USMLE Step 1

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Pharmacology

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Antiepileptics

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Gabapentin

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Summary

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Key Points

  • Gabapentin
    • Mechanism
      • Primarily inhibits high-voltage-activated Ca+ channels
        • Inhibits voltage-gated Ca2+ channel via α2δ subunit
      • Originally designed as a GABA analog
        • Hence the name, “GABA-pentin”
    • Clinical Use
      • Peripheral neuropathy (esp. postherpetic neuralgia)
        • Severe pain after episodes of shingles/varicella
        • Used along with pregabalin
      • Partial (focal) seizures
        • Considered a narrow-spectrum anti-epileptic
    • Adverse Effects
      • Sedation, ataxia