Epileptic Medchem Flashcards
Phenobarbital:
Drug class
Target
Side effect(s)
metabolism
inducer/inhibitor of?
barbiturate
GABA potentiation
sedation
p-hydroxylation via cyp2c9/2c19
inducer of p450s and some UGTs
Primidone:
Drug class
Side effect(s)
barbiturate
some sedation due to oxidation into phenobarbital
Phenytoin:
Drug class
Target
Side effect(s)
metabolism
inducer/inhibitor of?
metabolites
hydantoin
Na+ channel blocker
associated with steven’s johnson syndrome
CYP2C9/2C19
inducer of p450s and UGTs
p-hydroxylated metabolite and arene oxide intermediate
Fosphenytoin sodium:
Drug class
metabolism
hydantoin (prodrug)
metabolized by phosphatase into its active form phenytoin
Ethosuximide:
Drug class
Target
Side effect(s)
metabolism
inducer/inhibitor of?
metabolites
(Note: Ethosuximide can be identified by what structural feature?)
succinimide
T-type Ca2+ blocker
aplastic anemia, hepatotoxicity
hydroxylation via CYP3A4/2E1
Has only 1 Ntrogen
Valproic acid
Target
Side effect(s)
metabolism
inducer/inhibitor of?
Na+ channel blocker
hepatotoxicity
direct glucuronidation (inactive) and oxidation to active metabolite
inhibit 2C9, UGTs, and epoxide hydrolase
Carbamazepine
Target
Side effect(s)
metabolism
inducer/inhibitor of?
Sodium channel blocker
aplastic anemia, stevens-johnson syndrome
metabolized by 3A4 into Carbamazepine 10,11-epoxide (active) and further metabolized by epoxide hydrolase into Carbamazepine 10,11-diol (inactive)
inducer of p450s, UGTs (it is an autoinducer)
Oxcarbazepine
metabolism
inducer/inhibitor of?
reduction to non-hydroxy metabolite
inhibits p450 metabolism
Eslicarbazepine acetate
metabolism
inducer/inhibitor of?
prodrug which undergoes rapid esterase hydrolysis into Eslicarbazepine (active)
inhibits p40 metabolism
GABA metabolism pathway =>
L-Glutamate metabolized by GAD into GABA which is metabolized by GABA-AT into SSA which is metabolized by SSA-DH into Succinate
which 2 drugs inhibit the GABA metabolism pathway?
valproate and vigabatrin
Vigabatrin
Target
Side effect(s)
inducer/inhibitor of?
Irreversible inhibitor of GABA aminotransferase
permanent vision loss
2C9
Felbamate:
Side Effects
aplastic anemia and hepatic failure
Lamotrigine
major route of metabolism
minor route of metabolism
metabolite
glucuronidation
p450
reactive arene oxide metabolite