Fospropofol

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Fospropofol
Fospropofol disodium.svg
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
category
  • B
Legal status
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 Number 258516-87-9 YesY
ATC code N01
PubChem CID: 3038497
DrugBank DB06716 N
UNII LZ257RZP7K N
KEGG D04257 YesY
ChEMBL CHEMBL1201766 N
Chemical data
Formula C13H19Na2O5P
Molecular mass 332.240261 g/mol[1]
 NYesY (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

  1. ↑ 1.0 1.1 Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ 2.0 2.1 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  7. ↑ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

Further reading

  • Lua error in package.lua at line 80: module 'strict' not found. (Retracted, see PMID 22345970)
  • Lua error in package.lua at line 80: module 'strict' not found. (Retracted, see PMID 22345970)
  • Lua error in package.lua at line 80: module 'strict' not found. (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: Lua error in package.lua at line 80: module 'strict' not found.


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