Intravenous Anesthetics and their
Chemistry
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Abstract:
The use of anesthesia revolutionized the medical world, without it many
operations performed today would be nearly impossible and very
impractical. Over time many different forms of anesthetics have been
produced being categorized into four classes: general anesthesia, regional
anesthesia, sedation, and local anesthesia. This study focuses on general
anesthetics, specifically intravenous anesthetics (IV anesthetics). The
different elements studied were the kinetics, energetics, intermolecular
forces, and the target of the common drugs within this class of anesthesia.
The purpose of this study is to identify the chemical make-up of each drug of
this class of anesthetics to better help undergraduate students to
understand the drug’s role in the medical world while relating to principles
taught within CHEM 1220.
Propofol
Kinetics:
-Rapid onset, metabolism, and recovery. Goes into effect in about 10 seconds. 10-minute half-
Jackson Thomas
life.
Energetics:
-Metabolized by conjugation of sulfate and glucuronide, making the molecule more hydrophilic
to be processed. Bonds ae formed and require energy of around 358 kJ/mol to 821 kJ/mol.
Intermolecular Forces:
-London-dispersion forces, Hydrogen bonding
-Hydrophobic, non-polar
Target:
-Blood-Brain Barrier -> GABA-A receptor.
Etomidate
Alfaxlone
Kinetics:
Kinetics:
-“Similar to thiopental but more rapidly metabolized.” (textbook from eves). Half-life of
22.3± 10.4 minutes. Elimination half-life of 2.9-5.5 hours.
-Elimination half-life is 45.2-76.6
Energetics:
-Metabolized by the cytochrome P450
Energetics:
-ATP is absorbed during the metabolism of the drug from the hepatic esterase.
Intermolecular Forces:
Intermolecular Forces:
-London-dispersion forces, dipole-dipole attraction.
-London-dispersion, dipole-dipole attraction, hydrogen bonding.
-polar, hydrophobic
Target:
-Blood-Brain Barrier -> GABA-A receptors
-Polar, hydrophobic.
Target:
-Blood-Brain Barrier -> GABA-A receptor.
Fentanyl
Thiopental
Kinetics:
Kinetics:
-Duration of action is about 30 minutes. Half life elimination of 3.5 hours.
-Short duration of action (5 minutes). Takes 10-20 seconds to take effect. Half-life of 3 minutes,
elimination half-life of 9±1.6 hours
Energetics:
Energetics:
Intermolecular Forces:
-London-dispersion forces, dipole-dipole attraction.
-The CYP3A4 enzyme is the primary metabolizer of fentanyl
-Metabolized by ring desulfurization by cytochrome P450. In this process ATP is released
Intermolecular Forces:
-London-dispersion forces, dipole-dipole attraction.
-Polar, hydrophilic
Target:
-Blood-Brain Barrier -> GABA-A receptor.
-Non-polar
Target:
-Blood-Brain Barrier -> GABA-A receptor.
Ketamine
Midazolam
Kinetics:
Kinetics:
-Half life of 1.95 minutes, elimination half-life 2-3 hours.
-Duration of action 60-12 minutes. Elimination half-life 1.5-3 hours.
Energetics:
Energetics:
-ATP is absorbed to form bonds during the metabolization from the cytochrome P450 enzyme.
-ATP is absorbed during the metabolism of the drug from the hepatic CYP450 enzymes and
glucuronide conjugation.
Intermolecular Forces:
-London-dispersion forces, dipole-dipole attraction, Hydrogen Bonding.
-Non-polar and polar, hydrophilic and lipophilic
Target:
-Blood-Brain Barrier -> Cerebral cortex & limbic system.
Intermolecular Forces:
-London-dispersion forces, dipole-dipole attraction.
-Polar, hydrophilic and lipophilic
Target:
-Blood-Brain Barrier -> Benzodiazepine receptor (GABA-A receptor).