Halazepam

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]

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
  • CA: Schedule IV
  • DE: Prescription only (Anlage III for higher doses)
  • US: Schedule IV
Pharmacokinetic data
MetabolismHepatic
Elimination half-life14 hours (halazepam), 50–100 hours (metabolites).
ExcretionRenal
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.041.281
Chemical and physical data
FormulaC17H12ClF3N2O
Molar mass352.7 g/mol g·mol−1
3D model (JSmol)
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Medical uses

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

Adverse effects

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

Pharmacokinetics and pharmacodynamics

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

Onset of actionIntermediate to slow
Plasma half life14 hr for parent drug and 30-100 hr for its metabolite
Peak plasma levels1-3 hr for parent drug and 3-6 hf for its metabolite
MetabolismMetabolized into desmethyldiazepam and 3-hydroxyhalazepam (in the liver)
ExcretionExcreted through kidneys
Protein binding98% 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).[5]

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 However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[1]

See also

References

  1. "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 Regulations. 2012-04-01. pp. § 1308.14 Schedule IV. Retrieved December 12, 2014.


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