Katzung 12th ed - Chapter 25 - General Anaesthetics - Intravenous (1) Flashcards
What class of drug is thiopentone?
Thiopentone is an ultra-short-acting barbiturate given IV.
Describe the basic pharmacodynamics of thiopentone and phenobarbitone.
Bind to GABA receptors, prolong the duration of chloride channel opening, causing inhibition of action potential propagation. These can cause sedation, hypnosis, and anticonvulsant activity.
Describe the distribution of thiopentone.
Thiopentone is highly lipid-soluble, and achieves plasma:brain equilibrium within one minute of IV administration.
What is the duration of action of thiopentone? What pharmacokinetic feature of thiopentone determines the offset of its CNS effects?
Duration of action is 20-30 minutes, due to its rapid redistribution from CNS to skeletal muscle and adipose tissues.
Describe the metabolism and elimination of thiopentone and phenobarbitone.
Both are metabolized SLOWLY in the liver to produce water-soluble inactive metabolites that are excreted in the urine.
Describe the basic pharmacodynamics of propofol.
Propofol potentiates the inhibitory effect of GABA and glycine, causing hypnosis. It is used for both induction and maintenance of anaesthesia.
What dose of propofol is given to achieve sedation?
0.5 - 1 mg/kg.
What dose of propofol is given to achieve anaesthesia?
2-2.5 mg/kg.
Describe the cardiovascular adverse effects of propofol.
Reduced PVR –> hypotension.
Negative inotrope.
How is propofol presented?
As an oil in water emulsion.
Describe the metabolism and excretion of propofol.
Rapidly metabolized in the liver (10 times faster than thiopentone) and excreted in urine.
In one word, explain what largely determines the offset of CNS effect of propofol.
Redistribution.
What is the distribution half-life of propofol?
What is the elimination half-life of propofol?
Distribution half-life 2-8 minutes.
Elimination half-life 30-60 minutes.
What is the volume of distribution of propofol: small or large? Why?
Small Vd, due to being 90% protein-bound.
What do we know about the mechanism of action of ketamine?
Largely unknown, but it may involve blockade of glutamate (NMDA) receptors.