GABA Agonists and Their Applications
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Questions and Answers

Which GABA receptor is an ion channel?

  • GABAb
  • GABAa (correct)
  • Both GABAb and GABAa
  • None of the above

    • Which GABA receptor is a GPCR?

  • GABAb (correct)
  • GABAa
  • Both GABAb and GABAa
  • None of the above

    • What type of channel is the GABA receptor?

    Cl- Channel

    Between barbiturates and benzodiazepines, which causes a bigger potentiation of GABA?

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

    To which drug class does phenobarbital belong?

    <p>GABAa Agonist (Barbiturate)</p> Signup and view all the answers

    What is the clinical use of phenobarbital?

    <p>Anti-convulsant</p> Signup and view all the answers

    What sort of half-life does phenobarbital have?

    <p>Very long (80-120 hours)</p> Signup and view all the answers

    How is phenobarbital administered?

    <p>Parenteral administration</p> Signup and view all the answers

    To which drug class does methohexital belong?

    <p>GABAa agonist (barbiturate)</p> Signup and view all the answers

    What is the clinical use of methohexital?

    <p>Pre-op sedation, Anesthesia for ECT</p> Signup and view all the answers

    What is the half-life of methohexital?

    <p>Short (3.5 minutes)</p> Signup and view all the answers

    To which drug class does etomidate belong?

    <p>GABAa agonist</p> Signup and view all the answers

    What is the clinical use of etomidate?

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

    What is the mechanism of action for etomidate?

    <p>Binds to the B3 subunit of GABAa to keep the channel open</p> Signup and view all the answers

    To which drug class does propofol belong?

    <p>GABAa agonist</p> Signup and view all the answers

    What are the clinical uses of propofol?

    <p>Preanesthetic, Anti-emetic</p> Signup and view all the answers

    What are the side effects of using propofol?

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

    What is the mechanism of action for propofol?

    <p>Binds to the B3 subunit of GABAa to keep it open</p> Signup and view all the answers

    Which anesthetic causes a unique euphoria?

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

    What is the half-life of propofol?

    <p>Short (1hr)</p> Signup and view all the answers

    To which drug class does meprobamate belong?

    <p>GABAa agonist</p> Signup and view all the answers

    What is the clinical use of meprobamate?

    <p>Approved anxiolytic but used as a sedative</p> Signup and view all the answers

    What are the effects of meprobamate overdose?

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

    What is the half-life of meprobamate?

    <p>6-17 hours</p> Signup and view all the answers

    What happens if you abruptly stop taking meprobamate?

    <p>Anxiety, insomnia, tremors, hallucinations and seizures</p> Signup and view all the answers

    To which drug class does carisoprodol belong?

    <p>GABAa agonist</p> Signup and view all the answers

    Which drug is an analogue of meprobamate?

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

    What is the clinical use of carisoprodol?

    <p>Muscle relaxant</p> Signup and view all the answers

    What happens if you abruptly stop using carisoprodol?

    <p>Anxiety, insomnia, tremors, hallucinations and seizures</p> Signup and view all the answers

    To which drug class does diazepam belong?

    <p>GABAa Agonist: BZ Anxiolytics</p> Signup and view all the answers

    What is the clinical use of diazepam?

    <p>Anxiolytic, Acute treatment of status epilepticus</p> Signup and view all the answers

    Which drug is used to treat status epilepticus?

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

    What two issues commonly seen with other BZ drugs are not seen with diazepam?

    <p>Lack of respiratory depression, Lack of synergy with ethanol</p> Signup and view all the answers

    To which drug class does clonazepam belong?

    <p>GABAa Agonist: BZ</p> Signup and view all the answers

    What is the clinical use of clonazepam?

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

    What is the half-life of clonazepam?

    <p>23 hours</p> Signup and view all the answers

    What is the half-life of diazepam?

    <p>20-80 hours (long)</p> Signup and view all the answers

    To which drug class does zolpidem belong?

    <p>GABAa Agonist: Non-BZ</p> Signup and view all the answers

    What is the clinical use of zolpidem?

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

    What is the half-life of zolpidem?

    <p>2.1 hours</p> Signup and view all the answers

    What is a result if you use a biphasic form of zolpidem?

    <p>Hangover effect but it will keep you asleep throughout the night</p> Signup and view all the answers

    What is the mechanism of action for zolpidem?

    <p>Selectively binds the a1 subunit</p> Signup and view all the answers

    Study Notes

    GABA Agonists Overview

    • GABAa receptors function as ion channels
    • GABAb receptors act as G protein-coupled receptors (GPCRs)
    • GABA receptor specifically facilitates Cl- ion flow

    Barbiturates vs Benzodiazepines

    • Barbiturates cause greater potentiation of GABA compared to benzodiazepines

    Phenobarbital

    • Classified as a GABAa agonist (barbiturate)
    • Acts as an anti-convulsant
    • Features a very long half-life of 80-120 hours
    • Administered parenterally

    Methohexital

    • Another GABAa agonist (barbiturate)
    • Used for pre-operative sedation and anesthesia for ECT
    • Exhibits a short half-life of about 3.5 minutes
    • Administered via IV

    Etomidate

    • GABAa agonist used primarily as a preanesthetic
    • Effective in decreasing intracranial pressure during brain injuries
    • Mechanism involves binding to the B3 subunit of GABAa to keep the channel open

    Propofol

    • Classified as a GABAa agonist
    • Used for pre-anesthesia and as an anti-emetic (unique feature among anesthetics)
    • Short half-life of 1 hour
    • Side effects include hypotension and respiratory depression
    • Induces a unique euphoric effect
    • Also binds to the B3 subunit of GABAa

    Meprobamate

    • GABAa agonist primarily used as a sedative
    • Known side effects of overdose include respiratory depression and severe hypotension
    • Half-life ranges from 6-17 hours
    • Abrupt cessation leads to anxiety, insomnia, tremors, hallucinations, and seizures

    Carisoprodol

    • A GABAa agonist analogue of meprobamate
    • Clinically used as a muscle relaxant
    • Similar withdrawal symptoms to meprobamate if stopped abruptly

    Benzodiazepines Overview

    • Diazepam is a GABAa agonist and classified as a BZ anxiolytic
    • Used as an anxiolytic and for acute status epilepticus treatment
    • Lack of respiratory depression and synergy with ethanol distinguishes it from other BZ drugs
    • Clonazepam, another GABAa agonist (BZ), serves as an anticonvulsant with a half-life of 23 hours
    • Diazepam has a long half-life between 20-80 hours

    Zolpidem

    • Non-benzodiazepine GABAa agonist used as a sedative
    • Exhibits a short half-life of 2.1 hours
    • A biphasic form may reduce hangover effects but promotes prolonged sleep
    • Mechanism of action involves selective binding to the a1 subunit of the GABAa receptor

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    Description

    Explore the diverse functions and applications of GABA agonists, including barbiturates and benzodiazepines. Learn about the mechanisms of action for various compounds like phenobarbital, methohexital, etomidate, and propofol. This quiz will test your knowledge on their therapeutic uses and pharmacokinetics.

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