Anti-Epileptic Drugs - Glutamate Flashcards
With Epilepsy, there is a neuronal imbalance that causes increased CNS excitation. What are the molecules and their changes in levels that are associated with that?
Glutamate/Aspartate = increased = more excitation GABA = decreased = less inhibition
The goal of Anti-epileptic drugs is to _____ glutamate actions and _____ GABA actions
Suppress glutamate and Enhance GABA
What are the 10 Na voltage gated channel blockers?
Carbamazepine Oxcarbazepine Eslicarbazepine Lamotrigine Phenytoin Topiramate Valproic Acid Lacosamide Zonisamide Rufinamide
What are the 10 Na voltage gated channel blockers?
Carbamazepine Oxcarbazepine Eslicarbazepine Lamotrigine Phenytoin Topiramate Valproic Acid Lacosamide Zonisamde Rufinamide
Where do the Na voltage gated channel blockers work?
Pre-synaptic neuron
What is the IV form of Phenytoin?
Fosphenytoin
What is the main action of all 10 of the Na voltage gated channel blockers?
Prolong fast inactivation state
What Na voltage gated channel blocker also works to enhance the slow inactivation state?
Lacosamide
What are the 2 AMPA receptor blockers?
Topiramate
Perampanel
What are the 2 AMPA receptor blockers?
Topiramate
Perampanel
Where do AMPA receptor blockers work?
Post-synaptic
What is the NMDA receptor blocker?
Felbamate
What is the NMDA receptor blocker?
Felbamate
Where does the NMDA receptor blocker work?
Post-synaptic
Low-threshold T-type Ca++ channels mediate the activity of what type of seizures?
Absence seizures
The 2 drugs that block low-threshold T-type Ca++ channels will block what seizure type?
Absence seizures
- Ethosuximide
- Zonisamide
What are the 2 low-threshold T-type Ca++ channel blockers?
Ethosuximide
Zonisamide
What are the 2 low-threshold T-type Ca++ channel blockers?
Ethosuximide
Zonisamide
Where do the low-threshold T-type Ca++ channels work?
Pre-synaptic
What is the job of the SV2AP?
Closes the pre-synaptic vesicles that contain glutamate for release
What are the 2 drugs that inhibit SV2AP?
Levetiracetam
Brivaracetam
What are the drugs that inhibit SV2AP?
Levetiracetam
Brivaracetam
Where do SV2AP inhibitors work?
Pre-synaptic
What are the 2 drugs that block alpha-2-delta subunit of T-type Ca++ channels?
Gabapentin
Pregablin
What are the 2 drugs that block alpha-2-delta subunit of T-type Ca++ channels?
Gabapentin
Pregabalin
Which drug opens K+ channels (KCNQ) in order for K+ to leave the cell?
Ezogabine
Which drug opens K+ channels (KCNQ) in order for K+ to leave the cell?
Ezogabine
Ezogabine opens KCNQ K+ channels where?
Pre AND Post synaptic
What are 2 side effects of Carbamazepine?
(Na voltage gated channel blocker)
- Self metabolism
- Decreases WBC’s
What is 1 side effect of Phenytoin?
(Na voltage gated channel blocker)
1. Gingival Hyperplasia
Which drug is both a Na voltage gated channel blocker and an AMPA receptor blocker?
Topiramate
Which drug is both a Na voltage gated channel blocker and a low-threshold T-type Ca++ channel blocker?
Zonisamide
All of the drugs in this deck affect which neuronal imbalance molecule that controls seizures?
Glutamate
– Decreasing!
What gate must be open in order for Na voltage gated channel blockers to bind and work?
Activation gate must be open
