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At least 667 records · Page 37Linked to original sources
PubMed1985

The kappa opioid receptor and food intake.

Many studies have suggested a role of opioid receptors in the modulation of food intake. Several distinct classes of opioid receptors have been postulated. In an attempt to establish which opioid receptor(s) modulate feeding we studied the effect of the kappa agonist, bremazocine, on feeding and compared its effects to the preferential mu agonist, morphine, and the mixed kappa-sigma agonist, butorphanol and the kappa agonist, ethylketocyclazocine. Bremazocine increased feeding to the same extent as morphine and was less potent than the mixed agonist/antagonists. The bremazocine effect demonstrated a bell-shaped dose response curve. Daily administration of bremazocine or morphine enhances the effect on increasing food intake. However, this effect of daily injections on enhancing food intake is not present when animals receiving morphine are crossed over to bremazocine and vice versa. The bremazocine effect is enhanced by diprenorphine and not inhibited by naloxone. Low doses of the dopamine antagonist, haloperidol, enhance the bremazocine effect and higher doses inhibit it. Finally, using another kappa agonist, tifluadom, we showed that the effect on food intake is stereospecific. Our studies provided further evidence for a role for the kappa opioid receptor in feeding. However, they also suggest that more than one subpopulation of opioid receptors is involved in feeding modulation.

Animals↗
PubMed1985

Profile of activity of kappa receptor agonists in the rabbit vas deferens.

The purpose of this study was to investigate further the kappa opioid receptor selectivity of the field-stimulated isolated rabbit vas deferens preparation and to study the profile of a series of kappa agonists in this tissue. Agonists acting at mu, delta and sigma receptors were without detectable effect in the rabbit vas deferens. But a number of kappa agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves. Mr 2034 generally produced a shallower dose-response curve and achieved a lower maximum effect, thus acting like a partial agonist. The effect of ethylketocyclazocine was not reduced by the irreversible mu antagonist, beta-funaltrexamine, confirming that it is not acting via mu receptors. Another group of drugs, including nalorphine, butorphanol and proxorphan, which produce an agonist action via kappa receptors in the guinea-pig ileum and mouse vas deferens, were antagonists in the rabbit vas deferens, suggesting that this tissue will only respond to high efficacy kappa agonists.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed1985

The pineal gland and opiate-induced feeding.

Opiate systems in the brain are thought to play a major, though not exclusive, role in the regulation of intake. The rough correspondence of feeding and pineal activity rhythms in the rat offers the possibility that the pineal may also modulate ingestive behavior. In these studies we measured the possibility that pineal manipulations would influence feeding responses to opiate agonists and the antagonist naloxone. Male rats received one of four treatments (or a corresponding control treatment): pinealectomy, removal of the superior cervical ganglia (SCG), transection of the optic nerves or chronic melatonin treatment (1 mg/kg daily). Pinealectomy and melatonin treatment reduced intake during the first half of the dark period, and removal of the SCG reduced intake during the second half of the light period. The most striking effect was seen after optic nerve transection, which reduced nocturnal and increased diurnal intake. Pinealectomy, but no other manipulation, caused a slight decrease in sensitivity to the inhibitory effects of naloxone on intake. None of the treatments affected daytime feeding responses to morphine, ketocyclazocine, or butorphanol. These results suggest that the pineal gland has a minimal role in modulating the opioid regulation of food intake.

Animals↗
PubMed1986

Seasonal variation in opioid modulation of feeding in the 13-lined ground squirrel.

Opioids are well recognized to modulate ingestive behaviors in a variety of species. To study the potential role of opioids in the alteration of ingestive behaviors that occur prior to hibernation, we have administered opiate agonists and the antagonist, naloxone, to the 13-lined ground squirrel (Spermophilus tridecemlineatus) during periods when they were hyperphagic and hypophagic. Naloxone consistently reduced feeding during both phases of the feeding cycle. Hypophagic animals, however, were 10 times more sensitive to the effects of naloxone. The effect of the opiate agonists (morphine and butorphanol, 1 and 10 mg/kg) on feeding also varied between seasons. The low dose of morphine produced a slight, but significant increase in feeding at one hour in hyperphagic animals, while the high doses tended to decrease feeding. When administered to hypophagic animals, feeding was decreased by both doses of each agonist. Immunoreactive (IR)-dynorphin levels in the cortex, hypothalamus and striatum were higher during the hypophagic phase compared with the hyperphagic phase. These data indicate that the 13-lined ground squirrel possesses an opiate sensitive feeding system which is affected by season.

Animals↗
PubMed1983

Adrenal modulation of opiate induced feeding.

Endogenous opioids have been shown to initiate feeding in sated animals. In the present study adrenalectomy enhanced the feeding response to the kappa opiate agonist, ethylketocyclazocine and the kappa/sigma opiate agonist, butorphanol tartrate. Adrenalectomy abolished the anorectic effect of naloxone at doses as high as 10 mg/kg. Corticosterone replacement did not alter the opiate induced feeding and adrenal demedullated rats continued to show enhancement to opiate induced feeding. These data suggest that in addition to the central nervous system, the adrenal medulla is involved in opiate related induction of feeding.

Adrenal Glands↗
PubMed1984

Food intake: opioid/purine interactions.

The exogenous opioids butorphanol tartrate (BT) and ethylketocyclazocine (EKC) have been reported to stimulate feeding in rats. In this study we evaluated the effects of purines (known to suppress feeding) and the adenosine antagonist, caffeine, on opioid induced feeding. Adenosine and inosine significantly suppressed BT and EKC induced feeding at various doses and time points. Caffeine enhanced food consumption was suppressed by various doses of naloxone, but was not suppressed by adenosine or inosine. Although caffeine itself induced further feeding, it did not enhance BT induced food consumption. Adenosine and inosine failed to suppress BT induced feeding when 12.5 mg/kg of caffeine was administered to the rats suggesting blockade of the adenosine receptor by caffeine. In contrast to 12.5 mg/kg caffeine, high dose caffeine (50 mg/kg) suppressed BT induced feeding over a 4 hour time period. Adenosine (50 mg/kg) and inosine (50 mg/kg) injected one hour after injection of BT and caffeine (50 mg/kg) reversed the suppressive effect of high dose caffeine in BT induced feeding. These studies indicate that opioid induced feeding can be suppressed by adenosine and inosine. Also, caffeine can reverse the suppressive effect of adenosine and inosine on feeding and vice versa. Naloxone's suppression of caffeine enhanced food consumption indicate that at least part of caffeine's effect on food intake may be mediated through an opioid mechanism.

Animals↗
PubMed1985

The effect of opiates and naloxone on food intake in virgin and lactating rats.

Lactation provides an excellent model of non-obese hyperphagia. There is accumulating evidence that endogenous opioids play a role in the modulation of the hormonal changes that occur during lactation. Because endogenous opioids appear also to play a role in the regulation of feeding, we studied the effects of the opiate agonist, butorphanol tartrate, and an opiate antagonist, naloxone, on food intake in virgin female rats and in rats during early, mid and late lactation and during post-weaning. It has been reported that female rats are less sensitive to the suppressant effects of nalmefene, an opioid antagonist, than male rats. Therefore, we also examined the effect of naloxone, an opioid antagonist, on spontaneous nocturnal feeding and 24 hour food deprivation-induced food intake in virgin female rats. We found that female rats were relatively insensitive to the food suppressant effects of naloxone following 24 hour food deprivation, while male rats tested under similar conditions had a decreased intake in response to naloxone. Despite the marked hyperphagia that occurred during lactation, there were minimal alterations in the response to opiate agonists and antagonists during this time period. Our data suggest that endogenous opioids may not play a pivotal role in the hyperphagia of lactation.

Animals↗
PubMed1994

Food deprivation history and cocaine self-administration: an animal model of binge eating.

In this two-part study, an animal model of binge eating was first produced, then the rate of acquisition of cocaine self-administration was assessed. Initially, 16 female weanling rats were food deprived (DEPR) at 25, 95, and 143 days of age. Another group of 16 age-matched controls was allowed ad lib access to food. Each time the DEPR group was food deprived, they were allowed to recover to normal weight. They were then injected with butorphanol tartrate (BUTR), an opioid that stimulates feeding, and food intake was measured for 4 h. All rats given BUTR consumed significantly more food than those given saline. Animals with DEPR history consumed food over a longer period of time, and at h 4 after BUTR injection, they consumed significantly more food than controls. In the second part of the experiment, an autoshaping procedure was used to quantitatively evaluate the rate of acquisition of cocaine self-administration. By day 30, 86% of the DEPR and 69% of the control groups had acquired cocaine self-administration.

Aging↗
PubMed1988

Objective assessment of opioid action by facial muscle surface electromyography (SEMG).

1. Activity of the mimetic muscles of the upper face were recorded from awake and anesthetized patients by surface electromyography (SEMG). 2. High amplitude SEMG accompanied ketamine anesthesia and/or the presentation of pain-provoking stimuli. 3. During periods of elevated facial muscle activity, fentanyl or butorphanol decreased SEMG amplitude. 4. The opioid-induced SEMG depression was not consistently associated with either lowered vigilance or analgesia but did provide an objective measure of drug effect.

Adult↗
PubMed1985

Review of self-administration.

The reinforcing properties of drugs can be evaluated pre-clinically using self-administration procedures in laboratory animals. This paper reviews self-administration studies of the four opioid agonist/antagonist analgesics pentazocine, butorphanol, nalbuphine and buprenorphine, and compares these results to those from studies of morphine and cyclazocine. All four agonist/antagonists possess reinforcing properties under at least some test conditions. In this respect they more resemble morphine than cyclazocine. These results suggest that they all may have some potential for recreational use. On the other hand, some data point to a lower reinforcing efficacy for these agonist/antagonists than for the pure agonists such as morphine. Studies comparing the reinforcing efficacy among the agonist/antagonists are also reviewed, however more data are needed before definitive conclusions can be drawn within the class.

Animals↗
PubMed2006

Impact of sedation method on the diagnosis of hip and elbow dysplasia in Swedish dogs.

Our objective was to investigate the effect of sedation method on the screening result for hip and elbow dysplasia. The study was based on a questionnaire survey of routines for hip and elbow screening at Swedish veterinary clinics and results of hip and elbow status, for eight breeds (Bernese Mountain Dog, Boxer, German Shepherd Dog, Golden Retriever, Labrador Retriever, Newfoundland, Rottweiler, and Saint Bernard) recorded by the Swedish Kennel Club. In total 5877 and 5406 dogs examined for hip and elbow dysplasia, respectively, from January 2002 through March 2003 were included. We used logistic regression to examine whether the type of chemical restraint used for sedation affected the screening result for hip and elbow dysplasia. In addition to sedation method, the effects of veterinary clinic, sex, breed, and age at screening were studied. The type of chemical restraint used for sedation affected the screening result for hip but not for elbow dysplasia. Acepromazine gave less than half the odds of hip dysplasia compared with medetomidine and butorphanol (the most common method), medetomidine alone or xylazine. Females had about 25% higher odds for developing hip dysplasia whereas males had almost 40% higher odds for developing elbow dysplasia. Saint Bernard, Newfoundland and German Shepherd Dog had the highest odds of developing hip dysplasia, whereas Rottweiler and Labrador Retriever had the lowest odds. Boxer had the lowest risk for elbow dysplasia, followed by Labrador Retriever. Saint Bernard and Rottweiler had the highest odds of elbow dysplasia. Increasing age increased the odds of both hip and elbow dysplasia, by about 2.5% per month. Following the results in this study, recording of the type of chemical restraint used for sedation during hip screening has now become mandatory in Sweden. This makes it possible to account for the effect of sedation method in a model for prediction of breeding values for hip dysplasia.

Acepromazine↗
PubMed1983

Determination of drugs in biological samples by thin-layer chromatography-tandem mass spectrometry.

In this work thin-layer chromatography-tandem mass spectrometry (TLC-MS-MS) allowed detection and confirmation of caffeine and nicotine in human urine and of butorphanol, betamethasone, and clenbuterol in equine urine. In most cases of trace analysis of labile compounds the drugs could not be identified unless they were developed on a TLC plate, scraped from the plate and the TLC scrape eluted with a suitable organic solvent prior to MS-MS. Usually a sample prepared in this way still had several components in it, but was sufficiently cleaned up to allow collision-induced dissociation (CID) experiments to unequivocally identify the drug. In contrast, trace levels of labile drugs could not be identified by CID experiments either directly from the raw urine extracts or by thermally desorbing them from the TLC scrape.

Animals↗
PubMed2001

Role of opioid receptors in neurogenic dural vasodilation and sensitization of trigeminal neurones in anaesthetized rats.

Migraine headache is thought to be caused by a distension of meningeal blood vessels, the activation of trigeminal sensory neurones and the the development of a central sensitization within the trigeminal nucleus caudalis (TNC). It has been proposed that clinically effective 5-HT(1B/1D) agonists act peripherally to inhibit the release of calcitonin gene-related peptide (CGRP) and neurogenic dural vasodilation, and to attenuate nociceptive neurotransmission within the TNC. Since opioids are also effective anti-migraine agents the present studies investigated the role of opioids within the trigemino-vascular system in anaesthetised rats. Electrical stimulation of the dura mater evoked neurogenic dural vasodilation which was significantly inhibited by morphine (1 mg kg(-1)) the selective mu-opioid agonist DAGO (10 microg kg(-1)) and the mixed agonist/antagonist butorphanol (1 mg kg(-1)) but not by the kappa- and delta-opioid agonists (+/-) U50488H (100 microg kg(-1)) and DPDPE (1 mg kg(-1)). Morphine had no effect on CGRP-evoked dural vasodilation. In electrophysiological studies morphine (1 - 10 mg kg(-1)) significantly attenuated brainstem neuronal activity in response to electrical stimulation of the dura by 65% at 10 mg kg(-1). Morphine (3 mg kg(-1)) also inhibited the TNC neuronal sensitization following CGRP-evoked dilation. The present studies have demonstrated that opioids block the nociceptive neurotransmission within the trigeminal nucleus caudalis and in addition inhibit neurogenic dural vasodilation via an action on mu-opioid receptors located on trigeminal sensory fibres innervating dural blood vessels. These peripheral and central actions are similar to those of the 'triptan' 5-HT(1B/1D) agonists and could account for the anti-migraine actions of opioids.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed2000

An open-label evaluation of the efficacy and safety of Stadol NS with ibuprofen in the treatment of pain after removal of impacted wisdom teeth.

PURPOSE: This study evaluated the efficacy and safety of transnasal butorphanol tartrate (Stadol NS; Bristol-Myers Squibb, New York, NY) in the treatment of patients with moderate to severe pain after oral surgery for the removal of impacted third molars. PATIENTS AND METHODS: In this open-label study, third molar extraction was performed on 25 male and 25 female patients. These patients were given Stadol NS nasal spray, 1 mg, administered in a single dose every 4 hours as needed. However, patients were allowed to remedicate 60 to 90 minutes after the initial dose, if necessary. They also took ibuprofen (400 mg) as concomitant medication every 4 to 6 hours for the first 48 hours. Patients recorded pain intensity on a visual analog scale, with 0 representing no pain, to 10 representing the most severe pain. RESULTS: Stadol NS significantly reduced pain (by 50%) after third molar extraction within 15 minutes after administration. It had a high level of patient acceptance, 81% on day 1, and was well tolerated. CONCLUSION: The rapid onset of analgesia and long duration of action shown by Stadol NS in this study, as well as its ease of administration and high level of patient acceptance, suggest that this drug would be an excellent primary choice for the management of pain after third molar extraction and oral surgery in general.

Administration, Inhalation↗
PubMed1999

Behavioural, endocrine and cardiac responses in young calves undergoing dehorning without and with use of sedation and analgesia.

Behaviour, plasma cortisol and heart rate were measured in 4-6-week-old calves during and after dehorning with and without the use of sedation and analgesia. Six groups of eight Friesian male and female calves were studied; four groups were dehorned using an electrical cauterizing dehorner, heated to approximately 600 degrees C. In group 1, a cornual nerve block was performed and the animals were sham-dehorned using a cold dehorner. Group 2 was treated similarly but dehorned with the heated dehorner. Group 3 received a mixture of xylazine and butorphanol intramuscularly, and were hot dehorned 20 min after the injection. Group 4 received the same sedatives-analgesics as group 3, and after 5 min also had a cornual nerve block, followed by hot dehorning 15 min later. Group 5 was hot dehorned without any form of sedation or analgesia. A sixth group of calves without any treatment or handling was used as controls for the behavioural observations. Head and leg movements during dehorning were significantly reduced when the cornual nerve was blocked. During the 4 h after dehorning, the behaviour of calves having a cornual block continued to differ from those in group 5. The cornual block prevented short-term increases in plasma cortisol concentrations and the long-term increases in heart rate seen in group 5. It was concluded that routine field use of local analgesia using a cornual nerve block improved the welfare of young calves subjected to dehorning with a hot iron.

Adrenergic alpha-Agonists↗
PubMed2005

High rectal temperature indicates an increased risk of unexpected recovery in anaesthetized badgers.

OBJECTIVE: To identify factors associated with sudden early recovery (SER) from anaesthesia in badgers (Meles meles). STUDY DESIGN: Experimental trial. ANIMALS: Ninety-three adult wild badgers. METHODS: Animals were randomly assigned to receive one of four anaesthetics based on medetomidine (M) ketamine (K) and butorphanol (B) combined in different ratios: (i) MKB 20:40:80 microg kg(-1); (ii) MKB 20:40:60 microg kg(-1); (iii) MKB 20:60:40 microg kg(-1); and (iv) ketamine alone 0.2 mg kg(-1). For each animal, induction time was measured and physiological variables (heart rate, respiratory rate and rectal temperature) were recorded at 5-minute intervals during anaesthesia. Cases of SER were recorded and binary logistic regression applied to identify predictive factors. RESULTS: Fourteen animals (15%) exhibited SER. Rectal temperature was the only variable that was a significant predictor of SER. Animals showing SER had significantly higher rectal temperatures which, in contrast to other cases, did not fall during the first 10 minutes of anaesthesia, which was when most SERs occurred. CONCLUSION AND CLINICAL RELEVANCE: We recommend that (i) rectal temperature is closely monitored during wild badger anaesthesia and (ii) that animals with higher than expected temperatures are treated with additional caution.

Analgesics↗
PubMed1981

An effective method of inducing analgesia and anesthesia for dermatoplastic surgery in an office.

Butorphanol tartrate (Stadol [Bristol]) and diazepam (Valium [Roche]) given intravenously in combination, in proper doses, and properly monitored are effective and safe to induce analgesia and calmness preliminary to extensive infiltration of local anesthetics that are otherwise painful and distressin. They are particularly good for moderately long and prolonged dermatoplastic procedures, and all the better because their analgesic and calmative effects last well into the postoperative period.

Analgesia↗
PubMedDate not supplied

Evaluation of three midazolam-xylazine mixtures. Preliminary trials in dogs.

The depressant effects of midazolam and xylazine on the central nervous system (CNS) were evaluated in 12 dogs. Xylazine was administered to six dogs (1.1 mg/kg intravenously [IV]) followed in 5 minutes by midazolam (1.0 mg/kg intramuscularly [IM]). In a second group of six dogs, xylazine (2.2 mg/kg IM) was followed in 5 minutes by midazolam (1.0 mg/kg IV). Both drug regimens induced rapid and profound sedation or anesthesia. Duration of action varied with the doses and routes of administration. Dogs given the high dose of xylazine IM had an arousal time of 95.4 +/- 8.9 minutes and a walking time of 155.4 +/- 8.8 minutes. These values exceeded the IV xylazine values threefold. Partial reversal of CNS depression was accomplished with either a benzodiazepine antagonist (flumazenil) or an alpha-2 antagonist (yohimbine). In a separate trial, a mixture of xylazine (0.55 mg/kg), midazolam (1.0 mg/kg), and butorphanol (0.1 mg/kg) with and without glycopyrrolate was evaluated in eight dogs. As with the xylazine-midazolam combinations, the CNS depressant effect of this mixture was clinically indistinguishable from anesthesia achieved with other rapid-acting injectable agents. Clinical signs of CNS depression were readily and completely antagonized by the simultaneous injection of flumazenil and yohimbine.

Anesthesia↗