Restless legs syndrome is a common neurological condition affecting a substantial portion of the population. It can be an idiopathic disorder, or one that is secondary to another cause. Given that the underlying pathophysiology of restless legs syndrome is not well understood, several drug classes have been studied for symptom control. While dopamine agonists have long been the mainstay of first-line treatment for restless legs syndrome, recently, the α2δ ligands have been increasingly used. These agents have proven both efficacious and safe in a number of clinical trials. Additionally, compared with the dopamine agonists, they have been associated with less augmentation, a phenomenon whereby symptoms emerge earlier in the day, become more severe, and may spread to areas of the body previously unaffected. Newer clinical guidelines for restless legs syndrome are increasingly recommending the α2δ ligands as a logical first-choice medication for patients needing drug therapy for symptom control.