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96 Cards in this Set

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What is carbamazepine used for?
DOC for tonic clonic and partial seizures, useful in trigeminal neuralgia; may make absence of myoclonic seizures worse
what is the structure, administration and absorption of carbamazepine?
carbamazepine is closely related to TCA, PO only, poorly absorbed and dissolution of tables is a problem
how is carbamazepine metabolized? Does it induce those enzymes?
by P450s and it is a strong inducer of liver enzymes
What is the M.O. of carbamazepine?
decreases sodium conductance
What are the ADRs of carbamazepine?
diplopia, ataxia and rash are most common; hypersensitivities - rash, blood dyscarias, hepatits and Steven-Johnson syndrome can occur; memory loss
What are the interactions of carbamazepine?
induces the metabolism of valproic acid, TCAs, haloperidol and imaotrigine; P450 inhibitors decrease the metabolism = decrease activity because of active metabolites
What is indicated for carbamazepine's use in pregnancy?
postive evidence of risk - ONLY use if benefit outweighs risk
What is clonazepam used for?
it is a backup in absence, clonic/myoclonic and atonic seizures
what is the structure, half life and metabolism of clonazepam?
it is a BZD, half life = 12 hours - adults, 6 hours - kids; highly metabolized by the liver (P450s)
What is the M.O. of clonazepam?
GABA potentiation
What are the ADRs of clonazepam?
ataxia, dose limiting sedation, dependence, respiratory despresion at high doses
what are the interactions with clonazepam?
alcohol and phenytoin increase drowsiness and dizziness
What is ethosuximide used for?
drug of choice for absence seizures
What is the structure, administration, half life and metabolism of ethosuximide?
structure = succinamide, it is well absorbed PO, metabolized by liver to hyroxylated metabolites; half life = 60 hrs - adults, 30 hrs - kids
What is the M.O. of ethosuximide?
reduces low threshold (t-type) calcium current in thalamic 'pacemaker' neurons thus reduces discharge from the thalamus
What are the ADRs of ethosuximide?
GI distress, lethargy, weight loss, blood dyscrasias
What is the indication of use during pregnancy of ethosuximide?
risk cannot be ruled out
what is felbamate used for?
Lennox Gestaut syndrome
What is the administration and half life of felbamate?
PO, half life = 20 hrs
What is the M.O. of felbamate?
glutamate antagonist
what are the ADRs of felbamate?
N&V, aplastic anemia, hepatitis and liver failure - can be fatal
What are the interactions of felbamate?
carbamazepine and phenytoin increase the metabolism of felbamate, and vice versa
what is the indication of felbamate use during pregnancy?
risk cannot be ruled out
What is gabapentin used for?
back up in partial seizures, used from chronic pain (especially neruopathic), bipolar disoder and migraines; can exacerabate myoclonic seizures
What is the structure and time it takes to see effects of gabapentin?
amino acid analog of GABA, it takes weeks to see full effects although peak blood levels are reached 1-3 hours
What is the M.O. of gabapentin?
does NOT act on GABA receptor, may alter GABA metabolism, transport or reuptake
What are the ADRs of gabapentin?
ataxia, fatigue, sedation but there is less incidence of ADRs than with other drugs
What are the interactions of gabapentin?
may increase phenytoin blood levels at higher doses
What is lamotrigine used for?
DOC for partial and atypical absence seizures, backup in clonic-tonic and absence seizures; can be given alone better tolerated than other
In addition to lamotrigine's effects on seizure activity what other action does it have?
improves depression
what is the structure, administration and metabolism of lamotrigine?
looks vaguely like anti-folate drugs, well absorbed PO, metabolized by liver enzymes to inactive metabolites
What is the M.O. of lamotrigine?
like phenytoin - suppresses sustained rapid firing of neurons via sodium channels, is a glutamate antagonist and may can on calcium channels
what are the ADRs of lamotrigine?
diplopia, blurred vision, rhinits, skin reactions due to hypersenstivity, Steven-Johnson syndrome
What are the interactions of lamotrigine?
increased breakdown when given with carbamazepine
What is the indication of use of lamotrigine in pregnancy?
risk cannot be ruled out
What is levetiracetam used for?
back up in tonic-clonic and partial seizures
What is the structure, administration, binding and metabolism of levetiracetam?
cyclized version of GABA, well absorbed PO, low PP binding, small amount metabolied by P450s
what are the ADRs of levetiracetam?
dizziness, sedation, irritability; phychosis; tolearnce can develop rapidly
what is the indication of use of levetiracetam in pregnancy?
risk cannot be ruled out
What is oxcarbazepin used for?
DOC for partial seizures
what is the structure and half life of oxcarbazepin?
it is an active metabolite of carbamazepine with a shorter half life - 8-10 hours
what is the desired blood concentration of oxcarbazepin?
double that of carbamazepine
what are the ADRs of oxcarbazepin?
sedation, dizziness, diplopia, ataxia, N&V, less induction of P450 than with carbamzepine
What is the indication of use of oxcarbazepin in pregnancy?
positive evidience of risk - ONLY use of benefit outweighs risk
What are the uses of phenobarbital and primidone?
reserved for infants due to fast absorption for quick effects; but cognitive effects with long term use in kids under 6 occurs
what is the structure, administration and half lives of phenobarbital and primidone?
they are barbiturates, well absorbed PO; phenobarbital half life = 24 hours; primidone half life = 100 hrs
What are the ADRs of phenobarbital and primidone?
CNS depression, dependence, tolerance, cognitive effects; primidone has more N&V
how are phenobarbital and primidone related?
primidone is a prodrug that is converted to phenobarbital
What are the interactions of phenobarbital and primidone?
they are inducers of P450 = many interactions
What is the indication of use of phenobarbital or primidone in pregnancy?
risk cannot be ruled out
What is phenytoin used for?
DOC in tonic clonic and partial seizures - VERY EFFECTIVE!
what is the administration, binding and metabolism of phenytoin?
can be given IV or PO - acidic = poor PO absorption; highly PP bound, non-linear metabolism
What is dilantin?
an extended release form of phenytoin
what is the M.O. of phenytoin?
alters multiple channels, NA >>> Ca; and is an anti-arrhythmic drug
What are the ADRs of phenytoin?
drowsiness, gingival hyperplasia, mystagmus, hirsutism, skin rash and fever, lymphadenopathy - can be fata, may present like leukemia
what are the interactions of phenytoin?
potent inducer of many liver enzymes (P450s, MFOs) = many interactions
what is the indication of use of phenytoin in pregnancy?
positive evidience of risk - ONLY use of benefit outweighs risk
what is pregabalin used for?
DOC for peripheral neuropathy, secondary agent for partial seizures; NOT used for myoclonic or absence seizures
What ist he structure and half life of pregabalin?
GABA analog, half life = 6 hrs
What is the M.O. of pregabalin?
GABA potentiation
What are the ADRs of pregabalin?
dizziness, somnolence, dry mouth, blurred vision, peripheral edema, abnormal thinking, euphoria, myoclonus
what are the interactions fo pregabalin?
thiazolidinedions + pregabalin cause increased weight gain and peripheral edema
What is tiagabine used for?
back up in partial seizures
What is the structure, binding and metabolism of tiagabine?
"rationally designed" based on GABA structure, highly PP bound, metabolized by P450s but NOT an inducer
what are the ADRs of tiagabine?
GI upset, dizziness, tremor and drowsiness
What are the interactions of tiagabine?
does NOT affect liver enzymes = less chance of interactions
what is the indication of use of tiagabine during pregnancy?
risk cannot be ruled out
What is topiramate used for?
back up in partial seizures
What is the structure, administration, binding, metabolism and half life of topiramide?
substituted monosaccharide (structurally different from AEDs), well absorbed PO, low PP binding, metabolized by the liver; half life = 21 horus
What is the M.O. of topiramide?
acts on GABA receptors, decreases sodium channels/repetitive firing of neurons, decrease glutamate-mediated neurotransmission
What are the ADRs of topiramide?
sedation, nervousness, dizziness, drowsiness, fatigue, mental dulling, speech problems, renal stones
What are the interations of topiramide?
CNS depressants can increase drowsiness
What is the indication of use of topiramide in pregnancy?
risk cannot be ruled out
What is valproate used for?
BROADEST SPECTRUM AED, DOC for absence seizures, also used in migraines and bipolar disorder
What is the braodest spectrum AED?
valproate
What is the M.O. of valproate?
decreases sodium cahnnels, increases GABA availability at the neuronal synapse
What are the ADRs of valproate?
GI upset, hepatoxicity, thrombocytopenia
What are the interactions of valproate?
displaces phenytoin from PP binding, especially at high doses
What is zonisamide used for?
back up for absence seizures
What is the structure, administration, half life, binding and metabolism of zonisamide?
sulfonamide derivative, well absorbed PO, half life = 1-3 days, low PP binding, metabolized by CYP3A4 but does NOT induce liver enzymes
What is the M.O. of zonisamide?
braod spectrum - increases GABA function, decreases sodium and t-type calcium channels, decreases glutamate transmission
What are the ADRs of zonisamide?
congitive impariment, drowsiness, nausea, diarrhea, hypersensitivity - Stevens-Johnson syndrome
When is zonisamide contraindicated?
in patients with sulfonamide allergies
What are the interactions of zonisamide?
drugs that induce of reduce P450 levels
What AEDs can be used to treat neuropathic pain?
gabapentin, pregabalin and duloxetine
What AEDs can be used to treat migraine headaches?
used as prophylaxis - valproic acid, topiramide, zonisamide and iamotrigine
What AEDs can be used to treat bipolar disorder?
valproic acid - may be as effective as lithium; carbamazepine and lamotrigine
What is the effect of AEDs that act at chloride channels?
GABA potentiation that causes global downregulation in neuronal firing
What is the effect of AEDs that act at sodium channels?
block sodium channels by binding to/stabilizing inactivated channels
What is the effect of AEDs that act at calcium channels?
block calcium channels and thus block rhythmic firing of thalamic neurons
What are the DOCs for tonic-clonic seizures?
phenytoin and carbamazine
What are the DOCs for absence seizures?
ethosuximid and valproate
What is the DOC for Lennox-Gestaut syndrome?
felbamate
What are the DOCs for partial seizures?
phenytoin, carbamazine, lamotrigine and oxcarbazepin
What is the DOC for atypical absence seizures?
lamotrigine
What is the DOC for peripheral neuropathy?
pregabalin