Bentazepam
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| Systematic (IUPAC) name | |
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5-phenyl-3,4,6,7,8,9-hexahydro-[1]benzothiolo[2,3-e][1,4]diazepin-2-one
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| Clinical data | |
| Trade names | Tiadipona (ES) |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration |
Oral (tablets) |
| Legal status | |
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| Pharmacokinetic data | |
| Metabolism | Hepatic |
| Biological half-life | 2–4 hours |
| Excretion | Renal |
| Identifiers | |
| CAS Number | 29462-18-8  |
| PubChem | CID 34592 |
| ChemSpider | 11248641 |
| UNII | 66JKK43S1Z |
| KEGG | D03083 |
| ChEMBL | CHEMBL1521495  |
| Chemical data | |
| Formula | C17H16N2OS |
| Molar mass | 296.387 g/mol |
| 3D model (Jmol) | Interactive image |
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Bentazepam[1] (also known as Thiadipone, Tiadipona) is a thienodiazepine which is a benzodiazepine analog.[2] It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Peak plasma rates are achieved in around 2,5 hours after oral administration.[3] The elimination half-life is between approximately 2–4 hours.[2][4] Bentazepam is effective as an anxiolytic. A severe benzodiazepine overdose with bentazepam may result in coma and respiratory failure.[5] Adverse effects include dry mouth, somnolence, asthenia, dyspepsia, constipation, nausea[6] and drug-induced lymphocytic colitis has been associated with bentazepam.[7][8] Severe liver damage and hepatitis has also been associated with bentazepam.[9][10][11] Whilst liver failure from bentazepam is considered to be rare, liver function monitoring has been recommended for all patients taking bentazepam.[12]
See also[edit]
References[edit]
- ^ DE Patent 2005276
- ^ a b Gonzalez López, F; Mariño, EL; Dominguez-Gil, A (1986). "Pharmacokinetics of tiadipone: a new anxiolytic". International journal of clinical pharmacology, therapy, and toxicology. 24 (9): 482–4. PMID 2877954.
- ^ Mariño, EL; Fernandez Lastra, C; Gonzalez Lopez, F; Dominguez-Gil, A; Garcia Santalla, JL; Vorca, G; Izquierdo, JA; Ledesma-Jimeno, A (1987). "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. 25 (11): 627–32. PMID 3429066.
- ^ Colino, CI; Lastra, CF; López, FG; Ledesma, A; Mariño, EL (1991). "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. 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 (1989). "Mixed benzodiazepine poisoning and reversal with flumazenil (Ro 15-1788)". Revista espanola de anestesiologia y reanimacion. 36 (1): 48–50. PMID 2565591.
- ^ Honorato, J; Rubio, A; Tristán, C; Otero, FJ; Garrido, J (1990). "A pharmacovigilance study with bentazepam in a sample of 1046 psychiatric outpatients". Revista de medicina de la Universidad de Navarra. 34 (2): 80–8. PMID 1983365.
- ^ Fernández-Bañares, F; Salas, A; Esteve, M; Espinós, J; Forné, M; Viver, JM (2003). "Collagenous and lymphocytic colitis. evaluation of clinical and histological features, response to treatment, and long-term follow-up.". The American journal of gastroenterology. 98 (2): 340–7. doi:10.1111/j.1572-0241.2003.07225.x. PMID 12591052.
- ^ De-La-Serna, C; Gil-Grande, LA; Sanromán, AL; Gonzalez, M; Ruiz-Del-Arbol, L; Garcia Plaza, A (1997). "Bentazepam-induced hepatic bridging necrosis.". Journal of Clinical Gastroenterology. 25 (4): 710–1. doi:10.1097/00004836-199712000-00042. PMID 9451703.
- ^ Andrade, RJ; Lucena, MI; Kaplowitz, N; García-Muņoz, B; Borraz, Y; Pachkoria, K; García-Cortés, M; Fernández, MC; et al. (2006). "Outcome of acute idiosyncratic drug-induced liver injury: Long-term follow-up in a hepatotoxicity registry". Hepatology (Baltimore, Md.). 44 (6): 1581–8. doi:10.1002/hep.21424. PMID 17133470.
- ^ Tuca, Albert (2003). "Utilidad clinica del acetato de megestrol para la ganancia de peso en los enfermos con neoplasia y caquexia". Medicina Clinica (in Spanish). 120 (17): 678. doi:10.1157/13047309.
- ^ Andrade, RJ; Lucena, MI; Alcantara, R; Fraile, JM (1994). "Bentazepam-associated chronic liver disease.". Lancet. 343 (8901): 860. doi:10.1016/S0140-6736(94)92065-6. PMID 7908109.
- ^ Andrade, RJ; Lucena, MI; Aguilar, J; Lazo, MD; Camargo, R; Moreno, P; García-Escaño, MD; Marquez, A; et al. (2000). "Chronic liver injury related to use of bentazepam: an unusual instance of benzodiazepine hepatotoxicity". Digestive diseases and sciences. 45 (7): 1400–4. doi:10.1023/A:1005520523502. PMID 10961721.
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