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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Coronary artery reperfusion: The ADP receptor P2Y(1) mediates early reactive hyperemia in vivo in pigs. | 2004 Dec |
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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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Placentation in the paca (Agouti paca L). | 2005 Feb 28 |
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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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Physiological routes from intra-uterine seminal contents to advancement of ovulation. | 2006 Aug 3 |
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Euthanasia of exotic pigs. | 2006 Jul 8 |
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Gelatinases, endonuclease and Vascular Endothelial Growth Factor during development and regression of swine luteal tissue. | 2006 Nov 30 |
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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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Mild hypothermia reduces cardiac post-ischemic reactive hyperemia. | 2007 Feb 26 |
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Bioavailability of heme iron in biscuit filling using piglets as an animal model for humans. | 2008 Feb 18 |
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Immobilization of black bears (Ursus americanus) with a combination of butorphanol, azaperone, and medetomidine. | 2008 Jul |
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A novel method for transuterine identification of piglets. | 2008 Jul |
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Comprehensive screening and quantification of veterinary drugs in milk using UPLC-ToF-MS. | 2008 Jul |
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Thermal, cardiorespiratory and cortisol responses of impala (Aepyceros melampus) to chemical immobilisation with 4 different drug combinations. | 2008 Sep |
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Resource efficiency and economic implications of alternatives to surgical castration without anaesthesia. | 2009 Nov |
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Haloperidol and azaperone in drive-net captured Southern chamois (Rupicapra pyrenaica). | 2010 Jul |
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Increasing abdominal pressure with and without PEEP: effects on intra-peritoneal, intra-organ and intra-vascular pressures. | 2010 Jul 4 |
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Prothrombin complex concentrate mitigates diffuse bleeding after cardiopulmonary bypass in a porcine model. | 2010 Nov |
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64-channel multi-detector row CT angiographic evaluation of the micropigs for potential living donor lung transplantation. | 2010 Sep |
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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QN01AX91
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QN05AD90
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CFR |
21 CFR 522.150
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ACTIVE MOIETY