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Pharmacology > Unit 3-Antiepileptics > Flashcards

Unit 3-Antiepileptics Flashcards

1
Q

Phenytoin

Drug class

A

Voltage-gated Na channel stabilizer

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2
Q

Phenytoin

Mechanism

A

Stabilize inactive conformation of Na channel

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3
Q

Phenytoin

Uses

A

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

IV route useful for status epilepticus

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4
Q

Phenytoin

Side effects

A
  • Rash, gingival hyperplasia, hirsutism, lupus-like reaction;
  • can cause contraceptive failure
  • Mild myelosuppression, increased LFT;
  • long-term: cerebellar degeneration, peripheral neuropathy, osteoporosis
  • IV infusion limited by hypotension;
  • hepatic enzyme inducer (both auto- and hetero-inducer), highly protein bound
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5
Q

Carbamazepine

Drug class

A

Voltage-gated Na channel stabilizer

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6
Q

Carbamazepine

Mechanism

A

Stabilize inactive conformation of Na channel

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7
Q

Carbamazepine

Uses

A
  • More effective for complex partial seizure than primary generalized;
  • bipolar disorder;
  • neuropathic pain
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8
Q

Carbamazepine

Side effects

A
  • Rash (rarely, Stevens-Johnson), mild myelosuppression, mild increase in LFTs;
  • can cause contraceptive failure
  • 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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9
Q

Oxcarbamazepine

Drug class

A

Voltage-gated Na channel stabilizer

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10
Q

Oxcarbamazepine

Mechanism

A

Stabilize inactive conformation of Na channel

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11
Q

Oxcarbamazepine

Uses

A
  • More effective for complex partial seizure than primary generalized;
  • bipolar disorder;
  • neuropathic pain
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12
Q

Oxcarbamazepine

Side effects

A
  • Rash (rarely, Stevens-Johnson), mild myelosuppression, mild increase in LFTs;
  • can cause contraceptive failure
  • Designed to bypass carbamazepine epoxide;
  • less protein-bound, less autoinduction, fewer interactions, less toxic, longer half-life than carbamazepine
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13
Q

Lamotrigine

Drug class

A

Voltage-gated Na channel stabilizer

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14
Q

Lamotrigine

Mechanism

A

Stabilize inactive conformation of Na channel

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15
Q

Lamotrigine

Uses

A
  • Primary generalized epilepsies, absence seizures;
  • indicated in children;
  • bipolar disorder;
  • neuropathic pain
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16
Q

Lamotrigine

Side effects

A
  • Rash, (rarely, Stevens-Johnson):
  • slow initial titration important;
  • may lead to contraceptive failure
  • May exacerbate myoclonic seizures;
  • competes with valproic acid for excretion (potential synergy);
  • hepatic enzyme inducer;
  • not very protein bound
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17
Q

Valproate

Mechanism

A

Unknown; likely affects Na-gated channels and GABA system

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18
Q

Valproate

Uses

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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19
Q

Valproate

Side effects

A

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

Pancreatitis

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20
Q

Vigabatrin

Drug class

A

GABAergic anti-epileptic

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21
Q

Vigabatrin

Mechanism

A

GABA transaminase binder (slows down intracellular breakdown of GABA)

Works on GABA-A

22
Q

Vigabatrin

Uses

A

Anti-epileptic

23
Q

Tigabine

Drug class

A

GABAergic anti-epileptic

24
Q

Tigabine

Mechanism

A

GABA reuptake inhibitor

Works on GABA-A

25
Q

Tigabine

Uses

A

Anti-epileptic

26
Q

Benzodiazapines

Uses

A

GABAergic anti-epileptic

27
Q

Benzodiazapines

Mechanism

A

Bind GABA-A

28
Q

Benzodiazapines

Uses

A

Status epilepticus (refractory); anesthesia

29
Q

Benzodiazapines

Side effects

A

Sedation

Long-term usefulness limited by tolerance

30
Q

Gabapentin

Drug class

A

GABA analog

31
Q

Gabapentin

Mechanism

A

Block presynaptic influx of Ca

32
Q

Gabapentin

Uses

A
  • Adjunct for partial complex epilepsy;
  • more commonly used for neuropathic pain
33
Q

Gabapentin

Side effects

A

Sedation

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

34
Q

Pregabalin

Drug class

A

GABA analog

35
Q

Pregabalin

Mechanism

A

Block presynaptic influx of Ca

36
Q

Pregabalin

Uses

A
  • Adjunct for partial complex epilepsy;
  • more commonly used for neuropathic pain
37
Q

Topiramate

Drug class

A

Glutamate Receptor Blockers

38
Q

Topiramate

Mechanism

A
  • Partial AMPA, Kainate Ca receptor blocker
  • secondary effect at voltage-gated Na channel, GABA system
39
Q

Topiramate

Uses

A
  • Partial onset seizures, secondary generalized seizures, primary generalized epilepsy;
  • migraine prevention, long-term prevention of cluster headaches
40
Q

Topiramate

Side effects

A

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

Word-finding problems

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)

41
Q

Felbamate

Drug class

A

Glutamate Receptor Blockers

42
Q

Felbamate

Mechanism

A

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

43
Q

Felbamate

Uses

A

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

44
Q

Felbamate

Side effects

A

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

45
Q

Levetiracetem

Drug class

A

Synaptic vesicle binder

46
Q

Levetiracetem

Mechanism

A

Binds synaptic vesicle protein 2, leading to less NT release

47
Q

Levetiracetem

Uses

A

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

48
Q

Levetiracetem

Side effects

A

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

49
Q

Ethosuximide

Drug class

A

Voltage-gated Ca channel blocker

50
Q

Ethosuximide

Mechanism

A

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

Readily absorbed, minimal first pass metabolism; not protein bound

51
Q

Ethosuximide

Uses

A

Absence seizures only (and neuropathic pain)

52
Q

Ethosuximide

Side effects

A

Nausea (transient), sedation, irritability

Pharmacology (26 decks)

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