gabapentin

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


Best Augmenting Agents for AEs

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Feb 16, 2017 | Posted by in PHARMACY | Comments Off on gabapentin

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