Disease relevance of Epanolol

• The effects of epanolol (a new selective beta-adrenoceptor antagonist), diltiazem and placebo were compared in a group of 16 patients with chronic stable angina pectoris [1].
• Evidence is available which shows that attenuation of the tachycardia of exercise persists for 24 hours after a single dose of epanolol 200mg, a dose which retains selectivity for the beta 1-adrenoceptor [2].
• A tolerability questionnaire comprising 43 questions and covering 7 different body systems showed that epanolol had a better profile than nifedipine for the following 7 side effects: poor sleep, abdominal pain, flushing, swollen ankles, palpitations, headache and a general feeling of being unwell [3].
• 1 Eight men with primary hypertension were treated for 3 weeks with placebo, epanolol (200 mg or 400 mg), or atenolol 100 mg in a randomised cross-over study [4].
• Post-exercise hypotension: the effects of epanolol or atenolol on some hormonal and cardiovascular variables in hypertensive men [4].

High impact information on Epanolol

• The pharmacodynamic consequences in man of the degree of agonist activity possessed by the beta 1-selective partial agonist epanolol include little reductions at rest in heart rate, blood pressure, various measures of cardiac haemodynamic parameters, peripheral blood flow and renal function [2].
• The mean heart rate during 24 hours was significantly lower with metoprolol compared with epanolol treatment (64 vs 72 beats/min, respectively, p less than 0.001) [5].
• Pharmacokinetics of epanolol (ICI 141,292) in healthy young volunteers and comparative data in elderly patients with angina and subjects with renal or hepatic impairment [6].
• Clinical pharmacology of epanolol. Pharmacodynamic aspects [2].
• The bioavailability of epanolol for the tablet and solution administered to fasted volunteers was similar (7-8%), but it was about 25% lower when administered as a tablet with food [6].

Chemical compound and disease context of Epanolol

• This questionnaire was used in a Swedish subsample (n = 211) of the epanolol versus metoprolol study in patients with stable angina pectoris (VISA 1) [7].
• 3 The reduction of exercise-induced tachycardia by epanolol 400 mg was comparable to that of atenolol [4].
• Long-term hemodynamic effects at rest and during exercise of newer antihypertensive agents and salt restriction in essential hypertension: review of epanolol, doxazosin, amlodipine, felodipine, diltiazem, lisinopril, dilevalol, carvedilol, and ketanserin [8].
• The pharmacokinetic profile of a single dose of 100 mg of (+/-)-N-[2-[[3-(o-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]- 2-(p-hydroxyphenyl) acetamide (epanolol, Visacor), has been determined in an open study of 15 elderly patients with stable angina pectoris [9].

Biological context of Epanolol

• 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) [10].
• 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 [10].
• 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 [11].

Anatomical context of Epanolol

• Acute systemic and antiischemic effects of epanolol in patients with coronary artery disease [10].
• The effect of epanolol on intra-arterial ambulatory blood pressure and baroreceptor heart rate reflex in essential hypertension [12].

Associations of Epanolol with other chemical compounds

• During the 'sleeping' period (23.00 h-08.00 h) heart rate was significantly increased by pindolol, lowered with atenolol and unaffected on epanolol [13].
• Peak heart rate (mean and 95% confidence intervals) was lower (P < 0.05) with epanolol (121 (115-130) beats min-1) than with diltiazem (137 (126-148) beats min-1) or placebo (141 (130-152) beats min-1) [14].
• Heart rate during the 'waking' period (14.00-23.00 h) was lower than placebo after epanolol and atenolol but unaffected by pindolol [13].
• A comparison of epanolol and nifedipine in stable angina patients: results of a multicentre trial [15].

Gene context of Epanolol

• The long-term effects of metoprolol and epanolol on tissue-type plasminogen activator and plasminogen activator inhibitor 1 in patients with ischaemic heart disease [16].
• ANP did not change from resting values with placebo or diltiazem, but rose significantly (P < 0.05) with epanolol from 19.7 (13.0-29.8) pg ml-1 (geometric mean and 95% confidence intervals) during supine rest to 49.6 (33.7-73.0) pg ml-1 at peak exercise [14].
• 5. The exercise-induced rise in PRA was suppressed by atenolol but not by epanolol [17].
• There was no change in SAB/HR reflex set point, sensitivity or latency with epanolol [12].

Analytical, diagnostic and therapeutic context of Epanolol

• Single doses of epanolol (ICI 141,292) were administered to 12 healthy young male volunteers in a randomised crossover study [6].
• Urinary recovery of epanolol was about 25% of the administered intravenous dose, but recoveries were much lower (about 1%) following oral administration [6].
• The concentrations of epanolol in plasma were determined by use of a radio-immunoassay technique, whereas those in urine samples were measured by a high pressure liquid chromatographic (HPLC) method [6].
• Effects of epanolol and metoprolol on the heart measured by 24-hour holter monitoring [5].
• Epanolol as a model for assessing patient preference in anti-anginal drug therapy [18].

References