Pharm: AEDs Flashcards by Savannah Smith

voltage gated Na channel blockers

-zepine
promote inactivated state to limit sustained, repetitive firing of neurons
Tx: partial and secondarily generalized tonic-clonic seizures

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GABA enhancers

pre- or postsynaptic enhancement of GABA synaptic inhibition

Tx: partial and secondarily generalized tonic-clonic seizures

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voltage gated Ca channel blockers

inhibition of T-type Ca currents

Tx: absence seizure

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carbamazepine

Na channel blocker
induces its own metabolism
AE: aplastic anemia; constipation/dry mouth
BBW: AGRANULOCYTOSIS
TERATOGEN: FETAL HYDANTOIN syndrome, SPINA BIFIDA
Tx: partial, including secondarily generalize seizures

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clonazepam

GABA agonist

NO skin AE

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ethosuximide

Ca channel blocker

Tx: absence seizure

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felbamate

NMDA antagonist, GABA agonist

BBW: APLASTIC ANEMIA,bone marrow suppression, HEPATIC

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gabapentin

inhibit alpha-2 delta-1 subunit of Ca channel

enhancement of presynaptic GABA release

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lacosamide

PO, IV
Na channel blocker
NO skin AE

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lamotrigine

Na channel blocker
BBW: SKIN (TEN/SJS)
TERATOGEN: inhibits dihydrofolate reductase; cleft
Tx: partial, including secondarily generalize seizures; primary generalized tonic-conic seizures; atypical absence, myoclonic, atonic seizures

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levetiracetam

PO, IV
MoA: unknown
Tx: partial, including secondarily generalized seizures; primary generalized tonic-clonic seizures; atypical absence, myoclonic, atonic seizures

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oxcarbazepine

Na channel blocker
possibly: increase K and decrease Ca effects
Tx: partial, including secondarily generalize seizures

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phenytoin

PO, IV
Na channel blocker
PROTEIN BINDING
CYP induction: lots of drug interactions
highly variable metabolism
elimination: stool; ZERO order (T1/2 varies with dose)
AE: GINGIVAL HYPERPLASIA; HYPERTRICHOSIS; BLOOD DYSCRASIA
TERATOGEN: FETAL HYDANTOIN syndrome, cardiac, cleft, growth deficiency

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pregabalin

inhibit alpha-2 delta-1 subunit of Ca channel

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topiramate

Na channel blocker
decrease glutamate activity
increase K current and GABA

carbonic anhydrase inhibitor: renal bicarb loss
AE: renal stones
TERATOGEN: cleft lip/palate

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valproate

PO, IV
Na channel blocker
inhibit GABA metabolism
(Ca channel blocker)
binds protein
AE: THROMBOCYTOPENIA, PROLONGED BLEEDING; HEPATIC, nausea, diarrhea
TERATOGEN: greatest risk; NEURAL TUBE, cleft, skeletal, developmental
Tx: primary generalized tonic-clonic seizures; absence seizures; atypical absence, myoclonic, atonic seizures

zonisamide

Na/Ca channel blocker
accumulates in RBCs

carbonic anhydrase inhibitor: renal bicarb loss
AE: renal stones

benzodiazepines

postsynaptic
GABA(A) receptor agonist: enhances Cl- influx
increase FREQUENCY (shift dose-response curve)
AE: dependence, withdrawal, sedation, tolerance
can give RAPID IV for seizure

barbiturates

postsynaptic
GABA(A) receptor agonist: enhances Cl- influx
increase DURATION
AE: dependence, withdrawal, sedation, tolerance
can give RAPID IV for seizure

AED’s in general

oral (slow release available)
limited protein binding
long T1/2
CYPs and UGT
hepatic metabolism
elimination: urine
AE: suicidal ideation, CNS effects, RASH (SJS/DRESS/TEN)
renal dysfunction can cause drug accumulation
need to routine monitoring: if levels high, ok if no AE
TAPER: prevent status epilepticus

fosphenytoin

phenytoin pro-drug

HLA-B 1502

Asians
increase chance of Steven Johnson’s and toxic epidermal necrolysis
CARBAMAZEPINE
also avoid: (fos)phenytoin, lamotrigine, oxcarbazepine

phenobarbital

CYP induction

teratogen: cleft, cardiac, urinary tract

Type of teratogenicity

valproate
phenytoin
carbamazepine
phenobarbital
lamotrigine
topirmate

neural tube, cleft, skeletal, developmental delay
FHS, cardiac, cleft
FHS, spina bifida
cleft, cardiac, urinary tract
low folate; cleft
cleft lip/palate

fetal hydantoin syndrome

upturned nose, mid facial hypoplasia, long upper lip with vermilion border digital/ fingernail hypoplasia CARBAMAZEPINE, PHENYTOIN

Tx of partial, including secondarily generalized seizures

lamotrigine carbamazepine levetiracetam oxcarbazepine

Tx of primary generalized tonic-clonic seizures

valproate lamotrigine levetiracetam

Tx of absence seizures

ethosuximide | valproate

Tx of atypical absence, myoclonic, atonic seizures

valproate lamotrigine levatiracetam

status epilepticus

EMERGENCY prolonged seizure or cluster of seizures without return to baseline lasting longer than 30 min Tx: BENZODIAZEPINE followed by other IV AED

1. benzodiazepines for status epilepticus | 2. option for following IV AED

1. IV LORAZEPAM, IM midazolam, rectal diazepam | 2. valproate, phenytoin, midazolam, levetiracetam, phenobarbital (can't be given rapid IV so use benzodiazepines first)