Mechanism of Delivery

GRALISE is absorbed gradually to manage PHN throughout the night and day

GRALISE is a unique formulation that delivers a gradual release of gabapentin over time.

The GRALISE Mechanism of Delivery

When taken with an evening meal, the unique technology of GRALISE allows for once-daily dosing.12

2 hours post-dose

Tablet expands and remains in the stomach to gradually release gabapentin to the upper gastrointestinal tract, the optimal site of absorption.134

8-10 hours post-dose

A gradual release of gabapentin from the stomach to the upper small intestine occurs over 8 to 10 hours.1

~15 hours post-dose

The GRALISE tablet completely dissolves approximately 15 hours after dosing.4

PHARMACOKINETIC DATA DO NOT PREDICT EFFICACY OR SAFETY
Do not use GRALISE interchangeably with other gabapentin products because of differing pharmacokinetic profiles that affect frequency of administration.2
GRALISE should be taken with an evening meal. If it is taken on an empty stomach, the bioavailability will be substantially lower.2

Pharmacokinetics

GRALISE vs gabapentin immediate release

GRALISE reaches peak concentration at 8 hours when taken once daily with the evening meal.1

GRALISE plasma levels peak overnight1

PHARMACOKINETIC DATA DO NOT PREDICT EFFICACY OR SAFETY
When GRALISE (1800 mg once daily) and gabapentin immediate release (600 mg three times a day) were administered with high-fat evening meals (50% of calories from fat), GRALISE had a higher Cmax and lower AUC at steady state compared to gabapentin immediate release. Time to reach maximum plasma concentration (Tmax) for GRALISE is 8 hours, which is about 4 to 6 hours longer compared to gabapentin immediate release.2
Do not use GRALISE interchangeably with other gabapentin products because of differing pharmacokinetic profiles that affect frequency of administration.2
GRALISE should be taken with an evening meal. If it is taken on an empty stomach, the bioavailability will be substantially lower.2

QD=Once daily; TID=3x/day.

References:

  1. Argoff CE, Chen C, Cowles VE. Clinical development of a once-daily gastroretentive formulation of gabapentin for treatment of postherpetic neuralgia: an overview. Expert Opin Drug Deliv. 2012;9(9):1147-1160.
  2. GRALISE. Prescribing information. Almatica Pharma LLC; 2023.
  3. Sang CN, Sathyanarayana R, Sweeney M; DM-1796 Study Investigators. Gastroretentive gabapentin (G-GR) formulation reduces intensity of pain associated with postherpetic neuralgia (PHN). Clin J Pain. 2013;29(4):281-288.
  4. Gordi T, Hou E, Kasichayanula S, Berner B. Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive-extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in healthy subjects. Clin Ther. 2008;30(5):909-916.
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Gabapentin is a controlled substance in several states. Contact local authorities for more information. Advise patients to take GRALISE only as prescribed.