Propofol (2,6-diisopropylphenol) is a commonly used short-acting intravenous anesthetic agent. However, because of the risk of drug abuse and propofol related death, in Korea propofol is a controlled drug. In this review, the analytical methods using liquid chromatography (LC), gas chromatography/mass spectrometry, or LC coupled with tandem mass spectrometry to detect and quantify propofol or its metabolites in blood were described. The validation data for the analytical methods and propofol concentrations in the blood were reviewed.