ANTISEIZURE DRUGS Flashcards
GENERAL MOA of the Antiseizure Drugs? (3)
o Modification of ionic conductance (mostly sodium) and
presynaptic transmitter release (SV2A)
o Enhancement of GABAergic (INHIBITORY) Transmission
o Diminution of excitatory (usually GLUTAMATERGIC)
transmission
Side effects of Phenytoin,
Fosphenytoin,
Phenacemide
MNEMONICS: Phenytoin
cyP-450 induction
Hirsutism
Enlarged gums (gingival hyperplasia), Nystagmus
Yellow-brown skin
Teratogenicity (fetal
hydantoin syndrome)
Osteopenia
Inhibited folate absorption
Neuropathy
DOC for trigeminal neuralgia
Carbamazepine
most teratogenic AED
Valproic Acid
MOA Valproic Acid
- Also blocks NMDA and increases GABA
MOA Lamotrigine
Also blocks Ca channels, decreases glutamate
Notable SE of Lamotrigine?
Rash and SJS/TEN
- AED with the most anti-seizure MOAs
(also acts on K, Ca, GABA, AMPA-glutamate,
and is a weak carbonic anhydrase inhibitor) - Also used for Lennox-Gestaut & West
syndrome - Causes sleepiness, cognitive slowing,
confusion - Urolithiasis (carbonic anhydrase activity)
Topiramate,
Felbamate
MOA ETHOSUXIMIDE [C], PHENSUXIMIDE, METHSUXIMIDE
Decreases Ca2+ currents (T-type) in thalamus
Ethosuximide reduces low threshold T-type Ca2+
currents in the thalamic neurons
Absence seizures (DOC)
ETHOSUXIMIDE [C], PHENSUXIMIDE, METHSUXIMIDE
Blocks Ca2+ α2δ channels. Decrease glutamate
release. Inhibits neuronal discharge from seizure foci.
GABAPENTIN [C], PREGABALIN [C]
Inhibits GABA reuptake via GAT-1
TIAGABINE
Irreversibly inhibits GABA transaminase
VIGABATRIN
SE of VIGABATRIN
Permanent bilateral vision loss
Selectively binds synaptic vesicular protein SV2A →
selectively inhibiting hypersynchronization of
epileptiform burst firing; Modifies synaptic release of
glutamate and GABA. Inhibits Ca2+ channels also
LEVETIRACETAM, BRIVARACETAM