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[普索洛尔(一种具有α-肾上腺素能阻断特性的新型β-肾上腺素能阻滞剂)单次用于劳力性稳定型心绞痛患者的疗效]

[The efficacy of proxodolol, a new beta-adrenoblockader with alpha-adrenoblockader properties, in its single use in patients with stable stenocardia of effort].

作者信息

Metelitsa V I, Martsevich S Iu, Kozyreva M P, Slastnikova I D, Vakulovskaia M K

出版信息

Eksp Klin Farmakol. 1994 May-Jun;57(3):47-50.

PMID:7914121
Abstract

The paper presents the results of the first phase of clinical trials of prodoxolol, a beta-adrenoblocker having alpha-adrenoblocking activity in a ratio of 100:1, in patients with coronary heart disease concurrent with stable exercise-induced angina pectoris. The tolerance of single proxodolol doses (10 mg in 4 patients, 20 mg in 2 and 40 mg in 2) was studied. In all cases, proxodolol reduced resting heart rate by 6-18 beats/min, which lasted for 5 hours or more. Four patients had a proxodolol-induced 20 mm Hg or more decrease in systolic blood pressure lasting for 5 hours. In 10 patients, the antianginal and anti-ischemic effects of proxodolol were evaluated by pharmaco-dynamic studies consisting in threshold treadmill exercise tests before and 30 min, 2 and 6 hours after single placebo (in 10 patients) and proxodolol (40 and 80 mg in 3 and 7 patients, respectively) administration. In addition, 7 patients underwent pharmacodynamic studies with propranolol, 80 mg. The efficacy was judged from the increased exercise duration before an anginal episode (antianginal effect) and from the decreased ST segment depression during the identical exercise (anti-ischemic effect). The antianginal effect of proxodolol began 30 min later, reaching its peak 2 hours later and retained 6 hours later. During all study periods it was more marked than that of propranolol. The anti-ischemic effect of proxodolol was similar to the antianginal effects and it did not correlated with its chronotropic one. Proxodolol was well tolerated with patients. Thus, proxodolol in single doses of 40 and 80 mg produced antianginal and anti-ischemic effects and its action was similar to that of propranolol.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

本文介绍了普多洛尔(一种α-肾上腺素能阻断活性与β-肾上腺素能阻断活性之比为100:1的β-肾上腺素能阻滞剂)在伴有稳定运动诱发型心绞痛的冠心病患者中进行的第一阶段临床试验结果。研究了单次服用普多洛尔剂量(4例患者服用10mg,2例患者服用20mg,2例患者服用40mg)的耐受性。在所有病例中,普多洛尔使静息心率降低6 - 18次/分钟,持续5小时或更长时间。4例患者收缩压因普多洛尔降低20mmHg或更多,持续5小时。10例患者通过药效学研究评估普多洛尔的抗心绞痛和抗缺血作用,该研究包括在服用单次安慰剂(10例患者)和普多洛尔(分别为3例患者服用40mg和7例患者服用80mg)前、30分钟、2小时和6小时进行阈下跑步机运动试验。此外,7例患者用80mg普萘洛尔进行了药效学研究。疗效根据心绞痛发作前运动持续时间的增加(抗心绞痛作用)以及相同运动期间ST段压低的减少(抗缺血作用)来判断。普多洛尔的抗心绞痛作用在30分钟后开始,2小时后达到峰值,并在6小时后仍保持。在所有研究期间,其作用比普萘洛尔更显著。普多洛尔的抗缺血作用与抗心绞痛作用相似,且与变时作用无关。患者对普多洛尔耐受性良好。因此,单次服用40mg和80mg的普多洛尔产生了抗心绞痛和抗缺血作用,其作用与普萘洛尔相似。(摘要截选至250字)

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