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PubMed2005

High inspired oxygen concentrations increase intrapulmonary shunt in anaesthetized horses.

OBJECTIVES: To compare pulmonary function and gas exchange in anaesthetized horses during and after breathing either O2-rich gas mixtures or air. ANIMALS: Six healthy standard bred trotters (age range 3-12 years; mass range 423-520 kg), four geldings and two mares. Study design Randomized, cross-over experimental study. METHODS: Horses were anaesthetized on two occasions with tiletamine-zolazepam after pre-anaesthetic medication with acepromazine, romifidine and butorphanol. After endotracheal intubation and positioning in left lateral recumbency, animals were allowed to breathe spontaneously. One of two, randomly allocated inspired gas treatments was provided: either i) room air (fractional concentration of inspired O2 [FIO2] = 0.21) provided throughout anaesthesia; or ii) an O2-rich gas mixture (FIO2 = >0.95) for 15 minutes, followed by room air. The alternative treatment was delivered at the second anaesthetic. Respiratory and haemodynamic variables and the distribution of ventilation-perfusion (VA/Q) ratios (using the multiple inert gas elimination technique) were determined in the standing conscious horse (baseline) after sedation and during anaesthesia. RESULTS: Breathing O2-rich gas was associated with a decreased respiratory rate (p = 0.015) increased PaCO2 (p < 0.001) and increased PaO2 (p = 0.004) compared with breathing air. All horses developed intrapulmonary shunt during anaesthesia, but shunt was significantly greater (13 +/- 5%) when O2-rich gas was delivered compared with air breathing (5 +/- 2%; p = 0.013). Ten minutes after O2-rich gas was replaced by air, shunt remained larger in horses that had initially received oxygen compared with those breathing air (p = 0.042). Mixed venous oxygen tensions were significantly lower during sedation than at baseline (p < 0.001) and during anaesthesia (p < 0.001). CONCLUSIONS: During dissociative anaesthesia, arterial oxygenation was greater when horses breathed gas containing more than 95% oxygen, compared with when they breathed air. However, breathing O2-rich gas increased intrapulmonary shunt and caused hypoventilation. The intrapulmonary shunt created during anaesthesia by high inspired O2 concentrations remained larger when FIO2 was reduced to 0.21, indicating that absorption atelectasis produced during O2-rich gas breathing persisted throughout anaesthesia. CLINICAL RELEVANCE: In healthy horses undergoing short-term dissociative anaesthesia, air breathing ensures a level of oxygen delivery that meets tissue demand. There is no benefit to horses in breathing O2-rich gas after the gas supply is discontinued. On the contrary, the degree of shunt induced by breathing O2-rich gas persists. The clinical relevance of this during recovery requires investigation.

Anesthesia↗
PubMed2006

A comparison of cardiorespiratory variables during isoflurane-fentanyl and propofol-fentanyl anaesthesia for surgery in injured cats.

OBJECTIVE: To compare haemodynamic and respiratory variables during isoflurane-fentanyl (IF) and propofol-fentanyl (PF) anaesthesia for surgery in injured cats. STUDY DESIGN: Prospective, randomized, controlled clinical study. ANIMALS: Thirty-three client-owned injured cats undergoing orthopaedic surgery. MATERIALS AND METHODS: Pre-anaesthetic medication was intravenous midazolam 1 mg kg(-1), butorphanol 0.4 mg kg(-1) and ketamine 2 mg kg(-1). Anaesthesia was induced with propofol (P) and maintained with either: (a) a continuous rate infusion (CRI) of fentanyl (F) 0.02 mg kg(-1) hour(-1) and isoflurane (initial end-tidal concentration of 1%), (b) a fentanyl CRI (dose as before) and sevoflurane (initial end-tidal concentration of 2%) or (c) a CRI of propofol (12 mg kg(-1) hour(-1)). All three techniques were given to effect until surgical anaesthesia was achieved. Heart rate and rhythm (ECG), mean arterial blood pressure, respiratory rate, tidal volume and end-tidal CO(2) concentration were recorded. Venous blood gas analysis was performed before and after sedation, and at the end of anaesthesia. Blood chemistry and blood cell counts were assessed before, at the end of, and 24 hours after anaesthesia. The variables recorded from cats anaesthetized with IF and PF were compared. RESULTS: Mean end-expiratory isoflurane concentration was 1.19 +/- 0.19%. The propofol infusion rate was 11.4 +/- 0.8 mg kg(-1) hour(-1). No significant differences between the two groups in heart rate were identified; no cardiac dysrhythmias were recorded. Mean arterial blood pressure was significantly lower in IF cats during skin incision (p = 0.01), during surgery without intense surgical stimulation (p < 0.01) and during surgery with intense surgical stimulation (p = 0.01). Nine of 11 cats in the IF group were markedly hypotensive (34-49 mmHg) while seven of 11 cats in group PF were mildly hypotensive (49-59 mmHg). One of 11 cats in group IF and nine of 11 cats in group PF required intermittent positive pressure ventilation (IPPV) to maintain end-tidal CO(2) levels below 6.66 kPa (50 mmHg). CONCLUSION AND CLINICAL RELEVANCE: Despite the necessity to ventilate the lungs of cats in the PF group, arterial blood pressure was better maintained. Propofol-fentanyl anaesthesia is better for surgery in injured cats providing the means to impose IPPV are available.

Anesthesia, General↗
PubMed2006

Laryngeal mask airway insertion requires less propofol than endotracheal intubation in dogs.

OBJECTIVE: To compare the doses of propofol required for insertion of the laryngeal mask airway (LMA) with those for endotracheal intubation in sedated dogs. STUDY DESIGN: Randomized prospective clinical study. Animals Sixty healthy dogs aged 0.33-8.5 (3.0 +/- 2.3, mean +/- SD) years, weighing 2.2-59.0 (23.4 +/- 13.6, mean +/- SD) kg, presented for elective surgery requiring inhalation anaesthesia. METHODS: Animals were randomly assigned to receive either a LMA or an endotracheal tube. Pre-anaesthetic medication was intravenous (IV) glycopyrrolate (0.01 mg kg(-1)) medetomidine (10 microg kg(-1)) and butorphanol (0.2 mg kg(-1)). Repeated IV propofol injections (1 mg kg(-1) in 30 seconds) were given until LMA insertion or endotracheal intubation was achieved, when the presence or absence of laryngospasm, the respiratory rate (fr) and the total dose of propofol used were recorded. RESULTS: The total propofol dose (mean +/- SD) required for LMA insertion (0.53 +/- 0.51 mg kg(-1)) was significantly lower than for endotracheal intubation (1.43 +/- 0.57 mg kg(-1)). The LMA could be inserted without propofol in 47% of dogs; the remainder needed a single 1 mg kg(-1) bolus (n = 30). Endotracheal intubation was possible without propofol in 3.3% of the dogs, 47% needed one bolus and 50% required two injections (n = 30). The f(r) (mean +/- SD) was 18 +/- 6 and 15 +/- 7 minute(-1) after LMA insertion and intubation, respectively. CONCLUSION AND CLINICAL RELEVANCE: Laryngeal mask airway insertion requires less propofol than endotracheal intubation in sedated dogs therefore propofol-induced cardiorespiratory depression is likely to be less severe. The LMA is well tolerated and offers a less invasive means of securing the upper airway.

Anesthesia, General↗
PubMed2006

A clinical study of the effects of rocuronium in isoflurane-anaesthetized cats.

OBJECTIVE: To evaluate the neuromuscular blocking and chronotropic effects of rocuronium bromide in cats anaesthetized for surgery. STUDY DESIGN: Prospective clinical trial. ANIMALS: Twenty-two healthy cats of mixed breed presented for ovariectomy (n = 13) or castration (n = 9). Mean body mass (+/-SD) was 3.6 +/- 0.65 kg and mean age was 10.25 +/- 2.63 months. METHODS: Anaesthesia was induced with intravenous (IV) midazolam (0.3 mg kg(-1)), ketamine (3 mg kg(-1)) and butorphanol (0.4 mg kg(-1)). Tracheal intubation was performed and anaesthesia was maintained with isoflurane delivered in 100% oxygen. Neuromuscular function was monitored using acceleromyography applied at the ulnar nerve. This was stimulated by using the train-of-four (TOF) stimulus pattern (2 Hz) delivered every 15 seconds. The first train was made to establish baseline values for the first twitch (T1) and the TOF-ratio (T4:T1). Rocuronium (0.6 mg kg(-1) IV) was given and the following periods were recorded beginning at the end of injection: (1) lag time (LT) - to the first signs of T1 depression; (2) onset time (OT) - to the total ablation of T1; (3) duration of action (T1(25)) - to 25% recovery of the baseline value for T1; (4) T1(50)- to 50% baseline T1 restoration; (5) to TOF-ratios of 0.7 and 0.9. The time taken for T1 to recover from 75% to 25% depression (T1(25-75)) was also recorded. Heart rate (HR) was taken every minute for 15 minutes, beginning 5 minutes before rocuronium was injected. RESULTS: Rocuronium (0.6 mg kg(-1)) had a mean LT of 15.0 +/- 0 seconds, OT of 46 +/- 11 seconds and T1(25) of 13.2 +/- 2.7 minutes. The mean time for TOF 0.7 and 0.9 was 17.3 +/- 5.4 and 20.7 +/- 5.4 minutes respectively. The mean T1(25-75) was 4.8 +/- 2.4 minutes. No significant changes in HR were observed at any of the time intervals recorded. CONCLUSION: Rocuronium is an effective nondepolarizing muscle relaxant in the cat under the clinical conditions of this study. It has a rapid onset, a short duration of action and did not cause significant changes in HR.

Androstanols↗
PubMed1985

Determination of the receptor selectivity of opioid agonists in the guinea-pig ileum and mouse vas deferens by use of beta-funaltrexamine.

The irreversible inhibitor of mu-opioid receptor-mediated effects, beta-funaltrexamine (beta-FNA), was used to investigate the selectivity of various opioid agonists at mu-opioid receptors in the electrically stimulated guinea-pig ileum and mouse vas deferens preparations in vitro. In the guinea-pig ileum, pretreatment with beta-FNA (3 X 10(-8) - 3 X 10(-6)M) produced a concentration-dependent antagonism of the inhibitory effect produced by the mu-opioid receptor agonist [D-Ala2, MePhe4, Gly(ol)5]enkephalin (DAGO). High concentrations of beta-FNA (3 X 10(-6) - 1 X 10(-5)M) also antagonized the inhibitory effects of the kappa-opioid agonist U50488. Pretreatment of guinea-pig ileum with beta-FNA at 1 X 10(-6)M resulted in blockade of the effect of some opioid agonists. The compounds which showed the largest rightward shifts in their concentration-response curves, and hence the greatest mu/kappa opioid receptor selectivity, were nalbuphine, [D-Ser2, Leu5]enkephalinyl-Thr6(DSLET), morphine, DAGO and normorphine. Responses to tifluadom, Mr 2034, ethylketocyclazocine, butorphanol, nalorphine, proxorphan and U50488 were not inhibited by beta-FNA. In the mouse vas deferens, pre-treatment with beta-FNA (1 X 10(-6)M) produced a similar shift in the dose-response curves for normorphine as in the guinea-pig ileum. The concentration-response curves for the delta-receptor agonists [D-Ala2, D-Leu5] enkephalin (DADLE) and DSLET were, however, also shifted, indicating that beta-FNA will also block delta-opioid receptors. Since beta-FNA does not block kappa-opioid receptor-mediated effects, it can be used in the guinea-pig ileum preparation as a selective mu-receptor inhibitor. However, its lack of selectivity between mu- and delta-opioid receptors should be taken into account in many other isolated tissues and experiments in vivo.

Animals↗
PubMed1986

Inhibitory actions of opioid compounds on calcium fluxes and neurotransmitter release from mammalian cerebral cortical slices.

The effects of opioid agonists on veratrine-stimulated Ca2+ influx and amino acid neurotransmitter release in rat cerebrocortical brain slices were studied. Inhibitory effects were seen on both of these parameters with all of the opioid agonists used. None of the drugs used affected basal 45Ca2+ uptake, basal K+ content or basal amino acid release from the slices. At high concentrations (100 microM) fentanyl, tifluadom, U50,488H, butorphanol and bremazocine greatly inhibited the depolarization of the slices by veratrine as determined by the reduced release of K+. The opioid receptor subtypes at which the drugs were acting were characterized by the antagonistic effects of naloxone and WIN44441-3. The opioid-induced inhibition of stimulated Ca2+ uptake and amino acid release were not antagonized by WIN44441-2, the inactive enantiomer of WIN44441-3. It is concluded that opioid agonists acting through mu- and kappa-receptors and probably through delta- and sigma-receptors, have an inhibitory effect on Ca2+ uptake into cerebrocortical brain slices and the subsequent release of aspartate, glutamate and gamma-aminobutyric acid (GABA).

Amino Acids↗
PubMedDate not supplied

Analgesia after lateral thoracotomy in dogs. Epidural morphine vs. intercostal bupivacaine.

One of two analgesic treatments was randomly assigned to 40 dogs undergoing lateral thoracotomy. Group E (20 dogs) received an epidural injection of morphine (0.1 mg/kg) before surgery. Group I (20 dogs) received injections of bupivacaine around five intercostal nerves when the thorax was about to be closed. All dogs were given an opioid as part of their preoperative medication (meperidine or butorphanol), followed by thiopental for induction and halothane or methoxyflurane for maintenance of anesthesia. Scores were assigned for pre-operative demeanor and response to restraint and injection. Alertness, undisturbed pain behavior, and response to palpation of the wound were assessed 3, 6, 12, and 24 hours after surgery. Dogs that appeared uncomfortable were given analgesics. Blood for evaluation of arterial blood gases was obtained at 3 and 6 hours after surgery. The person scoring the dogs was blinded to the treatment given. There were no statistically significant differences between the groups. Group E contained more "nervous" dogs (12 vs. 6) and more dogs in group E received postoperative analgesics (8 vs. 2). Both techniques appeared to provide adequate analgesia for most dogs.

Analgesia, Epidural↗
PubMedDate not supplied

Laparoscopic cryptorchid castration in standing horses.

OBJECTIVE: This article describes a new technique for laparoscopic cryptorchid castration in standing horses. STUDY DESIGN: Prospective study. ANIMALS OR SAMPLE POPULATION: Eight horses aged 11 months to 3 years and weighing between 300 and 643 kg. METHODS: Food was withheld for 24 to 36 hours, and then horses were sedated with detomidine HCl (0.02 to 0.03 mg/kg) and butorphanol tartrate (0.02 mg/kg). The paralumbar fossa region was desensitized with 2% mepivacaine in an inverted "L" pattern and caudal epidural anesthesia was administered with either xylazine (0.18 mg/kg diluted to 10 to 15 mL with 0.9% sodium chloride) or a combination of 2% mepivacaine and xylazine (0.18 mg/kg). Initial laparoscopic exploration was performed from the left flank; in three horses, right flank laparoscopy was needed to complete the procedure. The spermatic cord was ligated within the abdomen with one or two sutures of 0 polydioxanone suture, and the testis or testes removed through a flank incision. RESULTS: In five horses with no palpably descended testes, standing laparoscopy was the only procedure performed, whereas in two horses, the abdominal testis was removed laparoscopically, and the descended testis was removed under short acting anesthesia. In one horse, with nonpalpable testes, it was determined by laparoscopic observation that the testes were in the inguinal canal, and castration was performed under general anesthesia. No surgical or postoperative complications were noted. The right side of the abdomen, and especially the right vaginal ring, could be easily observed from the left side by passing the laparoscope through a small perforation in the mesocolon of the descending colon or by elevating the descending colon with an instrument or by use of an arm in the rectum. CONCLUSIONS: The standing laparoscopic approach combined with or without short-acting anesthesia to remove the descended testis is easily performed. CLINICAL RELEVANCE: This approach will provide surgeons with another option to castrate cryptorchid stallions.

Anesthesia, General↗
PubMedDate not supplied

Perioperative management of calves undergoing implantation of a left ventricular assist device.

OBJECTIVE: To describe perioperative management of calves that underwent left lateral thoracotomy, aortic cross-clamping, partial left heart bypass and implantation of a left ventricular assist device. SAMPLE POPULATION: A total of 43 healthy castrated male calves, weighing 121 +/- 24 kg. RESULTS: Diazepam (mean +/- SD, 0.26 +/- 0.07 mg/kg), ketamine (5.9 +/- 2.17 mg/kg) and isoflurane were used in the anesthetic management of calves undergoing implantation of a left ventricular assist device in the descending thoracic aorta. Other adjunctive agents administered were fentanyl (11 +/- 5.4 microg/kg), lidocaine (4.9 +/- 3.19 mg/kg), bupivacaine (0.75%) and butorphanol (0.49 +/- 0.13 mg/kg). None of the calves regurgitated at induction or during intubation. A tube was used to drain the rumen and prevent bloat during the procedure. Partial left heart bypass was used to perfuse the caudal half of the body during the period of aortic cross clamp and device implantation. Initial mean systemic blood pressure was 96 +/- 25 mm Hg, and pressures measured in the auricular artery increased during aortic cross-clamping and bypass. Vasoconstrictor therapy was required to treat caudal arterial hypotension during the procedure in 9 calves. Mean systemic arterial pressures returned to baseline values by the end of the anesthetic period. Initial mean pulmonary arterial pressures (PAP) were 22 +/- 3 mm Hg. A significant but transient increase in pulmonary arterial pressure occurred after both heparin and protamine administration. CONCLUSIONS: The described anesthetic protocol was effective for thoracotomy and implantation of an intra-aortic left ventricular assist device in normal calves. Partial left ventricular bypass was a useful adjunct during the period of aortic cross clamp. The doses of heparin and protamine administered were effective. Responsibility to monitor oxygenation of the cranial half of the animal continues during the bypass period as hypoxemia due to pulmonary dysfunction will not be detected by the perfusionist.

Analysis of Variance↗
PubMedDate not supplied

Effects of various anesthetic agents on laryngeal motion during laryngoscopy in normal dogs.

OBJECTIVE: To evaluate the effects of various drugs and drug combinations conventionally used for anesthesia on arytenoid cartilage motion during laryngoscopy in normal dogs. STUDY DESIGN: Experimental study. ANIMALS: Six large breed healthy dogs with no previous history of respiratory dysfunction. METHODS: Each dog was randomly assigned to a different injectable anesthetic protocol once weekly for 6 weeks, then in the 7th week all dogs were anesthetized with isoflurane. Videolaryngoscopy was performed and recorded starting immediately after induction until dogs could no longer be safely restrained for endoscopy. Video was digitized and 3 still images of maximal inspiration and expiration from the first 15 seconds (induction) and the last 15 seconds (recovery) were captured and imported into an image analysis software program. The height and area of the laryngeal ostium were measured in pixels. Normalization of the glottal gap area was performed using the formula (normalized glottal gap area (NGGA)=area in pixels/height(2)). ANOVA was performed on the NGGA of images collected at inspiration and expiration during induction and recovery. Fischer's exact test was performed when significance (P<.05) was found. RESULTS: Within each protocol, laryngeal motion (defined as change in NGGA) at induction was not significantly different from laryngeal motion measured at recovery. Additionally, no significant differences were found in arytenoid motion immediately after induction when anesthetic protocols were compared. Arytenoid motion before recovery was significantly greater with thiopental when compared with propofol (P=.046), ketamine+diazepam (P=.0098), acepromazine+thiopental (P=.0021), and acepromazine+propofol (P=.0065). No significant difference in arytenoid motion was seen immediately after induction or before recovery when acepromazine+butorphanol+ isoflurane and thiopental were compared. CONCLUSION: We concluded that intravenous thiopental given to effect is the best choice for assessing laryngeal function in dogs. Dogs premedicated with acepromazine with or without opioids that require further anesthetic restraint for laryngoscopy should be anesthetized with isoflurane administered by mask. CLINICAL RELEVANCE: Misdiagnosis of laryngeal paralysis during laryngoscopy can be avoided by selecting the anesthetic regimens with the least effect on arytenoid motion.

Acepromazine↗
PubMedDate not supplied

Effects of ovariohysterectomy on canine blood neutrophil respiratory burst: a chemiluminescence study.

OBJECTIVE: To examine blood neutrophil counts and luminol-enhanced chemiluminescence (CL) responses in dogs undergoing ovariohysterectomy (OH), premedicated with 2 different drugs. STUDY DESIGN: Randomized clinical study. ANIMALS: Forty-two healthy client-owned bitches. METHODS: Dogs had OH under isoflurane anesthesia with either acepromazine or medetomidine, both in combination with butorphanol, administered as preanesthetic medication. Blood samples were collected when the dog was admitted, at the end of surgery, and the next day (approximately 20 hours after surgery). Blood neutrophils were counted automatically, and neutrophil oxidative activity was assessed by measuring blood CL responses (induced by opsonized zymosan and enhanced by luminol) at 37 degrees C for 40 minutes. RESULTS: Number of circulating neutrophils was significantly increased the day after surgery reflected by enhanced blood CL responses. Neutrophil CL, however, was not significantly altered. No significant differences were detected for perioperative Polymorphonuclear neutrophil (PMN) characteristics between the 2 preanesthetic regimens. CONCLUSIONS: In conclusion, despite clearly increasing the number of circulating neutrophils, OH did not significantly affect neutrophil respiratory burst, as measured by whole-blood CL responses. CLINICAL RELEVANCE: Surgical operation of moderate intensity (e.g., OH) did not significantly alter one of the important immune functions, neutrophil oxidative activity. Further studies are warranted to confirm the significance of this finding, and to assess the value of following this variable in different animal patient populations.

Anesthesia↗
PubMed2004

A review of drugs and techniques used for sedation and anaesthesia in captive rhinoceros species.

Captive rhinoceros species are most frequently sedated and/or anaesthetised with the potent opioid, etorphine hydrochloride in combination with an alpha-2 adrenoreceptor agonist or the butyrophenone, azaperone. Carfentanil citrate based combinations have also been used to a lesser extent. In recent years butorphanol tartrate based combinations have been used with good success to induce neuroleptanalgesia. Sedation and anaesthesia are complicated by the large size of all rhinoceros species and their sensitivity to potent opioids. Potential complications include respiratory depression, hypoxaemia, hypertension, pulmonary shunting and ventilation/perfusion mismatch. The pharmacology of the principal drugs used for sedating/anaesthetising rhinoceros is reviewed. Techniques for sedating/anaesthetising the various species and potential complications associated with chemical restraint are discussed.

Adrenergic alpha-Agonists↗
PubMedDate not supplied

Cisplatin and doxorubicin toxicosis in dogs with osteosarcoma.

Toxicosis associated with doxorubicin and cisplatin administration starting either 2 or 10 days after limb amputation for osteosarcoma was examined retrospectively in dogs. The purpose was to determine whether dosage and timing of chemotherapy affected rates of toxicosis after administration of the 1st treatment. Records of 100 dogs with appendicular osteosarcoma without evidence of metastases or concurrent disease were examined. Dogs received chemotherapy with doxorubicin and cisplatin every 3 weeks for 3 treatments starting 2 days (n = 51) or 10 days (n = 49) after amputation. The dosage of cisplatin was 60 mg/m2 and was given with 6-hour saline diuresis and butorphanol. Doxorubicin was given at 12.5-25 mg/ml during fluid administration. Hematologic data were collected before and weekly after treatment. Client interviews were conducted to assess gastrointestinal toxicosis during the interval between treatments. The reported toxicoses were graded on a scale of 0 to 4. Dogs receiving 25 mg/m2 of doxorubicin experienced greater rates of grade 4 toxicity (67%; n = 6) than dogs in groups receiving 12.5-20 mg/m2 of doxorubicin (< or = 25%; n = 94, P = .03). Dogs in the Day 2 group experienced greater rates (35%) of grade 4 toxicity than dogs in the Day 10 group (12%, P = .007). We concluded that chemotherapy administered 2 days after surgery produced an unacceptable level of toxicoses. except at greatly reduced dosages, and that even with a delay of treatment, 25 mg/m2 of doxorubicin, when given in combination with cisplatin at 60 mg/m2, was too toxic for routine use.

Amputation, Surgical↗
PubMed1988

Dose related effects of the kappa agonist U-50, 488H on behaviour, nociception and autonomic response in the horse.

Current opiate receptor theory suggests that kappa agonists should provide good analgesia without producing marked central nervous system stimulation. U-50,488H is an experimental narcotic analgesic that is a selective kappa agonist. In the present study, U-50,488H produced good analgesia in horses using both the skin twitch and hoof withdrawal reflex assays. Further, the analgesia was relatively long lasting (120 mins) compared to other mu-agonists tested in horses. The locomotor response to U-50,488H was less than observed with ethylketazocine and butorphanol, and has yielded the smallest locomotor response of any of the narcotic analgesics tested to date. Other work showed that the autonomic responses to U-50,488H were less than those of other narcotic analgesics, and that the analgesic response to this drug was blocked by naloxone. Based on its ability to produce analgesia with little other stimulatory action, U-50,488H shows promise of becoming a useful narcotic analgesic in equine medicine.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed1992

Intravenous catheterisation of foetus and mare in late pregnancy: management and respiratory, circulatory and metabolic effects.

The uterine and umbilical vessels of 12 pregnant ponies were catheterised to study foetal metabolism. The effects of this procedure on maternal and foetal cardiovascular, respiratory, metabolic and adrenocortical activity were monitored during and after surgery. Premedication with acepromazine-butorphanol-detomidine was followed by induction of anaesthesia with detomidine and ketamine and maintenance, using mechanical ventilation, with halothane in oxygen and nitrous oxide. Mean maternal arterial blood pressure was greater than 70 mmHg during anaesthesia and arterial oxygen tension remained over 100 mmHg. The foetuses were adequately oxygenated but were hypercapnic and lactic acidaemic. Most maternal and foetal blood gases and metabolites had returned to normal by 24 h, although foetal plasma lactate fell more slowly. The maternal adrenocortical discharge was less severe than reported previously and plasma cortisol had fallen to basal levels by 48 h after surgery. Foetal plasma cortisol remained low and did not change during or after surgery. Arterio-venous metabolite and gas tension differences across the uterine and umbilical circulations were slightly greater at operation than in the recovery period, suggesting that uteroplacental perfusion may have been impaired during surgery. Post-operative recovery of the mare and foetus was satisfactory and subsequent problems associated with the foetal catheters were not related to the anaesthesia or surgery.

Acid-Base Equilibrium↗
PubMed2004

Effects of opioids in morphine-treated pigeons trained to discriminate among morphine, the low-efficacy agonist nalbuphine, and saline.

In opioid-dependent subjects, the low-efficacy mu agonist nalbuphine generally precipitates withdrawal or withdrawal-like stimulus effects. To provide a more complete characterization of the discriminative stimulus effects of nalbuphine in opioid-treated subjects, seven White Carneux pigeons were treated daily with 10 mg/kg morphine i.m. and trained 6 h later to discriminate among 10 mg/kg morphine, 1.0 mg/kg nalbuphine, and saline by responding on one of three different keys. When tested, morphine produced morphine-key responding and nalbuphine produced nalbuphine-key responding. Replacing the daily morphine injection with saline produced nalbuphine-key responding, and this effect was reversed by the administration of morphine. In substitution tests with other compounds, the antagonists naltrexone (i.m.) and CTAP (D-Phe-Cys-Tyr-D-Tryp-Lys-Thr-Pen-Thr-NH2) (i.c.v.) produced nalbuphine-key responding. High-efficacy agonists fentanyl and etorphine produced morphine-key responding. The intermediate-efficacy agonists buprenorphine, dezocine, and butorphanol produced a pattern of morphine-, saline-, and/or nalbuphine-key responding that differed across individual pigeons. The lower efficacy agonists nalorphine and levallorphan produced predominantly nalbuphine-key responding. The kappa agonists spiradoline and U50,488 [trans-3,4-dichloro-N-methyl-N-(2-[1-pyrrolidinyl]cyclohexyl)benzeneacetamide methanesulfonate], the nonopioid d-amphetamine, and saline produced predominantly saline-key responding. Naltrexone and nalbuphine dose dependently reversed the morphine-key responding produced by the training dose of morphine. Together, these data suggest that the discriminative-stimulus effects of the low-efficacy micro agonist nalbuphine in morphine-treated pigeons are similar to those of other low-efficacy agonists, naltrexone, and the termination of daily morphine treatment.

Animals↗
PubMed2002

Relationship between rate and extent of G protein activation: comparison between full and partial opioid agonists.

Opioid agonists acting at their receptors alter intracellular events by initiating activation of various types of Gi/Go proteins. This can be measured by the binding of the stable GTP analog [(35)S]guanosine-5'-O-(3-thio)triphosphate ([(35)S]GTPgammaS). In this study agonist efficacy is defined by the degree to which an opioid stimulates the binding of [(35)S]GTPgammaS. This allows for a definition of full and partial agonists; a full agonist causing a greater stimulation of [(35)S]GTPgammaS binding than a partial agonist. The hypothesis that the rate of agonist-stimulated [(35)S]GTPgammaS binding is dependent upon agonist efficacy was tested using membranes from C6 glioma cells expressing mu- or delta-opioid receptors. At maximal concentrations the rate of agonist-stimulated [(35)S]GTPgammaS binding followed the efficacy of mu-agonists in stimulating [(35)S]GTPgammaS binding, i.e., [D-Ala(2),N-Me-Phe(4),Gly(5)-ol]-enkephalin > morphine > meperidine > butorphanol > nalbuphine. At submaximal concentrations of mu- or delta-full agonists the [(35)S]GTPgammaS association rate was also reduced, such that the rate of [(35)S]GTPgammaS binding correlated with the extent of [(35)S]GTPgammaS bound, whether this binding was stimulated by a full agonist or a partial agonist. Agonists also stimulated [(35)S]GTPgammaS dissociation, showing that binding of this stable nucleotide was reversible. Comparison of the delta-agonists [D-Ser(2),Leu(5)]-enkephalin-Thr and (+/-)-4-((alpha-R*)-alpha-((2S*,5R*)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxylbenzyl)-N,N-diethylbenzamide, a compound with slow dissociation kinetics, showed the measured rate of G protein activation was not influenced by the agonist switching between receptors. The results are consistent with the idea that the active state(s) of the receptor induced by full or partial agonists is the same, but the number of activated receptors determines the rate of G protein activation.

Biotransformation↗
PubMed1994

Humane destruction of horses with a mixture of quinalbarbitone and cinchocaine.

One hundred and-two horses requiring to be euthanased for a variety of reasons were killed by the intravenous injection of a mixture of quinalbarbitone sodium (400 mg/ml) and cinchocaine hydrochloride (25 mg/ml). The dose rates used were 1 ml/10, 15, 20 and 30 kg bodyweight, and the time of injection was varied between 5 and 25 seconds. The average time to collapse from the start of the injection was 34 seconds and the average time to clinical death was 230 seconds. Slow injection (particularly of the low dose rates) and premedication with detomidine resulted in a longer time to collapse (median 46 seconds). Premedication with xylazine and low dose rates of the mixture resulted in an unacceptable degree of muscular activity and agonal gasping and death was delayed. Premedication with romifidine and butorphanol resulted in an apparent (but insignificant) reduction in the time to collapse and death but was also accompanied by significant agonal gasping. Without premedication quinalbarbitone and cinchocaine resulted in a smooth and quiet collapse with the cessation of cardiac and respiratory functions within three minutes in all cases, but the palpebral reflex of the horses was prolonged significantly beyond the time when all other reflex activity was lost. Occasional gasping and muscular tremors, particularly of the upper forelimb, occurred particularly when lower dose rates and either very slow or very fast rates of injection were used. One horse which was premedicated with xylazine and received a very low dose at a slow rate showed unacceptably violent muscular activity. At no other time was the procedure regarded as violent or unacceptable.(ABSTRACT TRUNCATED AT 250 WORDS)

Animal Welfare↗