Fospropofol disodium, a water-soluble prodrug of the intravenous anesthetic propofol (2,6-diisopropylphenol)

Background: Today, propofol or 2,6-diisopropylphenol is the anesthetic mainly used for monitored anesthetic care sedation and during intravenous anesthesia. The formulation, a lipid macroemulsion, shows several disadvantages. Therefore, during the past years considerable scientific effort has been undertaken to find either a better formulation or a prodrug of propofol. Fospropofol is the first propofol prodrug that has been intensively studied in man. It has been licensed in 2008 by the FDA for monitored anesthetic care sedation. Objectives and methods: This review describes first published study results of fospropofol with regard to its pharmacokinetics/pharmacodynamics, drug safety, tolerability and drug side effects. Using a Medline search all published articles and abstracts containing the words fospropofol or GPI 15715 were included. Results and conclusion: As the impact of an errorness drug assay for propofol liberated from fospropofol is not exactly defined, no clear conclusions can be drawn from the first published pharmacokinetic/pharmacodynamic studies. Fospropofol was well tolerated in the first two clinical studies and no serious side effects were reported. After characterization of the true pharmacokinetic/pharmacodynamics profile, fospropofol, an aqueous solution, has the potential to favorably compare with benzodiazepines for procedural sedation and also may be used for long-term sedation and intravenous anesthesia.