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Questions and Answers
Which medication has minimal detrimental effects when accidentally injected into an artery?
Which medication has minimal detrimental effects when accidentally injected into an artery?
Which medication may stimulate ventilation independent of medullary centers?
Which medication may stimulate ventilation independent of medullary centers?
Which medication is effective for acute insomnia but may lead to cognitive problems and mortality?
Which medication is effective for acute insomnia but may lead to cognitive problems and mortality?
Which medication has a built-in ceiling effect, preventing it from exceeding the physiologic maximum of GABA inhibition?
Which medication has a built-in ceiling effect, preventing it from exceeding the physiologic maximum of GABA inhibition?
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Which medication may accelerate cognitive decline in elderly patients and inhibit platelet aggregation in aging and liver disease?
Which medication may accelerate cognitive decline in elderly patients and inhibit platelet aggregation in aging and liver disease?
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Which medication can lead to adrenocortical suppression for 4 to 8 hours after an induction dose?
Which medication can lead to adrenocortical suppression for 4 to 8 hours after an induction dose?
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What is the recommended pediatric dosing for midazolam for induction of anesthesia?
What is the recommended pediatric dosing for midazolam for induction of anesthesia?
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How is diazepam metabolized in the body?
How is diazepam metabolized in the body?
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What is the elimination half-time of diazepam in healthy volunteers?
What is the elimination half-time of diazepam in healthy volunteers?
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How does midazolam affect blood pressure and heart rate?
How does midazolam affect blood pressure and heart rate?
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What is the commercial preparation of diazepam dissolved in?
What is the commercial preparation of diazepam dissolved in?
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What is the peak effect onset time for intravenous sedation with midazolam?
What is the peak effect onset time for intravenous sedation with midazolam?
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What is the plasma concentration at which awakening occurs in children and the elderly when using propofol for induction of anesthesia?
What is the plasma concentration at which awakening occurs in children and the elderly when using propofol for induction of anesthesia?
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What effect does propofol have on cerebral blood flow?
What effect does propofol have on cerebral blood flow?
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What is a potential adverse effect of propofol on the cardiovascular system?
What is a potential adverse effect of propofol on the cardiovascular system?
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How does propofol affect hepatic or renal function?
How does propofol affect hepatic or renal function?
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What is a potential risk associated with prolonged infusions of propofol?
What is a potential risk associated with prolonged infusions of propofol?
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Which adverse event is most commonly reported with propofol?
Which adverse event is most commonly reported with propofol?
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What is a potential trigger for allergic reactions to propofol?
What is a potential trigger for allergic reactions to propofol?
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Which organ system does propofol affect?
Which organ system does propofol affect?
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What is the mechanism of action of etomidate?
What is the mechanism of action of etomidate?
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What is a characteristic effect of etomidate on ICP (intracranial pressure)?
What is a characteristic effect of etomidate on ICP (intracranial pressure)?
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Which drug induces a state of calm or sleep?
Which drug induces a state of calm or sleep?
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What is the chemical structure of Propofol?
What is the chemical structure of Propofol?
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What risk is associated with mixing lidocaine and propofol?
What risk is associated with mixing lidocaine and propofol?
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Which propofol alternative has a higher pain on injection?
Which propofol alternative has a higher pain on injection?
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What is the main concern with Aquavan and fospropofol?
What is the main concern with Aquavan and fospropofol?
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What is the function of Sedatives?
What is the function of Sedatives?
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What is a potential adverse effect of propofol on the cardiovascular system?
What is a potential adverse effect of propofol on the cardiovascular system?
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What is the mechanism of action of etomidate?
What is the mechanism of action of etomidate?
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Which adverse event is most commonly reported with propofol?
Which adverse event is most commonly reported with propofol?
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Which organ system does propofol affect?
Which organ system does propofol affect?
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What is a potential trigger for allergic reactions to propofol?
What is a potential trigger for allergic reactions to propofol?
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What risk is associated with mixing lidocaine and propofol?
What risk is associated with mixing lidocaine and propofol?
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Which medication has minimal detrimental effects when accidentally injected into an artery?
Which medication has minimal detrimental effects when accidentally injected into an artery?
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Which medication may accelerate cognitive decline in elderly patients and inhibit platelet aggregation in aging and liver disease?
Which medication may accelerate cognitive decline in elderly patients and inhibit platelet aggregation in aging and liver disease?
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Which medication has a built-in ceiling effect, preventing it from exceeding the physiologic maximum of GABA inhibition?
Which medication has a built-in ceiling effect, preventing it from exceeding the physiologic maximum of GABA inhibition?
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Which medication is effective for acute insomnia but may lead to cognitive problems and mortality?
Which medication is effective for acute insomnia but may lead to cognitive problems and mortality?
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What risk is associated with mixing lidocaine and propofol?
What risk is associated with mixing lidocaine and propofol?
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What is a characteristic effect of etomidate on ICP (intracranial pressure)?
What is a characteristic effect of etomidate on ICP (intracranial pressure)?
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What is the recommended timing for administering midazolam before surgery?
What is the recommended timing for administering midazolam before surgery?
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What is the onset time for intravenous sedation with midazolam?
What is the onset time for intravenous sedation with midazolam?
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How is diazepam metabolized in the body?
How is diazepam metabolized in the body?
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What is the elimination half-time of diazepam in healthy volunteers?
What is the elimination half-time of diazepam in healthy volunteers?
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What is the commercial preparation of diazepam dissolved in?
What is the commercial preparation of diazepam dissolved in?
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Which medication has a longer elimination half-time than lorazepam but shorter duration of action?
Which medication has a longer elimination half-time than lorazepam but shorter duration of action?
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What is the plasma concentration at which awakening occurs in children and the elderly when using propofol for induction of anesthesia?
What is the plasma concentration at which awakening occurs in children and the elderly when using propofol for induction of anesthesia?
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What is one of the non-hypnotic therapeutic applications of propofol?
What is one of the non-hypnotic therapeutic applications of propofol?
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What effect does propofol have on cerebral blood flow?
What effect does propofol have on cerebral blood flow?
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What risk is associated with mixing lidocaine and propofol?
What risk is associated with mixing lidocaine and propofol?
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How does propofol affect hepatic or renal function?
How does propofol affect hepatic or renal function?
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What is a potential adverse effect of propofol on the cardiovascular system?
What is a potential adverse effect of propofol on the cardiovascular system?
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What is the chemical structure of Propofol?
What is the chemical structure of Propofol?
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Which organ system does propofol affect?
Which organ system does propofol affect?
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What is a potential risk associated with mixing lidocaine and propofol?
What is a potential risk associated with mixing lidocaine and propofol?
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What is the alternative to Propofol that has a higher pain on injection?
What is the alternative to Propofol that has a higher pain on injection?
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What is the function of Anxiolytics?
What is the function of Anxiolytics?
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What is the primary component in Propofol's formulation that supports bacterial growth and increases triglycerides with prolonged infusion?
What is the primary component in Propofol's formulation that supports bacterial growth and increases triglycerides with prolonged infusion?
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What is the primary characteristic of dissociative anesthesia produced by ketamine?
What is the primary characteristic of dissociative anesthesia produced by ketamine?
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What is the main limitation of ketamine as a sole anesthetic agent?
What is the main limitation of ketamine as a sole anesthetic agent?
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What is the structure-activity relationship of ketamine?
What is the structure-activity relationship of ketamine?
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Which isomer of ketamine is used for treatment resistant depression?
Which isomer of ketamine is used for treatment resistant depression?
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What type of anesthesia does ketamine produce?
What type of anesthesia does ketamine produce?
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What risk limits the clinical usefulness of ketamine as a sole anesthetic agent?
What risk limits the clinical usefulness of ketamine as a sole anesthetic agent?
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Which molecule does ketamine structurally resemble?
Which molecule does ketamine structurally resemble?
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What characterizes the patient's state during dissociative anesthesia produced by ketamine?
What characterizes the patient's state during dissociative anesthesia produced by ketamine?
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What distinguishes the S(+) isomer of ketamine from the R (-) isomer?
What distinguishes the S(+) isomer of ketamine from the R (-) isomer?
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What distinguishes dissociative anesthesia from other types of anesthesia produced by ketamine?
What distinguishes dissociative anesthesia from other types of anesthesia produced by ketamine?
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What is the mechanism of action of ketamine-induced analgesia and dissociative anesthesia?
What is the mechanism of action of ketamine-induced analgesia and dissociative anesthesia?
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What is a clinical use of ketamine?
What is a clinical use of ketamine?
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What effect does chronic administration of ketamine have on enzyme activity?
What effect does chronic administration of ketamine have on enzyme activity?
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What is a potential adverse effect of ketamine on the cardiovascular system?
What is a potential adverse effect of ketamine on the cardiovascular system?
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How does subanesthetic doses of ketamine affect opioid tolerance?
How does subanesthetic doses of ketamine affect opioid tolerance?
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What is a potential approach for preventing emergence delirium caused by ketamine?
What is a potential approach for preventing emergence delirium caused by ketamine?
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What is a characteristic of ketamine's metabolism by cytochrome P450?
What is a characteristic of ketamine's metabolism by cytochrome P450?
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What is a potential application for ketamine induction of anesthesia?
What is a potential application for ketamine induction of anesthesia?
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What is the pharmacokinetic characteristic of ketamine's volume of distribution?
What is the pharmacokinetic characteristic of ketamine's volume of distribution?
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What is a potential effect of subanesthetic doses of ketamine on psychiatric disorders?
What is a potential effect of subanesthetic doses of ketamine on psychiatric disorders?
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Which drug is considered the 'Gold Standard' in anesthesia and was introduced in 1934?
Which drug is considered the 'Gold Standard' in anesthesia and was introduced in 1934?
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What is a key risk factor for dreams and hallucinations occurring up to 24 hours after administration of ketamine?
What is a key risk factor for dreams and hallucinations occurring up to 24 hours after administration of ketamine?
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What is a potential side effect of barbiturates?
What is a potential side effect of barbiturates?
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Which drug is a highly selective alpha-2 adrenergic agonist and is used to calm patients and reduce the hemodynamic response to tracheal intubation?
Which drug is a highly selective alpha-2 adrenergic agonist and is used to calm patients and reduce the hemodynamic response to tracheal intubation?
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What is a use of thiopental in clinical practice?
What is a use of thiopental in clinical practice?
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What can intra-arterial injection of thiopental cause?
What can intra-arterial injection of thiopental cause?
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What is a potential allergic reaction that can occur with thiopental due to histamine release?
What is a potential allergic reaction that can occur with thiopental due to histamine release?
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What is a notable interaction involving ketamine?
What is a notable interaction involving ketamine?
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What do barbiturates potentiate?
What do barbiturates potentiate?
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What is the primary characteristic of dissociative anesthesia produced by ketamine?
What is the primary characteristic of dissociative anesthesia produced by ketamine?
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What is the commercial preparation of diazepam dissolved in?
What is the commercial preparation of diazepam dissolved in?
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What is a notable interaction involving ketamine?
What is a notable interaction involving ketamine?
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What do the two optical isomers of ketamine refer to?
What do the two optical isomers of ketamine refer to?
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What is a potential application for ketamine induction of anesthesia?
What is a potential application for ketamine induction of anesthesia?
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What risk is associated with mixing lidocaine and propofol?
What risk is associated with mixing lidocaine and propofol?
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What is a characteristic of ketamine's metabolism by cytochrome P450?
What is a characteristic of ketamine's metabolism by cytochrome P450?
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What distinguishes dissociative anesthesia from other types of anesthesia produced by ketamine?
What distinguishes dissociative anesthesia from other types of anesthesia produced by ketamine?
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What is the structure-activity relationship of ketamine?
What is the structure-activity relationship of ketamine?
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Which medication has minimal detrimental effects when accidentally injected into an artery?
Which medication has minimal detrimental effects when accidentally injected into an artery?
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Which of the following is a risk factor for the occurrence of dreams and hallucinations after administration of ketamine?
Which of the following is a risk factor for the occurrence of dreams and hallucinations after administration of ketamine?
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What is a key interaction involving thiopental?
What is a key interaction involving thiopental?
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What characterizes the effect of barbiturates on GABAA channel activity?
What characterizes the effect of barbiturates on GABAA channel activity?
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What is a clinical use of dexmedetomidine?
What is a clinical use of dexmedetomidine?
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What are the dose requirements for thiopental based on?
What are the dose requirements for thiopental based on?
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What is a potential side effect of barbiturates on ventilatory centers?
What is a potential side effect of barbiturates on ventilatory centers?
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What can intra-arterial injection of thiopental cause?
What can intra-arterial injection of thiopental cause?
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What is a notable characteristic of dexmedetomidine compared to clonidine?
What is a notable characteristic of dexmedetomidine compared to clonidine?
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What is a potential adverse effect associated with allergic reactions to thiopental?
What is a potential adverse effect associated with allergic reactions to thiopental?
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What is a potential side effect of barbiturates due to enzyme induction?
What is a potential side effect of barbiturates due to enzyme induction?
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What is the mechanism of action of ketamine-induced analgesia and dissociative anesthesia?
What is the mechanism of action of ketamine-induced analgesia and dissociative anesthesia?
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What is a potential use of ketamine induction of anesthesia?
What is a potential use of ketamine induction of anesthesia?
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How does ketamine affect the central nervous system?
How does ketamine affect the central nervous system?
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What is a notable pharmacokinetic property of ketamine?
What is a notable pharmacokinetic property of ketamine?
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What is a potential adverse effect of ketamine on the cardiovascular system?
What is a potential adverse effect of ketamine on the cardiovascular system?
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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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Test your knowledge about the effects, formulations, and mechanisms of action of Intravenous Anesthetics Propofol and Etomidate with this quiz.