苯他西泮

苯他西泮
临床资料
商品名（英语：Drug nomenclature）	Tiadipona (ES)
AHFS/Drugs.com	国际药品名称
给药途径	Oral (tablets)
ATC码	N05BA24 (WHO) ;
法律规范状态
法律规范	美：未列入管制;
药物动力学数据
药物代谢	Hepatic
生物半衰期	2–4 hours
排泄途径	Renal
识别信息
	IUPAC命名法 5-phenyl-3,4,6,7,8,9-hexahydro-[1]benzothiolo[2,3-e][1,4]diazepin-2-one; ;
CAS号	29462-18-8
PubChem CID	34592;
ChemSpider	11248641 ;
UNII	66JKK43S1Z;
KEGG	D03083 ;
ChEMBL	ChEMBL1521495 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID40897431 ;
ECHA InfoCard	100.123.659
化学信息
化学式	C17H16N2OS
摩尔质量	296.39 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C1CN=C(C2=CC=CC=C2)C3=C(N1)SC4=C3CCCC4;
	InChI InChI=1S/C17H16N2OS/c20-14-10-18-16(11-6-2-1-3-7-11)15-12-8-4-5-9-13(12)21-17(15)19-14/h1-3,6-7H,4-5,8-10H2,(H,19,20) ; Key:AIZFEOPQVZBNGH-UHFFFAOYSA-N ;

苯他西泮（英语：Bentazepam^[1]），商品名为Thiadipone、Tiadipona，是一种噻吩并二氮䓬，也就是一种苯二氮䓬类似物。^[2]

它具有抗焦虑、抗惊厥、镇静和骨骼肌松弛作用。口服给药后约2.5小时将达到血浆峰值速率。^[3]消除半衰期约为2至4小时。^[2]^[4]苯他西泮是种有效的抗焦虑药。

严重的过量服用苯他西泮可能会导致昏迷和呼吸衰竭。^[5] 不良反应包括口干、嗜睡、乏力、消化不良、便秘、恶心^[6]和药物引起的淋巴细胞性结肠炎与苯他西泮有关。^[7]^[8]严重的肝损伤和肝炎也与苯他西泮有关。^[9]^[10]^[11]虽然苯他西泮引起的肝衰竭被认为是罕见的，但建议对所有服用苯他西泮的患者进行肝功能监测。^[12]

参见

苯二氮䓬列表

参考资料

^ DE 2005276
^ ^2.0 ^2.1 Gonzalez López F, Mariño EL, Dominguez-Gil A. Pharmacokinetics of tiadipone: a new anxiolytic. International Journal of Clinical Pharmacology, Therapy, and Toxicology. September 1986, 24 (9): 482–4. PMID 2877954.
^ Mariño EL, Fernandez Lastra C, Gonzalez Lopez F, Dominguez-Gil A, Garcia Santalla JL, Vorca G, et al. Parametrization by non-linear regression and bayesian estimation of bentazepam in a multiple dosage regimen in humans. International Journal of Clinical Pharmacology, Therapy, and Toxicology. November 1987, 25 (11): 627–32. PMID 3429066.
^ Colino CI, Lastra CF, López FG, Ledesma A, Mariño EL. Open-loop feedback control of serum bentazepam concentrations and Bayesian estimation in multiple dosage regimens in patients. International Journal of Clinical Pharmacology, Therapy, and Toxicology. November 1991, 29 (11): 457–62. PMID 1800395.
^ Rivas López FA, López Soriano F, Mendoza Cerezo A, Jiménez Ferré J, Azurmendi Rodríguez JI, de la Rubia Nieto MA. [Mixed benzodiazepine poisoning and reversal with flumazenil (Ro 15-1788)]. Revista Espanola de Anestesiologia y Reanimacion. 1989, 36 (1): 48–50. PMID 2565591.
^ Honorato J, Rubio A, Tristán C, Otero FJ, Garrido J. [A pharmacovigilance study with bentazepam in a sample of 1046 psychiatric outpatients]. Revista de Medicina de la Universidad de Navarra. 1990, 34 (2): 80–8. PMID 1983365.
^ Fernández-Bañares F, Salas A, Esteve M, Espinós J, Forné M, Viver JM. Collagenous and lymphocytic colitis. evaluation of clinical and histological features, response to treatment, and long-term follow-up. The American Journal of Gastroenterology. February 2003, 98 (2): 340–7. PMID 12591052.
^ de-la-Serna C, Gil-Grande LA, Sanromán AL, Gonzalez M, Ruiz-del-Arbol L, Garcia Plaza A. Bentazepam-induced hepatic bridging necrosis. Journal of Clinical Gastroenterology. December 1997, 25 (4): 710–1. PMID 9451703. doi:10.1097/00004836-199712000-00042.
^ Andrade RJ, Lucena MI, Kaplowitz N, García-Muņoz B, Borraz Y, Pachkoria K, et al. Outcome of acute idiosyncratic drug-induced liver injury: Long-term follow-up in a hepatotoxicity registry. Hepatology. December 2006, 44 (6): 1581–8. PMID 17133470. S2CID 9067701. doi:10.1002/hep.21424  .
^ Tuca A. Utilidad clinica del acetato de megestrol para la ganancia de peso en los enfermos con neoplasia y caquexia. Medicina Clinica. 2003, 120 (17): 678 [2023-01-20]. doi:10.1157/13047309. （原始内容存档于2018-09-16）（西班牙语）.
^ Andrade RJ, Lucena MI, Alcantara R, Fraile JM. Bentazepam-associated chronic liver disease. Lancet. April 1994, 343 (8901): 860. PMID 7908109. S2CID 33991843. doi:10.1016/S0140-6736(94)92065-6.
^ Andrade RJ, Lucena MI, Aguilar J, Lazo MD, Camargo R, Moreno P, et al. Chronic liver injury related to use of bentazepam: an unusual instance of benzodiazepine hepatotoxicity. Digestive Diseases and Sciences. July 2000, 45 (7): 1400–4. PMID 10961721. doi:10.1023/A:1005520523502.

[1] DE 2005276

[potana-2] 2.0 ^2.1 Gonzalez López F, Mariño EL, Dominguez-Gil A. Pharmacokinetics of tiadipone: a new anxiolytic. International Journal of Clinical Pharmacology, Therapy, and Toxicology. September 1986, 24 (9): 482–4. PMID 2877954.

[3] Mariño EL, Fernandez Lastra C, Gonzalez Lopez F, Dominguez-Gil A, Garcia Santalla JL, Vorca G, et al. Parametrization by non-linear regression and bayesian estimation of bentazepam in a multiple dosage regimen in humans. International Journal of Clinical Pharmacology, Therapy, and Toxicology. November 1987, 25 (11): 627–32. PMID 3429066.

[4] Colino CI, Lastra CF, López FG, Ledesma A, Mariño EL. Open-loop feedback control of serum bentazepam concentrations and Bayesian estimation in multiple dosage regimens in patients. International Journal of Clinical Pharmacology, Therapy, and Toxicology. November 1991, 29 (11): 457–62. PMID 1800395.

[5] Rivas López FA, López Soriano F, Mendoza Cerezo A, Jiménez Ferré J, Azurmendi Rodríguez JI, de la Rubia Nieto MA. [Mixed benzodiazepine poisoning and reversal with flumazenil (Ro 15-1788)]. Revista Espanola de Anestesiologia y Reanimacion. 1989, 36 (1): 48–50. PMID 2565591.

[6] Honorato J, Rubio A, Tristán C, Otero FJ, Garrido J. [A pharmacovigilance study with bentazepam in a sample of 1046 psychiatric outpatients]. Revista de Medicina de la Universidad de Navarra. 1990, 34 (2): 80–8. PMID 1983365.

[7] Fernández-Bañares F, Salas A, Esteve M, Espinós J, Forné M, Viver JM. Collagenous and lymphocytic colitis. evaluation of clinical and histological features, response to treatment, and long-term follow-up. The American Journal of Gastroenterology. February 2003, 98 (2): 340–7. PMID 12591052.

[8] -la-Serna C, Gil-Grande LA, Sanromán AL, Gonzalez M, Ruiz-del-Arbol L, Garcia Plaza A. Bentazepam-induced hepatic bridging necrosis. Journal of Clinical Gastroenterology. December 1997, 25 (4): 710–1. PMID 9451703. doi:10.1097/00004836-199712000-00042.

[9] Andrade RJ, Lucena MI, Kaplowitz N, García-Muņoz B, Borraz Y, Pachkoria K, et al. Outcome of acute idiosyncratic drug-induced liver injury: Long-term follow-up in a hepatotoxicity registry. Hepatology. December 2006, 44 (6): 1581–8. PMID 17133470. S2CID 9067701. doi:10.1002/hep.21424  .

[10] Tuca A. Utilidad clinica del acetato de megestrol para la ganancia de peso en los enfermos con neoplasia y caquexia. Medicina Clinica. 2003, 120 (17): 678 [2023-01-20]. doi:10.1157/13047309. （原始内容存档于2018-09-16）（西班牙语）.

[11] Andrade RJ, Lucena MI, Alcantara R, Fraile JM. Bentazepam-associated chronic liver disease. Lancet. April 1994, 343 (8901): 860. PMID 7908109. S2CID 33991843. doi:10.1016/S0140-6736(94)92065-6.

[12] Andrade RJ, Lucena MI, Aguilar J, Lazo MD, Camargo R, Moreno P, et al. Chronic liver injury related to use of bentazepam: an unusual instance of benzodiazepine hepatotoxicity. Digestive Diseases and Sciences. July 2000, 45 (7): 1400–4. PMID 10961721. doi:10.1023/A:1005520523502.

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