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Namespace Prefixes

PrefixIRI
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n20http://linked.opendata.cz/resource/AHFS/
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n17http://linked.opendata.cz/resource/drugbank/dosage/
n18http://www.drugs.com/ppa/
n7http://linked.opendata.cz/resource/drugbank/drug/DB06716/identifier/wikipedia/
n12http://www.rxlist.com/
n6http://linked.opendata.cz/resource/drugbank/drug/DB06716/identifier/pharmgkb/
n16http://bio2rdf.org/drugbank:
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n13http://linked.opendata.cz/resource/drugbank/patent/
n9http://wifo5-03.informatik.uni-mannheim.de/drugbank/resource/drugs/
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n3http://linked.opendata.cz/ontology/drugbank/
n4http://linked.opendata.cz/resource/drugbank/property/
n10http://linked.opendata.cz/resource/drugbank/drug/DB06716/identifier/national-drug-code-directory/
xsdhhttp://www.w3.org/2001/XMLSchema#
n19http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06716
rdf:type
n3:Drug
n3:description
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.
n3:dosage
n17:271B50FD-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# 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
n3:group
approved illicit
n3:halfLife
When given to a patient, the half-lives are as follows: Fospropofol = 0.81 hours; Propofol metabolite = 1.13 hours
n3:indication
For monitored anaesthesia care sedation in patients undergoing diagnostic procedures like bronchoscopy and colonscopy or minor surgical procedures like arthroscopy and bunionectomy.
owl:sameAs
n9:DB06716 n16:DB06716
dcterms:title
Fospropofol
adms:identifier
n6:PA165958389 n7:Fospropofol n10:62856-350-08 n14:DB06716 n15:D04257
n3:mechanismOfAction
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.
n3:patent
n13:6204257
n3:routeOfElimination
Chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney. There is negligible renal elimination of unchanged fospropofol (<0.02%).
n3:synonym
Fospropofol
n3:toxicity
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.
n3:volumeOfDistribution
Fospropofol = 0.33±0.069 L/kg; Propofol metabolite = 5.8 L/kg.
n19:hasAHFSCode
n20:28-04-92
n3:proteinBinding
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.
n3:salt
foaf:page
n12:lusedra-drug.htm n18:fospropofol.html
n3:IUPAC-Name
n4:271B5102-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5108-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5107-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5104-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5105-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5106-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5100-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B50FE-363D-11E5-9242-09173F13E4C5 n4:271B5101-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B50FF-363D-11E5-9242-09173F13E4C5
n3:pKa
n4:271B5118-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B510E-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B510F-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5109-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B510A-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B510C-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B510B-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B510D-363D-11E5-9242-09173F13E4C5
n3:absorption
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 μg/mL; Tmax = 4 minutes; AUC(0-∞) = 19.0 μg ⋅ h/mL;
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
258516-87-9
n3:category
n3:clearance
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.
n3:Bioavailability
n4:271B5114-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5116-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5117-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5113-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5112-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5115-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5103-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5110-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5111-363D-11E5-9242-09173F13E4C5