Summary

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• Horizant (gabapentin enacarbil) is indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults and for the management of postherpetic neuralgia (PHN) in adults.
• This summary is based on the review of three systematic review(s)/meta-analysis(es). ^[1-3]
• Gabapentin, gabapentin enacarbil, and pregabalin are recommended as first-line treatments for Restless Legs Syndrome/Willis-Ekbom Disease (RLS/WED) due to their significant efficacy in reducing symptoms and low occurrence of augmentation, with cabergoline showing the greatest reduction in IRLS scores (MD -11.98).
• Gabapentin enacarbil offers consistent and predictable pharmacokinetics with low interindividual variability in bioavailability, contributing to its effectiveness in treating RLS/WED, particularly in patients with primary RLS and those with comorbid insomnia, chronic pain syndromes, impulse control disorders, and anxiety.
• Iron supplements are effective in alleviating RLS symptoms in patients with iron deficiency but not in those with normal serum ferritin levels; oxycodone-naloxone is recommended for severe RLS cases unresponsive to first-line treatments like gabapentin enacarbil. 6. α2δ ligands, including gabapentin enacarbil, are generally safe for treating RLS/WED, with good tolerability and a low risk of augmentation. Common adverse effects include nausea, somnolence, fatigue, headache, and nasopharyngitis.
• Gabapentin, gabapentin enacarbil, and pregabalin demonstrate a favorable safety profile with good tolerability, comparable to dopamine agonists, though dopamine agonists are less favored due to the risk of augmentation.
• There is no population types or subgroups information available in the reviewed studies.