Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H22FN3O |
Molecular Weight | 327.3959 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(C=C1)C(=O)CCCN2CCN(CC2)C3=CC=CC=N3
InChI
InChIKey=XTKDAFGWCDAMPY-UHFFFAOYSA-N
InChI=1S/C19H22FN3O/c20-17-8-6-16(7-9-17)18(24)4-3-11-22-12-14-23(15-13-22)19-5-1-2-10-21-19/h1-2,5-10H,3-4,11-15H2
DescriptionSources: http://www.elephantcare.org/Drugs/azaperon.htm
Sources: http://www.elephantcare.org/Drugs/azaperon.htm
Azaperone (Stresnil, Fluoperidol) is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects. It is mainly as a tranquilizer in veterinary medicine. Azaperone is officially indicated for the “control of aggressiveness when mixing or regrouping weanling or feeder pigs weighing up to 36.4 kg”. It is also used clinically as a general tranquilizer for swine, in particular with aggressive sows to allow piglets to be accepted, and as a preoperative agent prior to general anesthesia or cesarian section with local anesthesia. Azaperone has also been used as a neuroleptic in horses, but some horses develop adverse reactions (sweating, muscle tremors, panic reaction, CNS excitement) and IV administration has resulted in significant arterial hypotension in the horse; because of these effects, most clinicians avoid the use of this drug in equines. Azaperone appears to have minimal effects on respiration and may inhibit some of the respiratory depressant actions of general anesthetics. A slight reduction of arterial blood pressure has been measured in pigs after IM injections of azaperone, which is apparently due to slight alpha-adrenergic blockade. Azaperone has been demonstrated to prevent the development of halothane-induced malignant hyperthermia in susceptible pigs. Preliminary studies have suggested that the effects of butyrephenones may be antagonized by 4-aminopyridine. Azaperone acts primarily as a dopamine antagonist but also has some antihistaminic and anticholinergic properties as seen with similar drugs such as haloperidol. Azaperone may cause hypotension and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression which may be why it is rarely used in humans. Higher doses are used for anesthesia in combination with other drugs such as xylazine, tiletamine and zolazepam. Azaperone is also used in combination with strong narcotics such as etorphine or carfentanil for tranquilizing large animals such as elephants.
CNS Activity
Sources: http://www.redalyc.org/html/919/91931189013/
Curator's Comment: Azaperone is thought to act on CNS to make animals indifferent to their surrounding environment
Originator
Sources: http://www.google.co.ve/patents/CA2732940A1
Curator's Comment: # Janssen Pharmaceutica laboratories
Approval Year
PubMed
Title | Date | PubMed |
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Rapid brain cooling in intubated pigs through nasal flushing with oxygen: prevention of brain hyperthermia. | 2001 |
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Rectal prolapse associated with a healed pelvic fracture in a pregnant free-ranging African black rhinoceros (Diceros bicornis). Part 1: anaesthesia. | 2001 Dec |
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Chemical anesthesia of northern sea otters (Enhydra lutris): results of past field studies. | 2001 Jun |
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Use of azaperone and zuclopenthixol acetate to facilitate translocation of white-tailed deer (Odocoileus virginianus). | 2002 Jun |
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Provision of anaesthesia for porcine cardiac transplantation at the veterinary school in Trinidad and Tobago. | 2003 Jun |
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Induction of anaesthesia in pigs using a new alphaxalone formulation. | 2003 Nov 15 |
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Development of a rapid screening test for veterinary sedatives and the beta-blocker carazolol in porcine kidney by ELISA. | 2004 Feb |
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Severe hypoxaemia in field-anaesthetised white rhinoceros (Ceratotherium simum) and effects of using tracheal insufflation of oxygen. | 2004 Jun |
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A review of drugs and techniques used for sedation and anaesthesia in captive rhinoceros species. | 2004 Sep |
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Use of buspirone and enrichment to manage aberrant behavior in an American badger (Taxidea taxus). | 2005 Sep |
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Euthanasia of exotic pigs. | 2006 Jul 8 |
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Evaluation of the effects of the sedation with azaperone/acepromazine and immobilization with guaiphenesin/thiopentone in mules. | 2007 Feb |
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Determination of residues of azaperone in the kidneys by liquid chromatography with fluorescence detection. | 2007 Mar 14 |
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Reliability of continuous cardiac output measurement during intra-abdominal hypertension relies on repeated calibrations: an experimental animal study. | 2008 |
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A novel method for transuterine identification of piglets. | 2008 Jul |
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Computer tomographic investigation of subcutaneous adipose tissue as an indicator of body composition. | 2009 Jul 1 |
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Resource efficiency and economic implications of alternatives to surgical castration without anaesthesia. | 2009 Nov |
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Different solutions used for submucosal injection influenced early healing of gastric endoscopic mucosal resection in a preclinical study in experimental pigs. | 2009 Sep |
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Standardized intensive care unit management in an anhepatic pig model: new standards for analyzing liver support systems. | 2010 |
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The use of in vitro technologies coupled with high resolution accurate mass LC-MS for studying drug metabolism in equine drug surveillance. | 2010 Jan |
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Enhanced blood pressure and appetite responses to chronic central melanocortin-3/4 receptor blockade in dietary-induced obesity. | 2010 Jul |
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Preclinical electrogastrography in experimental pigs. | 2010 Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.elephantcare.org/Drugs/azaperon.htm
Swine: a) For approved indication of mixing feeder or weanling pigs: 2.2 mg/kg deeply IM' b) Preanesthetic: 2 - 4 mg/kg IM; Immobilizing agent: 5.3 - 8 mg/kg IM; c) Sedation: 1 mg/kg IM; Reduction of aggressiveness: 2.5 mg/kg IM;
Total dose of azaperone for adult Asian captive elephants 80-100 mg; up to 140 mg for a large elephant. Induction in 20-30 minutes; duration 45-60 minutes Knock-down or immobilant: 5 - 10 mg/kg IM
Route of Administration:
Intramuscular
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NCI_THESAURUS |
C29710
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WHO-VATC |
QN01AX91
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QN05AD90
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CFR |
21 CFR 522.150
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ACTIVE MOIETY