Gabapentin enacarbil

What is Gabapentin enacarbil?

• Gabapentin enacarbil (HORIZANT) is a prodrug of gabapentin used as an anticonvulsant and analgesic drug.

Gabapentin enacarbil

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What are the uses of this medicine?

HORIZANT is a prescription medicine used to treat adults with:

• moderate-to-severe primary Restless Legs Syndrome (RLS).
• pain from damaged nerves (postherpetic pain) that follows healing of shingles (a painful rash that comes after a herpes zoster infection).

How does this medicine work?

• Gabapentin enacarbil is a prodrug of gabapentin.
• The precise mechanism by which gabapentin is efficacious in RLS and PHN is unknown.
• Gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli).
• Gabapentin also decreases pain-related responses after peripheral inflammation , but does not alter immediate pain-related behaviors.
• In vitro studies have shown that gabapentin binds with high affinity to the α2δ subunit of voltage-activated calcium channels; however, the relationship of this binding to the therapeutic effects of gabapentin enacarbil in RLS and PHN is unknown.

Who Should Not Use this medicine ?

• Limitations of use:
• HORIZANT is not for people with RLS who need to sleep during the daytime and need to stay awake at night.
• HORIZANT is not the same medicine as gabapentin (for example, NEURONTIN® or GRALISE®) and should not be used in its place.
• It is not known if HORIZANT is safe and effective in children.

What drug interactions can this medicine cause?

• Consumption of alcohol is not recommended when taking HORIZANT.
• HORIZANT taken in conjunction with morphine causes increased somnolence/sedation, dizziness, and nausea when compared with either drug alone.

Is this medicine FDA approved?

• Gabapentin enacarbil was denied approval by the U.S. Food and Drug Administration (FDA) in February 2010, citing concerns about possible increased cancer risk shown by some animal studies.
• On April 6, 2011, Xenoport received FDA approval for Horizant (gabapentin enacarbil) for the treatment of moderate-to-severe restless legs syndrome.
• On June 7, 2012, FDA approved Horizant for the treatment of postherpetic neuralgia in adults.

How should this medicine be used?

Recommended dosage: Restless Legs Syndrome:

• The recommended dosage for HORIZANT is 600 mg once daily at about 5 PM.
• A daily dose of 1,200 mg 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.

Postherpetic Neuralgia

• The recommended dosage of HORIZANT is 600 mg twice daily.
• HORIZANT should be initiated at a dose of 600 mg in the morning for 3 days of therapy, then increased to 600 mg twice daily (1,200 mg/day) on day four.
• If the dose is not taken at the recommended time, skip this dose, and the next dose should be taken at the time of the next scheduled dose.

Administration:

• Take HORIZANT tablets whole. Do not cut, crush, or chew your tablet.
• Take HORIZANT tablets with food.
• Do not stop taking HORIZANT without talking to your healthcare provider first. If you stop taking HORIZANT suddenly, you may develop side effects.
• If you forget to take your medicine at the time recommended by your healthcare provider, just skip the missed dose. Take the next dose at your regular time. Do not take 2 doses at one time.
• If you take too much HORIZANT, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-Release Tablets: 300 mg and 600 mg

This medicine is available in fallowing brand namesː

• HORIZANT

What side effects can this medication cause?

The most common side effects of this medicine include:

• sleepiness
• dizziness
• headache

HORIZANT can cause serious side effects:

• suicidal thoughts
• life-threatening allergic reaction
• Serious breathing problems

What special precautions should I follow?

• Do not take other medicines that make you sleepy or dizzy while taking HORIZANT without first talking with your healthcare provider. Taking HORIZANT with medicines that cause sleepiness or dizziness may make your sleepiness or dizziness worse.
• Do not take other gabapentin drugs (for example, NEURONTIN or GRALISE) while you take HORIZANT.
• Do not consume alcohol when taking HORIZANT.
• 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.
• Respiratory depression may occur with HORIZANT when used with concomitant central nervous system (CNS) depressants or in the setting of concurrent respiratory impairment. Monitor patients and adjust dosage as appropriate.
• HORIZANT (gabapentin enacarbil) is a prodrug of gabapentin, an antiepileptic drug (AED). AEDs increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication. Behaviors of concern should be reported immediately to healthcare providers.
• Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), also known as multiorgan hypersensitivity, has been reported in patients taking antiepileptic drugs, including gabapentin. If such signs or symptoms are present, the patient should be evaluated immediately. HORIZANT should be discontinued if an alternative etiology for the signs or symptoms cannot be established.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• dizziness
• somnolence/sedation
• double vision
• tremor
• slurred speech
• drowsiness
• altered mental status
• dizziness
• lethargy
• diarrhea

Management of overdosage:

• In the event of an overdose, the patient should be treated supportively with appropriate monitoring as necessary.
• Gabapentin derived from gabapentin enacarbil can be removed from plasma by hemodialysis.
• Further management should be as clinically indicated or as recommended by a poison control center.

Can this medicine be used in pregnancy?

• There are no adequate data on the developmental risk associated with the use of HORIZANT in pregnant women.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been studied.

What are the active and inactive ingredients in this medicine?

• Active ingredients: gabapentin enacarbil

• Inactive ingredients: Both the 300 mg and 600 mg tablets contain colloidal silicon dioxide, dibasic calcium phosphate dihydrate, glyceryl behenate, magnesium stearate, sodium lauryl sulfate, and talc.

Who manufactures and distributes this medicine?

Manufactured for: Arbor Pharmaceuticals, LLC Atlanta, GA

• HORIZANT is a registered trademark of Arbor Pharmaceuticals, LLC.

What should I know about storage and disposal of this medication?

• Store HORIZANT between 59° and 86°F (15° and 30°C).
• Keep HORIZANT dry and away from moisture.
• Keep HORIZANT tightly closed in the bottle provided to you. Do not remove any moisture control packs that may come in the bottle.

• Dailymed label info on Gabapentin enacarbil
• FDA Gabapentin enacarbil

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