Recent advances in the understanding of the pathogenesis of premenstrual syndrome (PMS) have allowed the development of appropriate pharmacological interventions. Although at the present time there are no approved medications for this indication in the US, several well-designed studies have been conducted that guide the clinician's treatment of PMS. As a result, less-proven nonpharmacological modalities, such as dietary modification, exercise regimens and psychotherapy, are more quickly supplanted by the use of medication. Three classes of agents have been proven efficacious and are widely used to treat the disorder. These include benzodiazepines (especially alprazolam), selective serotonin reuptake inhibitors (especially fluoxetine), and gonadotropin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH)] agonists. In addition to these medications which are used to treat the generalised syndrome of PMS, a variety of other drugs are used in the treatment of specific aspects of this disorder. Despite the success of these treatments, each has a substantial adverse effect profile which modulates their use in some patients. Knowledge of these potential adverse effects and their management should help optimise therapy. In addition, a variety of less well-proven pharmacological remedies are commonly in use. The adverse effects of these medications may well outweigh their benefits.