Chemistry:Fospropofol
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| AHFS/Drugs.com | Monograph |
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| Dependence liability | unknown |
| Routes of administration | Intravenous |
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| Protein binding | 98%[1] |
| Metabolism | Hepatic glucuronidation |
| Elimination half-life | 0.81 hours[1] |
| Excretion | Renal |
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| Formula | C13H21O5P |
| Molar mass | 288.280 g·mol−1 |
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Fospropofol (INN[3]), often used as the disodium salt (trade name Lusedra[4]) 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.[5][6] 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; as an organophosphate it is metabolized by alkaline phosphatases to phosphate and formaldehyde and the active metabolite, propofol.
Pharmacodynamics
Pharmacokinetics
Initial trial results on fospropofol pharmacokinetics were retracted by the investigators. As of 2011, new results were not available.[7]
Controlled substance
Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.[8]
See also
References
- ↑ 1.0 1.1 "LUSEDRA (fospropofol disodium) Injection". Woodcliff Lake, New Jersey: Eisai Inc.. October 2009. http://www.eisai.com/package_inserts/Lusedra%20PI.pdf.
- ↑ "Fospropofol disodium". PubChem Compound. Bethesda, Maryland: U.S. National Library of Medicine. https://pubchem.ncbi.nlm.nih.gov/compound/3038497.
- ↑ "Recommended INNs 2006, pt 56". https://www.who.int/entity/medicines/publications/druginformation/innlists/RL56.pdf?ua=1.
- ↑ "FDA Approves Fospropofol and Follows ASAs Labeling Recommendation". American Society of Anesthesiologists. 2008-12-15. http://www.asahq.org/news/asanews121508.htm.
- ↑ "Water-soluble propofol analogues with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters 11 (7): 927–930. April 2001. doi:10.1016/S0960-894X(01)00088-9. PMID 11294393.
- ↑ "Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters 13 (12): 1971–1975. June 2003. doi:10.1016/S0960-894X(03)00346-9. PMID 12781176.
- ↑ "Fospropofol: pharmacokinetics?". Journal of Anaesthesiology Clinical Pharmacology 28 (1): 134–135. January 2012. doi:10.4103/0970-9185.92472. PMID 22345970.
- ↑ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV[yes|permanent dead link|dead link}}]," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.
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