Left ventricular hypertrophy (LVH) dramatically worsens hypertensive illness. Because the genesis of LVH appears to be multifactorial, antihypertensive treatment should aim to reduce not only pressor values but also the hypertrophic ventricular mass. This result can be obtained only when drugs able to act on both pathogenetic factors are used. To evaluate the effectiveness of antihypertensive therapy on regression of LVH, 21 patients with stage 2 essential hypertension were treated for a year with either atenolol (120 mg/d orally), a cardioselective beta-blocker without intrinsic sympathomimetic activity, or ramipril (5 mg/d orally), an angiotensin-converting enzyme inhibitor with high tissue activity. Both treatments produced significant control of hypertension and regression of LVH. No statistically significant difference between treatments was noted, except for heart rate, which was substantially unchanged by ramipril but significantly decreased by atenolol. Both drugs were well tolerated. Atenolol and ramipril have a major role in the long-term treatment of hypertension and in the regression of hypertension-associated LVH.