Fospropofol Explained

Fospropofol (INN^[1]), often used as the disodium salt (trade name Lusedra^[2]) 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.^{[3] [4]} 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; as an organophosphate it is metabolized by alkaline phosphatases to phosphate and formaldehyde and the active metabolite, propofol.

Pharmacokinetics

Initial trial results on fospropofol pharmacokinetics were retracted by the investigators. As of 2011, new results were not available.^[5]

Controlled substance

Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.^[6]

See also

• Ciprofol

Notes and References

1. Web site: Recommended INNs 2006, pt 56. World Health Organization. 20 April 2016.
2. Web site: FDA Approves Fospropofol and Follows ASAs Labeling Recommendation . American Society of Anesthesiologists . 2008-12-15 . 2011-03-30 . https://web.archive.org/web/20110526075212/http://www.asahq.org/news/asanews121508.htm . 2011-05-26 . dead .
3. Cooke A, Anderson A, Buchanan K, Byford A, Gemmell D, Hamilton N, McPhail P, Miller S, Sundaram H, Vijn P . 6 . Water-soluble propofol analogues with intravenous anaesthetic activity . Bioorganic & Medicinal Chemistry Letters . 11 . 7 . 927–930 . April 2001 . 11294393 . 10.1016/S0960-894X(01)00088-9 .
4. Bennett DJ, Anderson A, Buchanan K, Byford A, Cooke A, Gemmell DK, Hamilton NM, Maidment MS, McPhail P, Stevenson DF, Sundaram H, Vijn P . 6 . Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity . Bioorganic & Medicinal Chemistry Letters . 13 . 12 . 1971–1975 . June 2003 . 12781176 . 10.1016/S0960-894X(03)00346-9 .
5. Mahajan B, Kaushal S, Mahajan R . Fospropofol: pharmacokinetics? . Journal of Anaesthesiology Clinical Pharmacology . 28 . 1 . 134–135 . January 2012 . 22345970 . 3275955 . 10.4103/0970-9185.92472 . free .
6. "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234 - 51236.