Propofol (2,6-diisopropylphenol) is an alkyl phenol derivative that possesses sedative and hypnotic properties.22 It is a simple phenol substituted with two isopropyl groups in each of the positions adjacent to the hydroxyl group, the ortho positions.23 Administration of propofol, 1.5 to 2.5 mg/kg IV produces unconsciousness within about 30 seconds. Awakening is more rapid and complete. The more rapid return of consciousness with minimal residual central nervous system (CNS) effects is one of the most important advantages of propofol.24 Figure 1 : Chemical structure of Propofol Molecular Formula: C12H18O Molecular Weight: 178.27072 g/mol Mechanism of Action: Propofol is a relatively …show more content…
This formulation is equipotent to Diprivan but is associated with a higher incidence of pain on injection.24 An alternative to emulsion formulations of propofol and associated side effects (pain on injection, risk of infection, hypertriglyceridemia, pulmonary embolism) is creation of a prodrug (Aqauvan) by cleaving groups to the parent compound that increase its water solubility (phosphate monoesters, hemisuccinates). Propofol is liberated after hydrolysis by endothelial cell surface alkaline phosphatases. In this regard, injection of the water-soluble prodrug results in propofol and dose dependent sedative effects. Compared with propofol, this prodrug has a larger volume of distribution and higher potency.24 A nonlipid formulation of propofol uses cyclodextrins as a solublilizing agent. Cyclodextrins are ring sugar molecules that form guest (propofol)-host complexes migrating between the hydrophilic center of the cyclodextrin molecule and the water-soluble phase. This allows propofol, which is poorly soluble in water, to be presented in an injectable form. After injection, propofol migrates out of the cyclodextrin into the