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60 Cards in this Set
- Front
- Back
DOC for tonic-clonic seizures
|
-carbamazepine
-phenytoin |
|
DOC for simple partial seizures
|
-carbamazepine
-phenytoin |
|
DOC for complex partial seizures
|
-carbamazepine
-phenytoin |
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DOC for absence seizures
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-ethosuximide
|
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DOC for myoclonic
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-clonzazepam
|
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what drugs are ineffective in the tx of absence and myoclonic seizures?
|
-carbamazepine
-phenytoin |
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which drug is ineffective in simple and complex partial seizures?
|
-ethosuximide
|
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what drug is considered 1st generation antiepileptic drug (AED)?
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phenytoin
|
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what are the major clinical uses of phenytoin?
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-1st line AED for chronic outpatient therapy
-2nd line drug in management of status epilepticus |
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phenytoin sodium injection has been replaced with ______
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-fosphenytoin sodium
|
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fosphenytoin sodium injection
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-a water-soluble disodium phosphate ester prodrug of phenytoin that is rapidly converted to phenytoin in plasma
|
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fosphenytoin sodium injection is indicated for?
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-short-term tx of acute seizures (IV for status epilepticus)
-prevention of seizures during neurosurgery -and as a substitute for oral phenytoin when oral dosing is not feasible |
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suspension and tablet forms of phenytoin contain__________and are NOT intended for________
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1. the free acid form of phenytoin
2. once daily dosing |
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capsule contain the ______ of phenytoin and are the only oral formulation approved for ________ due to its ________
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1. sodium salt
2. once-a-day dosing (extended release) 3. slow dissolution and absorption |
|
describe the biotransformation of phenytoin
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-dose-dependent metabolism
-saturates hepatic P450 enzymes responsible for metabolism -small increases in dosage results in large increases in plasma levels |
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ADR of the IV dosage forms of phenytoin
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-hypotension, bradycardia
|
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dose-related effects of phenytoin:
1. toxicity due to elevated plasma levels 2. overdose |
1. nystagmus, ataxia, decreased mentation
2. hypotension, seizures |
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ADR due to chronic toxicity of phenytoin
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-gingival hyperplasia
-hypertrichosis -coarsening,/thickening of facial features -osteomalacia due to abnl vitD metabolism |
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idiosyncratic rxns to phenytoin
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severe skin lesions
|
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teratogenicity of phenytoin?
|
fetal hydantoin syndrome (FHS):
-cleft lip/palate -craniofacial abnormalities -mental and physical growth retardation -congenital heart dz |
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phenytoin use in pregnancy/lactation?
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-risk/benefit ratio favors continued use of phenytoin during pregnancy
-compatible with breast feeding |
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indications for carbamazepine
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-DOC for mgmt of generalized tonic-clonic, simple or complex partial, mixed partial, or generalized seizure disorder
-pain relief of trigeminal neuralgia |
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carbamazepine has ___________; it induces its own metabolism
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autoinduction
|
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common ADR of carbamazepine
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-GI distress
-CNS: sedation, dizziness, fatigue, nystagmus, ataxia |
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occasional ADR of carbamazepine
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-rash, severe skin lesions
-fluid retention and causes SIADH |
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rare ADR of carbamazepine
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-bone marrow suppression with aplastic anemia or agranulocytosis (extremely rare)
-hepatotoxicity |
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Sx of carbamazepine overdose
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-ataxia, nystagmus, seizures
|
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__________ and ________ inhibit the metabolism of carbamazepine
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1. erythromycin
2. cimetidine |
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carbamazepine is a potent P450 inducing agent and increases the clearance of _______
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-theophylline, oral contraceptives, warfarin, and other AEDs
|
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use of carbamazepine with pregnancy/lactation?
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-risk/benefit ratio favors continued use during pregnancy
-compatible with breast-feeding |
|
_____________is GABAergic/GABAmimetic
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valproic acid
|
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anticonvulsant indications for valproic acid
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-monotherapy and adjunctive therapy in simple and complex absence seizures
-adjunct in multiple seizure types that include absence seizures -monotherapy and adjunctive therapy of pts with complex partial seizures that occur either in isolation or in association with other seizure types |
|
unlabeled indications for valproic acid
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-alone or in combo tx of myoclonic and tonic-clonic seizures
-may be effective in status epilepticus intractable to other agents |
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ADR of valproic acid
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-GI distress: take with food or use enteric coated form
|
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boxed warnings for valproic acid
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-rare, but life-threatening toxicities
-hepatoxicity -teratogenicity |
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use of valproic acid in pregnancy/lactation
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-teratogenic (must be essential to seizure mgmt to justify use)
-compatible with breast feeding |
|
___________ is the DOC for absence seizures
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ethosuximide
|
|
indications for clonazepam in seizure mgmt
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-tx of absence seizures unresponsive to ethosuxamide
-alone or as adjunctive tx of the Lennox-Gestaut syndrome (petit mal variant), akinetic, and myoclonic seizures |
|
prolonged (30-60 min) and continuous, rapidly repeating seizures without recovery from epileptic state
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status epilepticus (medical emergency)
|
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convulsive status epilepticus
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80% cases are the secondary generalized type with focal onset
|
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management of convulsive status epilepticus
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-dextrose to correct hypoglycemia
-IV lorazepam or diazepam -concurrent admin of a longer-acting anticonvulsant: IV loading dose of phenytoin sodium or fosphenytoin sodium |
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DOC for terminating seizures in convulsive status epilepticus are _____
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-IV lorazepam or diazepam
|
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IV lorazepam or diazepam in the tx of status epilepticus are contraindicated in__________
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acute alcohol intoxication with depression of vital signs
|
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typical anticonvulsant indications for adjuvants (2nd generation anticonvulsants)
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-adjunct therapy for partial seizures in adults
-adjunct therapy for patial seizures in kids -adjunct therapy for seizures associated with Lennox-Gestaut syndrome |
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Lennox-Gestatut syndrome characteristics
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-multiple seizure types, mentalretardation
-permanent intellectual, cognitive, and psychological defects -status epilepticus is common |
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gabapentin (adjuvant) indications in Lennox-Gestaut syndrome
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-adjunctive tx of partial seizures with/without secondary generalization in pts >12
-adjunctive tx of partial seizures in children 3-12yrs |
|
metabolism of gabapentin
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-excreted renally unchanged
-doesn't interact with other anticonvulsants which depend on P450 Sx for hepatic metabolism |
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hypersensitivity rxns with zonisamide (adjuvant)
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-may have cross-reactivity with other sulfa drugs, with hematological and dermatological toxicity
|
|
ADR of zonisamide (adjuvant)
|
-hypersensitivity rxns
-tendency for renal stone formation -psychiatric Sx -oligohydrosis-induced hyperthermia |
|
additive toxicity of zonisamide (adjuvant) with _________ can occur causing stone formation
|
topiramate
|
|
indications for pregabalin (adjuvant)
|
-adjunctive therapy in adults with partial onset seizures
-mgmt of postherpetic neuralgia -neuropathic pain associated with diabetic peripheral neuropathy -fibromyalgia |
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metabolism of pregabalin (adjuvant)
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-nonmetabolized; excreted unchanged in the urine
|
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ADR of pregabalin (adjuvant)
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-euphoria
-withdrawal symptoms when abruptly d/c |
|
adjuvant agents with monotherapy indications (3)
|
-felbamate
-lamotrigine -topiramate |
|
indications for felamate
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-monotherapy or adjuncitve therapy of partial and generalized seizures associated with Lennox-gestaut syndrome in children >2yrs
-rrecommended only in pts where other txs have failed such that the risk of hepatic failure and aplastic anemia is justified |
|
boxed warnings for felbamate
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-aplastic anemia
-acute hepatitis and hepatic failure -use only if benefit outweighs risk |
|
iondications for lamotrigine
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-adjunctive therapy in generalized seizures of Lennox-Gestaut syndrome in adult and pediatric pts >2yr
-conversion to monotherapy in adults >16yrs with partial seizures who are on tx with a single AED |
|
boxed warning for lamotrigine
|
-rash due to hypersensitivity rxn
-potential for severe, life-threatening rash -children are at high risk |
|
indications for topiramate
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-adjunctive therapy for pts >2 with partial onset seizures (primary generalized tonic-clonic seizures) and seizures associated with Lennox-Gestaut syndrome
-initial monotherapy of partial onset or primary generalized tonic-clonic seizures in pts >10yrs |
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topiramate is a _________________ which increases the risk of urolithiasis, particularly if used concurrently with _______; pt must maintain adequate fluid intake
|
1. weak carbonic anhydrase inhibitor (CAI)
2. another CAI |