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Fospropofol

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Subject: Sigmodal, Tetronal, Metomidate, Sodium thiopental, Alcoholic beverage
Collection: Gabaa Receptor Positive Allosteric Modulators, General Anesthetics, Phenol Ethers, Prodrugs, Sedatives
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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
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  YesY
ATC code N01
PubChem CID:
DrugBank  N
UNII  N
KEGG  YesY
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.

Contents

  • Clinical applications 1
  • Clinical pharmacology 2
    • Mechanism of action 2.1
    • Pharmacodynamics 2.2
    • Pharmacokinetics 2.3
  • Controlled substance 3
  • References 4
  • Further reading 5

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

  1. ^ a b
  2. ^ a b
  3. ^
  4. ^
  5. ^
  6. ^
  7. ^ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.

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:


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