Twenty-six patients with mild-to-moderate essential hypertension participated in a 6-week outpatient, multicenter, randomized, double-blind, placebo-controlled two-way crossover study to assess the hemodynamic effects of bisoprolol (20 mg QD) at steady state. Hemodynamic assessments included sitting blood pressure, heart rate, and left-ventricular ejection fraction by radionuclide ventriculography after 7 days of bisoprolol or placebo at trough (24 h post-dose) and peak (3 h post-dose) values. The group adjusted mean ejection fraction was not significantly different in patients receiving bisoprolol compared with the placebo group at either peak or trough measurements; in fact, means in patients taking bisoprolol were slightly higher than in the placebo group. No symptomatic hypotension was documented. Blood pressure, measured 24 hours after dosing, was significantly lower in those receiving bisoprolol when compared with the placebo group, by 7.7 mm Hg and 9 mm Hg for diastolic and systolic blood pressure, respectively. Similarly, mean values of heart rate were 10 beats/min lower in the bisoprolol patients than in the placebo group. Only headache and insomnia occurred as adverse events. Bisoprolol (20 mg QD) effectively lowered blood pressure over a 24-hour period without significantly reducing ejection fraction or causing adverse clinical or biochemical events.