New drug, fospropofol disodium: a propofol prodrug.
The use of propofol presents chemical and clinical concerns, including pain on injection, allergy risks, possible bacteria growth, and hyperlipidemia. These concerns have encouraged the search for alternative propofol formulations. Elimination of the soybean oil and lecithin carrier agents is difficult because the highly lipophilic diisopropyl phenol molecule does not dissolve in water. Propofol in aqueous solution would be a preferable alternative to lipid-based emulsions. One formulation of propofol is fospropofol disodium (Lusedra, Eisai Corporation of North America, Woodcliff Lake, New Jersey), previously known as Aquavan (MGI Pharma, Bloomington, Minnesota). Fospropofol is an aqueous solution of a propofol prodrug intended for injection. The discovery and development of this drug may address the concerns with the current propofol emulsion formulations while offering altered pharmacokinetics and pharmacodynamics for sedation. The structure, pharmacokinetics, pharmacodynamics, clinical studies, clinical applications, and implications are discussed.
Welliver
Mark
M
School of Nurse Anesthesia, Harris College of Nursing and Health Sciences, Texas Christian University, Fort Worth, Texas, USA. Mark.welliver@gmail.com
Rugari
Susan M
SM
D018686:Anesthetics, Intravenous; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002986:Clinical Trials as Topic; D016292:Procedural Sedation / Q000009:adverse effects / Q000379:methods; D016903:Drug Monitoring / Q000379:methods; D004655:Emulsions; D006801:Humans; D008657:Metabolic Clearance Rate; D008956:Models, Chemical; D018579:Patient Selection; D011355:Prodrugs / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D015742:Propofol / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D012995:Solubility; D012996:Solutions
D018686:Anesthetics, Intravenous; D004655:Emulsions; D011355:Prodrugs; D012996:Solutions; C472965:fospropofol; D015742:Propofol