Disease relevance of R-1929

• Occupational (photo)allergic contact dermatitis from azaperone in a piglet dealer [1].
• Azaperone, a drug used to calm the pigs before anesthesia, caused hypotension and bradycardia but did not affect plasma metabolites [2].
• The acute toxicity of mafoprazine in mice was slightly stronger than that of azaperone [3].
• The rapid intravenous administration of the butyrophenone tranquilliser, azaperone, at a dose rate of 0.29-0.57 mg/kg body weight resulted in the immediate onset of excitement and ataxia of varying degree in over half the animals [4].
• Mutagenicity evaluation of azaperone in the Salmonella/microsome test [5].

Psychiatry related information on R-1929

• The present results point at a normalizing effect of azaperone on social interaction through inhibition of aggressive responsiveness [6].

High impact information on R-1929

• METHODS: Healthy volunteers received single oral doses of placebo, the benzodiazepine agonist triazolam (0.25 mg) or the azaperone anxiolytic buspirone (20 mg), in a double-blind, three-way crossover study [7].
• BACKGROUND AND OBJECTIVES: Benzodiazepine agonists and azaperone derivatives are used clinically as anxiolytics but have different neuroreceptor mechanisms of action [7].
• METHODS: After approval of the animal care committee, six Pietrain MHS and six control (MHN) swine were anesthetized with azaperone 4 mg/kg intramuscularly and metomidate 10 mg/kg intraperitoneally [8].
• The behavior of individual Romney ewes in an open field was observed after intramuscular injection of isotonic saline or two doses of azaperone (0.5, 1.0 mg/kg) or acetylpromazine (0.1, 0.25 mg/kg) [9].
• 5 Azaperone reduced mean arterial blood pressure (MAP) for at least 4 h, by which time its ataractic action was generally no longer apparent [10].

Chemical compound and disease context of R-1929

• Hypersensitivity to noise was associated with azaperone metomidate anaesthesia [11].

Biological context of R-1929

• 3 Azaperone did not modify plasma protein concentration but venous blood packed cell volume and haemoglobin concentration were reduced by 5 to 10% for at least 4 hours [10].
• In previous experiments, azaperone was found to be weakly mutagenic, after metabolic activation, in the Ames assay [12].
• Fifteen minutes after administration of azaperone, systemic arterial pressure was reduced by 35% as a result of a 45% increase in systemic vascular conductance and 10% decrease in cardiac output (Q) [13].
• Urine samples collected from a horse after intramuscular administration of 40 mg of azaperone were extracted at pH 10 before and after acid hydrolysis [14].
• Treatment with azaperone was not related to farrowing environment, piglet weight or litter size [15].

Anatomical context of R-1929

• We conclude that azaperone alone and in combination with metomidate had only a moderate effect on Q, but caused a redistribution in favour of arteriovenous anastomoses [13].
• Two metabolites of the tranquilizer azaperone were extracted from alkalinized horse urine after treatment with beta-glucuronidase/sulfatase from limpets (Patella vulgata) [16].
• After azaperone, 23% of the radioactive labelled microspheres (15 (SD 1) microns) injected into the left atrium were detected in the lungs as a result of opening of arteriovenous anastomoses (baseline 3%) [13].
• The responses of 83 Meishan gilts given azaperone (1.0 mg/kg) and ketamine (5 mg/kg) intramuscularly at one of four sites: the cervical muscles (20); the triceps muscle (m triceps brachii) (20); the middle gluteal muscle (m gluteus medius) (22); and the fascia lata muscle (m fascia lata) (21) were recorded [17].
• The effect of intramuscular azaperone on the cardiovascular responses to stimulation of the sympathetic nervous system was examined in thiopentone-anaesthetized stress-sensitive pigs [18].

Associations of R-1929 with other chemical compounds

• The effects of azaperone, a sedative neuroleptic of the butyrophenone series, on dominant-subordinate behaviour in wistar rats competing for food [6].
• This has been verified by combined gas chromatography-mass spectrometry of biological samples from rats given orally a series of heterocyclic derivatives bearing a 4-aryl(phenyl, pyrimidinyl, pyridyl or thiazolyl)-1-piperazinylalkyl moiety (oxypertine, zolertine, millipertine, empiprazole, dapiprazole, antrafenine, piribedil, azaperone) [19].
• In the ELISA, the detection capabilities of the six sedatives, azaperol, azaperone, carazolol, acepromazine, chlorpromazine, and propionylpromazine are 5, 15, 5, 5, 20 and 5 [micro sign]g kg(-1), respectively [20].
• No semen was obtained from animals when azaperone was used instead of xylazine, despite the use of a successful standardised method of electrical stimulation [21].
• Adequate pre-medication with azaperone and a smooth induction were ensured for both pigs, which were anaesthetized simultaneously with sodium thiopentone followed by endotracheal intubation and intermittent positive pressure ventilation [22].

Analytical, diagnostic and therapeutic context of R-1929

• Standing anesthesia, incorporating butorphanol and azaperone together with local anesthetic infiltration, facilitated the laparoscopy [23].
• In captive rhinoceroses conditioned to routine handling, a combination of butorphanol and azaperone at mean (+/- SD) doses of 69.3 +/- 18.0 mg and 103.1 +/- 20.9 mg, respectively, was used to produce levels of neuroleptanalgesia ranging from light "standing" sedation to deeper planes of anesthesia producing sternal and lateral recumbency [24].
• Determination of residues of azaperone in the kidneys by liquid chromatography with fluorescence detection [25].
• Combined azaperone and metomidate anaesthesia in liver transplantation in the pig [26].
• Butorphanol and azaperone produced adequate muscle relaxation and apparently adequate analgesia for minor surgical interferences, including abdominal laparoscopy [24].

References