Doxazosin, a quinazoline derivative, is a selective alpha 1-inhibitor that reduces calculated coronary heart disease risk by lowering blood pressure while favorably affecting blood lipid levels. The aim of this study was to compare the efficacy and toleration of doxazosin with atenolol, one of the most frequently used cardioselective beta-blockers in Italy. Forty patients with mild-to-moderate hypertension were treated with either atenolol (100 mg) or doxazosin (mean dose, 3.3 mg) once daily for 8 weeks. Both drugs significantly reduced supine and standing systolic and diastolic blood pressures. Atenolol induced marked bradycardia, whereas doxazosin had very little effect on heart rate. Doxazosin produced a favorable effect on blood lipid levels by decreasing triglyceride and total cholesterol levels and increasing high-density lipoprotein cholesterol and high-density lipoprotein total cholesterol ratio. Atenolol had exactly the opposite effect on blood lipid levels. Both drugs had equivalent toleration profiles. It was concluded that doxazosin was as effective as atenolol in reducing elevated supine and standing blood pressures. In addition, doxazosin had a beneficial effect on lipid profiles and minimal effect on heart rate. Therefore doxazosin may reduce calculated coronary heart disease risk in hypertensive patients.