Drugbox
IUPAC_name = dihydrogen (2,6-diisopropylphenoxy)methyl phosphate
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PubChem = 3038497
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C=13 | H=21 | O=5 | P=1
molecular_weight = 288.276 g/mol
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routes_of_administration = Intravenous
Fospropofol is a new sedative / hypnotic / anesthetic drug awaiting FDA approval in the USA. It will be marked under the brand name “Aquavan”.
As a water-soluble prodrug of the popular sedative / hypnotic / anesthetic drug propofol, fospropofol is metabolized into propofol by the liver. This fact means that blood levels of propofol after the administration of a bolus of fospropofol reach lower peak levels than for an equipotent dose of propofol and also that its clinical effect is more sustained. These traits can be desirable for endoscopic procedures such as upper GI endoscopy, colonoscopy, bronchoscopy, as well as for some surgical procedures done under local or regional anesthesia. Often, fospropofol is administered in conjunction with an opioid such as fentanyl.
One advantage of fospropofol is that, being water-soluble, the problems associated with lipid formulated propofol (e.g., pain at the IV catheter site, potential for hyperlipidemia with long-term administration, and an increased chance for bacteremia) are expected to be less frequent.
Following the administration of fospropofol 12.5 mg/kg (the maximum recommended dose) loss of consciousness takes about four minutes, compared to one circulatory time with propofol 2.5 mg/kg (the maximum recommended dose).[cite journal |author=Gan TJ |title=Pharmacokinetic and pharmacodynamic characteristics of medications used for moderate sedation |journal=Clin Pharmacokinet |volume=45 |issue=9 |pages=855–69 |year=2006 |pmid=16928150 |doi= |url=] ]References
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*cite journal |author=Fechner J, Ihmsen H, Hatterscheid D, "et al" |title=Comparative pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 and propofol emulsion |journal=Anesthesiology |volume=101 |issue=3 |pages=626–39 |year=2004 |month=September |pmid=15329587 |doi= |url=http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0003-3022&volume=101&issue=3&spage=626
*cite journal |author=Gibiansky E, Struys MM, Gibiansky L, "et al" |title=AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 1): pharmacokinetics |journal=Anesthesiology |volume=103 |issue=4 |pages=718–29 |year=2005 |month=October |pmid=16192764 |doi= |url=http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0003-3022&volume=103&issue=4&spage=718
*cite journal |author=Struys MM, Vanluchene AL, Gibiansky E, "et al" |title=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 |journal=Anesthesiology |volume=103 |issue=4 |pages=730–43 |year=2005 |month=October |pmid=16192765 |doi= |url=http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0003-3022&volume=103&issue=4&spage=730
*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): Web Simulation of Fospropofol Pharmacokinetics. Retrieved 18 March 2008, from University of Florida Department of Anesthesiology Virtual Anesthesia Machine Web site: [http://vam.anest.ufl.edu/simulations/fospropofolpharmacokinetics.php]
