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Withdrawn drugs
Halazepam
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Halazepam

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Halazepam
Halazepam.svg
Halazepam3d.png
Clinical data
Other names 9-chloro-6-phenyl-2-(2,2,2-trifluoroethyl)-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one
AHFS/Drugs.com Micromedex Detailed Consumer Information
MedlinePlus a684001
Pregnancy
category
  • ?
Routes of
administration		 Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Metabolism Hepatic
Elimination half-life 14 hours (halazepam), 50–100 hours (metabolites).
Excretion Renal
Identifiers
  • 7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-2-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.041.281
Chemical and physical data
Formula C17H12ClF3N2O
Molar mass 352.74 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 is a benzodiazepine derivative that was marketed under the brand names Paxipam in the United States,Alapryl in Spain, and Pacinone in Portugal.

Medical uses

Halazepam was used for the treatment of anxiety.

Adverse effects

Adverse effects include drowsiness, confusion, dizziness, and sedation. Gastrointestinal side effects have also been reported including dry mouth and nausea.

Pharmacokinetics and pharmacodynamics

Pharmacokinetics and pharmacodynamics were listed in Current Psychotherapeutic Drugs published on June 15, 1998 as follows:

Onset of action Intermediate to slow
Plasma half life 14 hr for parent drug and 30-100 hr for its metabolite
Peak plasma levels 1-3 hr for parent drug and 3-6 hf for its metabolite
Metabolism Metabolized into desmethyldiazepam and 3-hydroxyhalazepam (in the liver)
Excretion Excreted through kidneys
Protein binding 98% bound to plasma protein

Regulatory Information

Halazepam is classified as a schedule 4 controlled substance with a corresponding code 2762 by the Drug Enforcement Administration (DEA).

Commercial production

Halazepam was invented by Schlesinger Walter in the U.S. It was marketed as an anti-anxiety agent in 1981. However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.

See also

External links



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