Gabapentin

Class
Anticonvulsants and anxiolytics
Subclass
Gabapentinoids
Substance name
Gabapentin
Brand names
Neurontin®, Gralise®
Common formulations
Film-coated tablet
See also
Gabapentin ER (Horizant®)
Dosage and administration
Adults patients
Symptomatic relief
CKD-associated pruritus • Off-label
•
100-300 mg PO daily after each dialysis session
Diabetic neuropathy • Off-label
•
Start at: 100-300 mg PO q8-24h
•
Maintenance: 900-3,600 mg PO daily, in 3 divided doses, for 4-8 weeks
Neuropathic pain • Off-label
•
400-1,200 mg PO TID
Neuropathic pruritus • Off-label
•
Start at: 100-300 mg PO qHS
•
Maintenance: 300-900 mg PO daily, in 1-3 divided doses
•
Maximum: 1,800 mg per day
Nystagmus • Off-label
•
Start at: 100 mg PO q8-24h
•
Maintenance: 300-1,200 mg PO TID
•
Maximum: 3,600 mg per day
Titrate over 3 weeks.
Pruritus in patients with cutaneous T-cell lymphoma • Off-label
•
Start at: 300 mg PO qHS
•
Maintenance: 900-2,400 mg PO daily, in 2-3 divided doses
Treatment
Postherpetic neuralgia
•
Start at: 300 mg PO daily on day 1
•
Maintenance: 300-600 mg PO TID
•
Maximum: 1,800 mg per day
Increase to 300 mg BID on day 2 and 300 mg TID on day 3.
Alternative
•
Start at: 300 mg PO daily on day 1
•
Maintenance: 1,800 mg PO daily
Increase to 600 mg on day 2, 900 mg on days 3-6, 1,200 mg on days 7-10, 1,500 mg on days 11-14, and 1,800 mg thereafter.
Alcohol use disorder • Maintenance of abstinence • Off-label
•
Start at: 300 mg PO daily on day 1
•
Maintenance: 600 mg PO TID
•
Maximum: 3,600 mg per day
Increase to 300 mg BID on day 2 and 300 mg TID on day 3.
Alcohol withdrawal syndrome • Off-label
•
Loading: 1,200 mg PO once
•
Subsequently: 600 mg PO QID on day 1
•
Maintenance: 300-600 mg PO daily for up to 4-7 days
Alternative
•
Loading: 1,200 mg PO once
•
Subsequently: 1,200 mg PO daily for 1-3 days
•
Maintenance: 300-600 mg PO daily for up to 4-7 days
Alternative
•
400 mg PO q6-8h
Administered in combination with benzodiazepines.
Burning mouth syndrome • Off-label
•
300-900 mg PO daily
Chronic cough • Off-label
•
Start at: 300 mg PO daily
•
Maintenance: 1,800 mg PO daily, in 1-2 divided doses
Complex regional pain syndrome • Off-label
•
600-1,800 mg PO daily, in 3 divided doses
Essential tremor • Off-label
•
1,200-1,800 mg PO daily, in 2-3 divided doses
Fibromyalgia • Off-label
•
Start at: 300 mg PO qHS for 1 week
•
Maintenance: 1,200-2,400 mg PO daily, in 3 divided doses, of which 1,200 mg at bedtime
•
Maximum: 2,400 mg per day
Titrate over 6 weeks, wtih a larger dose administered at bedtime.
Insomnia • Off-label
•
300-600 mg PO qHS
Restless legs syndrome • Off-label
•
Start at: 300 mg PO qHS
•
Maintenance: 900-2,400 mg PO qHS
Social anxiety disorder • Off-label
•
300-1,200 mg PO TID
Trigeminal neuralgia • Off-label
•
Start at: 100-300 mg PO qHS
•
Maintenance: 300-1,200 mg PO TID
•
Maximum: 3,600 mg per day
Vasomotor symptoms of menopause in females • Off-label
•
Start at: 100-300 mg PO qHS
•
Maintenance: 900-2,400 mg PO daily, in 3 divided doses
Vulvodynia • Off-label
•
Start at: 300 mg PO daily for 3 days
•
Maintenance: 300 mg PO TID
•
Maximum: 3,600 mg per day
Adjunctive treatment
Adjunctive treatment for focal seizures
•
Start at: 300 mg PO TID
•
Maintenance: 300-600 mg PO TID
•
Maximum: 2,400-3,600 mg per day
Prevention
Prevention of postoperative pain • Off-label
•
600-1,200 mg PO × 1 1-2 hours before surgery
Other off-label uses
•
Treatment of intractable hiccups
•
Treatment of pudendal neuralgia
Indications for use
Labeled indications
Adults
•
Treatment of postherpetic neuralgia
•
Adjunctive treatment for focal seizures
Children
•
Adjunctive treatment for focal seizures
Off-label indications
Adults
•
Symptomatic relief of CKD-associated pruritus
•
Symptomatic relief of diabetic neuropathy
•
Symptomatic relief of neuropathic pain
•
Symptomatic relief of neuropathic pruritus
•
Symptomatic relief of nystagmus
•
Symptomatic relief of pruritus in patients with cutaneous T-cell lymphoma
•
Treatment of alcohol use disorder (maintenance of abstinence)
•
Treatment of alcohol withdrawal syndrome
•
Treatment of burning mouth syndrome
•
Treatment of chronic cough
•
Treatment of complex regional pain syndrome
•
Treatment of essential tremor
•
Treatment of fibromyalgia
•
Treatment of insomnia
•
Treatment of intractable hiccups
•
Treatment of pudendal neuralgia
•
Treatment of restless legs syndrome
•
Treatment of social anxiety disorder
•
Treatment of trigeminal neuralgia
•
Treatment of vasomotor symptoms of menopause in females
•
Treatment of vulvodynia
•
Prevention of postoperative pain
Safety risks
Contraindications
Hypersensitivity to gabapentin or its components
Warnings and precautions
DRESS syndrome, anaphylaxis, angioedema
•
Maintain a high level of suspicion, as gabapentin has been associated with an increased risk for these adverse events.
Pancreatic cancer
•
Maintain a high level of suspicion, as gabapentin has been associated with an increased incidence of pancreatic acinar cell tumors in rats.
Respiratory depression
•
Use caution in patients taking CNS depressants, including opioids. Monitor for symptoms of respiratory depression.
Seizure
•
Do not discontinue abruptly in patients with seizure disorder. Taper gradually to minimize the risk of seizures.
Somnolence
•
Use extreme caution in patients performing activities requiring mental alertness, such as driving or operating machinery.
Sudden unexplained death
•
Use caution in patients with seizure disorder.
Suicidal ideation
•
Maintain a high level of suspicion, as an increased risk of suicidal thoughts and behavior has been reported in patients receiving gabapentin. Monitor closely for suicidality and unusual changes in behavior.
Specific populations
Renal impairment
CrCl ≥ 60 mL/min
•
Maximal dose of 900-3,600 mg per day, in 3 divided doses.
CrCl 30-60 mL/min
•
Maximal dose of 400-1,400 mg per day, in 2 divided doses. Do not exceed frequency of BID.
CrCl 15-30 mL/min
•
Maximal dose of 200-700 mg per day. Do not exceed frequency of once daily.
CrCl < 15 mL/min
•
Maximal dose of 100-300 mg per day. Do not exceed frequency of once daily.
Renal replacement therapy
Continuous renal replacement
•
Dose as in CrCl < 15 mL/min.
Intermittent hemodialysis
•
Administer an additional dose after each session. Dose as in CrCl < 15 mL/min.
Peritoneal dialysis
•
Dose as in CrCl < 15 mL/min.
Hepatic impairment
Any severity
•
Use acceptable. No dose adjustment required.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: B3
•
Use only if benefits outweigh potential risks. Evidence of fetal harm in animals. Enroll patients in a dedicated pregnancy outcome monitoring registry. The risk of having a child with a congenital defect as a result of antiepileptic medication is far outweighed by the dangers to the mother and fetus of uncontrolled epilepsy; folic acid supplementation (5 mg) should be started 4 weeks prior to and continued for 12 weeks after conception.
•
Women of childbearing potential should receive counseling on the risk of fetal abnormalities with the use of antiepileptic drugs (AEDs) during pregnancy; AEDs should generally be continued during pregnancy utilizing monotherapy at the lowest effective dose as this has been shown to minimize risks of fetal abnormalities compared to combination AED therapy.
Breastfeeding
Use only if benefits outweigh potential risks.
Low levels in breastfed infants (5-25%).
Unlikely to cause adverse effects in breastfed infants.
Adverse reactions
Very common > 10%
•
Ataxia, dizziness, headache
Common 1-10%
•
Amblyopia, bone fracture, bronchitis, conjunctivitis, ↓ WBC count, dysarthria, ↑ blood glucose, nasopharyngitis, pharyngitis, nystagmus, peripheral edema, abdominal pain, asthenia, back pain, blurred vision, constipation, cough, depression, diarrhea, diplopia, dry mouth, dyspepsia, erectile dysfunction, fatigue, flatulence, gait disturbance, loss of balance, myalgia, incoordination, ↑ appetite, insomnia, memory impairment, memory impairment, nausea, pruritus, skin rash, somnolence, vertigo, vomiting, weight gain, respiratory tract infections, tremor
Unknown frequency
•
Anaphylaxis, angioedema, bullous pemphigoid, cardiomyopathy, DRESS syndrome, ↓ serum sodium, erythema multiforme, gynecomastia, jaundice, ↑ liver enzymes, ↓ libido, emotional lability, restlessness, ↑ serum CK, suicidal ideation, amenorrhea, ↑ serum creatinine, respiratory depression, rhabdomyolysis, myositis, Stevens-Johnson syndrome
Interactions
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