Gabapentin enacarbil for the treatment of restless legs syndrome (RLS).

Abstract

INTRODUCTION:

Gabapentin enacarbil is a new treatment for restless legs syndrome (RLS). It is a prodrug of the anticonvulsant gabapentin. However, unlike gabapentin, gabapentin enacarbil does not demonstrate saturable absorption. This allows for once-daily dosing and less variability in serum levels.

AREAS COVERED:

This review focuses on therapies used to treat RLS, both historical and recent. Data from available trials are summarized, with a particular focus on the efficacy and safety of gabapentin enacarbil. Potential advantages and disadvantages of this therapy in comparison with other RLS treatment modalities are discussed.

EXPERT OPINION:

Placebo-controlled trials of gabapentin enacarbil demonstrate considerable efficacy in the treatment of RLS. However, head-to-head trials comparing gabapentin enacarbil with other medications used in the treatment of RLS, including gabapentin, are lacking. Potential advantages with gabapentin enacarbil related to its pharmacokinetic profile are thus difficult to ascertain. Efficacy of gabapentin enacarbil appears comparable with that of the dopamine agonists, long considered the therapy of choice in patients with RLS. Given the lack of direct-comparison trials, and the significant cost differential of gabapentin enacarbil versus established therapies, the drug is likely to be used for patients who have failed other medication trials, or those who experience prolonged symptoms and prefer once-daily dosing.

• Authors: Rachel A Burke, Michele A Faulkner
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 12 Issue 18 Pg. 2905-14 (Dec 2011) ISSN: 1744-7666 [Electronic] England
• PMID: 22077768 (Publication Type: Journal Article, Review)

Chemical References

• 1-(((alpha-isobutanoyloxyethoxy)carbonyl)aminomethyl)-1-cyclohexaneacetic acid
• CACNA2D1 protein, human
• Calcium Channels
• Carbamates
• gamma-Aminobutyric Acid

Topics

• Administration, Oral
• Calcium Channels (metabolism)
• Carbamates (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
• Clinical Trials as Topic
• Humans
• Molecular Structure
• Protein Binding
• Restless Legs Syndrome (drug therapy, etiology, metabolism)
• Treatment Outcome
• gamma-Aminobutyric Acid (administration & dosage, adverse effects, analogs & derivatives, pharmacokinetics, therapeutic use)