"# Garnock-Jones KP, Scott LJ: Fospropofol. Drugs. 2010 Mar 5;70(4):469-77. doi: 10.2165/11204450-000000000-00000. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/20205488 # Schywalsky M, Ihmsen H, Tzabazis A, Fechner J, Burak E, Vornov J, Schwilden H: Pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 in rats. Eur J Anaesthesiol. 2003 Mar;20(3):182-90. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/12650488 # Bengalorkar GM, Bhuvana K, Sarala N, Kumar T: Fospropofol: clinical pharmacology. J Anaesthesiol Clin Pharmacol. 2011 Jan;27(1):79-83. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/21804712 # Garnock-Jones KP, Scott LJ: Fospropofol. Drugs. 2010 Mar 5;70(4):469-77. doi: 10.2165/11204450-000000000-00000. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/20205488 # Patwardhan A, Edelmayer R, Annabi E, Price T, Malan P, Dussor G: Receptor specificity defines algogenic properties of propofol and fospropofol. Anesth Analg. 2012 Oct;115(4):837-40. Epub 2012 May 14. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/22584560"@en . . . . . "approved"@en . "Total body clearance (CLp), Fospropofol, healthy subject = 0.28 L/h/kg; CLp, fospropofol, patients = 0.31 L/h/kg; CLp/F, propofol, healthy subjects or patients = 2.74 L/h/kg. "@en . . . . . "For monitored anaesthesia care sedation in patients undergoing diagnostic procedures like bronchoscopy and colonscopy or minor surgical procedures like arthroscopy and bunionectomy. "@en . "Overdosage may lead to cardiorespiratory depression, formic acid toxicity (methanol toxicity-like effects), and/or phosphate-induced hypocalemia. Most common adverse reactions (> 20%) are paresthesia and pruritus."@en . " "@en . . . . " "@en . . . . "After in-vivo conversion of fospropofol into propofol by endothelial alkaline phosphatase, propofol crosses the blood-brain barrier, binds to GABA-A receptors and acts as an agonist. By binding to GABA-A receptor, it will cause an increase in chloride conductance, thus inhibiting the firing of new action potentials in the post-synaptic neuron. "@en . . "Adequate sedation achieved after 7 minutes with a IV bolus dose of 10mg/kg. It takes 21-45 minutes for patients to recover for fospropopol-induced sedation. Following an intravenous bolus administration of 6 mg/kg in a healthy subject, the pharmacokinetic parameters of fospropofol are as follows: Cmax = 78.7 \u03BCg/mL; Tmax = 4 minutes; AUC(0-\u221E) = 19.0 \u03BCg \u22C5 h/mL; "@en . . . "Both fospropofol and its active metabolite propofol are highly protein bound (approximately 98%), primarily to albumin. Fospropofol does not affect the binding of propofol to albumin. "@en . . . . . . "Fospropofol = 0.33\u00B10.069 L/kg; Propofol metabolite = 5.8 L/kg. "@en . . . . . . . . "Fospropofol is a water soluble prodrug and is converted to propofol in the liver. Fospropofol is a short acting hypnotic/sedative/anesthetic agent. Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1. FDA approved in December 2008. Fospropofol is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act."@en . . . . . . "Fospropofol"@en . "When given to a patient, the half-lives are as follows: Fospropofol = 0.81 hours; Propofol metabolite = 1.13 hours "@en . . . . "Fospropofol"@en . "illicit"@en . . "258516-87-9"@en . "Chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney. There is negligible renal elimination of unchanged fospropofol (<0.02%). "@en . . . "Humans and other mammals"@en .