Pharm anticonvulsants Flashcards

1
Q

definition of epilepsy

A

at least 2 unprovoked seizures separated by 24 hours

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2
Q

what single events can precipitate seizusres

A

withdrawal of CNS depressants
acute neuro illness or toxic systemic
fever

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3
Q

what is a simple partial seizure

A

minimal spread of abnormal discharge, normal consciousness, preserved awareness

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4
Q

what is a complex partial seizure

A

localized onset but discharge becomes widespread, almost always involves limbic system

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5
Q

characterstics of complex partial seizure

A

lip smacking, swallowing fubmling, scratching, memory loss or aberrant behavior

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6
Q

secondarily generalized seizure

A

partial that immediately precedes a generalized tonic clonic seizure

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7
Q

what is a generalized seixure

A

without evidence of localized onset, both brain hemispheres involved

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8
Q

what is a grand mal seizure

A

generalized tonic clonic
sudden, sharp tonic contraction followed by rigidity and clonic movements
patient may cry, moan, lose sphincter control, bite tongue or develop cyanosis

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9
Q

after grand mal seizure, patient may have

A

altered consciousness, drowsiness or confusion

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10
Q

postictal Sx of seizure

A

grand mal

generalized tonic clonic

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11
Q

what is an absence seizure

A

sudden onset and abrupt cessation, altered consciousness,
a blank stare
usually young children through adolescence

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12
Q

myoclonic jerking

A

brief shock like muscle contractions

occur in wide variety of seizures

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13
Q

atonic seizures

A

sudden loss of postural tone, head drop, fall to floor, slumping
many patients wear helmets to prevent head injury

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14
Q

AED treatments

A

suppress seizures but do not cure of prevent epilepsy

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15
Q

how do you switch AED Tx monotherapy

A

taper off initial AED after second AED is titrated to therapeutic level

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16
Q

MOA AED

A

affect ion channel kinetics
augmenting inhibitory neurotransmission
modulating excitatory neurotransmission

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17
Q

which AEDs are highly protein bound

A

phenytoin
tigabine
valproic acid

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18
Q

how are AEDs cleared

A

hepatic metabolism

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19
Q

Adverse effects AEDs

A

sedation, dizziness, blurred or double vision, difficulty concentrating and ataxia

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20
Q

MOA phenytoin

A

blocks sustained high frequency firing action potentials due to preferential binding to and prolongation of inactivated state of Na channel
also dec glutamate and enhances GABA release

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21
Q

PK phenytoin

A
not IM
erratic absorption
highly protein bound
low dose first order kinetics
high dose disproprotionate elimination
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22
Q

use of phenytoin

A

partial seizures, generalized tonic-clonic seizures

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23
Q

adverse effects phenytoin

A

diplopia, ataxia, nystagmus, sedation, gingival hyperplasia, hirsutism

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24
Q

long term adverse effects phenytoin

A

worsening facial features, mild peripheral neuropathy

abnormalities in vit D metabolism causing osteomalacia

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25
cardiac effects of phenytoin
hypotension, bradycardia, cardaic arrhythmia, CV collapse, venous irritation and pain, thrombophlebitis
26
DDI phenytoin
related to protein binding sulfonamides by dispalce phenytoin from site increasing the amount of free drug! CYP2C9, increased warfarin!!! CYP3A4, increased risk pregnancy on oral contraceptives
27
MOA carbamazepine
acts on Na Ch resulting in inhibition of high frequency repetitive firing also acts presynaptically to decrease synaptic release of glutamate
28
PK carbamezepine
autounduction, increased expression of CYPs and UGT
29
use of carbamezapine
partial seizures, generalized tonic-clonic seizures, trigeminal neuralgia, mania in bipolar disorder
30
adverse effects carbamazepine
diplopia, ataxia, mild GI upset, unsteadiness, drowsiness hyponatremia and water intoxication idiosyncratic blood dyscrasias rash, sometimes stevens johnson
31
what patients at higher risk stevens johnson syndrome reaction from carbamazepine
asians with HLA B*1502
32
DDI carbamazepine
hepatic enzyme induction leading to increased metabolism of other drugs
33
what drug inhibits carbamazepine clearance (increased levels)
valproic acid
34
what drug has fewer DDI than carbamazepine
oxcarbazepine
35
MOA phenobarbital
binds GABA and enhances GABA mediated current by prolonging Cl Ch
36
MOA gabapentin
analogs of GABA | bind 2alphadelta on vNtype Ca Ch decreasing Ca, decreasing release of glutamate
37
use of gabapentin
partial seizures, generalized tonic-clonic seizures, neuropathic pain post herpetic neuralgia
38
adverse to gabapentin
somnolence, dizziness, ataxia, HA, tremor
39
MOA lamotrigine
like pheytoin suprres neurons through inactivation Na Ch | inhibits vCa Ch
40
uses of lamotrigine
> 2y.o with partial seizures or generalized also used for monotherpay partial seizures adjunct in primary generalized tonic clonic absence bipolar
41
adverse effects lamotrigine
dizziness, HA, diplopia, ataxia, nausea, somnolence, skin rash
42
DDI lamotrigine
concentrations decrease with use oral contraceptives (E component) may lead to contraceptive failure in P only pill
43
MOA levetiracetam
binds to synaptic vesicular protein SV2A modifies synaptic release of glutamate and GABA through action on vesicular function
44
use of levetiracetam
adjunct for partial seizures in adults and children primary generalized tonic clonix myoclonic seizures of jevenile epilipsy
45
adverse effects levetiracetam
somnolence, asthenia, ataxia dizziness
46
adverse effect tigabine
cause seizures in some patients who take tiagabine for bipolar disorder, anxiety and neuropathic pain
47
MOA ethosuximide
reduce threshold Ca T type which are pacemaker for thalamic neurons
48
use of ethosuximide
absence seizures
49
adverse effects ethosuximide
gastric distress, pain , nausea and vomiting
50
DDI ethosuximide
valproic acid can inhibit metabolism of ethosuximide
51
MOA valproic acid and Na valporate
blocks firing of neurons through Na currents blocks NMDA R mediated excitation increased levels GABA in brain
52
use of valproic acid
``` absence seizures myoclonic seizures generalized tonic clonic seizures partial seizures status epilepticus (IV bipolar disorder migraine prophylaxis ```
53
adverse effects valproic acid
nausea, vomiting, abdominal pain, heartburn fine tremor weight gain, hair loss hepatotoxicity and thrombocytopenia
54
what must you monitor if put patient on valproic acid
liver function because of hepatotoxicity
55
MOA diazepam
bind GABAa R | increase GABA Cl Ch to increase inhibitory membrane potentials
56
PK diazepam
lipophilic, goes to CNS in sec when IV | redistributes to fat quickly
57
why do you give a longer acting AED after giving diazepam
prevent seizure recurrence
58
therapeutic use diazepam
status epilepticus, adjunct, myoclonic, partial, and generalized tonic clonic seizures
59
adverse effects to diazepam
sedative drowsiness ataxia behavior disorders
60
first DOC for partial seizures and secondarily generalized
carbamazepine or lamotrigrine or oxcarbazepine or levetiracetam
61
second line of drugs for partial seizures or secondarily generalized
topiramate, gabapentin, pheytoin
62
first DOC for primary generalized tonic clonic or grand mal
valporate lamotrigine levetiracetam
63
second line for grand mal seizure
carbamazepine, phenytoin
64
first DOC for absence seizures
ethosuximide | or valproate
65
second DOC for absence seizures
lamotrigine | levetiracetam
66
first DOC for atypical absence of myoclonic or atonic seizures
valproate lamotrigine levetiracetam
67
teratogenicity of AED
increased risk congenital malformations
68
phenytoin teratogenicity
fetal hydantoin syndrome (abnormal skull, facial features, growth deficiency, underdeveloped nails or mild developmental delays)
69
what AED indicated in spina bifida
valproate