Pharmacology of Sleep Agents

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Questions and Answers

Which of the following is classified as an ultrashort acting barbiturate?

  • Amobarbital
  • Phenobarbital
  • Diazepam
  • Thiopental (correct)

What distinguishes benzodiazepines from barbiturates in their chemical structure?

  • Fusion of benzine and diazepine rings (correct)
  • Longer duration of action
  • Rapid metabolism in the liver
  • Presence of barbituric acid

Which medication category includes both short-acting and intermediate-acting types?

  • Barbiturates
  • Anxiolytics
  • Benzodiazepines (correct)
  • Melatonin

What is the primary role of barbiturates in clinical practice?

<p>Sedation and anesthesia (B)</p> Signup and view all the answers

Which medication is known for its potential to cause dependency when used long-term?

<p>Diazepam (C)</p> Signup and view all the answers

Melatonin is primarily known for its role in treating which condition?

<p>Insomnia (C)</p> Signup and view all the answers

Which medication is primarily used as a hypnotic in children before short procedures?

<p>Chloral Hydrate (A)</p> Signup and view all the answers

What is the mechanism of action of Buspirone?

<p>It acts as an agonist of 5-HT1A receptors. (B)</p> Signup and view all the answers

Which of the following statements about Ramelteon is true?

<p>It selectively agonizes MT1 and MT2 melatonin receptors. (D)</p> Signup and view all the answers

What precaution should be taken when administering Buspirone?

<p>Avoid using it with SSRIs to prevent Serotonin Syndrome. (A)</p> Signup and view all the answers

What is the main pharmacological effect of Chloral Hydrate?

<p>It produces sedative and hypnotic effects. (A)</p> Signup and view all the answers

How long does it typically take for Buspirone to effectively suppress anxiety?

<p>10-14 days (C)</p> Signup and view all the answers

What is a primary characteristic of Z-hypnotics compared to benzodiazepines?

<p>They act specifically as hypnotics without multiple effects. (A)</p> Signup and view all the answers

Which of the following is true regarding the treatment of benzodiazepine overdose?

<p>Flumazenil is used to counteract benzodiazepine effects. (A)</p> Signup and view all the answers

What role does melatonin play in sleep regulation?

<p>It regulates circadian rhythm and mediates sleep. (A)</p> Signup and view all the answers

Which class of medications is specifically indicated for treating insomnia in patients with narrow-angle glaucoma?

<p>Z-hypnotics such as zolpidem. (A)</p> Signup and view all the answers

Which of the following statements about the pharmacologic effects of Z-hypnotics is accurate?

<p>They act rapidly and have a short duration of action. (A)</p> Signup and view all the answers

What is a key difference between benzodiazepines and Z-hypnotics regarding withdrawal symptoms?

<p>Benzodiazepines withdrawal is milder overall. (A)</p> Signup and view all the answers

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Study Notes

Melatonin Congeners

  • Ramelteon selectively acts as an agonist at melatonin MT1 & MT2 receptors, promoting sleep and regulating circadian rhythms.

Chloral Hydrate

  • An alcohol derivative with sedative and hypnotic effects, onset within 30 minutes and duration of about 6 hours.
  • Primarily used as a hypnotic in children prior to short procedures, like dental work.

Buspirone

  • Functions as an agonist of the 5-HT1A serotonin receptor in the midbrain.
  • Anxiolytic effects develop slowly, typically within 10 to 14 days.
  • Preferred anxiolytic for geriatrics, with no muscle relaxant or hypnotic effects.
  • Has no potential for drug dependence.
  • Combining buspirone with SSRIs can lead to dangerous serotonin syndrome.

Serotonin

  • Known as 5-hydroxytryptamine (5-HT), it is a crucial monoamine neurotransmitter that facilitates communication between nerve cells in the brain.

Z-Hypnotics

  • Includes medications such as Zolpidem, Zaleplon, Zopiclone, and Eszopiclone.
  • Mechanism involves binding to GABA receptors similarly to benzodiazepines.
  • Specifically effective as hypnotics without anticonvulsant or anxiolytic properties, characterized by rapid and short action duration.
  • Primarily used to treat insomnia, valued for lower risk of tolerance and milder withdrawal symptoms compared to benzodiazepines.
  • Detected overdose can be treated with Flumazenil.

Melatonin

  • A hormone from the pineal gland influencing sleep regulation and circadian rhythms via MT1 (sleep mediation) and MT2 (circadian regulation) receptors.
  • Widely recognized as a natural hypnotic, particularly effective for alleviating jet lag symptoms.

Sedative-Hypnotics and Anxiolytics Classification

  • Non-Benzodiazepines: Ramelteon, Melatonin
  • Barbiturates: Classified by duration (ultra-short, short, intermediate, long-acting)
  • Benzodiazepines: Sub-categorized into ultra-short (e.g., Remimazolam), short (e.g., Triazolam), and long-acting (e.g., Diazepam).

Barbiturates vs. Benzodiazepines

  • Barbiturates: Derived from barbituric acid with varied durations (ultra-short acting like Thiopental to long-acting like Phenobarbital).
  • Benzodiazepines: Characterized by the fusion of benzene and diazepine rings, having varying onset and duration profiles across different drugs.

Key Differences

  • Barbiturates generally have immediate onset and longer durations compared to benzodiazepines, which may have varied rapid effects and longer half-lives.

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