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
Molecular Formula | C19H22FN3O |
Molecular Weight | 327.3959 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
---|---|---|
Chemical anesthesia of northern sea otters (Enhydra lutris): results of past field studies. | 2001 Jun |
|
Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth. | 2001 Oct |
|
A review of drugs and techniques used for sedation and anaesthesia in captive rhinoceros species. | 2004 Sep |
|
Successful treatment of a squamous cell carcinoma in a white rhinoceros, Ceratotherium simum. | 2007 Dec |
|
Evaluation of the effects of the sedation with azaperone/acepromazine and immobilization with guaiphenesin/thiopentone in mules. | 2007 Feb |
|
Mild hypothermia reduces cardiac post-ischemic reactive hyperemia. | 2007 Feb 26 |
|
Anaesthesia for castration of piglets: comparison between intranasal and intramuscular application of ketamine, climazolam and azaperone. | 2007 Sep |
|
Alveolar recruitment can be predicted from airway pressure-lung volume loops: an experimental study in a porcine acute lung injury model. | 2008 |
|
Bioavailability of heme iron in biscuit filling using piglets as an animal model for humans. | 2008 Feb 18 |
|
Thermal, cardiorespiratory and cortisol responses of impala (Aepyceros melampus) to chemical immobilisation with 4 different drug combinations. | 2008 Sep |
|
[Determination of azaperone and carazolol residues in animals kidney using LC-MS/MS method]. | 2009 |
|
Butorphanol, azaperone, and medetomidine anesthesia in free-ranging white-tailed deer (Odocoileus virginianus) using radiotransmitter darts. | 2009 Apr |
|
Butorphanol-azaperone-medetomidine for immobilization of captive white-tailed deer. | 2009 Apr |
|
Rapid method for the determination of tranquilizers and a beta-blocker in porcine and bovine kidney by liquid chromatography with tandem mass spectrometry. | 2009 Apr 1 |
|
Computer tomographic investigation of subcutaneous adipose tissue as an indicator of body composition. | 2009 Jul 1 |
|
Resource efficiency and economic implications of alternatives to surgical castration without anaesthesia. | 2009 Nov |
|
Different solutions used for submucosal injection influenced early healing of gastric endoscopic mucosal resection in a preclinical study in experimental pigs. | 2009 Sep |
|
Psychological interventions in the management of common skin conditions. | 2010 |
|
Anti- or profibrillatory effects of Na(+) channel blockade depend on the site of application relative to gradients in repolarization. | 2010 |
|
Standardized intensive care unit management in an anhepatic pig model: new standards for analyzing liver support systems. | 2010 |
|
Postmortem Evaluation of Left Flank Laparoscopic Access in an Adult Female Giraffe (Giraffa camelopardalis). | 2010 |
|
Holmium-166 poly(L-lactic acid) microsphere radioembolisation of the liver: technical aspects studied in a large animal model. | 2010 Apr |
|
Granuloma encapsulation is a key factor for containing tuberculosis infection in minipigs. | 2010 Apr 6 |
|
The use of in vitro technologies coupled with high resolution accurate mass LC-MS for studying drug metabolism in equine drug surveillance. | 2010 Jan |
|
Acid-base balance and ventilation during sternal and lateral recumbency in field immobilized black rhinoceros (Diceros bicornis) receiving oxygen insufflation: a preliminary report. | 2010 Jan |
|
Apyrase treatment of myocardial infarction according to a clinically applicable protocol fails to reduce myocardial injury in a porcine model. | 2010 Jan 4 |
|
Haloperidol and azaperone in drive-net captured Southern chamois (Rupicapra pyrenaica). | 2010 Jul |
|
Enhanced blood pressure and appetite responses to chronic central melanocortin-3/4 receptor blockade in dietary-induced obesity. | 2010 Jul |
|
Increasing abdominal pressure with and without PEEP: effects on intra-peritoneal, intra-organ and intra-vascular pressures. | 2010 Jul 4 |
|
Preclinical electrogastrography in experimental pigs. | 2010 Jun |
|
Use of haloperidol and azaperone for stress control in roe deer (Capreolus capreolus) captured by means of drive-nets. | 2010 Jun |
|
Low plasma potassium in deep hypothermic cardiac arrest indicates that cardiac arrest is secondary to hypothermia: a porcine study. | 2010 Jun |
|
Multidetector row computed tomography evaluation of the micropig kidney as a potential renal donor. | 2010 Mar |
|
Minimum alveolar concentrations and hemodynamic effects of two different preparations of sevoflurane in pigs. | 2010 May |
|
Prothrombin complex concentrate mitigates diffuse bleeding after cardiopulmonary bypass in a porcine model. | 2010 Nov |
|
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 15:51:00 GMT 2023
by
admin
on
Sat Dec 16 15:51:00 GMT 2023
|
Record UNII |
19BV78AK7W
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C29710
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
||
|
WHO-VATC |
QN01AX91
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
||
|
WHO-VATC |
QN05AD90
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
||
|
CFR |
21 CFR 522.150
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
2331
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
1649-18-9
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
DB11376
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
19BV78AK7W
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
2601502
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
88301
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
D001376
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
m2161
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | Merck Index | ||
|
19BV78AK7W
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
SUB05636MIG
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
1045756
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
170976
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
15443
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
Azaperone
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
216-715-8
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
C74187
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
DTXSID2045361
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
100000086911
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY | |||
|
CHEMBL340211
Created by
admin on Sat Dec 16 15:51:00 GMT 2023 , Edited by admin on Sat Dec 16 15:51:00 GMT 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
USP
|
||
|
BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |