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