Adinazolam
Encyclopedia
Adinazolam is a benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...

 derivative. It possesses anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

, anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...

, sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....

, and antidepressant
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...

 properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam
Alprazolam
Alprazolam is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor...

, which he also developed.

Pharmacology

Adinazolam produces inhibitory effects by binding to GABA receptors. This increases the effects of GABA.

Metabolism

Adinazolam was reported to have active metabolites in the August 1984 issue of The Journal of Pharmacy and Pharmacology. The main metabolite is N-desmethyladinazolam. The other two metabolites are alpha-hydroxyalprazolam and estazolam
Estazolam
Estazolam is a benzodiazepine derivative drug developed by Upjohn in the 1970s. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties...

. In the August 1986 issue of that same journal, Sethy, Francis and Day reported that proadifen
Proadifen
Proadifen is an inhibitor of cytochrome P450 enzymes, preventing some types of drug metabolism....

inhibited the formation of N-desmethyladinazolam.

Chemistry

Hester, J. B.; Rudzik, A. D.; Von Voigtlander, P. F.; J. Med. Chem. 1980, 23, 392.

http://dx.doi.org/10.1021/jm00178a009
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