Pharmacodynamics and Pharmacokinetics of Propofol

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32 Questions

Which induction agent is preferred in shock, for long procedures, or when extra analgesia is important?

Ketamine

Which induction agent is good in haemodynamically unstable patients, but is not available in Australia?

Etomidate

Which induction agent is good for haemodynamically stable patients or short procedures?

Propofol

Which induction agent has excellent amnesic properties?

Midazolam

Which induction agent has bronchorelaxant properties making it useful in critical asthma, but also increases bronchial secretions?

Ketamine

Which induction agent is best for longer, painful procedures, particularly in children?

Ketamine-midazolam

What is the duration of action for ketamine when administered intravenously?

5 - 15 minutes

Which of the following is an adverse effect associated with ketamine administration?

Lacrimation and salivation

What is the usual dose of ketamine for induction of anaesthesia intravenously?

1.5 - 2 mg/kg

What led to the change in scheduling for ketamine from Schedule 4 to 8 in 2005?

Increasing illicit use and diversion

What effect does ketamine have on the patient's eyes?

They often remain open

What is the mechanism of action of ketamine as an analgesic?

Blocks NMDA receptors

What adverse effect is associated with ketamine administration in children under 2 years of age?

Hypotension

What is the most common cardiovascular effect of ketamine administration?

Increased heart rate and blood pressure

What adverse effect can occur if the total intravenous dose of ketamine exceeds 5 mg/kg?

Vomiting

True or False: Ketamine has a rapid onset of action when administered intramuscularly.

What is the primary mechanism of action of propofol in altering neuronal function?

Potentiation of GABAergic inhibition

What is the most significant route of metabolism for propofol in the body?

Glucuronidation

What is the approximate half-life of distribution for propofol?

10-15 minutes

What is the primary reason for the anti-emetic effect of propofol?

Potentiation of GABAergic inhibition in the brainstem

What is the usual dose of propofol for induction of anaesthesia in adults?

2 mg/kg

Which adverse effect is associated with propofol related infusion syndrome?

Bradycardia

What is the main disadvantage of using propofol?

Risk of hypotension

What is the distribution half-life of etomidate?

3 minutes

What is the duration of effect of etomidate?

5-10 minutes

What adverse effect is associated with etomidate administration in up to 70% of cases?

Myoclonus

What is the main advantage of using remifentanil?

Rapid onset and offset

What is the metabolism of remifentanil?

< 50% excreted unchanged

What special use is associated with fentanyl in hypovolaemic conditions?

Causes less hypotension than thiopentone, propofol, and morphine

What adverse effect can occur if the total intravenous dose of ketamine exceeds 5 mg/kg?

Anion gap metabolic acidosis

What effect does ketamine have on the patient's eyes?

Mydriasis

What led to the change in scheduling for ketamine from Schedule 4 to 8 in 2005?

Concerns about its potential for abuse and dependence

Study Notes

Induction Agents

  • Etomidate is preferred in shock, for long procedures, or when extra analgesia is important.
  • Ketamine is good in haemodynamically unstable patients, but it's not available in Australia.
  • Propofol is good for haemodynamically stable patients or short procedures.

Properties of Induction Agents

  • Ketamine has excellent amnesic properties.
  • Ketamine has bronchorelaxant properties, making it useful in critical asthma, but it also increases bronchial secretions.
  • Ketamine is best for longer, painful procedures, particularly in children.

Ketamine

  • The duration of action of ketamine when administered intravenously is 10-15 minutes.
  • One adverse effect associated with ketamine administration is hallucinations.
  • The usual dose of ketamine for induction of anaesthesia intravenously is 1-2 mg/kg.
  • The change in scheduling for ketamine from Schedule 4 to 8 in 2005 was due to its abuse potential.
  • Ketamine causes the patient's eyes to become dilated and unreactive.
  • The mechanism of action of ketamine as an analgesic is NMDA receptor antagonism.
  • In children under 2 years of age, ketamine administration is associated with increased secretions and respiratory problems.
  • The most common cardiovascular effect of ketamine administration is increased heart rate and blood pressure.
  • If the total intravenous dose of ketamine exceeds 5 mg/kg, it can cause respiratory depression.

Propofol

  • The primary mechanism of action of propofol in altering neuronal function is GABA receptor activation.
  • The most significant route of metabolism for propofol in the body is liver metabolism.
  • The approximate half-life of distribution for propofol is 2-8 minutes.
  • The primary reason for the anti-emetic effect of propofol is its antagonism of dopamine receptors.
  • The usual dose of propofol for induction of anaesthesia in adults is 1-2 mg/kg.
  • Propofol-related infusion syndrome is associated with cardiovascular and metabolic acidosis.
  • The main disadvantage of using propofol is its cost.

Etomidate

  • The distribution half-life of etomidate is 2-5 minutes.
  • The duration of effect of etomidate is 3-5 minutes.
  • Up to 70% of cases of etomidate administration are associated with myoclonus.

Remifentanil

  • The main advantage of using remifentanil is its rapid onset and offset of action.
  • Remifentanil is metabolized by esterases in the blood.

Fentanyl

  • Fentanyl is specially used in hypovolaemic conditions due to its vasopressor effects.
  • If the total intravenous dose of ketamine exceeds 5 mg/kg, it can cause respiratory depression.

Test your knowledge of the pharmacodynamics and pharmacokinetics of propofol, a very short-acting induction agent used in anesthesia. Explore its exact mechanism of action, pharmacokinetic properties, and effects on the body.

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