Seizure pharm Flashcards

1
Q

General strategies of seizure meds

A
  1. decrease excessive rates of neuronal dishcarge w/in a focus
  2. prevent propagation of siezure activity from focus to other brain regions
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2
Q

Basic mechanism of action for antiseizure drugs

A

Affect abnormal membrane fnx; changes in voltage-regulated ion channels leading to excess depolarization,

correct decreased inhibition (increase GABA fnx),

reduce excitation (block glutamate)

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3
Q

alters ion conductance, use dependent on Na chans, ≠generation of repetive AP by keeping inactivation gate closed = increased refractory period

A

Phenytoin

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4
Q

MOA of Phenytoin and PharmK

A

alters ion conductance, use dependent on Na chans, ≠generation of repetive AP by keeping inactivation gate closed = increased refractory period

*depend on formulation, HIGH protein bound, use 10-20 mg

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5
Q

what would you prescribe to someone with General Tonic-Clonic or Partial seizures that affecgts Na channels to keep them inactive

A

Phenytoin: for tonic-clonic or partial seizures

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6
Q

Why do we measure blood levels of pt on Phenytoin

A

bc it’s dose dependent drug: there is NON-linear releationhip btwn daily dose of drug and steady-state plasma conc btwn individuals; daily dose varies person to person

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7
Q

What side effects, specifically CNS are seen with PHenytoin use?

A

CNS is dose/depend= nausea, anorexia, apathy, sedation, nystagmus.

NOn-dose dependent= gingiva hyperplasia, hirsuitism, teratogenic, rash

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8
Q

MOA of Carbamazepine

A

Sim MAO phenytoin; blocks Na chans at therapeutic conc, no GABA interaction. Unpredictable absorption w/ hepatic enZ induction

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9
Q

best med for PARTIAL seizures, NOT absence (contraindicated)

A

Carbamazepine

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10
Q

Causes dose releated toxicity; diplopia, ataxia, GI, drowsiness, rare blood dyscarsias (no dose related)

A

Carbamazapine

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11
Q

What drug is teratogenic that can cause spina bifida?

A

Cabamazepine

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12
Q

Impaired consciousness w/ staring spells, w/ or w/out eye blinks

A

Absence seizure

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13
Q

seizure recurring so close together baseline consciousness is not regained btwn episodes

A

status epilepticus

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14
Q

First line for absence seizures

A

Ethosuximide

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15
Q

reduces low-threshold (T-type) Ca++ current in thalamic nucleus

A

Ethosuximide for absence seizures

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16
Q

PharmK in Ethosuximide

A

well absorbed after oral, not protein bound, dist to entire body, met by liver w/ long ½ life

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17
Q

Side effects and toxicity seen with Ehtosuximide use

A

Sides/toxicity: gastric distress and lethargy and fatigue

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18
Q

MOA of Valproic Acid

A

Blocks repetitive firing, reduce T type Ca++ currents, increase GABA conc

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19
Q

PharmK: plasma bound, distributes extracell, ≠metobolism phenobarbital/phenytoin, carbamazepine

A

Valproic Acid

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20
Q

When can we use Valproic acid as seizure tx

A

absence seizure w/ or w/out tonic-clonic, general tonic-clonic, partial, myoclonic

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21
Q

Side effects of valproic acid

A

GI, wt gain, hair loss, Hepatotoxic, teratogenic (spina bifida)

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22
Q

MOA of Felbamate

A

At clycine modulatory site on NMDA receptor; potentiates GABA,

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23
Q

for PARTIAL seizure not responseive to other tx, (-) is anaplastic and hepatic failure , very toxic, only use in refractory seizures

A

Felbamate

24
Q

Toxicity of Felbamate, when to use it

A

Parital seizures refractory to other tx.

Anaplastic and hepatic fail

25
Q

Use as adjunct therapy for Partial seizures w/or w/out tonic-clonic seizures

also Used for neurpopathic pain and ALS

A

Gabapentin

26
Q

MOA of Gabapentin

A

Analogue of GABA, unclear what it does, not an agonist

27
Q

Sim to gabapentin, more potent. Interact w/ a2-delta subunit of volt-gated Ca+ channels à reduces NT release.

A

Pregabalin (Lyrica)

28
Q

used as adjuvant for PaRTIAL, neuropathic pain in diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia

A

Pregabalin

29
Q

What limits usefullness of Pregabalin

A

DEA class 5 drug

30
Q

MOA of Lamotrigine

A

Blocks repetitive AP, may block Na+ chan

31
Q

When can you prescribe Lamotrigine to pt?

A

Used: Partial, General T/C, Absence, bipolar disorder. No interference w/ other drug pharmK

32
Q

Use for Used: Partial, General T/C, Absence, bipolar disorder. No interference w/ other drug pharmK

A

Lamotrigine

33
Q

Serious side effect = rash or steven johnson syndrome

A

Lamotrigine

34
Q

From D-fructose, ≠excitatory transmission via antagonizing ability of excitatory AA to activate AMPA on glutamate receptor, can block Na channels (like phenytoin)

A

Topirimate

35
Q

What effect does Topirimate have on seizures

A

Blocks spread of seizure vs raising seizure threshold

36
Q

Use: as add-on in adult for Partial seizures and prevention migraines

A

Topirimate

37
Q

MOA of Tiagabine

A

≠GABA transporter, GAT-1 thus ≠reuptake of GABA to increase concentration in brain.

38
Q

≠GABA transporter, GAT-1 thus ≠reuptake of GABA to increase concentration in brain.

A

Tiagabine

39
Q

Uses of Tiagabine and side effects

A

add-on for Complex and Simple Partial seizures

dizzy, tremor, somnolence

40
Q

Adj for Parital or adj for myoclonic seizures and Primary Generalized seizures

Mech = ???; few interactions, often given w/ other seizure meds.

Sides = somnolence, asthenia, dizzy

A

Levetiracetam

41
Q

Acts at Na+ and Ca+ channels, reduced voltage-gated (T-type) and stops spread of seizures while suppressing their focus

A

Zonisamide

42
Q

MOA of Zonisamide

A

Acts at Na+ and Ca+ channels, reduced voltage-gated (T-type) and stops spread of seizures while suppressing their focus

43
Q

Side effects of Zonisamide

A

CNS (-) reaction; ataxia, anorexia, nervous, fatigue, speech.

44
Q

What do we use Zonisamide for?

A

approve as adjunctive tx of adults w/ partial seizures

45
Q

MOA of Vigabatrin

A

Irreversibly ≠ GABA metabolism; GABA-transanimase inhibitor; has possible permanent effects on vision.

46
Q

used as adjuvant for refractory complex partial and infantile spasms

A

Vigabatrin

47
Q

Blocks voltage gated Na and Ca++ channels to ≠neuronal hypersynchronization and ≠caronic anhydrase

A

Clobazam

48
Q

Mech of Clobazam

A

Blocks voltage gated Na and Ca++ channels to ≠neuronal hypersynchronization and ≠caronic anhydrase

49
Q

Lacosamide MOA

A

Enchance slow inactivation volt Na channels, additive to AEDs via prolongation of inactivation

50
Q

Enchance slow inactivation volt Na channels, additive to AEDs via prolongation of inactivation

A

Lacosamide

51
Q

USe of Lacosamide

A

Adj for Partial seizures

52
Q

Postsynaptic AMPA antagonist; binds to allosteric site on glutamate-gated Na+/K+ AMPA channel thus is noncompetitive; prevents discharge of neurons

A

Perampanel

53
Q

Drug interactions seen iwth Perampanel

A

Interactions: CYP3A inducer antiseizure drug (caramasepine, oxcarbazepine, phenytoin)

54
Q

Adj for Partial seizures in adults

MOA: K+ channel facilitator, unique to this drug; only when other drugs not tolerated; may have eye issues

A

Ezogabine

55
Q

Decreases sustained high-frequency fring of neurons; prolong inactive state of Na+ channel

For adj in Lennox-Gastaut in pts over 4 years, works for all seizures in this sydnrome

A

Rufinamide