Chapter 5: IV Anesthetics
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Questions and Answers

Which medication has minimal detrimental effects when accidentally injected into an artery?

  • Etomidate (correct)
  • Barbiturates
  • Propofol
  • Benzodiazepines
  • Which medication may stimulate ventilation independent of medullary centers?

  • Benzodiazepines
  • Etomidate (correct)
  • Propofol
  • Barbiturates
  • Which medication is effective for acute insomnia but may lead to cognitive problems and mortality?

  • Etomidate
  • Propofol
  • Barbiturates
  • Benzodiazepines (correct)
  • Which medication has a built-in ceiling effect, preventing it from exceeding the physiologic maximum of GABA inhibition?

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

    Which medication may accelerate cognitive decline in elderly patients and inhibit platelet aggregation in aging and liver disease?

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

    Which medication can lead to adrenocortical suppression for 4 to 8 hours after an induction dose?

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

    What is the recommended pediatric dosing for midazolam for induction of anesthesia?

    <p>1 - 2.5 mg IV</p> Signup and view all the answers

    How is diazepam metabolized in the body?

    <p>Oxidative N-demethylation</p> Signup and view all the answers

    What is the elimination half-time of diazepam in healthy volunteers?

    <p>$21 - 37$ hrs.</p> Signup and view all the answers

    How does midazolam affect blood pressure and heart rate?

    <p>Decrease in BP &amp; increase in HR</p> Signup and view all the answers

    What is the commercial preparation of diazepam dissolved in?

    <p>Propylene glycol and Sodium benzoate</p> Signup and view all the answers

    What is the peak effect onset time for intravenous sedation with midazolam?

    <p>$30 - 60$ seconds</p> Signup and view all the answers

    What is the plasma concentration at which awakening occurs in children and the elderly when using propofol for induction of anesthesia?

    <p>1.0 to 1.5 𝜇/mL</p> Signup and view all the answers

    What effect does propofol have on cerebral blood flow?

    <p>Decreases cerebral blood flow</p> Signup and view all the answers

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

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

    How does propofol affect hepatic or renal function?

    <p>Does not affect hepatic or renal function</p> Signup and view all the answers

    What is a potential risk associated with prolonged infusions of propofol?

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

    Which adverse event is most commonly reported with propofol?

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

    What is a potential trigger for allergic reactions to propofol?

    <p>Phenyl nucleus</p> Signup and view all the answers

    Which organ system does propofol affect?

    <p>Intraocular pressure</p> Signup and view all the answers

    What is the mechanism of action of etomidate?

    <p>Selective modulation of GABAA receptors</p> Signup and view all the answers

    What is a characteristic effect of etomidate on ICP (intracranial pressure)?

    <p>Decreases ICP</p> Signup and view all the answers

    Which drug induces a state of calm or sleep?

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

    What is the chemical structure of Propofol?

    <p>$2,6$-diisopropyl phenol</p> Signup and view all the answers

    What risk is associated with mixing lidocaine and propofol?

    <p>Pulmonary embolism</p> Signup and view all the answers

    Which propofol alternative has a higher pain on injection?

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

    What is the main concern with Aquavan and fospropofol?

    <p>Risk of infection</p> Signup and view all the answers

    What is the function of Sedatives?

    <p>Induce a state of calm or sleep</p> Signup and view all the answers

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

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

    What is the mechanism of action of etomidate?

    <p>Selective modulation of GABAA receptors</p> Signup and view all the answers

    Which adverse event is most commonly reported with propofol?

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

    Which organ system does propofol affect?

    <p>Intraocular pressure and coagulation</p> Signup and view all the answers

    What is a potential trigger for allergic reactions to propofol?

    <p>Phenyl nucleus and diisopropyl side chain</p> Signup and view all the answers

    What risk is associated with mixing lidocaine and propofol?

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

    Which medication has minimal detrimental effects when accidentally injected into an artery?

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

    Which medication may accelerate cognitive decline in elderly patients and inhibit platelet aggregation in aging and liver disease?

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

    Which medication has a built-in ceiling effect, preventing it from exceeding the physiologic maximum of GABA inhibition?

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

    Which medication is effective for acute insomnia but may lead to cognitive problems and mortality?

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

    What risk is associated with mixing lidocaine and propofol?

    <p>Allergic reaction</p> Signup and view all the answers

    What is a characteristic effect of etomidate on ICP (intracranial pressure)?

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

    What is the recommended timing for administering midazolam before surgery?

    <p>20 minutes before surgery</p> Signup and view all the answers

    What is the onset time for intravenous sedation with midazolam?

    <p>30 - 60 seconds</p> Signup and view all the answers

    How is diazepam metabolized in the body?

    <p>Oxidative N-demethylation</p> Signup and view all the answers

    What is the elimination half-time of diazepam in healthy volunteers?

    <p>$21 - 37$ hours</p> Signup and view all the answers

    What is the commercial preparation of diazepam dissolved in?

    <p>Organic solvents (propylene glycol, sodium benzoate)</p> Signup and view all the answers

    Which medication has a longer elimination half-time than lorazepam but shorter duration of action?

    <p>$\text{Diazepam}$</p> Signup and view all the answers

    What is the plasma concentration at which awakening occurs in children and the elderly when using propofol for induction of anesthesia?

    <p>1.0 to 1.5 𝜇/mL</p> Signup and view all the answers

    What is one of the non-hypnotic therapeutic applications of propofol?

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

    What effect does propofol have on cerebral blood flow?

    <p>Decreases cerebral blood flow</p> Signup and view all the answers

    What risk is associated with mixing lidocaine and propofol?

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

    How does propofol affect hepatic or renal function?

    <p>Does not affect hepatic or renal function</p> Signup and view all the answers

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

    <p>Inhibits sympathetic vasoconstrictor nerve activity</p> Signup and view all the answers

    What is the chemical structure of Propofol?

    <p>2,6-diisopropyl phenol</p> Signup and view all the answers

    Which organ system does propofol affect?

    <p>Central Nervous System</p> Signup and view all the answers

    What is a potential risk associated with mixing lidocaine and propofol?

    <p>Pulmonary embolism</p> Signup and view all the answers

    What is the alternative to Propofol that has a higher pain on injection?

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

    What is the function of Anxiolytics?

    <p>To reduce anxiety</p> Signup and view all the answers

    What is the primary component in Propofol's formulation that supports bacterial growth and increases triglycerides with prolonged infusion?

    <p>Soybean oil</p> Signup and view all the answers

    What is the primary characteristic of dissociative anesthesia produced by ketamine?

    <p>Eyes remain open with slow nystagmic gaze</p> Signup and view all the answers

    What is the main limitation of ketamine as a sole anesthetic agent?

    <p>Frequency of emergence delirium</p> Signup and view all the answers

    What is the structure-activity relationship of ketamine?

    <p>Water soluble molecule resembling phencyclidine</p> Signup and view all the answers

    Which isomer of ketamine is used for treatment resistant depression?

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

    What type of anesthesia does ketamine produce?

    <p>&quot;Dissociative anesthesia&quot;</p> Signup and view all the answers

    What risk limits the clinical usefulness of ketamine as a sole anesthetic agent?

    <p>Frequency of emergence delirium</p> Signup and view all the answers

    Which molecule does ketamine structurally resemble?

    <p>Phencyclidine (angel dust)</p> Signup and view all the answers

    What characterizes the patient's state during dissociative anesthesia produced by ketamine?

    <p>Noncommunicative with open eyes and slow nystagmic gaze</p> Signup and view all the answers

    What distinguishes the S(+) isomer of ketamine from the R (-) isomer?

    <p>It is used for treatment resistant depression (Spravato)</p> Signup and view all the answers

    What distinguishes dissociative anesthesia from other types of anesthesia produced by ketamine?

    <p>Evidence on EEG of dissociation between thalamocortical and limbic systems</p> Signup and view all the answers

    What is the mechanism of action of ketamine-induced analgesia and dissociative anesthesia?

    <p>Binding to N-methyl-D-aspartate receptors and exerting effects at other sites</p> Signup and view all the answers

    What is a clinical use of ketamine?

    <p>Managing postoperative pain</p> Signup and view all the answers

    What effect does chronic administration of ketamine have on enzyme activity?

    <p>Enzyme induction and tolerance</p> Signup and view all the answers

    What is a potential adverse effect of ketamine on the cardiovascular system?

    <p>Causes tissue damage</p> Signup and view all the answers

    How does subanesthetic doses of ketamine affect opioid tolerance?

    <p>Reduces opioid tolerance</p> Signup and view all the answers

    What is a potential approach for preventing emergence delirium caused by ketamine?

    <p>The use of benzodiazepines preoperatively</p> Signup and view all the answers

    What is a characteristic of ketamine's metabolism by cytochrome P450?

    <p>Forms a metabolite that is less potent than ketamine</p> Signup and view all the answers

    What is a potential application for ketamine induction of anesthesia?

    <p>Burn patients and pediatrics</p> Signup and view all the answers

    What is the pharmacokinetic characteristic of ketamine's volume of distribution?

    <p>Large volume of distribution due to high lipid solubility</p> Signup and view all the answers

    What is a potential effect of subanesthetic doses of ketamine on psychiatric disorders?

    <p>Improvement in psychiatric disorders</p> Signup and view all the answers

    Which drug is considered the 'Gold Standard' in anesthesia and was introduced in 1934?

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

    What is a key risk factor for dreams and hallucinations occurring up to 24 hours after administration of ketamine?

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

    What is a potential side effect of barbiturates?

    <p>Enhanced action of NMBD’s</p> Signup and view all the answers

    Which drug is a highly selective alpha-2 adrenergic agonist and is used to calm patients and reduce the hemodynamic response to tracheal intubation?

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

    What is a use of thiopental in clinical practice?

    <p>Induction of anesthesia, increased intracranial pressure, and ischemic injury</p> Signup and view all the answers

    What can intra-arterial injection of thiopental cause?

    <p>Vasoconstriction, pain, gangrene, and permanent damage</p> Signup and view all the answers

    What is a potential allergic reaction that can occur with thiopental due to histamine release?

    <p>Anaphylactic or anaphylactoid reactions</p> Signup and view all the answers

    What is a notable interaction involving ketamine?

    <p>Hypotension with inhaled anesthetics</p> Signup and view all the answers

    What do barbiturates potentiate?

    <p>Enhanced action of NMBD’s</p> Signup and view all the answers

    What is the primary characteristic of dissociative anesthesia produced by ketamine?

    <p>Eyes remain open with slow nystagmic gaze</p> Signup and view all the answers

    What is the commercial preparation of diazepam dissolved in?

    <p>Propylene glycol</p> Signup and view all the answers

    What is a notable interaction involving ketamine?

    <p>Monoamine oxidase inhibitors (MAOIs)</p> Signup and view all the answers

    What do the two optical isomers of ketamine refer to?

    <p>$S(+) ketamine &amp; R (-) ketamine$</p> Signup and view all the answers

    What is a potential application for ketamine induction of anesthesia?

    <p>Pediatric anesthesia</p> Signup and view all the answers

    What risk is associated with mixing lidocaine and propofol?

    <p>Risk of seizures</p> Signup and view all the answers

    What is a characteristic of ketamine's metabolism by cytochrome P450?

    <p>It undergoes extensive metabolism by CYP3A4</p> Signup and view all the answers

    What distinguishes dissociative anesthesia from other types of anesthesia produced by ketamine?

    <p>Patient experiences amnesia and intense analgesia</p> Signup and view all the answers

    What is the structure-activity relationship of ketamine?

    <p>It structurally resembles phencyclidine (angel dust)</p> Signup and view all the answers

    Which medication has minimal detrimental effects when accidentally injected into an artery?

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

    Which of the following is a risk factor for the occurrence of dreams and hallucinations after administration of ketamine?

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

    What is a key interaction involving thiopental?

    <p>Enhanced action of non-depolarizing neuromuscular blocking drugs (NMBD’s)</p> Signup and view all the answers

    What characterizes the effect of barbiturates on GABAA channel activity?

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

    What is a clinical use of dexmedetomidine?

    <p>Reducing plasma catecholamine concentration during anesthesia</p> Signup and view all the answers

    What are the dose requirements for thiopental based on?

    <p>Patient characteristics</p> Signup and view all the answers

    What is a potential side effect of barbiturates on ventilatory centers?

    <p>$CO_2$ retention</p> Signup and view all the answers

    What can intra-arterial injection of thiopental cause?

    <p>Vasoconstriction, pain, and permanent damage</p> Signup and view all the answers

    What is a notable characteristic of dexmedetomidine compared to clonidine?

    <p>More rapid onset of action</p> Signup and view all the answers

    What is a potential adverse effect associated with allergic reactions to thiopental?

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

    What is a potential side effect of barbiturates due to enzyme induction?

    <p>Reduced metabolism of various drugs</p> Signup and view all the answers

    What is the mechanism of action of ketamine-induced analgesia and dissociative anesthesia?

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

    What is a potential use of ketamine induction of anesthesia?

    <p>Treating psychiatric disorders</p> Signup and view all the answers

    How does ketamine affect the central nervous system?

    <p>Decreases presynaptic release of glutamate</p> Signup and view all the answers

    What is a notable pharmacokinetic property of ketamine?

    <p>Rapid onset of action</p> Signup and view all the answers

    What is a potential adverse effect of ketamine on the cardiovascular system?

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

    Study Notes

    Intravenous Anesthetics: Propofol and Etomidate

    • Propofol has effects on organ systems, including intraocular pressure and coagulation
    • Propofol's oil-in-water emulsion formulation is associated with side effects such as bradycardia and risk of infection
    • Allergic reactions to propofol can be triggered by allergenic components like phenyl nucleus and diisopropyl side chain
    • Propofol has effects on organ systems, including lactic acidosis and proconvulsant activity
    • Propofol has antioxidant properties and can inhibit lipid peroxidation
    • Pain on injection is the most commonly reported adverse event with propofol
    • Etomidate is a carboxylated imidazole-containing compound with altered pharyngeal function and a risk of aspiration
    • Etomidate's mechanism of action involves selective modulation of GABAA receptors
    • Etomidate is rapidly metabolized by hydrolysis and has a large tissue uptake
    • Etomidate is an alternative to propofol or barbiturates for IV induction, with an onset from arm to brain circulation
    • Etomidate has potent direct cerebral vasoconstrictor effects and decreases ICP
    • Cardiovascular stability is characteristic of induction with etomidate, with minimal changes in HR, SV, and CO.

    Propofol: Clinical Uses and Effects

    • Propofol is a selective modulator of GABAA receptors with evidence of potentiation at glycine receptors.
    • The clearance of propofol from plasma exceeds hepatic blood flow, with first-pass uptake into lung and hepatic oxidative metabolism.
    • It is widely used for induction of anesthesia in children and the elderly, with awakening occurring at plasma concentrations of 1.0 to 1.5 𝜇/mL.
    • Propofol is used for intravenous sedation, mechanical ventilation, and cardiac surgery to modulate postoperative hemodynamic responses.
    • It is also employed for maintenance of anesthesia and has non-hypnotic therapeutic applications such as antiemetic effects, anticonvulsant activity, and attenuation of bronchoconstriction.
    • Propofol interacts with opioids, affecting their plasma concentration, distribution clearance, and elimination clearance.
    • Propofol decreases cerebral metabolic rate for oxygen, cerebral blood flow, intracranial pressure, and does not affect cerebral autoregulation.
    • It decreases systemic blood pressure, inhibits sympathetic vasoconstrictor nerve activity, and has a negative inotropic effect on the cardiovascular system.
    • Profound bradycardia and asystole have been reported in healthy adult patients even with anticholinergic prophylaxis, and it can increase the risk of oculocardiac reflex during pediatric strabismus surgery repair.
    • Propofol does not affect hepatic or renal function, but it can cause dose-dependent depression of ventilation and may lead to Propofol Infusion Syndrome with prolonged infusions.
    • It can also potentiate respiratory depression when used with opioids and decrease the ventilatory response to arterial hypoxemia.
    • Formulations with cyclodextrins can have significant effects on wheezing and respiratory resistance after tracheal intubation.

    Anesthesia Drugs: Key Facts and Clinical Applications

    • Dreams and hallucinations can occur up to 24 hours after administration of ketamine, with an incidence of 5 to 30% and risk factors including age, gender, dose, and personality problems.
    • Ketamine interactions include hypotension with inhaled anesthetics, enhanced action of NMBD’s, and interference with heart preconditioning and succinylcholine recovery.
    • Thiopental, introduced in 1934, revolutionized anesthesia practice and is considered the "Gold Standard" in anesthesia.
    • Barbiturates, derived from barbituric acid, have different substitutions determining their properties, including oxygen or sulfur in different positions affecting lipid solubility and potency.
    • Barbiturates potentiate GABAA channel activity and have been replaced by benzodiazepines for pre-op medication and treating seizures.
    • Barbiturates have rapid onset and awakening due to redistribution, prolonged context-sensitive half-time, and hangover-type CNS effects.
    • Thiopental is used for increased intracranial pressure, ischemic injury, and induction of anesthesia, with dose requirements varying with patient characteristics.
    • Side effects of barbiturates include changes in somatosensory evoked potentials, dose-dependent depression of ventilatory centers, and enzyme induction leading to accelerated metabolism of various drugs.
    • Intra-arterial injection of thiopental can cause vasoconstriction, pain, gangrene, and permanent damage.
    • Allergic reactions, including anaphylactic and anaphylactoid, can occur with thiopental due to histamine release.
    • Dexmedetomidine is a highly selective alpha-2 adrenergic agonist, with a shorter duration of action compared to clonidine and is used to calm patients and reduce the hemodynamic response to tracheal intubation.
    • Clinical use of dexmedetomidine includes attenuating the hemodynamic response to tracheal intubation, decreasing plasma catecholamine concentration during anesthesia, reducing perioperative requirements of opioids and inhaled anesthetics, and treating post-op shivering.

    Ketamine: Mechanism, Pharmacokinetics, Clinical Uses, and Side Effects

    • Esketamine is widely used in Europe and has more intense analgesia, faster metabolism, less salivation, and lower incidence of emergence reactions.
    • Both isomers of ketamine inhibit reuptake of catecholamines back into postganglionic sympathetic nerve endings.
    • Mechanism of action of ketamine-induced analgesia and dissociative anesthesia is unknown, but it binds to N-methyl-D-aspartate receptors and exerts effects at other sites including opioid receptors, monoaminergic receptors, and muscarinic receptors.
    • Ketamine inhibits neutrophil production of inflammatory mediators, improves blood flow, and inhibits cytokines in blood, contributing to its analgesic effect.
    • Ketamine is a member of the glutamate receptor family, inhibits activation of NMDA receptors by glutamate, and decreases presynaptic release of glutamate.
    • Ketamine has a rapid onset of action, relatively short duration of action, and high lipid solubility. It is not significantly bound to plasma proteins and has high hepatic clearance and large volume of distribution.
    • Ketamine undergoes extensive metabolism by cytochrome P450, forming the norketamine metabolite, which is 1/5 to 1/3 as potent as ketamine. Chronic administration causes enzyme induction and tolerance.
    • Ketamine is used for analgesia, inducing anesthesia, managing postoperative pain, and providing analgesia during labor without neonatal depression.
    • Ketamine induction of anesthesia is safe, does not produce pain or irritation on injection, and has useful applications in burn patients, pediatrics, and hypovolemic patients.
    • Subanesthetic doses of ketamine reduce the likelihood of opioid tolerance, improve analgesia, and have shown improvement in psychiatric disorders and restless leg syndrome.
    • Ketamine has various effects on the central nervous system, cardiovascular system, ventilation and airway, and can cause tissue damage, allergic reactions, and emergence delirium.
    • Prevention of emergence delirium can be achieved through the use of benzodiazepines preoperatively, as emergence delirium may result in visual, auditory, proprioceptive, and confusional illusions.

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