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NS2 Test 3 > Pharmacology of Seizures and Epilepsy > Flashcards

Pharmacology of Seizures and Epilepsy Flashcards

1
Q

AEDs (anti-epilepsy drugs) stop seizures from occuring in how many patints

A
  • 2/3

- many stop because of SE’s

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2
Q

drugs used to treat epilepsy–target

A
  • glutamate (suppress excitatory)

- GABA (enhance inhibitory)

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3
Q

generalized onset seizures

A
  • absence
  • myotonic, atonic, clonic
  • tonic/clonic
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4
Q

partial onset seizures

A
  • tonic/clonic

- simple complex

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5
Q

absence seizures–drugs used

A
  • Ethosuximide

- Valproic acid

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6
Q

Myotonic clonic seizures–drugs used

Tonic/clonic seizures–drugs used

A

-Benzodiazepines–clonazepam

-Phenytoin
-Phenobarbital
-Carbamazepine (only partial onset
narrow spectrum drugs)

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7
Q

Simple complex seizures–drugs used

A

-Carbamazepine (narrow spectrum)
-Gabapentin
-Pregabalin
-Oxcarbazepine
-Lacosamide
-Tiagabine
-Vigabatrin
-Ezogabin
CGPOLTVE

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8
Q

Broad spectrum–drugs used (used for more than 1 type of seizure)

A

-Valproate
-Lamotrigine
-Topirimate
Levetiracetam
-Zonisamide
(VLTLZ)

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9
Q

AEDs that antagonize excitation by targeting

A
  • NAv (voltage gated Na ion channels)

- low-threshold (T type) Ca channels

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10
Q

AEDs that antagonize Nav

A
  • phenytoin
  • carbamazepine
  • oxcarbazepine
  • lamotrigine
  • zonisamide
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11
Q

inactivation of Nav

A

-channels close from inside of neuron–go into a fast inact state where they cannot be react

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12
Q

repolarization of new

A

-Na channel goes into a slow inactivated state by closing the pore from inside

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13
Q

prolong fast inactivation state of Nav ion channels

A
  • phenytoin, carbamazepine

- oxcarbazepine, lamotrigine (newer)

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14
Q

enhance slow inactivation of Nav channels

A

-lacosamide

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15
Q

Na channels during depolarization

A
  • resting state–activation gate closed
  • open state–activation gate and inactivation gate open
  • fast-inactivation state–inactivation gate closes!
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16
Q

Na channels during repolarization

A
  • fast-inactivated state–inactivation gate closes
  • inactivation closed state–activation gate closes
  • resting state–activation gate closed
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17
Q

AEDs binding site of Na channel?

A
  • at interior side of Nav channel pore
  • if activation gate opens–AEDs can access pore
  • if activation gate closed–AEDs cannot access pore
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18
Q

probability of Nav blockage proportional to?

A

-frequency of Nav channel opening

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19
Q

Nav blockers–act preferentially on?

A

-neurons involved in disease (neurons firing at higher frequency)

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20
Q

phenytoin and carbamazepine differences

A

-carbamazepine–binds Nav less effectively, but faster–more effective in blocking high frequency firing

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21
Q

Lamotrigine vs phenytoin and carbamazepine

A
  • Nav ion channels (similar to phenytoin and carbamazepine)

- also acts on other molecular targets–voltage gated Ca channels

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22
Q

lacosamide–difference from other AEDs how?

A
  • treats partial seizures

- stabilizes the slow-inactivated state (other AEDs act primarily on fast-inactivation state)

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23
Q

hallmark of absence seizures

A

-T-type Ca channels mediate 3 Hz spike and wave activiy in thalamus

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24
Q

Ethosuximide

A

only for absence seizures

  • only limits excitation (Ca channel)
  • Non-sedating drug!!
25
Q

if ethosuximide doesnt work for absence seizures, use?

A
  • valproate

- lamotrigine

26
Q

valproate

A
  • first line therapy
  • adverse side effects (weight gain, tremor, hair loss, lethargy)
  • neural tube defects in babies whose moms take it during pregnancy
27
Q

Lamotrigine

A
  • MOA on Nav ion channels–similar to phenytoin and carbamazepine
  • also acts on Ca channels
28
Q

Zonisamide

A
  • sulfonamide derivative
  • blocks Nav channels
  • blocks T-type Ca channels
29
Q

pre-synaptic modulation of GABA re-uptake or syn-drugs?

A
  • Tiagabine–inhibits GABA reuptake

- Vigabatrin–inhibits GABA metabolism

30
Q

post-synaptic modulation of GABA receptor drugs

A
  • phenobarbital (barbiturates)
  • primidone (older drug)
  • bensodiazepines
31
Q

phenobarbital–complications

A
  • cause sedation
  • lethal respiratory depression
  • abuse and addiction potential
  • needed search for better drugs (benzodiazepines)
32
Q

Benzodiazepines MOA

Barbituates (phenobarbital MOA)

A
  • bind to distinct site–allosteric change
  • potentiate GABA binding–Cl channels opens with greater frequency
  • bind to distinct site
  • increases the duration of Cl channel opening
  • toxicity–high doses are GABA independent
33
Q

differential lethality of GABAa R agonists

A
  • phenobarbital–GABA independent–lethal resp depression

- Benzodiazepine–GABA dependent

34
Q

indicated for treatment of status epilepticus

A

-Benzodiazepines (Diazepam or Lorazepam)

35
Q

Status epilepticus

A
  • seizures occur without epilepsy due to
  • drug withdrawl (AEDs, sedatives–natural disasters)
  • stimulant abuse (cocaine)
  • poisons
  • brain tumor
  • high fever
36
Q

Status Epilepticus treatment

A
  • lorazepam/diazepam

- if seizure doesnt stop, Fosphenytoin IV Na channel antagonist

37
Q

clonazepam,

A
  • benzodiazepine–drug of choice for myoclonic seizures and subcortical myoclonus
  • IV or rectal
38
Q

drugs with multiple MOAs

A
  • Topirimate

- Valproic acid

39
Q

Valproic acid–MOAs

A
  • Nav channels
  • T type Ca channels
  • increases GABA
40
Q

Topirimate–MOAs

A
  • Nav channels
  • Ligand gated Na channels (AMPA/glutamate R)
  • increases GABA
  • potentiates GABA Receptors
41
Q

Topirimate unique MOA

A

-glutamate (AMPA) R antagonist!!

42
Q

Gabapentin–mechanism

A

-voltage dependent Ca channels

43
Q

Leviteracetam–mech, key points

A
  • binds to synaptic vescicle protein SV2a–blunts glutamate release
  • No CYP interaction
44
Q

Pregabalin–mech, key points

A

multiple

100% renal clearance

45
Q

Ezogabine–mech, key points

A
  • opens voltage gated K channels

- causes urinary retention

46
Q

complications with phenytoin

A
  • zero order pharmacokinetics (dose adjustment difficult)
  • induces CYP 450
  • gingival hyperplasia
  • Hirsutism
  • hypocalcemia, osteoporosis
47
Q

Complications with carbamazepine

A
  • induces CYP450
  • aplastic anemia (Rare, fatal)
  • leukopenia, neutropenia, thrombocytopenia–infections,bruising
  • hypocalcemia, osteoporosis
48
Q

induces CYP450 drugs, effects

A
  • carbamazepine
  • phenytoin
  • phenobarbital
  • valproate
  • CYP 450 dependent Vitamin D catabolism–decreased abs of intestinal calcium–demineralize bone (PTH mediated)
49
Q

carbamazepine–induces what?

A
  • its own metabolism (CYP450)

- have it adjust dose–loss of efficacy

50
Q

carbamazepine increases clearance of?

A
  • oral contraceptives (risk for pregnancy)

- warfarin (risk for thrombosis)

51
Q

increases clearance of oral contraceptives

A

carbamazepine

52
Q

increases clearance of warfarin

A

carbamazepine

53
Q

drugs have mixed clearance (Renal, hepatic)

A
  • Topiramate
  • Oxcarbaxepine
  • Levetiracetam
  • Zonisamide
54
Q

Oxcarbazepine

A
  • analogue of carbamazepine
  • fewer adverse effects–lack of formation of an active metabolite
  • minimally affects CYP450
55
Q

Associated with oxcarbazepine and carbamazepine

A

-hyponatremia

56
Q

100% renal clearance drugs

A

-Gabapentin
-Pregabalin
(renal insufficiency requires dose adjustment)

57
Q

life threatening allergic reaction –drugs

A
  • Carbamazepine–Stevens-John syndrome, aplastic anemia

- Lamotrigin

58
Q

When these 2 drugs are used together–inhibits conjugation of drugs by UGT enzymes–causes accumulation of parent drug

A
  • Valproate

- Iamotrigine

59
Q

Class D teratogens

A

-Valproic acid
Carbamazepine
-Phenytoin

NS2 Test 3 (14 decks)

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