Delorazepam

Structural formula
General
Non-proprietary name	Delorazepam
other names	7-chloro-5- (2-chlorophenyl) -1,3-dihydro-1,4-benzodiazepin-2 (2 H ) -one Chlordesmethyldiazepam
Molecular formula	C 15 H 10 Cl 2 N 2 O
External identifiers / databases
CAS number 2894-67-9 EC number 220-771-9 ECHA InfoCard 100,018,884 PubChem 17925 ChemSpider 16929 DrugBank DB01511 Wikidata Q3705147
properties
Molar mass	304.02 g · mol -1
safety instructions
GHS hazard labeling no classification available
Toxicological data	940 mg kg −1 ( LD 50 ,  mouse ,  oral ) 2000 mg kg −1 ( LD 50 ,  rat ,  oral )
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Delorazepam is a chemical compound from the benzodiazepine group with calming and anxiolytic properties. Chemically, it is a C-2 ' chlorinated derivative of north azepam .

Of course, delorazepam occurs in small amounts (100–200 ng / g) in tarragon ( Artemisia dracunculus ).

use

Delorazepam has a long plasma half-life and is therefore mostly used as an anxiolytic , for example as a premedication for dental phobia . Delorazepam is mainly marketed as a medicinal substance in Italy.

pharmacology

Delorazepam has high bioavailability and is quickly absorbed by the body. The maximum concentration in the blood plasma is reached after 1–2 hours. It has a very long half-life because delorazepam can still be found in the blood even after 72 hours. The plasma half-life varies according to age: in adults it is around 97 to 100 hours, in children aged 2 to 3 years it is around 27 hours. Part of the delorazepam is metabolized to the likewise active lorazepam . In proportion, 1 mg delorazepam is about as effective as 10 mg diazepam .

Delorazepam is also formed when the drug cloxazolam is metabolized as a pharmacologically active metabolic product ( metabolite ).

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
2. ↑ ^{a b} Entry on delorazepam in the ChemIDplus database of the United States National Library of Medicine (NLM)
3. ^ Archives internationales de Pharmacodynamie et de Thérapie . Vol. 154, p. 131, 1965.
4. ^ Medicamentos de Actualidad . Vol. 15, p. 173, 1979.
5. ↑ Dominique Kavvadias: Ligands of the benzodiazepine receptor: Studies on benzodiazepines in plant tissues as well as on hispidulin. (PDF; 1.8 MB) Dissertation at the Julius Maximilians University of Würzburg , 2003, p. 5.
6. ↑ P. Rocca, V. Fonzo, M. Scotta, E. Zanalda, L. Ravizza: Paroxetine efficacy in the treatment of generalized anxiety disorder. . In: Acta Psychiatr Scand . 95, No. 5, 1997, pp. 444-450. doi : 10.1111 / j.1600-0447.1997.tb09660.x . PMID 9197912 .
7. ↑ G. Manani, L. Baldinelli, G. Cordioli, E. Consolati, F. Luisetto, L. Galzigna: Premedication with chlordemethyldiazepam and anxiolytic effect of diazepeam in implantology . In: Anesth Prog . 42, No. 3-4, 1995, pp. 107-112. PMID 8934975 . PMC 2148912 (free full text).
8. ↑ L. Dal Bo, F. Marcucci, E. Mussini, D. Perbellini, A. Castellani, P. Fresia: Plasma levels of chlorodesmethyldiazepam in humans . In: Biopharm Drug Dispos . 1, No. 3, 1980, pp. 123-126. doi : 10.1002 / bdd.2510010306 . PMID 6778522 .
9. ↑ Technical information EN compresse, gocce , as of October 1999.