Clinical data
AHFS/ Monograph
License data
  • B
Routes of
ATC code N01
Legal status
Legal status
Pharmacokinetic data
Protein binding 98%[1]
Metabolism Hepatic glucuronidation
Biological half-life 0.81 hours[1]
Excretion Renal
CAS Number 258516-89-1 N
258516-87-9 (disodium salt)
PubChem (CID) 3038498
DrugBank DB06716 N
ChemSpider 2302062 N
KEGG D04257 YesY
ECHA InfoCard 100.217.213
Chemical and physical data
Formula C13H21O5P
Molar mass


3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

Fospropofol (INN[3]), often used as the disodium salt (trade name Lusedra[4]) is an intravenous sedative-hypnotic agent. It is currently approved for use in sedation of adult patients undergoing diagnostic or therapeutic procedures such as endoscopy.

Clinical applications

Several water-soluble derivatives and prodrugs of the widely used intravenous anesthetic agent propofol have been developed, of which fospropofol has been found to be the most suitable for clinical development thus far.[5][6] Purported advantages of this water-soluble chemical compound include less pain at the site of intravenous administration, less potential for hyperlipidemia with long-term administration, and less chance for bacteremia. Often, fospropofol is administered in conjunction with an opioid such as fentanyl.

Clinical pharmacology

Mechanism of action

Fospropofol is a prodrug of propofol; it is metabolized by alkaline phosphatases to an active metabolite, propofol.


Initial trial results on fospropofol pharmacokinetics were retracted by the investigators. As of 2011, new results were not available.[7]

Controlled substance

Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.[8]


  1. 1 2 Eisai Inc. (October 2009). "LUSEDRA (fospropofol disodium) Injection" (PDF). Woodcliff Lake, New Jersey: Eisai Inc. Retrieved 2 August 2010. External link in |publisher= (help)
  2. 1 2 PubChem Compound. = pccompound&term = fospropofol "fospropofol disodium - Compound Summary (CID 3038497)" Check |url= value (help). Bethesda, Maryland: National Center for Biotechnology Information. Retrieved 2 August 2010. External link in |publisher= (help)
  3. "Recommended INNs 2006, pt 56" (PDF). World Heath Organisation. World Heath Organisation. Retrieved 20 April 2016.
  4. "FDA Approves Fospropofol and Follows ASAs Labeling Recommendation". American Society of Anesthesiologists. 2008-12-15. Retrieved 2011-03-30.
  5. Cooke, A; Anderson, A; Buchanan, K; Byford, A; Gemmell, D; Hamilton, N; McPhail, P; Miller, S; Sundaram, H; Vijn, P (2001). "Water-soluble propofol analogues with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters. 11 (7): 927–30. doi:10.1016/S0960-894X(01)00088-9. PMID 11294393.
  6. Bennett, DJ; Anderson, A; Buchanan, K; Byford, A; Cooke, A; Gemmell, DK; Hamilton, NM; Maidment, MS; McPhail, P; Stevenson, DFM; Sundaram, H; Vijn, P (2003). "Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters. 13 (12): 1971–5. doi:10.1016/S0960-894X(03)00346-9. PMID 12781176.
  7. Mahajan B, Kaushal S, Mahajan R (January 2012). "Fospropofol: pharmacokinetics?". J Anaesthesiol Clin Pharmacol. 28 (1): 134–5. doi:10.4103/0970-9185.92472. PMC 3275955Freely accessible. PMID 22345970.
  8. "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 5123451236.

Further reading

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