地平控释片治疗高血压病疗效显著,无明显不良反应,值得临床推广应用。     

缬沙坦与贝那普利治疗老年轻中度高血压疗效观察

目的:观察缬沙坦与贝那普利治疗原发性轻、中度高血压的临床降压疗效.方法:72例临床确诊为轻、中度高血压患者,随机分为缬沙坦组(37例)和贝那普利组(35例),分别每日早晨服缬沙坦80 mg,贝那普利10 mg,观察时间为6周.服药后1、4、6周测定血压,入选时与服药后第六周测定血钾、肝功能、肾功能和血脂.结果:服药1,4,6周两组血压均较治疗前显著降低(P＜0.05),两组疗效差异无统计学意义(P＞0.05),到第六周末,缬沙坦组与贝那普利组降压总有效率分别为78.37%与75.75%.与治疗开始前比较,第六周末血钾、肝功能、肾功能无明显改变,缬沙坦组TC、TG、LDL-C较贝那普利组显著降低,HDL-C无明显变化.结论:缬沙坦与贝那普利对老年原发性轻、中度高血压患者均有良好的降压效果,服用安全,缬沙坦能改善高血压患者的脂质代谢.     

A comparative trial of lisinopril and nifedipine in mild to moderate hypertension in general practice.

AIMS: to compare lisinopril and nifedipine in the management of essential hypertension in 52 patients in general practice with respect to the obtaining of target diastolic blood pressure and freedom from side effects. METHOD: an open label, parallel randomised trial over an eight week period. RESULTS: lisinopril and nifedipine were found to effectively lower diastolic blood pressure with the latter having a significantly higher level of withdrawals and clinical side effects. CONCLUSION: lisinopril is equivalent to nifedipine in its hypertensive effect and has a better side effect profile.