Gabapentin enacarbil

HORIZANT is indicated for: treatment of moderate-to-severe primary Restless Legs Syndrome (RLS) in adults. management of postherpetic neuralgia (PHN) in adults.

Gabapentin enacarbil is a prodrug of gabapentin and, accordingly, its therapeutic effects in RLS and PHN are attributable to gabapentin. The precise mechanism by which gabapentin is efficacious in RLS and PHN is unknown. The mechanism of action by which gabapentin is efficacious in PHN is unknown but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). Gabapentin prevents pain-related responses in several models of neuropathic pain in rats and mice (e.g., spinal nerve ligation models, spinal cord injury model, acute herpes zoster infection model).

Instruct patients to swallow tablets whole and not to cut, crush, or chew tablets. Take with food. RLS: 600 mg once daily taken at about 5 PM. A dose of 1,200 mg once daily provided no additional benefit compared with the 600-mg dose, but caused an increase in adverse reactions. If the dose is not taken at the recommended time, the next dose should be taken the following day as prescribed. PHN: The starting dose is 600 mg in the morning for 3 days, then increase to 600 mg twice daily beginning on day 4. A daily dose greater than 1,200 mg provided no additional benefit. If the dose is not taken at the recommended time, skip this dose, and the next dose should be taken at the time of next scheduled dose. Patients with renal impairment: Doses of HORIZANT must be adjusted in accordance with renal function.

None. None.

Driving impairment: Warn patients not to drive until they have gained sufficient experience with HORIZANT to assess whether it will impair their ability to drive. Somnolence/sedation and dizziness: May impair the patient's ability to operate complex machinery. HORIZANT is not substitutable with other gabapentin products. Suicidal thoughts or behaviors: HORIZANT is a prodrug of gabapentin, an antiepileptic drug (AED). AEDs increase the risk of suicidal thoughts or behaviors. Monitor for suicidal thoughts or behaviors. Abrupt or rapid discontinuation may increase the risk for seizures. Withdrawal symptoms, or suicidal behavior and ideation have been observed after discontinuation. Respiratory depression: May occur with HORIZANT when used with concomitant central nervous system (CNS) depressants or in the setting of concurrent respiratory impairment.

The following clinically significant adverse reactions are described in more detail in the Warnings and Precautions section of the labeling: Effects on Driving Somnolence/Sedation and Dizziness Suicidal Behavior and Ideation Increased Risk of Seizures and Other Adverse Reactions with Abrupt or Rapid Discontinuation Respiratory Depression Drug Reaction With Eosinophilia and Systemic Symptoms (DRESS)/Multiorgan Hypersensitivity RLS: Most common adverse reactions (≥10% and at least 2 times the rate of placebo) were somnolence/sedation and dizziness. PHN: Most common adverse reactions (≥10% and greater than placebo) were dizziness, somnolence, and headache.

Gabapentin enacarbil is released faster from HORIZANT Extended-Release tablets in the presence of alcohol. Consumption of alcohol is not recommended when taking HORIZANT. Morphine: HORIZANT taken in conjunction with morphine causes increased somnolence/sedation, dizziness, and nausea when compared with either drug alone.

Store at 25°C (77°F), excursions permitted 15°C to 30°C (59°F to 86°F). Protect from moisture.