Thienodiazepines
In pharmacy and chemistry , thienodiazepines are heterocycles that contain a diazepine ring and a fused thiophene ring. These include drugs and psychotropic substances : bentazepam , brotizolam , Ciclotizolam , Clotiazepam , Deschloroetizolam , Desmethyletizolam (Metizolam) etizolam , israpafant and JQ1 (CAS No. 1268524-70-4) .
structure
Basic body of the thienodiazepines | Blue- marked fused thiophene ring with two carbon atoms that are also part of the diazepine ring. | Green- marked, fused-on diazepine ring with two carbon atoms, which are also part of the thiophene ring. |
Individual substances
Active ingredient | Trade name (s) | Effect type | Chemical name |
Plasma half-life (metabolite half-life ) |
Equivalent dose to 10 mg diazepam | Year of launch |
---|---|---|---|---|---|---|
Bentazepam | Tiadipona (ES) | Tranquilizer, anxiolytic | 5-phenyl-1,3,6,7,8,9-hexahydro-2 H - [1] benzothieno [2,3- e ] [1,4] diazepin-2-one | 2.8-4.5 h | 50 mg | 1986 |
Brotizolam |
Lendormin (D), Lendorm (AT, DK), Lendormine (CH), Sintonal (ES) |
Hypnotic, sedative | 2-Bromo-4- (2-chlorophenyl) -9-methyl-6 H -thieno [3,2- f ] [1,2,4] triazolo [4,3- a ] [1,4] diazepine | 3–6 h (4–19 h) | 0.5 mg | 1985 |
Ciclotiazolam | - | Anxiolytic, anti-epileptic | 8-Bromo-6- ( o -chlorophenyl) -1-cyclohexyl-4 H -5-triazolo (3,4-c) thieno (2,4-e) -1,4-diazepine | Designer drug | ||
Clotiazepam |
Distensan (ES), Rize (JP), Trecalmo (D), Tienor (IT), Veratran (FR) |
Anxiolytic, tranquilizer | 5- (2-Chlorophenyl) -7-ethyl-1,3-dihydro-1-methyl-2 H -thieno [2,3-e] -1,4-diazepin-2-one | 5-6 h | 5 mg | 1975 |
Deschloroetizolam | - | 4- (2-Chlorophenyl) -2-ethyl-9-methyl-6 H -thieno [3,2- f ] [1,2,4] triazolo [4,3- a ] [1,4] diazepine | ~ 8-10 h | 2-4 mg | Designer drug | |
Etizolam |
Depas (JP), Etilaam (ID), Pasaden (IT) |
Hypnotic, anxiolytic | 7- (2-chlorophenyl) -4-ethyl-13-methyl-3-thia-1,8,11,12-tetraazatricyclo [8.3.0.0 2,6 ] trideca-2 (6), 4,7,10, 12-pentaen | 3.5 h (8 h) | 1 mg | 1984 |
Fluclotiazepam | - | Hypnotic | 2-Chloro-4- (2-fluorophenyl) -9-methyl-4 H -thieno [3,2-f] [1,2,4] triazolo [4,3-a] [1,4] diazepine | ~ 6-13 h | 0.5-0.75 mg | Designer drug |
Metizolam | - | Hypnotic, tranquilizer | 4- (2-Chlorophenyl) -2-ethyl-6 H -thieno [3.2- f ] [1,2,4] triazolo [4,3- a ] [1,4] diazepine | ~ 12 h | 2-4 mg | Designer drug |
See also
Individual evidence
- ↑ Otto-Albrecht Neumüller (Ed.): Römpps Chemie-Lexikon. Volume 2: Cm-G. 8th revised and expanded edition. Franckh'sche Verlagshandlung, Stuttgart 1981, ISBN 3-440-04512-9 , p. 930.
- ↑ Otto-Albrecht Neumüller (Ed.): Römpps Chemie-Lexikon. Volume 6: T-Z. 8th revised and expanded edition. Franckh'sche Verlagshandlung, Stuttgart 1988, ISBN 3-440-04516-1 , p. 4234.
- ↑ Frank Schneider, Sabrina Weber (eds.): Clinic Manual - Psychiatry, Psychosomatics and Psychotherapy. Springer, Heidelberg 2008, ISBN 978-3-540-78466-1 , p. 209.
- ↑ Erika Montes Gómez, Mercedes Plasencia Núñez. Ana Teresa López Navarro, Mª Elidia Guerra Rodríguez, José Luis Castellano Cabrera, Ángela Martín Morales, Fidelina de la Nuez Viera: DESPRESCRIPCIÓN DE BENZODIAZEPINAS E HIPNÓTICOS Z . In: SERVICIO CANARIO DE LA SALUD (ed.): Bolcan . tape 2 , no. 9 . Servicio Canario de la Salud, September 2017, ISSN 1889-0938 , p. 3 (Spanish, gobiernodecanarias.org [PDF; accessed February 2, 2019]).
- ↑ Information on all trademarks registered through the Madrid System .: Tiadipona® in the Madrid System. Real-time status - WIPO reference 50513901. In: WIPO Madrid Monitor. WIPO, September 4, 1986, accessed February 22, 2019 .
- ↑ Jürgen Klauber, Helmut Schröder, Gisbert W. Selke: Innovation in the drug market . Springer-Verlag, 2013, ISBN 978-3-642-59796-1 , pp. 95 (254 pp., Google.de ): "The present volume makes a contribution to the objectification of this topic by bringing together the relevant approaches to assessing drug innovations as well as the essential international experiences."
- ^ S. Desmet, D. Kindt, A. Verhaeghe, K. Verhelle, Clinical pharmacy department AZ Groeninge: Deprescribing psychoactive medication for geriatric patients in a multidisciplinary way. (PDF) In: The European Association of Hospital Pharmacists. AZ Groeninge, Kortrijk, Belgium, March 2016, p. 1 , accessed on February 28, 2019 (English): "List dose X (mg) equivalent to 10mg diazepam "
- ↑ WHO Expert Committee on Drug Dependence: Etizolam (INN). (PDF) In: World Health Organization. World Health Organization, November 20, 2015, p. 16 , accessed on February 23, 2019 (English): "Etizolam is an anxiolytic medicine, originally developed in Japan, where it was introduced under the brand name of Depas in 1984."