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modified on 29 April 2009 at 06:37 ••• 1,924 views

Halazepam

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Halazepam is a benzodiazepine derivative. Halazepam is indicated for the treatment of anxiety. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a trifluoromethyl derivative of nordazepam. While its structure may be similar to chlordiazepoxide and diazepam, it has both less toxicity and less tendency to cause paradoxical hostility and aggression than either of them.

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Halazepam
Systematic (IUPAC) name
7-chloro- 5-phenyl- 1-(2,2,2-trifluoroethyl) -1,3-dihydro- 2H-1,4-benzodiazepin- 2-one
Identifiers
CAS number 23092-17-3
ATC code N05BA13
PubChem 31640
DrugBank APRD01009
Chemical data
Formula C17H12ClF3N2O 
Mol. mass 352.7
Synonyms 9-chloro- 6-phenyl- 2-(2,2,2-trifluoroethyl)- 2,5-diazabicyclo[5.4.0] undeca- 5,8,10,12-tetraen -3-one
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life  ?
Excretion Renal
Therapeutic considerations
Pregnancy cat.

?

Legal status

Schedule IV (US)

Routes Oral

Mechanism of Action

Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

Brand names for Halazepam

  • Pacinone
  • Paxipam
  • Alapryl