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Tapentadol (brand names: Nucynta, Palexia and Tapal) is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI).〔 Its analgesic properties come into effect within thirty-two minutes of oral administration, and last for 4–6 hours. It is similar to tramadol in its dual mechanism of action; namely, its ability to activate the mu opioid receptor and inhibit the reuptake of norepinephrine.〔 Unlike tramadol, it has only weak effects on the reuptake of serotonin and is a significantly more potent opioid with no known active metabolites.〔 Its general potency is somewhere between that of tramadol and morphine, with an analgesic efficacy comparable to that of oxycodone despite a far lower incidence of side effects. It was approved by the US FDA on the 20th of November, 2008,〔(【引用サイトリンク】url=http://www.drugs.com/history/nucynta.html )〕 by the MHRA of the UK on the 4th of February 2011 and by the TGA of Australia on the 24th of December 2010. ==History== Tapentadol was developed by Grünenthal in conjunction with Johnson & Johnson Pharmaceutical Research and Development (as of April 2015, both NUCYNTA and NUCYNTA ER are owned and marketed by Depomed Inc.). It is being marketed as immediate release oral tablets of 50 mg, 75 mg, and 100 mg under the brand name Nucynta, as well as extended release oral tablets of 50 mg, 100 mg, 150 mg, 200 mg, and 250 mg under the brand name Nucynta ER. Dosage for Nucynta immediate-release is initiated with 50–100 mg every 4 to 6 hours to a maximum of 700 mg on the first day of therapy. Thereafter the maximum recommended dose is 600 mg per day. Higher doses have not been clinically studied. Nucynta ER in non-tolerant patients is initiated at 50 mg twice daily (approximately every 12 hours). The maximum recommended daily dose for Nucynta ER is 500 mg. It is the first new drug of the centrally acting analgesic class approved in the United States in more than 25 years. Internationally, tapentadol's status is in various stages of development at this time. *On 23 January 2008, a New Drug Application (NDA) for tapentadol was submitted to the U.S. FDA. *On 21 November 2008, Johnson & Johnson announced that it has received approval for immediate-release tapentadol tablets.〔(FDA Approves Tapentadol Immediate-Release Tablets for Relief of Moderate to Severe Acute Pain ) November 21, 2008. Retrieved on November 24, 2008.〕 *On 17 February 2009 the U.S. Drug Enforcement Administration proposed a rule which would add tapentadol to Schedule II of the Controlled Substances Act of 1970.〔(Proposed Rule - Schedules of Controlled Substances: Placement of Tapentadol Into Schedule II (February 17, 2009) )〕 The original commercial release date for tapentadol was planned for 17 March 2009; however, the placement of the compound in Schedule II interrupted commercial development. It was the manufacturer's intention to have tapentadol approved as a Schedule III compound, based upon limited preclinical animal data that show a reduced liability for abuse and tolerance compared with morphine. *On 22 June 2009, the Drug Enforcement Administration approved the proposal to make tapentadol schedule II under the Controlled Substance Act. Tapentadol has a DEA Administrative Controlled Substances Control Number of 9780. As a Schedule II controlled substance, an annual aggregrate manufacturing quota is imposed by the DEA; in recent years it has held constant at 13 750 kilos. The aggregate manufacturing quota for 2014 has increased to 17,500 Kilos. *On 23 June 2009, after having received approval from the FDA and DEA, tapentadol became available for prescription on the US market. It is available in immediate-release oral doses of 50, 75, and 100 mg. *On 10 August 2010, the European decentralised procedure regarding tapentadol concluded positively, which will result in the granting of national marketing authorisations in 26 European markets. Tapentadol will then be available as an oral, solid, immediate-release formulation (tablets) for the relief of moderate to severe acute pain in adults, which can be adequately managed only with opioid analgesics, and an oral, solid, prolonged-release formulation (tablets) for the management of severe chronic pain in adults, which can be adequately managed only with opioid analgesics. *On 28 March 2011 the United Kingdom made tapentadol a Class A controlled drug.〔(Misuse of Drugs Act 1971 (Amendment) Order 2011 )〕 *On 29 August 2012, Nucynta ER, an extended release formulation of tapentadol was released to the United States market in doses of 50, 100, 150, 200, and 250 mg for the treatment of neuropathic pain associated with diabetic peripheral neuropathy. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Tapentadol」の詳細全文を読む スポンサード リンク
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