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File:Fospropofol disodium.png
Systematic (IUPAC) name
disodium [2,6-di(propan-2-yl)phenoxy]methyl phosphate[1]
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]
  • B
Routes of
Legal status
Legal status
Pharmacokinetic data
Protein binding 98%[2]
Metabolism Hepatic glucuronidation
Biological half-life 0.81 hours[2]
Excretion Renal
CAS Number 258516-87-9
ATC code N01
PubChem CID 3038497
Chemical data
Formula C13H19Na2O5P
Molar mass 332.240261 g/mol[1][[Script error: No such module "String".]]
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Fospropofol (trade name Lusedra[3]) 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.[4][5] 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.[citation needed] Often, fospropofol is administered in conjunction with an opioid such as fentanyl.[citation needed]

Warnings and precautions

Drug interactions

Clinical pharmacology

Mechanism of action

Fospropofol is a prodrug of propofol; it is metabolized by alkaline phosphatases to an active metabolite, propofol. One millimole (mmol) of propofol is generated for each mmol of fospropofol sodium administered. 1.86 mg of fospropofol sodium is the molar equivalent of 1 mg propofol.




Following the administration of fospropofol 12.5 mg/kg (the maximum recommended dose) loss of consciousness takes about four minutes, compared to one arm-brain circulation time with propofol 2.5 mg/kg (the maximum recommended dose).[6]


Fospropofol is metabolized in the liver by alkaline phosphatases to propofol, formaldehyde, and phosphate. The hepatic metabolism of this prodrug to an active metabolite means that peak plasma levels of propofol after the administration of a bolus of fospropofol are lower than for an equipotent dose of propofol and also that its clinical effect is more sustained.[7][8] These features can be desirable for endoscopic procedures such as esophagogastroduodenoscopy, colonoscopy, bronchoscopy, as well as for some surgical procedures done under local or regional anesthesia.

Propofol is further metabolised to propofol glucuronide (34.8%) and quinol glucuronide.[citation needed] Formaldehyde is a known carcinogen but label information states that serum formaldehyde levels are similar to background levels. No long term studies have been done on the cancer risks. The parent drug has a terminal elimination half-life of 0.88+/-0.08 hours, which is non-renal.[9]


Controlled substance

Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.[10]

See also


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Further reading

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  • Pruitt R, Cohen LB, Gibiansky E, et al. A randomized, open-label, multicenter, dose-ranging study of sedation with Aquavan injection (GPI 15714) during colonoscopy. Gastrointest Endosc 2005; 61: AB111.
  • Lampotang S, Lizdas D, Gravenstein N, Yavas S (2006): Web Simulation of Fospropofol Pharmacokinetics. Retrieved 18 March 2008, from University of Florida Department of Anesthesiology Virtual Anesthesia Machine Web site: [1]

External links

  1. 1.0 1.1 PubChem Compound. "fospropofol disodium - Compound Summary (CID 3038497)". Bethesda, Maryland: National Center for Biotechnology Information. Retrieved 2 August 2010.  External link in |publisher= (help)
  2. 2.0 2.1 Eisai Inc. (October 2009). "LUSEDRA™ (fospropofol disodium) Injection" (PDF). Woodcliff Lake, New Jersey: Eisai Inc. Retrieved 2 August 2010.  External link in |publisher= (help)
  4. Cooke A, Anderson A, Buchanan K, Byford A, Gemmell D, Hamilton N, McPhail P, Miller S, Sundaram H, Vijn P. Water-soluble propofol analogues with intravenous anaesthetic activity. Bioorganic and Medicinal Chemistry Letters. 2001 Apr 9;11(7):927-30. PMID 11294393
  5. Bennett DJ, Anderson A, Buchanan K, Byford A, Cooke A, Gemmell DK, Hamilton NM, Maidment MS, McPhail P, Stevenson DF, Sundaram H, Vijn P. Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity. Bioorganic and Medicinal Chemistry Letters. 2003 Jun 16;13(12):1971-5. PMID 12781176
  6. Gan TJ (2006). "Pharmacokinetic and pharmacodynamic characteristics of medications used for moderate sedation". Clin Pharmacokinet. 45 (9): 855–69. doi:10.2165/00003088-200645090-00001. PMID 16928150. 
  7. Fechner J, Schwilden H, Schüttler J. Pharmacokinetics and pharmacodynamics of GPI 15715 or fospropofol (Aquavan injection) - a water-soluble propofol prodrug. Handbook of Experimental Pharmacology. 2008;(182):253-66. PMID 18175095
  8. Shah A, Mistry B, Gibiansky E, Gibiansky L. Fospropofol assay: issues and impact on pharmacokinetic and pharmacodynamic evaluation. European Journal of Anaesthesiology. 2009 Jan;26(1):81; discussion 81-2. PMID 19122558
  9. [2]
  10. "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.