Antiepileptics Flashcards
Drugs that Enhance Na+ Channel mediated inhibition. - promote Na channel inactivation conformation.
Phenytoin, Carbamazepine, Valproic Acid, Lamotrigine, and Lacosamide
Strong specificity for FOCAL and SECONDARILY GENERALIZED seizures, not absence seizures
Phenytoin, Carbamazepine, Lamotrigine, and Lacosamide
Major drug of use in FOCAL and TONIC-CLONIC seizures. Use dependent slows recovery of Na channel to resting state.
Phenytoin
metabolized by liver P450. P450 inhibitors – cimetidine, isoniazid, disulfiram – increase serum levels and toxicity
Phenytoin
Order of DOC for ABSENCE seizures.
Ethosuximide, Valproic Acid, Lamotrigine, then Clonazepam.
Most teratogenic AEDs
Valproic Acid, then Carbamazepine
AEDs and pregnancy recommendations
single agent at lowest possible dose. 90% normal pregnancies.
Tx of Status Epilepticus
ABCs (airway and vascular access) then Lorazepam or Diazepam, Fosphenytoin and if unsuccessful an additional dose, then phenobarbital and transfer to ICU.
Potent agent with lack of sedative effects. Inhibits NMDA-NR2B. Use restricted to REFRACTIVE EPILEPSY. - associated with aplastic anemia and liver failure.
Felbamate
Tx of FOCAL seizures and Lennox-Gastaut syndrome (refractive epilepsy). Na channel inhibition.
Rufinamide
drugs that inhibit glutamate receptors. Neither is routinely used.
Felbamate and Rufinamide
DOC for FOCAL seizures. Better option to phenytoin in patients with potential drug interactions.
Carbamazepine
Na+ channel drug that is contraindicated in children – Stevens-Johnsons Syndrome, Toxic epidermal necrosis.
Lamotrigine
Adjunctive therapy to FOCAL seizures and alternate to Phenytoin and Carbamazepine with fewer drug interactions.
Lacosamide
Drugs that block T-type Ca2+ channels. Specific to ABSENCE seizures.
Ethosuximide and Valproic Acid…..Clonazepam
Most effective for Generalized epilepsy with mixed seizure types. Alternate to Phenytoin and Carbamazepine in FOCAL seizure Tx.
Valproic Acid
Most serious side effect of Valproic Acid.
Hepatotoxicity
Drugs that block High Voltage Ca channels. Impedes transmitter release – pleiotrophic effects.
Gabapentin and Pregabalin
Primarily for FOCAL seizures with or w/out secondary generalization and GENERALIZED seizures other than absence.
Gabapentin and Pregabalin
Structural analogue of GABA. Not generally first line – not as effective. Very few drug interactions
Gabapentin
Pt with Hepatic impairment. Adjunct to FOCAL seizures and supresses just about everything. Preferable to Gabapentin.
Pregabalin
Drugs that enhance GABA mediated inhibition.
Benzodiazepines, Phenobarbital, Vigabatrin, Tiagabine
Used to abort seizures acutely – dizziness, ataxia, drowsiness. Suited for FOCAL and TONIC-CLONIC seizures.
Benzodiazepines – Diazepam, Lorazepam, and Midazolam
Can exacerbate absense seisure. Tx – of FOCAL, TONIC-CLONIC, and acute, resistant seizures of all types. Use falling out of favor.
Phenobarbital
Inhibits GABA-transaminase – increasing brain GABA.
Vigabatrin
Infantile spasms and refractory focal epilepsy. Pts in treatment should undergo baseline and routine visual field testing.
Vigabatrin
Potentiates actions of GABA modulators – BZ Barbs and EtOH
Tiagabine