Anticonvulsants Flashcards
Anticonvulsants/ AEDs are used for what?
1) long term management of chronic epilepsy
2) management of seizures not caused by epilepsy
What is off-label use of anticonvulsants? Hint: 4
1) anxiety
2) bipolar disorder
3) chronic pain
4) migraines
What will happen if a pt abruptly stops taking their anticonvulsant?
It can trigger recurrence of seizures
What are the mechanisms of action of anticonvulsants?
1) sodium channel blockers
2) calcium channel blockers
3) GABA enhancers
4) glutamate blockers
Mechanisms of actions:
Sodium channel blockers
Prevent the rapid firing of neurons
prevent return of channel to active state – stabilizes them – inactive state
Mechanisms of action:
Calcium channel blockers
Slow down the flow of calcium into cells, limiting the development of action potentials
Mechanisms of action:
GABA enhancers
Enhances inhibitory effects, making neurons less likely to fire
Mechanisms of action:
Glutamate blockers
Prevent excitatory signaling by blocking glutamate
How do we select which medication is used for Tx of seizures?
By the classification of the seizure and epilepsy
What type of seizures are broad spectrum meds used for?
Effective for Tx of focal & generalized seizures
What type of seizures are narrow spectrum meds used for?
Used primarily for focal-onset seizures (including focal which evolve to B/L convulsive seizures)
List 9 things to base selection of meds for seizure Tx off of
1) efficacy
2) tolerability
3) presence of comorbidities
4) pharmacokinetic profile
5) potential drug-drug interactions
6) ease of use
7) cost
8) age
9) gender
List 10 AEDs thats mechanism of action is Na+ channel blockers
1) carbamazepine
2) oxcarbazepine (trileptal)
3) eslicarbazepine
4) felbamate
5) lamotrigine
6) lacosamide (vimpat)
7) phenytoin (fosphenytoin (IV))
8) topiramate
9) valproate
10) rufinamide
List 6 AEDs thats mechanism of action is glutamate blockers
1) topiramate
2) zonisamide (zonegran)
3) perampanel
4) felbate
5) levetiracetam
6) Brivaracetam (PO, IV only > 16 yrs)
List 6 AEDs thats mechanism of action is calcium channel blockers
1) ethosuxmide
2) gabapentin
3) lamotrigine (lamictal)
4) pregabalin
5) valproic acid
6) zonisamide
List 6 AEDs thats mechanism of action is GABA enhancers
1) benzodiazepines
2) barbiturates
3) valproic acid (depakote)
4) gabapentin
5) pregabalin
6) ethosuximide
How do AEDs that act as Ca channel blockers work?
Ca going in during cells resting state facilitates development of an action potential; however these meds slow the flow of Ca++ into the cell
What do AEDs that act as Ca channel blockers inhibit?
Slow depolarization which is needed for spike-wave bursts
help “lock the channel”
How do AEDs that act as GABA enhancers work?
May enhance Cl- influx which makes cell more negative & harder for cell to generate AP
some ↓ metabolism of GABA so more is available
How do AEDs that act as glutamate blockers work?
Bind glutamate (excitatory neurotransmitter)
Glutamate has 5 binding sites
What do many AEDs require?
Drug monitoring
List 3 patient education tips when using AEDs
1) take as prescribed
2) NEVER stop taking on own
3) side effect management
How does Phenytoin (Dilantin) work?
Na+ channel blocker
Works to stabilize neurons from becoming too excited
Stops spread of seizure activity in motor cortex
Which AED is highly (90%) protein-bound drug?
Phenytoin (Dilantin)