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PubMed2004

Retrospective study of the risk factors and prevalence of colic in horses after orthopaedic surgery.

The records of 496 orthopaedic operations on 428 horses were reviewed to estimate the prevalence of, and identify the risk factors for, the development of colic in horses after surgery. Colic was defined as any recognised sign of abdominal pain that could not be attributed to a concurrent disease. Fourteen of the horses developed colic; eight of them were undiagnosed, three were classified as impactions, one as tympanic colic of the colon, one as incarceration of the small intestine in the epiploic foramen, and one as left dorsal displacement of the colon in the nephrosplenic space. Morphine was associated with a four-fold increased risk of colic compared with the use of no opioid or butorphanol, and out-of-hours surgery was also associated with an increased risk.

Animals↗

PubMed2006

Echocardiographic and Doppler echocardiographic findings in 11 wolves (Canis lupus).

Two-dimensional real-time, M-mode and Doppler echocardiographic measurements were made in 11 adult wolves (Canis lupus) anaesthetised with an intramuscular combination of medetomidine, ketamine, butorphanol and acepromazine followed by isoflurane in oxygen. M-mode measurements of the left ventricle, B-mode measurements of the left atrium and aorta, systolic indices, and Doppler measurements of aortic and pulmonary blood outflow, and of mitral and tricuspid blood inflow, were recorded. The values obtained were compared with those reported for dogs of similar bodyweight and body type. The diastolic measurements of the cardiac chambers and walls were similar to those reported for healthy, conscious dogs, but the use of anaesthesia probably resulted in the markedly different systolic cardiac measurements, systolic indices and Doppler blood flow velocities observed in the wolves. Mild mitral regurgitation, probably due to mitral endocardiosis, was observed in one wolf, and trivial functional mitral insufficiency was observed in five others.

Animals↗

PubMed1984

Feeding systems in Chinese hamsters.

Modulation of feeding by opiates, putative satiety peptides, and dopamine was explored in the Chinese hamster, an animal that develops diabetes mellitus in certain inbred strains. Diabetic hamsters were hyperphagic relative to their nondiabetic controls, but both groups exhibited natural circadian variation in feeding. Starvation provoked hyperphagia of about 1-h duration in both groups. Naloxone and butorphanol had no effects on Chinese hamster feeding. Opiate receptor binding on Chinese hamster brains demonstrated no specific binding of naloxone or ethylketocyclazocine, but IR-dynorphin concentrations were comparable with that in rats. N-allylnormetazocine, a sigma-opiate receptor agonist, appeared to stimulate diabetic hamster feeding. Peptides reputed to have satiety effects in rats were without effect in Chinese hamsters: cholecystokinin, bombesin, somatostatin, and pancreatic polypeptide. Calcitonin limited feeding in both groups but may be nonspecific. Dopaminergic blockade by haloperidol also limited feeding, and diabetic hamsters were more sensitive to this. Although Chinese hamsters clearly can modulate their food intake when diabetic, we conclude that the opiatergic and peptidergic influences on feeding are very different from those in rats and may be of little importance.

Animals↗

PubMed2000

Lack of pharmacokinetic interaction between sumatriptan and naproxen.

Sumatriptan is a 5HT1D agonist used in the treatment of migraine. Nonsteroidal anti-inflammatory drugs, beta-blockers, and calcium channel-blocking antagonists are used in the prophylaxis of migraine. Hence, there is a need to investigate the interaction of these prophylactic drugs with sumatriptan. The interaction of sumatriptan with propranolol, flunarizine, pizotifen, and butorphanol were reported earlier. Naproxen is shown to be effective in prophylactic treatment of migraine. In this study, the authors have investigated the circadian rhythm effect of naproxen on the pharmacokinetics of sumatriptan at 1000 and 2200 hours. Twelve healthy volunteers were treated with 100 mg sumatriptan succinate either alone or along with 500 mg naproxen orally at either 1000 or 2200 hours in a randomized Latin square design with a washout period of 10 days. Serum samples were collected at predetermined time intervals and analyzed for unchanged sumatriptan by high-performance liquid chromatography. The pharmacokinetic parameters were calculated by using model-independent methods. Naproxen had no statistically significant (p > 0.05) effect on any pharmacokinetic parameters of sumatriptan both at 1000 and 2200 hours treatment. The results of this study suggest that no alteration in the sumatriptan dosage will be necessary for migraine patients taking naproxen prophylactic therapy.

Adult↗

PubMed2002

Activation profiles of opioid ligands in HEK cells expressing delta opioid receptors.

BACKGROUND: The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only delta opioid receptors. Activation profiles of most of these ligands at delta opioid receptors had not been previously characterized in vitro. Receptor activation was assessed by measuring the inhibition of forskolin-stimulated cAMP production. RESULTS: Naltrexone and nalorphine were classified as antagonists at delta opioid receptor. The other ligands studied were agonists at delta opioid receptors and demonstrated IC50 values of 0.1 nM to 2 microM, maximal inhibition of 39-77% and receptor binding affinities of 0.5 to 243 nM. The rank order of efficacy of the ligands tested was metazocine = xorphanol > or = fentanyl = SKF 10047 = etorphine = hydromorphone = butorphanol = lofentanil > WIN 44,441 = Nalbuphine = cyclazocine > or = met-enkephalin >> morphine = dezocine. For the first time these data describe and compare the function and relative efficacy of several ligands at delta opioid receptors. CONCLUSIONS: The data produced from this study can lead to elucidation of the complete activation profiles of several opioid ligands, leading to clarification of the mechanisms involved in physiological effects of these ligands at delta opioid receptors. Furthermore, these data can be used as a basis for novel use of existing opioid ligands based on their pharmacology at delta opioid receptors.

Animals↗

PubMed2006

Dissociative anaesthesia during field and hospital conditions for castration of colts.

The principal aim of this study was to evaluate dissociative anaesthesia for castration of colts during field conditions. Three dissociative anaesthetic protocols were evaluated during castration of colts in an animal hospital. The protocol considered to be the most suitable was thereafter evaluated during castration of colts under field conditions. Respiratory and haemodynamic parameters and the response to surgery were determined during anaesthesia. All horses breathed air spontaneously during anaesthesia. Under hospital conditions 26 colts were randomised to receive one of three anaesthetic protocols: Romifidine and tiletamine-zolazepam (RZ); acepromazine, romifidine and tiletamine-zolazepam (ARZ); or acepromazine, romifidine, butorphanol and tiletamine-zolazepam (ARBZ). The surgeon was blinded to the anaesthetic protocol used and decided whether supplemental anaesthesia was needed to complete surgery. Under field conditions 31 colts were castrated during anaesthesia with the ARBZ protocol. All inductions, anaesthesia and recoveries were calm and without excitation under both hospital and field conditions. Surgery was performed within 5-20 minutes after the horses had assumed lateral recumbency during both hospital and field castrations. Under hospital conditions some horses needed supplemental anaesthesia with all three anaesthetic protocols to complete surgery. Interestingly, none of the horses castrated with protocol ARBZ under field conditions needed additional anaesthesia. Cardiorespiratory changes were within acceptable limits in these clinically healthy colts.

Anesthesia↗

PubMed2002

Investigation on the influx transport mechanism of pentazocine at the blood-brain barrier in rats using the carotid injection technique.

The influx transport mechanism of pentazocine (PTZ) at the blood-brain barrier (BBB) was investigated in rats using the carotid injection technique. The uptake kinetics of PTZ into the rat brain exhibited saturability, which occurred by both nonsaturable and carrier-mediated transport processes. The in vivo kinetic parameters were estimated as follows: the maximal uptake rate (Jmax), 3.6 +/- 1.2 micromol/min/g brain and the apparent Michaelis constant (K1), 3.7 +/- 1.7 mM for the saturable component of PTZ into the brain, and the nonsaturable uptake rate constant (Kd), 0.06 +/- 0.04 ml/min/g brain. The uptake of PTZ by the brain was strongly inhibited by lidocaine, imipramine and propranolol, and also by H1-antagonists such as mepyramine, diphenhydramine. In addition, narcotic-antagonist analgesic (buprenorphine, butorphanol or eptazocine) and an opioid antagonist (naloxone) significantly inhibited PTZ transport. These results suggest that PTZ permeates into the brain via a carrier-mediated transport system, which may widely recognize the cationic drugs.

Animals↗

PubMed1989

Reversal of fentanyl/fluanisone neuroleptanalgesia in the rabbit using mixed agonist/antagonist opioids.

The reversal of the neuroleptanalgesic combination of fentanyl/fluanisone using mixed agonist/antagonist opioids has been investigated in the rabbit. All of the compounds studied (naloxone, nalbuphine, meptazinol, butorphanol, buprenorphine, pentazocine, doxapram) reversed the respiratory depression and sedation produced by fentanyl/fluanisone. Fentanyl/fluanisone produced profound analgesia for 180 min, which was rapidly and completely antagonized by naloxone. The mixed agonist/antagonist opioids produced a reduction in the degree of analgesia but, in contrast to naloxone, analgesic activity persisted from 120 min (meptazinol) to 420 min (buprenorphine). Administration of buprenorphine to rabbits anaesthetized with fentanyl/fluanisone and midazolam confirmed that the reversal of respiratory depression was accompanied by the return of arterial pH, PCO2 and PCO2 to preanaesthetic values. The use of neuroleptanalgesic anaesthetic regimens, which have been shown to provide effective surgical anaesthesia, combined with reversal using a mixed agonist/antagonist opioid to provide postoperative analgesia, appears to be a valuable refinement of current laboratory animal anaesthetic practice.

Analgesics↗

PubMed2004

Oral clonidine premedication exacerbates hypotension following tourniquet deflation by inhibiting noradrenaline release.

Clonidine premedication prevents tourniquet pain and reduces sympathetic nerve activity. We evaluated hemodynamic changes and catecholamine release following tourniquet deflation during spinal anesthesia in patients who received oral clonidine premedication. The final analysis included 24 otherwise healthy patients undergoing lower-limb surgery randomly assigned to two groups: those receiving approximately 5 micrograms/kg of oral clonidine 1 hr before anesthesia (clonidine group, n = 12), and those receiving no premedication (control group, n = 12). After lumbar anesthesia, a tourniquet was applied for approximately 60 minutes to each patient. Electrocardiogram, arterial blood pressure, and consumption of butorphanol for tourniquet pain were monitored. Blood samples were obtained at different times to measure serum concentration of catecholamine. In the clonidine group, mean blood pressure decreased from 87 +/- 7 mmHg at baseline to 65 +/- 10 mmHg after tourniquet deflation (P < 0.05). This peak reduction of mean blood pressure in the clonidine group was significantly lower than in the control group. After receiving clonidine premedication, the plasma noradrenaline concentrations in the clonidine group were significantly lower than those in the control group. Noradrenaline concentration increased in the control group from 162.3 +/- 89.2 pg/mL before tourniquet deflation to 199.3 +/- 95.7 pg/mL afterward (P < 0.01), but there was no significant change in noradrenaline concentration after tourniquet deflation in the clonidine group. We conclude that oral clonidine premedication exacerbated the reduction in mean blood pressure following tourniquet deflation by inhibiting noradrenaline release.

Administration, Oral↗

PubMed1997

Thoracoscopic wedge resection of blebs under local anesthesia with sedation for treatment of a spontaneous pneumothorax.

We performed thoracoscopic wedge resections of blebs with a stapling device under local anesthesia with sedation in 34 consecutive patients who presented with spontaneous pneumothoraces. The indications for surgery included the absence of parietal pleural adhesions and knowledge of the precise bleb location prior to the procedure. Prior to surgery, 0.5% lidocaine was administered into the pleural space, and IV butorphanol tartrate and diazepam were administered to reduce pain and anxiety during the procedure. In our series, the thoracoscopic procedure resulted in favorable outcomes in all but two patients. There was no evidence of hemodynamic instability or arterial blood gas abnormalities encountered during the procedure. Minor postoperative complications were seen in only three patients (two with air leakage and one with transient atelectasis). One patient had a recurrence of his spontaneous pneumothorax 3 months following the procedure. Therefore, the overall success rate was 91%. We compared the results of this therapeutic modality (group 1) with those of 38 patients who underwent the procedure under general anesthesia (group 2) during the same period. The length of hospital stay was shorter in group 1 than in group 2 (4.5 +/- 1.3 vs 5.8 +/- 1.1 days; p < 0.01). Thoracoscopic wedge resections under local anesthesia are safe and offer the benefit of shorter hospital stays. We believe that this thoracoscopic technique will further simplify the surgical treatment of pneumothoraces without incremental risks.

Adolescent↗

PubMed2002

Do butalbital-containing products have a role in the management of migraine?

STUDY OBJECTIVE: To evaluate the role of butalbital-containing products in the management of migraine. METHODS: Qualitative systematic search using MEDLINE (January 1966-November 2001), review of the United States Headache Consortium's evidence-based guidelines for migraine treatment, and review of other pertinent literature. RESULTS: Over 28 million people suffer with migraine, yet this illness is less than optimally diagnosed and managed. Between 14% and 36% of diagnosed migraineurs are prescribed butalbital-containing products, often as initial therapy. However, the only identified controlled trial of these drugs for migraine treatment showed that butalbital-containing products were inferior to butorphanol. The consortium's guidelines specifically discourage administration of butalbital-containing products for migraine. In addition, other published literature highlights the frequent adverse consequences of butalbital-containing products for migraineurs, such as poor migraine control, disability, drug-induced headaches, and withdrawal symptoms. CONCLUSION: Although butalbital-containing products commonly are prescribed for migraine, no evidence in the literature demonstrates their benefit over other agents or placebo. Drugs with proven migraine efficacy, as listed in the consortium's evidence-based guidelines, should be prescribed instead.

Analgesics↗

PubMed2004

Surgical management of rectal prolapse in an Indian rhinoceros (Rhinoceros unicornis).

An acute rectal mucosal prolapse in a 26-yr-old Indian rhinoceros (Rhinoceros unicornis) was repaired surgically by mucosal resection. Two days postoperatively, suture line dehiscence accompanied by substantial hemorrhage was managed by ligation and hemostasis during a second immobilization. Medical management with nonsteroidal anti-inflammatory drugs and diuretics reduced the mucosal edema and prevented recurrence of the prolapse. A combination of butorphanol and detomidine provided excellent reversible chemical restraint for this animal.

Animal Husbandry↗

PubMed2000

Sedative and cardiopulmonary effects of medetomidine and reversal with atipamezole in desert tortoises (Gopherus agassizii).

Ten desert tortoises (Gopherus agassizii) were given i.m. injections of 150 microg/kg of medetomidine. Sedation was achieved in all tortoises by 20 min postinjection and was accompanied by a significant decrease in mean heart and respiratory rates, systolic, diastolic, and mean ventricular pressures, and mean ventricular partial pressure of oxygen (PO2). There was no change in mean blood pH, HCO3, Na+, K+, ionized calcium values, and mean ventricular partial pressure of carbon dioxide (PCO2). There were statistically significant but clinically insignificant changes in mean base excess and pH-corrected ionized calcium values. Atipamezole given to five of the tortoises at 0.75 mg/kg i.m. significantly reversed the sedative effects of the medetomidine, with all tortoises returning to a normal state by 30 min after administration of the reversal agent. In comparison, the other five tortoises given an equal volume of physiologic saline in place of atipamezole (control group) remained significantly sedated for the duration of the study. In addition, the heart rate and ventricular PO2 returned to baseline, but the respiratory rate and ventricular blood pressures were not significantly altered by the atipamezole as compared with those of the control group. These cardiopulmonary and physiologic effects are similar to those seen in some domestic mammals. Medetomidine can be used to safely induce sedation in desert tortoises. For procedures lasting greater than 120 min, supplemental oxygen should be provided. Atipamezole will reverse the sedation but not all of the cardiopulmonary effects, thus necessitating continued monitoring after reversal. Future studies should address the anesthetic and cardiopulmonary effects of medetomidine in combination with other agents such as ketamine and/or butorphanol.

Acid-Base Equilibrium↗

PubMed2001

Diagnosis and management of a patent urachus in a white rhinoceros calf (Ceratotherium simum simum).

A 10-day-old female southern white rhinoceros calf (Ceratotherium simum simum) was diagnosed with a patent urachus after urine was observed dribbling from the umbilicus. After being separated from its mother, the animal was sedated with i.m. butorphanol and anesthetized with isoflurane in oxygen for surgical correction of the patent urachus. Mild postoperative complications involved seroma formation and partial skin incision dehiscence, which necessitated three follow-up immobilizations for reevaluation and treatment of the surgical site. Histopathology did not reveal an infectious etiology as the cause for the complications or for the patent urachus. The etiology of the patent urachus in this animal remains undetermined. This report represents the first documented case of a patent urachus in a white rhinoceros.

Animals↗

PubMedDate not supplied

The effects of doxapram hydrochloride (dopram-V) on laryngeal function in healthy dogs.

Laryngeal dysfunction is assessed most accurately by direct visualization of the larynx under a light plane of anesthesia. If the plane of anesthesia used is too deep, laryngeal structures may appear paralyzed and remain in a paramedian position. Doxapram hydrochloride is a known respiratory stimulant. We hypothesized that doxapram would significantly increase intrinsic laryngeal motion in healthy anesthetized dogs. The goal of this study was to evaluate the effect of doxapram on the area of rima glottidis (RG) in healthy dogs. Thirty healthy dogs were studied. Dogs were premedicated with butorphanol tartrate (0.22 mg/kg IV), acepromazine maleate (0.05 mg/kg SC), and glycopyrrolate (0.005 mg/kg SC), followed by induction with propofol (4 mg/kg IV). Intrinsic laryngeal motion observed in each dog was recorded on videotape after induction. Doxapram then was administered (2.2 mg/kg IV) and respirations again were recorded. Representative breaths for each dog were photographed during 4 phases of respiration (inspiration at rest, inspiration with doxapram, expiration at rest, and expiration with doxapram). The area of the RG then was calculated by using a computer-assisted analysis program. Results of each category were compared by using a 1-way analysis of variance; P < or = .05 was considered significant. Doxapram visibly increased respiratory effort, and was associated with increased intrinsic laryngeal motion. Compared to the resting state, the area of the RG was significantly increased after doxapram administration during both inspiration and expiration. We propose the routine use of doxapram during laryngoscopy to increase intrinsic laryngeal motion and aid in the diagnosis of laryngeal dysfunction.

Animals↗

PubMed1989

Dezocine. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.

Dezocine is an analgesic agent with opioid agonist and antagonist activity. After parenteral administration of therapeutic doses it is approximately equipotent with morphine, and has proved at least as effective an analgesic as morphine, pethidine (meperidine) and butorphanol in moderate to severe postoperative pain. However, preliminary pharmacodynamic data indicate that the ceiling of analgesic activity of dezocine occurs at a higher level of analgesia than that of reference agonist/antagonist agents. Also, the drug exhibited a morphine-like degree of anaesthetic-sparing activity in animals. Although long term data are very limited, single doses of dezocine are well tolerated, with mild and transient sedation and gastrointestinal upset the principal adverse effects. As with some other agonist/antagonist analgesics, a 'ceiling' effect to dezocine-induced respiratory depression occurs with increasing dosage, beyond which further depression has not been observed. In single analgesic doses, however, dezocine is a slightly more potent respiratory depressant than morphine. Clinically important haemodynamic changes have not been observed with usual analgesic doses of dezocine. As an agonist/antagonist opioid, the dependence liability of dezocine would be expected to be lower than that of pure agonist opioids, but extended clinical use is required before more definitive conclusions can be drawn in this regard. Unlike older drugs of its type, dezocine produced opiate-like subjective effects and was identified as morphine-like by drug abusers. Thus, provided the promising conclusions of currently available clinical studies are confirmed with its wider use, dezocine should be a useful additional agent for the treatment of moderate to severe postoperative pain.

Analgesics↗

PubMed2004

Intranasal medications for the treatment of migraine and cluster headache.

Intranasal medications for the treatment of headache have recently received increased attention. This paper reviews intranasal formulations of a variety of available medications (dihydroergotamine mesylate [dihydroergotamine mesilate], sumatriptan, zolmitriptan, butorphanol, capsaicin and lidocaine [lignocaine]) and one experimental medication (civamide, a cis-isomer of capsaicin) for the treatment of migraine and cluster headache. Although the efficacy of intranasal agents varies with the product used, intranasal delivery may be both convenient and more effective than other modes of drug delivery for a variety of reasons: (i) intranasal administration bypasses small bowel gastrointestinal tract absorption, which is often significantly delayed during the acute phase of a migraine attack; (ii) nauseated patients may prefer non-oral formulations as they decrease the chance of vomiting and are more rapidly effective; (iii) intranasal administration causes no pain or injection site reaction and is easier and more convenient to administer than injection or suppository and so may be used earlier in a migraine attack, resulting in better efficacy; (iv) intranasal medication produces the same number or fewer adverse events than injections; and (v) intranasal formulations offer a more rapid onset of action than oral medications, for some of the above reasons and, as such, may be more useful in patients with cluster headache, although this needs to be verified. However, it is important to emphasise that a preference study showed that most patients prefer oral tablets to an intranasal formulation. Also, some nasal preparations have significant adverse effects or are not well absorbed and therefore do not work consistently; others are more challenging to administer as a result of their delivery apparatus. Nevertheless, it is our opinion that nasal preparations increase therapeutic options and may result in faster response times and better efficacy than oral formulations and better patient satisfaction than injectable preparations.

Administration, Intranasal↗

PubMed2005

Opioids: other routes for use in recovery room.

Opioids remain the main pharmacological tools for pain control in the postoperative patient. Recent concerns about chronic use of non-steroidal anti-inflammatory drugs have put extra pressure on health care workers to device and develop new medications and delivery methods to provide patients with appropriate pain relief after surgery. New technologies and better understanding of the pharmacology of the opioids administered by non-traditional ways will be reviewed in this manuscript. Understanding the anatomy of the nose cavity is important to use the inhaled way to deliver fentanyl, sufentanyl or butorphanol in surgical patients. High concentration and small volume are keys to good absorption and effect by nasal administration. Transdermal delivery of fentanyl has been used in chronic pain for some years. A new fentanyl self-administration method is in advanced trials for clinical use. It has a huge potential in giving good pain relief with lower side effects and more patient independence because of its reduced size and lack of tubing attached to it. Day surgery patients could be great candidates for this therapeutic alternative. Finally, oral transmucosal fentanyl is also in the market. Better suited to be used in controlling breakthrough pain in chronic settings, it has been so far marketed in the perioperative period. Side effects are a concern in its use for preoperative sedation in children. Large studies are now required for drugs approval and for new indications at regulatory agencies level. Good clinical judgment is more relevant now than ever before to avoid complications and new withdraw of old good medications inappropriately prescribed from the market place.

Administration, Cutaneous↗