Fospropofol

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.

Fospropofol
Clinical data
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • B
Dependence
liability		unknown
Routes of
administration		Intravenous
ATC code
Legal status
Legal status
  • US: Schedule IV
Pharmacokinetic data
Protein binding98%[1]
MetabolismHepatic glucuronidation
Elimination half-life0.81 hours[1]
ExcretionRenal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC13H21O5P
Molar mass332.243[2] g·mol−1
3D model (JSmol)
 NY (what is this?)  (verify)

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.

Pharmacodynamics

Pharmacokinetics

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]

References
  1. Eisai Inc. (October 2009). "LUSEDRA (fospropofol disodium) Injection" (PDF). Woodcliff Lake, New Jersey: Eisai Inc. Retrieved 2 August 2010.
  2. PubChem Compound. "Compound Summary for CID 3038497): Fospropofol disodium". Bethesda, Maryland: National Center for Biotechnology Information. Retrieved 9 February 2017.
  3. "Recommended INNs 2006, pt 56" (PDF). World Health Organization. World Health Organization. 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 3275955. PMID 22345970.
  8. "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

Further reading
  • Fechner J, Ihmsen H, Hatterscheid D, et al. (September 2004). "Comparative pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 and propofol emulsion". Anesthesiology. 101 (3): 626–39. doi:10.1097/00000542-200409000-00011. PMID 15329587. (Retracted, see PMID 22345970)
  • Gibiansky E, Struys MM, Gibiansky L, et al. (October 2005). "AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 1): pharmacokinetics". Anesthesiology. 103 (4): 718–29. doi:10.1097/00000542-200510000-00010. PMID 16192764. (Retracted, see PMID 22345970)
  • Struys MM, Vanluchene AL, Gibiansky E, et al. (October 2005). "AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 2): pharmacodynamics and safety". Anesthesiology. 103 (4): 730–43. doi:10.1097/00000542-200510000-00011. PMID 16192765. (Retracted, see PMID 22345970)
  • 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). University of Florida Department of Anesthesiology Virtual Anesthesia Machine Web site: "Web Simulation of Fospropofol Pharmacokinetics". University of Florida. Retrieved 2011-03-30.
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