Gabapentin ER
GRALISE
Pronunciation: gab-a-PEN-tin (gra-LEEZ)
“Gray leash”
Must take with food
Tablet swells → stays in stomach → releases gabapentin to intestine gradually
What it isGastroretentive extended-release gabapentin tablets (GRALISE, 2011) — the tablet swells in gastric fluid and is held in the stomach, releasing gabapentin gradually into the intestine, which is what makes once-daily dosing possible; titrated to 1800 mg taken with the evening meal and swallowed whole.
Why this oneFood is not a convenience here — the evening meal is what keeps the swollen tablet in the stomach long enough to work, so a dose taken on an empty stomach is a different drug.
What limits itApproved only for postherpetic neuralgia; effectiveness in epilepsy has not been studied, and the label states it is not interchangeable with other gabapentin products. Avoid if CrCl is under 30 or on hemodialysis.
FDA-approved for
- postherpetic neuralgia (2011)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Postherpetic neuralgia | Adults | 300 mg QD | 1,800 mg QD (with evening meal) | 1,800 mg QD |
Titration Titrate over 15 days: 300 mg (day 1) → 600 mg (day 2) → 900 mg (days 3-6) → 1,200 mg (days 7-10) → 1,500 mg (days 11-14) → 1,800 mg (day 15)
Renal CrCl >=60: 1,800 mg QD; CrCl 30-60: 600-1,800 mg QD (individualize); CrCl <30 or hemodialysis: do not use. Reduced-renal patients initiate at 300 mg QD.
Hepatic Undefined
Not substitutable with other gabapentin products because of differing pharmacokinetic profiles affecting frequency of administration.
Instructions
- Swallow tablets whole with the evening meal; do not crush, split, or chew
- Not substitutable with other gabapentin products (differing PK)
- If reduced, discontinued, or switched, taper gradually over a minimum of 1 week
Available strengths
- tab 300, 450, 600, 750, 900 mg
- cap 100, 200, 300, 400 mg
- sol 250 mg/5 mL
Cautions
- Suicidal behavior and ideation (antiepileptic drug class effect)
- Increased risk of adverse reactions (incl. withdrawal, seizures) with abrupt/rapid discontinuation - taper over >=1 week
- Respiratory depression (life-threatening/fatal) with concomitant CNS depressants/opioids or underlying respiratory impairment
- DRESS/multiorgan hypersensitivity
- Tumorigenic potential
Adverse reactions
- Dizziness (most common)
- Somnolence
- Headache
- Peripheral edema
- Diarrhea
- Dry mouth
- Weight increased
Pregnancy Human data over decades have not identified a drug-associated risk of major birth defects; animal studies showed developmental toxicity; NAAED pregnancy registry available.
Lactation Gabapentin is present in human milk; effects on the breastfed infant and milk production unknown; weigh benefits against risk.
Cost
| Strength | #/mo | generic $/mo | brand $/mo | CostPlus | |
|---|---|---|---|---|---|
| 300 mg | tab | 30 qd | $19.15 | — | not offered |
| 450 mg | tab | 30 qd | — | $304.28 | not offered |
| 600 mg | tab | 30 qd | $1.92 | — | not offered |
| 750 mg | tab | 30 qd | — | $455.57 | not offered |
| 900 mg | tab | 30 qd | — | $456.22 | not offered |
Other forms: Gabapentin (NEURONTIN)
NO BOXED WARNINGS
Principal riskSedation and dizziness, additive with opioids; not interchangeable with other gabapentin products
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySedation, dizziness and misuse potential; respiratory depression increases with opioids.
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