他噴他竇

他噴他竇
臨床資料
商品名（英语：Drug nomenclature）	Nucynta, Palexia, Yantil, Tapenta, Tapal, Aspadol, others
其他名稱	BN-200; CG-5503; R-331333
AHFS/Drugs.com	Monograph
MedlinePlus	a610006
懷孕分級	澳: C ; ;
依賴性	高
成癮性	非常高
给药途径	口服给药
藥物類別	類阿片
ATC碼	N02AX06 (WHO) ;
法律規範狀態
法律規範	澳：受管控（S8）; 加：Schedule I; 德：Anlage III; 歐：Rx-only; 英：Class A (Schedule 2 CD); 美： Schedule II（英语：List of Schedule II drugs (US)）; UN：未列入管制;
藥物動力學數據
生物利用度	32% (oral)
血漿蛋白結合率	20%
药物代谢	肝 (主要透過葡萄糖醛酸化（英语：glucuronidation）但也可透過CYP2C9、CYP2C19、CYP2D6)
藥效起始時間（英语：Onset of action）	~30 分鐘
生物半衰期	4 小時
作用時間	4-6 小時
排泄途徑	尿液和糞便 (1%)
识别信息
	IUPAC命名法 3-[(1R,2R)-3-(Dimethylamino)-1-ethyl-2-methylpropyl]phenol; ;
CAS号	175591-23-8 ; 175591-09-0
PubChem CID	9838022;
IUPHAR/BPS	7477;
DrugBank	DB06204 ;
ChemSpider	8013742 ;
UNII	H8A007M585; HCl: 71204KII53 ;
KEGG	D06007 ;
ChEMBL	ChEMBL1201776 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID30170003 ;
ECHA InfoCard	100.131.247
化学信息
化学式	C14H23NO
摩尔质量	221.34 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
沸点	(decomposes)
	SMILES Oc1cc(ccc1)[C@@H]([C@@H](C)CN(C)C)CC;
	InChI InChI=1S/C14H23NO/c1-5-14(11(2)10-15(3)4)12-7-6-8-13(16)9-12/h6-9,11,14,16H,5,10H2,1-4H3/t11-,14+/m0/s1 ; Key:KWTWDQCKEHXFFR-SMDDNHRTSA-N ;

他噴他竇（INN：Tapentadol）是一种口服的類阿片镇痛药^[8]。可治疗急性或慢性的中度至重度疼痛^[8] ^[9]。藥效约在 30 分钟出現，並可持续 4-6 小时^[10] ^[11]。

常见副作用包括恶心、嗜睡、便秘和瘙痒^[8]。其他副作用包括可能癲癇發作、低血压、成瘾、血清素综合症和因呼吸抑制而產生換氣不足^[8]。孕期使用可能對婴儿有害^[8]。滥用风险与其他强效阿片类药物相似^[8]。虽然其作用原理尚不完全清楚，但主要作用在μ-（英语：μ-opioid receptor）阿片受體，也能提高血清素和去甲肾上腺素的濃度^[8]。

他噴他竇在各國取得醫療使用許可的時間，分別是美国2008年^[8] ，澳大利亚2010年^[12] ，英国和印度2011年^[13] ^[14]。市面上也有修飾釋放劑型（英语：Modified-release dosage）的他噴他竇^[9]。

参考文獻

^ ^1.0 ^1.1 Tapentadol (Monograph). American Society of Health-System Pharmacists (AHFS). 19 April 2023 [2025-01-26]. （原始内容存档于2021-03-05） –通过Drugs.com.
^ Tapentadol Consumer Medicine Information. NPS MedicineWise. September 2020 [2025-01-26]. （原始内容存档于2025-02-18） –通过nps.org.au.
^ Tapentadol. MedLine Plus. 2024-03-15 [2024-11-25]. （原始内容存档于2025-02-22）（英语）.
^ Active substance(s): tapentadol (PDF). List of nationally authorised medicinal products. European Medicines Agency. 21 July 2022 [2022-09-06]. （原始内容存档 (PDF)于2022-09-06）.
^ ^5.0 ^5.1 ^5.2 ^5.3 Smit JW, Oh C, Rengelshausen J, Terlinden R, Ravenstijn PG, Wang SS, Upmalis D, Mangold B. Effects of acetaminophen, naproxen, and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. January 2010, 30 (1): 25–34. PMC 2888545 . PMID 20030470. doi:10.1592/phco.30.1.25.
^ Brayfield A (编). Tapentadol. Martindale: The Complete Drug Reference. Pharmaceutical Press. 14 November 2011 [2 April 2014]. （原始内容存档于29 August 2021）.
^ Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União（英语：Diário Oficial da União）. 2023-03-31 (2023-04-04) [2023-08-16]. （原始内容存档于2023-08-03）（巴西葡萄牙语）.
^ ^8.0 ^8.1 ^8.2 ^8.3 ^8.4 ^8.5 ^8.6 ^8.7 Tapentadol Monograph for Professionals. Drugs.com. [22 September 2021]. （原始内容存档于5 March 2021）（英语）.
^ ^9.0 ^9.1 BNF 80. BMJ Group and the Pharmaceutical Press. September 2020 - March 2021: 491. ISBN 978-0-85711-369-6. 请检查|date=中的日期值 (帮助)
^ Emmett, Stevan R.; Hill, Nicola; Dajas-Bailador, Federico. Clinical Pharmacology for Prescribing. Oxford University Press. 30 October 2019: 441 [22 September 2021]. ISBN 978-0-19-258564-6. （原始内容存档于22 September 2021）（英语）.
^ Fischer, János; Ganellin, C. Robin; Rotella, David P. Analogue-based Drug Discovery III. John Wiley & Sons. 15 October 2012: 44 [22 September 2021]. ISBN 978-3-527-65110-8. （原始内容存档于22 September 2021）（英语）.
^ TGA eBS - Product and Consumer Medicine Information Licence. www.ebs.tga.gov.au. [22 September 2021]. （原始内容存档于30 March 2020）.
^ Palexia film coated tablets. electronic Medicines Compendium. Grunenthal Ltd. 13 November 2013 [2 April 2014]. （原始内容存档于7 April 2014）.
^ Mukherjee, Diptadhi; Shukla, Lekhansh; Saha, Priyanka; Mahadevan, Jayant; Kandasamy, Arun; Chand, Prabhat; Benegal, Vivek; Murthy, Pratima. Tapentadol abuse and dependence in India. Asian Journal of Psychiatry. March 2020, 49: 101978. PMID 32120298. doi:10.1016/j.ajp.2020.101978 （英语）.

[AHFS2014-1] 1.0 ^1.1 Tapentadol (Monograph). American Society of Health-System Pharmacists (AHFS). 19 April 2023 [2025-01-26]. （原始内容存档于2021-03-05） –通过Drugs.com.

[PalexiaCMI-2] Tapentadol Consumer Medicine Information. NPS MedicineWise. September 2020 [2025-01-26]. （原始内容存档于2025-02-18） –通过nps.org.au.

[3] Tapentadol. MedLine Plus. 2024-03-15 [2024-11-25]. （原始内容存档于2025-02-22）（英语）.

[4] Active substance(s): tapentadol (PDF). List of nationally authorised medicinal products. European Medicines Agency. 21 July 2022 [2022-09-06]. （原始内容存档 (PDF)于2022-09-06）.

[Fidman2010rev-5] 5.0 ^5.1 ^5.2 ^5.3 Smit JW, Oh C, Rengelshausen J, Terlinden R, Ravenstijn PG, Wang SS, Upmalis D, Mangold B. Effects of acetaminophen, naproxen, and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. January 2010, 30 (1): 25–34. PMC 2888545 . PMID 20030470. doi:10.1592/phco.30.1.25.

[MD-6] Brayfield A (编). Tapentadol. Martindale: The Complete Drug Reference. Pharmaceutical Press. 14 November 2011 [2 April 2014]. （原始内容存档于29 August 2021）.

[7] Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União（英语：Diário Oficial da União）. 2023-03-31 (2023-04-04) [2023-08-16]. （原始内容存档于2023-08-03）（巴西葡萄牙语）.

[AHFS2021-8] 8.0 ^8.1 ^8.2 ^8.3 ^8.4 ^8.5 ^8.6 ^8.7 Tapentadol Monograph for Professionals. Drugs.com. [22 September 2021]. （原始内容存档于5 March 2021）（英语）.

[BNF80-9] 9.0 ^9.1 BNF 80. BMJ Group and the Pharmaceutical Press. September 2020 - March 2021: 491. ISBN 978-0-85711-369-6. 请检查|date=中的日期值 (帮助)

[Onset2019-10] Emmett, Stevan R.; Hill, Nicola; Dajas-Bailador, Federico. Clinical Pharmacology for Prescribing. Oxford University Press. 30 October 2019: 441 [22 September 2021]. ISBN 978-0-19-258564-6. （原始内容存档于22 September 2021）（英语）.

[Duration2012-11] Fischer, János; Ganellin, C. Robin; Rotella, David P. Analogue-based Drug Discovery III. John Wiley & Sons. 15 October 2012: 44 [22 September 2021]. ISBN 978-3-527-65110-8. （原始内容存档于22 September 2021）（英语）.

[12] TGA eBS - Product and Consumer Medicine Information Licence. www.ebs.tga.gov.au. [22 September 2021]. （原始内容存档于30 March 2020）.

[13] Palexia film coated tablets. electronic Medicines Compendium. Grunenthal Ltd. 13 November 2013 [2 April 2014]. （原始内容存档于7 April 2014）.

[Dip2020-14] Mukherjee, Diptadhi; Shukla, Lekhansh; Saha, Priyanka; Mahadevan, Jayant; Kandasamy, Arun; Chand, Prabhat; Benegal, Vivek; Murthy, Pratima. Tapentadol abuse and dependence in India. Asian Journal of Psychiatry. March 2020, 49: 101978. PMID 32120298. doi:10.1016/j.ajp.2020.101978 （英语）.

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