Pharmacology 1.3
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Questions and Answers

Which induction agent has distinct antiemetic properties?

  • Ketamine
  • Etomidate
  • Midazolam
  • Propofol (correct)

    • Which induction agent produces the greatest degree of hypotension and apnea?

  • Propofol (correct)
  • Ketamine
  • Midazolam
  • Etomidate

    • What is a significant disadvantage to the use of etomidate, particularly as an infusion?

  • Tachycardia
  • Hypertension
  • Adrenal suppression (correct)
  • Respiratory depression

    • Which drug produces a dissociative state and has intrinsic analgesic properties?

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

    Which of the following is a potential clinical feature of propofol infusion syndrome?

    <p>Severe, refractory bradycardia</p> Signup and view all the answers

    What is a potential effect of propofol on the respiratory system?

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

    What is a potential effect of propofol on the cardiovascular system?

    <p>May suppress SVT</p> Signup and view all the answers

    Which statement about fospropofol (AQUAVAN) is true?

    <p>It is a water-soluble prodrug rapidly metabolized by alkaline phosphatase in the blood and tissues.</p> Signup and view all the answers

    What is a potential disadvantage of fospropofol (AQUAVAN)?

    <p>Delayed systemic appearance of propofol from hydrolysis</p> Signup and view all the answers

    Which organ system effect may be observed during pediatric strabismus surgery with propofol anesthesia?

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

    Which statement about propofol infusion syndrome is true?

    <p>It may lead to skeletal myopathy</p> Signup and view all the answers

    What is a potential effect of propofol on the neuromuscular blockers?

    <p>No potentiation of the neuromuscular blockers</p> Signup and view all the answers

    Which organ system effect may be observed with propofol administration in patients with COPD?

    <p>May produce bronchodilation in COPD patients</p> Signup and view all the answers

    What is a potential recommendation for handling propofol?

    <p>Aseptic technique should be used when handling propofol</p> Signup and view all the answers

    What is a potential effect of propofol on pain perception during injection?

    <p>Pain on injection</p> Signup and view all the answers

    Which anesthetic agent is associated with a high incidence of bradycardia?

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

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

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

    What property is NOT included in the ideal anesthetic agent properties?

    <p>Long duration of action</p> Signup and view all the answers

    Which anesthetic agent's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane?

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

    Which anesthetic agent demonstrates rapid induction and more complete awakening than other induction agents?

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

    Which of the following is NOT a potential clinical feature of propofol infusion syndrome?

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

    What is a potential effect of propofol on the neuromuscular blockers?

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

    Which anesthetic agent's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane?

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

    What is a potential recommendation for handling propofol?

    <p>Discard opened ampule after 24 hours</p> Signup and view all the answers

    Which organ system effect may be observed with propofol administration in patients with COPD?

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

    What is a potential effect of propofol on pain perception during injection?

    <p>No pain on injection due to its unique formulation</p> Signup and view all the answers

    What is a potential disadvantage of fospropofol (AQUAVAN)?

    <p>Delayed systemic appearance of propofol from hydrolysis</p> Signup and view all the answers

    Which drug produces a dissociative state and has intrinsic analgesic properties?

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

    Which statement about fospropofol (AQUAVAN) is true?

    <p>It is rapidly metabolized by alkaline phosphatase in the blood</p> Signup and view all the answers

    What property is NOT included in the ideal anesthetic agent properties?

    <p>Potentiation of neuromuscular blockers</p> Signup and view all the answers

    Which of the following is a potential dosing range for maintenance of anesthesia with propofol?

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

    What is the recommended dosing for sedation with propofol?

    <p>25-100 $μg/kg/min$</p> Signup and view all the answers

    In which population is a 25-50% reduction in propofol dose recommended?

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

    What is the typical bolus dose for postoperative nausea and vomiting (N/V) in PACU with propofol?

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

    What is the dose of propofol recommended for effective treatment of neuraxial opioid-associated pruritis?

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

    What percentage decrease in intraocular pressure can be expected with propofol induction?

    <p>30-40%</p> Signup and view all the answers

    Which organ system effect may be observed following propofol administration in patients with COPD?

    <p>Arterial and venous vasodilation</p> Signup and view all the answers

    What effect does propofol have on the tachycardic response to hypotension?

    <p>Blunted response</p> Signup and view all the answers

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

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

    What is the approximate reduction in cerebral blood flow (CBF) that can be achieved with propofol?

    <p>30%</p> Signup and view all the answers

    Which induction drug has been shown to provide cerebral protection following incomplete ischemia when titrated to EEG burst suppression?

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

    What is the potential mechanism underlying the neuroprotective activity of propofol?

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

    Which anesthetic agent's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane?

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

    Which anesthetic agent is initially suspended in Cremaphor EL and now provided in an emulsion of propofol, soybean oil, glycerol, and purified egg phosphatide?

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

    Which anesthetic agent demonstrates rapid induction and more complete awakening than other induction agents?

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

    Which anesthetic agent's clearance exceeds hepatic blood flow and is eliminated by the kidneys with a prolonged half-life due to slow release from the peripheral compartment?

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

    Which anesthetic agent's pharmacokinetics are best described with a three-compartment model with very high clearance and a slow peripheral compartment?

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

    Which anesthetic agent is associated with a high incidence of bradycardia due to its inhibition of norepinephrine release from the locus coeruleus?

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

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

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

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

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

    What is the recommended dosing for sedation with propofol?

    <p>25-100 μg/kg/min</p> Signup and view all the answers

    In which condition is propofol as efficacious as ondansetron for reducing postoperative nausea and vomiting?

    <p>Chemotherapy related N/V</p> Signup and view all the answers

    What is the effect of propofol on intraocular pressure (IOP)?

    <p>$30-40% decrease</p> Signup and view all the answers

    What is the mechanism of propofol's anticonvulsant activity?

    <p>$\text{GABA receptors activation}$</p> Signup and view all the answers

    What effect does propofol have on cerebral metabolic rate of oxygen (CMRO2)?

    <p>$\text{~40% decrease}$</p> Signup and view all the answers

    Which organ system is directly affected by propofol-induced hypotension?

    <p>Cardiovascular system</p> Signup and view all the answers

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

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

    What is the primary mechanism behind the cardiovascular effects of propofol?

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

    Which benzodiazepine has a slower onset than thiopental or propofol but provides reliable amnesia?

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

    What is the primary route of clearance for midazolam?

    <p>Renal excretion</p> Signup and view all the answers

    Which benzodiazepine is insoluble in water and undergoes hepatic oxidative reduction?

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

    Which benzodiazepine has a lower lipid solubility resulting in delayed onset of CNS effects despite a higher affinity for GABA receptors?

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

    What are the principal pharmacologic effects of benzodiazepines?

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

    Which new ultra-short acting benzodiazepine has been submitted for FDA approval and shows a rapid loss of consciousness and a short context-sensitive half-time compared to midazolam?

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

    What is 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 pharmacokinetic characteristic of etomidate?

    <p>Best described by a three compartment model with high clearance</p> Signup and view all the answers

    What is a clinical use of etomidate?

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

    What preparation change has essentially eliminated pain and venous irritation associated with etomidate administration?

    <p>Preparation in a lipid emulsion</p> Signup and view all the answers

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

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

    Which anesthetic agent's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane?

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

    What is a potential effect of propofol on the neuromuscular blockers?

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

    Which organ system effect may be observed during pediatric strabismus surgery with propofol anesthesia?

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

    Which of the following is a potential clinical feature of propofol infusion syndrome?

    <p>Severe, refractory bradycardia</p> Signup and view all the answers

    What is a potential recommendation for handling propofol?

    <p>Avoid rapid bolus administration</p> Signup and view all the answers

    What is a potential disadvantage of fospropofol (AQUAVAN)?

    <p>Delayed systemic appearance of propofol from hydrolysis</p> Signup and view all the answers

    Which anesthetic agent produces a dissociative state and has intrinsic analgesic properties?

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

    What is the primary mechanism behind the cardiovascular effects of propofol?

    <p>May suppress SVT</p> Signup and view all the answers

    What is a potential effect of propofol on the cardiovascular system?

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

    What is a potential effect of propofol on the respiratory system?

    <p>$25-40%$ of apnea following induction</p> Signup and view all the answers

    Which statement about fospropofol (AQUAVAN) is true?

    <p>It has a rapid onset of action similar to propofol</p> Signup and view all the answers

    What is a potential recommendation for handling propofol?

    <p>$Aseptic$ technique</p> Signup and view all the answers

    Which drug produces the greatest degree of hypotension and apnea among the listed induction agents?

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

    What is a potential effect of propofol on the tachycardic response to hypotension?

    <p>Tachycardic response to atropine attenuated during propofol anesthesia</p> Signup and view all the answers

    What is a potential clinical feature of propofol infusion syndrome?

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

    Which anesthetic agent's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane?

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

    What is a significant disadvantage to the use of etomidate, particularly as an infusion?

    <p>Adrenal suppression</p> Signup and view all the answers

    What is a potential dosing range for maintenance of anesthesia with propofol?

    <p>$0.5-3.5 ext{mg/kg/hr}$</p> Signup and view all the answers

    Which organ system effect may be observed with propofol administration in patients with COPD?

    <p>May produce bronchodilation in COPD patients</p> Signup and view all the answers

    What is a potential effect of propofol on pain perception during injection?

    <p>Pain on injection</p> Signup and view all the answers

    What is a potential clinical feature associated with fospropofol (AQUAVAN)?

    <p>Metabolic acidosis</p> Signup and view all the answers

    What is the mechanism of action of etomidate?

    <p>Activates the GABAA receptor directly</p> Signup and view all the answers

    What is a potential clinical use of etomidate?

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

    What is a significant disadvantage to the use of propofol?

    <p>Potential for adrenocortical suppression</p> Signup and view all the answers

    What is a potential side effect associated with etomidate administration?

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

    Which of the following is a potential contraindication for using etomidate as an anesthetic agent?

    <p>Reactive airways disease</p> Signup and view all the answers

    What is a potential side effect of etomidate that may limit its use in certain patient populations?

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

    Which of the following is a potential advantage of using etomidate in patients with compromised cardiovascular function?

    <p>Minimal effects on baroreceptor function</p> Signup and view all the answers

    Which potential adverse effect limits the use of etomidate in patients with a history of seizure disorder?

    <p>Activation of epileptogenic foci</p> Signup and view all the answers

    What is the primary mechanism of action for benzodiazepines as anesthetic agents?

    <p>Activation of GABA receptors</p> Signup and view all the answers

    What factor determines the drug effect of benzodiazepines?

    <p>Receptor occupancy</p> Signup and view all the answers

    Which characteristic distinguishes midazolam from other benzodiazepines?

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

    What is a potential consequence of midazolam's hepatic oxidative hydroxylation?

    <p>Prolonged duration of action</p> Signup and view all the answers

    What distinguishes methoxycarbonyletomidate (MOC) from etomidate?

    <p>Lower myoclonus incidence</p> Signup and view all the answers

    What distinguishes carboetomidate from etomidate?

    <p>Greater adrenal suppression</p> Signup and view all the answers

    What distinguishes carboetomidate from methoxycarbonyletomidate (MOC)?

    <p>Greater adrenal suppression</p> Signup and view all the answers

    Which benzodiazepine has a slower onset than thiopental or propofol but provides reliable amnesia?

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

    What is the primary route of clearance for midazolam?

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

    Which benzodiazepine is insoluble in water and undergoes hepatic oxidative reduction?

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

    What is a potential effect of propofol on the cardiovascular system?

    <p>Decreased blood pressure</p> Signup and view all the answers

    What is the approximate reduction in cerebral blood flow (CBF) that can be achieved with propofol?

    <p>~50%</p> Signup and view all the answers

    Which anesthetic agent's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane?

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

    Which anesthetic agent is beneficial for patients with compromised cardiovascular status, questionable intravascular volume status, and elevated ICP?

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

    What effect does etomidate have on steroid synthesis?

    <p>It inhibits steroid synthesis</p> Signup and view all the answers

    Which side effect is associated with etomidate?

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

    What is the primary mechanism of benzodiazepines' effect on GABAA receptors?

    <p>Enhanced receptor affinity for GABA</p> Signup and view all the answers

    Which benzodiazepine has the highest clearance?

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

    What distinguishes methoxycarbonyletomidate (MOC) from etomidate?

    <p>It has a different chemical structure</p> Signup and view all the answers

    What is the primary route of clearance for midazolam?

    <p>Renal excretion</p> Signup and view all the answers

    Which benzodiazepine has a slower onset than thiopental or propofol but provides reliable amnesia?

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

    What distinguishes diazepam from other benzodiazepines in terms of metabolism?

    <p>Hepatic oxidative reduction</p> Signup and view all the answers

    What is the mechanism of action of flumazenil?

    <p>Benzodiazepine receptor ligand</p> Signup and view all the answers

    What characteristic distinguishes midazolam from lorazepam and diazepam in terms of metabolism?

    <p>Greater hepatic clearance</p> Signup and view all the answers

    What are the clinical uses of benzodiazepines?

    <p>Preoperative anxiolysis and IV sedation</p> Signup and view all the answers

    What are the pharmacologic effects of benzodiazepines?

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

    What distinguishes remimazolam from midazolam?

    <p>Ultra-short acting with rapid loss of consciousness compared to midazolam</p> Signup and view all the answers

    What is the dosing recommendation for flumazenil for reversal of benzodiazepine effects?

    <p>3.0 mg total dose</p> Signup and view all the answers

    What organ system effects are associated with propofol administration?

    <p>CNS, cardiovascular, respiratory, and musculoskeletal system effects</p> Signup and view all the answers

    What is the mechanism of action of flumazenil?

    <p>Antagonizes the effects of benzodiazepines at the GABAA receptor complex</p> Signup and view all the answers

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

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

    What was the first intravenous barbiturate introduced?

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

    Which barbiturate became the preferred intravenous barbiturate due to its rapid onset, short duration, and lack of excitatory effects?

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

    Who clinically used thiopental for the first time?

    <p>$Ralph$ Waters and John Lundy</p> Signup and view all the answers

    What is a known use of flumazenil?

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

    What is a characteristic feature of hexobarbital?

    <p>It saw a great deal of use in Europe, but not North America.</p> Signup and view all the answers

    When was thiopental first used clinically?

    <p>1930s</p> Signup and view all the answers

    What is the recommended dose of droperidol for antiemetic use?

    <p>10-20 μg/kg IV</p> Signup and view all the answers

    What is the management approach for central anticholinergic syndrome induced by scopolamine?

    <p>Physostigmine 15-60 μg/kg IV repeated at 1-2 hour intervals</p> Signup and view all the answers

    What is the primary current use of droperidol?

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

    What is the side effect associated with scopolamine administration that may interfere with drainage of aqueous humor?

    <p>Mydriasis and Cycloplegia</p> Signup and view all the answers

    What is the potential treatment for failure of thermoregulatory sweating caused by scopolamine or atropine fever?

    <p>$Physostigmine$ $15-60$ $rac{ ext{μg}}{ ext{kg}}$ $IV$ repeated at $1-2$ hour intervals</p> Signup and view all the answers

    What are the organ system effects of droperidol in terms of cardiovascular response?

    <p>Mild hypotension secondary to vasodilation with blockade of α2 receptors</p> Signup and view all the answers

    What is the mechanism behind the CNS depression caused by droperidol?

    <p>Submaximal inhibition of GABAA receptors and full inhibition of α2 -acetylcholine receptors, producing an imbalance between dopamine and acetylcholine</p> Signup and view all the answers

    What is a potential side effect associated with scopolamine administration that may lead to a wide range of symptoms from restlessness and hallucinations to somnolence and unconsciousness?

    <p>Central Anticholinergic Syndrome</p> Signup and view all the answers

    What is the primary mechanism of action of dexmedetomidine?

    <p>Agonism at alpha2 adrenergic receptors</p> Signup and view all the answers

    What is the primary site of analgesic action for dexmedetomidine?

    <p>Spinal cord</p> Signup and view all the answers

    What is the half-life of dexmedetomidine?

    <p>$2-3$ hours</p> Signup and view all the answers

    Which receptor does dexmedetomidine primarily agonize to produce hypotension and bradycardia?

    <p>Alpha2B adrenergic receptor</p> Signup and view all the answers

    What is the recommended dosing for pre-procedure sedation with dexmedetomidine intravenously?

    <p>$0.33 - 0.67 μg/kg IV 15$ minutes pre-procedure</p> Signup and view all the answers

    In which setting is dexmedetomidine a very useful tool for sedation during airway management?

    <p>$ ext{Difficult airway}$</p> Signup and view all the answers

    What is the primary effect of dexmedetomidine when used as an adjunct to general anesthesia?

    <p>Reduces MAC of isoflurane by $35-50 ext{%}$</p> Signup and view all the answers

    Which receptor does dexmedetomidine primarily agonize to produce vasoconstriction in the cerebral vessels?

    <p>Alpha1 adrenergic receptor</p> Signup and view all the answers

    What is the primary effect of dexmedetomidine on the neuroendocrine stress response to surgery?

    <p>Decreased release of cortisol, vasopressin, epi, NE</p> Signup and view all the answers

    What is the renal effect of dexmedetomidine?

    <p>Diuretic effect by opposing the action of vasopressin</p> Signup and view all the answers

    What is the most common subtype of porphyria?

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

    Which drug is NOT listed as a potential trigger for porphyria?

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

    What is the primary mechanism of action for ketamine?

    <p>Inhibition of NMDA receptors</p> Signup and view all the answers

    Which isomer of ketamine has approximately 4 times greater affinity for the phencyclidine binding site on NMDA receptor than the other?

    <p>S(+) ketamine</p> Signup and view all the answers

    What effect may be observed with chronic dosing of ketamine?

    <p>Tolerance due to downregulation of NMDA receptors</p> Signup and view all the answers

    What is a potential clinical use of ketamine at sub-anesthetic doses?

    <p>$0.2 - 0.5 mg/kg/hr$ infusion for analgesia</p> Signup and view all the answers

    What organ system effect may be observed with ketamine use?

    <p>$Decreased intracranial pressure$</p> Signup and view all the answers

    What is the primary route of clearance for ketamine?

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

    What is a potential side effect associated with ketamine use?

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

    What preparation is ketamine supplied in?

    <p>1%, 5%, and 10%</p> Signup and view all the answers

    Which receptor type does ketamine act as an antagonist at?

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

    What is the approximate duration of action for thiopental?

    <p>6-8 minutes</p> Signup and view all the answers

    What is the primary route of clearance for barbiturates like thiopental?

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

    Which effect has been observed at lower doses of methohexital in patients with existing seizure disorders?

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

    What is the approximate percentage decrease in cerebral metabolic rate of oxygen (CMRO2) achievable with barbiturates?

    <p>~40-50%</p> Signup and view all the answers

    Which cardiovascular effect is typically observed with barbiturates like thiopental?

    <p>Peripheral vasodilation with venous pooling</p> Signup and view all the answers

    What is a potential respiratory effect of barbiturate induction?

    <p>Decreased tidal volume</p> Signup and view all the answers

    Which receptor does ketamine primarily act on to induce sedation and hypnosis?

    <p>NMDA receptor</p> Signup and view all the answers

    What is the approximate duration of action following a single induction dose of ketamine?

    <p>10-20 minutes</p> Signup and view all the answers

    Which organ system effect may be observed with ketamine administration?

    <p>Increased systemic blood pressure</p> Signup and view all the answers

    What is the primary mechanism behind the cardiovascular effects of dexmedetomidine?

    <p>Inhibition of vagal outflow</p> Signup and view all the answers

    What is the primary route of clearance for dexmedetomidine?

    <p>$90 ext{%}$ renal excretion</p> Signup and view all the answers

    Which organ system effect may be observed with dexmedetomidine administration?

    <p>$10-20 ext{ minutes}$ duration of action</p> Signup and view all the answers

    What is a potential clinical use of dexmedetomidine?

    <p>Sedation in patients with acute bronchospasm</p> Signup and view all the answers

    What are the potential side effects associated with ketamine use?

    <p>Increased ICP and emergence reactions</p> Signup and view all the answers

    Which effect is NOT primarily associated with alpha-2A receptor stimulation by dexmedetomidine?

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

    What are the potential CNS effects associated with ketamine use?

    <p>Increased CMRO2</p> Signup and view all the answers

    What is a potential concern when using ketamine for induction in patients with known coronary artery disease?

    <p>Increased myocardial work and MVO2</p> Signup and view all the answers

    Which of the following is a potential trigger for Acute Intermittent Porphyria?

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

    What are the primary symptoms of porphyria?

    <p>Pain and skin changes</p> Signup and view all the answers

    Which sedative/hypnotic has a rapid onset of action and high lipid solubility?

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

    Which ketamine isomer has greater affinity for the phencyclidine binding site on the NMDA receptor?

    <p>$S(+) ketamine$</p> Signup and view all the answers

    What is the active metabolite produced when ketamine is metabolized by hepatic microsomal enzymes?

    <p>$Norketamine$</p> Signup and view all the answers

    Which receptor does ketamine affect in addition to NMDA receptors?

    <p>$Opioid receptors$</p> Signup and view all the answers

    What is a potential clinical use of ketamine at sub-anesthetic doses?

    <p>Analgesia for somatic pain</p> Signup and view all the answers

    What are some contraindications for barbiturates?

    <p>Severe cardiovascular instability and respiratory obstruction without secured airway</p> Signup and view all the answers

    What are some side effects associated with barbiturates?

    <p>Cardiovascular and respiratory side effects, with methohexital associated with excitatory phenomenon</p> Signup and view all the answers

    What are some uses of barbiturates other than sedation?

    <p>Lethal injections and truth serum, also abused and known by various street names</p> Signup and view all the answers

    Which of these drugs is a non-GABA agonist sedative/hypnotic?

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

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

    <p>Excitatory activity</p> Signup and view all the answers

    What is a potential benefit of using etomidate in patients with compromised cardiovascular function?

    <p>Minimal effects on the sympathetic nervous system</p> Signup and view all the answers

    What is a potential limitation for using etomidate in patients with a history of seizure disorder?

    <p>Activation of epileptogenic foci</p> Signup and view all the answers

    Which anesthetic agent has a much greater potency in inhibiting steroid synthesis than as a sedative-hypnotic?

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

    What distinguishes methoxycarbonyletomidate (MOC) from etomidate?

    <p>Similar hypnotic potency and reduced adrenal suppression</p> Signup and view all the answers

    What characteristic distinguishes midazolam from lorazepam and diazepam in terms of metabolism?

    <p>Hepatic oxidative hydroxylation and prolonged elimination in the elderly</p> Signup and view all the answers

    What is the primary mechanism of action for benzodiazepines as anesthetic agents?

    <p>Increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane</p> Signup and view all the answers

    What is a potential dosing range for maintenance of anesthesia with propofol?

    <p>2-3 mg/kg/hr</p> Signup and view all the answers

    What is the primary current use of droperidol?

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

    What is the approximate duration of amnesia and disorientation following return of consciousness caused by ketamine?

    <p>60-90 minutes</p> Signup and view all the answers

    Which of the following is a potential side effect of ketamine's cardiovascular effects?

    <p>Increased heart rate</p> Signup and view all the answers

    What is the primary mechanism of action of dexmedetomidine?

    <p>$\alpha2$ receptor agonism</p> Signup and view all the answers

    What is a potential side effect of ketamine's respiratory effects?

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

    What is the dosing range for ketamine used for induction of anesthesia?

    <p>$1-2 mg/kg$ IV</p> Signup and view all the answers

    Which personality type may be more susceptible to emergence reactions caused by ketamine?

    <p>Type A personality type</p> Signup and view all the answers

    What are the indications for ketamine induction?

    <p>Hemodynamic instability, active bronchospasm, lack of IV access</p> Signup and view all the answers

    What is the primary effect of ketamine on cerebral metabolic rate of oxygen consumption (CMRO2)?

    <p>Increased CMRO2</p> Signup and view all the answers

    Which receptor does dexmedetomidine primarily agonize to produce sympatholysis?

    <p>$\alpha2A$ receptor</p> Signup and view all the answers

    What are the clinical uses of ketamine?

    <p>Postoperative sedation, analgesia, and induction of anesthesia</p> Signup and view all the answers

    What is a potential side effect associated with ketamine administration?

    <p>Decreased platelet aggregation</p> Signup and view all the answers

    What distinguishes dexmedetomidine from medetomidine?

    <p>Non-selective receptor agonism vs highly specific $\alpha2A$ receptor agonism</p> Signup and view all the answers

    Study Notes

    Anesthetic Agents: Properties, Mechanisms, and Clinical Uses

    • Ketamine's dominant cardiovascular effect in a patient with an intact autonomic nervous system is hypertension and tachycardia
    • Dexmedetomidine inhibits release of norepinephrine from the locus coeruleus and is associated with a high incidence of bradycardia
    • Ideal anesthetic agent properties include drug compatibility, lack of pain on injection, rapid onset of hypnosis, and absence of postoperative complications
    • Most commonly used induction agents include propofol, etomidate, ketamine, and barbiturates
    • GABA agonist sedative-hypnotics include propofol, etomidate, benzodiazepines, and barbiturates
    • Propofol's mechanism of action involves increasing duration of GABA-activated opening of chloride channels and hyperpolarizing the postsynaptic cell membrane
    • Propofol is initially suspended in Cremaphor EL and now provided in an emulsion of propofol, soybean oil, glycerol, and purified egg phosphatide
    • Propofol decreases the rate of dissociation of GABA from the GABAA receptor and increases the duration of GABA-activated opening of chloride channels
    • Propofol's clearance exceeds hepatic blood flow and it is eliminated by the kidneys with a prolonged half-life due to slow release from the peripheral compartment
    • Propofol's pharmacokinetics are best described with a three-compartment model with very high clearance and a slow peripheral compartment
    • Clinical uses of propofol include rapid induction of anesthesia with dosing in healthy adults at 1.5-2.5 mg/kg for unconsciousness at 2-6 μg/ml
    • Propofol demonstrates rapid induction and more complete awakening than other induction agents

    Benzodiazepines: Pharmacokinetics and Clinical Uses

    • Midazolam has a rapid metabolism via hepatic oxidative hydroxylation and is primarily cleared by the kidneys, with potential accumulation in renal insufficiency.
    • Presence of drugs inhibiting cytochrome P-450 can delay midazolam metabolism, and its hepatic clearance is significantly greater than that of diazepam and lorazepam.
    • Diazepam is insoluble in water, so it is dissolved in organic solvents, and it undergoes hepatic oxidative reduction, with prolonged elimination half-time in cirrhosis due to decreased protein binding and hepatic blood flow.
    • Lorazepam is metabolized via hepatic glucuronidation to inactive metabolites, and its lower lipid solubility results in delayed onset of CNS effects despite a higher affinity for GABA receptors.
    • Benzodiazepines are clinically used for preoperative anxiolysis, IV sedation, induction and maintenance, and other uses such as termination of seizure activity and management of delirium tremens.
    • Midazolam dosing guidelines recommend 0.05-0.15 mg/kg for induction and 0.05 mg/kg maintenance, while lorazepam and diazepam have different dosing ranges for various indications.
    • Midazolam has a slower onset than thiopental or propofol but provides reliable amnesia, and its dose and onset are affected by premedication, anesthetic agents, ASA classification, and patient characteristics.
    • Benzodiazepines have five principal pharmacologic effects: anxiolysis, sedation, anticonvulsant, skeletal muscle relaxation, and amnesia.
    • Benzodiazepines have organ system effects on the CNS, cardiovascular, respiratory, and musculoskeletal systems, with implications for intracranial compliance, seizure management, blood pressure, and respiratory depression.
    • Remimazolam, a new ultra-short acting benzodiazepine, has been submitted for FDA approval and shows a rapid loss of consciousness and a short context-sensitive half-time compared to midazolam.
    • Flumazenil is a benzodiazepine receptor ligand with high receptor affinity, minimal intrinsic effect, and rapid clearance by hepatic microsomal enzymes, used for reversal of residual benzodiazepine-induced sedation and suspected benzodiazepine overdose.
    • Flumazenil is administered incrementally to a total dose of 3.0 mg for reversal of benzodiazepine effects, as it prevents or reverses all effects of other benzodiazepines in a dose-dependent manner.

    Benzodiazepines: Pharmacokinetics and Clinical Uses

    • Midazolam has a rapid metabolism via hepatic oxidative hydroxylation and is primarily cleared by the kidneys, with potential accumulation in renal insufficiency.
    • Presence of drugs inhibiting cytochrome P-450 can delay midazolam metabolism, and its hepatic clearance is significantly greater than that of diazepam and lorazepam.
    • Diazepam is insoluble in water, so it is dissolved in organic solvents, and it undergoes hepatic oxidative reduction, with prolonged elimination half-time in cirrhosis due to decreased protein binding and hepatic blood flow.
    • Lorazepam is metabolized via hepatic glucuronidation to inactive metabolites, and its lower lipid solubility results in delayed onset of CNS effects despite a higher affinity for GABA receptors.
    • Benzodiazepines are clinically used for preoperative anxiolysis, IV sedation, induction and maintenance, and other uses such as termination of seizure activity and management of delirium tremens.
    • Midazolam dosing guidelines recommend 0.05-0.15 mg/kg for induction and 0.05 mg/kg maintenance, while lorazepam and diazepam have different dosing ranges for various indications.
    • Midazolam has a slower onset than thiopental or propofol but provides reliable amnesia, and its dose and onset are affected by premedication, anesthetic agents, ASA classification, and patient characteristics.
    • Benzodiazepines have five principal pharmacologic effects: anxiolysis, sedation, anticonvulsant, skeletal muscle relaxation, and amnesia.
    • Benzodiazepines have organ system effects on the CNS, cardiovascular, respiratory, and musculoskeletal systems, with implications for intracranial compliance, seizure management, blood pressure, and respiratory depression.
    • Remimazolam, a new ultra-short acting benzodiazepine, has been submitted for FDA approval and shows a rapid loss of consciousness and a short context-sensitive half-time compared to midazolam.
    • Flumazenil is a benzodiazepine receptor ligand with high receptor affinity, minimal intrinsic effect, and rapid clearance by hepatic microsomal enzymes, used for reversal of residual benzodiazepine-induced sedation and suspected benzodiazepine overdose.
    • Flumazenil is administered incrementally to a total dose of 3.0 mg for reversal of benzodiazepine effects, as it prevents or reverses all effects of other benzodiazepines in a dose-dependent manner.

    Benzodiazepines: Pharmacokinetics and Clinical Uses

    • Midazolam has a rapid metabolism via hepatic oxidative hydroxylation and is primarily cleared by the kidneys, with potential accumulation in renal insufficiency.
    • Presence of drugs inhibiting cytochrome P-450 can delay midazolam metabolism, and its hepatic clearance is significantly greater than that of diazepam and lorazepam.
    • Diazepam is insoluble in water, so it is dissolved in organic solvents, and it undergoes hepatic oxidative reduction, with prolonged elimination half-time in cirrhosis due to decreased protein binding and hepatic blood flow.
    • Lorazepam is metabolized via hepatic glucuronidation to inactive metabolites, and its lower lipid solubility results in delayed onset of CNS effects despite a higher affinity for GABA receptors.
    • Benzodiazepines are clinically used for preoperative anxiolysis, IV sedation, induction and maintenance, and other uses such as termination of seizure activity and management of delirium tremens.
    • Midazolam dosing guidelines recommend 0.05-0.15 mg/kg for induction and 0.05 mg/kg maintenance, while lorazepam and diazepam have different dosing ranges for various indications.
    • Midazolam has a slower onset than thiopental or propofol but provides reliable amnesia, and its dose and onset are affected by premedication, anesthetic agents, ASA classification, and patient characteristics.
    • Benzodiazepines have five principal pharmacologic effects: anxiolysis, sedation, anticonvulsant, skeletal muscle relaxation, and amnesia.
    • Benzodiazepines have organ system effects on the CNS, cardiovascular, respiratory, and musculoskeletal systems, with implications for intracranial compliance, seizure management, blood pressure, and respiratory depression.
    • Remimazolam, a new ultra-short acting benzodiazepine, has been submitted for FDA approval and shows a rapid loss of consciousness and a short context-sensitive half-time compared to midazolam.
    • Flumazenil is a benzodiazepine receptor ligand with high receptor affinity, minimal intrinsic effect, and rapid clearance by hepatic microsomal enzymes, used for reversal of residual benzodiazepine-induced sedation and suspected benzodiazepine overdose.
    • Flumazenil is administered incrementally to a total dose of 3.0 mg for reversal of benzodiazepine effects, as it prevents or reverses all effects of other benzodiazepines in a dose-dependent manner.

    Intravenous Anesthetic Agents: Etomidate and Benzodiazepines

    • Etomidate has a dosage of 4 mg/kg and is beneficial for patients with compromised cardiovascular status, questionable intravascular volume status, elevated ICP, electroconvulsive therapy, mapping of epileptogenic foci, and maintenance of anesthesia.
    • Etomidate may not be suitable for patients with a history of seizure disorder due to its activation of epileptogenic foci and amplification of SSEP signal.
    • Etomidate has minimal effects on the sympathetic nervous system and baroreceptor function, making it useful in patients with poor cardiovascular function and settings where any reduction in blood pressure may be significant.
    • Etomidate induces less depression of ventilation compared to other induction agents and is safe to use in patients with reactive airways disease.
    • Etomidate has a much greater potency (20x) in inhibiting steroid synthesis than as a sedative-hypnotic, leading to suppression of adrenal steroidogenesis and cortisol production for up to 72 hours.
    • Side effects of etomidate include excitatory activity, myoclonus, pain on injection, and high incidence of postoperative nausea and vomiting (PONV).
    • Methoxycarbonyletomidate (MOC) and carboetomidate are potential etomidate derivatives with similar hypnotic potency and reduced adrenal suppression.
    • Midazolam, a benzodiazepine, has a unique structure with a substituted imidazole ring and is lipid-soluble.
    • Benzodiazepines enhance the affinity of the GABAA receptors for GABA, resulting in increased chloride conductance and hyperpolarization of the postsynaptic cell membrane.
    • The drug effect of benzodiazepines is a function of receptor occupancy, with less than 20% occupancy leading to anxiolysis and over 60% leading to unconsciousness.
    • Benzodiazepines are highly protein bound, with Lorazepam having slightly greater volume of distribution despite lower lipid solubility, and Midazolam having the highest clearance.
    • Midazolam undergoes hepatic oxidative hydroxylation and has a rapid onset, short duration, and high hepatic clearance, with prolonged elimination in the elderly due to decreased hepatic blood flow and enzyme activity.

    Ketamine and Dexmedetomidine: Pharmacology and Clinical Uses

    • Ketamine dosed at 1-3 μg/kg/min IV infusion for postoperative sedation and analgesia
    • Ketamine used for induction of anesthesia with dosing at 1-2 mg/kg IV and 4-8 mg/kg IM
    • Indications for ketamine induction include hemodynamic instability, active bronchospasm, and lack of IV access
    • Ketamine may produce amnesia and disorientation for 60-90 minutes following return of consciousness
    • Ketamine's effects on the CNS include functional disorganization of midbrain and thalamic pathways
    • Ketamine is associated with increased cerebral metabolic rate of oxygen consumption (CMRO2) and intracranial pressure (ICP)
    • Ketamine may lead to emergence reactions in 10-30% of adults, with certain personality types being more susceptible
    • Ketamine's cardiovascular effects include increased systemic blood pressure and heart rate
    • Ketamine has minimal effect on respiratory drive and may cause increased salivation and bronchodilation
    • Side effects of ketamine include emergence delirium and inhibition of platelet aggregation
    • Dexmedetomidine is the S-enantiomer of medetomidine, a highly specific α2 receptor agonist
    • Dexmedetomidine's mechanism of action includes sedation, sympatholysis, analgesia, and neuroprotection through α2 receptor agonism

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    Description

    Test your knowledge of anesthesia dosing variables with this quiz. Explore how different factors such as age, weight, and gender can impact the dosing of anesthesia for maintaining anesthesia and achieving rapid awakening.

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