Epileptic Medchem Flashcards

1
Q

Phenobarbital:
Drug class
Target
Side effect(s)
metabolism
inducer/inhibitor of?

A

barbiturate
GABA potentiation
sedation
p-hydroxylation via cyp2c9/2c19
inducer of p450s and some UGTs

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2
Q

Primidone:
Drug class
Side effect(s)

A

barbiturate
some sedation due to oxidation into phenobarbital

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3
Q

Phenytoin:
Drug class
Target
Side effect(s)
metabolism
inducer/inhibitor of?
metabolites

A

hydantoin
Na+ channel blocker
associated with steven’s johnson syndrome
CYP2C9/2C19
inducer of p450s and UGTs
p-hydroxylated metabolite and arene oxide intermediate

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4
Q

Fosphenytoin sodium:
Drug class
metabolism

A

hydantoin (prodrug)
metabolized by phosphatase into its active form phenytoin

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5
Q

Ethosuximide:
Drug class
Target
Side effect(s)
metabolism
inducer/inhibitor of?
metabolites
(Note: Ethosuximide can be identified by what structural feature?)

A

succinimide
T-type Ca2+ blocker
aplastic anemia, hepatotoxicity
hydroxylation via CYP3A4/2E1
Has only 1 Ntrogen

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6
Q

Valproic acid
Target
Side effect(s)
metabolism
inducer/inhibitor of?

A

Na+ channel blocker
hepatotoxicity
direct glucuronidation (inactive) and oxidation to active metabolite
inhibit 2C9, UGTs, and epoxide hydrolase

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7
Q

Carbamazepine
Target
Side effect(s)
metabolism
inducer/inhibitor of?

A

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)

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8
Q

Oxcarbazepine
metabolism
inducer/inhibitor of?

A

reduction to non-hydroxy metabolite
inhibits p450 metabolism

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9
Q

Eslicarbazepine acetate
metabolism
inducer/inhibitor of?

A

prodrug which undergoes rapid esterase hydrolysis into Eslicarbazepine (active)
inhibits p40 metabolism

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10
Q

GABA metabolism pathway =>

A

L-Glutamate metabolized by GAD into GABA which is metabolized by GABA-AT into SSA which is metabolized by SSA-DH into Succinate

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11
Q

which 2 drugs inhibit the GABA metabolism pathway?

A

valproate and vigabatrin

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12
Q

Vigabatrin
Target
Side effect(s)
inducer/inhibitor of?

A

Irreversible inhibitor of GABA aminotransferase
permanent vision loss
2C9

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13
Q

Felbamate:
Side Effects

A

aplastic anemia and hepatic failure

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14
Q

Lamotrigine
major route of metabolism
minor route of metabolism
metabolite

A

glucuronidation
p450
reactive arene oxide metabolite

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