LORMETAZEPAM

Toxicity

The primary manifestation of overdosage ranges from drowsiness to coma and symptoms may include ataxia, hypotension, hypotonia, respiratory depression which may lead to death .
Experimental LD50 values are as follows : Mouse - 780 mg/kg (intraperitoneal), 1790 mg/kg (oral), 10000 mg/kg (subcutaneous). Rat - 6250 mg/kg (intraperitoneal), 10000 mg/kg (oral), 10000 mg/kg (intraperitoneal).

Chemical properties

Pale Green Solid

Originator

Loramet ,Wyeth, W. Germany,1980

The Uses of LORMETAZEPAM

An analog of Lorazepam (L469850). Sedative, hypnotic. Controlled substance (depressant).

Background

Lormatazepam is an orally available benzodiazepine used in the UK for the treatment of short-term insomnia . It is marketed by Auden Mckenzie (Pharma Division) in 0.5 and 1 mg tablet formulations.

Indications

For the treatment of short-term insomnia

Definition

ChEBI: Lormetazepam is a 1,4-benzodiazepinone compound having a methyl substituent at the 1-position, a hydroxy substituent at the 3-position, a 2-chlorophenyl group at the 5-position and a chloro substituent at the 7-position. It has a role as a sedative. It is a 1,4-benzodiazepinone and an organochlorine compound.

Manufacturing Process

To a suspension of 3.4 g of 3-acetoxy-7-chloro-1,3-dihydro-5-(ochlorophenyl)-2H-1,4-benzodiazepin-2-one in 80 ml of alcohol was added 6 ml of 4 N sodium hydroxide. After complete solution had taken place a solid precipitated that redissolved upon the addition of 80 ml of water. The solution was acidified with acetic acid to give white crystals. After recrystallization from alcohol the compound melted at 192°C to 194°C.

Therapeutic Function

Hypnotic

Pharmacokinetics

Lormetazepam is a benzodiazepine which reduces central nervous system (CNS) activity . It produces anxiolytic, muscle relaxant, sedative and hypnotic effects. Because it is a short-acting benzodiapine, it does not produce significant sedation after waking.

Metabolism

Metabolised to an inactive metabolite via glucuronide conjugation