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Pharm U3 > 11) Antiepileptics > Flashcards

11) Antiepileptics Flashcards

1
Q

What is the class for Phenytoin (Dilantin)

A

Voltage-gated Na channel stabilizer

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2
Q

What is the mechanism for Phenytoin (Dilantin)

A

Stabilize inactive conformation of Na channel

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3
Q

What are the therapeutics for Phenytoin (Dilantin)

A

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

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4
Q

What are the important side effects for Phenytoin (Dilantin)

A

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

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5
Q

What are the other side effects for Phenytoin (Dilantin)

A

Mild myelosuppression, increased LFT; long-term: cerebellar degeneration, peripheral neuropathy, osteoporosis

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6
Q

What are the miscellaneous for Phenytoin (Dilantin)

A

IV infusion limited by hypotension; hepatic enzyme inducer (both auto- and hetero-inducer), highly protein bound

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7
Q

What is the class for Carbamazepine (Tegretol)

A

Voltage-gated Na channel stabilizer

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8
Q

What is the mechanism for Carbamazepine (Tegretol)

A

Stabilize inactive conformation of Na channel

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9
Q

What are the therapeutics for Carbamazepine (Tegretol)

A

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

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10
Q

What are the important side effects for Carbamazepine (Tegretol)

A

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

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11
Q

What are the miscellaneous for Carbamazepine (Tegretol)

A

Hepatic enzyme inducer (both auto- and hetero-inducer); highly protein bound; must increase dose in 1-2 wks due to autoinduction; side effects likely due to epoxide metabolite

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12
Q

What is the class for Oxcarbamazepine (Trileptal)

A

Voltage-gated Na channel stabilizer

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13
Q

What is the mechanism for Oxcarbamazepine (Trileptal)

A

Stabilize inactive conformation of Na channel

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14
Q

What are the therapeutics for Oxcarbamazepine (Trileptal)

A

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

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15
Q

What are the important side effects for Oxcarbamazepine (Trileptal)

A

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

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16
Q

What are the miscellaneous for Oxcarbamazepine (Trileptal)

A

Designed to bypass carbamazepine epoxide; less protein-bound, less autoinduction, fewer interactions, less toxic, longer half-life than carbamazepine

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17
Q

What is the class for Lamotrigine (Lamictal)

A

Voltage-gated Na channel stabilizer

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18
Q

What is the mechanism for Lamotrigine (Lamictal)

A

Stabilize inactive conformation of Na channel

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19
Q

What are the therapeutics for Lamotrigine (Lamictal)

A

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

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20
Q

What are the important side effects for Lamotrigine (Lamictal)

A

Rash, (rarely, Stevens-Johnson): slow initial titration important; may lead to contraceptive failure

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21
Q

What are the miscellaneous for Lamotrigine (Lamictal)

A

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

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22
Q

What is the mechanism for Valproate (Depakote)

A

Unknown; likely affects Na-gated channels and GABA system

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23
Q

What are the therapeutics for Valproate (Depakote)

A

Broad spectrum: absence, myoclonic, tonic-clonic, primary generalized, partial onset, and secondary generalized seizures (but not absence seizures); IV for status epilepticus; bipolar treatment, migraine and long-term cluster headache prophylaxis

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24
Q

What are the important side effects for Valproate (Depakote)

A

Weight gain, hair turnover, hyperammonemia (which can be mitigated with oral carnitine), teratogenicity, blood dyscrasias

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25
Q

What are the other side effects for Valproate (Depakote)

A

Pancreatitus

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26
Q

What is the class for Vigabatrin (Sabril)

A

GABAergic anti-epileptic

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27
Q

What is the mechanism for Vigabatrin (Sabril)

A

GABA transaminase binder (slows down intracellular breakdown of GABA)

28
Q

What are the therapeutics for Vigabatrin (Sabril)

A

Anti-epileptic

29
Q

What are the miscellaneous for Vigabatrin (Sabril)

A

Works on GABA-A

30
Q

What is the class for Tigabine (Gabitril)

A

GABAergic anti-epileptic

31
Q

What is the mechanism for Tigabine (Gabitril)

A

GABA reuptake inhibitor

32
Q

What are the therapeutics for Tigabine (Gabitril)

A

Anti-epileptic

33
Q

What are the miscellaneous for Tigabine (Gabitril)

A

Works on GABA-A

34
Q

What is the class for Benzodiazapines

A

GABAergic anti-epileptic

35
Q

What is the mechanism for Benzodiazapines

A

Bind GABA-A

36
Q

What are the therapeutics for Benzodiazapines

A

Status epilepticus (refractory); anesthesia

37
Q

What are the important side effects for Benzodiazapines

A

Sedation

38
Q

What are the miscellaneous for Benzodiazapines

A

Long-term usefulness limited by tolerance

39
Q

What is the class for Gabapentin (Neurontin)

A

GABA analog

40
Q

What is the mechanism for Gabapentin (Neurontin)

A

Block presynaptic influx of Ca

41
Q

What are the therapeutics for Gabapentin (Neurontin)

A

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

42
Q

What are the important side effects for Gabapentin (Neurontin)

A

Sedation

43
Q

What are the miscellaneous for Gabapentin (Neurontin)

A

Absorption limited by intestinal AA transporter (there is a Tm); limited protein binding; no metabolism or drug interaction in humans (so few side effects)

44
Q

What is the class for Pregabalin (Lyrica)

A

GABA analog

45
Q

What is the mechanism for Pregabalin (Lyrica)

A

Block presynaptic influx of Ca

46
Q

What are the therapeutics for Pregabalin (Lyrica)

A

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

47
Q

What is the class for Topiramate (Topamax)

A

Glutamate Receptor Blockers

48
Q

What is the mechanism for Topiramate (Topamax)

A

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

49
Q

What are the therapeutics for Topiramate (Topamax)

A

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

50
Q

What are the important side effects for Topiramate (Topamax)

A

Mild metabolic acidosis, kidney stones (due to some carbonic anhydrase activity); modest weight loss; rare acute glaucoma; sedation

51
Q

What are the other side effects for Topiramate (Topamax)

A

Word-finding problems

52
Q

What are the miscellaneous for Topiramate (Topamax)

A

Carbonic anhydrase activity leads to mild metabolic acidosis, which leads to respiratory compensation, which leads to mild alkalosis, which leads to calcium ionization, which leads to tingling; treat with vitamin C (acidify urine)

53
Q

What is the class for Felbamate (Felbatol)

A

Glutamate Receptor Blockers

54
Q

What is the mechanism for Felbamate (Felbatol)

A

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

55
Q

What are the therapeutics for Felbamate (Felbatol)

A

Partial onset seizures with or without secondary generalization; medically refractory epilepsy

56
Q

What are the important side effects for Felbamate (Felbatol)

A

Uncommon but potentially fatal. Aplastic anemia, acute hepatic failure. Requires monitoring.

57
Q

What is the class for Levetiracetam (Keppra)

A

Synaptic vesicle binder

58
Q

What is the mechanism for Levetiracetam (Keppra)

A

Binds synaptic vesicle protein 2, leading to less NT release

59
Q

What are the therapeutics for Levetiracetam (Keppra)

A

Partial onset seizures, secondary generalized seizures; maybe primary generalized epilepsy

60
Q

What are the important side effects for Levetiracetam (Keppra)

A

Well tolerated; sedation, mostly; rarely, irritability, aphasia, thrombocytopenia

61
Q

What is the class for Ethosuximide (Zarontin)

A

Voltage-gated Ca channel blocker

62
Q

What is the mechanism for Ethosuximide (Zarontin)

A

Blocks T-type Ca-channels in thalamo-cortical circuits

63
Q

What are the therapeutics for Ethosuximide (Zarontin)

A

Absence seizures only (and neuropathic pain)

64
Q

What are the important side effects for Ethosuximide (Zarontin)

A

Nausea (transient), sedation, irritability

65
Q

What are the miscellaneous for Ethosuximide (Zarontin)

A

Readily absorbed, minimal first pass metabolism; not protein bound

Pharm U3 (13 decks)

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