Arfendazam
Encyclopedia
Arfendazam is a drug which is a benzodiazepine
derivative. Arfendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring, and so is most closely related to other 1,5-benzodiazepines such as clobazam
.
Arfendazam has sedative
and anxiolytic
effects similar to those produced by other benzodiazepine derivatives, but is a partial agonist
at GABAA receptors, so the sedative effects are relatively mild and it produces muscle relaxant
effects only at very high doses.
Arfendazam produces an active metabolite
lofendazam
, which is thought to be responsible for part of its effects.
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
derivative. Arfendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring, and so is most closely related to other 1,5-benzodiazepines such as clobazam
Clobazam
Clobazam , is a drug which is a benzodiazepine derivative. It has been marketed as an anxiolytic since 1975 and an anticonvulsant since 1984...
.
Arfendazam has sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
and anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
effects similar to those produced by other benzodiazepine derivatives, but is a partial agonist
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
at GABAA receptors, so the sedative effects are relatively mild and it produces muscle relaxant
Muscle relaxant
A muscle relaxant is a drug which affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics...
effects only at very high doses.
Arfendazam produces an active metabolite
Metabolite
Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...
lofendazam
Lofendazam
Lofendazam is an organic molecule which is a benzodiazepine derivative. Lofendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring; therefore, lofendazam is most closely related to other 1,5-benzodiazepines such as clobazam...
, which is thought to be responsible for part of its effects.