5581. Lormetazepam
Nomenclature
CAS number: 848-75-9
7-Chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-1-methyl-2H-1,4-benzodiazepin-2-one; N-methyllorazepam; Wy-4082; Ergocalm (Teofarma); Loramet (Wyeth); Noctamid (Schering AG). C16H12Cl2N2O2; mol wt 335.18.
C 57.33%, H 3.61%, Cl 21.15%, N 8.36%, O 9.55%.
Description and references
Analog of lorazepam, q.v. Prepn: S. C. Bell, BE 621819 C.A. 60, 2993b (1964); idem, US 3296249 (1963, 1967 both to Am. Home Products); idem, J. Med. Chem. 11, 457 (1968); A. Nudelman et al., J. Pharm. Sci. 63, 1886 (1974). Pharmacokinetics and biotransformation in humans: M. Hümpel et al., Eur. J. Drug Metab. Pharmacokinet. 4, 237 (1979). Hypnotic effect: A. Doenicke et al., Anaesthesist 28, 578 (1979). Comparative study: H. Ott et al., ibid. 29. Absorption, distribution, excretion of 14C-lormetazepam: R. Girkin et al., Xenobiotica 10, 401 (1980). Radioimmunologic study: M. Hümpel et al., Clin. Pharmacol. Ther. 28, 673 (1980).
Properties
Crystals from ethanol/THF, mp 205-207°.Note
This is a controlled substance (depressant): 21 CFR, 1308.14.Therapeutic Category
Sedative, hypnotic.
Keywords
Sedative/Hypnotic; Benzodiazepine Derivatives