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词条 Halazepam
释义

  1. Medical uses

  2. Adverse effects

  3. Pharmacokinetics and pharmacodynamics

  4. Regulatory Information

  5. Commercial production

  6. See also

  7. References

  8. External links

{{Drugbox
| Watchedfields = changed
| verifiedrevid = 461743655
| IUPAC_name = 7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-2-one
| image = Halazepam.svg
| width = 170
| image2 = Halazepam3d.png
| width2 = 150
| tradename =
| Drugs.com = {{drugs.com|CONS|halazepam}}
| MedlinePlus = a684001
| pregnancy_category = ?
| legal_CA = Schedule IV
| legal_DE = Rx-only/Anlage III
| legal_US = Schedule IV
| routes_of_administration = Oral
| bioavailability =
| metabolism = Hepatic
| elimination_half-life = 14 hours (halazepam), 50–100 hours (metabolites).
| excretion = Renal
| IUPHAR_ligand = 7195
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 23092-17-3
| ATC_prefix = N05
| ATC_suffix = BA13
| PubChem = 31640
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00801
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 29343
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 320YC168LF
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00338
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 970
| C=17 | H=12 | Cl=1 | F=3 | N=2 | O=1
| molecular_weight = 352.7 g/mol
| smiles = FC(F)(CN1C(CN=C(C2=CC=CC=C2)C3=C1C=CC(Cl)=C3)=O)F
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = WYCLKVQLVUQKNZ-UHFFFAOYSA-N
| synonyms = 9-chloro-6-phenyl-2-(2,2,2-trifluoroethyl)-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-3-one
}}Halazepam is a benzodiazepine derivative that was marketed under the brand names Paxipam in the United States,[1] Alapryl in Spain,[1] and Pacinone in Portugal.[2]

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:[3]

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).[4]

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.[5]

See also

  • Benzodiazepines
  • Nordazepam
  • Diazepam
  • Chlordiazepoxide
  • Quazepam, fletazepam, triflubazam — benzodiazepines with trifluoromethyl group attached

References

1. ^{{cite web|title=Alapryl|url=https://www.drugs.com/international/alapryl.html|publisher=Drugs.com|accessdate=December 11, 2014}}
2. ^{{cite web|title=Pacinone|url=https://www.drugs.com/international/pacinone.html|publisher=Drugs.com|accessdate=December 11, 2014}}
3. ^{{cite book|last1=Quitkin|first1=Frederick M. ... |title=Current therapeutic drugs|date=1998|publisher=American Psychiatric Press|location=Washington|isbn=0880489944|page=166|edition=2nd}}
4. ^{{cite web|title=SCHEDULES OF CONTROLLED SUBSTANCES|url=http://www.gpo.gov/fdsys/pkg/CFR-2012-title21-vol9/xml/CFR-2012-title21-vol9-part1308.xml|publisher=Code of Federal Reguations|accessdate=December 12, 2014|pages=§ 1308.14 Schedule IV|date=2012-04-01}}
5. ^{{cite web|title=halazepam|url=https://www.drugs.com/mtm/halazepam.html|publisher=Drugs.com|accessdate=December 11, 2014}}

External links

  • Inchem - Halazepam
{{Benzodiazepines}}{{Anxiolytics}}{{GABAAR PAMs}}{{sedative-stub}}

6 : Abandoned drugs|Benzodiazepines|Chloroarenes|GABAA receptor positive allosteric modulators|Lactams|Trifluoromethyl compounds

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