Halazepam is a benzodiazepine derivative that was marketed under the brand names Paxipam in the United States,[2] Alapryl in Spain,[3] and Pacinone in Portugal.[4]
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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 |
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Routes of administration | Oral |
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Metabolism | Hepatic |
Elimination half-life | 14 hours (halazepam), 50–100 hours (metabolites). |
Excretion | Renal |
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ECHA InfoCard | 100.041.281 |
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Formula | C17H12ClF3N2O |
Molar mass | 352.74 g·mol−1 |
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Adverse effects include drowsiness, confusion, dizziness, and sedation. Gastrointestinal side effects have also been reported including dry mouth and nausea.[2]
Pharmacokinetics and pharmacodynamics were listed in Current Psychotherapeutic Drugs published on June 15, 1998 as follows:[5]
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 |
Halazepam is classified as a schedule 4 controlled substance with a corresponding code 2762 by the Drug Enforcement Administration (DEA).[6]
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 However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[2]