Comparative Anti-Hypertensive Effectiveness of β-Adrenoreceptor Antagonists with Different Pharmacological Properties: Dose—Response Studies during Acute and Chronic Administration (original) (raw)
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British Journal of Clinical Pharmacology, 2010
At rest, both b-ARB reduced brachial but not central SBP (compared with placebo). During exercise, b-ARB reduced brachial SBP (reductions of 19.9 Ϯ 4.3 mmHg and 23.2 Ϯ 2.7 mmHg for propranolol and bisoprolol, respectively, at 100 W, each P < 0.0001) but not central SBP. The difference between peripheral and central SBP was reduced, relative to that during placebo, by 21.5 mmHg (95% confidence interval 8.8, 34.1) and 26.4 mmHg (18.1, 34.8) for propranolol and bisoprolol, respectively, at 100 W (each P < 0.01). There was no significant effect of b-ARB on diastolic blood pressure or peripheral vascular resistance.
Comparison of antihypertensive activity of beta-blocking drugs during chronic treatment
BMJ, 1976
The hypotensive activity of five beta-adrenoceptor antagonists with different ancillary pharmacological properties was compared in a randomised double-blind factorial trial in 25 untreated patients with stable, uncomplicated, essential hypertension. In doses that produced similar reductions in exercise tachycardia all drugs had similar blood-pressure lowering activity, greater on systolic than diastolic pressure and greatest during exercise. With the exception of vasodilator activity the possession of any particular combination of ancillary pharmacological properties did not significantly influence the specific antihypertensive activity of these compounds.
Journal of the American College of Cardiology, 1985
The ability of cardioselective and nonselective beta-adrenoceptor blocking drugs, with and without partial agonist activity, to control increases in blood pressure associated with mental and physical activity was compared in 3S subJects with hypertension. Direct measurements of blood pressure and radioenzymatic determinations of plasma norepinephrine were obtained before, during and after four activities, and were repeated after random allocation to treatment with atenolol, metoprolol, pindolol or propranolol. Cardioselective and nonselective drugs modestly reduced the pressor response to reaction time testing, but not to mental arithmetic or isometric exercise. The increase in systolic blood pressure during bicycling was attenuated significantly by the cardioselective drugs atenolol (by 23 mm Hg, or 38%) and metoprolol (21 mm Cardioselective and nonselective beta-adrenoceptor blocking agents are equally effective in lowering the blood pressure at rest of subjects with hypertension (1,2). Differences in the antihypertensive potential of these drugs may be difficult to detect under rest conditions, however, but emerge with sympathoadrenal activation because nonselective betablocking drugs favor vasoconstriction in the presence of circulating epinephrine by inhibiting betarmediated vaso-From the
Blood pressure and catecholamines following exercise during selective beta-blockade in hypertension
European Journal of Clinical Pharmacology, 1986
This study examines and compares the hemodynamic and sympathoadrenal response to bicycle exercise in hypertensive subjects during two weeks' treatment with a cardio-selective (metoprolol) and nonselective (propranolol) beta-blocker. The increase in plasma norepinephrine and epinephrine concentration following exercise was augmented to a similar degree with each beta-blocker. Pre-exercise blood pressure and heart rate were similar for the two drugs. However immediately after exercise and particularly after resting for 20 min post exercise, diastolic blood pressure was lower during metoprolol treatment. Systolic blood pressure was also lower 20 min post exercise during metoprolol treatment. These observations indicate that cardio-selective beta-blockers offer advantages in blood pressure control during exercise through intact vascular fl2-adrenoceptors opposing sympathetically mediated vasoconstriction.
British Journal of Clinical Pharmacology, 1988
The effects of atenolol administration on maximal exercise capacity and exercise haemodynamics have been compared in eight normotensive and eight mildly hypertensive subjects, matched for sex, age, body weight, and maximal oxygen uptake, and familiar with maximal exercise testing. 2 Supine and exercise blood pressure, and exercise total peripheral resistance were significantly higher, and exercise cardiac output was significantly lower in the hypertensive than in the normotensive subjects. 3 Administration of atenolol (1 x 100 mg day-') for 3 days reduced supine and exercise systolic blood pressure, heart rate, and cardiac output, and increased exercise stroke volume. Supine and exercise diastolic blood pressure and exercise total peripheral resistance were unaffected by atenolol. The effects of atenolol did not differ in the normotensive and the hypertensive subjects. 4 Maximal work load, maximal oxygen uptake, and maximal heart rate were reduced to a similar extent in normotensive and hypertensive subjects during atenolol treatment. 5 It is concluded that there is no difference in the effects of short-term atenolol administration on exercise haemodynamics and maximal exercise capacity in normotensive and mildly hypertensive subjects.
American Journal of Hypertension, 1995
The effect of different antihypertensive drugs on the increased surface J3,-adrenoceptor density in essential hypertension was evaluated to elucidate whether the possible effect of the treatment on these receptors was secondary to blood pressure decreases or a specific effect of the drugs. Thirtynine untreated essential hypertensive patients and 28 normotensive control subjects were studied in basal conditions. Hypertensive patients were randomly assigned to three treatment groups: biso-pro101 (10 mg/day, n = 151, enalapril (20 mg/day, n = 12), and verapamil SR (240 mg/day, n = 121, and were studied before and after 1 month of treatment. Plasma catecholamines were determined by a radioenzymatic assay. Surface P,-adrenoceptors were measured in intact lymphocytes by radioligand binding assay using the hydrophilic ligand [3Hl-CGP12177. Pa-adrenoceptor density was increased in hypertensive patients (P < .Ol). After treatment, mean blood pressure decreased similarly in the three groups, while plasma catecholamines showed no significant changes in any group. J3,-adrenoceptor
British Journal of Pharmacology, 1992
SK&F 104856 (2‐vinyl‐7‐chloro‐3,4,5,6‐tetrahydro‐4‐methylthieno[4,3,2ef][3]benzazepine) is a novel postjunctional α.1‐ and α.2‐adrenoceptor antagonist. SK&F 104856 as well as prazosin and SK&F 86466 reduced blood pressure in the anaesthetized normotensive dog. SK&F 86466 and rauwolscine but not SK&F 104856 or prazosin, produced a marked increase in myocardial contractility which corresponds with their ability to block prejunctional α.2‐adrenoceptors. Intravenous or oral administration of SK&F 104856 resulted in dose‐dependent antihypertensive responses in 1‐kidney, 1‐clip (1‐K, 1‐C) Goldblatt hypertensive dogs with baseline blood pressure of approximately 140 mmHg. At 0.1 and 1 mg kg−1, i.v., mean arterial blood pressure fell by 11 ± 5 and 23 ± 5 mmHg, respectively. At 3 and 10 mg kg−1, p.o., blood pressure fell by 9 ± 3 and 22 ± 5 mmHg, respectively. At 10 mg kg−1, p.o., the antihypertensive effect of SK&F 104856 was still evident at 4 h. The data indicate that SK&F 104856 shows se...