Name: Gabapentin (Neurontin)
Class: Antiepileptic Agent (Complex-Partial)
Mechanism: Unknown. Transp. into brain. Binds to unique specific receptor. Appears to inhib Na+-med. sustained firing. brain GABA levels.
Absorption: Oral ® 60% bioavailability. Actively absorbed by l-amino acid transport system. Dose-dependent decrease in absorption at doses > 600 mg.
Dist.: <10%>
Metabolism.:
Excret. t½: Almost 100% excret. unchanged by kidney (µ to creatinine clearance). 5-7 hr (adults).
Toxicity/S.E.s: Somnolence, dizziness, ataxia, fatigue, nystagmus, headache, tremor, diplopia, n/v. No drug interactions.
Utility: Adj. therapy of partial seizures, including secondarily generalized. Management of neuropathic pain (off-label).
Special Features: Cleanest (regarding drug interactions) antiepileptic drug. Low toxicity profile. However, there is limited clinical experience w/it against other seizure types, limited experience w/monotherapy, and it has a short t½.