Pharmacology 1: Sedative-Hypnotic CNS Drugs

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Questions and Answers

What is the primary effect of sedative anxiolytics?

Inducing sleep

Providing anterograde amnesia

Reducing anxiety and exerting a calming effect (correct)

Suppressing reflexes

Which of the following benzodiazepines is classified as short-acting?

Alprazolam

Diazepam

Flurazepam

Triazolam (correct)

What is the primary effect of hypnotic agents?

Reducing anxiety

Providing anterograde amnesia

Inducing drowsiness and encouraging sleep (correct)

Suppressing reflexes

Which of the following is an atypical sedative-hypnotic agent?

Zolpidem Signup and view all the answers

What is the effect of benzodiazepines on REM sleep?

Reduced REM sleep Signup and view all the answers

What is the primary use of Thiopental in anesthesia?

Inducing anesthesia Signup and view all the answers

What is the main inhibitory neurotransmitter in the CNS that benzodiazepine binds to?

Gamma-aminobutyric acid Signup and view all the answers

Which of the following is a potential side effect of benzodiazepine in the cardiovascular system?

Hypotension Signup and view all the answers

What is the primary indication for benzodiazepine in anesthesia?

Anesthesia induction Signup and view all the answers

What is the mechanism of action of flumazenil?

It binds to a similar site to the benzodiazepine, antagonizing its effect Signup and view all the answers

Which of the following is a potential interaction with benzodiazepine?

Strong CYP3A4 or CYP2C19 inhibitor Signup and view all the answers

What is the resulting effect of benzodiazepine binding to the GABA receptor?

Increased frequency of chloride channel opening Signup and view all the answers

What is the effect of barbiturates on the flow of chloride through channels?

Increases the flow Signup and view all the answers

What is a use of Phenobarbital?

Treatment of neonatal hyperbilirubinemia Signup and view all the answers

What is a common toxicity of barbiturates?

All of the above Signup and view all the answers

What is an advantage of Zolpidem?

Physical dependence is rare Signup and view all the answers

What receptors does Ramelteon act on?

MT1 and MT2 receptors Signup and view all the answers

What enzymes metabolize Ramelteon?

CYP1A2 and 2C9 Signup and view all the answers

Study Notes

Benzodiazepines

Benzodiazepines act by binding to the gamma subunit of GABA A receptors, enhancing GABA's effect, and increasing chloride channel opening frequency.
Indications include seizure disorders, alcohol withdrawal, anxiety disorders, insomnia, and as induction agents in anesthesia.
Side effects encompass cardiovascular issues (hypotension), musculoskeletal effects (muscle weakness), neurologic effects (amnesia, drowsiness, euphoria, ataxia), respiratory depression, dermatologic rashes, and genitourinary difficulties.
Drug interactions can occur with strong inhibitors or inducers of CYP3A4 or CYP2C19.

Flumazenil

Flumazenil is a benzodiazepine antagonist used as a reversal agent in overdose cases.
It competes for the same binding site as benzodiazepines.

Barbiturates

Classified into ultra-short (Thiopental), short (Secobarbital), intermediate (Amobarbital), and long-acting (Phenobarbital) categories.
May antagonize glutamic acid, enhance GABA effects, and increase chloride flow through channels.
Commonly used for sedation, induction of anesthesia, seizure control, and treatment of neonatal hyperbilirubinemia.
Toxicity includes oversedation, rapid tolerance, high abuse potential, and risk of acute overdose leading to coma, respiratory depression, cardiovascular collapse, and renal failure.

Atypical Agents

Zolpidem acts on benzodiazepine receptors, providing significant sedation with minimal anxiolytic action; less likely to cause physical dependence.
Ramelteon functions as an agonist at MT1 and MT2 receptors in the suprachiasmatic nucleus, with low abuse risk and is metabolized by CYP1A2 and 2C9, interacting with fluvoxamine and azole antifungals.

Sedative-Hypnotic Overview

Sedatives reduce anxiety and produce a calming effect, while hypnotics promote drowsiness and sleep maintenance.
Newer unclassified agents demonstrate a flatter dose-response curve compared to traditional benzodiazepines.

Dose-Response Characteristics

Benzodiazepines can induce hypnosis, which reduces REM sleep and can cause REM rebound.
They are associated with amnesia and suppressed reflexes during anesthesia; short-acting options for IV use include Lorazepam and Diazepam.

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Description

This quiz covers the pharmacology of sedative and hypnotic drugs that affect the central nervous system, including benzodiazepines and barbiturates. Topics include the different types of sedatives and hypnotics, their mechanisms of action, and their clinical uses.