Treatment of hypertension with beta-adrenergic blockers (BB) slightly increases plasma triglycerides and decreases high density lipoprotein (HDL) cholesterol levels. However, only little is known about BB-related lipid changes in patients with coronary artery disease (CAD), who usually a priori have decreased HDL cholesterol levels; and even less data exist on HDL subfraction cholesterol in these patients. We therefore quantified levels of lipids, lipoprotein lipids including HDL2 and HDL3 cholesterol, and apolipoproteins in 107 consecutive men undergoing elective coronary angiography. Of the 107 patients, 84 had angiographically established coronary atherosclerosis (>or=1 lesion with >or=50% narrowing, CAD+), and 23 had no major lesion (CAD-); 67 were taking ss1-selective BB (metoprolol or atenolol) for treatment of angina and/or hypertension and 40 were not. Patients using BB had significantly higher cholesterol levels than patients not using BB (5.99 +/- 0.93 vs. 5.63 +/- 1.07 mmol/l, mean +/- SD, p = 0.029). Their HDL cholesterol and HDL2 cholesterol levels were significantly lower (1.19 +/- 0.27 vs. 1.28 +/- 0.33 mmol/l, p = 0.048, and 0.22 +/- 0.12 vs. 0.27 +/- 0.18 mmol/l, p = 0.038, respectively). Accordingly, the total cholesterol/HDL cholesterol ratio was significantly higher in patients taking BB than in those not taking BB (5.23 +/- 1.27 vs. 4.68 +/- 1.63, p = 0.010). Considering CAD+ and CAD- patients separately, there was a trend towards lower HDL cholesterol and its subfractions with significantly lower HDL2 cholesterol in patients with BB in the CAD- group, suggesting a stronger dyslipidemic effect of BB in these patients with a priori normal or near normal baseline lipid levels.