gabapentin enacarbil, Horizant, Gralise, Neurontin

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

What is gabapentin enacarbil, and how does it work (mechanism of action)?

Gabapentin enacarbil is used for treating restless leg syndrome (RLS) and postherpetic neuralgia. It is a prodrug of the anticonvulsant gabapentin, which means it is first converted to gabapentin in the body before it can have its effects. The mechanism of action of gabapentin in treating restless leg syndrome (RLS) or postherpatic neuralgia is not known. Gabapentin structurally resembles the neurotransmitter, gamma aminobutyric acid (GABA). (A neurotransmitter is a chemical that nerves use to communicate with one another.) It is possible that this similarity is related to gabapentin's mechanism of action. In animal models used for testing the anti-seizure and anti-pain (analgesic) activities of drugs, gabapentin prevents seizures and reduces pain-related responses. The FDA approved gabapentin enacarbil in April 2011.

What brand names are available for gabapentin enacarbil?

Horizant, Gralise, Neurontin

Is gabapentin enacarbil available as a generic drug?

GENERIC AVAILABLE: No

Do I need a prescription for gabapentin enacarbil?

Yes

What are the side effects of gabapentin enacarbil?

The most common side effects of gabapentin enacarbil are:

Gabapentin enacarbil may cause significant driving impairment. Fluid retention, hostility, nausea and vomiting also occur. Other adverse events associated with gabapentin enacarbil include:

Gabapentin enacarbil is converted to gabapentin, which is an anti-seizure medication. Anti-seizure medications have been associated with an increased risk of suicidal thinking and behavior. Anyone considering the use of anti-seizure drugs must balance this risk of suicide with the clinical need. Patients who are started on therapy should be closely observed for clinical worsening, suicidal thoughts, or unusual changes in behavior.

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