Bentazepam

Bentazepam
Systematic (IUPAC) name
5-phenyl-3,5a,6,7,8,9-hexahydro-2H-[1]benzothieno[2,3-e][1,4]diazepin-2-one
Clinical data
AHFS/Drugs.com International Drug Names
  • ?
  • Schedule IV(US)
Oral
Pharmacokinetic data
Bioavailability ?
Metabolism Hepatic
Excretion Renal
Identifiers
29462-18-8 Yes
None
PubChem CID 34592
ChemSpider 11248641 Yes
UNII 66JKK43S1Z Yes
KEGG D03083 Yes
ChEMBL CHEMBL1521495 
Chemical data
Formula C17H16N2OS
296.387 g/mol
  (what is this?)  (verify)

Bentazepam[1] (also known as Thiadipone) 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 two and a half 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]

It is marketed in Spain as Tiadipona.

See also

References

  1. ↑ DE Patent 2005276
  2. ↑ 2.0 2.1 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.
  3. ↑ 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.
  4. ↑ 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.
  5. ↑ 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.
  6. ↑ 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.
  7. ↑ 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.
  8. ↑ 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.
  9. ↑ 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.
  10. ↑ 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.
  11. ↑ 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.
  12. ↑ 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.