Sedative and Hypnotic Agents Overview

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Questions and Answers

Which of the following benzodiazepines is likely to have the longest duration of action for anxiety management?

Alprazolam

Triazolam

Clonazepam (correct)

Oxazepam

What factor primarily differentiates sedative/hypnotics from barbiturates in terms of safety and therapeutic use?

Potency levels

Safety margin (correct)

Mechanisms of action

Risk of dependence

What is a potential long-term effect of chronic benzodiazepine use?

Reduced risk of dependence

Enhanced sedation during treatment

Development of tolerance (correct)

Increased efficacy over time

Which of the following benzodiazepines is indicated for acute anxiety management and characterized by rapid onset and a short half-life?

Triazolam Signup and view all the answers

What adverse effect is commonly associated with prolonged benzodiazepine use?

Dependence and tolerance Signup and view all the answers

What is the mechanism of action for benzodiazepines?

Potentiation of inhibitory neurotransmission via GABA-A receptors Signup and view all the answers

Which of the following correctly describes a key difference between barbiturates and benzodiazepines?

Benzodiazepines tend to have a safer profile than barbiturates. Signup and view all the answers

Which sedative/hypnotic agent potentially poses a fatal risk when combined with other CNS depressants?

Midazolam Signup and view all the answers

Which of the following agents is often associated with the management of acute anxiety?

Benzodiazepines Signup and view all the answers

What accounts for the increased safety of benzodiazepines over barbiturates?

Benzodiazepines have a broader therapeutic range. Signup and view all the answers

What is the primary mechanism of action for benzodiazepines?

Increase the frequency of channel openings in the presence of GABA Signup and view all the answers

Which statement accurately distinguishes barbiturates from benzodiazepines?

Barbiturates directly open channels without the presence of GABA Signup and view all the answers

Which of the following agents is classified as having a short duration of action?

Triazolam (Halcion) Signup and view all the answers

What is one of the common side effects associated with long-term use of benzodiazepines?

Next-day drowsiness and rebound insomnia Signup and view all the answers

Which of the following characteristics does NOT relate to the pharmacological properties of benzodiazepines?

Direct interaction with serotonin receptors Signup and view all the answers

Which benzodiazepine is specifically indicated for the management of anxiety disorders and has a medium duration of action?

Alprazolam (Xanax) Signup and view all the answers

What major metabolic process do benzodiazepines rely on?

Hepatic metabolism through cytochrome P450 enzymes Signup and view all the answers

Which factor is NOT relevant to determining the safety profile of sedative agents?

The color of the drug when ingested Signup and view all the answers

Study Notes

Antiepileptics

Gabapentin and pregabalin are commonly used antiepileptic agents.

Sedative/Hypnotics

Benzodiazepines (BZDs) and barbiturates (Barbs) differ in CNS depression levels.
Both classes enhance GABA-A receptor activity, leading to sedation and anxiolytic effects.
Barbiturates can cause severe respiratory and cardiovascular depression; they have a higher risk of coma and death compared to BZDs.
BZDs are generally safer; they induce calmness and sedation without fatal respiratory depression (except midazolam in specific contexts).

Mechanisms of Action

BZDs increase the frequency of GABA-A channel openings; barbiturates increase the mean open time.
Barbiturates can open channels directly without GABA, risking respiratory failure.

Pharmacological Properties

Varying characteristics include potency, onset (influenced by lipophilicity), and duration of action, influencing side effects such as rebound insomnia or daytime drowsiness.

Therapeutic Uses

Classification based on effects:
- Anxiolytics
- Hypnotics
- Antiepileptics
- Muscle relaxants
- Anesthesia
- Alcohol withdrawal
Drugs like diazepam and clonazepam have long half-lives suitable for antiepileptic use, while triazolam is preferred for its short half-life in treating insomnia.

Specific Agents and Their Uses

Diazepam (Valium): Long duration (1-3 days), treats anxiety, status epilepticus, and muscle spasms.
Alprazolam (Xanax): Medium duration (10-20 hrs), used for anxiety disorders and agoraphobia.
Lorazepam (Ativan): Medium duration (10-20 hrs), anxious disorders and seizures.
Clonazepam (Klonopin): Long duration (1-3 days), for panic disorders and as a prophylactic for petit mal seizures.
Midazolam (Versed): Short duration (3-8 hrs), used in pre-anesthesia and conscious sedation.

Pharmacokinetics

BZDs are rapidly absorbed orally, crossing the blood-brain barrier and placental barrier.
Hepatic metabolism occurs via cytochrome P450 enzymes (CYP3A4 and CYP2C19).
Certain substances like erythromycin and grapefruit juice can inhibit metabolism, leading to increased effects.

Adverse Effects

Despite a high safety margin, prolonged use of BZDs can result in dependence and tolerance.

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Description

This quiz covers key concepts related to sedative and hypnotic agents, including various classes of medications such as benzodiazepines, barbiturates, and newer alternatives like orexin antagonists. It also discusses their mechanisms, safety profiles, and potential side effects. Test your knowledge on these important pharmacological agents!