Pharmacology and Toxicology: Sedatives, Hypnotics, and CNS Stimulants
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Questions and Answers

What is the consequence of taking high doses of benzodiazepines?

  • Enhanced REM sleep
  • Coma and respiratory depression (correct)
  • Respiratory stimulation
  • Increased slow-wave sleep

    • What is the mechanism of action of benzodiazepines?

  • Activate GABA receptors without GABA presence
  • Directly hyperpolarize neuronal membranes
  • Inhibit GABA binding and decrease chloride channel opening
  • Bind to a BZ allosteric site and increase chloride channel opening (correct)

    • What is a characteristic of benzodiazepines compared to barbiturates?

  • They have no ceiling effect
  • They have a similar effect on sleep patterns
  • They have a greater margin of safety (correct)
  • They have a smaller margin of safety

    • What is the effect of benzodiazepines on sleep patterns?

    <p>They reduce slow-wave sleep and REM sleep</p> Signup and view all the answers

    What is a therapeutic use of benzodiazepines?

    <p>Short-term management of anxiety disorders</p> Signup and view all the answers

    What is a characteristic of oxazepam, temazepam, and lorazepam?

    <p>They are metabolized by phase II conjugation</p> Signup and view all the answers

    What is the mechanism of action of barbiturates?

    <p>They bind to an allosteric site on the GABA A receptor–chloride ion channel and increase the affinity of the receptor for GABA</p> Signup and view all the answers

    What is the main therapeutic use of thiopental?

    <p>Short IV anesthetic in short procedures</p> Signup and view all the answers

    What is a characteristic of barbiturates that distinguishes them from benzodiazepines?

    <p>They have a GABA-mimic action</p> Signup and view all the answers

    What is a contraindication for the use of barbiturates?

    <p>Acute intermittent porphyria</p> Signup and view all the answers

    What is a side effect of barbiturates?

    <p>Rebound insomnia after discontinuation</p> Signup and view all the answers

    What is the classification of phenobarbitone?

    <p>Long acting</p> Signup and view all the answers

    What is the use of phenobarbital in neonates?

    <p>Treatment of hyperbilirubinemia</p> Signup and view all the answers

    Why are barbiturates limited in their therapeutic use?

    <p>Due to their strong sedative effects</p> Signup and view all the answers

    Study Notes

    Sedatives, Hypnotics, and CNS Stimulants

    Barbiturates

    • Classification: Ultrashort acting (Thiopental), Short acting (Pentobarbitone), Long acting (Phenobarbitone)
    • Mechanism of Action: Bind to an allosteric site on the GABA A receptor–chloride ion channel, increasing the affinity of the receptor for GABA, opening chloride channel, and enhancing hyperpolarization of neurons
    • Therapeutic uses:
      • Anesthesia: Thiopental is used as a short IV anesthetic in short procedures
      • Anticonvulsant: Phenobarbital is used in the treatment of grand mal epilepsy
      • Neonatal jaundice: Phenobarbital is used in the treatment of hyperbilirubinemia in neonates (physiological jaundice)
    • Adverse effects:
      • Tolerance and dependence
      • Sedation and hangover effect
      • Rebound insomnia after discontinuation
      • Induce the rate-limiting enzyme in porphyrin biosynthesis, making them contraindicated in acute intermittent porphyria
      • Acute poisoning may occur at high doses, leading to coma and respiratory depression
    • Drug interactions: Microsomal enzyme inducers

    Benzodiazepines

    • Classification: Short acting (Triazolam, Midazolam), Intermediate acting (Temazepam, Lorazepam, Oxazepam), Long acting (Diazepam, Clonazepam)
    • Mechanism of Action: Bind to a BZ allosteric site, facilitating GABA binding and increasing the frequency of chloride channel opening, leading to neuronal membrane hyperpolarization
    • Characteristics:
      • Great margin of safety compared to barbiturates
      • Can produce anterograde amnesia, useful for stressful procedures
      • Reduce slow-wave sleep and REM sleep, disrupting sleep patterns
    • Pharmacokinetics:
      • Oxazepam, Temazepam, and Lorazepam are metabolized only by phase II conjugation, making them safer for elderly patients
    • Therapeutic uses:
      • Anxiety disorders: effective for short-term management

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    Description

    This quiz covers the classification and characteristics of sedatives, hypnotics, and CNS stimulants, including barbiturates, their uses, and effects.

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