Halazepam
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| Systematic (IUPAC) name | |
|---|---|
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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 |
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| Legal status |
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| Routes of administration | Oral |
| Pharmacokinetic data | |
| Metabolism | Hepatic |
| Biological half-life | 14 hours (halazepam), 50–100 hours (metabolites). |
| Excretion | Renal |
| Identifiers | |
| CAS Number |
23092-17-3  |
| ATC code | N05BA13 |
| PubChem | CID 31640 |
| IUPHAR/BPS | 7195 |
| DrugBank |
DB00801 |
| ChemSpider |
29343 |
| UNII |
320YC168LF |
| KEGG |
D00338 |
| ChEMBL |
CHEMBL970 |
| 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 |
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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 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
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 However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[1]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
- Benzodiazepines
- Nordazepam
- Diazepam
- Chlordiazepoxide
- Quazepam, fletazepam, triflubazam — benzodiazepines with trifluoromethyl group attached
References
- 1 2 3 4 "halazepam". Drugs.com. Retrieved December 11, 2014.
- ↑ "Alapryl". Drugs.com. Retrieved December 11, 2014.
- ↑ "Pacinone". Drugs.com. Retrieved December 11, 2014.
- ↑ Quitkin, Frederick M. ... (1998). Current therapeutic drugs (2nd ed.). Washington: American Psychiatric Press. p. 166. ISBN 0880489944.
- ↑ "SCHEDULES OF CONTROLLED SUBSTANCES". Code of Federal Reguations. 2012-04-01. pp. § 1308.14 Schedule IV. Retrieved December 12, 2014.
External links
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