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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
if ethosuximide doesnt work for absence seizures, use?
- valproate | - lamotrigine
26
valproate
- first line therapy - adverse side effects (weight gain, tremor, hair loss, lethargy) - neural tube defects in babies whose moms take it during pregnancy
27
Lamotrigine
- MOA on Nav ion channels--similar to phenytoin and carbamazepine - also acts on Ca channels
28
Zonisamide
- sulfonamide derivative - blocks Nav channels - blocks T-type Ca channels
29
pre-synaptic modulation of GABA re-uptake or syn-drugs?
- Tiagabine--inhibits GABA reuptake | - Vigabatrin--inhibits GABA metabolism
30
post-synaptic modulation of GABA receptor drugs
- phenobarbital (barbiturates) - primidone (older drug) - bensodiazepines
31
phenobarbital--complications
- cause sedation - lethal respiratory depression - abuse and addiction potential - needed search for better drugs (benzodiazepines)
32
Benzodiazepines MOA Barbituates (phenobarbital MOA)
- 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
differential lethality of GABAa R agonists
- phenobarbital--GABA independent--lethal resp depression | - Benzodiazepine--GABA dependent
34
indicated for treatment of status epilepticus
-Benzodiazepines (Diazepam or Lorazepam)
35
Status epilepticus
- seizures occur without epilepsy due to - drug withdrawl (AEDs, sedatives--natural disasters) - stimulant abuse (cocaine) - poisons - brain tumor - high fever
36
Status Epilepticus treatment
- lorazepam/diazepam | - if seizure doesnt stop, Fosphenytoin IV Na channel antagonist
37
clonazepam,
- benzodiazepine--drug of choice for myoclonic seizures and subcortical myoclonus - IV or rectal
38
drugs with multiple MOAs
- Topirimate | - Valproic acid
39
Valproic acid--MOAs
- Nav channels - T type Ca channels - increases GABA
40
Topirimate--MOAs
- Nav channels - Ligand gated Na channels (AMPA/glutamate R) - increases GABA - potentiates GABA Receptors
41
Topirimate unique MOA
-glutamate (AMPA) R antagonist!!
42
Gabapentin--mechanism
-voltage dependent Ca channels
43
Leviteracetam--mech, key points
- binds to synaptic vescicle protein SV2a--blunts glutamate release - No CYP interaction
44
Pregabalin--mech, key points
multiple | 100% renal clearance
45
Ezogabine--mech, key points
- opens voltage gated K channels | - causes urinary retention
46
complications with phenytoin
- zero order pharmacokinetics (dose adjustment difficult) - induces CYP 450 - gingival hyperplasia - Hirsutism - hypocalcemia, osteoporosis
47
Complications with carbamazepine
- induces CYP450 - aplastic anemia (Rare, fatal) - leukopenia, neutropenia, thrombocytopenia--infections,bruising - hypocalcemia, osteoporosis
48
induces CYP450 drugs, effects
- carbamazepine - phenytoin - phenobarbital - valproate - CYP 450 dependent Vitamin D catabolism--decreased abs of intestinal calcium--demineralize bone (PTH mediated)
49
carbamazepine--induces what?
- its own metabolism (CYP450) | - have it adjust dose--loss of efficacy
50
carbamazepine increases clearance of?
- oral contraceptives (risk for pregnancy) | - warfarin (risk for thrombosis)
51
increases clearance of oral contraceptives
carbamazepine
52
increases clearance of warfarin
carbamazepine
53
drugs have mixed clearance (Renal, hepatic)
- Topiramate - Oxcarbaxepine - Levetiracetam - Zonisamide
54
Oxcarbazepine
- analogue of carbamazepine - fewer adverse effects--lack of formation of an active metabolite - minimally affects CYP450
55
Associated with oxcarbazepine and carbamazepine
-hyponatremia
56
100% renal clearance drugs
-Gabapentin -Pregabalin (renal insufficiency requires dose adjustment)
57
life threatening allergic reaction --drugs
- Carbamazepine--Stevens-John syndrome, aplastic anemia | - Lamotrigin
58
When these 2 drugs are used together--inhibits conjugation of drugs by UGT enzymes--causes accumulation of parent drug
- Valproate | - Iamotrigine
59
Class D teratogens
-Valproic acid Carbamazepine -Phenytoin

NS2 Test 3 (14 decks)

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