Names and pronunciation
(gab′a-pen-tin) Gralise, Gralise Starter, Horizant, Neurontin
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Individual generic drug information
Extracted information for gabapentin only.
(gab′a-pen-tin) Gralise, Gralise Starter, Horizant, Neurontin
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Func. class.: Anticonvulsant
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Chem. class.: GABA analogue
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Do not confuse: Neurontin/Noroxin/Motrin/Neoral
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ACTION: Mechanism unknown; may increase seizure threshold; structurally similar to GABA but does not bind to GABAa or GABAb; gabapentin binding sites in neocortex, hippocampus
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USES: Adjunct treatment of partial sei- zures, with/without generalization in patients >12 yr; adjunct for partial sei- zures in children 3-12 yr, postherpetic neuralgia, primary restless leg syndrome in adults, ALS, neuropathic pain
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Extracted information for gabapentin only.
CONTRAINDICATIONS: Hyper- sensitivity to this product Precautions: Pregnancy, breastfeeding, children <3 yr, geriatric patients, renal disease, hemodialysis, suicidal thoughts, depression
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SIDE EFFECTS CNS: Dizziness, fatigue, somnolence, ataxia, amnesia, abnormal thinking, depression; children 3-12 yr old, emotional lability, aggression, thought disorder, hyperkinesia, hostility CV: Vasodilation, peripheral edema EENT: Dry mouth, blurred vision, diplopia, nystagmus; otitis media (child 3-12 yr) GI: Constipation, weight gain, increased appetite, nausea, vomiting; diarrhea (Gralise) GU: Impotence, UTI HEMA: Leukopenia INTEG: Pruritus, abrasion, acne vulgaris MS: Myalgia, back pain, gout RESP: Cough, upper respiratory infec- tion (child 3-12 yr) SYST: Drug reaction with eosinophilia and systemic symptoms (DRESS); dehy- dration (child 3-12 yr)
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INTERACTIONS Increase: CNS depression—alcohol, sed- atives, antihistamines, all other CNS depressants; monitor for CNS depression Increase: effect of—HYDROcodone; dosage reduction may be needed Decrease: gabapentin levels—antacids, separate by 2 hr Drug/Herb Increased: CNS depression—chamomile, kava, valerian Drug/Lab Test Decrease: WBC False positive: urinary protein using Ames N-Multistix SG
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Extracted information for gabapentin only.
DOSAGE AND ROUTES Adjunctive in partial seizures with or without secondary generalized tonic-clonic seizures (Neurontin only) • Adult/child >12 yr: PO 300 mg tid; may titrate to 1800 mg/day in 3 divided doses • Child 3-12 yr: PO 10-15 mg/kg/day in 3 divided doses initially titrate dose up- ward over approximately 3 days; if >5 yr old, use 25-35 mg/kg/day; if 3-4 yr old, 40 mg/kg/day divided in 3 doses Postherpetic neuralgia (PHN) • Adult: PO (Neurontin) 300 mg on day 1, 600 mg/day divided bid on day 2, 900 mg/day on day 3 divided tid, may titrate to 1800-3600 mg divided tid if needed; EXT REL (Gralise only) 300 mg on day 1, 600 mg on day 2, 900 mg on days 3-6, 1200 mg on days 7-10, 1500 mg on days 11-14, 1800 mg on day 15 and thereafter; (Horizant only) 600 mg in AM × 3 days, day 4 give 600 mg bid Moderate to severe restless legs syndrome (RLS) (Horizant only) • Adult: PO EXT REL 600 mg daily with food at about 5 PM; if dose missed, take next day at 5 PM Neuropathic pain (immediate release) • Adult: PO 1200-3600 mg/day in 3 di- vided doses, maintenance 300-1200 mg tid, max 3600 mg/day Renal dose • Adult: PO EXT REL tablets (Gralise tablets only): CCr 30-59 mL/min: 600- 1800 mg/day as tolerated; CCr <30 mL/ min: do not use; ext-rel tablets (Horizant tablets only) CCr 30-59 mL/min: for RLS, 300 mg/day, increase to 600 mg/day as needed, for PHN, 300 mg in the AM × 3 days, then increase to 300 mg bid, in- crease to 600 mg bid as needed; for dose tapering, reduce the maintenance dose to daily in the AM × 1 wk before discontinu- ing; CCr 15-29 mL/min: for RLS, 300 mg/ day; for PHN, 300 mg PO on days 1 and 3, then 300 mg daily in the AM, increase to 300 mg bid as needed, for tapering, if dose is 300 mg bid, reduce to 300 mg daily in AM × 1 wk before discontinuation; if the dose is 300 mg daily, no taper is required; CCr <15 mL/min: for RLS and PHN, 300 mg every other day; for PHN, dose can be increased to 300 mg daily in AM; no dose taper is required
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Available forms: Caps 100, 300, 400 mg; tablets 100, 300, 400, 600, 800 mg; oral sol 250 mg/5 mL; ext rel tab: 300, 600 mg
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Administer: • Do not crush or chew caps, ext rel tabs; caps may be opened and contents put in applesauce or dissolved in juice; scored tabs may be cut in half • 2 hr apart when giving antacids • Give without regard to meals (immedi- ate release) • Give with food (ext rel) • Refrigerate oral solution • Gradually withdraw over 7 days; abrupt withdrawal may precipitate seizures • Beginning dose at bedtime to minimize daytime drowsiness • Oral sol: measure with calibrated de- vice, refrigerate • Ext rel: give with food at about 5 PM (Gralise); bioavailability increased with food; swallow whole; do not interchange Gralise with Horizant • Store at room temperature away from heat and light
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Extracted information for gabapentin only.
Assess: • Seizures: aura, location, duration, fre- quency, activity at onset; use seizure pre- cautions if present • Pain: location, duration, characteris- tics if using for chronic pain, migraine • Vision changes: obtain testing base- line, during and after treatment • RLS: restless leg syndrome characteris- tics baseline and periodically • Mental status: mood, sensorium, affect, G behavioral changes, suicidal thoughts/ behaviors; if mental status changes, no- tify prescriber • WBC, gabapentin level (therapeutic 5.9-21 mcg/mL, toxic >85 mcg/mL), se- rum creatinine/BUN, weight • Drug reaction with eosinophilia and systemic symptoms • Increased fluids, bulk in diet for con- stipation • Beers: avoid in older adults unless safer alternative is unavailable; ataxia, impaired psychomotor function may occur • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk
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Evaluate: • Therapeutic response: decreased seizure activity; decrease in chronic pain
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To carry emergency ID stating patient’s name, products taken, condition, prescrib- er’s name and phone number • To avoid driving, other activities that require alertness until response is known because dizziness, drowsiness may occur • Not to discontinue medication quickly after long-term use; to taper over ≥1 wk because withdrawal-precipitated seizures may occur; not to double doses if dose is missed; to take if 2 hr or more before next dose • To report changes in vision, diplopia, eye irritation to provider • Not to use with alcohol, sedative, anti- histamines, or other products that cause dizziness/sleepiness • To notify providers of use before surgery • To take as prescribed; not to inter- change formulations; that ext rel prod- uct should not be crushed or chewed, if tablet is to be broken in half, use within 28 days or discard • To report suicidal thoughts or feelings, increased depression, panic attacks, hos- tility, confusion to provider • Not to use within 2 hr of antacid, may take regular release without regard to meals; ext rel should be taken with food; doses interval should not be ≥12 hr • To obtain emergency treatment for sei- zures or dizziness, cyanosis of extremities or lips, trouble breathing, unusual sleepi- ness • To keep oral solution refrigerated • To notify prescriber if pregnancy is planned or suspected; to avoid breast- feeding
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Extracted information for gabapentin only.
PHARMACOKINETICS half-life 5-7 hr; immediate release peak 2 hr, ext rel peak 8 hr (Gralise); 5-7 hr (Horizant)
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Filter the extracted dose blocks for this individual drug.
or without secondary generalized tonic-clonic seizures (Neurontin only)
• Adult/child >12 yr: PO 300 mg tid; may titrate to 1800 mg/day in 3 divided doses
Candidate age grouping · source page 612
or without secondary generalized tonic-clonic seizures (Neurontin only)
• Adult: PO (Neurontin) 300 mg on day 1, 600 mg/day divided bid on day 2, 900 mg/day on day 3 divided tid, may titrate to 1800-3600 mg divided tid if needed; EXT REL (Gralise only) 300 mg on day 1, 600 mg on day 2, 900 mg on days 3-6, 1200 mg on days 7-10, 1500 mg on days 11-14, 1800 mg on day 15 and thereafter; (Horizant only) 600 mg in AM × 3 days, day 4 give 600 mg bid Moderate to severe restless legs syndrome (RLS) (Horizant only)
Candidate age grouping · source page 612
or without secondary generalized tonic-clonic seizures (Neurontin only)
• Adult: PO EXT REL 600 mg daily with food at about 5 PM; if dose missed, take next day at 5 PM Neuropathic pain (immediate release)
Candidate age grouping · source page 612
or without secondary generalized tonic-clonic seizures (Neurontin only)
• Adult: PO 1200-3600 mg/day in 3 di- vided doses, maintenance 300-1200 mg tid, max 3600 mg/day Renal dose
Candidate age grouping · source page 612
or without secondary generalized tonic-clonic seizures (Neurontin only)
• Adult: PO EXT REL tablets (Gralise tablets only): CCr 30-59 mL/min: 600- 1800 mg/day as tolerated; CCr <30 mL/ min: do not use; ext-rel tablets (Horizant tablets only) CCr 30-59 mL/min: for RLS, 300 mg/day, increase to 600 mg/day as needed, for PHN, 300 mg in the AM × 3 days, then increase to 300 mg bid, in- crease to 600 mg bid as needed; for dose tapering, reduce the maintenance dose to daily in the AM × 1 wk before discontinu- ing; CCr 15-29 mL/min: for RLS, 300 mg/ day; for PHN, 300 mg PO on days 1 and 3, then 300 mg daily in the AM, increase to 300 mg bid as needed, for tapering, if dose is 300 mg bid, reduce to 300 mg daily in AM × 1 wk before discontinuation; if the dose is 300 mg daily, no taper is required; CCr <15 mL/min: for RLS and PHN, 300 mg every other day; for PHN, dose can be increased to 300 mg daily in AM; no dose taper is required
Candidate age grouping · source page 612