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Phar 752 > Antiepileptics > Flashcards

Antiepileptics Flashcards

1
Q

Phenobarbital target

A

GABA-a modulator

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2
Q

Primidone target

A

GABA-a modulator as Phenobarbital

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3
Q

Phenytoin target

A

Na+ Channel blocker

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4
Q

Fosphenytoin target

A

Na+ Channel blocker as Phenytoin

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5
Q

Ethosuximide target

A

Ca2+ Channel blocker

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6
Q

Valproate target

A

GABA-AT and SSA-DH Inhibitor

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7
Q

Divalproex sodium target

A

GABA-AT and SSA-DH Inhibitor: as Valproate

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8
Q

Carbamazepine target

A

Na+ Channel blocker

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9
Q

Oxcarbazepine target

A

Unknown, but known to be due to the “mono-hydroxy metabolite” : Licarbazepine

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10
Q

Eslicarbazepine acetate target

A

Unknown, but known to be due to Eslicarbazepine metabolite : S - Licarbazepine

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11
Q

Gabapentin target

A

alpha2delta-Ca2+ Channel blocker

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12
Q

Gabapentin enacarbil target

A

alpha2delta-Ca2+ Channel blocker

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13
Q

Pregabalin target

A

alpha2delta-Ca2+ Channel blocker

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14
Q

Vigabatrin target

A

Irreversible GABA-AT inhibitor (synthesis)

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15
Q

Felbamate target

A

Unknown

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16
Q

Lamotrigine target

A

Unknown

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17
Q

Topiramate target

A

Unknown

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18
Q

Zonisamide target

A

Unknown

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19
Q

Tiagabine target

A

GAT-1 Transporter blocker

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20
Q

Lacosamide target

A

Unknown

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21
Q

Levetiracetam target

A

SV2A modulator (vesicle protein)

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22
Q

Brivaracetam target

A

SV2A modulator (vesicle protein) > Levetiracetam

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23
Q

Rufinamide target

A

Na+ Channel modulator

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24
Q

Ezogabine target

A

K+ Channel activator

25
Q

Perampanel target

A

AMPA antagonist (glutamate)

26
Q

Cannabadiol target

A

Unknown

27
Q

AED: Strong Inducers

A

Of various P450’s and UGT’s:
Phenobarbital / Primidone
Phenytoin / Fosphenytoin
Carbamazepine

28
Q

AED: Moderate Inducers

A 
3A4:
Oxcarbazepine
Eslicarbazepine acetate (due to metabolite)
2C9:
Vigabatrin
29
Q

AED: Weak Inducers

A

3A4:
Topiramate
Rufinamide

30
Q

AED: 2C19 Inhibitors

A 
Oxcarbazepine
Eslicarbazepine acetate (due to metabolite)
31
Q

AED: 2C9 Inhibitor

A

Valproate

32
Q

AED: 2E1 Inhibitor

A

Rufinamide (weak)

33
Q

AED: Epoxide Hydrolase Inhibitor

A

Valproate

34
Q

AED: UGT Inhibition

A

Valproate (specific types - not in general)

35
Q

AED’s most associated with skin disorders:

A 
Most strongly with...
- Phenobarbital
- Phenytoin
- Carbamazepine
Less so with...
- Oxcarbazepine
- Lamotrigine
36
Q

Phenobarbital metabolism

A

Para-hydroxylation by 2C9 / 2C19

37
Q

Primidone metabolism

A

Oxidation to Phenobarbital
or
Multiple steps to Phenylethylmalonamide (PEMA)

38
Q

Phenytoin metabolism

A

Para-hydroxylation by 2C9 > 2C19
Arene Oxide Intermediate

May proceed to inactive metabolite.

May proceed to Glutathione / Mercapturic acid metabolites which cause toxicities.

39
Q

Fosphenytoin metabolism

A

Dephosphorylation by various phosphatases

40
Q

Ethosuximide metabolism

A

Ethyl-hydroxylation by 3A4 / 2E1

41
Q

Valproic acid metabolism

A 
Direct Glucuronidation - Inactive
or
beta-oxidation to form 2-ene product - Active
or
* Reactive minor metabolite - Toxicity
42
Q

Carbamazepine metabolism

A

3A4 oxidation - Epoxide intermediate

  • Alkylation of proteins
  • Epoxide Hydrolase to catechol (inactive)

Multi-Step metabolism to Iminoquinone form
- Alkylation of proteins

43
Q

Oxcarbazepine metabolism

A

Reduction to mono-hydroxy metabolite (active)

- “Licarbazepine”

44
Q

Eslicarbazepine acetate metabolism

A

Ester Hydrolysis - Eslicarbazepine

- S form of Licarbazepine

45
Q

Gabapentin metabolism

A

Not appreciably metabolized

46
Q

Gabapentin enacarbil metabolism

A

Amide-like bond broken to release Gabapentin - Not appreciably metabolized

47
Q

Pregabalin metabolism

A

Less than 2% metabolized

48
Q

Vigabatrin metabolism

A

Not significantly metabolized

49
Q

Felbamate metabolism

A

Practice pathway: Results in electrophilic “atropaldehyde” metabolite that is toxic.

50
Q

Lamotrigine metabolism

A

Major route - Glucuronidation

Minor route - P450’s create Arene Oxide

  • Some Glucuronidated, some not.
  • Serious skin rashes
51
Q

Topiramate metabolism

A

70% unchanged.

30% many pathways.

52
Q

Zonisamide metabolism

A

3A4 reduction in five membered ring
or
N-Acetylation of the sulfonamide group

53
Q

Tiagabine metabolism

A

3A4 to 5-oxo-metabolite

54
Q

Lacosamide metabolism

A

40% unchanged.
O-demethylation by 2C19 (mainly)
- Minor effects from inducers

55
Q

Levetiracetam metabolism

A

No P450
66% excreted unchanged
Most hydrolyzed to inactive acid product

56
Q

Brivaracetam metabolism

A 
40% unchanged
2C19 - Hydroxylation on propyl side chain (inactive)
Amide hydrolysis (inactive)
57
Q

Rufinamide metabolism

A

Extensively metabolized.
Major route - Amide hydrolysis (inactive)
Can then be Glucuronidated

58
Q

Ezogabine metabolism

A

No P450
Glucuronidation
N-acetylation

59
Q

Perampanel metabolism

A

3A4 hydroxylation

Phar 752 (12 decks)

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