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NSP Exam 3 > Anticonvulsants and Antiepileptic Drugs > Flashcards

Anticonvulsants and Antiepileptic Drugs Flashcards

(48 cards)

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1
Q

what is anticonvulsant therapeutics?

A

reduce seizure activity either by decreasing excessive excitatory glutamatergic neurotransmission and/or increasing inhibitory neurotransmission= restore balance

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2
Q

what are the drugs used for Tonic-clonic and/or Partial seizures?

A

phenytoin
carbamazepine
Valproate
Topiramate
Lamotrigine
Levetiracetam

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3
Q

what are the drugs used for absence seizures?

A

Ethosuximide
Valproate (multiple MOA)

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4
Q

what are the drugs used for Status Epilepticus and Acute Seizures?

A

BZDs (1st line) Lorazepam (Ativan) Clonazepam (Klonopin)
Barb’s (2nd line) Phenobarbital (Luminal)

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5
Q

what are the drugs used for neuropathic pain?

A

Gabapentin
Pregabalin
Carbamazepine

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6
Q

List the drugs whose MOA is Voltage-Gated Na⁺ Channel (VGNa⁺) Blockers

A

Phenytoin (Dilantin)
Carbamazepine (Tegretol)
Lamotrigine (Lamictal)
Valproate (Depakote)

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7
Q

List the drugs whose MOA is T type Voltage-Gated Ca²⁺ Channel (VGCC) Blocker

A

Valproate (Depakote)
Ethosuximide (Zarontin)

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8
Q

List the drug whose MOA is GABA Metabolism Inhibitor

A

Valproate (Depakote)

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9
Q

List the drugs whose MOA is N Type voltage- gated calcium channel (VGCC) blockers

A

Gabapentin (Neurontin)
Pregabalin

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10
Q

what is a benefit to using Barbiturates as an anti-epileptic drug?

A

reduce intracranial pressure if brain injury

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11
Q

what are the main differences between Benzodiazepines and Barbiturates ?

A
  • BZDs: safer, wide therapeutic index, has reversal agents
  • BARBs: drug interactions, narrow therapeutic index, death, respiratory depression, and lacks reversal agents
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12
Q

what are first line BZDs used for and can they be used long term?

A

acute drug induced seizures, acute relief of Status Epilepticus, or drug withdrawal seizures
- no they cannot be used long term (tolerance)

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13
Q

what is the BZD antidote if dose is too high?

A

flumazenil, but use with care: can precipitate more seizures if use too much

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14
Q

Why are lorazepam (Ativan) and clonazepam (Klonopin) the top choices for acute siezures?

A

L: due to no active metabolites;
C: long-acting if drug withdrawal causing seizures

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15
Q

how does Phenobarbital (Luminal) cause lots of dangerous drug interactions?

A

it is a CYP enzyme inducer

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16
Q

what is the MOA for the Voltage-gated Na+ Channel (VGNaC) Blockers (Phenytoin, Carbamazepine, Lamotrigine, Valproate)

A
  • Do NOT bind to resting sodium channels
  • Bind to the inactivated state of VGNaC
  • “Use-Dependent” Block (bind to Overactive Neurons)
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17
Q

what are the pharmacokinetics for Phenytoin?

A
  • Zero order kinetics
  • narrow therapeutic index (TI)
  • can use IV fosphenytoin for rapid onset (metabolized to phenytoin in body)
  • Cyp450 enzyme inducer can cause drug interactions
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18
Q

what are the pharmacokinetics for Carbamazepine?

A
  • first order kinetics
  • induces CYP3A4, it speeds up metabolism of many drugs, reducing their effectiveness
  • induces its own metabolism
  • need to monitor blood levels
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19
Q

what are other clinical uses for Carbamazepine?

A

mood stabilizer and for neuropathic pain
- 1st line treatment for trigeminal neuralgia

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20
Q

what are the major adverse effects for Phenytoin?

Study These Flashcards
A
  • gingival hyperplasia
  • dermatological: Steven-Johnson and TENS
  • hepatotoxicity
  • arrythmia (can be fatal)
21
Q

what are the major adverse effects for Carbamazepine?

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A
  • dermatological: Steven-Johnson and TENS
  • hepatotoxicity
  • hematological
  • suicidal ideation risk
22
Q

what are other uses for Lamotrigine (Lamictal)?

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A

Mood stabilizer ~ helps bipolar depression
- some efficacy in absence seizures but some black box issues

23
Q

what are the benefits of Lamotrigine (Lamictal)?

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A
  • Less drug interactions than others
  • Doesn’t inhibit/induce enzymes
  • Doesn’t promote weight gain
24
Q

what are the adverse effects for Lamotrigine (Lamictal)?

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A
  • Generally better tolerated then others
  • Diplopia common
  • Mild rash common (10%): less than 0.1% develop serious rash
25
what is the black boxed for Lamotrigine (Lamictal)?
Higher incidence of SJS & TENS then other VGNaC blockers
26
AED "Jack of All Trades"
Valproate (Depakote) due to multiple MOA * Inhibits GSK-3 & decreases protein kinase C
27
what is a common use for Valproate (Depakote)?
mood stabilizer in bipolar depression
28
what are the issues of Valproate (Depakote)?
- no rapid onset - Undergoes complicated hepatic metabolism & can produce hepatotoxic metabolites Major Adverse: Common - hair loss, weight gain (increases risk metabolic syndrome), dermatological possible
29
what are the 2 Black Boxes for Valproate (Depakote)?
- Hepatotoxicity…monitor liver function...especially dangerous to infants - Pancreatitis…uncommon but can progress rapidly… monitor for severe abdominal pain
30
what are the benefits of Levetiracetam (Keppra)?
- Rapid onset and generally well tolerated - Versatile ~ don’t know all mechanisms - can be used in pregnant patients
31
what are the adverse effects of Levetiracetam (Keppra)?
- Dizziness, ataxia - Anxiety ~ Recent FDA warnings of Increase in moodiness/aggressive behavior; Very rare but serious psychosis
32
drugs inhibiting the T-type Voltage-Gated Ca²⁺ Channel (VGCC) reduce the
abnormal T-current in absence seizures
33
what type of drug can worsen absence seizures?
pure Na+ blockers
34
what are the indications for Ethosuximide (Zarontin)?
1st line for absence seizures – not effective for generalized seizures
35
what are the adverse effects pf Ethosuximide (Zarontin)?
- Common effect –dizziness - Vomiting initially but generally well tolerated
36
what drug is often used in mixed tonic-clonic/absence seizures?
Valproate (Depakote)
37
what are the common uses for Topiramate (Topamax)?
- used for partial seizures - infantile seizures - adjuvant with other AEDs - migraine prevention - weight loss
38
what are the adverse effects of Topiramate (Topamax)?
dizziness paresthesias confusion some get mental health issues (including psychotic reactions) ***FDA warning: visual problems and glaucoma
39
what is the MOA of Gabapentin (Neurontin)?
- Voltage-Gated Ca²⁺ Channel (VGCC) Blockers α2delta subunit - increases GABA synthesis and release
40
what can Gabapentin (Neurontin) be used to treat and why?
Neuropathic and chronic pain - reduces aberrant sensitized C-fiber firing - use in diabetes with neuropathic pain Partial seizures - adjuvant “good mixer” drug - Lack hepatic metabolism - Generally well-tolerated
41
what are common issues with Gabapentin (Neurontin) ?
dizziness & ataxia
42
what are the special considerations for DISCONTINUATION?
- abrupt withdraw can cause rebound seizures - avoid drug interactions causing break-through seizures
43
what are the special considerations for PREGNANCY
several anticonvulsants are teratogenic - Polytherapy associated with birth defects - Monotherapy reduces birth defect risk
44
which drugs alter estrogen metabolism?
Carbamazepine, oxcarbazepine, phenobarbital, topiramate *decreases birth control effect
45
what drug can cause hepatotoxicity in infants & young children due breastfeeding or if taken during pregnancy?
Valproate
46
Valproate relative contraindication in pregnancy
- 1st trimester teratogenic: neural tube defects & Spina bifida - Low IQ in babies exposed later in pregnancy
47
PTH, CZB relative contraindication in pregnancy
- Fetal Hydantoin Syndrome (FHS) - Epoxide metabolites build up in baby & cause damage
48
Topiramate relative contraindication in pregnancy
- Increased risk cleft lip ~ common use as migraine preventative

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