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Class MOA Anti-epileptic Prolonged inactivation of Na+ channels No effect on glutamate or GABA neurotransmission Very high lipid solubility Oxidized to 10,11-epoxide which is as active as parent molecule t1/2 = 10-20h (high variability between patients) Phenobarbital or phenytoin reduces t1/2 to 9h Lots of DDIs due to metabolism through P450 system
Pharmacokinetics
Pharmacodynamics Clinical Use Initiation of therapy of simple and complex partial seizures Initiation of therapy of tonic-clonic seizures Therapeutic concentrations: 6-12 g/mL CNS side-effects prominent above 9 g/mL Add phenytoin if treatment unsatisfactory after a month or more Start 200 mg BID and titrate to 600-1200 mg/d Toxicity Drowsiness Diplopia Ataxia Aplastic anemia (1 in 200,000) Agranulocytosis Transient leucopenia Transient changes in hepatic enzymes Teratogen Primary generalized epilepsy (may induce status epilepticus)
Side Effects
Contraindications