anticonvulsant drugs Flashcards

1
Q

epilepsy

A

occurrence of at least 2 unprovoked seizures separated by 24 hours

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2
Q

partial/focal seizures

A
localized onset, ascertained either by observation or EEG
3 subcategories: 
-simple partial
-complex partial
-secondarily generalized seizure
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3
Q

simple partial seizure

A

minimal spread of abnormal discharge
normal consciousness
perserved awareness

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4
Q

complex partial seizure

A

localized onset, but discharge becomes widespread, almost always involves limbic system
pt may have automatisims, memory loss, aberrant behavior

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5
Q

secondarily generalized seizure

A

partial seizure immediately precedes a generalized tonic-clonic seizure

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6
Q

generalized seizures

A
those w/o evidence of localized onset
clinical manifestation indicate involvement of both brain hemispheres 
4 subcategories:
-generalized tonic-clonic/grand mal
-absence/ petit mal
-myoclonic jerking
-atonic
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7
Q

generalized tonic-clonic/grand mal

A

sudden sharp tonic contraction followed by rigidity and clonic mvmts
pt may cry/moan, lose sphincter control, bite tongue, cyanotic
after seizure pt may have altered consciousness, drowsiness, or confusion

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8
Q

absence/petit mal

A

sudden onset and abrupt cessation, altered consciousness, blank stare
young kids-adolescence

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9
Q

myoclonic jerking

A

brief, shock-like mm contraction’

occur in wide variety of seizures

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10
Q

atonic seizures

A

sudden loss of postural tone, head drop, fall to floor, slumping
many pts wear helmet

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11
Q

generalization of Rx seizure Tx

A

suppress do not cure
should try different monotherapies before combining drugs
compliance is VERY important
generics may not be a good idea

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12
Q

MOA of AEDs in general

A
  • affect ion Ch kinetics (delay NaCh recovery)
  • augmenting inhibitory neurotransmission
  • modulating excitatory neurotransmission
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13
Q

PK of AEDs in general

A

cleared chiefly by hepatic metabolism

many are potent CYP inducers

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14
Q

general ADRs of AEDs

A

common neurotoxic effects- sedation, dizziness, blurred or double vision, difficulty concentrating, and ataxia

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15
Q

phenytoin MOA

A
  • blocks sustained high frequency firing of APs d/t preferential binding and prolongation of inactivated NaCh
  • decrease synaptic release of glutamate and enhances release of GABA
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16
Q

phenytoin PK

A
cannot be given IM- fosphenytoin can be injected
highly protein bound 
elimination dose-dependent
CYP meta
narrow therapeutic index
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17
Q

phenytoin uses

A

partial seizures

generalized tonic-clonic seizures

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18
Q

phenytoin ADRs

A

gingival hyperplasia, hirsutism
in early use can present w/rash, fever, hepatits, and lymphadenopathy,
rarely causes dermatits and stevents-johnson syndrome

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19
Q

phenytoin long term ADRs

A

worsening facial features
mild peripheral neuropathy
vit D meta abnormalities -> osteomalacia

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20
Q

phenytoin cardiac ADRs

A

hypotension, bradycardia, cardiac arrythmia, CV collapse, venous irritation, pin, thrombophlebitis

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21
Q

Phenytoin DDIs

A

related to protein binding- sulfonamides

related to meta- warfarin (increased INR), OBC (increased risk of prego)

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22
Q

carbamazepine and oxcarbazepine MOA

A

NaCh -> inhibit high frequency repetitive firing

also acts presynaptically to decrease release of glutamate

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23
Q

carbamazepine and oxcarbazepine PK

A

hepatic meta

potent CYP inducer (including its own meta)

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24
Q

carbamazepine and oxcarbazepine uses

A

partial seizures, generalized tonic-clonic seizures, trigeminal neuralgia, mania in bipolar disorder

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25
Q

carbamazepine and oxcarbazepine ADRs

A
hyponatremia and water intoxication
blood dyscrasias (fatal aplastic anemia and agranulocytosis, leukopenia)- monitor
mild rash to stevens-johnson syndrome
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26
Q

carbamazepine and oxcarbazepine DDIs

A

increases meta of primidone, phenytoin, OBC, valpronic acid

valpronic acid may decrease clearance

27
Q

gabapentin and pregabalin MOA

A

analogs of GABA, but do not act directly on GABAR

bind N-type CaCh -> decrease Ca entry -> decrease release of glutamate

28
Q

gabapentin uses

A

partial seizures
generalized tonic-clonic seizures
neuropathic pain
post-herpetic neuralgia

29
Q

gabapentin and pregabalin ADRs

A

HA, tremor

pregabalin- controlled substance b/c may induce euphoria

30
Q

lamotrugine MOA

A

suppresses sustained rapid firing of neurons and produces volatage and use-dependent inactivation of NaChs
inhibits V-CaChS

31
Q

lamotrugine uses

A

adjunct when >2yrs old for partial seizures and generalized seizures
monotherapy in adults for partial seizures, adjucnt for primary genrealized tonic-clonic
also used for bipolar disorder

32
Q

lamotrugine ADRs

A

nausea
somnolence
rash
rare stevens-johnson syndrome

33
Q

lamotrugine DDIs

A

may increase concentration with concurrent use of OBC as well as decrease OBC efficacy

34
Q

levetiracetam MOA

A

binds selectively to synaptic vesicular protein modifies synaptic release of glutamate and GABA

35
Q

levetiracetam uses

A

adjunct
partial seizures in adults and kids
primary generalized tonic-clonic seizures
myoclonic seizures of juvenile myoclonic epilepsy

36
Q

levetiracetam ADRs

A

less common more serious mood and behavioral changes

37
Q

ethosuximide MOA

A

reduces the low T-type CaCH threshold (thalamic pace maker)

38
Q

ethosuximide uses

A

absence seizures

39
Q

ethosuximide ADRs

A

gastric distress

40
Q

ethosuximide DDIs

A

valproic acid may inhibit meta or ethosuximide

41
Q

valproic acid MOA

A

blocks sustained high frequency firing of neurons

action against partial seizures d/t effect on Na current via bockde of NMDARs

42
Q

valproic acid PK

A

fully ionized at body pH

highly protein bound

43
Q

valproic acid uses

A
absence seizures
myoclonic seizures
generalized tonic-clonic seizures
partial seizures
status epilepticus
bipolar
migraine prophylaxis
44
Q

valproic acid ADRs

A

GI, heartburn
fine tremor
weight gain, increased appetite, hair loss
hepatotoxic, thrombocytopenia *monitor

45
Q

first line for partial seizures, including seondarily gerneralized

A

carbamazepine
lamotrigine
oxcarbazepine
levetiracetam

46
Q

first line for primary generalized tonic-clonic

A

valproate
lamotrigine
levetiracetam

47
Q

first line for

absence seizures

A

ethosuximide

valproate

48
Q

atypical absence, myocloinic, atonic

A

valproate
lamotrigine
levetiracetam

49
Q

which drugs enhance NaCh inactivation?

A
carbamazepine
phenytoin
topiramate
lamotrigine
valproate
zonisamide
50
Q

which drugs enhance GABA synaptic transmission

A

vigabatrin and valproate (both decrease GABA breakdown in neuron)
tiagabine (inhibit GABA transport out of cleft)
benzodiazepines and barbituates (bind GABARs)

51
Q

which drugs reduce Ca current?

A

valproate

ethosuzimide

52
Q

Stevens-johnson syndrome

A

asians w/HLA-B1502

53
Q

topiramate MOA

A

NaCh
GABARs
CaChs
can also act on glutamate/NMDARs

54
Q

topiramate uses

A

partial, generalized tonic-clonic, infantile spasms, absence seizures, migranes

55
Q

topiramate ADRs

A

paresthesias
nervousness
weight loss

56
Q

diazepam MOA

A

enhance GABA mediated Cl influx

57
Q

diazepam MOA

A

extremely lipophillic

58
Q

diazepam uses

A

status epliepticus
myoclonic
partial
generalized tonic-clonic

59
Q

phenobarbital MOA

A

enahances GABA mediates current and decrease glutamate release

60
Q

phenobarbital P

A

hepatic enzyme inducer

61
Q

phenobarbitol uses

A

partial seizues

generalized tonic-clonic

62
Q

what drugs mess with OBC effectiveness

A
carbamazepine
oxcarbamazepine
phenobarbital
phenytoin
primidone
ruginamide
63
Q

which drugs are teratogenic

A

phenytoin
valproate
topiramate