Sedative Hypnotics Flashcards Preview

BB Test 3 > Sedative Hypnotics > Flashcards

Flashcards in Sedative Hypnotics Deck (16)
Loading flashcards...

What drugs are classified as sedative hypnotics?

  • Barbiturates
  • Benzodiazepines
  • Nonbenzodiazepines (Z-drugs)
  • Others (Buspirone)


Where on the GABA receptor do Benzodiazepines bind?

  • Between α1 and γ2 subunits
  • Benzodos increase the frequency of Cl- channel opening (results in hyperpolarization)


Where on the GABA receptor do Barbiturates bind?

  • Different site than Benzodiazepines and Z-drugs (Flumazenil, Zolpidem)
  • Increase the duration of Cl-channel opening (results in hyperpolarization)


What are the GABAA-α1 selective agonists?

  • Zolpidem
  • Zaleplon
  • Eszopiclone

More receptor specific

May lose specificity if you take a lot of them (dependence)


What are the other drugs that bind at a site on the GABA receptor close to where benzodiazepines bind?

  • Z-Drugs (α1 agonist; AKA BZ1 subtype receptor of GABA)
    • Zolpidem.
  • Flumazenil (Benzodiazepine antagonist)


Why are benzodiazepines less lethal than barbiturates?

  • Barbiturates cause greater CNS effects with greater doses (causes decreased respiration)
    • Especially if mixed with alcohol and/or opiates (other depressants)
    • Barbiturates have low therapeutic index
    • Barbiturates induce CYP450 so they have many drug interactions
  • CNS effects are lower for benzodiazepines (never reach respiratory decreasing levels)


What benzodiazepines don't require oxidative metabolism? Which patients would this be ideal for?

  • Oxazepam
  • Temazepam (sleep medication)
  • Lorazepam

Easy On The Liver


  • Good for patients with impaired liver function
  • They are only conjugated and don't have active metabolites


What is the mechanism of action for Flumazenil?

  • Competitive antagonist for BZ binding site (blocks action of benzodiazepines and Z-drugs)
    • But not barbiturates, ethanol, opioids, anesthetics (used for problems with anesthesia)



What are some adverse effects of Flumazenil? What drug is used more than Flumazenil?

  • Can cause precipitated withdrawal symptoms (including seizures) in benzodiazepine-dependent patients
  • Naloxone is used more (safer and more likely to act on the respiratory depression caused by opioids)


What is the half-life of Flumazenil?

  • Short (30-60 minutes)
    • Shortest of all BZDs so there may be need for frequent dosing


What patients are barbiturates contraindicated in?

Patients with acute intermittent porphyria or porphyria variegate


What is the mechanism of action for Buspirone? What is the onset?

  • 5-HT1A Partial agonist
  • Slow onset (2-6 weeks)


What is Buspirone used for clinically?

  • Generalized anxiety disorder (GAD)
    • No abuse potential


What is the mechanism of action for Ramelteon?

Agonist at MT1 and MT2 melatonin receptors (located in the suprachiasmatic nuclei of the brain)


What is Ramelteon used for clinically?

  • Insomnia
    • No abuse potential


Barbiturates (increase/decrease) the production of porphyrins.