Tapentadol
You don't need to be Editor-In-Chief to add or edit content to WikiDoc. You can begin to add to or edit text on this WikiDoc page by clicking on the edit button at the top of this page. Next enter or edit the information that you would like to appear here. Once you are done editing, scroll down and click the Save page button at the bottom of the page.
| Image:Tapentadol.svg | |
| Image:Tapentadol 3D.png | |
| Tapentadol
| |
| Systematic (IUPAC) name | |
| 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2- methylpropyl]phenol hydrochloride | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C14H24NO |
| Mol. mass | 257.799 g/mol |
| SMILES | & |
| Synonyms | Tapentadol hydrochloride BN-200 CG-5503 R-331333 |
| Pharmacokinetic data | |
| Bioavailability | 31.9 ± 6.8% (oral)[1] |
| Metabolism | Hepatic glucuronidation and sulfate conjugation |
| Half life | ? |
| Excretion | Renal (>95%) and fecal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | ? |
Tapentadol (INN) is a centrally-acting analgesic with a unique dual mode of action as an agonist at the μ-opioid receptor and as a norepinephrine reuptake inhibitor.[2] It is considered to have a potency between morphine and tramadol.[3]
Its dual mode of action provides analgesia at similar levels of more potent narcotic analgesics such as hydrocodone, oxycodone, and morphine with a more tolerable side effect profile.
Tapentadol was developed by Grünenthal in conjunction with Johnson & Johnson Pharmaceutical Research and Development. It is currently undergoing phase III clinical trials. If approved, it would be the first new drug in its class in more than 25 years.[4]
Adverse effects
Nausea, dizziness, constipation, and CNS sedation are common side effects of opioid pain medications. In phase II trials, tapentadol has been shown to provide equianalgesic effect with a lower incidence of side effects compared to oxycodone and morphine. One trial, sponsored by Grünenthal, comparing tapentadol to morphine and ibuprofen for relief of postoperative pain found tapentadol to cause less nausea and dizziness than morphine, with no significant difference in the incidence of vomiting or drowsiness.[5]
References
- ↑ Terlinden R, Ossig J, Fliegert F, Gohler K (2006). "Pharmacokinetics, excretion and metabolism of tapentadol HCl, a novel centrally acting analgesic in healthy subjects". Program and abstracts of the 25th Annual Scientific Meeting of the American Pain Society; May 3-6, 2006; San Antonio, Texas. Poster 689.
- ↑ Tzschentke TM, Christoph T, Kögel 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 μ-Opioid Receptor Agonist/Norepinephrine Reuptake Inhibitor with Broad-Spectrum Analgesic Properties. Journal of Pharmacology and Experimental Therapeutics. 2007 Oct;323(1):265-76.
- ↑ Tschentke, T.M. et al. "Tapentadol Hydrochloride." Drugs of the Future. 2006, Vol. 31, Issue 12, p. 1053. DOI: 10.1358/dof.2006.031.12.1047744
- ↑ Krüger-Hellwig, Anke. "Grünenthal GmbH Presents Tapentadol, a Novel Centrally Acting Analgesic, at the 25th Annual Scientific Meeting of The American Pain Society." PR Newswire. June 6, 2006. Retrieved on September 20, 2007.
- ↑ "Two New Analgesics May Help Patients After Bunionectomy", Journal of Anaesthesiology Clinical Pharmacology, September 26 2006. Retrieved on 2007-09-20.
External links
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
