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SBM neurology > PHARM - anti-epileptic drugs > Flashcards

PHARM - anti-epileptic drugs Flashcards

1
Q

4 types of AEDs

A
  • Na blockers
  • Ca blockers
  • GABA agonists
  • glutamate antagonists
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2
Q

Na blockers

A
  • phenytoin
  • carbamazapine
  • valproate
  • topiramate
  • lamotrigine
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3
Q

Ca blockers

A

ethosuximide

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4
Q

GABA agonists

A
  • topiramate
  • barbs
  • benzos
  • gabapentin?
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5
Q

glutamate antagonists

A
  • topiramate

- lamotrigine

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6
Q

absorption is essentially complete for all AEDs except…

A

gabapentin, which has a saturable transporter at high doses

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7
Q

speed of AED absorption

A
  • takes hours

- slowed by food

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8
Q

TIs in AEDs

A

generally good but hard to compare

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9
Q

typical cytochrome P-450 enzymes

A

2C9, 2C19, 3A4

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10
Q

some UGTs and what they metabolize

A

1A9 - valproate
2B7 - valproate, lorazepam
1A4 - lamotrigine

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11
Q

what do cytochrome P-450 inducers do?

A
  • increase clearance and decrease steady state concentrations of other drugs
  • phenobarbitol, ethosuximide, phenytoin, carbamazepine, tobacco
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12
Q

what do cytochrome P-450 inhibitors do?

A
  • decrease clearance and increase steady state concentrations of other drugs
  • erythromycin, valproate, fluconasol, trimethoprim, Ca blockers
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13
Q

what pharmacokinetic factors change in the elderly?

A

distribution - more fat, less albumin
metabolism slowed - less hepatic enzyme, less blood flow
excretion - less renal clearance

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14
Q

pharmacokinetic factors in pediatrics

A

neonates - need lower doses, low protein binding and metabolic rate
children - need higher per kg doses, faster metabolism

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15
Q

pharmacokinetic factors in pregnancy

A
  • increased volume of distribution
  • low serum albumin, but may not affect free drug level
  • faster hepatic metabolism
  • may need higher AED doses, but not as high as predicted
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16
Q

drug of choice for pregnancy

A

lamotrigine, few side effects

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17
Q

AEDs that cause weight gain

A

gabapentin, valproate, carbamazepine

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18
Q

AEDs that cause weight loss

A

topiramate

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19
Q

AEDs associated with PCOS

A
  • carbamazepine

- valproate

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20
Q

AEDs associated with osteoporosis

A
  • phenobarbitol
  • carbamazepine
  • phenytoin
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21
Q

phenobarbitol effective for:

A

all seizure types but absence

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22
Q

phenobarbitol mechanism

A

GABA agonist, opens Cl channels for hyper polarization

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23
Q

phenobarbitol metabolism

A
  • PO or IV
  • inducer
  • hepatic metabolism
  • needs to be loaded
  • half life 100hrs
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24
Q

phenobarbitol toxicity

A
  • hyperactivity in children
  • sedation in adults
  • joint problems
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25
Q

phenytoin used for

A
  • all seizure types except absence

- better for localized and secondary generalized than for primary generalized

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26
Q

phenytoin mechanism

A

blocks voltage gated Na channels

27
Q

phenytoin metabolism

A
  • IV or PO, PO bad in children
  • inducer
  • zero order kinetics at high doses due to enzyme saturation
  • half life 6-24hrs
  • hepatic metabolism
28
Q

phenytoin toxicity

A
  • gingival hyperplasia
  • ataxia
  • osteomalacia
29
Q

benzo used for

A
  • everything
  • especially status epilepticus, alcohol seizure and withdrawal
  • sedative and anxiolytic
30
Q

benzo mechanism

A

GABA agonist

31
Q

benzo metabolism

A
  • PO or IV
  • hepatic
  • non-inducer
32
Q

benzo toxicity

A

sedation, depression, withdrawal seizures

33
Q

carbamazepine use

A
  • good for focal and secondary
  • mood stabilizer
  • NOT a benzo
34
Q

carbamazepine mech

A

Na blocker

35
Q

carbamazepine metabolism

A
  • oral only
  • half life 12 hours
  • hepatic
  • inducer
  • levels increased by Ca blockers and microlide antibiotics
36
Q

carbamazepine toxicity

A

Blurred vision, sedation, neutropenia, hyponatremia, weight gain.

37
Q

ethosuximide use

A

only for absence

38
Q

ethosuximide mech

A

blocks T-type Ca channels

39
Q

ethosuximide metabolism

A
  • oral only
  • good GI absorption
  • half life 24-48hrs
  • hepatic
  • mild inducer
40
Q

ethosuximide toxicity

A
  • GI distress
  • sedation
  • behavioral
41
Q

valproate use

A
  • all seizures
  • migraine
  • bipolar disorder
42
Q

valproate mech

A

not well understood, Na? Ca? K? GABA?

43
Q

valproate metabolism

A
  • PO or IV
  • half life 15 hours
  • hepatic
  • non-inducer
44
Q

valproate toxicity

A
  • GI upset,
  • weight gain
  • menstrual problems
  • hair loss
  • low platelet count
  • hepatic encephalopathy sometimes but not always associated with elevated ammonia levels and carnitine deficiency
45
Q

gabapentin use

A
  • focal and secondarily generalized seizures
  • anxiolytic
  • sedative
  • anti-spasmodic
46
Q

gabapentin mech

A
  • increases GABA levels in brain

- may block Ca channels

47
Q

gabapentin metabolism

A
  • oral only
  • half life 6 hours
  • not in urine
  • not inducer
  • well absorbed
48
Q

gabapentin toxicity

A
  • sedation, especially in elderly
  • pedal edema
  • GI distress
49
Q

lamotrigine use

A
  • all seizures
  • bipolar
  • neuropathic pain
50
Q

lamotrigine mech

A
  • blocks glutamate release presynaptically

- blocks Na channels post synaptically

51
Q

lamotrigine metabolism

A
  • oral
  • non-inducer
  • hepatic metabolism and renal excretion
  • half life 24 hours
52
Q

lamotrigine toxicity

A

allergic rash

53
Q

topiramate use

A
  • broad, not good for absence
  • migraine
  • neuropathic pain
54
Q

topiramate mech

A
  • Na blockade
  • GABA agonist
  • glutamate antagonist
55
Q

topiramate metabolism

A
  • oral
  • non-inducer
  • half life 24 hours
  • some hepatic metabolism, mostly renal clearance unchanged
56
Q

topiramate toxicity

A
  • sedation
  • aphasia
  • parasthesias
  • kidney stones
57
Q

levetiracetam use

A
  • broad spectrum

- favorite in hospitals

58
Q

levetiracetam mech

A
  • Ca channels

- affects SV2 protein that allows vesicles to release NT

59
Q

levetiracetam metabolism

A
  • 2/3 renal unchanged
  • not inducer
  • not protein bound
  • some hepatic metabolism to inactive metabolites
60
Q

levetiracetam toxicity

A

cognitive and behavioral problems

61
Q

what is the most effective AED for generalized epilepsy?

A

valproate

62
Q

2 best drugs for child bearing women?

A

lamotrigine, levetiracetam

63
Q

most effective drug for localized epilepsy?

A
  • carbamazepine

- lamotrigine and levetiracetam tie for second

SBM neurology (22 decks)

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