Fospropofol
 | |
| Clinical data | |
|---|---|
| AHFS/Drugs.com | Monograph |
| License data |
|
| Pregnancy category |
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| Dependence liability | unknown |
| Routes of administration | Intravenous |
| ATC code | N01 |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Protein binding | 98%[1] |
| Metabolism | Hepatic glucuronidation |
| Biological half-life | 0.81 hours[1] |
| Excretion | Renal |
| Identifiers | |
| |
| CAS Number |
258516-89-1  258516-87-9 (disodium salt) |
| PubChem (CID) | 3038498 |
| DrugBank |
DB06716 |
| ChemSpider |
2302062 |
| UNII |
LZ257RZP7K |
| KEGG |
D04257  |
| ChEMBL |
CHEMBL1201766 |
| ECHA InfoCard | 100.217.213 |
| Chemical and physical data | |
| Formula | C13H21O5P |
| Molar mass |
288.27 [2] |
| 3D model (Jmol) | Interactive image |
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| (what is this?) (verify) | |
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. 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.
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]
References
- 1 2 Eisai Inc. (October 2009). "LUSEDRA (fospropofol disodium) Injection" (PDF). Woodcliff Lake, New Jersey: Eisai Inc. Retrieved 2 August 2010. External link in
|publisher=(help) - 1 2 PubChem Compound. = pccompound&term = fospropofol "fospropofol disodium - Compound Summary (CID 3038497)" Check
|url=value (help). Bethesda, Maryland: National Center for Biotechnology Information. Retrieved 2 August 2010. External link in|publisher=(help) - ↑ "Recommended INNs 2006, pt 56" (PDF). World Heath Organisation. World Heath Organisation. Retrieved 20 April 2016.
- ↑ "FDA Approves Fospropofol and Follows ASAs Labeling Recommendation". American Society of Anesthesiologists. 2008-12-15. Retrieved 2011-03-30.
- ↑ Cooke, A; Anderson, A; Buchanan, K; Byford, A; Gemmell, D; Hamilton, N; McPhail, P; Miller, S; Sundaram, H; Vijn, P (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.
- ↑ Bennett, DJ; Anderson, A; Buchanan, K; Byford, A; Cooke, A; Gemmell, DK; Hamilton, NM; Maidment, MS; McPhail, P; Stevenson, DFM; Sundaram, H; Vijn, P (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.
- ↑ 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. - ↑ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.
Further reading
- Fechner J, Ihmsen H, Hatterscheid D, et al. (September 2004). "Comparative pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 and propofol emulsion". Anesthesiology. 101 (3): 626–39. doi:10.1097/00000542-200409000-00011. PMID 15329587. (Retracted, see PMID 22345970)
- Gibiansky E, Struys MM, Gibiansky L, et al. (October 2005). "AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 1): pharmacokinetics". Anesthesiology. 103 (4): 718–29. doi:10.1097/00000542-200510000-00010. PMID 16192764. (Retracted, see PMID 22345970)
- Struys MM, Vanluchene AL, Gibiansky E, et al. (October 2005). "AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 2): pharmacodynamics and safety". Anesthesiology. 103 (4): 730–43. doi:10.1097/00000542-200510000-00011. PMID 16192765. (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: "Web Simulation of Fospropofol Pharmacokinetics". University of Florida. Retrieved 2011-03-30.