Epanolol

Abstract: Beta blockade constitutes efficient therapy for stable angina pectoris. The effects of lowering blood pressure and heart rate with such treatment are not always desired. Epanolol is a beta 1-selective partial agonist with minor effects on blood pressure and heart rate at rest. Atenolol is a pure beta 1-selective antagonist with more pronounced effects on blood pressure and heart rate at rest. The effects of epanolol, 200 mg o.d., and atenolol, 100 mg o.d., were compared in 173 middle-aged patients with stable angina pectoris in a randomized, double-blind, parallel group-controlled study for one year. No significant differences were shown in angina attack rate, nitrate consumption, or exercise performance. Resting heart rate and blood pressure were significantly lower on atenolol. Epanolol tended to be better tolerated than atenolol, as shown by visual analogue scales of well-being, activity, energy, and warm extremities, further supported by fewer reports on possible adverse reactions. In conclusion, epanolol appears to be as effective as atenolol and better tolerated in patients with stable angina pectoris.

Abstract: The efficacy of epanolol vs. metoprolol in stable angina pectoris was compared in 114 patients recruited to a randomized double-blind cross-over study, consisting of a 4-week period on each drug. Epanolol (200 mg) or metoprolol (200 mg) was administered daily. Bicycle ergometry was performed at the end of each treatment period. The maximum workload was 134 +/- 18 W on epanolol and 133 +/- 37 W on metoprolol (NS). Values for resting heart rate (epanolol, 72 +/- 11 beats min-1; metoprolol, 64 +/- 12 beats min-1; P less than 0.001), systolic blood pressure (epanolol, 143 +/- 21 mmHg; metoprolol, 137 +/- 21 mmHg; P less than 0.05) and diastolic blood pressure (epanolol, 88 +/- 10 mmHg; metoprolol, 84 +/- 11 mmHg; P less than 0.01) were all higher on epanolol treatment. During exercise, the increase in heart rate and blood pressure was of similar magnitude during the two treatment periods, and these parameters did not differ significantly at the last identical workload. The rating of chest pain, fatigue and dyspnoea did not differ between the two drugs during submaximal or maximal exercise. In conclusion, 200 mg of epanolol and metoprolol have similar efficacy with regard to exercise tolerance. As expected from the partial agonist activity present in epanolol but not in metoprolol, the former drug resulted in a higher heart rate and blood pressure at rest. The observed increase in these parameters during exercise was similar for both drugs.

Abstract: Hypertension is due to disturbance of the complex interplay between numerous known and unknown mechanisms that normally control blood pressure. Antihypertensive agents may, therefore, reduce blood pressure through widely different actions and, at the same time, elicit counterregulatory responses. This is a review of the long-term hemodynamic effects at rest as well as during exercise of nine relatively new antihypertensive compounds: a beta-blocker (epanolol), an alpha-receptor blocker (doxazosin), two double-acting compounds (dilevalol and carvedilol), three calcium antagonists (amlodipine, felodipine, and diltiazem), an angiotensin-converting enzyme inhibitor (lisinopril), a serotonin antagonist (ketanserin), and low-salt diet as a nonpharmacological treatment in 171 patients with mild to moderate essential hypertension. The results in the treatment groups are compared to the hemodynamic changes seen in 28 hypertensive patients left untreated for 10 years. The patient populations of the different groups were comparable. The invasive hemodynamic technique, including intraarterial blood pressure recording and measurements of cardiac output by Cardigreen, was the same in all studies. While blood pressure remained nearly unchanged in the untreated group, all antihypertensive compounds induced significant and sustained blood pressure reduction both at rest and during exercise. The modest reduction (3–5%) in blood pressure during a low-salt diet was also statistically significant. This review shows the multiplicity of the long-term hemodynamic changes, ranging from a reduction in cardiac output to peripheral vasodilatation, during chronic antihypertensive therapy. In untreated hypertensives, the cardiac output is reduced by 1–2% per year and total peripheral resistance is increased by 2–3% per year. The review also focuses on counterregulatory responses that modify the initial reduction in blood pressure after drug treatment for hypertension. It is concluded that proper understanding of the hemodynamic effects of antihypertensive agents is useful in the selection of the right treatment for specific groups of hypertensive patients.

Abstract: This double-blind, randomized parallel group study investigated the effect of 6 months β-adrenoceptor antagonist therapy with either metoprolol (β1-selective without intrinsic sympathomimetic activity [ISA]) or epanolol (β1-selective with ISA) on markers of endogenous fibrinolysis in 20 patients with chronic stable angina receiving concurrent treatment with nifedipine.