Despite major advances in cardiac research over the past three decades, cardiovascular disease (CVD) still remains the leading cause of morbidity and mortality in women and men worldwide. However, a major challenge for health care providers is that the current guidelines for cardiovascular drug therapies do not consider the impact of sex in the development of treatment plan for optimizing therapies for women. Clinical research in recent years suggests significant pharmacological and pharmacokinetic differences between females and males which have been attributed in part to differences in body composition, plasma protein binding capacity, drug metabolism and excretion. Herein, we provide a comprehensive review regarding sex- specific differences and drugs commonly used for cardiovascular diseases in women and men. Understanding how sex related differences influence drug efficacy and cardiovascular disease outcomes is crucial for not only optimizing treatment strategies for women and men but to encourage the implementation of specific guidelines that address sex difference as a consideration for treatment of cardiovascular diseases.