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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
Perampanel target
AMPA antagonist (glutamate)
26
Cannabadiol target
Unknown
27
AED: Strong Inducers
Of various P450's and UGT's: Phenobarbital / Primidone Phenytoin / Fosphenytoin Carbamazepine
28
AED: Moderate Inducers
``` 3A4: Oxcarbazepine Eslicarbazepine acetate (due to metabolite) 2C9: Vigabatrin ```
29
AED: Weak Inducers
3A4: Topiramate Rufinamide
30
AED: 2C19 Inhibitors
``` Oxcarbazepine Eslicarbazepine acetate (due to metabolite) ```
31
AED: 2C9 Inhibitor
Valproate
32
AED: 2E1 Inhibitor
Rufinamide (weak)
33
AED: Epoxide Hydrolase Inhibitor
Valproate
34
AED: UGT Inhibition
Valproate (specific types - not in general)
35
AED's most associated with skin disorders:
``` Most strongly with... - Phenobarbital - Phenytoin - Carbamazepine Less so with... - Oxcarbazepine - Lamotrigine ```
36
Phenobarbital metabolism
Para-hydroxylation by 2C9 / 2C19
37
Primidone metabolism
Oxidation to Phenobarbital or Multiple steps to Phenylethylmalonamide (PEMA)
38
Phenytoin metabolism
Para-hydroxylation by 2C9 > 2C19 *Arene Oxide Intermediate* May proceed to inactive metabolite. May proceed to Glutathione / Mercapturic acid metabolites which cause toxicities.
39
Fosphenytoin metabolism
Dephosphorylation by various phosphatases
40
Ethosuximide metabolism
Ethyl-hydroxylation by 3A4 / 2E1
41
Valproic acid metabolism
``` Direct Glucuronidation - Inactive or beta-oxidation to form 2-ene product - Active or * Reactive minor metabolite - Toxicity ```
42
Carbamazepine metabolism
3A4 oxidation - Epoxide intermediate - Alkylation of proteins - Epoxide Hydrolase to catechol (inactive) Multi-Step metabolism to Iminoquinone form - Alkylation of proteins
43
Oxcarbazepine metabolism
Reduction to mono-hydroxy metabolite (active) | - "Licarbazepine"
44
Eslicarbazepine acetate metabolism
Ester Hydrolysis - Eslicarbazepine | - S form of Licarbazepine
45
Gabapentin metabolism
Not appreciably metabolized
46
Gabapentin enacarbil metabolism
Amide-like bond broken to release Gabapentin - Not appreciably metabolized
47
Pregabalin metabolism
Less than 2% metabolized
48
Vigabatrin metabolism
Not significantly metabolized
49
Felbamate metabolism
Practice pathway: Results in electrophilic "atropaldehyde" metabolite that is toxic.
50
Lamotrigine metabolism
Major route - Glucuronidation Minor route - P450's create Arene Oxide - Some Glucuronidated, some not. - Serious skin rashes
51
Topiramate metabolism
70% unchanged. | 30% many pathways.
52
Zonisamide metabolism
3A4 reduction in five membered ring or N-Acetylation of the sulfonamide group
53
Tiagabine metabolism
3A4 to 5-oxo-metabolite
54
Lacosamide metabolism
40% unchanged. O-demethylation by 2C19 (mainly) - Minor effects from inducers
55
Levetiracetam metabolism
No P450 66% excreted unchanged Most hydrolyzed to inactive acid product
56
Brivaracetam metabolism
``` 40% unchanged 2C19 - Hydroxylation on propyl side chain (inactive) Amide hydrolysis (inactive) ```
57
Rufinamide metabolism
Extensively metabolized. Major route - Amide hydrolysis (inactive) Can then be Glucuronidated
58
Ezogabine metabolism
No P450 Glucuronidation N-acetylation
59
Perampanel metabolism
3A4 hydroxylation

Phar 752 (12 decks)

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