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GABAA Receptor Subtypes and Addiction
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GABAA Receptor Subtypes and Addiction

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Questions and Answers

What is the primary goal of adjusting the dosage of midazolam in heart surgery patients?

  • To assess the efficacy of melatonin in benzodiazepine abuse
  • To consider pharmacokinetic differences in sedation management (correct)
  • To manage post-operative nausea and vomiting
  • To improve perioperative analgesia
  • Which type of GABA receptors is associated with the functional significance of zolpidem?

  • β2-containing GABA(B) receptors
  • α2-containing GABA(A) receptors
  • α1-containing GABA(A) receptors (correct)
  • γ2-containing GABA(C) receptors
  • What is the primary application of midazolam in pediatric neurosurgery?

  • As a prophylactic antiemetic
  • As a post-operative sedative
  • As an oral premedicant (correct)
  • As an intrathecal analgesic
  • What is the effect of midazolam on excitatory transmission in dorsal horn neurons?

    <p>Inhibits excitatory transmission</p> Signup and view all the answers

    What is the benefit of using midazolam in middle ear surgery?

    <p>Reduces post-operative nausea and vomiting</p> Signup and view all the answers

    What is the primary mechanism of action of midazolam on GABA receptors?

    <p>Binding to α1β2γ2S subunits</p> Signup and view all the answers

    What is the primary application of intrathecal midazolam?

    <p>To improve perioperative analgesia</p> Signup and view all the answers

    What is the primary goal of using melatonin in benzodiazepine abuse?

    <p>To curtail benzodiazepine abuse</p> Signup and view all the answers

    What is the effect of age on the clearance of cytochrome P450 3A substrates, such as benzodiazepines?

    <p>Decreased clearance with age</p> Signup and view all the answers

    What is the primary mechanism of action of benzodiazepines on GABA receptors?

    <p>Allosteric agonism</p> Signup and view all the answers

    Which of the following is a characteristic of remimazolam, a benzodiazepine used for sedation?

    <p>Short-acting sedative</p> Signup and view all the answers

    What is the effect of obesity on the distribution and clearance of benzodiazepines?

    <p>Decreased clearance in obese individuals</p> Signup and view all the answers

    Which GABA receptor subtype is selectively antagonized by FG-7,142?

    <p>α1β2γ2L</p> Signup and view all the answers

    What is the primary indication for midazolam in pediatric anesthesia?

    <p>Induction of anesthesia in neonates</p> Signup and view all the answers

    Which of the following is a potential side effect of benzodiazepine administration?

    <p>Respiratory depression</p> Signup and view all the answers

    What is the primary target for pharmacological modulation of benzodiazepine effects?

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

    What is the characteristic of midazolam's plasma protein binding?

    <p>Concentration-independent</p> Signup and view all the answers

    Which receptor is inhibited by midazolam, leading to reduced endothelial activation?

    <p>Peripheral-type benzodiazepine receptor</p> Signup and view all the answers

    What is the advantage of using intravenous propofol alone compared to intravenous propofol with oral midazolam premedication for deep sedation during endoscopic retrograde cholangiopancreatography?

    <p>Reduced risk of respiratory depression</p> Signup and view all the answers

    Why may elderly long-term benzodiazepine users experience increased postoperative confusion?

    <p>Due to the increased sensitivity to the drug's effects</p> Signup and view all the answers

    What is the benefit of using anticonvulsant therapy for status epilepticus?

    <p>Increased efficacy in treating seizures</p> Signup and view all the answers

    What is the characteristic of midazolam's pharmacokinetics in children?

    <p>Increased clearance</p> Signup and view all the answers

    What is the implication of midazolam's pharmacokinetics for sedation management?

    <p>Adjustment of dosage may be required</p> Signup and view all the answers

    What is the role of the peripheral-type benzodiazepine receptor in the cardiovascular system?

    <p>Involvement in endothelial activation</p> Signup and view all the answers

    Study Notes

    GABAA Receptor Subtypes and Addiction

    • GABAA receptors have various subtypes, including α1-containing receptors, which play a crucial role in addiction.
    • The behavioral pharmacology of zolpidem suggests that α1-containing GABAA receptors are functionally significant.

    Midazolam and GABAA Receptors

    • Midazolam interacts with α1β2γ2L and α1β2γ2S GABAA receptors expressed in human embryonic kidney cells.
    • Midazolam's actions on excitatory transmission in dorsal horn neurons of adult rat spinal cord are important for its pharmacological effects.

    Pharmacokinetics and Pharmacodynamics of Midazolam

    • Midazolam's pharmacokinetics are influenced by age, sex, and disease, particularly in neonates and children.
    • The clearance of midazolam is affected by cytochrome P450 3A substrates and obesity.
    • The plasma protein binding of midazolam is concentration-independent.

    Clinical Applications of Midazolam

    • Midazolam is used as a sedative in various medical procedures, including heart surgery, pediatric neurosurgery, and upper gastrointestinal endoscopy.
    • Midazolam has been used to curtail benzodiazepine/Z drug abuse and has been investigated as a potential treatment for addiction.
    • Midazolam's anticonvulsant properties make it useful for the treatment of status epilepticus.

    Adverse Effects of Midazolam

    • Long-term use of midazolam can lead to postoperative confusion, particularly in elderly patients.
    • Withdrawal symptoms can occur in critically ill children after long-term administration of midazolam and other sedatives/analgesics.

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    Description

    This quiz covers the relation between GABAA receptor subtypes and addiction, including pharmacokinetic considerations and behavioral pharmacology. It also explores the functional significance of α1-containing GABAA receptors.

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