Cardiovascular disease has been the leading cause of morbidity and mortality in American women; yet, until recently, there was no mandate to specifically include women in clinical trials of the major cardiovascular drugs. Despite new regulations, there is still a lack of readily available data for the clinician to use when planning drug therapy for women, as many of the drugs in use today were developed and tested prior to the new regulations being in effect. The purpose of this article is to provide advanced practice nurses with the most current information on the use of cardiovascular drugs in women. Information on the unique biological features of women is first presented to provide background material for subsequent sections. This is followed by an explanation of pharmacokinetic processes in women to include information on absorption, distribution, and clearance of drugs. A brief review of the effects of the phases of the menstrual cycle on drug therapy is given and then issues related to the profound physiologic changes in pregnancy and subsequent effects on drug therapy are reviewed. An analysis of the strength of the available evidence on drug therapies in women from the major trials on acute coronary syndromes, heart failure, dyslipidemia, atrial fibrillation, and hypertension is provided. Finally, implications for practice, including recommendations for drug prescription, are summarized.