Gabapentin Used In a Unique Pharmacokinetic Profile

Gabapentin Used In a Unique Pharmacokinetic Profile

Intended for patients experiencing post herpetic neuralgia, or pain after shingles, gabapentin is unique by design. Known as the brand name Gralise, which is marketed by Depomed and Abbott, this form of gabapentin is specifically made as an oral, once-a-day prescription medication, which offers 24-hour pain control for people with after-shingles pain. Gabapentin, CAS number 60142-96-3, will be highly sought after with the release of the patent for Gralise, which expires on September 19, 2016. Gabapentin is used in a different pharmacokinetic profile in Gralise, and this formula is not interchangeable with other gabapentin products because of this difference.


Gabapentin, as Gralise, is typically titrated to an 1800 milligram dose, taken once daily in the evening with a meal. An adult patient being treated with Gabapentin {Gralise} for post herpetic neuralgia would follow a schedule as follows:

Gralise dosage-table

Dosages of both 300 and 600 milligrams are available, as well as a 30 day starter pack for patients.


The illustration on the left shows the progression of herpes zoster. A cluster of small bumps (1) turns into blisters (2). The blisters fill with lymph, break open (3), crust over (4), and finally disappear. Postherpetic neuralgia can sometimes occur due to nerve damage (5). Source:

On July 23, 2012  Phase III clinical trial results of gabapentin/Gralise were published. This 11-week double-blind, placebo-controlled and randomized clinical trial evaluated the efficacy and safety of a once-daily gastroretentive formulation of Gralise (gabapentin) of 1,800 milligrams, in patients with post herpetic neuralgia. This extensive multi-center study evaluated patients with persistent pain for a period between six months and five years after the healing of their herpes zoster rash. Results from this 452 patient study  revealed that patients treated with Gralise reported “much” or “very much” improvement in comparison to their counterparts who were treated with a placebo. Depomed reported phenomenal product sales of Gralise in the second quarter of 2012- $3.2 million dollars. With roughly one million Americans developing shingles and as post herpetic neuralgia each year, this unique form of gabapentin is surely needed. With the main side effect being dizziness, gabapentin used in Gralise stands to be a formidable treatment for patients with post-shingles pain in the future. LGM Pharma is a provider of the API gabapentin, and offers clients total support throughout the entire research and development process.

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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