ketazolam

Toxicity

Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.

Description

Benzodiazepines are psychoactive compounds that act as sedatives, hypnotics, anxiolytics, anticonvulsants, and muscle relaxants. Ketazolam is a benzodiazepine derivative that was used as an anxiolytic in the 1980s. Tolerance within fifteen days, physical dependence, and benzodiazepine withdrawal syndrome are associated with ketazolam use. This product is intended for forensic purposes.

Originator

Anxon,Beecham,UK,1980

The Uses of ketazolam

A psychotropic benzodiazepine derivative with hypnotic and anxiolytic properties. Controlled Substance.

Indications

Ketazolam could be used for the treatment of anxiety. In approved countries, it is indicated for the treatment of anxiety, tension, irritability and similar stress related symptoms.

Background

Ketazolam is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant activity. Ketazolam is not approved in Canada or America.

Definition

ChEBI: Ketazolam is a benzodiazepine.

Manufacturing Process

A solution of 0.7 g of 2-(2-amino-N-methylacetamido)-5-chlorobenzophenone in 10 ml of a 50% solution (by weight) of diketene in acetone is refluxed for 3 hours and then evaporated to give a brown oil. The oil is chromatographed on 200 g of silica gel using a 1:1 (by volume) mixture of ethyl acetate cyclohexane; 25 ml fractions are collected. Fractions 11-14 are combined, mixed with chloroform, evaporated and triturated with ether to give 0.337 g of 11-chloro-8,12b-dihydro-2,8-dimethyl-12b-phenyl-4H-[1,3]oxazino[3,2-d] [1.4] benzodiazepine-4,7(6H)-dione as a pale yellow solid, MP 174°C to 176°C.

Therapeutic Function

Antianxiety

Pharmacokinetics

Benzodiazepines enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA), which results in sedative, hypnotic, anxiolytic, anticonvulsant, muscle relaxant and amnesic action. Benzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Metabolism

Ketazolam is metabolized to diazepam, followed by demoxepam, and finally desmethyldiazepam.