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Butorphanol and azaperone as a safe alternative for repeated chemical restraint in captive white rhinoceros (Ceratotherium simum).

Anesthesia in the white rhinoceros (Ceratotherium simum) has routinely involved potent narcotic anesthetic agents such as etorphine or carfentanil with their associated adverse side effects. 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. This combination was used for repeated (minimum repeat frequency of 3 days between events) anesthetic episodes (n = 26) in two animals, with the remaining episode performed in a white rhinoceros with chronic renal disease. The action of butorphanol was satisfactorily reversed with naltrexone (125 mg i.v. and 125 mg i.m.). Results (mean +/- SD) include sternal recumbency achieved in 14.1 +/- 8.1 min after i.m. dosing, standing and ambulation occurred in 1.7 +/- 0.6 min after reversal, heart rate was 62.0 +/- 10.1 beats/min, respiratory rate was 14.7 +/- 5.6 breaths/min, and percentage of oxygen saturation of hemoglobin (Spo2) was 89.2 +/- 3.0%. Without supplementation, the total elapsed time ranged from 44.9 min to 103.0 min, whereas elapsed times up to 214.3 min were achieved with supplementation (mean time to supplementation was 28.0 +/- 13.9 min after initial dosing). Butorphanol and azaperone produced adequate muscle relaxation and apparently adequate analgesia for minor surgical interferences, including abdominal laparoscopy. Respiratory rates and Spo2 measurements were improved compared with reports of using more potent opioids in this species.

Analgesics, Opioid↗

[Caesarean section in sows anesthetized with Azaperone and Metomidate (author's transl)].

213 caesarean sections and 157 hysterectomies were carried out in gilts and sows with different body weight (table I). The neuroleptic Azaperone and the hypnotic Metomidate were used for anaesthesia with different administration (table II). Local analgesia and premedication with Atropine. The duration of the anaesthesia was 45 minutes and where prolongation was necessary, Metomidate, Azaperone or barbiturates were used alone or in combinations once or more. The indications (table III) for caesarean section were retarded birth in 70 sows, dislocation of uterus in 74 sows and in 69 sows by other indications. Hysterectomy was indicated by retarded birth in 93 sows, dislocations of uterus in 40 cases and in 24 cases by other indications. In 183 operations (table IV) 1006 living piglets were delivered, and 703 were alive at discharge (70%). The chances of survival depends on the composition of the litter, in litters of piglets alive only, 76% survived at discharge; in litters consisting of both alive and stillborn 69% survived and 59% survived in litters consisting of piglets alive and post mortem piglets. The total survival of the sows was 78%, 80% after caesarean section and 76% after hysterectomy. It is pointed out that most of the patients operated were in a very late phase of birth.

Anesthesia, Obstetrical↗

Comparisons of rotamer populations of nialamide, azaperone, and chloroquine in solid state and in solution.

IR and NMR spectroscopy were combined with previously published X-ray crystallographic data to determine the solution conformations of the -(CH2)n- fragments of nialamide, azaperone, and chloroquine. The solution conformation of these compounds then was compared to the solid-state conformation. In addition, the limits of the IR-X-ray method are discussed. This paper shows that a combination of IR, NMR, and X-ray crystallographic data can lead to a complete picture of the conformations available to drugs. In addition, the danger of using solid-state conformational data alone to make pharmacological suggestions is illustrated.

Azaperone↗

Determination of a method for detecting and quantifying azaperone, azaperol and carazolol in pig tissues by liquid chromatography-tandem mass spectrometry.

A quick, simple method for quantifying carazolol, azaperol and azaperone is described. Liquid extraction was followed by a clean-up on an Oasis SPE cartridge. The analytes were separated by HPLC and analysed by MS-MS with atmospheric pressure chemical ionisation in the positive mode. The method was applied to muscle and kidney from untreated pigs, the samples being spiked with the three molecules of interest. Recovery was between 70 and 106%. Quantification parameters were also good: the accuracy was between 80 and 110% and the coefficient of variation did not exceed 16%, being below 8% for 90% of the samples. Linearity was good from MRL/4 to 2MRL. For unequivocal identification of each analyte, four ions were detected. The method proved very suitable for routine analysis.

Animals↗

Analysis and identification of azaperone and its metabolites in humans.

Azaperone, dihydroazaperone, and 4'[fluoro-4-(4-(2-pyridyl)-1-piperazinyl]butyrophenone are identified in the urine of an intoxicated patient. The structures of the metabolites were confirmed by comparison of their TLC, GC, and GC/MS data with those of synthesized materials.

Azaperone↗

Effects of azaperone and acetylpromazine on social and environmental behaviour in sheep.

1 Acetylpromazine (Acp, 0.05, 0.1 and 0.5 mg/kg) and azaperone (Azp, 1.0, 1.25 and 1.5 mg/kg) were given by intramuscular injection to separate groups of seven familiar Romney ewes. Thirty minutes after injection the sheep were led into a featureless arena and spatial distribution, activity and shade preference were monitored for 20 min by overhead photography. 2 Behavioural response was complex with both stimulant and depressant effects being seen. The response trends with increasing time for all three measures were significantly different for the two drugs. In particular, Azp tended to increase animal dispersion and Acp to decrease it, in agreement with earlier predictions. 3 The dosage range for Azp was adequate for reduction of individual movement and inter-animal distance but steady state effect was not reached in the time period studied. All doses of Azp initially caused disorientation, as measured by shade preference,, but this improved as sedation deepened. 4 The highest dose of Acp (0.5 mg/kg) achieved steady state effect on individual movement within the study period. The three doses of ACp caused either no change or a slight increase in inter-animal distance. Disorientation with Acp was less and briefer than that seen with Azp.

Acepromazine↗

The effect of pen design and the tranquilising drug, azaperone, on the growth and behaviour of weaned pigs.

Two experiments were carried out in a 55-sow, specific pathogen free commercial unit, to assess the effects of the tranquilising drug, azaperone, on pigs mixed at weaning. The drug is claimed to inhibit aggression in pigs mixed at weaning, and also to increase the average weight gain in groups of growing pigs. The first experiment used a single test and control group, and the second experiment was a 2 X 2 factorial design, the variables being the presence or absence of the drug, and the presence or absence of a box used to modify the weaner pen environment. In both experiments there were no significant differences in rates of agonistic interactions between treated and untreated groups, although the drug delayed the first agonistic encounters for about 8 hours. Nor was there any difference in the relative growth rate between treated and untreated groups in either experiment.

Animals↗

Paradoxical excitement following the intravenous administration of azaperone in the horse.

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. The severity of the reaction appeared to be related to the size of the animal. Other side effects such as salivation, sweating, muscle tremor and vocalisation were also observed. The possible causes of this paradoxical reaction to the tranquilliser are discussed.

Animals↗

Combined azaperone and metomidate anaesthesia in liver transplantation in the pig.

Combined azaperone and metomidate anaesthesia has been used in 86 surgical procedures on 84 piglets, either as such or deepened and prolonged. 51 animals were sacrificed at the end of the procedure as planned before. The anesthesia allowed the performance of various short and long operations. Out of the 33 remaining pigs, submitted to 35 operations, 4 died during the procedure of a technical fault; 2 did not recover from a deep hypothermia (below 10 degrees C); 1 died from the hepatic coma induced through the operative procedure. The other 26 awoke and recovered spontaneous breathing within 1-4 h following the type of anaesthesia and operating procedure they had submitted, which dured from 15 to 330 min.

Anesthesia, General↗

Comparison of sedative and analgesic/anesthetic effects induced by medetomidine, acepromazine, azaperone, droperidol and midazolam in laboratory pigs.

The sedative and analgesic/anesthetic effects of medetomidine, acepromazine, azaperone, droperidol and midazolam were compared in laboratory pigs. In these sedatives, medetomidine produced the most profound degree of sedation with greater drowsiness than was achieved by other sedatives tested. Medetomidine induced sedation accompanied with weak analgesia and muscle relaxation smoothly and quickly and depressed arousal reaction deeply as compared with other sedatives. Pigs given medetomidine were not aroused easily even by moderately rough stimulation for approximately 60 min after injection.

Acepromazine↗

Cardiopulmonary effects of the combination of neuroleptic azaperone and hypnotic metomidate in swine.

Cardiopulmonary measurements were made at given intervals up to 120 minutes on 6 awake, unanesthetized pigs given azaperone and metomidate. Decreases from control values occurred in arterial blood pressure (deltaBPart = 30 mm of Hg), heart rate (deltaHR = 30 to 35 beats/minute), and cardiac index (deltaCI = 1.5 L/minute/m2). Blood gas and pH measurements indicated no severe impairment of pulmonary function or arterial acidosis. Although the drugs led to decreases in the various functions, cardiopulmonary function remained stable and uncompromised.

Animals↗

A preliminary investigation into the immobilising potential of a tiletamine/zolazepam mixture, metomidate, a metomidate and azaperone combination and medetomidine in ostriches (Struthio camelus).

Ostrich chicks (n = 34) were successfully immobilised with intramuscular injections of a tiletamine/zolazepam mixture at dosages of 5, 10, 15 and 20 mg kg-1; with metomidate at dosages of 15 and 20 mg kg-1 and with a metomidate/azaperone combination at respectively 20 and 6.6 mg kg-1, and 10 and 3.3 mg kg-1. Unsatisfactory immobilisation with violent body movements and self traumatisation were observed in an adult ostrich after the intramuscular administration of a tiletamine/zolezepam mixture. Anaesthesia was achieved by the administration of metomidate in combination with azaperone. Medetomidine administered at a dosage rate of 0.1 mg kg-1 did not result in immobilisation of ostrich chicks (n = 4). Findings in ostrich chicks should not necessarily be extrapolated to adult birds.

Animals↗

The suppression of electro-ejaculation in the chacma baboon (Papio ursinus) by azaperone.

Six baboons (Papio ursinus) males were immobilised on five occasions at intervals of two weeks using a combination of ketamine hydrochloride and xylazine. The animals were subsequently successfully electro-ejaculated. No semen was obtained from animals when azaperone was used instead of xylazine, despite the use of a successful standardised method of electrical stimulation.

Animals↗

Presynaptic stimulation of dopaminergic CNS structures in sheep as a mechanism of immobilising action of Immobyl (fentanyl + azaperone).

The immobilising action of Immobyl (fentanyl : azaperone, 5:1) in six sheep has been analysed on the basis of the changes in dopamine, noradrenalin, adrenalin, homovanillic acid and 5-hydroxytryptamine concentrations in the corpus striatum, frontal motor cortex, pons, cerebellum and lumbosacral spinal cord as compared to the control animals which were given saline. Forty minutes after intramuscular injection of an immobilising dose (0.19 mg [kg bodyweight]-1), Immobyl caused a significant decrease in dopamine, noradrenalin and 5-hydroxytryptamine concentrations and a similarly large decrease in homovanillic acid concentration (47 per cent) in the corpus striatum with a simultaneous but insignificant increase in the concentrations of these substances in the frontal motor cortex region. In Immobyl immobilisation, sheep showed a significant increase in dopamine concentration with an equally significant decrease in homovanillic acid concentrations in the lumbosacral part of the spinal cord. It is suggested that fentanyl stimulates the presynaptic dopamine receptors in the corpus striatum in sheep, significantly decreasing synthesis and release of dopamine and noradrenalin and intensifying an inhibitory effect of the corpus striatum on locomotor activity and thus causes the immobilisation of the animal.

Animals↗

Respiratory and circulatory parameters of African elephants (Loxodonta africana) anaesthetised with etorphine and azaperone.

Respiratory rate, heart rate, blood-gas tensions (PO2 and PCO2) and pH of arterial (a) and peripheral venous (v) blood, concentration of haemoglobin in arterial blood (Hb), saturation of arterial haemoglobin with oxygen and the end-expiratory concentration of oxygen were measured in 22 juvenile African elephants (Loxodonta africana) anaesthetised with etorphine and azaperone during a period of 35-65 minutes after they had assumed lateral recumbency. Based on these parameters the alveolar-arterial and arterial-peripheral venous differences of PO2 [P(A-a)O2 and P(a-v)O2 respectively] and oxygen content of arterial blood (CaO2) were calculated. Elephants with body mass of < or = 600 kg showed statistically significant changes in the following parameters, compared with elephants with a body mass of more than 600 kg (x +/- SD): PaO2 (64 +/- 11 versus 82 +/- 8 mmHg), P(a-v)O2 (9 +/- 5 versus 22 +/- 9 mmHg), P(A-a)O2(37 +/- 16 versus 15 +/- 8 mmHg) and Hb (148 +/- 20 versus 130 +/- 10 g/l) (p < 0.05). These findings suggested a tendency towards impaired oxygen exchange in the lungs, reduced peripheral extraction of oxygen and elevated oxygen-carrying capacity of arterial blood in smaller elephants. These changes were theoretically attributed to the respiratory-depressant and sympathomimetic effects of higher dosages of etorphine used in the smaller elephants to maintain a clinically acceptable anaesthetic plane. Individual elephants spent 35-150 minutes under anaesthesia and all recovered uneventfully after reversal of etorphine with diprenorphine.

Anesthesia, General↗