Fospropofol

Fospropofol

Systematic (IUPAC) name
disodium [2,6-di(propan-2-yl)phenoxy]methyl phosphate[1]
Clinical data
AHFS/Drugs.com	monograph
Licence data	US FDA:link
Pregnancy cat.	B
Legal status	Schedule IV (US)
Dependence liability	unknown
Routes	Intravenous
Pharmacokinetic data
Protein binding	98%[2]
Metabolism	Hepatic glucuronidation
Half-life	0.81 hours[2]
Excretion	Renal
Identifiers
CAS number	258516-87-9 Y
ATC code	N01
PubChem	CID 3038497
DrugBank	DB06716
UNII	LZ257RZP7K N
KEGG	D04257 Y
ChEMBL	CHEMBL1201766 N
Chemical data
Formula	C13H19Na2O5P
Mol. mass	332.240261 g/mol[1]
N (what is this?)  (verify)

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]}

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

• 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. 

External links