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Unit 3 Pharm > Antiepileptic Drugs > Flashcards

Antiepileptic Drugs Flashcards

1
Q

Antiepileptic drugs limit the excitability of what channels/receptors?

A

Voltage-gated Na and Ca channels and Glu receptors

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2
Q

Antiepileptic drugs enhance the inhibition of what system?

A

GABA system

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3
Q

Membrane ion channel involved in action potential generation, and
stabilizes inactive state inhibiting recurrent depolarization

A

Voltage-gated sodium channel

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4
Q

What 4 drugs have primary activity against the VG-Na channel?

A

Phenytoin, carbamazepine, oxcarbamazepine, lamotrigine

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5
Q

What 3 drugs have secondary activity against the VG-Na channel?

A

Valproate, felbamate, topiramate

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6
Q

Presynaptic membrane channels
in which blocking the influx of the name’s ion leads to less excitatory neurotransmitter release? Blocking this is useful in treating what type of pain?

A

Voltage-gated calcium channel. Neuropathic pain

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7
Q

What are the two primary [high-voltage type-] VG-Ca channel blocking drugs?

A

Gabapentin and pregabalin

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8
Q

Blocker of the T-type VG-Ca channel in the thalamus

A

Ethosuximide

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9
Q

Name the 5 drugs with secondary activity against the VG-Ca channel

A

Topiramate, Felbamate, Phenobarbitol, Lamotrigine, Levitiracetam

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10
Q

Receptors that lie on the post synaptic membrane of excitatory synapses and are ligand-gated cation channels (Ca, Na)

A

Glutamate receptors (AMPA & kainate receptors or NMDA receptor)

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11
Q

NMDA receptor blocker

A

Felbamate

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12
Q

Partially active as AMPA and Kainate receptor blocker

A

Topiramate

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13
Q

Receptors are found on post synaptic membranes of inhibitory synapses and are ligand-gated Cl channels

A

GABA-A

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14
Q

What drug and other class of drug activate the GABA-A receptors?

A

Phenobarbital and benzos

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15
Q

What 5 drugs have secondary activity for the GABA-A system?

A

Valproate, Topiramate, Gabapentin, Leviteracetam, Felbamate

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16
Q

VG-Na blockers have similar efficacies, similar metabolism and toxicities. They’re all hepatic enz inducers, especially lamotrigine. This drug makes ppl metab steroids faster and can thus lower the efficacy of what drugs and create a problem in ppl already taking teratogens?

A

Birth-control pills

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17
Q

Carbamazepine toxicity: colloquial phrase but also list them

A

“Dizzy, drunk, dbl vision” = sedation, ataxia, diplopia

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18
Q

Carbamazepine AEs

A

Rash (15%), rarely Stevens-Johnson, mild hepatic enz elevation, mild myelosuppression

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19
Q

Carbamazepine uses

A

More effective for Complex Partial Epilepsy than Primary Generalized (preferred to Phenobarbitol, Phenytoin, Valproate which are also effective), useful in BAD and in treating neuropathic pain

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20
Q

Pharm considerations for what drug?:
Highly protein bound
Hepatic metabolism
Autoinduction and heteroinduction
Effects other hepatically metabolized meds
Can cause contraceptive failure
Short half-life, extended release preparations
Toxicity thought to be due to epoxide metabolite

A

Carbamazepine

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21
Q

Toxicity of Phenytoin (dilantin)

A

Dizzy, drunk, dbl vision = Dizziness, Nystagmus, Ataxia, Incoordination.

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22
Q

AEs of phenytoin

A

Mild hepatotoxicity and myelosuppression,
Gingival hyperplasia, rash, hirsutism, Lupus-like reaction
Long term: cerebellar degeneration, peripheral neuropathy, osteoporosis

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23
Q

IV infusion of phenytoin is limited by what side effect?

A

Hypotension

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24
Q

Effective against Tonic-Clonic seizures of Primary Generalized Epilepsy or Partial onset and Secondarily Generalized seizures. Effective for acute seizures, even those that may not be related to epilepsy. Less effective for Absence, Myoclonic or Atonic seizures

A

Phenytoin

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25
Q

What is the IV route of phenytoin useful in?

A

Status Epilepticus

26
Q

Pharmacologic Considerations of what drug?:
Highly protein bound
Hepatic metabolism
Enzyme inducer
Effects other hepatically metabolized meds.
Can be associated with contraceptive failure
Variable but longer half-life, usually once daily dosing

A

Phenytoin

27
Q

Designed to bypass cabamazepine epoxide. Less protein bound, less autoinduction, fewer interactions, less toxic, and longer half life

A

Oxcarbazepine

28
Q

Oxcarbazepine has the same efficacy and indications as carbazepine, notably usefulness in treating what?

A

Neuropathic pain

29
Q

Lamotrigine toxicity

A

Dizziness, Sedation, Ataxia, Diplopia

30
Q

AEs of lamotrigine

A

Dose-related rash (3%) (slow initial titration is important)

31
Q

If you don’t know by now, what is the toxicity of Na-channel blockers?

A

Dizzy, drunk, dbl vision

32
Q

The list of indications are for what drug Na-channel blocker?:
Effective for Primary Generalized Epilepsy, Partial Complex Epilepsy and secondary generalization, Absence.
Indication for use in children.
Less effective for and may exacerbate Myoclonic seizures.
Useful in Bipolar Affective disorder.
Useful in treating in neuropathic pain

A

Lamotrigine

33
Q 
Pharmacologic Considerations for what drug?
Hepatic metabolism
Less protein bound 
Hepatic enzyme inducer
Can cause contraceptive failure
A

Lamotrigine

34
Q

Lamotrigine competes for excretion and has synergistic action with what drug?

A

Valproic acid (Depakote)

35
Q

GABA transaminase binder (GABA-T, or GABA transaminase, makes GABA inactive in the presyn neuron)

A

Vigabatrine

36
Q

GABA reuptake inhibitor

A

Tiagabine

37
Q

Class of drugs used in Status Epilepticus that act at the GABA-A receptors and are dose limited by sedation

A

Benzos

38
Q

Benzo used in anesthesia or refractory Status Epilepticus

A

Midazolam

39
Q

Na-channel blocker and GABA-system enhancer with sedation and tremor as its toxicity

A

Valproate

40
Q

AEs of valproate

A

Nausea, wt gain, hair loss, hyperammonemia, teratogenic (4-8%)

41
Q

Effective against Absence, Myoclonic and Tonic-Clonic seizures of Primary Generalized Epilepsy as well as Partial onset and secondarily generalized seizures. Used in treatment of Bipolar Affective disorder. Used in Migraine prophylaxis

A

Valproate

42
Q

Valproate in IV route is useful in?

A

Status Epilepticus

43
Q 
Pharmacologic Considerations for what drug?
Highly protein bound
Hepatic metabolism
Rapidly Absorbed and Metabolized
Short half-life
Extended release preparations
A

Valproate

44
Q

GABA analogs, inhibits Ca currents

A

Gabapentin and pregabalin

45
Q

Gabapentin and pregabalin used as adjunctive tx for what type of epilepsy? More commonly used for treating what?

A

Partial complex. Neuropathic pain

46
Q

Toxicity of gabapentin is related to what?

A

Sedation

47
Q

Pharmacologic Considerations for what drug?
Absorption limited at amino acid transporter in the intestine
Limited protein binding
No evidence of metabolism in humans
No interaction with other medications
Eliminated unchanged in urine
No serious organ toxicity

A

Gabapentin

48
Q

Effective against Absence Seizures only

A

Ethosuximide

49
Q

Drug with a 40-60 hr half-life and side effects of transient nausea, sedation, and irritability

A

Ethosuximide

50
Q

Effective against Partial onset and secondarily generalized seizures as well as Primary Generalized Epilepsy. Effective for Migraine prophylaxis

A

Topiramate

51
Q

Toxicity of topiramate

A

Sedation, cognitive = ‘word-finding’

52
Q

Adverse rxns of what drug?:
Mild Metabolic Acidosis&raquo_space; Respiratory compensation&raquo_space; Mild Alkalosis&raquo_space; Calcium ionization&raquo_space; tingling (can be mitigated with Vit C). Modest wt loss, kidney stones, and rare acute glaucoma

A

Topiramate

53
Q

Effective against Partial onset and secondarily generalized seizures. Some evidence of activity against Primary Generalized Epilepsy. Named Keppra

A

Levetiracetam

54
Q

Mech of action of Levetiracetam

A

Binds to synaptic vesicle protein 2 resulting in less neurotransmitter release (Glu)

55
Q

Levetiracetam is well-tolerated with one toxicity, what is it?

A

Sedation

56
Q

AEs of irritability, aphasia, and thrombocytopenia characterize what drug?

A

Leveitracetam

57
Q

Lithium is used as what kind of stabilizer to tx what? Also tx’s what type of HA?

A

Mood-stabilizer used to tx BAD and Cluster Headache

58
Q

Alters Sodium transport. Inhibits Sodium re-absorption proximal tubule. Renal clearance related to serum concentration. What drug?

A

Lithium

59
Q

Given Lithium’s S.E.s, where is it contra’d?

A

In those with a arrhythmia or prone to dehydration

60
Q

Lithium interacts with what 3 drug classes?

A

Diuretics, ARBs, NSAIDs

61
Q

Toxicity of what drug?
Lower level: sedation, dizzy, thirst, inc. urination, fine tremor.
Higher level: “Giddiness”, ataxia, blurred vision, large amt of dilute urine.

A

Lithium

62
Q

In addition to being aware of ppl with arrythmias, what syndrome can be unmasked by lithium?

A

Brugada syndrome

Unit 3 Pharm (8 decks)

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