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gabapentin (Rx)Brand and Other Names:Neurontin, Gralise

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 100mg
  • 300mg
  • 400mg

tablet

  • 300mg (Gralise)
  • 600mg (Gralise, Neurontin)
  • 800mg (Neurontin)

oral solution

  • 250mg/5mL
more...

Partial Seizures

Neurontin

  • Adjunctive therapy for partial seizures with or without secondary generalization
  • Initial: 300 mg PO q8hr
  • May increase up to 600 mg PO q8hr; up to 2400 mg/day administered and tolerated in clinical studies; up to 3600 mg administered for short duration and tolerated

Postherpetic Neuralgia

Neurontin

  • Day 1: 300 mg PO qDay
  • Day 2: 300 mg PO q12hr
  • Day 3: 300 mg PO q8hr
  • Maintenance: Subsequently titrate as needed up to 600 mg PO q8hr; doses >1800 mg/day have demonstrated no additional benefit

Gralise

  • Titrate gradually to 1800 mg/day PO; take qDay with evening meal
  • Day 1: 300 mg PO qDay
  • Day 2: 600 mg PO qDay
  • Days 3-6: 900 mg PO qDay
  • Days 7-10: 1200 mg PO qDay
  • Days 11-14: 1500 mg PO qDay
  • Day 15 and after (maintenance): 1800 mg PO qDay

Dosing considerations

  • Gralise tablets swell in gastric fluid and gradually release gabapentin

Restless legs syndrome (Off-label)

100-300 mg PO 2 hr before bedtime on first day; may titrate every 2 weeks until symptom relieve achieved (range 300-1800 mg/day)

Cocaine withdrawal (Off-label)

800-1500 mg/day PO in divided doses for up to 9 months

Insomnia (Off-label)

Up to 1800 mg PO evenings for up to 9 weeks

Diabetic Neuropathy (Off-label)

900 mg/day PO initially; may increase gradually q3Days to 1800-3600 mg/day

Tremors in multiple sclerosis (Off-label)

1200-1800 mg/day PO as monotherapy

Hot flashes-cancer related (Off-label)

200-1600 mg PO qDay to q6hr for 4-8 weeks

Amyotrophic Lateral Sclerosis (Orphan)

Neurontin

Orphan indication sponsor

  • Warner-Lambert Company, Parke-Davis Pharmaceutical Research Division; 2800 Plymouth Road; Ann Arbor, MI 48105

Dosing Modifications

Renal impairment (Neurontin)

  • CrCl >60 mL/min: 300-1200 mg PO TID
  • CrCl 30-60 mL/min: 200-700 mg q12hr
  • CrCl 15-29 mL/min: 200-700 mg qDay
  • CrCl <15 mL/min: 100-300 mg qDay
  • Hemodialysis (CrCl <15 mL/min): Administer supplemental dose (range 125-350 mg) posthemodialysis, after each 4 hr dialysis interval; further dose reduction should be in proportion to CrCl (eg, CrCl of 7.5 mL/min should receive one-half daily posthemodialysis dose)

Renal impairment (Gralise)

  • CrCl ≥60 mL/min: 1800 mg qDay with evening meal
  • CrCl 30-59 mL/min: 600-1800 mg qDay with evening meal
  • CrCl <30 mL/min or hemodialysis: Do not administer

Administration

Reducing the dose, discontinuing the drug, or substituting an alternative medication should be done gradually over a minimum of 1 week or longer

Swallow Gralise tablets whole; do not cut, crush, or chew them

Dosage Forms & Strengths

capsule

  • 100mg
  • 300mg
  • 400mg

tablet

  • 300mg (Gralise)
  • 600mg (Gralise, Neurontin)
  • 800mg (Neurontin)

oral solution

  • 250mg/5mL
more...

Partial Seizures

Neurontin

  • Adjunctive therapy for partial seizures with or without secondary generalization in patients older than 12 years of age with epilepsy; also indicated as adjunctive therapy for partial seizures in pediatric patients aged 3-12 years
  • <3 years: Safety and efficacy not established
  • 3-12 years (initial dose): 10-15 mg/kg/day PO divided q8hr initially; titrate up in approximately 3 days to effective maintenance dose 
  • 3-4 years (maintenance dose): 40 mg/kg/day PO divided q8hr
  • 5-12 years (maintenance dose): 25-35 mg/kg/day PO divided q8hr
  • >12 years (initial dose): 300 mg PO q8hr; may increase up to 600 mg PO q8hr

Dosing Considerations

Gralise tablets swell in gastric fluid and gradually release gabapentin

Dosing Modifications

Renal impairment: Gabapentin dose reduction may be required, depending on renal function

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Interactions

Interaction Checker

gabapentin and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Ataxia (1-13%)

            Dizziness (16-20%)

            Drowsiness (5-21%)

            Fatigue (11-15%)

            Somnolence (16-20%)

            1-10%

            Diplopia (6-10%)

            Nystagmus (6-10%)

            Tremor (6-10%)

            Amblyopia (1-5%)

            Back pain (1-5%)

            Constipation (1-5%)

            Depression (1-5%)

            Dry mouth (1-5%)

            Dysarthria (1-5%)

            Dyspepsia (1-5%)

            Hostility (5-8% children)

            Hyperkinesia (3-5%)

            Increased appetite (1-5%)

            Leukopenia (1-5%)

            Myalgia (1-5%)

            Nervousness (1-5%)

            Peripheral edema (1-5%)

            Pharyngitis (1-5%)

            Pruritus (1-5%)

            Rhinitis (1-5%)

            Vasodilation (1-5%)

            Weight gain (1-5%)

            Abnormal vision (>1%)

            Anorexia (>1%)

            Arthralgia (>1%)

            Asthenia (>1%)

            HTN (>1%)

            Malaise (>1%)

            Paresthesia (>1%)

            Purpura (>1%)

            Vertigo (>1%)

            Postmarketing Reports

            Angioedema

            Blood glucose fluctuation

            Breast enlargement

            Erythema multiforme

            Elevated liver function tests

            Fever

            Hyponatremia

            Jaundice

            Stevens-Johnson syndrome

            Adverse events following abrupt discontinuation have also been reported; the most frequently reported events have been anxiety, insomnia, nausea, pain, and sweating

            Postmarketing reports

            Changes in libido, ejaculation disorders, and anorgasmia

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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            Increased blood CPK levels and rhabdomyolysis reported

            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

            Anaphylaxis and angioedema reported after first dose or at any time during treatment; instruct patients to discontinue therapy and seek medical care should they experience signs or symptoms of anaphylaxis or angioedema

            May cause CNS depression, which may impair ability to operate heavy machinery; advise patients not to drive until they have gained enough experience to assess whether therapy will impair ability to drive

            Extended release formulation (Garlise) not studied in the treatment of seizures

            Extended release formulation (Garlise), not interchangeable with immediate release

            May potentiate effects of other sedatives or ethanol when administered concomitantly

            Do not discontinue abruptly (may increase seizure frequency); gradually taper over a minimum of 1 week

            Ages 3-12 years: Risk of neuropsychiatric adverse events, including emotional lability, hostility, thought disorders, and hyperkinesia

            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, hematologic abnormalities, myocarditis, myositis) and may resemble an acute viral infection

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Enters breast milk; use with caution

            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.

            more...
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            Pharmacology

            Mechanism of Action

            GABA analogue; structurally related to neurotransmitter GABA, but has no effect on GABA binding, uptake, or degradation; presence of gabapentin binding sites throughout the brain reported; mechanism for analgesic and anticonvulsant activity unknown

            Absorption

            Variable from proximal small bowel by L-amino transport system

            Neurontin

            • Bioavailability: Inversely proportion to dose; 60% (900 mg/day); 47% (1200 mg/day); 34% (2400 mg/day); 33% (3600 mg/day); 27% (4800 mg/day)
            • Peak plasma time: 2-4 hr
            • Peak plasma concentration: 8536 ng/mL
            • AUC: 141,301 ng•hr/mL

            Gralise

            • Bioavailability: Increased with high fat meal
            • Peak plasma time: 8 hr
            • Peak plasma concentration: 9585 ng/mL (1800 mg qDay)
            • AUC: 132,808 ng•hr/mL

            Distribution

            Neurontin and Gralise

            • Protein bound: <3%
            • Vd: 58 L

            Metabolism

            Gabapentin is not appreciably metabolized in humans

            Not a substrate, inducer, or inhibitor of CYP450 isoenzymes

            Elimination

            Neurontin and Gralise

            • Half-life: 5-7 hr
            • Dialyzable: Yes
            • Renal clearance: 225 mL/min; 125 mL/min (if older than 70 y)
            • Total body clearance: Proportional to CrCl
            • Excretion: Urine
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            Images

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            Formulary

            FormularyPatient Discounts

            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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