Gabapentin enacarbil

FDA label

Read the full label on DailyMed ↗

Titration PHN: increase to 600 mg BID on day 4, after 3 days at 600 mg QAM. RLS: no titration — 600 mg QD from the start.

Renal Adjust by CrCl. RLS: >=60 600 mg/day; 30-59 start 300 mg/day, increase to 600 mg PRN; 15-29 300 mg/day; <15 300 mg QOD; <15 on hemodialysis not recommended. PHN: >=60 usual; 30-59 300 mg QAM x3 days then 300 mg BID, increase to 600 mg BID PRN; 15-29 300 mg QAM on days 1 and 3 then 300 mg QAM, increase to 300 mg BID PRN; <15 300 mg QOD in AM, increase to 300 mg QD PRN; <15 on hemodialysis 300 mg after each dialysis, increase to 600 mg after each dialysis PRN.

Hepatic Undefined

RLS dosing is time-of-day gated (~5 PM). Doses above 600 mg/day (RLS) or 1,200 mg/day (PHN) add adverse reactions without added benefit.

Instructions

• Swallow tablets whole — do not cut, crush, or chew.
• Take with food.
• RLS: take at about 5 PM; if a dose is missed, take the next dose the following day as prescribed.
• PHN: if a dose is missed, skip it and take the next dose at its scheduled time.
• Not substitutable with other gabapentin products (different pharmacokinetics).
• Taper — RLS: 600 mg QD or less may be stopped without tapering; if the dose exceeds 600 mg/day, reduce to 600 mg/day for 1 week before stopping.
• Taper — PHN: reduce the maintenance dose to once daily in the AM for 1 week before stopping (CrCl <15: no taper needed).
• Consider initiating at a low dose when co-prescribed with an opioid or other CNS depressant, or in underlying respiratory impairment.

Cautions

• Driving impairment — do not drive until experience with the drug shows it is not impairing; duration of impairment after initiation unknown.
• Somnolence/sedation and dizziness; may impair operation of complex machinery.
• Not substitutable with other gabapentin products; safety/efficacy in epilepsy not studied.
• Suicidal thoughts and behavior (antiepileptic class effect; prodrug of gabapentin) — monitor for new or worsening depression or mood change.
• Abrupt or rapid discontinuation increases seizure risk; withdrawal symptoms and suicidal behavior/ideation reported after stopping.
• Serious, life-threatening or fatal respiratory depression with concomitant CNS depressants (especially opioids) or underlying respiratory impairment.
• DRESS/multiorgan hypersensitivity — evaluate immediately and discontinue if no alternative etiology.
• Pancreatic acinar cell adenoma/carcinoma in rats; clinical significance unknown.

Adverse reactions

• RLS (600 mg/day): somnolence/sedation 20%, dizziness 13%, headache 12%.
• PHN (1,200 mg/day): dizziness 17%, somnolence 10%, headache 10%, nausea 8%, fatigue/asthenia 6%, peripheral edema 6%.
• Dose-related: somnolence/sedation, dizziness, feeling drunk, decreased libido, depression, headache, peripheral edema, vertigo.
• Also: dry mouth, flatulence, irritability, weight increase, increased appetite, blurred vision, insomnia, balance disorder.
• Postmarketing: breast enlargement, gynecomastia, elevated creatine kinase, bullous pemphigoid; respiratory depression with opioids/CNS depressants; withdrawal reactions including seizures.

Pregnancy No adequate human data; developmentally toxic in rats and rabbits at exposures above clinical. Neonatal withdrawal reported after prolonged in-utero gabapentin exposure with opioids near delivery — observe neonates.

Lactation Unknown whether gabapentin from Horizant enters human milk; gabapentin is secreted in milk after other gabapentin products. Weigh benefits of breastfeeding against maternal need.