Gabapentinoids

Summary

Gabapentinoids are a class of drugs that includes gabapentin and pregabalin. They work by blocking voltage-dependent calcium channels. Clinically, gabapentinoids are used as narrow-spectrum antiepileptic drugs to treat focal seizures. They are also effective at treating neuropathic pain. Side effects of gabapentinoids include weight gain, ataxia, dizziness, and sedation.

Key Points

• Gabapentinoids
  • Drug Names
    • Gabapentin
    • Pregabalin
  • Mechanism
    • Block voltage-dependent calcium channels
      • Inhibits voltage-gated calcium channel via α2δ subunit
    • Originally designed as GABA analogs
      • Hence the “GABApentin” and “preGABAlin” names
  • Clinical Use
    • Treats seizures (antiepileptic)
      • Narrow spectrum
      • Treats focal (partial) seizures
    • Treats neuropathic pain
      • May be used to treat neuropathic pain in diabetic neuropathy or postherpetic neuralgia (e.g. after shingles)
  • Side Effects
    • Sedation
    • Dizziness
    • Ataxia
    • Weight Gain