The proper use of antiplatelet agents in the cardiac catheterization laboratory is important for ensuring optimal results in patients undergoing percutaneous revascularization. Understanding the mechanisms by which these drugs exerts their effects is important for both interventional and non-interventional cardiologists. The effects of these agents on platelet function can be assessed and monitored using a variety of commercially available laboratory assays but so far these tests have not been adopted in routine clinical practice. Currently, aspirin, thienopyridines and glycoprotein IIb/IIIa inhibitors are the primary types of antiplatelet drugs being utilized. The use of these drugs and of several newer antiplatelet drugs in the treatment of patients undergoing percutaneous revascularization in the cardiac catheterization laboratory will be discussed, especially in the light of the recently published guidelines.