Name Gabapentin
Classes Central Nervous System Agent
Anticonvulsant / Antiepileptic Agent
Psychotherapeutic Agent
GABA Analogue
Diseases CNS Disorder
Seizure
Shingles

Gabapentin

Gabapentin belongs to a class of drugs called the anticonvulsants. It is unknown exactly how gabapentin produces its analgesic and antiepileptic effects. Gabapentin has a similar structure to the neurotransmitter gamma-aminobutyric acid (GABA), but it has no effect on GABA binding, uptake, or degradation. In vitro studies have shown that gabapentin binds to the 2 subunit of voltage-activated calcium channels with high affinity; however, the relationship of this binding to gabapentin's therapeutic effects is unknown.

 

Gabapentin is indicated for:

  • Postherpetic neuralgia in adults
  • Adjunctive therapy in the treatment of partial onset seizures, with and without secondary generalization, in adults and pediatric patients 3 years and older with epilepsy

 

Postherpetic Neuralgia 

  • Dose can be titrated up as needed to a dose of 1800 mg/day 
  • Day 1: Single 300 mg dose 
  • Day 2: 600 mg/day (i.e., 300 mg two times a day)
  • Day 3: 900 mg/day (i.e., 300 mg three times a day)

Epilepsy with Partial Onset Seizures 

  • Patients 12 years of age and older: starting dose is 300 mg three times daily; may be titrated up to 600 mg three times daily 
  • Patients 3 to 11 years of age: starting dose range is 10 to 15 mg/kg/day, given in three divided doses; recommended dose in patients 3 to 4 years of age is 40 mg/kg/day, given in three divided doses; the recommended dose in patients 5 to 11 years of age is 25 to 35 mg/kg/day, given in three divided doses. The recommended dose is reached by upward titration over a period of approximately 3 days 
  • Dose should be adjusted in patients with reduced renal function

 

Most common adverse reactions were: 

  • Postherpetic neuralgia: Dizziness, somnolence, and peripheral edema 
  • Epilepsy in patients >12 years of age: Somnolence, dizziness, ataxia, fatigue, and nystagmus 
  • Epilepsy in patients 3 to 12 years of age: Viral infection, fever, nausea and/or vomiting, somnolence, and hostility

 

  • Drug Reaction with Eosinophilia and Systemic Symptoms (Multiorgan hypersensitivity):  If an alternative etiology cannot be established, the treatment should be discontinued.
  • Anaphylaxis and Angioedema: Stop immediately and evaluate the patient.
  • If Gabapentin is abruptly discontinued, patients with seizure disorders may experience an increase in seizure frequency.
  • Driving Impairment; Somnolence/Sedation and Dizziness: Warn patients not to drive until they have gained sufficient experience to assess whether their ability to drive or operate heavy machinery will be impaired
  • Suicidal Behavior and Ideation: Suicidal thoughts/behavior should be monitored.

 

Contraindication

Contraindicated in patients with known hypersensitivity to gabapentin.