Percutaneous transluminal coronary angioplasty (PTCA) is one of the effective interventions for treating atheroclerotic corona ry heart disease. However, myocardial ischemia caused by balloon dilation during the operation has raised great concern. As a result, administration of drugs an d mechanical measures have been employed perioperatively to protect the cardiac muscle so as to prevent or reduce the myocardial ischemia and ensure the safety of the operation. This paper reviews the significance and methodology of pharmac ological myocardial protection during PTCA.