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Anesthesia/AEDs/Psych drugs > AEDs > Flashcards

AEDs Flashcards

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1
Q

What drugs are narrow spectrum and primarily used for partial seizures (and tonic-clonic seizures)?

A 
Phenytoin
Carbamazepine
Oxcarbazepine
ESL
Lacosamide
Benzodiazepines
Phenobarbital (Barbiturates)
Gabapentin and Pregabalin
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2
Q

What drugs are broad spectrum and used to treat both partial and all types of generalized seizures?

A 
Valproate
Lamotrigine
Zonisamide
Topiramate
Felbamate
Levetiracetam
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3
Q

What drug is used to treat only absence seizures?

A

Ethosuximide

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4
Q

What are the drugs that induce their own metabolism by CYP450s?

A 
Phenytoin
Carbamazepine
Oxcarbazepine
Phenobarbital
Topiramate
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5
Q

What are the first line drugs to treat partial seizures?

A

Phenytoin - lots of side effects, drug-drug interactions
Carbamazepine - less side effects, also has dual action to suppress seizure foci AND prevent spread (often drug of choice)
Oxcarbazepine - less side effects and interactions, usually used as add-on

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6
Q

What are first line drugs to treat generalized seizures?

A

Valproate

Also potentially Levetiracetam

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7
Q

What is mechanism of action of Phenytoin?

A

Na+ channel blocker –> slows rate of channel recovery

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8
Q

What is unique about the metabolism of Phenytoin?

A

Induces P450s, causing increase in own metabolism

Metabolism shows properties of saturation kinetics
- Enzymes become saturated at higher doses and small increase in dose can cause unpredictable increases in plasma drug concentration (causing toxicity)

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9
Q

What are side effects of Phenytoin?

A 
Gingival hyperplasia - common side effect
Ataxia
Nystagmus
Incoordination
Confusion
Hirsutism
Facial coarsening
Systemic skin rash
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10
Q

What is the mechanism of action of Carbamazepine?

A

Na+ channel blocker –> slows rate of channel recovery

Unique in that has dual action in suppression of seizure foci and prevention of spread of activity

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11
Q

What is unique about metabolism of Carbamazepine?

A

Induces P450s, causing increase in own metabolism
- Larger doses may be necessary to maintain constant serum concentrations in first 3-6 weeks

Active 10-11 epoxy metabolite may contribute to neurotoxicity

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12
Q

What are side effects of Carbamazepine?

A 
Sedation
Drowsiness
Headache
Dizziness
Blurred vision
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13
Q

What is the mechanism of action of Oxcarbazepine?

A

Na+ channel blocker –> slows rate of channel recovery

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14
Q

How dose oxcarbazepine compare to carbamazepine?

A

Some induction of P450s, but much less than Carbamazepine
Sedating, but less side effects
Fewer interactions with other AEDs - but does interact with oral contraception

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15
Q

What is the mechanism of action of ESL?

A

Na+ channel blocker (higher affinity for inactive state)

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16
Q

What is unique about the metabolism of ESL?

A

Is a pro-drug that gets metabolized into an active drug specific for the active site

NO autoinduction of P450s

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17
Q

What are side effects of ESL?

A 
Dizziness
Somnolence
Headache
Nausea
Vomiting
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18
Q

What major drug interaction does ESL have?

A

Decreases oral contraceptive ability

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19
Q

What is ESL used to treat?

A

Partial seizures

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20
Q

What is Lacosamide used to treat?

A

Partial seizures - as add-on therapy

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21
Q

What is mechanism of action of Lacosamide?

A

Na+ channel blocker by changing conformation of Na+ channel

22
Q

What are Benzodiazepines used to treat?

A

Partial seizures, Tonic-clonic seizures
But NOT first line choice for any treatment
Typically only used to ablate seizures acutely

23
Q

What is the mechanism of action of Benzodiazepines?

A

GABA-potentiation
Enhances affinity of GABA-A receptor for GABA –> increases frequency of Cl- channel opening when GABA is bound –> hyperpolarization –> reduced neuron firing

24
Q

What are side effects of Benzodiazepines?

A

Sedation, dizziness, ataxia, drowsiness, tolerance

25
Q

What drugs are given IV for status epilepticus?

A

Dizepam or Lorazepam (Benzos)

Phenytoin

26
Q

What is Phenobarbital used to treat?

A

Partial seizures, Tonic-clonic seizures

but NOT first line

27
Q

What is mechanism of action of Phenobarbital?

A

GABA-potentiation (increase affinity of GABA-A receptor for GABA)

GABA-mimetic (can open GABA receptor itself)

28
Q

What are side effects of Phenobarbital?

A

Heavily sedating, cognitive effects, tolerance, withdrawal

29
Q

What are Gabapentin and Pregabalin used to treat?

A

Partial seizures, Tonic-clonic seizures

but as Add-on therapy

30
Q

What is mechanism of action of Gabapentin and Pregabalin?

A

Bind Alpha2-Delta1 subunit of voltage-gated Ca2+ channels –> reduce Ca2+ current –> decreased neuron firing

31
Q

What is Valproate used to treat?

A

Generalized seizures - first line

And Partial seizures, Absence seizures

32
Q

What are mechanisms of action of Valproate?

A

Inhibits T-type Ca2+ channels

Na+ channel blocker

Increases availability of GABA at synapse by increasing its synthesis

33
Q

What are side effects of Valproate?

A 
Problematic sedation
Tremor
Hair loss
Weight gain
Elevated liver enzymes
GI disturbances
34
Q

What is a major deterrent to use of Valproate in women?

A

Teratogenicity - linked to ASD, sensory deprivation disorder, spina bifida

35
Q

What drug interactions does Valproate have?

A

Valproate and Carbamazepine induce each other’s metabolism (P450s)

Valproate inhibits Phenobarbital metabolism

Valproate displaces phenytoin from binding proteins - contributes to toxicity

36
Q

What is Lamotrigine used to treat?

A

Partial seizures, Secondary generalized tonic-clonic

but only Add-on (rarely monotherapy)

37
Q

What are mechanisms of action of Lamotrigine?

A

Na+ channel blocker

Reduced glutamate release - glutamate receptor antagonist

Inhibition of Ca2+ channels

38
Q

How is Lamotrigine metabolized?

A

Glucuronidation in liver

39
Q

What is Zonisamide used to treat?

A

Partial seizures (only thing FDA approved for)

Sometimes used for myoclonic type generalized or for absence seizures

40
Q

What are mechanisms of action of Zonisamide?

A

Na+ channel blocker

Inhibits T-type Ca2+ channels

Glutamate receptor antagonist (reduced glutamate release)

41
Q

What is Topiramate used to treat?

A

generalized seizures EXCEPT absence

42
Q

What are mechanisms of action of Topiramate?

A

Glutamate receptor antagonism

GABA-potentiation

Na+ and Ca2+ channel block

Carbonic anhydrase inhibitor

43
Q

What are side effects of Topiramate?

A

Kidney stones
Cognitive/language difficulties
Oral-contraceptive interaction

44
Q

What is Felbamate used to treat?

A

Restricted to patients with refractory-to-treatment epilepsy due to serious side effects

45
Q

What is mechanism of action of Felbamate?

A

Glutamate receptor antagonism

46
Q

What are side effects of Felbamate?

A

Adverse behavioral effects

Cases of fatal aplastic anemia and liver failure

47
Q

What is Levetiracetam used to treat?

A

Partial seizures

Generalized seizures

48
Q

What is mechanism of action of Levetiracetam?

A

Modulates synaptic vesicles –> enhances release of GABA

May prevent epileptogenesis

49
Q

What is Ethosuxamide used to treat?

A

Absence seizure

50
Q

What is mechanism of action of Ethosuxamide?

A

Inhibits T-type Ca2+ channels in thalamus

Anesthesia/AEDs/Psych drugs (4 decks)

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