[The relationship between the isosorbide-5-mononitrate concentration and its antianginal effect following the administration of regular and prolonged-action drug forms in patients with stenocardia of effort]. / Sviaz' mezhdu kontsentratsiei izosorbid-5-mononitrata i antianginal'nym éffektom posle priema obychnoi i prolongirovannoi lekarstvennykh form u bol'nykh stenokardiei napriazheniia.

Isosorbide-5-mononitrate (IMN) concentration-antianginal effect relationships were studied in 14 coronary heart diseases patients with stable exertion-induced angina after administration of Efox (Schwarz-Pharma) as two dosage forms: routinely acting tablets (20 mg) and long-acting capsules (50 mg). The antianginal effect index was an increase of treadmill exercise duration (sec) as compared with placebo, the concentration and effect were measured in points 0, 1, 3, and 7 hours after administration, in some patients, investigations were conducted 12 and 24 hours. The two formulations were found to be highly effective drugs whose action lasted 7 hours, by that time the effect of the tablets substantially decreased, which was associated with decreases in drug concentrations. The efficiency of the capsules at this point was significantly higher than that of the tablets. The use of the capsules resulted in tachyphylaxis--rapid decreasing responses to IMN. Following 7 hours of their administration there is a significant decrease in their effect with an increase in IMN concentrations.

[The efficacy of proxodolol, a new beta-adrenoblockader with alpha-adrenoblockader properties, in its single use in patients with stable stenocardia of effort]. / Izuchenie éffektivnosti proksodolola, novogo beta-adrenoblokatora so svoistvami al'fa-adrenoblokatora, pri odnokratnom primenenii u bol'nykh so stabil'noi stenokardiei napriazheniia.

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)

[Does captopril produce an antianginal effect in patients with stable exercise-induced angina pectoris?]. / Okazyvaet li kaptopril antianginal'noe deistvie u bol'nykh so stabil'noi stenokardiei napriazheniia?

Captopril (C), isosorbide dinitrate (ID), and nifedipine (N) were evaluated for antianginal effects (AAE) in 12 patients with ischemic heart disease. The effects were assessed by treadmill exercise tests performed before and repeatedly 1, 2, 3, and 6 hours after the single dose of a drug or placebo. C, ID, and N were given in doses of 50, 10, and 20 mg, respectively. The drugs were equally effective in lowering systolic blood pressure at rest. Unlike ID and N, C failed to affect the duration of exercise testing until an anginal episode occurred and the magnitude of ST-segment depression at the same exercise intensity. ID and N caused a significant increase in the duration of exercise and a decrease in ST-segment depression during exercise 1-3 h later. An individual analysis has shown that C, ID, and N produced an antianginal effect only in 2, 9, and 10 patients, respectively. Thus, C is unable to show a substantial antianginal effect.