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Adinazolam



Adinazolam
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 37115-32-5
ATC code N05BA07
PubChem 37632
DrugBank APRD00724
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]

Contents

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.[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]

Indications

Adinazolam is indicated as a treatment for anxiety and status epilepticus.

References

  1. ^ 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. PubMed.
  2. ^ Discovers Award 2004 (PDF). Special Publications 39. Pharmaceutical Research and Manufactureres of America (April 2004). Retrieved on August 18, 2006.
  3. ^ 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. PubMed.
  4. ^ Peng, G. W. (August 1984). "Assay of adinazolam in plasma by liquid chromatography.". Journal of Pharmaceutical Sciences 73 (8): 1173-5. PubMed.
  5. ^ 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. PubMed.
  6. ^ 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. PubMed.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Adinazolam". A list of authors is available in Wikipedia.
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