Fospropofol

Fospropofol

Systematic (IUPAC) name
disodium [2,6-di(propan-2-yl)phenoxy]methyl phosphate[1]
Clinical data
AHFS/Drugs.com
Licence data	US FDA:
Pregnancy category	B
Legal status	US: Schedule IV
Dependence liability	unknown
Routes of administration	Intravenous
Pharmacokinetic data
Protein binding	98%[2]
Metabolism	Hepatic glucuronidation
Biological half-life	0.81 hours[2]
Excretion	Renal
Identifiers
CAS Registry Number	Y
ATC code	N01
PubChem	CID:
DrugBank	N
UNII	N
KEGG	Y
ChEMBL	N
Chemical data
Formula	C13H19Na2O5P
Molecular mass	332.240261 g/mol[1]
N

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. 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. Theoretically, one millimole (mmol) of propofol may be generated for each mmol of fospropofol sodium administered. 1.86 mg of fospropofol sodium is the molar equivalent of 1 mg propofol.

Pharmacodynamics

Pharmacokinetics

Initial trial results on fospropofol pharmacokinetics were retracted by the investigators. As of 2011, new results were not available.^[6]

Controlled substance

Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.^[7]

References

Further reading

• (Retracted, see PMID 22345970)
• (Retracted, see PMID 22345970)
• (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: