Halazepam

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Halazepam
Halazepam.svg
Halazepam3d.png
Systematic (IUPAC) name
7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-2-one
Clinical data
AHFS/Drugs.com Micromedex Detailed Consumer Information
MedlinePlus a684001
Pregnancy
category
  •  ?
Routes of
administration		 Oral
Legal status
Legal status
Pharmacokinetic data
Metabolism Hepatic
Biological half-life 14 hours (halazepam), 50–100 hours (metabolites).
Excretion Renal
Identifiers
CAS Number 23092-17-3 YesY
ATC code N05BA13 (WHO)
PubChem CID 31640
IUPHAR/BPS 7195
DrugBank DB00801 YesY
ChemSpider 29343 YesY
UNII 320YC168LF YesY
KEGG D00338 YesY
ChEMBL CHEMBL970 YesY
Synonyms 9-chloro-6-phenyl-2-(2,2,2-trifluoroethyl)-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one
Chemical data
Formula C17H12ClF3N2O
Molar mass 352.7 g/mol
3D model (Jmol) Interactive image
  (verify)

Halazepam is a benzodiazepine derivative that was marketed under the brand names Paxipam in the United States,[1] Alapryl in Spain,[2] and Pacinone in Portugal.[3]

Medical uses[edit]

Halazepam was used for the treatment of anxiety.[1]

Adverse effects[edit]

Adverse effects include drowsiness, confusion, dizziness, and sedation. Gastrointestinal side effects have also been reported including dry mouth and nausea.[1]

Pharmacokinetics and pharmacodynamics[edit]

Pharmacokinetics and pharmacodynamics were listed in Current Psychotherapeutic Drugs published in June 15, 1998 as follows:[4]

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[edit]

Halazepam is classified as a schedule 4 controlled substance with a corresponding code 2762 by the Drug Enforcement Administration (DEA).[5]

Commercial production[edit]

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 However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[1]

See also[edit]

References[edit]

  1. ^ a b c d "halazepam". Drugs.com. Retrieved December 11, 2014. 
  2. ^ "Alapryl". Drugs.com. Retrieved December 11, 2014. 
  3. ^ "Pacinone". Drugs.com. Retrieved December 11, 2014. 
  4. ^ Quitkin, Frederick M. ... (1998). Current therapeutic drugs (2nd ed.). Washington: American Psychiatric Press. p. 166. ISBN 0880489944. 
  5. ^ "SCHEDULES OF CONTROLLED SUBSTANCES". Code of Federal Reguations. 2012-04-01. pp. § 1308.14 Schedule IV. Retrieved December 12, 2014. 

External links[edit]

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