Class
- Antiepileptic drug (AED)
Gabapentin
Commonly Prescribed for
(FDA approved in bold)
- Partial-onset seizures with and without secondary generalization (adjunctive for adults and children 12 and older)
- Partial-onset seizures in children 3 and older
- Pain associated with post-herpetic neuralgia
- Neuropathic pain
- Migraine prophylaxis
- Facial pain
- Allodynia and hyperalgesia
- Fibromyalgia
- Bipolar disorder
- Generalized anxiety disorder
- Alcohol and drug withdrawal
- Insomnia
Gabapentin
How the Drug Works
- Structural analog of gamma-aminobutyric acid (GABA) which binds at the alpha-2-delta subunit of voltage-sensitive calcium channels and reduces calcium influx. Changes calcium channel function but not as a blocker
- Reduces release of excitatory neurotransmitters, and decreases brain glutamate and glutamine levels
- Increases plasma serotonin levels
- Inactive at GABA receptors and does not affect GABA uptake or degradation
Gabapentin
How Long Until It Works
- Seizures – 2 weeks
- Pain/Anxiety – days-weeks
Gabapentin
If It Works
- Seizures – goal is the remission of seizures. Continue as long as effective and well-tolerated. Consider tapering and slowly stopping after 2 years without seizures, depending on the type of epilepsy
- Pain – goal is reduction of pain. Usually reduces but does not cure pain and there is recurrence off the medication. Consider tapering for conditions that may improve over time, i.e., post-herpetic neuralgia or migraine
Gabapentin
If It Doesn’t Work
- Increase to highest tolerated dose
- Epilepsy: Consider changing to another agent, adding a second agent or referral for epilepsy surgery evaluation
- Pain: If not effective in 2 months, consider stopping or using another agent
Gabapentin
Best Augmenting Combos for Partial Response or Treatment-Resistance
- Epilepsy: No major drug interactions with other AEDs. Using in combination may worsen CNS side effects
- Neuropathic pain: Can use with tricyclic antidepressants, SNRIs, other AEDs or opiates to augment treatment response. Gabapentin usually decreases opiate use
- Anxiety: Usually used as an adjunctive agent with SSRIs, SNRIs, monoamine oxidase (MAO) inhibitors or benzodiazepines
Gabapentin
Tests
- No regular blood tests are recommended
Adverse Effects (AEs)
Gabapentin
How Drug Causes AEs
- CNS AEs are probably caused by interaction with calcium channel function
Gabapentin
Notable AEs
- Sedation, dizziness, fatigue, ataxia
- Weight gain, nausea, constipation, dry mouth
- Blurred vision, peripheral edema
Gabapentin
Life-Threatening or Dangerous AEs
- None
Gabapentin
Weight Gain
- Not unusual
Gabapentin
Sedation
- Common
- May wear off with time but can limit titration
Gabapentin
What to Do About AEs
- Decrease dose or take a higher dose at night to avoid sedation
- Switch to another agent
Gabapentin