苯他西泮

苯他西泮
臨床資料
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碼
法律規範狀態
法律規範
  • 美：未列入管制
藥物動力學數據
药物代谢Hepatic
生物半衰期2–4 hours
排泄途徑Renal
识别信息
  • 5-phenyl-3,4,6,7,8,9-hexahydro-[1]benzothiolo[2,3-e][1,4]diazepin-2-one
CAS号29462-18-8  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.123.659 編輯維基數據鏈接
化学信息
化学式C17H16N2OS
摩尔质量296.39 g·mol−1
3D模型（JSmol（英语：JSmol））
  • O=C1CN=C(C2=CC=CC=C2)C3=C(N1)SC4=C3CCCC4
  • 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) checkY
  • Key:AIZFEOPQVZBNGH-UHFFFAOYSA-N checkY

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

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参考资料

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  1. ^ DE 2005276 
  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. ^ 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. 
  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 可免费查阅. 
  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.