Dental hypnotics
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Questions and Answers

Which receptor do barbiturates and benzodiazepines act on?

  • Acetylcholine receptor
  • GABA receptor (correct)
  • Serotonin receptor
  • Dopamine receptor

    • What does the GABAa ionophore regulate?

  • Sodium ion conductance
  • Potassium ion conductance
  • Calcium ion conductance
  • Chloride ion conductance (correct)

    • Which subunits can make up the GABA ionophore complex?

  • GABA and opioid receptors
  • GABA and serotonin receptors
  • GABA and benzodiazepine receptors (correct)
  • GABA ONLY

    • Where are the GABA and barbiturate receptors distributed throughout the CNS?

    <p>Differentially throughout the CNS</p> Signup and view all the answers

    Which neurotransmitter is GABA derived from?

    <p>Glutamate</p> Signup and view all the answers

    What blocks the chloride channel of GABA receptors?

    <p>Picrotoxin</p> Signup and view all the answers

    How is GABA's action terminated?

    <p>By uptake into presynaptic neuronal terminals and neighboring glial cells</p> Signup and view all the answers

    Which substance can interfere with GABA's action by blocking its binding?

    <p>Bicuculline</p> Signup and view all the answers

    What is the effect of bicuculline on GABA's action?

    <p>Reduces GABA's action</p> Signup and view all the answers

    Which neurotransmitter's action can be blocked by bicuculline?

    <p>GABA</p> Signup and view all the answers

    Which type of ligand for the benzodiazepine receptor produces sedative-hypnotic effects?

    <p>Agonists for the benzodiazepine receptor triazolam and diazepam</p> Signup and view all the answers

    Which ligand blocks the actions of benzodiazepines but not other sedatives/hypnotics?

    <p>Antagonists for the benzodiazepine receptor flumazenil</p> Signup and view all the answers

    Which ligand is an endogenous peptide that blocks the benzodiazepine receptor?

    <p>Diazepam binding inhibitor (DBI)</p> Signup and view all the answers

    Which ligand, derived from serotonin (5-HT) breakdown, produces anxiety reaction, proconvulsant activity, and seizures?

    <p>Inverse agonist for the benzodiazepine receptor beta-carbolines</p> Signup and view all the answers

    How many types of ligands are there for the benzodiazepine receptors?

    <p>3</p> Signup and view all the answers

    Which region of the brain is the most likely site for sedation and hypnotic action of benzodiazepines?

    <p>Brain stem</p> Signup and view all the answers

    What is the primary use of benzodiazepines?

    <p>As both sedatives-hypnotics and medication for anxiety and epilepsy</p> Signup and view all the answers

    Why do benzodiazepines have diverse actions in the brain?

    <p>They control different brain functions</p> Signup and view all the answers

    Which of the following is NOT a characteristic of benzodiazepines at the GABA synapse?

    <p>They increase the duration of the IPSP caused by GABA release</p> Signup and view all the answers

    What is the primary effect of benzodiazepines at the GABA synapse?

    <p>They enhance the action of GABA</p> Signup and view all the answers

    Which statement about benzodiazepines at the GABA synapse is true?

    <p>They have no activity in a GABA depleted system</p> Signup and view all the answers

    Which system does Benzodiazepines have minimal effects on in therapeutic doses?

    <p>All of the above</p> Signup and view all the answers

    Which drug is known to produce severe depression when combined with Benzodiazepines?

    <p>Alcohol</p> Signup and view all the answers

    Which class of drugs have lower dependence and abuse potential compared to Barbiturates?

    <p>Benzodiazepines</p> Signup and view all the answers

    Which cognitive effect can Benzodiazepines produce?

    <p>Motor incoordination</p> Signup and view all the answers

    Which of the following is a characteristic of barbiturates at the GABA synapse?

    <p>They release and block reuptake of GABA</p> Signup and view all the answers

    What is the effect of barbiturates on the duration of the chloride channel opening at the GABA synapse?

    <p>They increase the duration</p> Signup and view all the answers

    What is the primary effect of barbiturates at the GABA synapse?

    <p>They increase the duration of the IPSP caused by GABA release</p> Signup and view all the answers

    Which of the following is true about the metabolism of benzodiazepines?

    <p>Benzodiazepines have active metabolites that do not induce synthesis of liver microsomal enzymes.</p> Signup and view all the answers

    Which of the following effects do benzodiazepines have on the liver?

    <p>Benzodiazepines have no effect on the synthesis of liver microsomal enzymes.</p> Signup and view all the answers

    Which of the following is a general effect of Barbiturates?

    <p>Increased metabolism of other drugs</p> Signup and view all the answers

    What can happen when Barbiturates are used with other depressant agents?

    <p>Severe CNS depression</p> Signup and view all the answers

    Which of the following is true about the general and systemic effects of Barbiturates?

    <p>Barbiturates do not have any active metabolites.</p> Signup and view all the answers

    Which of the following is an advantage of benzodiazepines over barbiturates?

    <p>Benzodiazepines have a better therapeutic index</p> Signup and view all the answers

    Which of the following is NOT a characteristic of benzodiazepines in comparison with barbiturates?

    <p>They can produce seizures on withdrawal in epileptics</p> Signup and view all the answers

    What is an advantage of benzodiazepines over barbiturates in terms of withdrawal effects?

    <p>Benzodiazepines have reduced withdrawal effects</p> Signup and view all the answers

    Which type of insomnia is caused by a minor situational stress or jet lag?

    <p>Transient insomnia</p> Signup and view all the answers

    Which type of insomnia may be due to job loss or a death in the family?

    <p>Short-term insomnia</p> Signup and view all the answers

    What type of insomnia has no immediate or obvious cause and requires psychiatric evaluation?

    <p>Long-term insomnia</p> Signup and view all the answers

    Which type of insomnia is typically treated with a small dose of a rapidly eliminated hypnotic for 1-3 nights?

    <p>Insomnia caused by a minor situational stress or jet lag</p> Signup and view all the answers

    What is the recommended duration of treatment with a long-term hypnotic?

    <p>1 months</p> Signup and view all the answers

    What is the purpose of skipping the hypnotic drug for 1 or 2 nights during treatment?

    <p>To test if the patient can sleep without the drug</p> Signup and view all the answers

    Which benzodiazepine is recommended for use up to 42 days?

    <p>Triazolam</p> Signup and view all the answers

    Which benzodiazepine has been banned in the UK since 1991 due to high frequency of psychiatric side effects?

    <p>Triazolam</p> Signup and view all the answers

    Which benzodiazepine is more lipid soluble than Oxazepam?

    <p>Triazolam</p> Signup and view all the answers

    Which medication has a longer half-life, Zolpidem or Eszopiclone?

    <p>Eszopiclone</p> Signup and view all the answers

    Which medication is structurally unrelated to benzodiazepines?

    <p>Zolpidem</p> Signup and view all the answers

    Which medication has no anxiolytic properties?

    <p>Neither durgs have anxiolytic properties</p> Signup and view all the answers

    Which medication is FDA approved for long-term use? more than 42 days

    <p>Eszopiclone</p> Signup and view all the answers

    Which neurotransmitters does Amitriptyline block the reuptake of?

    <p>Serotonin (5-HT) and norepinephrine</p> Signup and view all the answers

    Which of the following drugs is mentioned as an antidepressant that is for blocking the reuptake of neurotransmitters such as serotonin and norepinephrine and is a sedative?

    <p>Amitriptyline</p> Signup and view all the answers

    Study Notes

    Barbiturates and Benzodiazepines

    • Barbiturates and benzodiazepines act on GABAa receptors.
    • The GABAa ionophore regulates chloride channels, influencing neuronal excitability.

    GABA Ionophore Complexity

    • GABA ionophore complex can consist of alpha, beta, gamma, delta, and rho subunits.
    • Distribution of GABA and barbiturate receptors is widespread throughout the central nervous system (CNS), affecting various brain regions.

    GABA Characteristics

    • GABA is derived from glutamate, serving as the main inhibitory neurotransmitter.
    • Certain substances, like picrotoxin, block the chloride channel of GABA receptors.
    • GABA's action is terminated primarily through reuptake by neurons or glial cells.

    Ligands and GABA Interaction

    • Flumazenil interferes with GABA's action by blocking its binding site on the receptor.
    • Bicuculline antagonizes GABA's action, leading to increased neuronal activity, and blocks GABA's neurotransmitter action.
    • Benzodiazepine receptors have two types of ligands: those producing sedative-hypnotic effects and antagonists like flumazenil.

    Sedative Effects

    • Sedative-hypnotic effects are produced by agonist ligands of the benzodiazepine receptor.
    • The brain region most associated with sedation and hypnotic effects of benzodiazepines is the hypothalamus.

    Medical Use and Effects

    • Benzodiazepines are primarily used for anxiety relief and insomnia treatment.
    • They exhibit diverse actions due to multiple receptor subtypes and their interaction with various neurotransmitter systems.

    Characteristics and Effects

    • Benzodiazepines enhance GABA's inhibitory effects, leading to anxiolytic and hypnotic action.
    • Minimal effects on the cardiovascular and respiratory systems at therapeutic doses.
    • Combining benzodiazepines with opioids can lead to severe depression.

    Barbiturates vs. Benzodiazepines

    • Barbiturates are associated with higher dependence and abuse potential compared to benzodiazepines.
    • Benzodiazepines can cause cognitive effects like amnesia and confusion.
    • Barbiturates increase the duration of chloride channel opening, leading to prolonged inhibition.

    Side Effects and Drug Interactions

    • Barbiturates pose risks when combined with other depressants, leading to compounded sedation.
    • Benzodiazepines have a more favorable withdrawal profile compared to barbiturates.

    Insomnia Types and Treatment

    • Acute insomnia may stem from minor stress or jet lag; treated with short-term hypnotics.
    • Adjustment insomnia may result from significant life changes; requires more thorough evaluation.
    • Chronic insomnia, lacking clear causes, may necessitate psychiatric intervention.

    Dosage Recommendations

    • Long-term hypnotic treatment should avoid continuous use beyond prescribed durations; breaks are recommended to prevent dependency.
    • Specific benzodiazepines like Lorazepam are suggested for short-term use (up to 42 days) due to their safety profile.

    Medications and Properties

    • Zolpidem and Eszopiclone differ in half-life, with Eszopiclone being longer lasting.
    • Non-benzodiazepine medications like Zaleplon, while effective as sleep aids, lack anxiolytic properties.
    • Amitriptyline is noted for its sedative effects due to serotonin and norepinephrine reuptake inhibition.

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    Description

    Test your knowledge of the GABA receptor and its role in the actions of barbiturates and benzodiazepines. Explore how these drugs interact with the GABAa ionophore and influence chloride ion conductance.

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