About: Methylnaltrexone     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...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 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • terminal: 8.89 ± 2.59 h (intravenous) terminal: 6.14- 8.83 h (subcutaneous) (en)
http://linked.open...ugbank/indication
  • Treatment of opioids induced constipation in palliative patients that are inadequately responding to laxative therapy. (en)
sameAs
Title
  • Methylnaltrexone (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • 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. (en)
http://linked.open.../drugbank/synonym
  • Methylnaltrexone (en)
  • MNTX (en)
http://linked.open...drugbank/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. (en)
http://linked.open...umeOfDistribution
  • Volume of distribution, steady state = 1.1 L/kg (en)
http://linked.open...nk/proteinBinding
  • 11% to 15% bound to human plasma proteins. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Harold Doshan, Julio Perez, "Synthesis of R-N-methylnaltrexone." U.S. Patent US20070099946, issued May 03, 2007. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/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; (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 73232-52-7 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • 10.5 ± 1.5 ml/min/kg (IV) (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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