Antiepileptics Flashcards
What is the mechanism of action of Carbamazepine?
Fast Na channel blocker
Carbamazepine is also known for its enzyme induction and autoinduction properties.
What are the major adverse drug reactions (ADRs) associated with Carbamazepine?
-Delayed rash
-SIADH
-Blood dyscrasias
-Decreased bone density
-Toxicity: slurred speech, N/V, diplopia, tremor, drowsiness
HLA-B*1502 genotype is associated with increased risk of SJS.
What is the therapeutic level of Carbamazepine?
4-12 mcg/ml
What is the mechanism of action of Fosphenytoin?
Fast Na channel blocker
Fosphenytoin is a prodrug for phenytoin.
What is the maximum administration rate for Fosphenytoin?
150 mg PE per minute
What are the common ADRs of Gabapentin?
Sedation, respiratory depression increase with other CNS depressants
What is the mechanism of action of Lacosamide?
Slow Na channel blocker
What is a significant cardiovascular concern associated with Lacosamide?
PR prolongation or 1st degree AV block
What is the mechanism of action of Lamotrigine?
Decrease glutamate and aspartate release; delays repetitive firing of neurons; block fast Na channels
What are the major black box warnings (BBW) for Lamotrigine?
Rash/SJS/DRESS
What is the mechanism of action of Levetiracetam?
Prevent hypersynchronization of epileptiform burst firing & propagation of seizure activity through binding at SV2A receptor
What are the common ADRs of Levetiracetam?
-Depression
-Behavior changes
-Agitation
-Coordination difficulties
-Drowsiness
What is the mechanism of action of Oxcarbazepine?
Fast Na channel blocker
What is a notable side effect of Oxcarbazepine compared to Carbamazepine?
Hyponatremia > CBZ
Rash < CBZ (cross reactivity)
Blood dyscrasias < CBZ
What is the mechanism of action of Phenobarbital?
Increase GABA-mediated chloride influx
What is the therapeutic level of Phenobarbital?
15-40 mcg/ml
What are the common ADRs of Phenytoin?
-Dose related: nystagmus, ataxia, drowsiness, cognitive impairment
-Non-dose related: gingival hyperplasia, hirsutism, acne, rash (DRESS), hepatotoxic
-Decrease bone density
What is the maximum administration rate for Phenytoin?
50 mg/min due to arrhythmia, hypotension
What is the mechanism of action of Pregabalin?
Inhibit subunit of voltage-dependent Ca channel
What are the common ADRs of Pregabalin?
-Somnolence
-Behavioral problems
-Dizziness
-Weight gain
-Ataxia
-Angioedema
What is the mechanism of action of Topiramate?
Fast Na channel blocker; enhance GABA; antagonize AMPA; carbonic anhydrase inhibitor
What are the common ADRs of Topiramate?
-Drowsiness
-Paresthesias
-Weight loss
-Nephrolithiasis
-Psychomotor slowing
-Glaucoma
-Metabolic acidosis
-Word-finding difficulties
-Oligohidrosis
What is the mechanism of action of Valproic acid?
Blocks T-type Ca current, block Na channel, increase GABA
What are the major black box warnings (BBW) for Valproic acid?
-Hepatotoxicity
-Teratogenic
-Pancreatitis
What is the therapeutic level of Valproic acid?
40-100 or 150 mcg/ml
What is the mechanism of action of Zonisamide?
No effect on CYP
What are the common ADRs of Zonisamide?
-Weight loss
-Rash
-Oligohidrosis
-Somnolence
-Agitation
-Hallucinations
-Metabolic acidosis
-Nephrolithiasis
What is the mechanism of action of Brivaracetam?
Unknown - high affinity for synaptic vesicle protein 2A
What are the common ADRs of Cannabidiol?
-Hepatotoxicity
-Sedation
-Diarrhea
What is the mechanism of action of Cenobamate?
Inhibit voltage gated Na channels, modulate GABA receptor
What is a significant ADR associated with Cenobamate?
DRESS (titrate slowly)
What is the mechanism of action of Clobazam?
Long acting benzo
What are the common ADRs of Ethosuximide?
-Anorexia
-N/V
-Leukopenia
-Agranulocytosis
-Pancytopenia
What is the mechanism of action of Felbamate?
Blocks glycine site on NMDA receptor
What is the major concern when using Felbamate?
Hepatotoxicity, aplastic anemia (must sign consent)
What is a major concern associated with Fenfluramine?
Serotonin syndrome with other serotonergic meds
What is the mechanism of action of Ganaxolone?
Positive modulation of GABA receptor
What are the common ADRs of Perampanel?
-Somnolence
-Sedation
-Dizziness
-Fatigue
What is the mechanism of action of Rufinamide?
Fast Na channel blocker
What is a significant ADR of Rufinamide?
HA, dizziness, fatigue, nausea, somnolence (slow dose titration), rash (children)
What is the mechanism of action of Tiagabine?
Block GABA uptake in presynaptic neuron
What is the major concern associated with Vigabatrin?
BBW: Vision loss