Antiepileptic pharmacotherapy Flashcards

1
Q

MOA of Na+ blocking antiepileptics

A

Binds to inactive form of Na+ channels, resulting in preferential inhibition of epileptic focus

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2
Q

MOA of Ca++ blocking antiepileptics

A

Thanlmic T-type Ca++ channels inhibit absence seizures

Presynaptic HVA Ca++ channels- suppresses Glu signalling

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3
Q

Ways of enhancing GABA signalling

A

Activate GABA-A receptors
inhibit GABA re-uptake GAT-1
Inhibit GABA degredation GABA-T

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4
Q

Ways of antagonizing glutamanergic transmission

A

antagonize receptors

block glu release SV2A

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5
Q

MOA of Ca++ blocking antiepileptics

A

Thanlmic T-type Ca++ channels inhibit absence seizures

Presynaptic HVA Ca++ channels- suppresses EAA release

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6
Q

Ways of antagonizing glutamanergic transmission

A

antagonize receptors

block glu release SV2A

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7
Q

Phenytoin MOA

A

blocks Na+ channels

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8
Q

Pharmacokinetics of phenytoin

A

oral, IV (fosphenytoin)
non-linear elimination- need to monitor in blood
plasma protein binding
hepatic CYP metabolism

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9
Q

Therapeutic use of phenytoin

A

focal and tonic-clonic seizures, SE

not effective against absence seizures

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10
Q

Drug interactions with phenytoin

A

OCPs, warfarin

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11
Q

Adverse effects of phenytoin

A
CNS- nystagmus, ataxia, and sedation
Rash and SJS
hirsutism
blood dyscrasias
teratogenic
gingival hyperplasia
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12
Q

MOA of carbamazepine

A

Na+ channel blockade

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13
Q

carbamazepine pharmacokinetics

A

linear kinetics

autoinduction of CYP3A4

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14
Q

Therapeutic use of carbamazepine

A

generalized tonic-clonic seizures, simple and complex partial seizures
trigeminal neuralgia
bipolar disorder

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15
Q

Adverse effects of carbamazepine

A

CNS- drowsiness, ataxia, vertigo, diplopia, blurred vision; nausea
hyponatremia
Boxed warning- rash and SJS, asian variant more susceptible
teratogenic

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16
Q

Valproic acid MOA

A

blocks Na+ channels
Blocks T-type Ca++ channels
Stimulates GABA synthesis and inhibits degredation

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17
Q

Therapeutic use of valproic acid

A

broad spectrum anti-seizure
absence, focal and tonic-clonic seizures
bipolar disorder and migraine prophylaxis

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18
Q

What is divalproex

A

1:1 acid/salt

19
Q

Adverse effects of valproic acid

A

GI
CNS
hepatic toxicity and pancreatitis (boxed warning)
Teratogenic (boxed warning)

20
Q

Drug interaction of valproic acid

A

phenytoin

21
Q

MOA of ethosuximide

A

Blocks t-type Ca++ channels in thalmic nucleus

Thalmic 3-Hz spike and wave rythms are characteristic of absence seizures

22
Q

Therapeutic use of ethosuximide

A

drug of choice for uncomplicated absence seizures

not effective for other types

23
Q

Adverse effects of ethosuximide

A

well-tolerated
GI
Rare SLE, leucopenia, aplastic anemia and SJS

24
Q

MOA of Gabapentin

A

blocks HVA Ca++ channels, may reduce glu release

25
Q

Pharmacokinetics of gabapentin

A

not metabolized; excreted unchanged in urine

26
Q

Therapeutic use of gabapentin

A

add-on for focal and generalized seizures
posttherpetic neuralgia
off-label pain, migrane, bipolar

27
Q

Adverse effects of gabapentin

A

some sedation and dizziness but mostly well tolerated

28
Q

Lamotrigine MOA

A

complex, major is blockade of Na+ channels

29
Q

Pharmacokinetics of lamotrigine

A

metabolized by glucuronidation, hepatic clearance is increased by enzyme inducers

30
Q

therapeutic use of lamotrigine

A

Lennox-Gastaut syndrome
monotherapy for partial and secondarily generalized tonic-clonic, alternative to ethosuximide for absence
biopolar

31
Q

Adverse effects of lamotrigine

A

dizziness, ataxia, blurred vision, nausea, vomiting
Rash/SJS boxed warning
teratogen

32
Q

Levetiracetam MOA

A

unknown, binds to SV2A

33
Q

Pharmacokinetics of levetiracetam

A

mostly devoid of drug interactions

34
Q

Therapeutic use of levetiracetam

A

add on for partial or generalized tonic-clonic and myoclonic seizures

35
Q

Adverse effects of levetiracetam

A

fatigue, dizziness, hypertension

behavioral symptoms

36
Q

MOA of tiagabine

A

prolongs inhibitory effect of gaba by blocking GAT-1

37
Q

Therapeutic use of tigabine

A

add on for refractory partial seizures without generalization
off-label discouraged-may promote seizures

38
Q

Topiramate MOA

A

blocks Na+ channels, hyperpolarization, Carbonic anydrase inhibitor

39
Q

Pharmacokinetics of topiramate

A

excreted unchanged in urine

40
Q

Therapeutic use of topiramate

A

monotherapy for partial and generalized tonic-clonic seizures, adjunct for lennox-gastaut syndrome
migrane prophylaxis

41
Q

Adverse effects of topiramate

A

well-tolerated
renal calculi from CA inhibition
cognitive impairment

42
Q

MOA of vigabatrin

A

irriversible inhibitor of GABA transaminase

43
Q

Therapeutic use of vigabatrin

A

restricted use for refractory complex partial seizures

monotherapy for infantile spasms

44
Q

Adverse effects of vigabatrin

A

boxed warning for progressive and permanent bilateral vision loss