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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | IM |
| ATCvet code | |
| Pharmacokinetic data | |
| Metabolism | Hepatic |
| Eliminationhalf-life | 4 hours |
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| CAS Number | |
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| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.015.197 |
| Chemical and physical data | |
| Formula | C19H22FN3O |
| Molar mass | 327.403 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 90 to 95 °C (194 to 203 °F) |
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Azaperone is apyridinylpiperazine andbutyrophenoneneurolepticdrug withsedative andantiemetic effects, which is used mainly as atranquilizer inveterinary medicine.[1] It is uncommonly used in humans as anantipsychotic drug.
Azaperone acts primarily as adopamineantagonist but also has someantihistaminic andanticholinergic properties as seen with similar drugs such ashaloperidol. Azaperone may causehypotension and while it has minimal effects on respiration in pigs, high doses in humans can causerespiratory depression.
The most common use for azaperone is in relatively small doses as a "serenic" (to reduce aggression) in farmed pigs, either to stop them fighting or to encourage sows to accept piglets. Higher doses are used foranesthesia in combination with other drugs such asxylazine,tiletamine andzolazepam. Azaperone is also used in combination with strong narcotics such asetorphine orcarfentanil for tranquilizing large animals such as elephants.[2] Use in horses is avoided as adverse reactions may occur.
TheEuropean Medicines Agency has established amaximum residue limit for azaperone when administered to pigs.[3]
Azaperone (under the brand nameStresnil) was approved for use in pigs in the USA in 1983, under NADA 115-732.[4]
The alkylation of2-chloropyridine (1) withpiperazine gives 1-(pyridin-2-yl)piperazine [67980-77-2] (2). The attachement of the sidechain by reaction with 4-chloro-4'-fluorobutyrophenone [3874-54-2] (3) completed the synthesis of azaperone (4).