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PPI-2 > Antiseizure drugs > Flashcards

Antiseizure drugs Flashcards

1
Q

What is the MOA of gabapentin?

A

Unknown but enhances GABAergic effects and blocks presynaptic calcium channels, which could decrease glutamate release

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2
Q

What is the MOA of phenytoin and carbamazepine?

A

Prolongs inactivated state of Na-channels by blocking a voltage gated sodium channel

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3
Q

What is the MOA of lamotrigine?

A
  1. Prolongs inactivated state of Na-channels by blocking a voltage gated sodium channel
  2. Inhibits excitatory neurotransmission by blocking glutamate release
  3. Blocks T-type calcium channels (absence seizures only)
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4
Q

What is the MOA of topiramate?

A
  1. Prolongs inactivated state of Na-channels by blocking a voltage gated sodium channel
  2. Inhibits excitatory neurotransmission by blocking AMPA
  3. Enhances inhibitory neurotransmission via GABA-A
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5
Q

What is the MOA of valproic acid?

A
  1. Prolongs inactivated state of Na-channels by blocking a voltage gated sodium channel
  2. Enhance inhibitory neurotransmission via GABA-T
  3. Blocks T-type calcium channels (absence seizures only)
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6
Q

What is the MOA of levetiracetam?

A

Targets excitatory glutamanergic synapse by blocking at the vesicle

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7
Q

What is the MOA of perampanel?

A

Targets excitatory glutamanergic synapse by blocking AMPA

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8
Q

What is the MOA of tiagabine?

A

Targets inhibitory GABAergic synapse via GAT-1 transporter

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9
Q

What is the MOA of barbituates and benzodiazepines?

A

Targets inhibitory GABAergic synapse via GABA-A

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10
Q

What is the MOA of ethosuximide?

A

Blocks T-type calcium channels and can be used in absence seizures only due to a single blockade

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11
Q

What antiseizure drugs are considered broad spectrum?

A

Valproic acid and lamotrigine

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12
Q

What are the clinical uses of phenytoin?

A

Any seizure type except absence seizures (effective against focal onset and generalized onset tonic-clonic seizures)

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13
Q

What are drug interactions with phenytoin?

A
  • Induces CYP3A4 (increases metabolism of other drugs) so would decrease effectiveness of birth control or other antiseizure drugs like carbamazepine
  • Caution w phenytoin dosage as it’s zero order and toxicity could occur easily
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14
Q

What are side effects seen with phenytoin?

A
  • CNS: nystagmus, ataxia, diplopia, sedation
  • Endocrine: osteomalacia w hypocalcemia
  • Hematologic effects: megaloblastic anemia (folate deficiency)
  • Misc: gingival hyperplasia, facial coarsening, hirsutism
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15
Q

What are contraindications with phenytoin?

A

Teratogenic–> can cause cleft lip and palate

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16
Q

What are clinical uses for carbamazepine?

A
  1. Any seizure type except absence seizures (effective against focal onset seizures with or without spread to bilateral tonic-clonic seizure)
  2. Trigeminal neuralgia (DOC)
  3. Bipolar disorders
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17
Q

T/F: You can start to see lower levels of carbamazepine if you take it for a while

A

True; this is due to it being an auto-inducer of its own metabolism

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18
Q

What are side effects seen with carbamazepine?

A

CNS: diplopia, ataxia, and drowsiness
Hypersensitivity: rash, steven johnson syndrome (BBW)
Hematologic: leukopenia and aplastic anemia (BBW)
Endocrine: Dilutional hyponatremia from ADH

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19
Q

What drug interactions are seen with carbamazepine?

A

There are many due to CYP450 induction and enhances the metabolism of drugs that are degraded by these enzymes

20
Q

What are contraindications of carbamazepine?

A

Teratogenic–> cleft lip/palate and spina bifida

21
Q

What are the clinical uses for ethosuximide?

A

Used only for absence seizures and is the drug of choice

22
Q

What are side effects seen with ethosuximide?

A

GI: anorexia, n/v
CNS: sedation, dizziness, ataxia

23
Q

What are clinical uses for valproic acid?

A

Any seizure states (including absence seizures), migraine prophylaxis, and bipolar disorders

24
Q

What are side effects seen with valproic acid?

A

GI: n/v and weight gain
Liver: toxic so monitor LFTs
CNS: tremor, dizziness, sedation
Misc: alopecia

25
Q

What are drug interactions for valproic acid?

A

Inhibits CYP2C9 so decreases metabolism of phenytoin and phenobarbital (can cause increased levels of these leading to toxicity)

26
Q

WWhat are contraindications of valproic acid?

A
  1. Patients with liver disease
  2. Children (d/t increased risk of fatal hepatotoxicity)
  3. Teratogenic: spina bifida (BBW for pregnancy and contraception requirement)
27
Q

What are the clinical uses of lamotrigine?

A

Any seizure state (including absence) but usually adjunct therapy + can be used for bipolar disorder

28
Q

What are side effects with lamotrigine?

A

CNS: dipolpia, headache, ataxia
Hypersensitivity: skin rash (BBW) and steven johnson syndrome

29
Q

What are the clinical uses of topiramate?

A

Any seizure type except absence seizures: effective against primary and secondary generalized tonic-clonic seizures; focal seizures

30
Q

What are adverse effects of topiramate?

A

CNS: cognitive problems (memory and language difficulties), headache, fatigue, dizziness
Misc: weight loss

31
Q

What is the combination of phentermine and topiramate used for?

A

Weight loss

32
Q

What are drug interactions for topiramate?

A

Induces CYP3A and inhibits CYP2C19

33
Q

What are contraindications of topirmate?

A

Teratogenic: cleft lip/palate

34
Q

What are clinical uses of gabapentin?

A
  1. Focal onset seizures and focal onset seizures with spread to bilateral tonic-clonic seizures (adjunct therapy)
  2. Neuropathic pain
35
Q

How do the pharmacokinetics of gabapentin affect dosing regimens?

A

The transport is saturable so its bioavailability decreases with dose: to increase the dose patients have to often take this more often (multiple times a day)

36
Q

What are side effects with gabapentin?

A

CNS: sedation, dizziness, ataxia
Misc: weight gain

37
Q

What is the clinical use for tiagabine?

A

Focal onset seizures and often used as adjunct therapy

38
Q

What are side effects seen with tiagabine?

A

CNS: sedation and dizziness

39
Q

What are clinical uses for diazepam and lorazepam?

A

Treatment for status epilepticus in emergency seizures over 5 minutes

40
Q

What are the clinical uses for phenobarbital and pentobarbital?

A

Treatment for status epilepticus

41
Q

What are side effects seen with diazepam and lorazepam?

A

Sedation, motor impairment, amnesia, physical dependence

42
Q

What are side effects seen with phenobarbital and pentobarbital?

A

Sedation (limiting), drowsiness, cognitive issues, and ataxia

43
Q

What are the treatment guidelines for status epilepticus?

A

IV lorazepam (or diazepam or midazolam) then wait one minute. If there is no response, additional lorazepam. Even if the seizure stops give nonbenzo seizure drug (fosphenytoin)

44
Q

What are clinical uses for levetiracetam (keppra) and brivaracetam?

A

Any seizures and FDA approved for adjunctive therapy

45
Q

What are side effects seen with levetiracetam and brivaracetam?

A

Minor CNS: sedation, depression

46
Q

What is the clinical use for perampanel?

A

Any seizure and approved for primary or adjunctive therapy

PPI-2 (7 decks)

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