"# 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 . . . . . "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 . . . "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 . "Humans and other mammals"@en . . . . . . . . . . . . . "BN-200"@en . "Nucynta"@en . "Tapentadol"@en . . . "Tapentadol"@en . . "Giuseppe Motta, Domenico Vergani, Giorgio Bertolini, \"PROCESS FOR THE PREPARATION OF TAPENTADOL AND INTERMEDIATES THEREOF.\" U.S. Patent US20120232306, issued September 13, 2012."@en . "CG-5503"@en . . . "~20% "@en . "Opioid analgesic for treatment of moderate to severe pain. FDA approved on Nov 20, 2008. "@en . . . . . "Food increases the AUC and Cmax of tapentadol. Despite this, tapentadol can be given without regards to food."@en . "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 . . . " "@en . "Total clearance = 1530 \u00B1 177 ml/min. "@en . "175591-23-8"@en . . . "Following IV administration, volume of distribution is 540 \u00B1 98 L. "@en . . . . . . . . . . . . "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 . . . . "Elimination half-life, IV: 4 hours. "@en . . . "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 . "approved"@en .