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At least 19 recordsLinked to original sources
PubMed1988

Azaperone and azaperone-ketamine as a neuroleptic sedative and anesthetic in rats and mice.

Azaperone alone and combined with ketamine were evaluated as sedative and anesthetic agents in outbred rats and mice. Using azaperone alone the duration of immobility was 1.9 to 10.8 hours for mice and 0.9 to 2.4 hours for rats. The withdrawal reflex was not eliminated from mice receiving azaperone alone; however, the withdrawal reflex was eliminated from 0.9 to 2.4 hours in rats receiving azaperone. Azaperone produced a tachypnea in rats and male mice while a depressed respiratory rate was observed in female mice. Using azaperone combined with ketamine, the duration of immobilization was 1.1 to 8.8 hours for mice and 1.3 to 6.0 hours for rats. The duration loss of the withdrawal reflex, which was used as an indication of surgical anesthesia, was 0.9 to 1.8 hours for mice and 1.0 to 6.0 hours for rats. An increase in respiratory rate was observed in rats given the combination while mice given the combination showed transient tachypnea followed by bradypnea. Overall, azaperone alone was shown to provide sedation in mice as compared to a dose dependent anesthesia in rats. The azaperone-ketamine combination produced a surgical plane of anesthesia in both rats and mice. Azaperone and the azaperone-ketamine combination appear to be a suitable alternative to sedatives and anesthetics currently used in rats and mice.

Anesthesia↗
PubMed1977

Fluorescence characteristics of azaperone and of an azaperone mononitrogen oxide.

The structure elucidation of the compound isolated after peroxide treatment of azaperone is described. A mononitrogen oxide was formed at the piperazine N1 atom after reaction with excess hydrogen peroxide. The fluorescence characteristics of derivative were examined and compared with the native fluorescence capacities of the azaperone base; both were identical, depending on the solvent nature. The phenomenon is explained by the fact that the fluorescent properties of the azaperone molecule are principally produced by its ortho-nitrogen substituted pyridine nucleus.

Azaperone↗
PubMed1977

Open-field behaviour in sheep following treatment with the neuroleptics azaperone and acetylpromazine.

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). Azaperone significantly reduced the distance travelled, urination, and the time spent walking. However it increased nosing of the walls and floor (investigation). Azaperone also increased the numbers of sheep seen grazing and pawing and decreased the number heart vocalizing at least once. The only effect acetylpromazine had was to reduce the number of sheep heart vocalizing. The main results were interpreted as supporting a superior reduction of emotional behaviour by azaperone. It was therefore suggested that, as with pigs, azaperone might be useful for treating stress in sheep.

Acepromazine↗
PubMed1989

Clinical effects of azaperone-metomidate, as compared to propionylpromazine-xylazine-metomidate or xylazine-ketamine combinations in anaesthesia of dogs.

Eighteen dogs of Tanzanian breeds divided into three groups of 6 were anaesthetized using either azaperone-metomidate (2 mg/kg, i.m. and 10 mg/kg i.p., respectively), propionyl promazine-xylazine-metomidate (2 mg/kg i.m., 1 mg/kg i.m. and 10 mg/kg i.p., respectively), or xylazine-ketamine (1 mg/kg i.m. and 11 mg/kg i.m., respectively). The clinical effects on respiration rate, heart rate and body temperature were studied until recovery. Hypersensitivity to noise was associated with azaperone metomidate anaesthesia. The other combination produced a smooth and uneventful induction and recovery from anaesthesia. Muscle relaxation and analgesia were adequate in all groups. Duration of xylazine-ketamine anaesthesia was shortest (30 +/- 5 minutes) followed by azaperone metomidate (50 +/- 15 minutes) and the longest duration was with propionyl promazine-xylazine-ketamine (120 minutes). Azaperone and metomidate was associated with marked increases in cardiac and respiration rates and marked hypothermia, which persisted throughout. Minimal changes were observed in the other combinations. Azaperone-metomidate seems to be preferable due to the moderate period of anaesthesia adequate for most operations. However, all the three combinations offer a practical application because of the convenient route of administration.

Anesthesia↗
PubMed1976

Effects of azaperone on cardiovascular and respiratory functions in the horse.

1 The butyrophenone tranquilizer, azaperone, was administered intramuscularly, at dose levels of 0.4 and 0.8 mg/kg, to ponies and its effects on cardiovascular and respiratory functions assessed. 2 Arterial blood pH, CO2 tension (PaCO2) and O2 tension (PaO2) remained relatively constant throughout the course of action of azaperone. 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. These changes were probably caused by uptake of erythrocytes into the splenic reservoir. 4 Small increases in heart rate occurred for up to 60 min after administration of the drug, and this was followed by a slight bradycardia in some ponies. 5 Azaperone reduced mean arterial blood pressure (MAP) for at least 4 h, by which time its ataractic action was generally no longer apparent. The hypotension was caused, during the early phase of action at least, by a reduction in peripheral resistance, since cardiac output was increased slightly 20 min after its administration. Possible mechanisms underlying the cardiovascular changes are discussed. 6 In spite of reductions in arterial blood O2 content and MAP produced by azaperone, it is likely that tissue oxygenation was adequate, since arterial blood lactate concentrations were not increased.

Animals↗
PubMed1976

The applied pharmacology of azaperone in ponies.

The butyrophenone tranquilliser, azaperone, was administered intramuscularly to ponies in five series of experiments, using a dose level of 0-4 mg/kg once and 0-8 mg/kg four times. An excellent or good sedative effect was usually obtained with both dose levels, but the response was more consistent with the higher dose. The onset of sedation was apparent within 10 min of administration, the maximal effect usually occurring between 20 and 60 min while sedation was no longer apparent after 2 to 6 h. Body temperature was reduced in all animals for at least 2 h and respiratory rate was increased in some ponies but not in others. A mild tachycardia occurred in the first hour after administering azaperone (0-8 mg/kg) and arterial blood pressure was reduced for at least 4 h. The hypothesis that azaperone reduced blood pressure by blocking alpha-adrenoceptors, thereby decreasing vasomotor tone, was tested by measuring the ability of azaperone (0-8 mg/kg) to antagonise the action of standard intravenous doses of adrenaline (1-5 mug/kg) on blood pressure, Azaperone partially antagonised the pressor action of adrenaline and in comparative studies the phenothiazine tranquilliser, acepromazine (0-1 mg/kg), also exerted a similar blocking effect.

Acepromazine↗
PubMed1975

The effects of azaperone, a sedative neuroleptic of the butyrophenone series, on dominant-subordinate behaviour in wistar rats competing for food.

The effects of azaperone, a sedative neuroleptic of the butyrophenone series with outstanding anti-aggressive and anti-shock activity on dominant-subordinate relationship in pairs of rats, competing for food, are described. Treating the dominant rat of a pair with azaperone, a dose related weakening (at 0.16 and 0.31 mg/kg) and reversal (at 0.63 mg/kg and above) of the initial strong dominant-subordinate relationship is demonstratedmat 5 mg/kg the dominant-subordinate reversal is complete until the end of the test session. Dominant-subordinate relationships are modified by azaperone at doses far below those inducing gross behavioural changes. The present results point at a normalizing effect of azaperone on social interaction through inhibition of aggressive responsiveness.

Aggression↗
PubMed1994

Investigation of the metabolism of azaperone in the horse.

Urine samples collected from a horse after intramuscular administration of 40 mg of azaperone were extracted at pH 10 before and after acid hydrolysis. The extracts were concentrated and analysed by LC-MS-MS. Two N-dealkylated metabolites, N-despyridinylazaperol and N-despyridinylazaperone, and a low concentration of azaperone were detected in the unhydrolysed urine. Six metabolites; hydroxyazaperol, two hydroxyazaperones, azaperol, N-despyridinylazaperol and N-despyridinylazaperone were detected in the hydrolysed urine extracts. Using XAD-2 resin extraction, three glucuronide conjugated azaperone metabolites (hydroxyazaperol glucuronide, hydroxyazaperone glucuronide and azaperol glucuronide) were detected in the urine. The mass spectra of these metabolites show the same characteristic daughter ions as the unconjugated metabolites. The glucuronide conjugated azaperone metabolites were partially hydrolysed in the heated nebulizer interface to the unconjugated metabolites.

Animals↗
PubMed1996

Identification of metabolites of azaperone in horse urine.

Two metabolites of the tranquilizer azaperone were extracted from alkalinized horse urine after treatment with beta-glucuronidase/sulfatase from limpets (Patella vulgata). The metabolites were identified by a combination of independent chemical synthesis and GC/MS and 1H NMR analysis. The metabolites were identified as 1-(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1-piperazinyl]-1-butanol, designated as 5'-hydroxy-azaperol, and 1-(fluorophenyl)-4-[4-(5-hydroxy-2-pyridinyl)-1-piperazinyl]-1-butanone, designated as 5'-hydroxyazaperone. A TLC screening test was developed for detecting both metabolites in basic extracts of horse urine treated with beta-glucuronidase/sulfatase. The screening test was used to detect azaperone metabolites in extracts of horse urine collected for 24 h after intravenous administration of azaperone. The administration of azaperone to horses was confirmed by GC/MS identification of 5'-hydroxyazaperone and 5'-hydroxyazaperol from basic extracts of horse urine treated with beta-glucuronidase/sulfatase. The extracted metabolites were treated with bis(trimethylsilyl)acetamide to produce trimethylsilyl (TMS) ether derivatives, and mass spectra and retention times were compared to those of the synthesized metabolites treated in the same manner.

Animals↗
PubMed1990

Redistribution of cardiac output caused by opening of arteriovenous anastomoses by a combination of azaperone and metomidate.

The effects of the butyrophenone, azaperone 5 mg kg-1 i.m. alone and after addition of the imidazole derivative metomidate 6 mg kg-1 i.v. were studied in eight conscious pigs. 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). 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%). The increase in arteriovenous anastomotic blood flow was at the expense of the nutritional (= capillary) channels. Flow to the brain was maintained, but that to the left ventricle decreased in parallel with the reduction in arterial pressure. Vascular conductance of most other organs, except the skin, increased or was maintained. The addition of metomidate had no effect on Q because an increase in stroke volume (by 30%) compensated for the decrease in heart rate. Systemic vascular conductance decreased, most noticeably in the brain, left ventricle and skeletal muscle. 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.

Animals↗
PubMed1987

Mutagenicity evaluation of azaperone in the Salmonella/microsome test.

Azaperone was evaluated for its mutagenic potential by the Salmonella/microsome test. No mutagenic activity towards six S. typhimurium strains could be evidenced with azaperone at doses up to 2,000 micrograms/plate, either without or with metabolic activation at usual test conditions. Higher concentrations of liver post-mitochondrial fraction from Aroclor 1254 (ARO)-pretreated rats did not reveal any increase in the number of revertants towards S. typhimurium strains TA1537, TA1538 and TA98. Moreover, a plate-incorporation test with liver post-mitochondrial fractions from mice pretreated with phenobarbital (PB) and a liquid preincubation test with liver post-mitochondrial fractions from rats pretreated with ARO also failed to reveal any mutagenic action of azaperone towards S. typhimurium strain TA98. Thus, none of the tests used provided any indication of azaperone having a mutagenic action.

Azaperone↗
PubMedDate not supplied

Confirmation of azaperone and its metabolically reduced form, azaperol, in swine liver by gas chromatography/mass spectrometry.

The method described confirms the use of the tranquilizer azaperone by detecting the parent compound and the metabolically reduced form, azaperol. Both are confirmed in swine liver at a target concentration of 10 ppb by gas chromatography/mass spectrometry (GC/MS) with electron ionization in the selected-ion-monitoring mode. Swine liver tissue is ground with dry ice. Acetonitrile is added to extract the drug from the tissue. Sodium chloride buffer is added to the extract in preparation for solid-phase extraction (SPE). The aqueous extract is loaded onto an SPE cartridge designed to extract acidic and neutral drug residues from biological matrixes. The cartridge is washed with methanol and conditioned with sodium phosphate buffer. Azaperone and azaperol residues are eluted with a 2% ammonium hydroxide in ethyl acetate. The extracts are evaporated to dryness under a stream of nitrogen and reconstituted in ethyl acetate for GC/MS analysis. A DB-1 analytical column is used to separate the compounds prior to electron ionization. The parent ion, the base peak ion, and one diagnostic fragment ion are monitored for both compounds. The method was validated with fortified tissue samples containing both azaperone and azaperol. Azaperone-incurred tissues also were analyzed, and the presence of the parent drug and the metabolically reduced form, azaperol, was confirmed.

Acetonitriles↗
PubMed1986

Effect of azaperone on cardiovascular responsiveness in stress-sensitive pigs.

The effect of intramuscular azaperone on the cardiovascular responses to stimulation of the sympathetic nervous system was examined in thiopentone-anaesthetized stress-sensitive pigs. Sympathetic stimulation was achieved with the Valsalva-like manoeuvre, and the intravenous tyramine, isoprenaline and phenylephrine tests. The responses were monitored as the changes in heart rate and blood pressure. Azaperone exerted an alpha adrenergic blocking action and possibly a mild beta adrenergic blocking effect. It also retarded pre-adrenoreceptor activation of heart rate. It is suggested that azaperone has peripheral actions which could contribute towards its prophylactic effect in preventing stress-induced deaths in pigs.

Animals↗
PubMed2002

Use of azaperone and zuclopenthixol acetate to facilitate translocation of white-tailed deer (Odocoileus virginianus).

Thirteen wild-caught white-tailed deer (Odocoileus virginianus) from two different holding sites were chemically immobilized to facilitate capture, processing, and translocation to a new facility. The deer were divided into two treatment groups on the basis of age and received i.m. injections of the immobilizing agents via remote drug delivery systems. Group 1 (<1 yr old; n = 6) animals were immobilized with a combination of xylazine 1 mg/kg i.m. and azaperone 0.3 mg/kg i.m. At the end of the procedure the deer received zuclopenthixol acetate 1 mg/kg i.m. and (to antagonize the xylazine) tolazoline 2 mg/kg i.m. Group 2 (>1 yr old; n = 7) deer were administered xylazine 1 mg/kg i.m.. tiletamine-zolazepam 1 mg/kg i.m., and ketamine 1 mg/kg i.m. The deer in this group received a combination of azaperone 0.3 mg/kg i.m. and zuclopenthixol acetate 1 mg/kg i.m. before reversal with tolazoline 2 mg/kg i.m. All deer were recovered in a trailer before being moved in small groups to the new facility and released into the new enclosures. Azaperone and zuclopenthixol acetate provided short- and long-term relief from anxiety and allowed the animals to gradually become familiar with their new surroundings without excitement, injuries, or mortalities. Two deer exhibited mild signs of extrapyramidal side effects, which suggests that they may have received a relative overdose of the tranquilizers.

Animals↗
PubMed1988

Effects of amperozide and azaperone on aggression and productivity of growing-finishing pigs.

Levels of aggression, activity and performance were determined in 270 pigs (initial wt 29.8 kg) injected with amperozide (1.0 mg/kg i.m.), azaperone (2.2 mg/kg i.m.) or saline (.1 ml/kg i.m.) immediately prior to mixing. Pigs had ad libitum access to feed in pens of 15, and six pens were allotted to each treatment. Each pen was video-taped for 48 h after injection. Aggression was determined by continuous observation and summarized for each 2-h period. Injuries on the ears and shoulders of each pig were scored prior to injection and 1, 2, 3 and 7 d after treatment. Eating, drinking and lying were determined by scan sampling at 2-min intervals and summarized for each 2-h period. Weight gain, feed consumption and efficiency were determined for periods ending on d 3, 7, 14, 28, 42, 56, 70 and 84. Both drugs reduced total fighting from 309.8 min for saline to 190.7 and 189.6 min for amperozide- and azaperone-treated pens, respectively (P less than .01). Treatment differences in aggression and lying were evident during the initial 6 h only. Amperozide resulted in fewer fights involving two pigs (197.3/pen) than did azaperone (260.2/pen) or saline (298.3/pen) (P less than .05). Injuries to the ears (P less than .01) and total injuries (P less than .05) were less severe in amperozide-treated pigs than in pigs on the other treatments.(ABSTRACT TRUNCATED AT 250 WORDS)

Aggression↗
PubMed1988

Thin-layer chromatographic screening method for the tranquillizers azaperone, propiopromazine and carazolol in pig tissues.

A procedure is described for the detection of azaperone, propiopromazine and carazolol in pig muscle, liver and kidney tissue. The method comprises extraction from an alkaline tissue homogenate with diethyl ether, followed by cleaning up and concentration of the extract on a silica gel solid-phase extraction column. Two-dimensional thin-layer chromatography on a silica plate was used for the detection of the tranquillizers. Detection levels were 25 micrograms kg-1 for propiopromazine, 50 micrograms kg-1 for azaperone (or its metabolite azaperol) and 125 micrograms kg-1 for carazolol. In pigs treated with the usual doses the presence of propiopromazine and azaperol could be established in kidney tissue 8 h after administration, whilst in injection sites all three tranquillizers could be detected.

Adrenergic beta-Antagonists↗