Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A single oral dosage of 100, 200 or 300 mg Epanolol or placebo was administered in a randomized double-blind, cross-over fashion to 12 patients with stable effort angina. Symptom limited bicycle ergometer tests were performed before and 2 and 8 hours after each drug administration. Spontaneous diurnal and day to day differences in exercise tolerance and related analyzed variables were not present; 48 hours after drug intake a carry-over effect of the previous Epanolol administration could not be demonstrated. At each dose level of Epanolol, 2 hours after drug intake, heart rate and rate pressure product at peak exercise fell while exercise duration rose significantly. After 8 hours these effects were less marked. No significant differences between the 3 dose levels were found. In the pooled data of the 3 Epanolol doses, systolic blood pressure at peak exercise and maximal ischemic ST segment depression during exercise were also significantly reduced after 2 hours, while total performed external work rose. The percentage increase in heart rate during exercise after Epanolol administration was similar to the control tests at lower exercise levels but was less marked during the later stages of the test. Heart rate after Epanolol intake was percentage wise more reduced at higher exercise levels. Plasma levels of Epanolol were lower 8 hours after drug administration than after 2 hours. There was no correlation between plasma levels of Epanolol and the observed changes of any of the exercise variables 2 hours after drug intake.
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PMID:Effects of a single oral administration of Epanolol on exercise tolerance in patients with stable effort angina pectoris. 167 94

Antiischemic effects of beta 1-blocking agents are based on intrinsic negative inotropic and chronotropic properties. Partial beta 1-agonistic activity, although useful in preserving cardiac function, may counteract such antiischemic properties by modulating the intrinsic negative cardiac effects of beta-blockade. To investigate the acute hemodynamic and antiischemic profile of epanolol, a cardioselective beta 1-antagonist and partial agonist, 20 patients with left coronary artery disease underwent two incremental atrial pacing tests, 45 minutes before (APST I) and 15 minutes after (APST II) 4 mg intravenous epanolol, administered over 5 minutes. Additional measurements were carried out at 1, 3, 5, 10, and 15 minutes after epanolol, at basal and fixed heart rates. Epanolol immediately reduced heart rate with a maximum of 10% at 15 minutes and decreased contractility (Vmax) by 7% (both p < .05), whereas cardiac output fell temporarily by 9% (p < .05). Other hemodynamic parameters did not change, except for a significant 11% reduction in myocardial oxygen demand. Despite comparable pacing conditions, both the double product and contractility decreased significantly less during APST II, resulting in a 17% lower myocardial oxygen consumption (p < .05). Myocardial ischemia was markedly reduced, indicated by normalization of lactate metabolism [lactate extraction 16 +/- 7% vs. -7 +/- 8% (APST I)], less ST depression (21%), and modulation of LV end-diastolic pressure postpacing (all p < .05 vs. APST I), whereas angina was absent or less in 14 patients. None of the patients reported an adverse effect. Thus, under resting conditions intravenous epanolol induces moderate, short-lasting negative chronotropic and inotropic effects, but does not alter cardiac pump function or vascular resistance, reflecting its additional beta 1-agonistic properties. Alternatively, during pacing it still reduces ischemia through negative inotropic effects and diminishes myocardial oxygen demand, reflecting its beta 1-antagonistic profile.
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PMID:Acute systemic and antiischemic effects of epanolol in patients with coronary artery disease. 791 33