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Fospropofol
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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%
Metabolism Hepatic glucuronidation
Elimination half-life 0.81 hours
Excretion Renal
Identifiers
  • disodium [2,6-di(propan-2-yl)phenoxy]methyl phosphate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C13H21O5P
Molar mass 288.280 g·mol−1
3D model (JSmol)
  • CC(C)c1cccc(c1OCOP(=O)(O)O)C(C)C
  • InChI=1S/C13H21O5P/c1-9(2)11-6-5-7-12(10(3)4)13(11)17-8-18-19(14,15)16/h5-7,9-10H,8H2,1-4H3,(H2,14,15,16) ☒N
  • Key:QVNNONOFASOXQV-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Fospropofol (INN), often used as the disodium salt (trade name Lusedra) 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. 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.


Controlled substance

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

See also


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