Adinazolam
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Adinazolam
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| Systematic (IUPAC) name | |
| 1-(8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,5-a][1,4]benzodiazepin-1-yl)-N,N-dimethylmethanamine | |
| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C19H18ClN5 |
| Mol. mass | 351.8 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic |
| Half life | < 3 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Schedule IV(US) |
| Routes | Oral |
Adinazolam (Deracyn) is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant[1] properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed.[2]
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[edit] Pharmacology
Adinazolam produces inhibitory effects by binding to GABA receptors. This increases the effects of GABA.
[edit] Metabolism
Adinazolam was reported to have active metabolites in the August 1984 issue of The Journal of Pharmacy and Pharmacology.[3] The main metabolite is N-desmethyladinazolam.[4] The other two metabolites are alpha-hydroxyalprazolam and estazolam.[5] In the August 1986 issue of that same journal, Sethy, Francis and Day reported that proadifen inhibited the formation of N-desmethyladinazolam.[6]
[edit] Indications
Adinazolam is indicated as a treatment for anxiety and status epilepticus.
[edit] References
- ^ Lahti, Robert A.; Vimala H. Sethy, Craig Barsuhn, Jackson B. Hester (November 1983). "Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine.". Neuropharmacology 22 (11): 1277–82. doi:. PMID 6320036.
- ^ Discovers Award 2004 (PDF). Special Publications 39. Pharmaceutical Research and Manufactureres of America (April 2004). Retrieved on August 18, 2006.
- ^ Sethy, Vimala H.; R. J. Collins and E. G. Daniels (August 1984). "Determination of biological activity of adinazolam and its metabolites.". Journal of Pharmacy and Pharmacology 36 (8): 546–8. PMID 6148400.
- ^ Peng, G. W. (August 1984). "Assay of adinazolam in plasma by liquid chromatography.". Journal of Pharmaceutical Sciences 73 (8): 1173–5. doi:. PMID 6491930.
- ^ Fraser, A. D.; A. F. Isner and W. Bryan (November-December 1993). "Urinary screening for adinazolam and its major metabolites by the Emit d.a.u. and FPIA benzodiazepine assays with confirmation by HPLC.". Journal of Analytical Toxicology 17 (7): 427–31. PMID 8309217.
- ^ Sethy, Vimala H.; Jonathan W. Francis and J. S. Day (August 1986). "The effect of proadifen on the metabolism of adinazolam.". Journal of Pharmacy and Pharmacology 38 (8): 631–2. PMID 2876087.
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