Epilepsy Flashcards
Identify the site where the following drugs act
Either gluatminergic/GABAergic synapes, presynaptic /postsynaptic
1. Phenytoin, CBZ, LTG, Lacosamide
2. Ethusiximide, LTG, Gabapentin, Pregabalin
3. Levetiracetam
4. Lacosamide
5. Felbamate
6. Topiramate, Perampanel
ALL are glutaminergic
- PreS VG Na channel
- PreS VG Ca++ channel
- PreSSV2A synaptic vesicle proteins
- PreS Collapsin response mediator protein 2 (CRMP2)
- PostS NMDA
- PostS AMPA
Identify the site where the following drugs act
Either glutamatergic/GABAergic synapes, presynaptic /postsynaptic
1. Tiagabine
2. Vigabatrin
3. Benzos and Barbiturates
ALL act in the GABAergic synapse
- PreS GABA transporter
- PreS GABA transaminase
- PostS GABA A receptor
What is AKA diphenylhydantoin?
Phenytoin
How does phenytoin affect Na channels?
Binds to and Prolongs the inactivated state of the Na channel resulting in decreased glutamate release– PreSynaptic Glutaminergic
What are the advantages of fosphenytoin over phenytoin?
Can be given IM
How does uremia affect phenytoin?
Low protein levels causes more unbound fraction of the drug.
Besides gingival hyperplasia and hirsutism what other adverse effects do we expect from phenytoin? Think cerebellar and eye movements
Ataxia, nystagmus, diplopia
But also remember osteomalacia from abnormal vitamin D metabolism
What are the most common dose related adverse effects of CBZ?
Diplopia and ataxia
Hyponatremia, aplastic anemia, leukopenia, agranulocytosis and unsteadiness also occurs
What is the advantage of eslicarbazepine over CBZ and OxCBZ?
Once a day dosing
What derivative of barbituric acid is a treatment option for essential tremor and is converted to Pb?
Primidone
Besides binding to the GABA receptor what is the other important MOA of Pb?
Similar to phenytoin on Na channels presynaptic glutaminergic
What is the therapeutic level of
- Phenobarbital
- Carbamazepine
- Phenytoin
- Valproic acid
- 10-40mcg per ml
- 4-8 mcg
- 10-20 mcg per ml
- 50-100mcg per ml
What are the deadly side effects of felbamate?
heptitis and aplastic anemia
How does the binding of pregabalin and gabapentin to Ca++ channels prevent seizures?
Decrease in Ca++ entry in the presynaptic terminal results in decrease in the release of glutamate in the synaptic cleft.
How are pregabalin and gabapentin metabolized?
Trick question. They ARE NOT metabolized– rather excreted unchanged in the urine