PROPOFOL PROPOFOL

Lauren Martinez Student pharmacist, Purdue University College of Pharmacy Fall 2022

Other Names

History & Background

Propofol was approved by the FDA in 1989 for induction and maintenance of anesthesia during surgeries.

It is also indicated for ICU sedation of intubated and mechanically ventilated patients.

It was initially developed as an alternative for thiopental and methohexital, which both had significant post-op fatigue, nausea, vomiting, and cognitive impairment.

Propofol gained worldwide attention in 2009 when singer Michael Jackson died of a propofol overdose while using the drug as a sleep aid.

Today, propofol abuse is almost exclusively seen in medical professionals, especially anesthesia providers.

Propofol abuse accounts for 1.6% of all healthcare addiction cases.

Animal studies have found that propofol use can result in physical dependence due to dose-dependent symptoms of a "high".

Diprivan® (Brand)

"Milk of Anesthesia"

Pharmacology

Propofol is thought to produce its sedative/anesthetic effects by positive modulation of the inhibitory function of the neurotransmitter GABA through GABAa receptors.

IV Propofol usually induces anesthesia within 40 seconds after the start of administration.

The duration of sedative action is 3 to 10 minutes depending on the dose, rate, and duration of treatment.

Half-life is bi-phasic, with the initial being 40 minutes and the terminal being 4 to 7 hours.

Propofol has a large volume of distribution and is highly lipophilic.

Metabolism is mainly hepatic, and excretion is via urine.