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MS 2 - Unit 3 > Pharmacology - Antiepileptic Drugs > Flashcards

Pharmacology - Antiepileptic Drugs Flashcards

1
Q

What are the molecular targets and actions of antiepileptic drugs?

A
  1. To limit excitability - voltage-gated Na and Ca channels and glutamate receptors
  2. To enhance inhibition of GABA system
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2
Q

Phenytoin
Carbamazepine
Oxcarbamazepine
Lamotrigine

These drugs all do what?

A

Antiepileptics and voltage-gated Na channels

Goal to stabilize the inactive state inhibiting recurrent depolarization

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3
Q

Blocking what channels decreases neuropathic pain?

A

Calcium channels

Ie Ethosuximide - T-type in thalamus

Gabapentin, Pregabalin - the high voltage type

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4
Q

Give the class: Felbamate

A

Glutamate receptor blocker

NMDA receptor blocker; secondary effect at voltage-gated Na and Ca channels, GABA system

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5
Q

Give the class: Topiramate

A

Glutamate receptor blocker

Partial AMPA, Kainate Ca receptor blocker; secondary effect at voltage-gated Na channel, GABA system

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6
Q

Phenobarbitol and benzodiazepines activate what system in treating epilepsy?

A

GABA system

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7
Q

Give the class: Carbamazepine

A

Sodium channel blocker

MOA: Stabilize inactive conformation of Na channel

AEs: Dizzy, drunk, double vision, mild myelosuppression

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8
Q

Give the indications for Carbamazepine.

A

Better for complex partial epilepsy than primary generalized seizures

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9
Q

In addition to epilepsy, carbamazepine is also useful in treating:

A

Bipolar Affective disorder (also neuropathic pain)

More effective for complex partial seizure than primary generalized; bipolar disorder; neuropathic pain

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10
Q

What is the most important thing to remember about carbamazepine?

A

Autoinduction - it can induce metabolism of itself (requires dose increase after reaching steady state)

Heteroinduction - it can induce metabolism of other drugs
for example: contraceptive pill failure

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11
Q

Give the side effects: carbamazepine

A

Rash (rarely, Stevens-Johnson), mild myelosuppression, mild increase in LFTs; can cause contraceptive failure

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12
Q

Give the class: Phenytoin

A

Voltage-gated Na channel stabilizer

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13
Q

Give the MOA: Phenytoin

A

Stabilize inactive conformation of Na channel

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14
Q

Give the indications: Phenytoin

A

Effective for tonic-clonic seizures of primary generalized epilepsy or partial onset and secondary generalized seizures

Less effective for absence (particular pediatric), myoclonic, atonic seizures

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15
Q

Give the side effects: Phenytoin

Long term side effects?

A

Rash, gingival hyperplasia, hirsutism, lupus-like reaction; can cause contraceptive failure

Long term: Cerebellar degeneration, peripheral neuropathy, osteoporosis

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16
Q

IV-Phenytoin is useful to treat what condition?

A

Status epilepticus

same with IV Valproate

17
Q

How is oxcarbazepine different from carbamazepine?

A

Oxcarbazepine is less protein-bound, less autoinduction, fewer interactions, less toxic, has a longer half-life than carbamazepine

18
Q

TEST QUESTION:

Lamotrigine is associated with what toxicity?

A

Dizziness
Sedation
Ataxia
Diplpia

AEs: rash (rarely Stevens-Johnson syndrome), slow initial titration is important

19
Q

Is Lamotrigine indicated for use in children to treat epilepsy?

A

Yes

Effective for primary generalized epilepsy, partial complex epilepsy and secondary generalization, absence

20
Q

Lamotrigine is NOT effective for what kind of seizures?

A

Myoclonic seizures

May exacerbate myoclonic seizures; competes with valproic acid for excretion (potential synergy); hepatic enzyme inducer; not very protein bound

21
Q

Give the indications for Lamotrigine.

A

Primary generalized epilepsies, absence seizures; indicated in children; bipolar disorder; neuropathic pain

22
Q

Lamotrigine has synergistic action with what drug?

A

Depakote (valproic acid)

23
Q

T/F: Lamotrigine can cause contraceptive failure.

A

True

Same with ALL voltage-gated sodium channel blockers - Phenytoin, Carbamazepine, Oxcarbamazepine

24
Q

Give the class: Gabapentin and Pregabalin

A

GABA analog

25
Q

Give the MOA of Gabapentin and Pregabalin.

A

Block presynaptic influx of Ca

26
Q

Give the indications for Gabapentin and Pregabalin.

A

Adjunct for partial complex epilepsy; more commonly used for neuropathic pain

27
Q

Ethosuximide is only effective against what kind of seizure?

A

Absence seizures

28
Q

Give the side effects: Ethosuximide

A

Nausea (transient)
Sedation
Irritability

29
Q

What is the half life of ethosuximide?

A

40-60 hours

30
Q

T/F: Topiramate is active at the postsynaptic membrane.

A

True

Partial AMPA, Kainate Ca receptor blocker; secondary effect at voltage-gated Na channel, GABA system

Use: Partial onset seizures, secondary generalized seizures, primary generalized epilepsy; migraine prevention, long-term prevention of cluster headaches

Side Effects: Mild metabolic acidosis, kidney stones (due to some carbonic anhydrase activity); modest weight loss; rare acute glaucoma; sedation and word finding difficulties

-Respiratory compensation from acidosis results in mild alkylosis, calcium ionization, and a sensation of tingling in fingers that can be alleviated with vitamin C

31
Q

What drug is a good choice to treat partial onset and secondarily generalized seizures?

A

Levetiracetam

32
Q

Give the class: Levetiracetam

A

Synaptic vesicle binder

Binds to vesicle protein 2 resulting in less neurotransmitter release

33
Q

Give the side effects: Levetiracetam

A

Irritability
Aphasia
Thrombocytopenia

Toxicity: Sedation

34
Q

What is the MOA for Ethosuximide?

A

Blocks T-type calcium channels in thalamus

35
Q

What is a common cause of temporal lobe epilepsy?

A

Head trauma

36
Q

What is the difference in molecular targets between Felbamate and Topiramate?

A 
Felbamate = NMDA antagonist
Topiramate = partial AMPA/Kinate antagonist
37
Q

Difference between side effect and toxicity?

A

Side effect is a drug effect that is not related to drug’s intended mechanism of action (e.g. developing a rash from taking a sodium channel blocker - Carbamazepine) whereas toxicity is an undesirable effect that is related to the mechanism of action (e.g. sedation, ataxia, diplopia from sodium channel blocking anti-epileptic - Carbamazepine)

38
Q

What causes carbamazepine toxicity (drunk, dizzy, double vision)?

A

epoxide metabolite

MS 2 - Unit 3 (45 decks)

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