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Neurology > Benzodiazepines > Flashcards

Benzodiazepines Flashcards

1
Q

T/F: Benzodiazepines are positive allosteric modulators

A

T

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2
Q

How are benzodiazepines different from barbituates and other CNS depressants?

A

CNS depression produced by benzodiazepines plateaus BEFORE achieving coma or lethal respiratory depression

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3
Q

Which benzodiazepines are short acting (2-5 hours)?

A
  • Triazolam (Halcion)
  • Midazolam (Versed)
  • Brotizolam (Lenormin)
  • Flurazepam (Dalmane)
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4
Q

Which benzodiazepines are intermediate acting (6-24 hours)?

A
  • Alprazolam (Xanax)
  • Lorazepam (Ativan)
  • Lormetazepam
  • Oxazepam (Serax)
  • Temazepam (Restoril)
  • Chlordiazepoxide (Librium)
  • Estazolam (ProSom)
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5
Q

Which benzodiazepines are long-acting (>24 hours)?

A
  • Clobazam (Onfi)
  • Clonazepam (Klonopin)
  • Chlorazepate (Tranxene)
  • Diazepam (Valium)
  • Flunitrazepam (Rohypnol)
  • Quazepam (Doral)
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5
Q

What is the benzodiazepine target?

A

GABA(A) receptor

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5
Q

Describe the GABA(A) Receptor

A
  • Macromolecular complex made up 5 subunits forming a Cl- channels
  • Alpha, beta, gamma are primary subunits
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6
Q

How is the GABA(A) receptor activated by GABA?

A
  • GABA binds to specific sites between the alpha and beta subunits
  • Two molecules of GABA are required to activate the receptor
  • Activitating the receptor increases Cl- conductance
  • Increasing Cl- conductance increases the threshold to produce an action potential
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7
Q

How are GABA(A) receptors activated by benzodiazepines?

A
  • BZs are positive allosteric modulators that enhance/facilitate GABA binding to the receptor complex. They are NOT receptor agonists
  • BZs bind to a site between the alpha and gamma subunits
  • BZs shift the GABA dose-response curve to the left
  • BZs increase the frequency of channel openings
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8
Q

BZ1

A
  • Responsible for sedation, amnesia, and possibly antiseizure effects
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9
Q

BZ2 and BZ3

A

Anxiolytic and muscle relaxant properties

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10
Q

What other compounds bind to the GABA(A)-Chloride Channel Complex?

A
  • Allopregnanolone, DHEA
  • Flumazenil (Romazicon) - BZ antagonist
  • Z-drugs: Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta) - selective BZ1 receptor agonists
  • General anesthetics
  • Ethanol
  • Barbituates.
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11
Q

Barbiturates (BAR)

A
  • Binds at a different site on the GABA(A) complex to facilitate GABA effect and increase chloride conductance: only alpha and beta subunits are required for action
  • Increase duration of each hyperpolarization event
  • Shift the GABA dose-response curve to the left and increase its maximum height
  • Less potent than BZ
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12
Q

What are the pros of diazepam?

A
  • Rapid onset
  • Rapid termination of CNS action due to redistribution to fat
  • Completely absorbed PO (94% bioavailability)
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13
Q

What are the cons of diazepam?

A

Not good to treat seizures b/c less than 30 min duration of action

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14
Q

What are the pros of lorazepam?

A
  • Slower redistribution into fat, therefore longer duration of effect
  • Better to treat acute seizures
15
Q

What are the cons of lorazepam?

A
  • Bioavailability of 90% by PO
  • Less lipophilic so slower onset
16
Q

Clorazepate (Tranxene)

A
  • Prodrug for nordiazepam
  • Hydrolyzed in the stomach to desmethyldiazepam
  • Used to treat anxiety
  • Also used along with other medications to treat seizures
17
Q

What is the metabolism of BZ?

A
  • Phase 1 N-dealkylation or hydroxylation
  • Phase II glucuronidation
18
Q

What are the drug interactions of benzodiazepines?

A
  • Alcohol
  • Opioids
  • Insomnia drugs
  • Fluoroquinolones
19
Q

The ‘Z’ Drugs

A
  • NOT benzodiazepines
  • To facilitate the onset and maintenance of sleep
  • Metabolized differently form benzodiazepines
20
Q

Zolpidem and Zaleplon

A
  • Selective BZ1 agonists
  • Produce sedation, minimal muscle relaxation, antiepileptic, and antianxiety effects
  • Indicated for sleep-onset insomnia
21
Q

Eszopiclone

A
  • Active S(+) isomer of zipiclone
  • Classified as a BZ1 agonist
  • Used for treatment of insomnia
22
Q

What is the FDA Boxed Warning of the ‘Z’ drugs?

A
  • Sleepwalking, sleep driving, and enagaging in the other activities while not fully awake

Neurology (21 decks)

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