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Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n10http://linked.opendata.cz/resource/drugbank/drug/DB06800/identifier/wikipedia/
foafhttp://xmlns.com/foaf/0.1/
n15http://linked.opendata.cz/resource/drugbank/dosage/
n8http://www.rxlist.com/
n6http://bio2rdf.org/drugbank:
n11http://linked.opendata.cz/resource/drugbank/drug/DB06800/identifier/kegg-drug/
admshttp://www.w3.org/ns/adms#
n16http://linked.opendata.cz/resource/drugbank/drug/DB06800/identifier/drugbank/
n13http://linked.opendata.cz/resource/drugbank/patent/
n12http://linked.opendata.cz/resource/drugbank/drug/DB06800/identifier/national-drug-code-directory/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
owlhttp://www.w3.org/2002/07/owl#
n3http://linked.opendata.cz/ontology/drugbank/
n14http://www.drugs.com/cdi/
n4http://linked.opendata.cz/resource/drugbank/property/
xsdhhttp://www.w3.org/2001/XMLSchema#

Statements

Subject Item
n2:DB06800
rdf:type
n3:Drug
n3:description
Methylnaltrexone is a pheriphally-acting μ-opioid antagonists that acts on the gastrointestinal tract to decrease opioid-induced constipation without producing analgesic effects or withdrawal symptoms. It is also a weak CYP2D6 inhibitor. FDA approved in 2008.
n3:dosage
n15:271B549C-363D-11E5-9242-09173F13E4C5 n15:271B549D-363D-11E5-9242-09173F13E4C5 n15:271B549A-363D-11E5-9242-09173F13E4C5 n15:271B549B-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Thomas J: Opioid-induced bowel dysfunction. J Pain Symptom Manage. 2008 Jan;35(1):103-13. Epub 2007 Nov 5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17981003 # Rotshteyn Y, Boyd TA, Yuan CS: Methylnaltrexone bromide: research update of pharmacokinetics following parenteral administration. Expert Opin Drug Metab Toxicol. 2011 Feb;7(2):227-35. doi: 10.1517/17425255.2011.549824. Epub 2011 Jan 11. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21222554 # Chandrasekaran A, Tong Z, Li H, Erve JC, DeMaio W, Goljer I, McConnell O, Rotshteyn Y, Hultin T, Talaat R, Scatina J: Metabolism of intravenous methylnaltrexone in mice, rats, dogs, and humans. Drug Metab Dispos. 2010 Apr;38(4):606-16. doi: 10.1124/dmd.109.031179. Epub 2010 Jan 6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20053817 # Bader S, Jaroslawski K, Blum HE, Becker G: Opioid-induced constipation in advanced illness: safety and efficacy of methylnaltrexone bromide. Clin Med Insights Oncol. 2011;5:201-11. doi: 10.4137/CMO.S4867. Epub 2011 Jul 14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/21836816 # FDA label
n3:group
approved
n3:halfLife
terminal: 8.89 ± 2.59 h (intravenous) terminal: 6.14- 8.83 h (subcutaneous)
n3:indication
Treatment of opioids induced constipation in palliative patients that are inadequately responding to laxative therapy.
owl:sameAs
n6:DB06800
dcterms:title
Methylnaltrexone
adms:identifier
n10:Methylnaltrexone n11:D06618 n12:0008-1225-10 n16:DB06800
n3:mechanismOfAction
Methylnaltrexone is a pheriphally-acting μ-opioid antagonists that acts on the gastrointestinal tract inhibit opioid-induced decrease in gastric motility and transit time. Because methylnaltrexone is a quaternary derivative of naltrexone, it produces its gastrointestinal effects without producing analgesic effects or withdrawal symptoms as it does not cross the blood-brain-barrier.
n3:patent
n13:8420663 n13:8247425 n13:6559158
n3:routeOfElimination
Most of the drug is eliminated as unchanged drug (85% of administered radioactivity). Approximately half of the dose is excreted in the urine and somewhat less in feces.
n3:synonym
Methylnaltrexone MNTX
n3:toxicity
LD50: 50 mg/kg (primates); Orthostatic hypotension at plasma levels in excess of 1.400 ng/mL. The most common (>5%) adverse reactions reported with methylnaltrexone bromide are abdominal pain, flatulence, nausea, dizziness, diarrhea and hyperhidrosis.
n3:volumeOfDistribution
Volume of distribution, steady state = 1.1 L/kg
n3:proteinBinding
11% to 15% bound to human plasma proteins.
n3:salt
n3:synthesisReference
Harold Doshan, Julio Perez, "Synthesis of R-N-methylnaltrexone." U.S. Patent US20070099946, issued May 03, 2007.
foaf:page
n8:relistor-drug.htm n14:methylnaltrexone.html
n3:IUPAC-Name
n4:271B54A2-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B54A8-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B54A7-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B54A4-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B54A5-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B54A6-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B54A0-363D-11E5-9242-09173F13E4C5 n4:271B54B8-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B549E-363D-11E5-9242-09173F13E4C5 n4:271B54A1-363D-11E5-9242-09173F13E4C5 n4:271B54B9-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B549F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Acceptor-Count
n4:271B54AE-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B54AF-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B54A9-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B54AA-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B54AC-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B54AB-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B54AD-363D-11E5-9242-09173F13E4C5
n3:absorption
Methylnaltrexone is rapidly absorbed. Tmax (SubQ): 30 minutes (regardless of dose); Cmax, 0.15 mg/kg SubQ dose = 117 ng/mL; AUC24, 0.15 mg/kg SubQ dose = 175 ng·hr/mL;
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
73232-52-7
n3:category
n3:clearance
10.5 ± 1.5 ml/min/kg (IV)
n3:Bioavailability
n4:271B54B4-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B54B6-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B54B7-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B54B3-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B54B2-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B54B5-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B54A3-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B54B0-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B54B1-363D-11E5-9242-09173F13E4C5