gabapentin enacarbil
Adjunctive therapy • Brands: Horizant
Last reviewed: 2025-12-30
General information
- Class: Adjunctive therapy
- Common US brands: Horizant
- Therapeutic drug monitoring not routinely recommended.
- Last reviewed: 2025-12-30
Dosing & forms
- Forms/strengths: —
- Frequency: —
- Food: —
- Typical range: —
Mechanism (brief)
Prodrug of gabapentin (alpha-2-delta ligand) used for moderate-to-severe primary restless legs syndrome and postherpetic neuralgia; converted by esterases to gabapentin (not CYP-mediated) with renal elimination of released gabapentin.
Metabolism & Half‑life
- Metabolism: Extensive first-pass hydrolysis to gabapentin (non-CYP; carboxylesterases) (label)., Released gabapentin is not appreciably metabolized (label).
- Half‑life: Single-dose range 5.1–6 h
Therapeutic Drug Monitoring (TDM)
Recommended: No
Monitoring highlights
- —
Sources
- HORIZANT (gabapentin enacarbil) extended-release tablets prescribing information — DailyMed (2025)
- Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline — Journal of Clinical Sleep Medicine (2025)
- The Management of Restless Legs Syndrome: An Updated Algorithm — Mayo Clinic Proceedings (2021)
- Gabapentin enacarbil in Japanese patients with restless legs syndrome: a 12-week, randomized, double-blind, placebo-controlled, parallel-group study — Current Medical Research and Opinion (2012)