30 Questions
What is the main route of metabolism before elimination for sedative-hypnotic drugs?
Hepatic metabolism
Which type of drugs are most sedative-hypnotic drugs?
Lipid-soluble drugs
Which drug enters the CNS rapidly and can be used as an induction agent in anesthesia?
Thiopental
Which drug undergoes extrahepatic conjugation and does not form active metabolites?
Lorazepam
Which drug is oxidized to an active metabolite known as trichloroethanol?
Chloral hydrate
What is responsible for the short duration of action of zolpidem?
Rapid metabolism by liver enzymes
Which enzyme is responsible for the rapid hepatic metabolism of zaleplon?
Aldehyde oxidase
What is the half-life of eszopiclone?
6 hours
Which receptor is most associated with inhibition in the CNS?
GABAA receptor
Which sedative-hypnotic drug has a duration of CNS action of more than 30 hours?
Diazepam
What isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits?
α1β2γ2δ1
Which sedative-hypnotic drug facilitates neuronal membrane inhibition by actions at specific receptors?
Diazepam
Which neurotransmitter is most associated with inhibition in the CNS?
GABA
What type of receptors do benzodiazepines bind to?
GABAA receptors
What effect do benzodiazepines have on GABA-mediated chloride ion channels?
They increase channel opening frequency
What is the primary transmitter associated with inhibition in the CNS?
GABA
Which sedative-hypnotic drug has the highest lipid solubility and can be used as an induction agent in anesthesia?
Thiopental
What is responsible for the short duration of action of zolpidem?
Rapid metabolism by liver enzymes
Which sedative-hypnotic drug is oxidized to an active metabolite known as trichloroethanol?
Chloral hydrate
What type of metabolism occurs before elimination for most sedative-hypnotic drugs?
Metabolism by hepatic enzymes
Which drug undergoes extrahepatic conjugation and does not form active metabolites?
Lorazepam
Which sedative-hypnotic drug has CNS effects terminated by rapid redistribution from brain to other highly perfused tissues, including skeletal muscle?
Thiopental
Which sedative-hypnotic drug has a duration of CNS action of more than 30 hours?
Diazepam
What receptor is located on the GABAA receptor molecule and is present in many brain regions, including the thalamus, limbic structures, and the cerebral cortex?
Benzodiazepine (BZ) receptors
What isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits?
α1β2γ2
What is the primary transmitter most associated with inhibition in the CNS?
GABA
Which drug undergoes even more rapid hepatic metabolism by aldehyde oxidase and cytochrome P450?
Zaleplon
Which sedative-hypnotic drug is also metabolized by cytochrome P450 with a half-life of 6 hours?
Eszopiclone
What effect do benzodiazepines have on GABA-mediated chloride ion channels?
Increase the frequency of channel opening
What type of receptors are coupled to potassium channels?
GABAB receptors
Study Notes
Metabolism of Sedative-Hypnotic Drugs
- Most sedative-hypnotic drugs undergo oxidative metabolism before elimination
- Oxidative metabolism occurs in the liver, primarily by cytochrome P450 enzymes
Characteristics of Sedative-Hypnotic Drugs
- Most sedative-hypnotic drugs are benzodiazepines
- Chloral hydrate is a sedative-hypnotic drug that enters the CNS rapidly and can be used as an induction agent in anesthesia
- Trichloroethanol is an active metabolite of chloral hydrate
Zolpidem
- Zolpidem is a sedative-hypnotic drug with a short duration of action due to its rapid hepatic metabolism
- Zolpidem is metabolized by aldehyde oxidase and cytochrome P450
Zaleplon
- Zaleplon is a sedative-hypnotic drug that undergoes rapid hepatic metabolism by aldehyde oxidase and cytochrome P450
- The enzyme responsible for the rapid hepatic metabolism of zaleplon is aldehyde oxidase
Eszopiclone
- Eszopiclone is a sedative-hypnotic drug with a half-life of 6 hours
GABAA Receptors
- The α1 subunit of the GABAA receptor is associated with sedative-hypnotic activity
- The GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits
- Benzodiazepines bind to the GABAA receptor, facilitating neuronal membrane inhibition
- The primary transmitter associated with inhibition in the CNS is GABA (gamma-aminobutyric acid)
Other Sedative-Hypnotic Drugs
- Flurazepam is a sedative-hypnotic drug with a duration of CNS action of more than 30 hours
- Chloral hydrate is a sedative-hypnotic drug that facilitates neuronal membrane inhibition by actions at specific receptors
Test your knowledge of sedative-hypnotic drugs, their lipid solubility, absorption, distribution to the brain, and CNS effects. Learn about the rapid onset of CNS action of drugs like thiopental, eszopiclone, and zaleplon.
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