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NU 624

Exam 2 - Induction Agents

What are the 5 types of induction agents used in anesthesia? Barbiturates, non-barbiturates, propofol, etomidate, ketamine
Identify 5 barbiturate induction agents. Thiopental, methohexital, pentobarbital, secobarbital, phenobarbital
What is the trade name of thiopental? Pentothal
What is the trade name of methohexital? Brevital
What is the trade name of pentobarbital? Nembutal
What is the trade name of secobarbital? Seconal
What are all barbiturates derived from? Barbituric acid
What two substances combine to form barbituric acid? Urea and malonic acid
Which CNS neurotransmitter is linked to the action of barbiturates? GABA
What element is involved with the use of barbiturates and how does it affect the nervous system? Barbiturate use results in chloride ion movement into nerve cells
In what area can a substitution be made in the barbituric acid molecule to form different barbiturates? Carbon atoms of the benzene ring
What change can be made to a barbiturate in order to increase its hypnotic activity? Creating a branched chain substitution on the #5 carbon atom
Name two different categories of barbiturates. Oxybarbiturates, thiobarbiturates
What is the molecular difference between oxy- and thio- barbiturates? Oxybarbiturates retain an oxygen atom on the #2 carbon and thiobarbiturates retain a sulfur atom on the #2 carbon atom.
What changes can result from making substitutions in the molecular structure of a barbiturate? Hypnotic potency, lipid solubility, anticonvulsant properties, duration of action
Methohexital is a commonly used type of ____________. Oxybarbiturate
Why do anesthetists like using methohexital (Brevital)? It is ultra-short acting
What are 4 different oxybarbiturates? Methohexital, pentobarbital, secobarbital, phenobarbital
What are 2 thiobarbiturates? Thiopental, thiamylal
What is the trade name of thiamylal? Surital
What replacement occurs in an oxybarbiturate that makes it change into a thiobarbiturate? The oxygen at on the #2 carbon is replaced with a sulfur atom
What are two ways that sodium thiopental can be abbreviated? STP, NaTPL
What substitution enhances the anticonvulsant effect of barbituric acid? A phenyl group at the #5 carbon
Give an example of a barbiturate with a phenyl group substitution. Where does this substitution occur and what does this enhance? Phenobarbital--substitution at the #5 position, with a phenyl group, increases its anticonvulsant effect
The addition of a methyl radical to a nitrogen atom on the #5 carbon of barbituric acid results in what 3 changes? More rapid onset, shorter duration, some convulsant effects
Give an example of a barbiturate with a methyl radical group substitution. Methohexital
What are the side effects of methohexital? Convulsant effects, manifested by involuntary but short-lived skeletal muscle movements.
Methohexital is a/an (long-acting/intermediate acting/short/acting/ultra short acting) barbiturate. ultra short acting
How are barbiturates metabolized and excreted? Metabolized by hepatic microsomal enzymes and renally excreted
The most significant metabolic pathway involves what position on a barbiturate and through what means of metabolism? #5 carbon side chains via oxidation
What byproduct forms from the breakdown of a barbiturate? Is it active or inactive? Thiopental carboxylic acid--inactive
After oxidation, the barbiturate becomes more (lipid/water) soluble. Water
What metabolic pathway do thiobarbiturates undergo? desulfuration
Desulfuration is a (Phase I/Phase II) reaction. Phase I
How many steps are involved in the breakdown of thiopental? 4
What is the most commonly used thiobarbiturate? Thiopental (Pentothal)
Describe the first step of thiopental metabolism? Desulfuration converts thiopental to the oxybarbiturate, pentabarbital
Describe the second step of thiopental metabolism? Oxidation of the side chain groups at the #5 carbon converts pentabarbital to water-soluble thiopental carboxylic acid
Describe the third step of thiopental metabolism? Conjugation with glucuronic acid
Describe the fourth step of thiopental metabolism? Excretion by the kidneys as glucuronide
What three products combine to give propofol its milky white appearance? 10% soybean, 2.25% glycerol, 1.2% purified egg phophatide
What does the soybean/glycerol/egg phosphatide formulation support? Bacterial growth
What have recent reports on propofol revealed? Bacterial contamination of the emulsion has led to post-op infections
What two pharmaceutical companies have created additives to combat the bacterial growth in propofol? AstraZeneca and Baxter Labs
What component did AstraZeneca add to propofol to inhibit bacterial growth? EDTA (ethylenediamenetetraacetate)
What component did Baxter Labs add to propofol to inhibit bacterial growth? 0.025% sodium meta-bisulfite
Propofol is highly bound to what component? Protein
Where and through what pathway is propofol metabolized? In the liver via conjugation
What is significant about the clearance rate of propofol? Clearance exceeds hepatic blood flow, suggesting extra hepatic methods of metabolism
How is etomidate classified? Nonbarbiturate anesthetic
The use of etomidate causes ________ effects to produce a __________ state. CNS, hypnotic
How is etomidate chemically classified? Ethyl ester of a carboxylated imidazole derivative
What are two important facts regarding the benefits of etomidate? Wide range of safety, maintains cardiovascular stability
What are two side effects of etomidate use? Pain with injection and myclonia
What is myoclonia? Involuntary, rapid, nonrhythmic muscle contractions
What types of enzymes are used to break down etomidate? Hepatic microsomal enzymes and plasma esterases
What is the primary means of etomidate metabolism and where does it occur? Ester hydrolysis in the liver and plasma
What type of adrenocortical effects does etomidate have and what does it lead to? Adrenocortical hypofunction leads to decreased levels of cortisol
What are beneficial uses of cortisol in the body? BP management, reduced inflammation, strengthened immune system
How long do the adrenocorticol effects of etomidate last? 4 days after initial administration
Adrenocorticol hypofunction as a result of etomidate is (reversible/irreversible). Reversible
Ketamine is a derivative of __________. Phenylcyclidine
Why has ketamine decreased in popularity? Causes serious psychic disturbances, including hallucinations and delirium
What type of neurological state does ketamine result in? Dissociative state
What do dissociative anesthetics distort and what do they produce? Distort perceptions of sight and sound to produce feelings of detachment from the environment and self
What effects occur in a dissociative state of anesthesia? Catatonia, split personality
BONUS: What is a unique characteristic of optical isomers? Their sequence of atoms and bonds creates a 3D structure
Bonus: What are chiral molecules? Non-superimposable mirror images of molecules
What are two characteristics of the molecular structure of ketamine? It is optically active with a chiral center that consists of two optical isomers
The racemic mixture of ketamine contains (equal/different) amounts of isomers. Equal
What are the two optical isomers in ketamine? S(+) and R(-)
What effects on patients does the S(+) isomer in ketamine have? Less spontaneous motor activity, more calm in recovery, fewer complaints of pain
What effects on patients does the R(-) isomer in ketamine have? Hallucinations, combativeness, delirium on emergence
Which isomer in ketamine is responsible for hallucinations and combativeness? R(-)
Where and through what system is ketamine metabolized? Liver by hepatic microsomal enzymes
What two Phase I metabolic processes occur in the metabolization of ketamine? Demethylation and hydroxylation
What does the demethylation and hydroxylation of ketamine produce? Glucuronide derivative
How is the glucuronide derivative of ketamine metabolism excreted? Renally excreted after it undergoes conjugation
Created by: philip.truong