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Psychiatry > SM_93b: Anticonvulsants > Flashcards

SM_93b: Anticonvulsants Flashcards

1
Q

Many people with epilepsy are ____ to antiseizure medications

A

Many people with epilepsy are refractory to antiseizure medications

  • Failure of previous AEDs diminishes seizure-free rates to future AEDs
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2
Q

Describe cellular mechanisms of seizure generation

A

Cellular mechanisms of seizure generation

  • Too much excitation: ionic (inward Na+ or Ca2+ currents), neurotrasnmitter (glutamate, aspartate)
  • Too little inhibition: ionic (inward Cl- or outward K+ currents), neurotransmitter (GABA)
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3
Q

Describe targets for anticonvulsants

A

Targets for anticonvulsants

  • Increase inhibitory neurotransmission via GABA
  • Decrease excitatory neurotransmission via glutamate
  • Block voltage gated inward Na+ or Ca2+ currents
  • Increase outward K+ current
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4
Q

1st generation enzyme-inducing anticonvulsants include ___, ___, and ___, while enzyme inhibitors include ___

A

1st generation enzyme-inducing anticonvulsants include phenobarbital, phenytoin, and carbamazepine, while enzyme inhibitors include valproate

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5
Q

Phenytoin acts by ____, can be dosed ____, and has ____

A

Phenytoin acts by inhibiting Na+ channel firing, can be dosed once per day, and has unpredictable kinetics

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6
Q

Phenytoin adverse effects include ____, ____, and ____

A

Phenytoin adverse effects include CNS sedation (drowsiness, ataxia, confusion, insomnia, nystagmus, etc), gum hyperplasia, and hirsutism

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7
Q

Carbamazepine acts by ____, is related to ____, and is dosed ____

A

Carbamazepine acts by inhibiting Na+ channels, is related to antidepressants (tricyclic structure), and is dosed twice per day

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8
Q

Carbamazepine side effects include ____ and ____ and has the interaction of ____

A

Carbamazepine side effects include agranulocytosis / aplastic anemia and hyponatremia and has the interaction of stimulating metabolism of other drugs by inducing enzymes (chemo, warfarin)

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9
Q

Phenobarbital acts by ____ and is dosed ____

A

Phenobarbital acts by allosterically modulating GABAA receptor to increase duration of opening and is dosed once daily

Can cause CNS sedation

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10
Q

Valproic acid is a first line drug for ____ but causes side effects of ____ and ____

A

Valproic acid is a first line drug for generalized epilepsy but causes side effects of hepatotoxicity and birth defects (NTDs)

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11
Q

Ethosuximide is used for ___ and acts by ____

A

Ethosuximide is used for abscence seizures and acts by blocking T-type Ca2+ currents in the thalamus

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12
Q

Oxcarbazepine acts by ____ but has side effect of ____

A

Oxcarbazepine acts by activity-dependent blockade of Na+ channels and augmentation of K+ channels but has side effect of prominent hyponatremia

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13
Q

____ worsens abscence

A

Carbamazepine worsens abscence

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14
Q

1st generation AEDs have ____ kinetics

A

1st generation AEDs have unfavorable kinetics (potent enzyme inducers and high protein binding)

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15
Q

Benzodiazepines are used for ____ and ____ and act by ____

A

Benzodiazepines are used for status epilepticus and myoclonic seizures and act by allosterically modulating GABAA receptors to increase the frequency of Cl- channel opening

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16
Q

_____ is an ineffective add-on therapy for partial seizures

A

Gabapentin is an ineffective add-on therapy for partial seizures

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17
Q

Lamotrigine acts by ____, ____, and ____ and is dosed ____

A

Lamotrigine acts by inhibiting Na+ channels, glutamate release, and Ca2+ channels and is dosed once daily

18
Q

Lamotrigine has side effect of ____

A

Lamotrigine has side effect of Stevens-Johnson syndrome

19
Q

____ is antiepileptic drug safe in pregnancy

A

Lamotrigine is antiepileptic drug safe in pregnancy

20
Q

Felbamate has adverse effects of ____ and ____

A

Felbamate has adverse effects of aplastic anemia and severe hepatitis

21
Q

Levetiracetam (Keppra) acts by ____

A

Levetiracetam (Keppra) acts by reducing high voltage-activated Ca2+ currents

22
Q

Levetiracetam (Keppra) has side effect of ____

A

Levetiracetam (Keppra) has side effect of irritability

23
Q

Zonisamide functions by ____, ____, and ____

A

Zonisamide functions by blocking Na+ channels, T-type Ca2+ channels, and carbonic anhydrase

Causes kidney stones

24
Q

Topiramate functions by ____ and is dosed ____

A

Topiramate functions by blocking Na+ channels / increasing frequency of GABAA channel openings / interferes with glutamate binding to AMPA/KA receptor and is dosed twice daily

25
Q

Topiramate side effects are ____, ____, and ____

A

Topiramate side effects are memory / cognitive, appetite suppression, and weight loss

26
Q

____ is an anticonvulsant effective for migraine prophylaxis and treats neuropathic pain and tremor

A

Topiramate s an anticonvulsant effective for migraine prophylaxis and treats neuropathic pain and tremor

27
Q

Lyrica (pregabalin) acts on ____ and is dosed ____

A

Lyrica (pregabalin) acts on voltage-gated Ca2+ channels and is dosed three times per day

28
Q

Lyrica (pregabalin) causes side effects of ____

A

Lyrica (pregabalin) causes side effects of appetite increase / weight gain

29
Q

Vigabatrin side effect is ____

A

Vigabatrin side effect is irreversible visual field constrrction

30
Q

Vigabatrin acts by _____

A

Vigabatrin acts by blocking GABA metabolism by irreversibly inhibiting GABA transaminase

31
Q

Lacosamide acts by ___

A

Lacosamide acts by prolonging the slow inactivation phase of Na channel opening (potent inhibitor of Na channel activity)

(dosed 2x/day)

32
Q

Second generation AEDs are ____ and ____ but not ____

A

Second generation AEDs are safer and better tolerated but not more potent

Fewever drug interactions, lower protein binding, less likely to cause significant enzyme induction or inhibition

33
Q

Absorption is ____

A

Absorption is entry of drug into blood

  • Essentially complete for all AEDs (except gabapentin)
  • Timing varies widely
  • Generally slowed by food in stomach (except CBZ)
  • Usually takes several hours
34
Q

Enzyme inducers ____

A

Enzyme inducers increase clearance and decrease steady-state concentrations of other substrates

  • CBZ autoinduces
  • Results from hepatic synthesis of additional enzyme
  • Slower in onset/offset than inhibition interactions
  • Broad spectrum inducers: CBZ, phenytoin, phenobarbital
  • Selective CYP3A inducers: felbamate, topiramate, oxcarbazepine
35
Q

Enzyme inhibitors ____

A

Enzyme inhibitors decrease clearance and increase steady-state concentrations of other substrates

  • Results from competition with other substrates at specific hepatic enzyme sites
  • Onset typically rapid and concentration dependent
36
Q

Valproate competitively inhibits ____, increasing plasma concentrations of ____ and ____, and inhibits ____, increasing plasma concentratiojns of ____ and ____

A

Valproate competitively inhibits UDP glucuronosyltransferase, increasing plasma concentrations of lamotrigine and lorazepam, and inhibits CYP2C19, increasing plasma concentrations of phenytoin and phenobarbital

37
Q

Topiramate and oxcarbazepine inhibit ____, increasing plasma concentrations of ____

A

Topiramate and oxcarbazepine inhibit CYP2C19, increasing plasma concentrations of phenytoin

38
Q

Felbamate inhibit ____, increasing plasma concentrations of ____ and ____

A

Felbamate inhibit CYP2C19, increasing plasma concentrations of phenytoin and phenobarbital

39
Q

Describe common acute dose-related adverse effects of AEDs

A

Common acute dose-related adverse effects of AEDs

40
Q

____ and ____ may exacerbate epileptic seizures

A

Tramadol and venflaxine may exacerbate epileptic seizures

Psychiatry (37 decks)

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