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Pharmacology > Antiepileptics > Flashcards

Antiepileptics Flashcards

1
Q

Voltage-gated Na blockers (stabilizers of inactive state)?

A

Carbamazepine, Oxcarbamazepine, Phenytoin, Lamotrigine

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2
Q

Carbamazepine class?

A

Sodium channel blocker

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3
Q

Carbamazepine for?

A

Complex partial epilepsy (versus primary generalized), bipolar affective disorder, neuropathic pain

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4
Q

Carbamazeipine toxicity?

A

Sedation, ataxia, diplopia

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5
Q

Carbamazepine adverse reactions?

A

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

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6
Q

Toxicity of carbamazepine is due to?

A

Epoxide metabolite

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7
Q

Pharmacologic considerations of carbamazepine?

A

Highly protein bound; Autoinduction & heteroinduction occur (so much so that increased dose is needed 1-2 weeks into treatment); Short half-life

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8
Q

`Phenytoin class?

A

Sodium channel blocker

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9
Q

Phenytoin for?

A

Tonic-Clonic seizures of Primary Generalized Epilepsy or Partial onset and Secondary Generalized Seizures. Effective for acute seizures.

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10
Q

Phenytoin is less effective for what seizures?

A

Absence, myoclonic, atonic

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11
Q

Phenytoin toxicity?

A

Dizziness, nystagmus, ataxia, incoordination

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12
Q

Phenytoin adverse reactions?

A

Mild hepatotoxicity, myelosuppression, gingival hyperplasia, rash, hersutism, Lupus-like reaction, contraceptive failure, & (with long term use) cerebellar degeneration, peripheral neuropathy, osteoporosis

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13
Q

IV infusion of Phenytoin limited by?

A

Hypotension

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14
Q

IV Phenytoin for?

A

Status epilepticus

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15
Q

Phenytoin half-life?

A

Longer, can be used for once daily dosing

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16
Q

Oxcarbazepine class?

A

Sodium channel blocker

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17
Q

Oxcarbazepine has the same…

A

efficacy & indications as Carbamazepine

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18
Q

How is oxcarbazepine better than carbamazepine?

A

Less protein bound, less autoinduction, fewer interactions, less toxic, longer half-life

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19
Q

Oxcarbazepine for?

A

Complex partial epilepsy (versus primary generalized), bipolar affective disorder, neuropathic pain

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20
Q

Oxcarbazepine toxicity?

A

Sedation, ataxia, diplopia

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21
Q

Oxcarbazepine adverse reactions?

A

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

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22
Q

Lamotrigine class?

A

Sodium channel blocker

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23
Q

Lamotrigine for?

A

Primary Generalized, Partial Complex, Secondary Generalization, Absence. Also: Bipolar Affective, Neuropathic pain

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24
Q

Unique about Lamotrigine?

A

Indication for use in children

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25
Q

Lamotrigine is less effective and may exacerbate?

A

Myoclonic seizures

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26
Q

Lamotrigine toxicity?

A

Dizziness, sedation, ataxia, diplopia, can cause contraceptive failure (more so than others)

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27
Q

Lamotrigine adverse reactions?

A

Rash (rarely, Stevens-Johnson) – rash is dose related, and slow initial titration is important.

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28
Q

Lamotrigine pharmacological considerations?

A

Less protein bound, hepatic metabolism, hepatic enzyme inducer

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29
Q

Lamotrigine competes with excretion with?

A

Valproic acid

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30
Q

Synergistic action with Lamotrigine?

A

Valproate (Depakote)

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31
Q

Benzodiazepines for?

A

Status Epilepticus, Anasthesia

32
Q

Benzodiazepines class?

A

GABA-A receptor agonists

33
Q

Benzodiazepine dose limited by?

A

Sedation. Long term use limited by tolerance

34
Q

Benzodiasepine timing?

A

Short acting due to distribution

35
Q

Name 3 benzodiazepines.

A

Lorazepam (Ativan) & Diazepam (Valium) & Midazolam (versed)

36
Q

Midazolam for?

A

Anasthesia or refractory status epilepticus

37
Q

Iv half-life of midazolam?

A

minutes (orally, 1 hr)

38
Q

Valproate mxn?

A

Unknown, probably Na channel and GABA system actions

39
Q

Valproate for?

A

Broad spectrum. Absence, myoclonic, Tonic-Clonic of Primary Generalized Epilepsy, partial onset, and secondary generalized. IV for status epilepticus. Bioplar affective. Migraine prophylaxis.

40
Q

5 pharmacoligical considerations of valproate?

A

Highly protein bound, hepatic mets, rapidly absorbed & metabolized, short half-life, extended release preparations

41
Q

Valproate toxicity?

A

Sedation, tremor

42
Q

Valproate adverse effects?

A

Nausea, weight gain, hair loss, hyperammonemia, teratogenic. Still, this won’t affect BC effectiveness and is considered a “very safe drug”

43
Q

Phenobarbitol and Benzodiazepines do what?

A

Bind to GABA receptor

44
Q

GABA transaminase binder?

A

Vigabatrine (slows intracellular breakdown of GABA)

45
Q

GABA reuptake inhibitor?

A

Tiagabine

46
Q

GABA channels use what ion?

A

Chloride

47
Q

GABA analogs?

A

Gabapentin & Pregabalin

48
Q

What do GABA analogs do?

A

Inhibit Ca current

49
Q

Gabapentin class?

A

GABA analog

50
Q

Pregabalin class?

A

GABA analog

51
Q

GABA analogs used for?

A

Adjunctive treatment for partial complex epilepsy, but especially more commonly for neuropathic pain

52
Q

What limits gapapentin absorption?

A

Amino acid transporter in the intestin

53
Q

Toxicity of gabapentin?

A

Sedation, but in general NO major organ toxicity

54
Q

Gabapentin binds proteins? Interacts with other drugs?

A

Limitedly, no interaction with other drugs

55
Q

Is gabapentin metabolized by the body?

A

No evidence of metabolism in humans, eliminated unchanged in urine

56
Q

Ethosuximide class?

A

T-type Ca-channel blocker in thalamo-cortical circuits

57
Q

Ethosuximide for?

A

Absence seizures only

58
Q

Ethosuximide side effects?

A

Transient nausea, sedation, irritability

59
Q

Ethosuximide absorption and metabolism?

A

Readily absorbed, minimal first pass metabolism, not protein bound

60
Q

Topiramate class?

A

AMPA & Kainate Ca channel blocker; also activity at Na and GABA channels

61
Q

Topiramate for?

A

Partial onset, secondarily generalized, primary generalized, migraine prophylaxis.

62
Q

Topiramate activates what enzyme, causing what?

A

Carbonic anhydrase –> mild met acidosis –> respiratory compensation –> mild alkalosis –> calcium ionization –> tingling

63
Q

How can tingling from topiramate be counteracted?

A

Vitamin C

64
Q

Besides tingling, adverse reactions of topiramate?

A

modest weight loss, kidney stones, (rarely) acute glaucoma

65
Q

Levitiracetam class?

A

Synaptic vesicle protein 2 binder resulting in less neurotransmitter release

66
Q

Levetiracetam for?

A

Partial onset & Secondarily Generalized seizures, maybe primary generalized.

67
Q

How is levetiracetam tolerated?

A

Well

68
Q

Levetiracetam toxicity?

A

Sedation

69
Q

Levetiracetam adverse reactions?

A

Irritability, aphasia, thrombocytopenia

70
Q

Lithium for?

A

Bipolar affective mood stabilization, cluster headache

71
Q

Lithium is cleared how?

A

Renal

72
Q

Lithium alters transport of? Where?

A

Sodium re-absorption in th eproximal tubule

73
Q

Lithium is contraindicated in?

A

Those with arrythmia or prone to dehydration

74
Q

Drug interactions of lithium?

A

Diuretics, ARB, NSAID

75
Q

Toxicity of lithium at low levels?

A

Sedation, dizzy, thirst, inc. urination, fine tremor

76
Q

Toxicity of lithium at high levels?

A

Giddiness, ataxia, blurred vision, large amt of dilute urine

77
Q

Cautions with lithium?

A

arrythmia, family Hx of sudden death < 45, Brugada syndrome

Pharmacology (46 decks)

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