Pharm: Epilepsy - Segars Flashcards

1
Q

carbamazepine

A

Na-channel blocker

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2
Q

oxcarbazepine

A

Na-channel blocker

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3
Q

lacosamide

A

Na-channel blocker

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4
Q

lamotigrine

A

Na-channel blocker

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5
Q

felbamate

A

NMDA-r blocker

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6
Q

tiagabine

A

GAT-1 channel blocker (PREsynaptic, GABA promoter)

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7
Q

vigabatrin

A

GABA-T enzyme inhibitor (PREsynaptic, GABA promoter)

NOTE: GABA-T converts GABA -> succinic semi-aldehyde)

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8
Q

phenobarbital

A

POST synaptic GABA promoter

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9
Q

primidone

A

POST synaptic GABA promoter

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10
Q
  • clonazepam
  • lorazepam
  • diazepam
  • clobazam
A

POST synaptic GABA promoter

- potentiate GABA binding by opening Cl-channels with greater frequency

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11
Q

ethosuximide

A

pre-synaptic Ca T-type channel blocker (used for absence seizures!)

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12
Q

zonisamide

A

pre-synaptic Ca T-type channel blocker (and Na-channel blocker)

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13
Q
  • levtiracetam

- bivatacetam

A

synaptic vesicle 2A protein blockers (SV2A)

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14
Q

gabapentin

A

a2 Ca-channel blocker

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15
Q

pregabalin

A

a2-channel blocker

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16
Q

ezogabine

A

K-channel opener (both pre and post-synaptic)

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17
Q

what are the 3 different MOA’s of topiramate?

A
  1. Na-channel blocker
  2. AMPA-r blocker
  3. POSTsynaptic GABA promoting agent
18
Q

what are the 3 different MOA’s of valproic acid?

A
  1. Na-channel blocker
  2. GABA-T inhibitor (presynaptic GABA promoter)
  3. Ca T-type channel blocker
19
Q

what are the 2 syndromes that CBD (Epidiolex) is approved to treat?

A
  • Dravet syndrome
  • Lennox-Gastaut syndrome

two very rare, hard to treat forms of epilepsy
- MOA unknown

20
Q

what are the 2 broad class-wide warnings of all AED’s?

A
  1. abrupt withdrawal of antiepileptic medication may precipitate status epilepticus
  2. suicidal behavior and ideation
21
Q

which AED is a well-known inducer of CYP-450 enzymes and has zero-order pharmacokinetics (taking higher doses makes the drug stay in their system longer)?

A

phenytoin

22
Q

what are the select toxicities of phenytoin (Na-channel blocker)?

A
  • gingival hyperplasia

- hypocalcemia/vit D deficiency/osteoporosis

23
Q

what are the select toxicities of carbamazepine?

A

leukopenia/neutropenia/thrombocytopenia

24
Q

which drug is a less-potent CYP450 inducer than carbamazepine, due to formation of an alternative active metabolite?

A

oxcarbazepine

- less-otent CYP450 inducer

25
Q

what drug causes permanent progressive, bilateral vision loss, and is prescribe able only via a REMS program

A

vigabatrin

NOTE: discontinue after 3 months if no effective response

26
Q

what 3 AED drugs a CPY450 inducers?

A

carbamazepine, phenytoin, phenobarbital

27
Q

what medications do AED (CYP450) inducers increase the clearance of?

A
  • hormonal contraceptives -> elevated risk of pregnancy!!
  • warfarin -> elevated risk for arterial/venous thrombosis
  • HIV medications -> elevated risk of HIV replication
28
Q

valproid acid and lamotrigine inhibit conjugation of drugs by UGT, causing accumulation of what?

A
parent drugs (less metabolite)
- especially when used together
29
Q

phenytoin, carbamazepine and phenobarbital induce conjugation of drugs by what non-CYP450 mechanism, causing a reduction of parent drug (increasing metabolites)?

A

UGT

NOTE: not used as 1st line treatment

30
Q

what is the first line therapy for status epilepticus?

A

first IV:

  • lorazepam
  • diazepam (then addition lorazepam)
31
Q

what is first like therapy for status epilepticus if no IV access?

A

midazolam

32
Q

what is first line therapy in second IV for status epilepticus?

A
  • fosphenytoin
  • phenytoin
  • valproid acid
  • levetiracetam
33
Q

what is the secondary therapy for status epilepticus?

A
  • repeat fosphenytoin if not given previously
  • intubation, BP monitor
  • prepare for continuous midalozam or propofol infusion
34
Q

what are the 2 AMPA-r blockers?

A

topiratamate

perampanel

35
Q

what are the 2 GABA-T enzyme inhibitors?

A

vigabatrin

valproic acid

36
Q

where are GAT-1 channels located?

A

on presynaptic GABA neurons and astrocytes

37
Q

what is primidone converted to in the body?

A

phenobarbital

38
Q

are barbiturates GABA independent or dependent?

A

INdependent, which is why overdose is so much more likely than benzos (which are GABA-dependent)

39
Q

what is the ONLY drug used for absence seizures?

A

ethosuximide KNOW

  • only limits excitation of PRE-synaptic GABA neuron Ca-channels
40
Q

what is the synnergistic combo that both Hon and Segars wanted us to know for AED meds?

A

valproic acid and lamotigrine

- inhibit conjugation of drugs by UGT, causing accumulation of parent drug