11. Anti-Epileptic Drugs PHARM Flashcards

1
Q

what is the single most effective drug for generalized epilepsy?

A

valproate

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2
Q

what drug is best for childhood petit mal/absence?

A

ethosuximide

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3
Q

what are best for child-bearing women?

A

lamotrigine, levetiracetam

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4
Q

metaphorically, levetiracetam is considered to be what?

A

the swiss army knife of anti-epilepsy drugs: works for everything, does nothing really well, favorite in hosp settings

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5
Q

what is the single most effective drug for focal epilepsy?

A

carbamazepine

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6
Q

what is equally effective to carbamazepine for focal sz, but has a worse side effect profile?

A

phenytoin

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7
Q

why do barbutuates have a high drop out rate?

A

sedation

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8
Q

what drug is best in the elderly? why?

A

lamotrigene. less sedating than others, few drug interactions.

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9
Q

opening of Ca2+ and Na+ channels tend to produce what in the neuron?

A

depolarization (both flow in, make interior less negative)

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10
Q

opening of K+ and Cl- channels tend to produce what in the neuron?

A

hyperpolarization (K flows out, makes interior more neg. Cl flows in, makes interior more neg)

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11
Q

what does GABA do?

A

inhibitory. opens a Cl- channel, hyperpolarizes the cell. makes firing less likely

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12
Q

what does glutamate do?

A

excitatory. binds to receptors, opens Na+ and Ca2+ channels. depolarize cell, make firing more likely

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13
Q

what drugs are agonists of GABA receptors?

A

benzodiazepines, barbituates, topiramate

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14
Q

what drugs are antagonists of glutamate?

A

lamotrigine, topiramate

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15
Q

drugs that block Na+ channels are inhibitory or exitatory?

A

inhibitory.

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16
Q

what drugs block Na+ channels?

A

phenytoin, carbamazepine, valproate, topiramate, lamotrigine

17
Q

what is the mechanism of action of ethosuximide?

A

blocks T-type Ca2+ channels in thalamus. effective because absence seizure is an uninterrupted cortico-thalamic circuit.

18
Q

how many half-lives does it take to reach steady state?

A

5

19
Q

what will be the effect of an INDUCER of CYP-450?

A

it will incr clearance and decrease concentration of other drugs

20
Q

what will be the effect of an INHIBITOR of CYP-450?

A

it will decr clearance and increase concentration of other drugs

21
Q

considerations of pharmacodynamics in preg?

A

incr volume due to hemodilution, higher doses usually needed, faster metabolism

22
Q

what other drugs may be less effective when taken with AEDs?

A

OCPs, coumadin, anti-depressants, cholesterol-lowering drugs, chemo (due to enzyme induction)

23
Q

Side effects of AEDs (systemic)?

A
rash (1-5%)
GI problems (1-10%)
24
Q

side effects of AEDs (CNS)?

A

depressants, sedatives, fatigue, headaches, blurred vision, double vision

25
Q

PCOS: worst AED for this? what should she switch to?

A

valproate is worst. switch to lamotrigine.

26
Q

AEDs: cause osteoporosis?

A

yes: phenobarbital, phenytoin, carbamazepine. supplement with Ca and Vit D

27
Q

phenobarbitol: seizure types? Mech?

A

all except absence. IV for useful for status epilepticus. GABA agonist: opens Cl channel

28
Q

Phenytoin: seizure types? mech?

A

all except absence, better for focal/secondarily generalized. Blocks VG Na+ channels.
need to supplement Ca.

29
Q

Benzodiazepines: seizure types? mech?

A

acute seizure control, not good long term due to tolerance. first line for status epilepticus or alc withdrawal.
agonist at GABA

30
Q

Carbamazepine: seiz types? mech?

A

first line for focal epil. also mood stabilizer and good for neuropathic pain. Na channel blocker. sig weight gain.

31
Q

ethosuximide: seiz types? mech?

A

only for absence seizures. blocks T type Ca channels in thalamus

32
Q

Valproate: seiz types? mech?

A

first line for generalized epil. Na channels. also: migraine, bipolar. very bad for preg women.

33
Q

gabapentin: seiz types? mech?

A

partial and secondarily generalized. incr GABA in the brain. also anxiolytic, sedative, good for neuropathy

34
Q

lamotrigine: seiz types? mech?

A

broad spectrum, all sz types. good for preg women. rash can lead to liver necrosis.
also bipolar, neuropathic pain

35
Q

topiramate: seiz types? mech?

A

all but absence. causes weight loss. sedation. mult mechanisms.

36
Q

levitiracetam: seiz types? mech?

A

focal and generalized. mech controversial.