Managing premenstrual symptoms at the most fundamental level necessitates careful consideration of female reproductive biology. Inhibiting ovulation using hormonal agents is a reasonable approach for reducing premenstrual symptoms, but the benefits of agents such as gonadotropin-releasing hormone agonists and the synthetic androgen danazol are largely offset by their adverse effects and costs. Combination oral contraceptives provide an alternative that is widely accepted by women experiencing premenstrual symptoms and by their physicians; and newer formulations with lower levels of estrogen and progestin, administered using a monthly regimen with a shortened pill-free interval, appear promising for alleviating patient distress from severe premenstrual symptoms.