Block 2 Lecture 5 -- ASDs Flashcards by Drew Spargo

Q

Indications for phenytoin:

A

1) focal seizures
2) generalized tonic-clonic
3) emergency status epilepticus

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Q

Indications for carbamazepine:

A

1) temporal lobe epilepsy

2) all others except absence

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Q

Indications for oxcarbazepine:

A

1) temporal lobe epilepsy

2) all others except absence

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Q

Indications for valproic acid:

A

1) absence

2) most others

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Q

Indications for lamotrigine:

A

all seizure types

– including generalized w/ absence attacks in children

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Q

Indications for topiramate:

A

1) focal seizures

2) generalized tonic-clonic

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Q

Indications for zonisamide:

A

1) focal seizures

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Q

Indications for lacosamide:

A

adjunct for focal-onset

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Q

Indications for gabapentin

A

focal seizures

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Q

Indications for pregabalin:

A

same as gabapentin

– focal seizures

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Q

Indications for ethosuximide:

A

absence seizures

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Q

Indications for retigabine:

A

adjunct for focal seizures

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Q

Indications for levetiracetam:

A

1) focal

2) generalized tonic-clonic

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Q

Indications for perampanel:

A

focal seizures

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Q

Indications for felbamate:

A

lennox-gastaut syndrome

retractable epilepsy with uncontrollable seizures

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Q

MoA of phenytoin

A

use-dependent Na+ channel blockade

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Q

MoA of carbamazepine

A

use-dependent Na+ channel blockade

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Q

MoA of oxcarbazepine

A

use-dependent Na+ channel blockade

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Q

MoA of lamotrigine

A

use-dependent Na+ channel blockade

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Q

MoA of lacosamide

A

use-dependent Na+ channel blockade

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Q

MoA of valproic acid

A

1) use-dependent Na+ channel blockade
2) stimulate GABA synthesis
3) inhibit GABA TA

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Q

MoA of topiramate

A

1) use-dependent Na+ channel blockade
2) augment GABA at GABAa
3) blockade of GluR (kainate and AMPA)

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Q

MoA of zonisamide

A

1) use-dependent Na+ channel blockade

2) t-type Ca channel blockade

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Q

MoA of Gabapentin

A

1) Ca channel blocker

2) GABAergic

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MoA of pregabalin

Ca channel blocker

MoA of ethosuximide

Ca channel blocker

MoA of retigabine

K channel stabilizer

MoA of levetiracetam

SV2A binder

MoA of perampanel

AMPAr blocker (non-competitive)

MoA of felbamate

NMDAr blocker

Which ASDs exhibit PPB?

1) phenytoin (95%) 2) perampanel (95%) 3) valproic acid (90%) 4) levetiracetam (10%)

Which ASDs are non-sedating?

1) phenytoin 2) lamotrigine 3) valproic acid 4) ethosuximide 5) felbamate

What is the black box warning on felbamate?

1) aplastic anemia | 2) acute hepatic failure

Which ASDs are secreted as a glucuronide?

1) oxcarbazepine 2) lamotrigine 3) valproic acid

Describe the metabolism of phenytoin.

1) non-linear (induces and saturates) 2) CYP2C9 + CYP2C19 3) t1/2 = 15-20h

Describe the metabolism of carbamazepine.

1) CYP2C9, C19, 3A4 2) t1/2 = 12-30h 3) long-term t1/2 = 15hr

Describe the metabolism of oxcarbazepine.

1) t1/2 = 1-2h | 2) t1/2 (active mets) = 8-12h

Describe the metabolism of lamotrigine.

t1/2 = 25h

Describe the metabolism of lacosamide.

1) cyp2c19 | 2) t1/2 = 12-16h

Describe the metabolism of valproic acid.

1) cyp2c19 | 2) t1/2 = 8-17h

Describe the metabolism of topiramate?

t1/2 = 20-30h

Describe the metabolism of zonisamide.

cyp3a4 | t1/2 = 60+ hr

Describe the metabolism of gabapentin.

hardly metabolized | t1/2 = 6h

Describe the metabolism of pregabalin.

hardly metabolized | t1/2 = 6h

Describe the metabolism of ethosuximide.

t1/2 = 60h

Describe the metabolism of retigabine.

t1/2= 8-11h

Describe the metabolism of levetiracetam.

hardly metabolized | t1/2 = 6-8h

Describe the metabolism of perampanel.

1) cyp3a4 | 2) t1/2= 70 - 105h

Describe the metabolism of felbamate

1) t1/2 = 20h

Which ASDs are affected by CYP3A4 inducer and inhibitors?

1) perampanel 2) zonisamide 3) oxcarbazepine (less) 4) carbamazepine (more) 5) phenytoin

Which ASDs are metabolized by CYP2C19?

phenytoin | lacosamide

What are DDIs for lamotrigine?

hepatic inducers that increase glucuronidation and clearance

What are DDIs of valproic acid?

1) PPB displacers | 2) inhibits metabolism of phenobarb, phenytoin, carbamazepine

What are DDIs for topiramate?

carbamazepine and phenytoin increase metabolism

Which ASDs don't have DDIs according to PK?

1) Ca channel blockers 2) K channel blockers (retigabine) 3) SV2a (keppra) 4) lacosamide

What drugs are metabolized by CYP3A4?

1) ASDs 2) OCC 3) warfarin 4) corticosteroids

What are CYP3A4 inhibitors?

1) valproic acid 2) cimetidine 3) erythromycin

What are CYP3A4 inducers?

1) phenytoin 2) primidone 3) phenobarbitol

What drugs displace PPB'ers?

1) valproate 2) phenytoin 3) salicylate

What ASD has a serine residue?

lacosamide

What drugs is cross-reactive to sulfonamide allergy?

zonisamide

What drug is a monosaccharide derivative?

topiramate (fructopyranose)

What drug has a triazine group?

lamotrigine

What is phenytoin's prodrug?

fosphenytoin

How does retigabine work?

increases relative refractory period by binding to retigabine binding site on K+ channel

What is the effect of SV2a modulation?

altered Glu and GABA release

What drugs affect the AMPAr?

1) primary = perampanel | 2) also: phenobarb, topiramate, lamotrigine

What ASDs carry black box warnings?

1) perampanel: aggression, anger, homocidal 2) felbamate: aplastic anemia, acute hepatic failure 3) retigabine: retinal abnormalities and skin discoloration

What is the intermediate in phenytoin metabolism?

reactive ARENE OXIDE | -- probably causes the ADRs

What ASDs act on CRMP2?

lacosamide has secondary activity