High levels of activity of the renin-angiotensin system (RAS) and sympathetic nervous system (SNS) are related to left ventricular hypertrophy (LVH). A percentage of subjects with hyperactivity to treadmill stress test show LVH to echocardiogram. This paper aims at evaluating neurohumoral influence over these subjects by comparing drugs that block both the RAS and the SNS. In a 1-year open protocol, 195 normotensive subjects, with hyperactivity to treadmill stress test and LVH, were randomly assigned to supervised physical exercise, rilmenidine 1 mg day À1 , atenolol 50 mg day À1 , enalapril 10 mg day À1 or losartan 50 mg day À1 . Changes in left ventricular mass index (LVMI), measured by means of echocardiogram, were the primary end point. Changes in systolic blood pressure (SBP) at rest and peak effort were also evaluated. Enalapril significantly brought LVMI down in relation to the basal value (28.2%; n ¼ 36) similarly to losartan (26.9%; n ¼ 42); P40.05. However, both were more efficient than physical exercise (2.9%; n ¼ 39), rilmenidine (5.1%; n ¼ 38) and atenolol (7.2%; n ¼ 40); Po0.001. There was no significant difference in SBP reduction at rest and peak effort in groups assigned to atenolol, enalapril and losartan; P40.05. In such groups, reduction was greater than in groups assigned to physical exercise and rimenidine; Po0.001. In conclusion, drugs that block RAS were more efficient in reducing LVH than physical exercise and drugs that block SNS, and such reduction took place regardless of SBP level reduction at rest and peak effort.