Antiepileptics
Group/Mech
Sodium channel
Blockers
- Prevent repetitive
AP propagation
- Stabilizes inactive
state
- General side
effects:
Due to inhibiting
high-frequency
neurons
oNystagmus
oDiplopia
oAtaxia
oSomnolence
oCognitive
slowing
GABA
transmission
chan: BZs, Barbs,
Topiramate
synthesis:
Gabapentin
GABA metab: Valproaic
ac.
Somnolence
Confusion,Memory
probs
Mark Tuttle, 2011
Drugs
Phenytoin (DilantinTM)
Fosphenytoin
TM
(Cerebyx )
- P450, not
autoinduced
- 1st order zeroorder *
Carbamazepine
(TegretolTM)
Oxcarbazepine
(TrileptalTM)
- P450, autoinduced
Valproic Acid
(DepakoteTM)
- Hepatic excretion
Lamotrigine
(LamictalTM)
- Hepatic excretion
Topiramate(TopamaxTM
)
- Renal excretion
Zonisamide
(ZonegranTM)
- Long t: once-daily
dosing
Benzodiazepines:
Clonazepam (Klonopin)
Diazepam (Valium)
Lorazepam (Ativan)
Barbiturates: P450
Phenobarbital
Adverse Effects
- Gingival hyperplasia
- Vitamin D deficiency - Osteopenia:
Ca2+
- Hepatotoxic
- Cardiac conduction defect
- Dizziness
- Sedation
- Diplopia
- Cardiac conduction defect
- Fat, shaky, bald, yellow
oWeight gain, tremor, alopecia,
hepatotoxicity
- Nausea / vomiting
- Pancreatitis
- Rash: Stevens-Johnson
- Asceptic meningitis
- Confusion/psychosis
- Kidney stones
- Weight loss
- Kidney stones*
- Hepatotoxic
- Weight loss
- Sedation
- Ataxia
- Psychosis
- Tolerance
- Sedation: Cognitive slowing,
respiratory
- Peripheral neuropathy
- Blood: Anemia (megaloblastic)
- Teratogenic
- Purple glove syndrome (Phenytoin only)
- Hyponatremia
- Osteoporosis
- Rash: Stevens 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)
T-type Ca channel
agents
- Stabilize inactive
state
- Prevent rhythmic
firing
Inhibition of
excitatory amino
acid synaptic
release
Ethosuximide
(ZarontinTM)
- Hepatic excretion
- Nausea / vomiting
- Hiccups
- Aggressiveness
- Headache
- concentration
- Blood: Leukopenia, agranulocytosis
Gabapentin
(NeurontinTM)
- Renal excretion
Pregabalin (LyricaTM)
- Dizziness
- Weight gain
- Pedal edema
- Pediatrics: aggressive behavior
- Sedation, cognitive impairment
- Blurred vision
- Weight gain
- Sedation, dizziness
- Ataxia
- Dry mouth
- Peripheral edema
- Blood: Thrombocytopenia
- Psychosis
- Blood: anemia, neutropenia
Levatiracetam
(KeppraTM)
- Renal excretion
Lacosamide (VimpatTM)
Slow inact. of Na+
chan.
Stab. inactive Na+
Rufinamide (BanzelTM)
- Lennoux Gastaut (MR, multiple seizure types)
chan.
Side effects (by effect):
Rash: Stevens-Johnson Syndrome
Phenytoin (DilantinTM), Carbamazepine (TegretolTM), Oxcarbazepine (TrileptalTM), Zonisamide
(ZonegranTM)
Blood problems
Phenytoin (DilantinTM), Carbamazepine (TegretolTM), Oxcarbazepine (TrileptalTM), Zonisamide
(ZonegranTM),
Valproic Acid (DepakoteTM), Ethosuximide (ZarontinTM), Pregabalin
TM
TM
(Lyrica ), Levatiracetam (Keppra )
Hepatotoxicity
Phenytoin (DilantinTM), Valproic Acid (DepakoteTM), Zonisamide (ZonegranTM)
Pediatric problems
Phenobarbital, Gabapentin (NeurontinTM), Lamotrigine (LamictalTM)
Kidney stones
Topiramate(TopamaxTM), Zonisamide (ZonegranTM)
Osteopenia
Carbamazepine (TegretolTM), Oxcarbazepine (TrileptalTM), Valproic Acid (DepakoteTM)
Weight gain
Valproic Acid (DepakoteTM), Gabapentin (NeurontinTM), Pregabalin (LyricaTM)
Weight loss
Topiramate(TopamaxTM), Zonisamide (ZonegranTM)
1st
2nd
1st
1st
1st
1st
2nd
X
X
X
X
1st
2nd
2nd
2n
d
2nd
2nd
X
1st
X
X
X
2nd
X
X
Weight loss
Weight gain
Osteopenia
Hepatotoxicity
Kidney Stones
Blood
2nd
Pediatric problems
conductionCardiac
1st
Rash
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)
Side Effects
Partial
Antiepileptics
Absence
Indications
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.
