Halazepam 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
CA : Schedule IV
DE : Prescription only (Anlage III for higher doses)
US : Schedule IV
Metabolism Hepatic Elimination half-life 14 hours (halazepam), 50–100 hours (metabolites). Excretion Renal
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 Formula C 17 H 12 Cl F 3 N 2 O 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
Y Key:WYCLKVQLVUQKNZ-UHFFFAOYSA-N
Y
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 [ ]
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 on 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 [ ]
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 However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[1]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 [ ]
^ a b c d "halazepam" . Drugs.com. Retrieved December 11, 2014 .
^ "Alapryl" . Drugs.com. Retrieved December 11, 2014 .
^ "Pacinone" . Drugs.com. Retrieved December 11, 2014 .
^ Sellers EM (1998). "Antianxiety agents: benzodiazepine derivatives". In Quitkin FM, et al. (eds.). Current Psychotherapeutic Drugs (2nd ed.). Washington: American Psychiatric Press. p. 166. ISBN 978-0-88048-994-2 .
^ "SCHEDULES OF CONTROLLED SUBSTANCES" . Code of Federal Regulations. 2012-04-01. pp. § 1308.14 Schedule IV. Retrieved December 12, 2014 .
External links [ ]
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