Drug updated on 4/10/2024
| Dosage Form | Tablet (oral; 300 mg, 600 mg) |
| Drug Class | Gamma-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.
Summary
- 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 Title | Year | Source |
|---|---|---|
| Horizant (gabapentin enacarbil) Prescribing Information. | 2022 | Azurity Pharmaceuticals, LLC, Atlanta, GA |
Systematic Reviews / Meta-Analyses
| Document Title | Year | Source |
|---|---|---|
| A comprehensive update on the ADMET considerations for α2δ calcium channel ligand medications for treating restless legs syndrome. | 2024 | Expert Opinion on Drug Metabolism & Toxicology |
| Interindividual Variability in the Bioavailability of Gabapentin Enacarbil Extended Release in Healthy Adults: An Analysis of Data From 6 Phase I Studies. | 2022 | Therapeutic drug monitoring |
| The Efficacy and Safety of Pharmacological Treatments for Restless Legs Syndrome: Systemic Review and Network Meta-Analysis. | 2021 | Frontiers in Neuroscience |
Clinical Practice Guidelines
| Document Title | Year | Source |
|---|---|---|
| The Management of Restless Legs Syndrome: An Updated Algorithm. | 2021 | Mayo Clinic Proceedings |