Pathologic gambling (PG) is an impulse control disorder according to Diagnostic and Statistical Manual of Mental Disorders that bridges impulsive, compulsive, and addictive behaviors. This review article discusses the pharmacotherapy of gambling between the age groups of 16 and 65. PG is a relatively common disorder, but there is only limited information available regarding the effectiveness of pharmacotherapy for this illness. The role and effectiveness of various medications including antipsychotics, mood stabilizers, opioid antagonists, and other pharmacological agents are reviewed in this article. Neurobiological research has shown the involvement of serotonergic, dopaminergic, and opioid dysfunction in PG, and particular attention is given to the role of genetics and neurophysiology.