Pharmacology - Epilepsy Flashcards
true or false
seizures are generally self-limiting
true
focal seizures are also known as ___ seizures
partial
some neonates are not treated with antiepileptics but with….
steroids
for isoniazid seizures use pyridoxial
***perampanel MOA
specific AMPA receptor antagonist
name 6 drugs that block voltage gated sodium channel
phenytoin
fospheyntoin
carbamazepine
oxcarbazepine
eslicarbazepine
zonisamide
name a drug that blocks voltage gated sodium channels AND enhances GABA release
cenobamate
what drug inhibits GABA transaminase with little - no metabolism?
vigabatrin
what drug inhibits GAT-1
tigabine
3 MOA of valproate (depakote)
- inhibits GABA transaminase
- blocks voltage gated sodium channels
- downregulates NMDA receptors
name 3 benzodiazepines
diazepam
lorazepam
clonazepam
**name 2 drugs that interact with SV2A proteins and what this does
inhibits repetitive burst firing of neurons
leviteracetam, brivaracetam
** AE of levitiracetam and briviracetam, particularly in kids
increased aggression
*MOA retigabine
neuronal KCNQ/Kv7 potassium channel opener
ethosuximide MOA
blocks T-type calcium channels
MOA of gabapentin and pregabalin
inhibits the alpha, delta subunits of voltage gated calcium channels
true or false
both gabapentin and pregabalin undergo little-no metabolism
true
**MOA phenytoin
blocks voltage gated sodium channels
*phenytoin dosing concern
dose correct WEEKLY
does not have a stable half life and follows non linear kinetics. also highly protein bound
true or false
fosphenytoin has much better kinetics than phenytoin
true, but also is a lot more money
what kind of seizures can phenytoin be used in
all except absence
**phenytoin inhibits both the ___ and ____ of seizures
spread and initiation
(inhibition of spread is greater)
if action potential DOES occur, prevents the spread
*AE of phenytoin
osteoporosis/osteomalacia (rickets)
wide array of blood disorders - have to look at CBC
SJS
encephalopathy (ataxia, slurred speech) - it’s a cerebellar toxin!
DISLE (drug induced lupus)
can lead to dysarrhtyhmias and SA/AV blocks (bc class IB antiarrhythmic)
lethargy
phenytoin DDI concerns
CYP2C9, 2C29
highly protein bound
1st AE that tends to show up in a person with phenytoin toxicity
horizontal gaze nystagmus
as phenytoin concentration gets above ______, toxicities begin
what to look for 1st
20mg/L
nystagmus
30-40 = ataxia
40-50 = lethargy
most antiepileptics ___ the CNS
what effect can this have in kids
depress the CNS
drugs like phenytoin can impair learning and memory in kids
*dihydroergotamine
false
**MOA carbamazepine
blocks sodium channels AND calcium channels
the MODERN antiepileptics mainly block what
calcium channels
common AE of carbamazepine
hyponatremia
true or false
eslicarbazepine is a prodrug
true
AE cenobamate (XCOPRI)
DRESS
drug induced eosinophilic syndrome
**lamotrigine MOAs
-blocks sodium channels
-suppresses release of glutamate and aspartate (excitatory amino acids)
lamotrigine concern
SJS if you rapidly dose escalate
*4 antiepileptics metabolized by CYP3A4
carbamazepine
zonisimide
ethosuximide
perampenal
**MOA valproate
-blocks GABA transaminase
-weak block on sodium channels
also downregulates NMDA receptors
*AE valproate
is it teratogenic?
weight gain/loss, increased or decreased appetite, mood swings
YES teratogenic
vigabatrin MOA
inhibits GABA transminase
what enzyme metabolizes phenobarbital
CYP2C19
tiagabine MOA
inhibits GABA reuptake - does not inhibit GABA transaminase
**ethosuximide MOA
inhibits voltage gated calcium channels
ethosuximide may worsen what kind of seizures
tonic-clonic
phenobarbital is an enzyme inducer or inhibitor
inducer
*MOA gabapentin
multi moa, but MAIN is blocking voltage gated calcium channels
but also elevates GABA and blocks sodium channel (possible select all that apply and the answer is all of the above)
advantage of pregabalin over gabapentin in diabetics
pregabalin works better for them for peripheral neuropathy
***MOA lacosamide
enhances the slow inactivation of voltage gated sodium channels without affecting the fast inactivation of sodium channels
*lacosamide modulates ____. this preventws what
modulates CRMP-2 (collapsin response mediator protein-2
prevents abnormal neuronal connections in the brain
*lacosamide only affects which nerons and how is this beneficial
neurons that are depolarized or active for long periods of time
this is good bc we want to target these neurons for epilepsy
*MOA topiramate
blocks sodium channels
downregulates AMPA/kainate receptors (so suppresses glutamate activity)
*felbamate MOA
blocks sodium channels
upregulates GABA receptors
downregulates NMDA receptors (inhibits glutamate effects)
**MOA keppra
reduces/inhibits neurotransmitter release by binding SV2A
also inhibits presynaptic calcium channels
2 MOA briviracetam
-blocks SV2A
-inhibits sodium channels
AMPA is a ___ receptor subtype
glutamate
BBW perampenal
aggression and unusual hostility
*AMPA receptor antagonist
perampenal
*tiagabine inhibits ____
GAT-1 transporter