Acute myocardial infarction (MI) remains a significant problem in terms of morbidity, mortality and healthcare costs. Pharmacologic reperfusion therapies for MI are becoming increasingly complex. This review therefore places contemporary pharmacologic MI developments into perspective. An historical overview of pharmacologic reperfusion therapy for MI is provided, followed by an analysis of current limitations, treatment options, and present and likely future pharmacologic therapies. Adjunctive percutaneous and other treatments are also discussed, to clarify what is becoming a rapidly changing field.