Sunday, 14 December 2014

Pharmacology and chemistry of antianxiety drugs

Antianxiety is an important class of drug for the preparation of GPAT. In this article you will complete pharmacology and chemistry of the drugs of this class including benzodiazepines.

Classification of antianxiety drugs
Classification antianxiety drugs


Individual pharmacology of each class


1. Benzodoazepines:


Structural activity relationship:

SAR of benzodiazepines


Ring A: Should be aromatic.
  • Electronegative substitution at 7 increase activity.
  • 6,8 or 9 substitution- decrease activity.
Ring B: Proton accepting group is the primary requirement to bind with GABAa receptor.
  • Proton accepting group at 2 must for benzodiazepine.
  • 3-OH/ 3-COOR has no effect increase excretion.
  • N1 has no effect but sterically bulky substituent can decrease activity.
  • C=N if changed to C-N decrease activity.
Ring C: 5-phenyl ring is not required for binding but for the hydrophobicity.
  • 4' substitution- Decrease activity ( Steric limitations).
2. Other antianxiety drugs:

a) Buspirone: 5-HT1A autoreceptors agonists- Decrease the activity of serotonergic neurons.

b) Hydroxyzine: Antihistaminic (H1).

c) β- blockers: In the symptoms of anxiety linked with sympathetic over activity.



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