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At least 703 records · Page 39Linked to original sources
PubMed1999

A technique for evaluating analgesia in conscious perching birds.

OBJECTIVE: To develop a technique for objective assessment of modulation of nociperception in conscious perching birds. ANIMALS: 31 adult African grey parrots. PROCEDURE: Birds were randomly assigned to receive saline (0.9% NaCl) solution (n = 10), butorphanol tartrate (11), or buprenorphine hydrochloride (10), i.m. Birds were fitted with a surface electrode on the medial metatarsus of 1 leg. An electrical stimulus was delivered to the bird's foot through an aluminum surface on half of the perch. The alternate side of the perch delivered a noxious thermal stimulus. A withdrawal response to either stimulus was recorded when the bird lifted its foot or vigorously flinched its wings. RESULTS: Responses to thermal stimuli were extremely variable during baseline testing and after administration of drugs. Thus, significant differences were not detected after drug injection. In contrast, responses to an electrical stimulus were predictable with much less variation. CONCLUSIONS AND CLINICAL RELEVANCE: This method and device allowed for the reliable determination of withdrawal threshold in perching birds. Use of this technique for objective assessment of modulation of nociperception in conscious perching birds will enable assessment of analgesic drugs.

Analgesia↗
PubMedDate not supplied

[Effects of opioid analgesics on potential-gated ion channels in the pond snail neurons].

The effects of opioid analgesics morphine, promedol, tramadol, and butorphanol on the transmembrane calcium, sodium, and potassium (fast and slow) ion currents in pond snail (Lymnaea stagnalis) neurons were studied by intracellular dialysis and membrane potential (voltage-clamp) measurements. It was established that all these drugs produce a dose-dependent reversible inhibition of the ion currents (sodium calcium potassium) and reduce nonspecific leak currents, thus producing a stabilizing action upon the sample membrane. The current-inhibiting effect of morphine was not eliminated by naloxone (500 microM); moreover, the latter drug significantly inhibited the ion currents as well.

Analgesics, Opioid↗
PubMed2002

Effects of two preanesthetic regimens for ophthalmic surgery on intraocular pressure and cardiovascular measurements in dogs.

The effects of different preanesthetic medications (acepromazine plus either meperidine or butorphanol) given before the induction of anesthesia with midazolam and ketamine on intraocular pressure, heart rate, and arterial blood pressure were investigated in 20 dogs. Following administration of preanesthetics and induction of anesthesia, dogs were intubated and anesthesia was maintained with halothane for 10 minutes. Intraocular pressure was significantly higher (P <.05) at several evaluations for dogs premedicated with acepromazine/meperidine than for those premedicated with acepromazine/butorphanol. Mean heart rate and diastolic arterial blood pressure were significantly (P <.05) higher 5 minutes after administration of acepromazine/meperidine than after acepromazine/butorphanol. Results of this study suggest that acepromazine/butorphanol is a satisfactory preanesthetic combination to use before induction of anesthesia with midazolam and ketamine for ophthalmic surgery in dogs.

Acepromazine↗
PubMed2003

Effects of epidural opioid analgesics on heart rate, arterial blood pressure, respiratory rate, body temperature, and behavior in horses.

Heart rate, arterial blood pressures, respiratory rate, body temperature, and central nervous system excitement were compared before and after epidural administration of morphine (0.1 mg/kg), butorphanol (0.08 mg/kg), alfentanil (0.02 mg/kg), tramadol (1.0 mg/kg), the k-opioid agonist U50488H (0.08 mg/kg), or sterile water using an incomplete Latin square crossover design in five conscious adult horses. Treatments were administered into the first intercoccygeal epidural space. Significant (P <.05) reductions in respiratory rate were detected after epidural administration of morphine, alfentanil, U50488H, and sterile water. Additionally, significant (P <.05) head ptosis was observed within the first hour after administration of morphine, U50488H, and tramadol, but neither of these changes appeared to be of clinical significance. No treatment-related changes in motor activity or behavior were observed.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed1990

Prolongation of anesthesia with xylazine, ketamine, and guaifenesin in horses: 64 cases (1986-1989).

On 74 occasions, 54 horses and 6 foals were anesthetized with xylazine and ketamine or xylazine, guaifenesin, and ketamine, with or without butorphanol. On 64 occasions, anesthesia was prolonged for up to 70 minutes (34 +/- 15 min) by administration of 1 to 9 supplemental IV injections of xylazine and ketamine at approximately a third the initial dosage. All horses except 5 were positioned in lateral recumbency, and oxygen was insufflated. In adult horses, the time from induction of anesthesia to the first supplemental xylazine and ketamine injection was 13 +/- 4 minutes and the time between supplemental injections was 12.1 +/- 3.7 minutes. These results were consistent with predicted plasma ketamine concentration calculated from previously published pharmacokinetic data for ketamine in horses. Respiratory and heart rates and coccygeal artery pressure remained consistent for the duration of anesthesia. The average interval between the last injection of ketamine and assumption of sternal position was approximately 30 minutes, and was the same regardless of the number of supplemental injections. The time to standing was significantly longer (P less than 0.05) in horses given 2 supplemental injections, compared with those not given any or only given 1, but was not longer in horses given 3 supplemental injections. Recovery was considered unsatisfactory in 5 horses, but did not appear to be related to prolongation of anesthesia.

Anesthesia↗
PubMedDate not supplied

Bupivacaine/butorphanol/epinephrine for epidural anesthesia in obstetrics: maternal and neonatal effects.

The effects of epidural bupivacaine/butorphanol with and without 1:300,000 epinephrine on maternal analgesia, uterine activity, progress of labor, fetal heart rate, maternal blood pressure, newborn Apgar scores, neonatal acid base status and the neurologic and adaptive capacity scores (NACS) were compared in 33 parturients during labor and delivery. Patients in Group I (n = 17) received 0.25% bupivacaine plus 1 mg butorphanol plus 1:300,000 epinephrine, and those in Group II (n = 16) received the same agents without the epinephrine. Addition of epinephrine to bupivacaine/butorphanol did not have any adverse effects on uterine activity, duration of first or second stages of labor or fetal heart rate parameters. The incidence of maternal hypotensive episodes did not differ significantly between the two groups of patients. Apgar scores, neonatal acid base status and the NACS were equally good and did not differ significantly between the two groups. Duration of analgesia was significantly longer in Group I as compared to Group II patients (177.5 +/- 11 versus 131.8 +/- 10 minutes, p less than 0.01). It is concluded that addition of epinephrine 1:300,000 to bupivacaine/butorphanol during epidural anesthesia in the normal parturient has no adverse effects on the mother, fetus or neonate or on the progress of labor and it significantly prolongs the duration of analgesia.

Acid-Base Equilibrium↗
PubMed1989

[Influence of four opioids on pulmonary oxygenation and naloxone's effects in mechanically ventilated dogs].

In order to examine effects of opioids on pulmonary oxygenation during constant ventilation, we investigated changes in PaO2 following four different opioids and after reversal with naloxone in mechanically ventilated, lightly anesthetized dogs. The systemic administration of morphine 1.0mg.kg-1, buprenorphine 0.03mg.kg-1, butorphanol 0.1mg.kg-1, and cyclazocine 0.05mg.kg-1, did not affect PaO2, although these opioids decreased mean arterial pressure and heart rate significantly. Naloxone 0.04mg.kg-1 after four opioids affected the hemodynamics, significantly, but it did not cause any detrimental effects on pulmonary oxygenation. Although naloxone alone did not affect mean arterial pressure and heart rate at all, subsequent morphine decreased mean arterial pressure and heart rate significantly. Neither naloxone nor subsequent morphine produced any change in PaO2. The results suggest that reversal with naloxone may not cause any significant influences on pulmonary oxygenation in mechanically ventilated and anesthetized patients.

Animals↗
PubMed1987

Use of beta-funaltrexamine to determine mu opioid receptor involvement in the analgesic activity of various opioid ligands.

Systemic administration of beta-funaltrexamine (beta-FNA) 24 hr before analgesic testing produced approximately a 10-fold parallel shift in the dose-response curves of the prototypic mu agonists morphine, I-methadone, fentanyl and etorphine in the mouse abdominal constriction test. In contrast, prior administration of beta-FNA produced no appreciable shift in the analgesic dose-response curve of the selective kappa agonist, U-50, 488H. These results suggest that beta-FNA is selective for mu over kappa receptors under the conditions used in this study. The dose-response curves for ethylketazocine and proxorphan were affected only to a small extent by beta-FNA pretreatment, suggesting that these compounds have analgesic actions mediated primarily through nonmu, probably kappa receptors. The dose-response curves for cyclazocine, buprenorphine, butorphanol, nalorphine and nalbuphine were shifted markedly to the right and frequently not in a parallel fashion by the prior administration of beta-FNA. These results seem to indicate a major role for the mu receptor in the analgesic actions of these compounds.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed1987

Kappa agonist-induced diuresis: evidence for stereoselectivity, strain differences, independence of hydration variables and a result of decreased plasma vasopressin levels.

Marked diuresis has previously been reported after administration of kappa opioid agonists. The present study shows that this effect is stereospecific; MR-2034 markedly increased urinary output over the dose range 0.08 to 1.25 mg/kg, whereas the opposite isomer, MR-2035, was markedly less potent. Bremazocine increased urinary output in Long-Evans hooded and Sprague-Dawley albino rats as well as lean and fatty Zucker rats. In the lean Zucker and the albino rats, bremazocine produced an inverted U-shaped diuretic dose-effect curve, an effect characteristic of kappa agonists with mu agonist activity. This pattern was not seen with the fatty Zucker rats or the Long-Evans hooded rats. The full kappa agonists bremazocine, ethylketazocine and U-50,488 increased urinary output under three different conditions of hydration: water loaded, normal hydration and water deprived. In contrast, the partial kappa agonists reliably only increase urinary output under the normal hydration condition. The diuretic effects of full and partial kappa agonists correlated with plasma vasopressin levels in water-deprived rats. The full kappa agonists (ethylketazocine, U-50,488, tifluadom and MR-2034) suppressed plasma vasopressin levels below the threshold of detectability of the radioimmunoassay, whereas the partial kappa agonists (nalorphine and butorphanol) suppressed vasopressin levels compared with control values but did not have the efficacy of the full kappa agonists. All these results support the hypothesis that kappa agonists produce their diuretic effect by suppression of plasma vasopressin levels.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMedDate not supplied

Intrathecal morphine as analgesia for labor pain.

In this descriptive study of intrathecal morphine sulfate used for pain control during labor, 49 parturients received morphine intrathecally, 78 were administered butorphanol tartrate (Stadol), and 34 received no analgesia. Significant differences for the intrathecal group included: (1) decreased requirement of nitrous oxide for delivery, (2) lower number of doses of postpartum intramuscular pain medication, and (3) increased use of forceps. The intrathecal morphine group showed no prolongation of labor and no major side effects in mothers or newborns. The results suggest that the use of lower levels of intrathecal morphine sulfate (0.5 mg) is as safe and effective as the more traditional intravenous analgesia for labor.

Anesthesia, Intravenous↗
PubMed1984

Reinforcing and discriminative stimulus properties of mixed agonist-antagonist opioids.

Nine mixed agonist-antagonist opioids were evaluated in macaque monkeys for their ability to serve as positive reinforcers and for their discriminative stimulus similarity to etorphine and ethylketazocine. For tests of reinforcing properties, various doses of each drug were substituted for codeine under a fixed-ratio 30 time-out 600 sec schedule of i.v. delivery. Discriminative properties were assessed in separate groups of monkeys for which etorphine and saline, or ethylketazocine and saline, were established as discriminative stimuli for responses maintained under a fixed-ratio 20 schedule of food delivery. Two patterns of reinforcing and discriminative stimulus properties were observed. Buprenorphine, butorphanol, GPA 1657, nalbuphine, propiram and WY 16225 (dezocine) functioned as positive reinforcers and occasioned etorphine-appropriate but not ethylketazocine-appropriate responses. dl-Profadol also functioned as a positive reinforcer; its stereoisomers occasioned etorphine-appropriate but not, in general, ethylketazocine-appropriate responses. In contrast, levallorphan and oxilorphan did not function as positive reinforcers and occasioned ethylketazocine-appropriate but no more than 30% etorphine-appropriate responses. Under these experimental conditions, the reinforcing and discriminative stimulus profiles of the mixed agonist-antagonist opioids paralleled those of etorphine-like (mu) or ethylketazocine-like (kappa) opioid agonists.

Animals↗
PubMed1983

The kappa opioid receptor, ingestive behaviors and the obese mouse (ob/ob).

Recent studies have suggested a role for the kappa opiate receptor and its endogenous ligand, dynorphin, in the central regulation of appetite. In this study we found that the ob/ob mouse was mildly resistant to the ability of three kappa agonists, viz, butorphanol, tifluadom, and ketocyclazocine to induce food intake. In addition, we could find no change in ir-dynorphin levels in 7 areas for the central nervous system. These findings do not provide evidence for a role of kappa opioid feeding system in the pathogenesis of obesity in the ob/ob mouse.

Animals↗
PubMed1994

Migraine: a pharmacologic review with newer options and delivery modalities.

The management of migraine usually centers on two approaches: preventive and abortive therapy. Preventive therapy, designed to reduce the frequency, duration, and intensity of attacks, can be accomplished through a wide variety of medications. The most commonly used are beta-blockers, but calcium channel blockers, antidepressants, anticonvulsants, and nonsteroidal anti-inflammatory agents have all been used with success. Agents used in abortive migraine therapy treat the intensity and duration of pain, as well as the associated symptoms. New treatment options have been developed, including such newly approved medications as sumatriptan. Sumatriptan is a very effective agent that has joined the ranks of other effective abortive migraine treatments, such as ergotamine, dihydroergotamine, and nonsteroidal anti-inflammatory agents, as well as narcotic analgesics. New delivery systems, such as the nasal-spray formulation of butorphanol, allow for a route of administration previously unavailable to migraine sufferers. These new and developing treatment modalities will give physicians a wider choice of outpatient therapy options.

Administration, Intranasal↗
PubMed1993

[Epidural opioids for post-operative pain control in pediatric patients with cerebral palsy].

The safety and efficacy of epidural opioids as postoperative analgesics for children with cerebral palsy were studied in 85 pediatric patients with cerebral palsy. The patients were 5 to 15 years of age and were undergoing elective orthopedic operations on the lower extremities. These patients were divided into four groups. All the patients received inhalational anesthesia combined with caudal anesthesia, while the patients in groups 2, 3, and 4 were given epidural morphine (40 micrograms.kg-1), buprenorphine (3 micrograms.kg-1), or butorphanol (30 micrograms.kg-1) at the end of operation, respectively. Number of patients who received analgesics more than 2 times within 24 hours after operation was larger in group 1 than in groups 2-4. Although groups 2-4 compared with group 1 were still sedated at 24 hours after the operation, there was no difference in degree of sedation among the groups 2-4. The epidural opioids did not increase the frequency of side effects such as nausea, vomiting etc. The authors conclude that epidural opioids achieve safe and useful postoperative pain control in children with cerebral palsy.

Adolescent↗
PubMed1995

[The mu, delta and kappa properties of various opioids].

Recently, the highly selective mu, delta and kappa radiolabeled opioid ligands, such as 3H-DAGO (mu ligand), 3H-DPDPE (delta ligand) and 3H-U69593 (kappa ligand) are available. Using the kappa-homogeneous preparations from human placenta and mu-enriched gerbil cerebellum membrane preparations with these highly selective radiolabeled opioid ligands, clinically used opioids were tested for their mu, delta and kappa properties. The mu agonists such as morphine and fentanyl display a very low affinity for delta and kappa receptor. Among the agonist-antagonist, buprenorphine and butorphanol appeared to be the most highly selective agonists for mu and kappa opioid receptors, respectively. Most ligands identified as specific agonists are in fact only selective and appear to interact at more than one receptor type.

Analgesics, Opioid↗
PubMedDate not supplied

[Combined general anesthesia using moradol in children].

The purpose of this study was to assess the efficacy of moradol (butorphanol tartrate) as an analgetic component of combined total anesthesia in children. The adequacy of anesthesia was assessed by echography, electrocardiography, and electroencephalography, measurements of stress hormones, electrolyte balance, and metabolic parameters at various stages of anesthesia and surgery. A total of 103 patients aged 1 to 4 years were examined, subjected to abdominal, thoracal, urological, orthopaedic, and ENT surgery. The stability of the basic hemodynamic parameters and some stress hormones in the blood during surgery indicated effective protection of the organism from surgical trauma, on the one hand, and evidenced the minimal effect of anesthesia on the adrenal and thyroid function, on the other. A single injection of moradol during induction narcosis was sufficient for 2.5 to 3 hours of surgery. No serious side effects of the drug were observed. Prolonged (10 hours on average) anesthesia persisted after the operation, this decreasing the postoperative use of analgesics.

Adolescent↗
PubMed1998

Comparison of five regimens for oral administration of medication to induce sedation in dogs prior to euthanasia.

OBJECTIVE: To compare regimens for oral administration of medication to induce sedation in dogs prior to euthanasia. DESIGN: Prospective randomized clinical study. ANIMALS: 37 dogs. PROCEDURE: Groups and medications were as follows: group 1, acepromazine (n = 8); group 2, tiletamine-zolazepam (8); group 3, tiletamine-zolazepam and acepromazine (8); group 4, tiletamine-zolazepam and butorphanol (6); and group 5, pentobarbital sodium (7). Capsules or tablets were placed in each dog's food. Sedation was scored at 3-minute intervals after consumption of medication for at least 60 minutes. Dogs with signs of persistent or progressive sedation were observed for 90 minutes. RESULTS: Only 2 dogs in group 1 became slightly ataxic. All group-2 dogs were slightly ataxic, and 4 of 8 became laterally recumbent (mean time to lateral recumbency, 62 minutes). Seven of 8 group-3 dogs became sternally recumbent, and 6 of these dogs became laterally recumbent (mean, 48.6 minutes). Four of 6 group-4 dogs were slightly or moderately ataxic, and 1 of these dogs became laterally recumbent (mean, 48 minutes). One dog in group 5 was not affected by the medication, but all other group-5 dogs became laterally recumbent (mean, 59 minutes). CLINICAL IMPLICATIONS: Of the medications evaluated, tiletamine-zolazepam and acepromazine at dosages of approximately 20 mg/kg (9.1 mg/lb) and 2 mg/kg (0.91 mg/lb), respectively, or pentobarbital sodium alone (63.2 +/- 5.1 mg/kg [28.7 +/- 2.3 mg/lb]) most consistently induced profound sedation and lateral recumbency after oral administration to dogs.

Acepromazine↗