L11- Anti-epileptics (MOA, AEs) Flashcards
what are the general MOAs of Anti-epileptic drugs, include subtypes
1) Blockade of V-gated ion channels
- Na+ V-gated channels
- T-type Ca++ channels
2) Modulation of synaptic transmission
- enhance GABA neurotransmission
- reduce Glutamate neurotransmission
list the anti-eplileptics that block Na V-gated channels
- phenytoin
- carbamazepine, oxcarbazepine
- lamotrigine
- zonisamide
list the anti-epileptics that block T-type Ca channels
-phenobarbital
-valproate
-topiramate
(ethosuximide)
Absence Seizures:
- (1) is the main neuronal activity involved
- (2) is the necessary mechanism for prevention and treatment, and (3) are the drugs with (2)
1- oscillatory neuronal activity between thalamus and cortex
2- blockade of T-type Ca channels; they’re responsible for oscillatory responses in thalamic neurons
3- valproate, ethosuximide
agents affecting GABA neurotransmission:
- (1) have direct GABA receptor actions
- (2) inhibits GABA degradation (include enzyme)
- (3) inhibits GABA reuptake
1- benzodiazepines, barbiturates, topiramate
2- Vigabatrin inhibits GABA aminotransferase
3- Tiagabine
describe the subtle difference in action of benzodiazepines and barbituates
Benzodiazepines: inc frequency of GABA channel opening (Ben likes it more often)
Barbituates: inc time GABA channels are open (Barb likes it longer)
agents affecting GABA neurotranmission:
- (1) block glutamate receptors
- (2) dec glutamate release from neurons by blocking (3)
- (4) binds to synaptic vesicle unit, (5), to prevent release of glutamate- exact mechanism is unknown
1- phenobarbital, topiramate
2- gabapentin, pregablin
3- blocking V-gated Ca channels (prevents Ca influx and vesicle release)
4- levetiracetam
5- SV2A- synpatic vesicle glycoprotein 2A
______ are the cytochrome P450 inducers
- carbamazepine (oxcarbazepine is weak inducer)
- phenobarbital
- phenytoin
list the AEs for valproate
(all liver effects)
- hepatotoxicity
- inhibits cytochrome P450 –> inhibits metabolism of itself and other drugs
list the AEs for phenytoin
- diplpia, ataxia
- gingival hyperplasia
- hirsuitism
- rash + Steven-Johnson syndrome
-coarsening of facial features in children
list the drugs with zero order kinetics
phenytoin, aspirin, ethanol
list the AEs for carbamazepine
- aplastic anemia
- agranulocytosis
-rash + Steven-Johnson
define Steven-Johnson syndrome
life-threatening disease consisting of mucosal changes w/ sloughing (reaction to disease or drug)
list the anti-epileptics with high risk for Steven-Johnson syndrome
- phenytoin
- lamotrigine
- carbamazepine
- phenobarbital
list the AEs for lamotrigine
rash + Steven-Johnson syndrome (black-box warning)