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Questions and Answers
What is a sedative drug also known as?
What is a sedative drug also known as?
Anxiolytic
Which of the following disorders are commonly managed using sedative drugs? (Select all that apply)
Which of the following disorders are commonly managed using sedative drugs? (Select all that apply)
A hypnotic drug produces drowsiness and facilitates sleep that resembles natural sleep.
A hypnotic drug produces drowsiness and facilitates sleep that resembles natural sleep.
True (A)
What neurotransmitter do Benzodiazepines promote the binding of?
What neurotransmitter do Benzodiazepines promote the binding of?
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Which of the following examples is NOT a Benzodiazepine?
Which of the following examples is NOT a Benzodiazepine?
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Benzodiazepines are __________ modulators of GABAA receptor function.
Benzodiazepines are __________ modulators of GABAA receptor function.
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All benzodiazepines are absorbed completely except clorazepate.
All benzodiazepines are absorbed completely except clorazepate.
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What is the primary mechanism by which Benzodiazepines affect GABAA receptors?
What is the primary mechanism by which Benzodiazepines affect GABAA receptors?
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Study Notes
Sedative-Hypnotic Drugs: Definitions and Differences
- Sedatives (also called anxiolytics) reduce activity and calm the patient; commonly used for anxiety (e.g., GAD, panic disorder, SAD, PTSD, OCD).
- Hypnotics induce drowsiness and sleep resembling natural sleep; involve stronger CNS depression than sedation; higher doses of sedative-hypnotics can achieve this effect.
Sedative-Hypnotics: Therapeutic Effects and CNS Depression
- Sedatives produce therapeutic effects at lower concentrations than those causing significant CNS depression.
- Benzodiazepine sedatives typically avoid generalized CNS depression (unlike older barbiturates, which can cause dose-dependent generalized depression potentially leading to death).
- Midazolam is an exception; it can decrease tidal volume and respiratory rate.
Benzodiazepines (BZDs): Mechanism of Action
- BZDs bind to the GABAA receptor, enhancing the binding of GABA (the major inhibitory neurotransmitter).
- Multiple mechanisms of action exist due to the involvement of distinct GABAA receptor subunits, leading to various effects (sedative-hypnotic, muscle relaxant, amnesic, anticonvulsant).
- BZDs are allosteric modulators; they increase Cl- conductance, hyperpolarizing neurons and reducing synaptic transmission by increasing the frequency of channel opening.
- GABA binds between α1 and β2 subunits of the GABAA receptor (which usually has 2α1, 2β2, and 1γ2 subunits), while BZDs bind between α1 and γ2 subunits.
- BZDs shift the GABA concentration-response curve to the left; they require GABA's presence to have an effect.
Benzodiazepines (BZDs): Examples
- “Azepam” group: Diazepam, Lorazepam, Clonazepam, Flurazepam, Oxazepam, Quazepam, Temazepam
- “Azolam” group: Midazolam, Alprazolam, Triazolam, Estazolam
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Chlordiazepoxide and Clorazepate are also examples.
Benzodiazepines (BZDs): Pharmacokinetics
- Except for clorazepate (a prodrug converted to nordiazepam in the stomach), all BZDs are completely absorbed.
- Oral absorption rate varies, influenced by lipophilicity; triazolam, diazepam, and nordiazepam are rapidly absorbed.
- Lipid solubility affects how quickly BZDs enter the CNS; highly lipophilic agents have rapid onset.
- Hepatic metabolism is responsible for clearing all BZDs, involving dealkylation (phase 1, mostly by CYP 3A4) and conjugation (phase 2).
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Description
This quiz covers the definitions and differences between sedatives and hypnotics, highlighting their therapeutic effects and mechanisms of action. It focuses on the role of benzodiazepines in the treatment of anxiety and sleep disorders while discussing the impacts of CNS depression.
