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SBM neurology > PHARM - anti-epileptic drugs > Flashcards

PHARM - anti-epileptic drugs Flashcards

(63 cards)

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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
phenytoin used for
- all seizure types except absence | - better for localized and secondary generalized than for primary generalized
26
phenytoin mechanism
blocks voltage gated Na channels
27
phenytoin metabolism
- 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
phenytoin toxicity
- gingival hyperplasia - ataxia - osteomalacia
29
benzo used for
- everything - especially status epilepticus, alcohol seizure and withdrawal - sedative and anxiolytic
30
benzo mechanism
GABA agonist
31
benzo metabolism
- PO or IV - hepatic - non-inducer
32
benzo toxicity
sedation, depression, withdrawal seizures
33
carbamazepine use
- good for focal and secondary - mood stabilizer - NOT a benzo
34
carbamazepine mech
Na blocker
35
carbamazepine metabolism
- oral only - half life 12 hours - hepatic - inducer - levels increased by Ca blockers and microlide antibiotics
36
carbamazepine toxicity
Blurred vision, sedation, neutropenia, hyponatremia, weight gain.
37
ethosuximide use
only for absence
38
ethosuximide mech
blocks T-type Ca channels
39
ethosuximide metabolism
- oral only - good GI absorption - half life 24-48hrs - hepatic - mild inducer
40
ethosuximide toxicity
- GI distress - sedation - behavioral
41
valproate use
- all seizures - migraine - bipolar disorder
42
valproate mech
not well understood, Na? Ca? K? GABA?
43
valproate metabolism
- PO or IV - half life 15 hours - hepatic - non-inducer
44
valproate toxicity
- 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
gabapentin use
- focal and secondarily generalized seizures - anxiolytic - sedative - anti-spasmodic
46
gabapentin mech
- increases GABA levels in brain | - may block Ca channels
47
gabapentin metabolism
- oral only - half life 6 hours - not in urine - not inducer - well absorbed
48
gabapentin toxicity
- sedation, especially in elderly - pedal edema - GI distress
49
lamotrigine use
- all seizures - bipolar - neuropathic pain
50
lamotrigine mech
- blocks glutamate release presynaptically | - blocks Na channels post synaptically
51
lamotrigine metabolism
- oral - non-inducer - hepatic metabolism and renal excretion - half life 24 hours
52
lamotrigine toxicity
allergic rash
53
topiramate use
- broad, not good for absence - migraine - neuropathic pain
54
topiramate mech
- Na blockade - GABA agonist - glutamate antagonist
55
topiramate metabolism
- oral - non-inducer - half life 24 hours - some hepatic metabolism, mostly renal clearance unchanged
56
topiramate toxicity
- sedation - aphasia - parasthesias - kidney stones
57
levetiracetam use
- broad spectrum | - favorite in hospitals
58
levetiracetam mech
- Ca channels | - affects SV2 protein that allows vesicles to release NT
59
levetiracetam metabolism
- 2/3 renal unchanged - not inducer - not protein bound - some hepatic metabolism to inactive metabolites
60
levetiracetam toxicity
cognitive and behavioral problems
61
what is the most effective AED for generalized epilepsy?
valproate
62
2 best drugs for child bearing women?
lamotrigine, levetiracetam
63
most effective drug for localized epilepsy?
- carbamazepine | - lamotrigine and levetiracetam tie for second

SBM neurology (22 decks)

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