Anticonvulsants Flashcards
What are the four mechanisms of Anticonvulsants?
- Enhance sodium channel inhibition
- Inhibit calcium channels
- Enhance GABA inhibition
- Inhibit glutamate receptors
Which drugs inhibit sodium channels?
Phenytoin, carbamazepine and lamotrigine
Which drugs inhibit calcium channels?
Ethosuximide, valproic acid, gabapentin, pregabalin
Which drugs enhance GABA ?
Benzodiazepines, barbiturates
What is the MOA of Phenytoin?
Prolongs the inactivation state of voltage gated sodium channels.
What are 2 pharmacokinectic properties of phenytoin?
- Induces CYP3A4
2. 90% bound to albumin
What are the side effects of phenytoin?
- Fatigue
- Dizziness
- Diplopia
- Cognitive impairment
What is the MOA for Carbamazepine?
- Blocks reactivation of voltage gated sodium channels.
2. Blocks NE reuptake
What are the side effects of carbamazepine?
- Dizziness
- Ataxia
- Nystagmus
Which drugs side effect can cause Steven-Johnson syndrome?
Lamotrigine
What are the MOAs of Valproate?
- Inhibits voltage gated sodium channels
- Inhibits T-type calcium channels
- May increase GABA synthesis and decrease degradation.
What are the side effects of Valproate?
- Tremor
- Hair loss
- Thrombocytopenia
What is the MOA of Ethosuximide?
Inhibits T-type calcium channels in thalamic neurons.
What population is Ethosuximide used for?
Absence seizures in children
What is the MOA of Zonisamide?
Inhibits T-type Calcium channels and prolongs the inactivation of sodium channels.
What is the side effect of Zonisamide?
Difficulty concentrating and renal stones.
Discuss Zabapentin
GABA analog that may interac with Alpha-2-Delta subuni of L type voltage-sensitive calcium channels. Unchanged in urine
What are the MOAs for Topimarate?
- Poteniates GABA response
- Decreases glutamate receptor activity
- Blocks voltage gated sodium channels
What is the main side effect of topimarate?
Weight loss
Which drugs have no effect of hepatic enzymes?
- Ethosuximide
- Gabapentin
- Levatirectam
- Pregabalin
Which drugs induce CYP450 enzymes?
- Carbamazepine
- Phenobarbital
- Phenytoin
Which drugs inhibit P450 enzymes?
Topimarate, Valproate