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60 Cards in this Set

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DOC for tonic-clonic seizures
-carbamazepine
-phenytoin
DOC for simple partial seizures
-carbamazepine
-phenytoin
DOC for complex partial seizures
-carbamazepine
-phenytoin
DOC for absence seizures
-ethosuximide
DOC for myoclonic
-clonzazepam
what drugs are ineffective in the tx of absence and myoclonic seizures?
-carbamazepine
-phenytoin
which drug is ineffective in simple and complex partial seizures?
-ethosuximide
what drug is considered 1st generation antiepileptic drug (AED)?
phenytoin
what are the major clinical uses of phenytoin?
-1st line AED for chronic outpatient therapy
-2nd line drug in management of status epilepticus
phenytoin sodium injection has been replaced with ______
-fosphenytoin sodium
fosphenytoin sodium injection
-a water-soluble disodium phosphate ester prodrug of phenytoin that is rapidly converted to phenytoin in plasma
fosphenytoin sodium injection is indicated for?
-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
suspension and tablet forms of phenytoin contain__________and are NOT intended for________
1. the free acid form of phenytoin
2. once daily dosing
capsule contain the ______ of phenytoin and are the only oral formulation approved for ________ due to its ________
1. sodium salt
2. once-a-day dosing (extended release)
3. slow dissolution and absorption
describe the biotransformation of phenytoin
-dose-dependent metabolism
-saturates hepatic P450 enzymes responsible for metabolism
-small increases in dosage results in large increases in plasma levels
ADR of the IV dosage forms of phenytoin
-hypotension, bradycardia
dose-related effects of phenytoin:
1. toxicity due to elevated plasma levels
2. overdose
1. nystagmus, ataxia, decreased mentation
2. hypotension, seizures
ADR due to chronic toxicity of phenytoin
-gingival hyperplasia
-hypertrichosis
-coarsening,/thickening of facial features
-osteomalacia due to abnl vitD metabolism
idiosyncratic rxns to phenytoin
severe skin lesions
teratogenicity of phenytoin?
fetal hydantoin syndrome (FHS):
-cleft lip/palate
-craniofacial abnormalities
-mental and physical growth retardation
-congenital heart dz
phenytoin use in pregnancy/lactation?
-risk/benefit ratio favors continued use of phenytoin during pregnancy
-compatible with breast feeding
indications for carbamazepine
-DOC for mgmt of generalized tonic-clonic, simple or complex partial, mixed partial, or generalized seizure disorder
-pain relief of trigeminal neuralgia
carbamazepine has ___________; it induces its own metabolism
autoinduction
common ADR of carbamazepine
-GI distress
-CNS: sedation, dizziness, fatigue, nystagmus, ataxia
occasional ADR of carbamazepine
-rash, severe skin lesions
-fluid retention and causes SIADH
rare ADR of carbamazepine
-bone marrow suppression with aplastic anemia or agranulocytosis (extremely rare)
-hepatotoxicity
Sx of carbamazepine overdose
-ataxia, nystagmus, seizures
__________ and ________ inhibit the metabolism of carbamazepine
1. erythromycin
2. cimetidine
carbamazepine is a potent P450 inducing agent and increases the clearance of _______
-theophylline, oral contraceptives, warfarin, and other AEDs
use of carbamazepine with pregnancy/lactation?
-risk/benefit ratio favors continued use during pregnancy
-compatible with breast-feeding
_____________is GABAergic/GABAmimetic
valproic acid
anticonvulsant indications for valproic acid
-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
-alone or in combo tx of myoclonic and tonic-clonic seizures
-may be effective in status epilepticus intractable to other agents
ADR of valproic acid
-GI distress: take with food or use enteric coated form
boxed warnings for valproic acid
-rare, but life-threatening toxicities
-hepatoxicity
-teratogenicity
use of valproic acid in pregnancy/lactation
-teratogenic (must be essential to seizure mgmt to justify use)
-compatible with breast feeding
___________ is the DOC for absence seizures
ethosuximide
indications for clonazepam in seizure mgmt
-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
status epilepticus (medical emergency)
convulsive status epilepticus
80% cases are the secondary generalized type with focal onset
management of convulsive status epilepticus
-dextrose to correct hypoglycemia
-IV lorazepam or diazepam
-concurrent admin of a longer-acting anticonvulsant: IV loading dose of phenytoin sodium or fosphenytoin sodium
DOC for terminating seizures in convulsive status epilepticus are _____
-IV lorazepam or diazepam
IV lorazepam or diazepam in the tx of status epilepticus are contraindicated in__________
acute alcohol intoxication with depression of vital signs
typical anticonvulsant indications for adjuvants (2nd generation anticonvulsants)
-adjunct therapy for partial seizures in adults
-adjunct therapy for patial seizures in kids
-adjunct therapy for seizures associated with Lennox-Gestaut syndrome
Lennox-Gestatut syndrome characteristics
-multiple seizure types, mentalretardation
-permanent intellectual, cognitive, and psychological defects
-status epilepticus is common
gabapentin (adjuvant) indications in Lennox-Gestaut syndrome
-adjunctive tx of partial seizures with/without secondary generalization in pts >12
-adjunctive tx of partial seizures in children 3-12yrs
metabolism of gabapentin
-excreted renally unchanged
-doesn't interact with other anticonvulsants which depend on P450 Sx for hepatic metabolism
hypersensitivity rxns with zonisamide (adjuvant)
-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
metabolism of pregabalin (adjuvant)
-nonmetabolized; excreted unchanged in the urine
ADR of pregabalin (adjuvant)
-euphoria
-withdrawal symptoms when abruptly d/c
adjuvant agents with monotherapy indications (3)
-felbamate
-lamotrigine
-topiramate
indications for felamate
-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
-aplastic anemia
-acute hepatitis and hepatic failure
-use only if benefit outweighs risk
iondications for lamotrigine
-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
-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
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