1385. Bromazepam

Nomenclature

CAS number: 1812-30-2
7-Bromo-1,3-dihydro-5-(2-pyridinyl)-2H-1,4-benzodiazepin-2-one; 7-bromo-5-(2-pyridyl)-3H-1,4-benzodiazepin-2(1H)-one; Ro-5-3350; Compendium (Polifarma); Creosedin (Osiris); Durazanil (Durachemie); Lectopam (Roche); Lexomil (Roche); Lexotan (Roche); Lexotanil (Roche); Normoc (Merckle).
C14H10BrN3O; mol wt 316.15.
C 53.19%, H 3.19%, Br 25.27%, N 13.29%, O 5.06%.

Description and references

Prepn: Berger et al., BE 619101; eidem, Fryer et al., US 3100770 (1962, 1963 to Hoffmann-La Roche); eidem, J. Pharm. Sci. 53, 264 (1964); US 3182065; US 3182067 (both 1965 to Hoffmann-La Roche). Pharmacology: Korol, Brown, Pharmacology 1, 115 (1968). Metabolism: M. A. Schwartz et al., J. Pharm. Sci. 62, 1776 (1973); Drug Metab. Dispos. 2, 31 (1974). Evaluation as pre-anesthesia medication: P. Chalmers, J. N. Horton, Anaesthesia 39, 370 (1984). Multicenter clinical comparison with lorazepam, q.v.: G. J. Cordingley et al., Curr. Med. Res. Opin. 9, 505 (1985). Evaluation of adverse effects and withdrawal reactions: R. Fontaine et al., Psychopharmacol. Bull. 21, 91 (l985). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Comprehensive description: M. M. Hassan, M. A. Abounassif, Anal. Profiles Drug Subs. 16, 1-51 (1987).

Chemical structure

Properties

Colorless prisms from acetone, mp 237-238.5° (dec). LD50 orally in rats: 3050 ±405 mg/kg (Goldenthal).

Note

This is a controlled substance (depressant): 21 CFR, 1308.14.

Therapeutic Category

Anxiolytic.

Keywords

Anxiolytic; Benzodiazepine Derivatives