Fospropofol

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Fospropofol
Fospropofol disodium.svg
Clinical data
AHFS/Drugs.com Monograph
License data
Pregnancy
category
  • B
Dependence
liability
unknown
Routes of
administration
Intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding 98%[1]
Metabolism Hepatic glucuronidation
Biological half-life 0.81 hours[1]
Excretion Renal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.217.213
Chemical and physical data
Formula C13H21O5P
Molar mass 332.243[2]
3D model (Jmol)
 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[edit]

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.[citation needed] Often, fospropofol is administered in conjunction with an opioid such as fentanyl.[citation needed]

Clinical pharmacology[edit]

Mechanism of action[edit]

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

Pharmacodynamics[edit]

Pharmacokinetics[edit]

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


Controlled substance[edit]

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

References[edit]

  1. ^ a b Eisai Inc. (October 2009). "LUSEDRA (fospropofol disodium) Injection" (PDF). Woodcliff Lake, New Jersey: Eisai Inc. Retrieved 2 August 2010. 
  2. ^ a b 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 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. PMID 11294393. doi:10.1016/S0960-894X(01)00088-9. 
  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. PMID 12781176. doi:10.1016/S0960-894X(03)00346-9. 
  7. ^ Mahajan B, Kaushal S, Mahajan R (January 2012). "Fospropofol: pharmacokinetics?". J Anaesthesiol Clin Pharmacol. 28 (1): 134–5. PMC 3275955Freely accessible. PMID 22345970. doi:10.4103/0970-9185.92472. 
  8. ^ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

Further reading[edit]