About: Tapentadol

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

Attributes	Values
rdf:type	http://linked.opendata.cz/ontology/drugbank/Drug
http://linked.open...gbank/description	Opioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008. (en)
http://linked.open...y/drugbank/dosage	http://linked.opendata.cz/resource/drugbank/dosage/271B49F6-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B49F7-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B49F8-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B49F9-363D-11E5-9242-09173F13E4C5 http://linked.opendata.cz/resource/drugbank/dosage/271B49FA-363D-11E5-9242-09173F13E4C5
http://linked.open...generalReferences	# Tzschentke TM, Christoph T, Kogel B, Schiene K, Hennies HH, Englberger W, Haurand M, Jahnel U, Cremers TI, Friderichs E, De Vry J: (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007 Oct;323(1):265-76. Epub 2007 Jul 26. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17656655 # Gohler K, Brett M, Smit JW, Rengelshausen J, Terlinden R: Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations. Int J Clin Pharmacol Ther. 2013 Apr;51(4):338-48. doi: 10.5414/CP201722. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23357834 # Xu XS, Smit JW, Lin R, Stuyckens K, Terlinden R, Nandy P: Population pharmacokinetics of tapentadol immediate release (IR) in healthy subjects and patients with moderate or severe pain. Clin Pharmacokinet. 2010 Oct;49(10):671-82. doi: 10.2165/11535390-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20818833 (en)
http://linked.open...gy/drugbank/group	approved (en)
http://linked.open...drugbank/halfLife	Elimination half-life, IV: 4 hours. (en)
http://linked.open...ugbank/indication	The immediate-release formulation of tapentadol is indicated for the relief of moderate to severe acute pain. The long-acting formulation serves as a continuous, around-the-clock analgesic that is indicated for the relief of moderate to severe chronic pain or neuropathic pain associated with diabetic peripheral neuropathy. (en)
sameAs	Tapentadol
Title	Tapentadol (en)
adms:identifier	http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/chemspider/8013742 http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/drugbank/DB06204 http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/kegg-drug/D06007 http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/national-drug-code-directory/35356-525-30 http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/pubchem-compound/9838022 http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/pubchem-substance/47207665 http://linked.opendata.cz/resource/drugbank/drug/DB06204/identifier/wikipedia/Tapentadol
http://linked.open...mechanismOfAction	Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition. (en)
http://linked.open...y/drugbank/patent	http://linked.opendata.cz/resource/drugbank/patent/6071970 http://linked.opendata.cz/resource/drugbank/patent/RE39593
http://linked.open...outeOfElimination	Tapentadol and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug. (en)
http://linked.open.../drugbank/synonym	Tapentadol (en) BN-200 (en) CG-5503 (en) Nucynta (en)
http://linked.open...drugbank/toxicity	Oral, rabbit: LD50 = 3200 mg/kg; Oral, mouse: LD50 = 300 mg/kg; Oral, rat: LD50: 980 mg/kg; The most common reasons for discontinuation due to adverse events were dizziness, nausea, vomiting, somnolence, and headache. (en)
http://linked.open...umeOfDistribution	Following IV administration, volume of distribution is 540 ± 98 L. (en)
http://linked.open...k/foodInteraction	Food increases the AUC and Cmax of tapentadol. Despite this, tapentadol can be given without regards to food. (en)
http://linked.open...nk/proteinBinding	~20% (en)
http://linked.open...ogy/drugbank/salt	(en)
http://linked.open...ynthesisReference	Giuseppe Motta, Domenico Vergani, Giorgio Bertolini, "PROCESS FOR THE PREPARATION OF TAPENTADOL AND INTERMEDIATES THEREOF." U.S. Patent US20120232306, issued September 13, 2012. (en)
foaf:page	http://www.drugs.com/monograph/tapentadol-hydrochloride.html http://www.rxlist.com/nucynta-drug.htm
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http://linked.open...ugbank/absorption	Bioavailability, immediate release (IR), 86 mg: 32%; Bioavailability, extended release (ER), 86 mg: 32%; Cmax, IR: 64.2 ng/mL; Cmax, ER: 22.5 ng/mL; T max, IR: 1.5 hours; T max, ER: 5.0 hours; Tapentadol accumulates following multiple repeat doses. (en)
http://linked.open.../affectedOrganism	Humans and other mammals (en)
http://linked.open...casRegistryNumber	175591-23-8 (en)
http://linked.open...rugbank/clearance	Total clearance = 1530 ± 177 ml/min. (en)
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