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Halazepam

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Halazepam
Clinical data
Other names9-chloro- 6-phenyl- 2-(2,2,2-trifluoroethyl)- 2,5-diazabicyclo[5.4.0] undeca- 5,8,10,12-tetraen -3-one
AHFS/Drugs.comMicromedex Detailed Consumer Information
MedlinePlusa684001
Pregnancy
category
  • ?
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability?
MetabolismHepatic
Elimination half-life14 hours (drug), 50-100 hours (metabolites).
ExcretionRenal
Identifiers
  • 7-chloro- 5-phenyl- 1-(2,2,2-trifluoroethyl) -1,3-dihydro- 2H-1,4-benzodiazepin- 2-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.041.281 Edit this at Wikidata
Chemical and physical data
FormulaC17H12ClF3N2O
Molar mass352.7 g·mol−1
3D model (JSmol)
  • FC(F)(CN1C(CN=C(C2=CC=CC=C2)C3=C1C=CC(Cl)=C3)=O)F
  • InChI=1S/C17H12ClF3N2O/c18-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)22-9-15(24)23(14)10-17(19,20)21/h1-8H,9-10H2 checkY
  • Key:WYCLKVQLVUQKNZ-UHFFFAOYSA-N checkY
  (verify)

Halazepam[1] is a benzodiazepine derivative and is marketed under the brand names Alapryl and Pacinone It is no longer marketed in the United States. It had been marketed under the name Paxipam, but was withdrawn by its manufacturer, Schering Plough, for poor sales. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a trifluoroethyl derivative of nordazepam.[2] 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.[3] Halazepam has active benzodiazepine metabolites.[4]

Indications

Halazepam is indicated for the treatment of anxiety.[5]

See also

References

  1. ^ FR Patent 1518382
  2. ^ Greenblatt, D. J. (June 12, 1982). "Halazepam, another precursor of desmethyldiazepam". Lancet. 1 (8285): 1358–9. doi:10.1016/s0140-6736(82)92424-2. PMID 6123659. {{cite journal}}: Unknown parameter |coauthors= ignored (|author= suggested) (help)
  3. ^ Fann, W. E. (Mar–Apr 1982). "Pharmacology, efficacy, and adverse effects of halazepam, a new benzodiazepine". Pharmacotherapy. 2 (2): 72–9. PMID 6152591. {{cite journal}}: Unknown parameter |coauthors= ignored (|author= suggested) (help)
  4. ^ Jochemsen R, Breimer DD (1984). "Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles". Curr Med Res Opin. 8. Suppl 4: 60–79. doi:10.1185/03007998409109545. PMID 6144464.
  5. ^ Lozano, Lozano, Lozano; et al. (1990). "[Open clinical study of the efficacy and safety of Halazepam in anxiety disorders]". Actas Luso Esp Neurol Psiquiatr Cienc Afines (in Spanish; Castilian). 18 (4): 205–11. PMID 1981637. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link) CS1 maint: unrecognized language (link)