Polycystic ovary syndrome (PCOS) is a multifaceted disorder that affects between 5% and 8% of women. As a syndrome, PCOS is comprised of reproductive, metabolic, and cardiovascular components. Hyperandrogenemia and hyperinsulinemia are central to the pathogenesis of PCOS and thus typically serve as the targets for treatment. The spectrum of therapeutic options is broad and ranges from lifestyle intervention to specific pharmacologic agents. This chapter details current pharmacologic treatments for women with PCOS using a symptom-specific approach with a special focus on the metabolic effects of each treatment. Generally, oligomenorrhea mandates regulation of menstrual cyclicity and protection of the endometrium against the development of dysplasia and carcinoma. Progestins, either alone or in combination with estrogen (in the form of an oral contraceptive) are the mainstay of treatment of oligomenorrhea. Insulin lowering therapies also improve menstrual regularity. When androgen excess is the main target for therapy, an antiandrogen and/or oral contraceptives is typically chosen. Metabolic concerns of PCOS include excess body weight and insulin resistance. Metformin and thiazolidenediones both improve hyperinsulinemia but their differential effects on body weight must be considered.