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.