We discuss the rationale of the pharmacological approaches to pathological gambling and review the current status of drug treatments in this area. Specifically, we summarize the treatment study results of serotonin reuptake inhibitors, mood stabilizers, and opioid antagonists in pathological gambling. We also briefly describe the animal and human studies of other pharmacologic agents that show future promise in treating this disorder. Finally, we discuss a research agenda to be addressed in future drug treatment studies in pathological gambling.