IV Sed Hyp, GABA Agonists
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Questions and Answers

Which induction agent is known for its distinct antiemetic properties?

  • Ketamine
  • Propofol (correct)
  • Etomidate
  • Midazolam

    • What is the significant disadvantage of using etomidate, particularly as an infusion?

  • Adrenal suppression (correct)
  • Hypotension
  • Hyperactivity
  • Respiratory depression

    • Which drug provides unequaled cardiovascular stability as an induction agent?

  • Propofol
  • Midazolam
  • Ketamine
  • Etomidate (correct)

    • What are the five principal effects of benzodiazepines mentioned in the text?

    <p>Anxiolysis, sedation, anticonvulsant activity, skeletal muscle relaxation, and amnesia</p> Signup and view all the answers

    What is the primary action of barbiturates at the GABA A receptor?

    <p>Enhancing its affinity for GABA and directly activating the receptor at high doses</p> Signup and view all the answers

    Which setting is etomidate unlikely to be used in?

    <p>A patient in status epilepticus</p> Signup and view all the answers

    What effect does etomidate have on cerebral blood flow?

    <p>Maintained or improved cerebral perfusion pressure</p> Signup and view all the answers

    What is a potential side effect of etomidate induction?

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

    Which etomidate derivative may not inhibit steroidogenesis?

    <p>Methoxycarbonyletomidate (MOC)</p> Signup and view all the answers

    What is the unique structure of midazolam among benzodiazepines?

    <p>Substituted imidazole ring</p> Signup and view all the answers

    How do benzodiazepines act on the GABAA receptor?

    <p>Enhance the affinity of the GABAA receptors for GABA</p> Signup and view all the answers

    What is true regarding the metabolism of lorazepam?

    <p>Undergoes hepatic glucuronidation</p> Signup and view all the answers

    Which statement is true regarding age and midazolam requirement?

    <p>Decrease in requirement with age</p> Signup and view all the answers

    In what setting is etomidate NOT a useful induction agent?

    <p>Patients with a history of PONV</p> Signup and view all the answers

    What is the primary effect of benzodiazepine bound by GABAA receptor?

    <p>Increased opening of chloride channels</p> Signup and view all the answers

    What is a potential side effect of etomidate induction?

    <p>Myocardial infarction</p> Signup and view all the answers

    Which patient population requires a 25-50% reduction in dose of propofol?

    <p>Elderly patients</p> Signup and view all the answers

    What is the recommended dosing range of propofol for maintenance of anesthesia?

    <p>100-300 μg/kg/min</p> Signup and view all the answers

    Which clinical use of propofol is valued due to its rapid effect-site equilibration and short context-sensitive half-time?

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

    What is the bolus dose of propofol for postoperative nausea and vomiting?

    <p>10-15 mg</p> Signup and view all the answers

    What organ system effect does propofol have on intracranial pressure?

    <p>~30% decrease in ICP</p> Signup and view all the answers

    What is the effect of propofol on evoked potentials in the auditory system?

    <p>No effect</p> Signup and view all the answers

    Which cardiovascular effect is associated with propofol administration?

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

    In which patient population is propofol-induced hypotension more common?

    <p>Elderly patients</p> Signup and view all the answers

    What is the mechanism of neuroprotection associated with propofol?

    <p>Antioxidant activity and free radical scavenging</p> Signup and view all the answers

    What is the risk of bradycardic death associated with propofol?

    <p>~ 1%</p> Signup and view all the answers

    What is the mechanism of action of barbiturates at low concentrations?

    <p>Enhance the effect of GABA</p> Signup and view all the answers

    Which barbiturate became the preferred intravenous barbiturate due to its rapid onset and short duration?

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

    What is the main form of hepatic metabolism for barbiturates?

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

    In pharmacokinetics, what results in the termination of action of a bolus dose of barbiturates?

    <p>Redistribution of drug into the central circulation</p> Signup and view all the answers

    Which receptors do barbiturates also act at, in addition to GABAA and glutamate receptors?

    <p>Adenosine receptors</p> Signup and view all the answers

    Which barbiturate may lead to accumulation of the active metabolite pentobarbital at high doses?

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

    What is the main basis for recommending that barbiturates be avoided in porphyria?

    <p>Influence on hepatic microsomes</p> Signup and view all the answers

    What is the primary metabolite of midazolam?

    <p>1-hydroxymidazolam glucuronide</p> Signup and view all the answers

    Which drug inhibits the hepatic clearance of midazolam?

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

    Which benzodiazepine has a metabolism that is relatively unaffected by inhibition of cytochrome P-450 or changes in hepatic function?

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

    Which benzodiazepine has a lower lipid solubility resulting in a delayed onset of effect in the central nervous system (CNS)?

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

    In children, what is the recommended dosage range for oral premedication with midazolam?

    <p>0.25-1 mg/kg</p> Signup and view all the answers

    Which benzodiazepine is known for its reliable amnesia and slower onset compared to thiopental or propofol?

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

    What effect do benzodiazepines have on cerebral blood flow (CBF) and cerebral metabolic rate of oxygen (CMRO2)?

    <p>They decrease both CBF and CMRO2</p> Signup and view all the answers

    How does flumazenil work?

    <p>It prevents or reverses all effects of other benzodiazepines as a competitive antagonist</p> Signup and view all the answers

    What is a known use for flumazenil?

    <p>Reversal of residual benzodiazepine-induced sedation</p> Signup and view all the answers

    Which of the following is a potential cardiovascular effect of propofol?

    <p>Increased incidence of the oculocardiac reflex</p> Signup and view all the answers

    What is a potential respiratory effect of propofol?

    <p>Dose-dependent depression of ventilation</p> Signup and view all the answers

    Which of the following is a potential side effect of propofol?

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

    What is a distinguishing feature of Fospropofol (AQUAVAN) compared to propofol?

    <p>Lipid emulsion preparation</p> Signup and view all the answers

    What is a potential disadvantage associated with Fospropofol (AQUAVAN) administration?

    <p>Difficult titration</p> Signup and view all the answers

    What is a characteristic of etomidate's mechanism of action?

    <p>Enhances the affinity of the GABAA receptor for GABA</p> Signup and view all the answers

    Which statement accurately describes etomidate's pharmacokinetics?

    <p>Rapid clearance in the liver by ester hydrolysis</p> Signup and view all the answers

    What is an advantage of etomidate's preparation in a lipid emulsion?

    <p>No pain on injection</p> Signup and view all the answers

    What best describes the mechanism of action of etomidate?

    <p>Enhances the affinity of the GABAA receptor for GABA</p> Signup and view all the answers

    What is the dominant cardiovascular effect of ketamine in a patient with an intact autonomic nervous system and adequate catecholamine stores?

    <p>Hypertension and tachycardia</p> Signup and view all the answers

    Which anesthetic agent, as an adjunct to general anesthesia, markedly reduces MAC but is associated with a high incidence of bradycardia?

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

    Which of the following anesthetic agents is a GABA Agonist Sedative-Hypnotic?

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

    What is the preparation of propofol that requires the presence of a preservative to prevent bacterial growth?

    <p>Emulsion of 1% propofol, 10% soybean oil, 2.25% glycerol, and 1.2% purified egg phosphatide</p> Signup and view all the answers

    Which anesthetic agent has minimal hysteresis, rapid termination of action due to redistribution, and high clearance relative to other induction agents?

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

    What is the expected elimination half-life of propofol?

    <p>0.5-1.5 hours</p> Signup and view all the answers

    What is the primary clinical use for propofol?

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

    What is the recommended dosing for healthy adults for propofol induction of anesthesia?

    <p>1.5-2.5 mg/kg</p> Signup and view all the answers

    Study Notes

    Induction Agents and Their Properties

    • Ondansetron is an induction agent characterized by distinct antiemetic properties.
    • Etomidate's significant disadvantage includes suppression of steroidogenesis, impacting adrenal function during infusion.
    • Propofol provides unparalleled cardiovascular stability as an induction agent.

    Benzodiazepines and Their Mechanism

    • Five principal effects of benzodiazepines: anxiolysis, sedation, amnesia, muscle relaxation, and anticonvulsant effects.
    • Barbiturates primarily act at the GABA A receptor, enhancing inhibitory neurotransmission.
    • Benzodiazepines enhance the opening of GABAA receptor channels, increasing chloride influx.
    • Midazolam has a unique structure with a nitrogen atom in its ring, differentiating it among benzodiazepines.

    Metabolism and Dosage Considerations

    • Lorazepam's metabolism is primarily through conjugation, making it less affected by liver dysfunction.
    • Midazolam requirements decrease with age, as older patients typically need lower dosages.
    • Propofol infusion may require a 25-50% dose reduction in the elderly or those with compromised hepatic function.
    • Recommended dosing range for propofol maintenance of anesthesia is typically 100-200 mcg/kg/min.

    Propofol Properties and Effects

    • Propofol is valued for its rapid effect-site equilibration and short context-sensitive half-time.
    • A bolus dose of propofol for postoperative nausea and vomiting is usually around 10-20 mg.
    • Propofol decreases intracranial pressure and has a beneficial effect on auditory evoked potentials.
    • Propofol administration is associated with hypotension, especially in patients with compromised cardiovascular function.

    Barbiturates: Mechanisms and Risks

    • Barbiturates' low-concentration mechanism of action involves increasing duration of GABA A receptor activation.
    • Thiopental is the preferred intravenous barbiturate due to its rapid onset and short duration of effects.
    • Hepatic metabolism is the main pathway for barbiturates, primarily through oxidative processes.
    • Accumulation of pentobarbital may occur at high doses of its respective barbiturate.

    Respiratory and Cardiovascular Effects

    • Benzodiazepines reduce cerebral metabolic rate of oxygen (CMRO2) and cerebral blood flow (CBF).
    • Flumazenil acts as a benzodiazepine antagonist, reversing sedation effects; useful in overdose situations.
    • Propofol may cause respiratory depression and hypotension, but has a minimal effect on the central nervous system's excitability.

    Fospropofol Considerations

    • Fospropofol (AQUAVAN) is distinguished from propofol by being water-soluble and having a slower onset.
    • A potential disadvantage of Fospropofol includes the risk of delayed respiratory depression.

    Etomidate and Its Use

    • Etomidate's mechanism of action involves enhancing GABAergic transmission, providing rapid sedation without significant cardiovascular effects.
    • Unlikely to be used in emergency settings due to the potential risk of adrenal suppression.
    • The lipid emulsion formulation of etomidate aids in reducing pain on injection.

    Ketamine's Cardiovascular Effects

    • Ketamine exhibits dominant cardiovascular stimulation in patients with intact autonomic and catecholamine stores.

    Induction Dosage and Administration

    • Clinically, propofol has an expected elimination half-life of around 30-60 minutes post-infusion.
    • Recommended dosage for propofol induction in healthy adults ranges from 1.5-2.5 mg/kg.

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