The acute efficacy of rapid loading of oral long-acting enalapril in congestive heart failure remains to be established. We evaluated the efficacy of this treatment modality in 22 patients with chronic congestive heart failure N.Y.H.A. functional class ranging from II-IV with Creatinine level less than 2 mg/dl. Following hemodynamic evaluation, there was significant favorable change in the left ventricular functional curve. Moreover, acute hemodynamic assessment showed a significant reduction in pulmonary capillary wedge pressure from 19.2 +/- 4.8 to 17.2 +/- 4.7 mmHg (p less than 0.005) and an increases in stroke volume index from 28.3 +/- 9.2 to 33.1 +/- 7.5 ml/m (p less than 0.005). After rapid enalaprilization, blood pressure fell from 127 +/- 21/78 +/- 15 to 108 +/- 21/68 +/- 15 mmHg (p less than 0.005), systemic vascular resistance from 1725 +/- 602 to 1370 +/- 376 dyne.sec.cm-5 (p less than 0.05) and pulmonary vascular resistance from 262 +/- 19 to 218 +/- 65 dyne.sec.cm-5 (p less than 0.05). Cardiac index rose significantly from 2.43 +/- 0.62 to 2.60 +/- 0.50 l/min/m2 (p less than 0.05). In terms of neurohumoral assessments, there was a significant inhibition of the renin-angiotensin-aldosterone system. Aldosterone fell from 21.3 +/- 13.4 to 9.4 +/- 8.0 ng/dl and plasma renin activity rose from 3.3 +/- 4.6 to 11.3 +/- 11.0 ng/nl/hr (p less than 0.005). Plasma norepinephrine and epinephrine levels were found to have significant reduction in addition to antidiuretic hormone concentration. During short-term trial, left ventricular ejection fraction was significantly elevated from 27.5 +/- 6% to 32.8 +/- 10.8% (p less than 0.005). Thus, this limited study clearly demonstrates the rapid administration of enalapril not only achieves inhibition of renin-angiotensin-aldosterone system but also reduces preload and afterload significantly in the failing heart. We conclude that rapid enalaprilization is an effective methodology which still needs meticulous attention, providing significant hemodynamic and symptomatic benefits in patients with chronic congestive heart failure.