pharm of anticonvulsants Flashcards
Fosphenytoin MOA
block voltage gated Na+ channels -> inhibit rapid repetitive AP’s
also secondarily decrease glutamate release and increase GABA release
Fosphenytoin ADME, therapeutics
prodrug (phenytoin); no active metabolites
highly bound to plasma proteins
IV and IM or oral with phenytoin
generalized tonic-clonic and partial seizures
Fosphenytoin AE’s and drug interaction
cardiovascular risk associated with rapid infusion
nystagmus, diplopia, gingival hyperplasia, ataxia, hirsutism
interactions with carbamazepine and topiramate
Ethosuximide MOA
blocks thalamic T-type Ca++ channels
Ethosuximide ADME, therapetuics
oral
half life ~40 hours
absence seizure
Ethosuximide AE’s and drug interactions
GI distress, lethargy, HA, uticaria valproic acid (decrease in metabolism, increase in steady-state concentration)
Levetiracetam MOA
binds synaptic vesicular protein (SV2A) to modulate glutamate and GABA release
Levetiracetam ADME, therapeutics
oral or IV
adjunctive
primary partial seizures in adults and children > 4yo
myoclonic seizures of juvenile myoclonic epilepsy
primary generalized epilepsy children > 6 yo
Barbiturates MOA
phenobarbital
facilitates GABA A activation -> increased DURATION of Cl- channel opening -> reduced excitation
Barbiturates ADME, therapeutics
IM or IV; half life ~4-5 days
partial seizures, tonic-clonic seizures, every seizure type for attacks that are hard to control
Barbiturates AE and drug interactions
respiratory and cardiac depression, tolerance and dependence, sedation, cognitive dysfunction
interactions: other sedative-hypnotics (alcohol), CNS depressants, increase CYP-450 enzymes
contraindication: porphyria (improperly made heme)
Stevens-Johnson syndrome
ethosuximide, phenytoin, carbamazepine
starts off flu-like and progresses to red / purple rash -> epidermal necrosis and sloughing
special toxicology of antiseizure drugs
stevens-johnson syndrome
teratogenicity
anticonvulsant hypersensitivity syndrome
antiseizure teratogenicity
fetal hydantoin syndrome: phenytoin, carbamazepine, phenobarbitol increased chances of malformation spina bifida: valproic acid
anticonvulsant hypersensitivity syndrome
fever, rash, organ (liver, kidney, blood) toxicity
higher risk with phenobarbitol, phenytoin, carbamazepine