Antiepileptics
Group/Mech
Sodium channel Blockers
- Prevent repetitive AP
propagation
- Stabilizes inactive state
- General side effects:
 Due to inhibiting highfrequency neurons
o Nystagmus
o Diplopia
o Ataxia
o Somnolence
o Cognitive slowing
Mark Tuttle, 2011
Drugs
Phenytoin (DilantinTM)
Fosphenytoin (CerebyxTM)
- ↑ P450, not autoinduced
- 1st order  zero-order *
Carbamazepine (TegretolTM)
Oxcarbazepine (TrileptalTM)
- ↑ P450, autoinduced
Adverse Effects
- Gingival hyperplasia
- Vitamin D deficiency - Osteopenia: Ca2+ ↓
- Hepatotoxic
- Cardiac conduction defect
- Dizziness
- Sedation
- Diplopia
- Cardiac conduction defect
Valproic Acid (DepakoteTM)
- Hepatic excretion
- “Fat, shaky, bald, yellow”
o Weight gain, tremor, alopecia, hepatotoxicity
- Nausea / vomiting
- Pancreatitis
- Rash: Stevens-Johnson
- Asceptic meningitis
- Confusion/psychosis
- Kidney stones
- Weight loss
Lamotrigine (LamictalTM)
- Hepatic excretion
Topiramate(TopamaxTM)
- Renal excretion
Zonisamide (ZonegranTM)
- Long t½: once-daily dosing
↑ GABA transmission
↑chan: BZs, Barbs, Topiramate
↑synthesis:
Gabapentin
↓GABA metab: Valproaic ac.
Somnolence
Confusion,Memory probs
T-type Ca channel agents
- Stabilize inactive state
- Prevent rhythmic firing
Inhibition of excitatory
amino acid synaptic
release
Slow inact. of Na+ chan.
Stab. inactive Na+ chan.
Benzodiazepines:
Clonazepam (Klonopin)
Diazepam (Valium)
Lorazepam (Ativan)
Barbiturates: ↑ P450
Phenobarbital
Ethosuximide (ZarontinTM)
- Hepatic excretion
Gabapentin (NeurontinTM)
- Renal excretion
Pregabalin (LyricaTM)
Levatiracetam (KeppraTM)
- Renal excretion
Lacosamide (VimpatTM)
Rufinamide (BanzelTM)
-
Kidney stones*
Hepatotoxic
Weight loss
Sedation
Ataxia
Psychosis
Tolerance
Sedation: Cognitive slowing, respiratory ↓
-
Nausea / vomiting
Hiccups
Aggressiveness
Dizziness
Weight gain
Sedation, cognitive impairment
Blurred vision
Weight gain
Sedation, dizziness
Ataxia
Lennoux Gastaut (MR, multiple seizure types)
-
Peripheral neuropathy
Blood: Anemia (megaloblastic)
Teratogenic
Purple glove syndrome (Phenytoin only)
Hyponatremia
Osteoporosis
Rash: Steven’s Johnson Syndrome
Blood: Neutropenia, thrombocytopenia, aplastic
anemia
Polycystic ovarian syndrome
Osteopenia
Blood: thrombocytopenia
Teratogenic: Neural tube defects
Dizziness, sedation
Pediatric: ADHD worse
Metabolic acidosis
Glaucoma
Paresthesias
Headache
Rash: Stevens-Johnson Syndrome
Blood: dyscrasias
Sulfonamide (allergies)
- Pediatric: Hyperactivity (paradoxical)
-
Headache
↓ concentration
Blood: Leukopenia, agranulocytosis
Pedal edema
Pediatrics: aggressive behavior
Dry mouth
Peripheral edema
Blood: Thrombocytopenia
Psychosis
Blood: anemia, neutropenia
Side effects (by effect):
 Rash: Stevens-Johnson Syndrome
 Blood problems
Cardiac conduction
Blood
Hepatotoxicity
2nd
X
X
X
X
1st
2nd
X
X
X
1st
2nd
1st
1st
1st
2nd
1st
2nd
X
X
X
X
X
X
X
X
X
X
X
2nd
2nd
2nd
X
1st
X
X
2nd
X
X
X
X
Weight loss
Rash
1st
Absence
Generalized
Phenytoin (DilantinTM)
Fosphenytoin (CerebyxTM)
Carbamazepine (TegretolTM)
Oxcarbazepine (TrileptalTM)
Valproic Acid (DepakoteTM)
Lamotrigine (LamictalTM)
Topiramate(TopamaxTM)
Zonisamide (ZonegranTM)
Clonazepam (KlonopinTM)
Diazepam (ValiumTM)
Lorazepam (AtivanTM)
Phenobarbital
Ethosuximide (ZarontinTM)
Gabapentin (NeurontinTM)
Pregabalin (LyricaTM)
Levatiracetam (KeppraTM)
Partial
Antiepileptics
Weight gain
Side Effects
Osteopenia
Indications
Kidney Stones
Hepatotoxicity
Pediatric problems
Kidney stones
Osteopenia
Weight gain
Weight loss
Pediatric problems
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Phenytoin (DilantinTM), Carbamazepine (TegretolTM), Oxcarbazepine (TrileptalTM), Zonisamide (ZonegranTM)
Phenytoin (DilantinTM), Carbamazepine (TegretolTM), Oxcarbazepine (TrileptalTM), Zonisamide (ZonegranTM),
Valproic Acid (DepakoteTM), Ethosuximide (ZarontinTM), Pregabalin (LyricaTM), Levatiracetam (KeppraTM)
Phenytoin (DilantinTM), Valproic Acid (DepakoteTM), Zonisamide (ZonegranTM)
Phenobarbital, Gabapentin (NeurontinTM), Lamotrigine (LamictalTM)
Topiramate(TopamaxTM), Zonisamide (ZonegranTM)
Carbamazepine (TegretolTM), Oxcarbazepine (TrileptalTM), Valproic Acid (DepakoteTM)
Valproic Acid (DepakoteTM), Gabapentin (NeurontinTM), Pregabalin (LyricaTM)
Topiramate(TopamaxTM), Zonisamide (ZonegranTM)
Determine if antiepileptic medication is
indicated:
 Recurrent seizures of unknown etiology
 Known cause that cannot be reversed
 Present with status epilepticus
 Family history of seizures
 Abnormal interictal EEG
 Job depends on no seizures (ex. driver)
Selection of antiepileptic drugs
 Begin with monotherapy. Add a second
drug with a different mechanism of
action if poorly controlled
 Surgery is an option in focal epilepsy with
poor control on medications.