We retrospectively evaluated the effect, timing and safety of different pharmacological strategies during 64-slice CT coronary angiography (CT-CA). From the institutional database of CT-CAwe enrolled 560 consecutive patients with suspected coronary artery disease. The type of drug preparation (group 1 = no treatment; group 2 = oral metoprolol; group 3 = other; group 4 = intravenous (IV) atenolol; group 5 = IV atenolol + nitrates; NR = non-responders), timing, and adverse effects were recorded. Heart rate (HR) during different preparation phases was recorded. Four adverse effects were recorded, none of which was attributable to pharmacological treatment. In all groups, except group 1, the HR on arrival was significantly reduced by the pharmacological treatment (p<0.01). Group 4 showed the best (-16±8 bpm) HR reduction. There was no significant effect on HR due to nitrates (p = 0.49), while a slight increase due to contrast material was noted (p<0.05). Average time required for preparation was 44±25min. Groups 4 and 5 showed the most effective timing (8±9 min and 8±8 min, respectively; p<0.01). Pharmacological preparation in patients undergoing CT-CA is safe and effective. Best results in terms of HR reduction and fast preparation are obtained with IV administration of beta-blockers.