Gabapentin Enacarbil: Pharmacotherapy of Restless Legs Syndrome

Restless Legs Syndrome (RLS) is a prevalent sleep-associated movement disorder greatly affecting patients’ quality of life (QoL). Several drugs can be used to control this condition although the first-line dopamine agents often cause adverse effects. Non-dopaminergic drugs such as oral gabapentin (GBP) have been more recently advocated. Despite ameliorating RLS symptoms, GBP’s pharmacokinetic limitations restrict its overall effectiveness. A novel specifically designed prodrug, gabapentin enacarbil (GE), has demonstrated successful RLS alleviation with a superior pharmacokinetic profile. This review aims to examine the efficacy and tolerability of both GBP and GE as pharmacotherapy for RLS. Despite some heterogeneity and limitations across research methodologies, GE appears to be a potential RLS therapy superior to GBP and other dopaminergic agents.