drugs for epilepsy Flashcards
what are the 3 general mechanisms of action for anti-epilepsy drugs?
- promote the inactivated state of voltage gated Na+ channels
- Pre or post synaptic enhancement of GABA medicated inhibition
- inhibition of T-type voltage-activated Ca2+ channels (absence seizures)
FDA has issued a warning of what adverse effect with the use of anticonvulsants?
suicidal ideation
- 2 fold increase
- monitor all pts for emerging depression/suicidal thoughts
- educate pts about risks
- use minimum drug levels for epilepsy
current drugs control seizures only in what percentage of pts?
50%
the adverse effects of anti epileptic drugs can have what effect on pts?
responsible for limited pt adherence
instead of adding a drug to an exisint anticonvulsant monotherapy regimen, what should you do?
substitute rather than additive treatment
MOA of carbamazepine
blocks voltage gated Na channels and decreases glutamate release
MOA of clonazepam
enhance GABA-A receptor responses
MOA ethosuximide
decreases T-Type Ca2+ currents (used for absence seizures)
MOA felbamate
blocks NMDA receptors; increase GABA
MOA gabapentin
blocks alpha-2 delta-1 subunit of Ca2+ channels
MOA of lacosamide
blocks Na+ channels
MOA lamotrigene
blocks Na+ channels
MOA oxcarbazepine
blocks Na+ channels, possibly increases K+ & decreases Ca2+ effects
MOA Phenytoin
blocks voltage gated Na+ channels
MOA pregablin
blocks alpha-2 delta-1 subunit of Ca2+ channel
MOA Topiramate
blocks Na+ channels; increases K+ current, increases GABA; decreases glutamate activity
MOA valproate
increases GABA activity; also decreases Na+ channnels
MOA zonisamide
blocks Na+ channels, & decreases T-type Ca2+ actions
the anti-epileptic drug have limited protein binding except which two drugs?
phenytoin & valproate
which antiepileptic drug accumulates in erythrocytes?
zonisamide
which type of formulation for anti-epileptic drugs promotes adherence?
slow release products (fewer doses / day)
what happens to the half-life of carbamazepine as treatment progresses?
the half life decreases due to an increased rate of hepatic metabolism
which two anti-epileptic drugs are not metabolized?
gabapentin & pregabalin
which antiepileptic drug has no CYP activity and is metabolized by uridine glucuronosyl transferasewith subsequent induction of UGT (hint its metabolites are eliminated in urine)?
lamotrigine
which antiepileptic drug is metabolically conjugated, decreases CYP2C19& increases CYP3A4/5?
OXCARBAZEPINE
what is the only antiepileptic drug that is eliminated in the stool?
phenytoin
Phenytoin is metabolized by what CYP Enzymes?
CYP2C9»CYP2C19
Routine monitoring of serum drug levels is required with what 3 drugs?
carbamazepine
Phenytoin
Valproate
what should the physician do for a pt experiencing good seizure control and no signs or symptoms of significant drug toxicity, despite serum drug levels being high?
physician doesn’t have to reduce drug dose, but rather use clinical presentation to guide treatment
which two drugs are weak carbonic anhydrase inhibitors?
topiramate/zonisamide