Gabapentin enacarbil

(Horizant®)

Horizant®

Drug updated on 4/10/2024

Dosage FormTablet (oral; 300 mg, 600 mg)
Drug ClassGamma-aminobutyric acid analogs
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • For the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults.
  • For the management of postherpetic neuralgia (PHN) in adults.

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Summary
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  • Gabapentin enacarbil (Horizant) is indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults and for the management of postherpetic neuralgia (PHN). It has been highlighted for its safety, efficacy, and advantages over other treatments such as gabapentin due to its linear kinetics.
  • Three studies provided unique insights into Horizant's pharmacological profile, absorption, bioavailability, and comparative analysis with other RLS treatments.
  • The first study emphasized that gabapentin enacarbil offers an advantage over drugs like gabapentin, which do not share this property. It also noted a low risk of augmentation with this drug compared to others used in treating RLS/WED.
  • According to the second study, one key benefit of using Horizant is predictable exposure to gabapentin due to consistent pharmacokinetic parameters across trials. This consistency provides more reliable therapeutic effects than oral formulations known for high interindividual variability in bioavailability.
  • In comparison with other drugs used in managing RLS/WED symptoms, it was found that α2δ ligands like Horizant are favored over dopamine agonists because they have fewer adverse effects such as nausea or somnolence while maintaining efficacy levels.
  • Despite positive findings about Gabapentin Enacarbil's effectiveness and safety profile, there remains a need for new long-term treatment options developed based on understanding pathophysiology related specifically to Restless Leg Syndrome/Willis-Ekbom Disease conditions.

Product Monograph / Prescribing Information

Document TitleYearSource
Horizant (gabapentin enacarbil) Prescribing Information.2022Azurity Pharmaceuticals, LLC, Atlanta, GA

Systematic Reviews / Meta-Analyses

Clinical Practice Guidelines

Document TitleYearSource
The Management of Restless Legs Syndrome: An Updated Algorithm.2021Mayo Clinic Proceedings