Antiepileptic Drugs Flashcards

1
Q

cannabidiol indications

A

seizures within the spectrum of Lennox-Gastaut, which includes all seizure types, even a small percentage of typical absence seizures
approved for seizures associated with DS

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2
Q

cannabidiol initial dose

A

5mg/kg/day bid x1 wk

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3
Q

cannabidiol maintenance dose

A

10mg/kg/day bid

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4
Q

cannabidiol maximum dose

A

20mg/kg/day bid

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5
Q

cannabidiol considerations

A

serum transaminases and bilirubin levels recommended before starting

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6
Q

cannabidiol adverse effects

A

somnolence, decreased appetite, diarrhea, elevation in transaminases, fatigue, and insomnia

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7
Q

cannabidiol drug interacitons

A

reduces metabolism of clobazam (reduce dose)

w/ valproate increases transaminase elevation

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8
Q

brivaracetam (briviact) mechanism

A

similar to levetiracetam
binds the presynaptic vesicle glycoprotein A2
no calcium channel or AMPA receptor effect

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9
Q

brivaracetam (briviact) indications

A

localization related epilepsies, but may have wide spectrum of efficacy

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10
Q

brivaracetam (brivact) doses available

A

10, 25, 50, 75, and 100mg tablets, IV solution of 50mg/5mL and oral 10mg/mL

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11
Q

brivaracetam (brivact) half life

A

9hrs

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12
Q

brivaracetam (brivact) initial dose

A

adolescents >16 years old: 50mg bid x1 wk

may be raised to 100mg bid

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13
Q

brivaracetam (brivact) adverse effects

A

overall greater tolerability with fewer behavioral or mood side effects

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14
Q

carbamazepine (tegretol) indications

A

partial seizures, primary or secondary generalized tonic-clonic seizures

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15
Q

carbamazepine (tegretol) considerations

A

increases the frequency of absence and myoclonic seizures and is therefore contraindicated

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16
Q

carbamazepine (tegretol) pharmacokinetics

A

85% protein-bound
induces its own metabolism
initial dose should be 25% of maintenance dose to prevent toxicity

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17
Q

carbamazepine (tegretol) usual maintenance dose

A

15-20mg/kg/day to provide blood concentration of 4-12 microg/mL

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18
Q

carbamazepine (tegretol) maintenance dose infants

A

often require 30mg/kg/day

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19
Q

carbamazepine (tegretol) half life

A

5-27hrs

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20
Q

carbamazepine (tegretol) dose frequency

A

children usually require 3x/day

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21
Q

carbamazepine (tegretol) drug interactions

A

concurrent use of cimetidine, erythromycin, grapefruit, fluoxetine, and propoxyphene interferes with carbamazepine metabolism and causes toxicity

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22
Q

carbamazepine (tegretol) adverse effects

A

depression of peripheral leukocytes is expected
screen for HLA-B*1502 in Asian ancestry to decrease risk of Stevens-Johnson syndrome and toxic epidermal necrosis
cognitive disturbances
sedation, ataxia, and nystagmus at toxic blood concentrations

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23
Q

clobazam (onfi) indications

A

seizures within the spectrum of Lennox-Gastaut, which includes all seizure types, even a small percentage of typical absence seizures

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24
Q

clobazam (onfi) initial dose

A

if <30kg: 5mg daily, titrating up to 20mg/day (divided bid)

if >30kg: 10mg daily, titrating up to 40mg/day (divided bid)

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25
Q

clobazam (onfi) adverse effects

A

sedation

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26
Q

clonazepam (klonopin) indications

A

infantile spasms, myoclonic seizures, absence, and partial seizures

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27
Q

clonazepam (klonopin) initial dose

A

0.025 mg/kg/day divided into 2 doses

increase 0.025 mg/kg q3-5 days

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28
Q

clonazepam (klonopin) usual maintenance dose

A

0.1 mg/kg/day in 3 divided doses

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29
Q

clonazepam (klonopin) therapeutic blood concentration

A

0.02-0.07 microg/mL

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30
Q

clonazepam (klonopin) pharmacokinetics

A

47% protein-bound

half life 20-40hrs

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31
Q

clonazepam (klonopin) adverse effects

A

toxic effects within therapeutic range include sedation, cognitive impairment, hyperactivity, and excessive salivation

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32
Q

ethosuximide indications

A

drug of choice for treating absence epilepsy

also useful for myoclonic absence

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33
Q

ethosuximide pharmacokinetics

A

absorbed rapidly
peak blood concentrations within 4 hours
half life 30hrs in children

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34
Q

ethosuximide initial dose

A

20mg/kg/day in 3 divided doses after meals

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35
Q

ethosuximide dose increments

A

10mg/kg/day as needed and tolerated

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36
Q

ethosuximide therapeutic levels

A

between 50 and 120 microg/mL

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37
Q

ethosuximide adverse effects

A

nausea and abdominal pain from gastric irritation

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38
Q

felbamate indications

A

wide spectrum of anti epileptic activity

primary use for refractory partial and generalized seizures, the LGS, atypical absence, and atonic seizures

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39
Q

felbamate pharmacokinetics

A

rapidly absorbed after oral intake

max plasma occurs in 2-6hrs

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40
Q

felbamate initial dose

A

15mg/kg/day in three divided doses

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41
Q

felbamate considerations

A

avoid nighttime doses if the drug causes insomnia

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42
Q

felbamate dose increments

A

weekly increments of 15mg/kg as needed

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43
Q

felbamate total dose

A

45mg/kg/day

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44
Q

felbamate therapeutic levels

A

between 50 and 100 microg/mL

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45
Q

felbamate adverse effects

A

mild and dose related - nausea, anorexia, insomnia, weight loss except in combination with other antiepileptic drugs
fatal liver damage and aplastic anemia in about 1 in 10,000 exposures

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46
Q

felbamate drug interactions

A

increases plasma concentrations of phenytoin and valproate by as much as 30%
carbamazepine concentration falls, but concentration of active epoxide metabolite increases almost 50%

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47
Q

gabapentin indications

A

partial seizures with and without secondary generalization and neuropathic pain

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48
Q

gabapentin titration dose

A

10-60mg/kg/day over 2 weeks

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49
Q

gabapentin adverse effects

A

sedation, edema, and increased weight

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50
Q

lacosamide (vimpat) indications

A

partial seizures with and without secondary generalization

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51
Q

lacosamide (vimpat) titration dose

A

from 2-10mg/kg/day over 2-4 weeks

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52
Q

lacosamide (vimpat) mechanism of action

A

on sodium channel, but different than traditional sodium channel anticonvulsants

53
Q

lacosamide (vimpat) adverse effects

A

sedation, ataxia, and dizziness

54
Q

lamotrigine (lamictal) indications

A

useful in absence epilepsy, absence seizures, JME, and LGS, partial epilepsies, and primary generalized tonic-clonic seizures
spectrum of activity similar to valproate

55
Q

lamotrigine (lamictal) initial doses

A

monotherapy: 0.3mg/kg/day
liver enzyme inducing drugs: 0.6mg/kg/day
with valproate: 0.15mg/kg/day for the first 2 weeks then increase by same amount daily

56
Q

lamotrigine (lamictal) maintenance doses

A

monotherapy: 5-7mg/kg/day
with valproate: 1-3mg/kg/day
liver enzyme inducers: 5-15mg/kg/day

57
Q

lamotrigine (lamictal) adverse effects

A

rash, which is more likely with titrations faster than recommended
dizziness, ataxia, diplopia, insomnia, and headache

58
Q

levetiracetam (keppra) indications

A

broad spectrum of activity and useful in most seizure types
especially effective in JME
excellent first line for most epilepsies

59
Q

levetiracetam (keppra) initial dose

A

20mg/kg/day divided bid

60
Q

levetiracetam (keppra) target dose

A

20-80mg/kg/day video BID

61
Q

levetiracetam (keppra) status epilepticus

A

bolus of 60mg/kg/day

62
Q

levetiracetam (keppra) adverse effects

A

minimally liver metabolized
excreted in urine
makes some children cranky
small dose of pyridoxine 50mg relieves irritability

63
Q

levetiracetam (keppra) mechanism of action

A

probably an effect on GABA as its cofactor

64
Q

oxcarbazepine (trileptal) indications

A

partial seizures, primary or secondary GTCS

65
Q

oxcarbazepine (trileptal) initial dose

A

10mg/kg in 2 divided doses

66
Q

oxcarbazepine (trileptal) maintenance

A

increased to 20-60mg/kg in two divided doses

67
Q

oxcarbazepine (trileptal) adverse effects

A

drowsiness

hyponatremia is a potential problem in older populations or patients taking diuretics and SSRIs

68
Q

perampanel (fycompa) indications

A

partial seizures with and without secondary generalization and primary generalized tonic-clonic seizures

69
Q

perampanel (fycompa) titration dose

A

2-12mg/day over 5-15 weeks

70
Q

perampanel (fycompa) mechanism of action

A

noncompetitive inhibition of glutaminergic AMPA receptors

71
Q

perampanel (fycompa) pharmacokinetics

A

half life 105hrs

72
Q

perampanel (fycompa) incremental dosing

A

increased from 2mg daily by 2mg every 2-3 weeks to desired target

73
Q

perampanel (fycompa) adverse effects

A

sedation, ataxia, and irritability

74
Q

phenobarbital indications

A

partial and generalized tonic-clonic-seizures

especially useful to treat status epilepticus

75
Q

phenobarbital initial and maintenance dosage

A

3-5mg/kg/day

76
Q

phenobarbital pharmacokinetics

A

half life 50-200hrs in term newborns

once daily dosing satisfactory

77
Q

phenobarbital steady state

A

after 2 weeks

78
Q

phenobarbital therapeutic blood concentrations

A

15-40 microg/mL

79
Q

phenobarbital adverse effects

A

dose related:
- hyperactivity
- adverse behavioral changes occur in half of children between ages 2 and 10
- cognitive impairment
stevens-johnson syndrome
drowsiness and cognitive dysfunction after 10 years
allergic rash

80
Q

phenytoin (dilantin) indications

A

tonic-clonic and partial seizures

81
Q

phenytoin (dilantin) pharmacokinetics

A

oral absorption is slow and unpredictable in newborns, erratic in infants, and probably not reliable until 3-5 years of age
70-95% protein-bound
half life up to 60hrs in term newborns; up to 140 in premature infants; 5-14hrs in children; 10-34hrs in adults

82
Q

phenytoin (dilantin) maintenance dose

A

7mg/kg/day in children in 2 or 3 divided doses

83
Q

phenytoin (dilantin) rapid oral loading

A

3x maintenance dose

84
Q

phenytoin (dilantin) adverse effects

A

hypersensitivity, gum hypertrophy, and hirsutism

hypersensitiviy within 6wks : rash, fever, and lymphadenopathy characteristic

85
Q

pregabalin (Lyrica) indications

A

partial seizures with and without secondary generalization and neuropathic pain

86
Q

pregabalin (Lyrica) titration dose

A

from 2-10mg/kg/day over 2 weeks

87
Q

pregabalin (Lyrica) mechanism of action

A

similar to gabapentin, but efficacy significantly higher

88
Q

pregabalin (Lyrica) adverse effects

A

sedation, edema, and increased weight

89
Q

primidone (mysoline) indications

A

tonic-clonic and partial seizures

90
Q

primidone (mysoline) pharmacokinetics

A

metabolizes to at least 2 active metabolites: phenobarbital and phenylethylmalonamide (PEMA)
half life 6-12 hrs; PEMA is 20hrs

91
Q

primidone (mysoline) maintenance dosage

A

10-25mg/kg/day

92
Q

primidone (mysoline) initial dose

A

25% of maintenance dosage or intolerable sedation occurs

93
Q

primidone (mysoline) therapeutic blood concentrations

A

8-12 microg/mL

94
Q

primidone (mysoline) adverse effects

A

same as phenobarbital except risk of intolerable sedation from first tablet is greater

95
Q

rufinamide (banzel) indications

A

seizures within the spectrum of Lennox-Gastaut, which includes all seizure types other than typical absence seizures (present in a small percent of LGS)

96
Q

rufinamide (banzel) initial dose

A

15mg/kg/day

97
Q

rufinamide (banzel) titrating dose

A

up to 45mg/kg/day divided into 2 doses over 2 weeks

98
Q

rufinamide (banzel) drug interactions

A

valproic acid may decrease the metabolism by 15-70%

99
Q

rufinamide (banzel) adverse effects

A

sedation, emesis, and GI symptoms

100
Q

stiripentol (diatomite) indications

A

approved for the treatment of seizures in DS as an adjunctive therapy to clobazam
inhibition of CYP3A4 and 2C19 results in increasing levels of clobazam and norclobazam

101
Q

stiripentol (diatomite) recommended dose

A

50mg/kg/day divided into 2 or 3 doses

102
Q

stiripentol (diatomite) max dose

A

3g divided into 2 or 3 doses

103
Q

stiripentol (diatomite) possible mechanisms of action

A

GABA-A receptors and inhibitor of cytochrome P450, resulting in increased levels of clobazam

104
Q

stiripentol (diatomite) pharmacokinetics

A

half life 4.5-13hrs

increases with dosage between 500 and 2000mg/day

105
Q

stiripentol (diatomite) adverse effects

A

decreased appetite and weight, drowsiness, ataxia, low muscle tone, dystonia, neutropenia, aggressiveness, irritability, insomnia, elevation of gamma-glutamyltransferase

106
Q

tiagabine (gabitril) indications

A

adjunctive therapy for partial-onset and generalized seizures

107
Q

tiagabine (gabitril) initial dose

A

single day dose of 0.2mg/kg/day

108
Q

tiagabine (gabitril) titration

A

increase every 2 weeks by 0.2 mg/kg until achieving optimal benefit or adverse reactions

109
Q

tiagabine (gabitril) adverse effects

A

somnolence and difficulty concentrating

110
Q

topiramate (topamax) indications

A

partial-onset and generalized epilepsies, especially the LGS. migraine prophylaxis and reasonable in children with both disorders

111
Q

topiramate (topamax) initial dose

A

1-2mg/kg/day

112
Q

topiramate (topamax) incremental increas

A

up to 10-15mg/kg/day divided into two doses

113
Q

topiramate (topamax) adverse effects

A

weight loss at therapeutic dosages
cognitive impairment
fatigue and altered mental status at toxic dosages
glaucoma rare indosyncratic reaction
oligohydrosis - advise patient to avoid overheating

114
Q

valproate (depakote) indications

A

mainly for generalized seizures
especially useful for mixed seizure disorders including myoclonic seizures, simple absence, myoclonic absence, myoclonus, and tonic-clonic seizures

115
Q

valproate (depakote) pharmacokinetics

A

oral absorption is rapid
half life 6-15hrs
3x daily dosing in oral suspension; enteric-coated capsule slows absorption so bid dosing
95% protein bound at 50microg/mL; 80% protein bound at 100microg/mL

116
Q

valproate (depakote) initial

A

20mg/kg/day

117
Q

valproate (depakote) increments

A

10mg/kg/day to dose of 60mg/kg/day provide a blood concentration of 50-100microg/mL

118
Q

valproate (depakote) IV

A

dose of 25mg/kg leads to serum level of 100microg/mL

maintenance start 1-3hrs after loading at 20mg/kg/day divided into 2 doses

119
Q

valproate (depakote) adverse effects

A

dose-related and idiosyncratic hepatotoxicity
dose-related reduction in platelet count, pancreatitis, and hyperammonemia (cognitive disturbance and nausea)
thrombocytopenia
carnitine supplement may help relieve cognitive impairment
idiosyncratic fatal liver necrosis d/t production of an aberrant and toxic metabolite - present similar to Reye syndrome

120
Q

vigabatrin (sabril) indications

A

effective treating infantile spasms and partial seizures

121
Q

vigabatrin (sabril) pharmacokinetics

A

long acting, so single day dosing

twice daily dosing preferable to reduce adverse effects

122
Q

vigabatrin (sabril) initial

A

50mg/kg/day

123
Q

vigabatrin (sabril) increases

A

incrementally as needed to 200-250mg/kg/day

124
Q

vigabatrin (sabril) adverse effects

A

peripheral loss of vision
consists of circumferential field constriction with nasal sparing
behavioral problems, fatigue, confusion, and GI upset mild and dose-related

125
Q

zonisamide (zonegran) indications

A

like levetiracetam, zonisamide is a broad spectrum of activity
effective against both primary generalized and partial onset epilepsies
one of the most effective drugs in myoclonic epilepsies

126
Q

zonisamide (zonegran) pharmacokinetics

A

long-acting drug given at bedtime

127
Q

zonisamide (zonegran) initial dose

A

2mg/kg/day

128
Q

zonisamide (zonegran) max dose

A

around 15mg/kg/day

129
Q

zonisamide (zonegran) adverse effects

A

drowsiness and anorexia

oligohydrosis and hyperthermia - monitor for decreased sweating and hyperthermia is required