Antiseizure Drugs

Question 1

the oldest organic antiseizure drug; GABA agonist; use for partial and generalized tonic-clonic; may worsen symptoms of absence, atonic attacks, and infantile spasms

Answer 1

phenobarbital

Question 2

benzodiazepine; generalized tonic-clonic status epilepticus; tolerance after repeated use

Answer 2

diazepam

Question 3

benzodiazepine; more effective and longer lasting vs. diazepam; tolerance

Answer 3

lorazepam

Question 4

benzodiazepine: effective against absence and myoclonic; long acting and highly potent; tolerance

Answer 4

clonazepam

Question 5

benzodiazepine: add-on treatment of complex partial seizures in adults

Answer 5

clorazepate

Question 6

1st non-sedative antiepileptic drug; prolongs the inactivated state of Na channels; partial and generalized tonic-clonic; highly bound to plasma protein

Answer 6

phenytoin

Question 7

more soluble prodrug that is converted to phenytoin in the blood

Answer 7

fosphenytoin

Question 8

elimination of low doses of phenytoin: … order kinetic

Answer 8

1st

Question 9

elimination of higher doses of phenytoin: … order kinetic

Answer 9

zero

Question 10

what drug displaces phenytoin from plasma proteins

Answer 10

valproic acid

Question 11

side effects of which drug?: diplopia and ataxia; gingival hypertrophy; hirsutism; peripheral neuropathy; osteomalacia; teratogenicity (fetal hydantoin syndrome)

Answer 11

phenytoin

Question 12

related to TCA; prolong the inactivated state of Na channels; partial and generalized tonic-clonic; not for absence and myoclonic seizures

Answer 12

carbamazepine

Question 13

2 potentially fatal side effects of carbamazepine

Answer 13

aplastic anemia and agranulocytosis

Question 14

analog of carbamazepine; less potent with improved toxicity profile

Answer 14

oxcarbazepine

Question 15

enhances slow inactivation of Na channels; binds to collapsin-response mediator protein–> prevent excitatory axonal sprouting; partial with/without secondary generalization

Answer 15

lacosamide

Question 16

enhances slow inactivation of Na channels; add-on treatment of Lennox-Gastaut syndrome

Answer 16

rufinamide

Question 17

inhibition of GABA uptake (GAT-1); significant binding to plasma proteins; add-on treatment of partial seizures

Answer 17

tiagabine

Question 18

an irreversible inhibitor of GABA aminotransferase; used for partial, infantile spasms, reserved for patients refractory to other drugs; side effect: permanent bilateral vision loss

Answer 18

vigabatrin

Question 19

analog of GABA; add-on treatment of partial with or w/o secondarily generalized

Answer 19

pregabalin

Question 20

analog of GABA; add-on treatment of partial and generalized tonic-clonic

Answer 20

gabapentin

Question 21

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

Answer 21

lamotrigine

Question 22

Lamotrigine is metabolized by …

Answer 22

UGT

Question 23

valproic acid … UGT

Answer 23

inhibits

Question 24

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

Answer 24

topiramate

Question 25

"pure petit mal" drug; absence seizure; blocks T-current: inhibits 3-Hz activity; valproic acid decrease clearance; side effect of leukopenia

Answer 25

ethosuximide

Question 26

blocks T-current; prolongs the inactivated state of Na channels; increase GABA levels; used for absence, myoclonic, partial and generalized tonic-clonic (broad spectrum)

Answer 26

valproic acid

Question 27

primarily metabolized by UGT with significant binding to plasma proteins; inhibits metabolism of CYP3A, CYP2C9 and UGT

Answer 27

valproic acid

Question 28

valproic acid displaces ... and ... from plasma proteins

Answer 28

phenytoin and lamotrigine

Question 29

side effects of which drug?: severe hepatitis and pancreatitis; teratogenicity (spina bifida); inhibition of platelet aggregation w/ gingival bleeding

Answer 29

valproic acid

Question 30

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

Answer 30

levetiracetam

Question 31

activation of voltage gated K channels; add on treatment for partial seizures in adults; causes psychosis in some pts

Answer 31

retigabine

Question 32

non competitive antagonist of AMPA receptors; add on for partial

Answer 32

perampanel

Question 33

Na channel blocker; analog of oxcarbazepine; add on for partial

Answer 33

eslicarbazepine