Antiseizure Drugs Flashcards
the oldest organic antiseizure drug; GABA agonist; use for partial and generalized tonic-clonic; may worsen symptoms of absence, atonic attacks, and infantile spasms
phenobarbital
benzodiazepine; generalized tonic-clonic status epilepticus; tolerance after repeated use
diazepam
benzodiazepine; more effective and longer lasting vs. diazepam; tolerance
lorazepam
benzodiazepine: effective against absence and myoclonic; long acting and highly potent; tolerance
clonazepam
benzodiazepine: add-on treatment of complex partial seizures in adults
clorazepate
1st non-sedative antiepileptic drug; prolongs the inactivated state of Na channels; partial and generalized tonic-clonic; highly bound to plasma protein
phenytoin
more soluble prodrug that is converted to phenytoin in the blood
fosphenytoin
elimination of low doses of phenytoin: … order kinetic
1st
elimination of higher doses of phenytoin: … order kinetic
zero
what drug displaces phenytoin from plasma proteins
valproic acid
side effects of which drug?: diplopia and ataxia; gingival hypertrophy; hirsutism; peripheral neuropathy; osteomalacia; teratogenicity (fetal hydantoin syndrome)
phenytoin
related to TCA; prolong the inactivated state of Na channels; partial and generalized tonic-clonic; not for absence and myoclonic seizures
carbamazepine
2 potentially fatal side effects of carbamazepine
aplastic anemia and agranulocytosis
analog of carbamazepine; less potent with improved toxicity profile
oxcarbazepine
enhances slow inactivation of Na channels; binds to collapsin-response mediator protein–> prevent excitatory axonal sprouting; partial with/without secondary generalization
lacosamide
enhances slow inactivation of Na channels; add-on treatment of Lennox-Gastaut syndrome
rufinamide
inhibition of GABA uptake (GAT-1); significant binding to plasma proteins; add-on treatment of partial seizures
tiagabine
an irreversible inhibitor of GABA aminotransferase; used for partial, infantile spasms, reserved for patients refractory to other drugs; side effect: permanent bilateral vision loss
vigabatrin
analog of GABA; add-on treatment of partial with or w/o secondarily generalized
pregabalin
analog of GABA; add-on treatment of partial and generalized tonic-clonic
gabapentin
prolong inactivated state of Na channels; inhibit voltage gated Ca channels; inhibit release of glutamate; add-on or monotherapy; used for partial, Lennox-Gastaut syndrome; side effect: Stevens-Johnson syndrome
lamotrigine
Lamotrigine is metabolized by …
UGT
valproic acid … UGT
inhibits
structurally different from all other antiseizure drugs; prolong inactivated state of Na channels; inhibit voltage gated Ca channels; agonist of GABA receptor; antagonist of kainate receptors; used for partial and generalized tonic-clonic and Lennox-Gastaut syndrome; its teratogenic
topiramate
“pure petit mal” drug; absence seizure; blocks T-current: inhibits 3-Hz activity; valproic acid decrease clearance; side effect of leukopenia
ethosuximide
blocks T-current; prolongs the inactivated state of Na channels; increase GABA levels; used for absence, myoclonic, partial and generalized tonic-clonic (broad spectrum)
valproic acid
primarily metabolized by UGT with significant binding to plasma proteins; inhibits metabolism of CYP3A, CYP2C9 and UGT
valproic acid
valproic acid displaces … and … from plasma proteins
phenytoin and lamotrigine
side effects of which drug?: severe hepatitis and pancreatitis; teratogenicity (spina bifida); inhibition of platelet aggregation w/ gingival bleeding
valproic acid
binds to synaptic vesicular protein SV2A and regulates release of glutamate and GABA; add-on therapy for partial, primary generalized tonic-clonic. myoclonic due to juvenile myoclonic epilepsy
levetiracetam
activation of voltage gated K channels; add on treatment for partial seizures in adults; causes psychosis in some pts
retigabine
non competitive antagonist of AMPA receptors; add on for partial
perampanel
Na channel blocker; analog of oxcarbazepine; add on for partial
eslicarbazepine
