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 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 YesY
ATC code N01
PubChem CID 3038497
DrugBank DB06716
UNII LZ257RZP7K N
KEGG D04257 YesY
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[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.[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[edit]

Mechanism of action[edit]

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[edit]

Pharmacokinetics[edit]

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


Controlled substance[edit]

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

References[edit]

  1. ^ a b PubChem Compound. = pccompound&term = fospropofol "fospropofol disodium - Compound Summary (CID 3038497)". Bethesda, Maryland: National Center for Biotechnology Information. Retrieved 2 August 2010. 
  2. ^ a b Eisai Inc. (October 2009). "LUSEDRA (fospropofol disodium) Injection". Woodcliff Lake, New Jersey: Eisai Inc. Retrieved 2 August 2010. 
  3. ^ "FDA Approves Fospropofol and Follows ASAs Labeling Recommendation". American Society of Anesthesiologists. 2008-12-15. Retrieved 2011-03-30. 
  4. ^ Cooke, A; Anderson, A; Buchanan, K; Byford, A; Gemmell, D; Hamilton, N; McPhail, P; Miller, S et al. (2001). "Water-soluble propofol analogues with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters 11 (7): 927–30. doi:10.1016/S0960-894X(01)00088-9. PMID 11294393. 
  5. ^ Bennett, DJ; Anderson, A; Buchanan, K; Byford, A; Cooke, A; Gemmell, DK; Hamilton, NM; Maidment, MS et al. (2003). "Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters 13 (12): 1971–5. doi:10.1016/S0960-894X(03)00346-9. PMID 12781176. 
  6. ^ Mahajan B, Kaushal S, Mahajan R (January 2012). "Fospropofol: pharmacokinetics?". J Anaesthesiol Clin Pharmacol 28 (1): 134–5. doi:10.4103/0970-9185.92472. PMC 3275955. PMID 22345970. 
  7. ^ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

Further reading[edit]

External links[edit]