Podcast
Questions and Answers
What is the main route of metabolism before elimination for sedative-hypnotic drugs?
What is the main route of metabolism before elimination for sedative-hypnotic drugs?
Which type of drugs are most sedative-hypnotic drugs?
Which type of drugs are most sedative-hypnotic drugs?
Which drug enters the CNS rapidly and can be used as an induction agent in anesthesia?
Which drug enters the CNS rapidly and can be used as an induction agent in anesthesia?
Which drug undergoes extrahepatic conjugation and does not form active metabolites?
Which drug undergoes extrahepatic conjugation and does not form active metabolites?
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Which drug is oxidized to an active metabolite known as trichloroethanol?
Which drug is oxidized to an active metabolite known as trichloroethanol?
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What is responsible for the short duration of action of zolpidem?
What is responsible for the short duration of action of zolpidem?
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Which enzyme is responsible for the rapid hepatic metabolism of zaleplon?
Which enzyme is responsible for the rapid hepatic metabolism of zaleplon?
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What is the half-life of eszopiclone?
What is the half-life of eszopiclone?
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Which receptor is most associated with inhibition in the CNS?
Which receptor is most associated with inhibition in the CNS?
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Which sedative-hypnotic drug has a duration of CNS action of more than 30 hours?
Which sedative-hypnotic drug has a duration of CNS action of more than 30 hours?
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What isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits?
What isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits?
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Which sedative-hypnotic drug facilitates neuronal membrane inhibition by actions at specific receptors?
Which sedative-hypnotic drug facilitates neuronal membrane inhibition by actions at specific receptors?
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Which neurotransmitter is most associated with inhibition in the CNS?
Which neurotransmitter is most associated with inhibition in the CNS?
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What type of receptors do benzodiazepines bind to?
What type of receptors do benzodiazepines bind to?
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What effect do benzodiazepines have on GABA-mediated chloride ion channels?
What effect do benzodiazepines have on GABA-mediated chloride ion channels?
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What is the primary transmitter associated with inhibition in the CNS?
What is the primary transmitter associated with inhibition in the CNS?
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Which sedative-hypnotic drug has the highest lipid solubility and can be used as an induction agent in anesthesia?
Which sedative-hypnotic drug has the highest lipid solubility and can be used as an induction agent in anesthesia?
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What is responsible for the short duration of action of zolpidem?
What is responsible for the short duration of action of zolpidem?
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Which sedative-hypnotic drug is oxidized to an active metabolite known as trichloroethanol?
Which sedative-hypnotic drug is oxidized to an active metabolite known as trichloroethanol?
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What type of metabolism occurs before elimination for most sedative-hypnotic drugs?
What type of metabolism occurs before elimination for most sedative-hypnotic drugs?
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Which drug undergoes extrahepatic conjugation and does not form active metabolites?
Which drug undergoes extrahepatic conjugation and does not form active metabolites?
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Which sedative-hypnotic drug has CNS effects terminated by rapid redistribution from brain to other highly perfused tissues, including skeletal muscle?
Which sedative-hypnotic drug has CNS effects terminated by rapid redistribution from brain to other highly perfused tissues, including skeletal muscle?
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Which sedative-hypnotic drug has a duration of CNS action of more than 30 hours?
Which sedative-hypnotic drug has a duration of CNS action of more than 30 hours?
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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?
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?
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What isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits?
What isoform of the GABAA receptor consists of 2 α1, 2 β2, and 1 γ2 subunits?
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What is the primary transmitter most associated with inhibition in the CNS?
What is the primary transmitter most associated with inhibition in the CNS?
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Which drug undergoes even more rapid hepatic metabolism by aldehyde oxidase and cytochrome P450?
Which drug undergoes even more rapid hepatic metabolism by aldehyde oxidase and cytochrome P450?
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Which sedative-hypnotic drug is also metabolized by cytochrome P450 with a half-life of 6 hours?
Which sedative-hypnotic drug is also metabolized by cytochrome P450 with a half-life of 6 hours?
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What effect do benzodiazepines have on GABA-mediated chloride ion channels?
What effect do benzodiazepines have on GABA-mediated chloride ion channels?
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What type of receptors are coupled to potassium channels?
What type of receptors are coupled to potassium channels?
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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
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Description
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.
