gabapentin NEURONTIN

Class: Gabapentinoid/​α2δ Ligand
FDA Indications: Partial Seizures With Or Without Secondary Generalization (adjunctive), Postherpetic Neuralgia
Off-Label Use: Neuropathic Pain, Anxiety, Fibromyalgia, Bipolar Disorder, Alcohol Withdrawal, Alcohol Dependence, Brachioradial Pruritus, Chronic Cough, Diabetic Neuropathy, Hot Flashes, Restless Leg Syndrome, Postoperative Pain (adjunct), Social Anxiety, Uremic Pruritus, Treatment Resistant Bipolar Disorder, Lewy Body Dementia, Agitation And Aggression In Dementia
Forms: 100, 300, 400mg capsule; 600, 800mg tablet; 250 mg/5 mL po soln
Dose Range: 900-3600 mg/day
Starting: start at 300 mg q.h.s., increasing gradually to 300 mg t.i.d., then higher as tolerated

NAMI drug fact sheet

Serious Side Effects: Can exacerbate myoclonus, but the effect is mild and does not require discontinuance of the drug
Side Effects: drowsiness (18-21%), fatigue (11%), ataxia, headache, dizziness (17-28%), diplopia, nystagmus, diarrhea, tremor, peripheral edema
1° MOA: Binds to the α2δ subunit of presynaptic N and P/Q VGCCs, block the release of excitatory neurotransmitters such as glutamate when neurotransmission is excessive
t½: 6.5 (5-8)° TMAX: 2-3°
Substrate of: Renally cleared
Inhibits: ∅ ; Induces:
Active Metabolites:
  • - caution when prescribing with other CNS depressants; can cause respiratory depression when combined with opioids
  • - concomitant treatment with opioids is associated with a substantial increase in the risk of opioid-related death
  • - Maalox ↓'s bioavailability by 20%, so have patient take Neurontin at least 2 hours after Maalox
  • - ↓'s hydrocodone levels by up to 20% for unknown reasons
  • - surprisingly has no direct GABA-mimetic activity
  • - relatively mild side effect profile besides sedation/fatigue
  • - few DDIs!
  • - ↑'s slow-wave δ sleep
  • - apparently no potential for overdose: 1 patient took 49 grams in overdose with no serious sequelae
Special Populations

Category C—Limited Human Data — Animal Data Suggest Risk

RID 1.3-3.8%; Limited Human Data—Probably Compatible

No dosage adjustment necessary

CrCl ≥60 mL/min: 300-1,200 mg tid
CrCl >15-59 mL/min: 200-700 mg tid
CrCl 15 mL/min:100-300 mg qd
CrCl <15 mL/min: ↓ dose in proportion to CrCl based on dose for CrCl of 15mL/min
ESRD requires hemodialysis

Not hepatically metabolized ∴ no dose adjustments required


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Last updated February 29 2024 20:54:18. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.