gabapentin enacarbil (Rx)

Brand and Other Names:Horizant
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet, extended-release

  • 300mg
  • 600mg
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Restless Leg Syndrome (RLS)

Indicated for moderate-to-severe primary restless legs syndrome

600 mg qDay with food at about 5:00 pm

Postherpetic neuralgia

600 mg PO x3 days, and then increase to 600 mg PO BID

Renal Impairment

CrCl >60 mL/min: 600 mg qDay

CrCl 30-59 mL/min: Start at 300 mg qDay; if needed may increase to 600 mg qDay

CrCL 15-29 mL/min: 300 mg qDay

CrCl <15 mL/min: 300 mg every other day

CrCl <15 mL/min and hemodialysis: Do not administer

Administration

Swallow tablet whole, do not cut, crush, or chew

Take with food

If dose not taken as scheduled, wait until next scheduled dose to resume administration

Discontinuation: Gradually taper downward; patients receiving 600 mg BID for postherpetic neuralgia should decrease dose to 600 mg qDay for 1 week

Safety and effectiveness have not been studied

May require a dose reduction depending on renal function (see Renal Impairment)

Postherpetic Neuralgia (Horizant)

600 mg PO x3 days, and then increase to 600 mg PO BID

Restless legs syndrome (Horizant)

Indicated for moderate-to-severe primary restless legs syndrome

600 mg PO qDay with food at about 5 PM

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Interactions

Interaction Checker

and gabapentin enacarbil

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            >10%

            Somnolence/sedation (10-27%)

            Dizziness (13-30%)

            Headache (7-15%)

            Fatigue/asthenia (6-10%)

            1-10%

            Nausea (4-9%)

            Fatigue/asthenia (6-10%)

            Peripheral edema (6-7%)

            Insomnia (3-7%)

            Irritability (4%)

            Weight increase (2-5%)

            Blurred vision (2-5%)

            Xerostomia (3-4%)

            Flatulence (2-3%)

            Vertigo (1-3%)

            Peripheral edema (1-3%)

            Drunk/abnormal sensation (1-3%)

            Depression (1-3%)

            Decreased libido (1-2%)

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            Warnings

            Contraindications

            None

            Cautions

            Not interchangeable with other gabapentin products because of differing pharmacokinetic profiles

            Somnolence, sedation, and dizziness may cause significant driving impairment

            Antiepileptic drugs increase risk of suicidal thoughts or behavior in patients taking these drugs for any indication; monitor for emergence or worsening depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior

            Discontinue gradually to minimize potential of withdrawal seizure; if taking 600 mg BID (for PHN), decrease to 600 mg qDay for 1 week prior to discontinuation

            Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), also known as multiorgan hypersensitivity, reported; some of these events have been fatal or life-threatening; typically presents with fever, rash, and/or lymphadenopathy in association with other organ system involvement (eg, hepatitis, nephritis, hematological abnormalities, myocarditis, myositis) and may resemble an acute viral infection

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            Pregnancy & Lactation

            Pregnancy Category: C

            Limited available data in pregnancy; use caution

            Lactation: Unknown whether distributed in breast milk

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            GABA analog; structurally related to neurotransmitter GABA, but has no effect on GABA binding, uptake, or degradation; mechanism for analgesic and anticonvulsant activity unknown

            Absorption

            Bioavailability: 75% (with food); 42-65% (fasting)

            Peak Plasma Time: 7.3 hr (with food); 5 hr (fasting)

            Distribution

            Protein Bound: <3%

            Vd: 76 L

            Metabolism

            Gabapentin is not appreciably metabolized in humans

            Gabapentin enacarbil undergoes extensive first-pass hydrolysis (primarily in enterocytes) to form gabapentin, carbon dioxide, acetaldehyde, and isobutyric acid

            Not a substrate, inducer, or inhibitor of CYP450 isoenzymes

            Elimination

            Half-life: 5.1 – 6.0 hr

            Dialyzable: yes

            Renal clearance: 5 -7 L/hr

            Total body clearance: 6-9.3 L/hr (oral)

            Excretion: 94% (urine); 5% (feces)

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            Administration

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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