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Fospropofol
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| Clinical data | |
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| AHFS/Drugs.com | Monograph |
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| Dependence liability | unknown |
| Routes of administration | Intravenous |
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| Pharmacokinetic data | |
| Protein binding | 98%[1] |
| Metabolism | Hepatic glucuronidation |
| Elimination half-life | 0.81 hours[1] |
| Excretion | Renal |
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| Chemical and physical data | |
| Formula | C13H21O5P |
| Molar mass | 288.280 g·mol−1 |
| 3D model (JSmol) | |
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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
[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.[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
[edit]Mechanism of action
[edit]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
[edit]Pharmacokinetics
[edit]Initial trial results on fospropofol pharmacokinetics were retracted by the investigators. As of 2011, new results were not available.[7]
Distribution
[edit]Following the administration of fospropofol 12.5 mg/kg (the maximum recommended dose) loss of consciousness takes about four minutes, compared to one arm-brain circulation time with propofol 2.5 mg/kg (the maximum recommended dose).[8]
Metabolism
[edit]Fospropofol is metabolized in the liver by alkaline phosphatases to propofol, formaldehyde, and phosphate. The hepatic metabolism of this prodrug to an active metabolite means that peak plasma levels of propofol after the administration of a bolus of fospropofol are lower than for an equipotent dose of propofol and also that its clinical effect is more sustained.[9][10] These features can be desirable for endoscopic procedures such as esophagogastroduodenoscopy, colonoscopy, bronchoscopy, as well as for some surgical procedures done under local or regional anesthesia.
Propofol is further metabolised to propofol glucuronide (34.8%) and quinol glucuronide.[11] Formaldehyde is a known carcinogen but label information states that serum formaldehyde levels are similar to background levels. No long term studies have been done on the cancer risks. The parent drug has a terminal elimination half-life of 0.88+/-0.08 hours, which is non-renal.[12]
Controlled substance
[edit]Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.[13]
See also
[edit]References
[edit]- ^ a b "LUSEDRA (fospropofol disodium) Injection" (PDF). Woodcliff Lake, New Jersey: Eisai Inc. October 2009. Archived from the original (PDF) on 22 November 2010. Retrieved 2 August 2010.
- ^ "Fospropofol disodium". PubChem Compound. Bethesda, Maryland: U.S. National Library of Medicine. Retrieved 9 February 2017.
- ^ "Recommended INNs 2006, pt 56" (PDF). World Health Organization. Retrieved 20 April 2016.
- ^ "FDA Approves Fospropofol and Follows ASAs Labeling Recommendation". American Society of Anesthesiologists. 2008-12-15. Archived from the original on 2011-05-26. Retrieved 2011-03-30.
- ^ Cooke A, Anderson A, Buchanan K, Byford A, Gemmell D, Hamilton N, et al. (April 2001). "Water-soluble propofol analogues with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters. 11 (7): 927–930. doi:10.1016/S0960-894X(01)00088-9. PMID 11294393.
- ^ Bennett DJ, Anderson A, Buchanan K, Byford A, Cooke A, Gemmell DK, et al. (June 2003). "Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity". Bioorganic & Medicinal Chemistry Letters. 13 (12): 1971–1975. doi:10.1016/S0960-894X(03)00346-9. PMID 12781176.
- ^ Mahajan B, Kaushal S, Mahajan R (January 2012). "Fospropofol: pharmacokinetics?". Journal of Anaesthesiology Clinical Pharmacology. 28 (1): 134–135. doi:10.4103/0970-9185.92472. PMC 3275955. PMID 22345970.
- ^ Gan TJ (2006). "Pharmacokinetic and pharmacodynamic characteristics of medications used for moderate sedation". Clinical Pharmacokinetics. 45 (9): 855–869. doi:10.2165/00003088-200645090-00001. PMID 16928150. S2CID 19952165.
- ^ Fechner J, Schwilden H, Schüttler J (2008). "Pharmacokinetics and pharmacodynamics of GPI 15715 or fospropofol (Aquavan injection) - a water-soluble propofol prodrug". Modern Anesthetics. Handbook of Experimental Pharmacology. Vol. 182. pp. 253–66. doi:10.1007/978-3-540-74806-9_12. ISBN 978-3-540-72813-9. PMID 18175095.
- ^ Shah A, Mistry B, Gibiansky E, Gibiansky L (January 2009). "Fospropofol assay: issues and impact on pharmacokinetic and pharmacodynamic evaluation". European Journal of Anaesthesiology. 26 (1): 81, discussion 81-81, discussion 82. doi:10.1097/EJA.0b013e32831bc285. PMID 19122558. S2CID 10033756.
- ^ "Propofol Monograph for Professionals". Drugs.com. 2024-06-10. Retrieved 2025-01-28.
- ^ "LUSEDRA (fospropofol disodium) Injection, for intravenous use" (PDF). Archived from the original (PDF) on February 16, 2017. Retrieved 2025-01-27.
- ^ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV[permanent dead link]," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.