Antiepileptic Drugs Flashcards
Oxcarbamazepine (Trileptal) Misc
Designed to bypass carbamazepine epoxide; less protein-bound, less autoinduction, fewer interactions, less toxic, longer half-life than carbamazepine
Phenytoin (Dilantin) Class
Voltage-gated Na channel stabilizer
Carbamazepine (Tegretol) Class
Voltage-gated Na channel stabilizer
Oxcarbamazepine (Trileptal) Class
Voltage-gated Na channel stabilizer
Lamotrigine (Lamictal) Class
Voltage-gated Na channel stabilizer
Benzodiazapines Class
GABAergic anti-epileptic
Gabapentin (Neurontin) Class
GABA analog
Pregabalin (Lyrica) Class
GABA analog
Topiramate (Topamax) Class
Glutamate Receptor Blockers
Levetiracetam (Keppra) Class
Synaptic vesicle binder
Ethosuximide (Zarontin) Class
Voltage-gated Ca channel blocker
Phenytoin (Dilantin) MOA
Stabilize inactive conformation of Na channel
Carbamazepine (Tegretol)MOA
Stabilize inactive conformation of Na channel
Oxcarbamazepine (Trileptal) MOA
Stabilize inactive conformation of Na channel
Lamotrigine (Lamictal) MOA
Stabilize inactive conformation of Na channel
Valproate (Depakote) MOA
Unknown; likely affects Na-gated channels and GABA system
Benzodiazapines MOA
Bind GABA-A
Gabapentin (Neurontin) MOA
Block presynaptic influx of Ca
Pregabalin (Lyrica) MOA
Block presynaptic influx of Ca
Topiramate (Topamax)MOA
Partial AMPA, Kainate Ca receptor blocker; secondary effect at voltage-gated Na channel, GABA system
Levetiracetam (Keppra) MOA
Binds synaptic vesicle protein 2, leading to less NT release
Ethosuximide (Zarontin) MOA
Blocks T-type Ca-channels in thalamo-cortical circuits
Phenytoin (Dilantin) Therapeutics
Less effective for absence (particular pediatric), myoclonic, atonic seizures
Carbamazepine (Tegretol) Therapeutics
More effective for complex partial seizure than primary generalized; bipolar disorder; neuropathic pain
Oxcarbamazepine (Trileptal) Therapeutics
More effective for complex partial seizure than primary generalized; bipolar disorder; neuropathic pain
Lamotrigine (Lamictal) Therapeutics
Primary generalized epilepsies, absence seizures; indicated in children; bipolar disorder; neuropathic pain
Valproate (Depakote) Therapeutics
Broad spectrum: absence, myoclonic, tonic-clonic, primary generalized, partial onset, and secondary generalized seizures (but not absence seizures); IV for status epilepticus; bipolar treatment, migraine and long-term cluster headache prophylaxis
Benzodiazapines Therapeutics
Status epilepticus (refractory); anesthesia
Gabapentin (Neurontin) Therapeutics
Adjunct for partial complex epilepsy; more commonly used for neuropathic pain
Pregabalin (Lyrica) Therapeutics
Adjunct for partial complex epilepsy; more commonly used for neuropathic pain
Topiramate (Topamax) Therapeutics
Partial onset seizures, secondary generalized seizures, primary generalized epilepsy; migraine prevention, long-term prevention of cluster headaches
Levetiracetam (Keppra) Therapeutics
Partial onset seizures, secondary generalized seizures; maybe primary generalized epilepsy
Ethosuximide (Zarontin) Therapeutics
Absence seizures only (and neuropathic pain)
Phenytoin (Dilantin) SE
- Rash, gingival hyperplasia, hirsutism, lupus-like reaction; can cause contraceptive failure 2. Mild myelosuppression, increased LFT; long-term: cerebellar degeneration, peripheral neuropathy, osteoporosis
Carbamazepine (Tegretol) SE
Rash (rarely, Stevens-Johnson), mild myelosuppression, mild increase in LFTs; can cause contraceptive failure
Oxcarbamazepine (Trileptal) SE
Rash (rarely, Stevens-Johnson), mild myelosuppression, mild increase in LFTs; can cause contraceptive failure
Lamotrigine (Lamictal) SE
Rash, (rarely, Stevens-Johnson): slow initial titration important; may lead to contraceptive failure
Valproate (Depakote) SE
- Weight gain, hair turnover, hyperammonemia (which can be mitigated with oral carnitine), teratogenicity, blood dyscrasias 2. Pancreatitis
Benzodiazapines SE
Sedation
Gabapentin (Neurontin) SE
Sedation
Pregabalin (Lyrica) SE
Topiramate (Topamax) SE
- Mild metabolic acidosis, kidney stones (due to some carbonic anhydrase activity); modest weight loss; rare acute glaucoma; sedation 2. Word-finding problems
Levetiracetam (Keppra) SE
Well tolerated; sedation, mostly; rarely, irritability, aphasia, thrombocytopenia
Ethosuximide (Zarontin) SE
Nausea (transient), sedation, irritability
Phenytoin (Dilantin) Misc
IV infusion limited by hypotension; hepatic enzyme inducer (both auto- and hetero-inducer), highly protein bound
Carbamazepine (Tegretol) Misc
Hepatic enzyme inducer (both auto- and hetero-inducer); highly protein bound; must increase dose in 1-2 wks due to autoinduction; side effects likely due to epoxide metabolite
Oxcarbamazepine (Trileptal) Misc
Designed to bypass carbamazepine epoxide; less protein-bound, less autoinduction, fewer interactions, less toxic, longer half-life than carbamazepine
Lamotrigine (Lamictal) Misc
May exacerbate myoclonic seizures; competes with valproic acid for excretion (potential synergy); hepatic enzyme inducer; not very protein bound
Benzodiazapines Misc
Long-term usefulness limited by tolerance
Gabapentin (Neurontin) Misc
Absorption limited by intestinal AA transporter (there is a Tm); limited protein binding; no metabolism or drug interaction in humans (so few side effects)
Topiramate (Topamax) Misc
Carbonic anhydrase activity leads to mild metabolic acidosis, which leads to respiratory compensation, which leads to mild alkalosis, which leads to calcium ionization, which leads to tingling; treat with vitamin C (acidify urine)
Ethosuximide (Zarontin) Misc
Readily absorbed, minimal first pass metabolism; not protein bound
