Educational only — not medical advice. If you’re in crisis or thinking about suicide: call or text 988 (U.S.) or your local emergency number. Support resources. Under construction and review—see the updates log.
Brand: Horizant
Published 2025-12-23 · Last reviewed 2025-12-30 · 4 references
Content sourced from FDA labeling (DailyMed) and peer-reviewed literature.
Gabapentin enacarbil (brand Horizant) is an extended-release prodrug of gabapentin indicated for moderate-to-severe primary RLS and for postherpetic neuralgia (label).
It is an alpha-2-delta ligand (via conversion to gabapentin). In RLS, alpha-2-delta ligands are often positioned when painful symptoms and insomnia are prominent or when avoiding long-term dopaminergic risks (including augmentation) is a priority (guideline/clinical).
The main tolerability issues are somnolence and dizziness; next-day impairment and fall risk are important follow-up topics, especially when combined with other sedatives (label/clinical).
Gabapentin enacarbil and released gabapentin are not CYP substrates, inhibitors, or inducers; interaction management focuses on additive sedation and kidney-function-based dosing (label).
The gabapentin enacarbil compare view, evidence feed, and print page support review of RLS options and monitoring topics.
Gabapentin enacarbil is often positioned as a non-dopaminergic option for RLS when sedation is acceptable or helpful and when avoiding dopamine-agonist long-term risks is important; tolerability depends on next-day function, fall risk, and total sedative burden (guideline/clinical).
View labelExactRefer to the Glossary entry on Neurotransmitters for background on receptor systems involved in serious mental illness.
Prodrug converted to gabapentin, an alpha-2-delta ligand that modulates voltage-gated calcium channels and reduces excitatory neurotransmitter release (class/mechanism).
It does not act through dopamine receptors and is not a dopamine agonist.
In RLS care frameworks, alpha-2-delta ligands are often used when painful sensations, insomnia, or risk of dopaminergic augmentation are key constraints (guideline/clinical).