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PubMed1988

Use of intramuscular butorphanol for the treatment of postoperative orthopedic pain in adolescents: a pilot study.

A pilot study was conducted to evaluate the use of butorphanol, administered intramuscularly in 0.7-mg to 3-mg doses, in 27 adolescents with postoperative orthopedic pain. Butorphanol provided good or excellent pain relief in 24 (89%) patients. The duration of the relief was about three to four hours. The only adverse effect experienced in more than one patient was urinary retention, possibly associated with the use of fentanyl, which was administered for balanced anesthesia, and/or with the surgical procedure (spinal fusion). Tolerance and safety were rated as good or excellent in 100% of the patients.

Adolescent↗
PubMed1983

[Clinical trial of butorphanol tartrate in cancer patients: evaluation for analgesic effects and safety on the basis of long term administration].

Twenty-eight cancer patients were treated with intramuscular butorphanol tartrate, a new non-narcotic analgesic, for investigating its clinical benefits in controlling cancer pain. Remarkable analgesic effects were observed approximately 30 minutes after administration by the single dose of either 1 or 2 mg of butorphanol. The effects lasted actively for 3 to 4 hours. Tolerance or drug dependency was rarely recognized even in the cases receiving repeated injections of the drug. Adverse effects, such as dizziness, nausea, thirst, numbness of the hands etc, observed in 5 patients were transient and required no medication. The above results may warrant a long-term administration of the drug for controlling varieties of pain in the cancer patients.

Aged↗
PubMed1984

Common bile duct pressure changes after fentanyl, morphine, meperidine, butorphanol, and naloxone.

Five groups of 10 patients received thiamylal, enflurane, nitrous oxide-oxygen anesthesia for elective cholecystectomy. The common bile duct was intubated via the cystic duct with a 16-g plastic catheter, and the control intraductal pressure was measured. Patients then were given equi-analgesic doses of fentanyl, morphine, meperidine, butorphanol, or placebo intravenously, and the common bile duct pressure was recorded for 20 min. Fentanyl, morphine, and meperidine significantly increased pressure in the common duct (P less than 0.001). Butorphanol produced only insignificant changes. Naloxone given 20 min later significantly (P less than 0.001) decreased pressure in patients given fentanyl, morphine, and meperidine. Naloxone given without narcotics caused an increase in pressure that, although statistically significant (P less than 0.03), was clinically insignificant. In five additional patients anesthetized with thiamylal, nitrous oxide-oxygen and intermittent doses of fentanyl, common bile duct pressures were normal.

Anesthesia↗
PubMed1980

Effects of butorphanol, fentanyl and morphine on the intrabiliary pressure of guinea pigs.

Alleged injury to the liver by halogenated hydrocarbon anesthetic agents has led to greater use of balanced anesthesia with analgesics, tranquilizers and nitrous oxide and oxygen. Reports of high intrabiliary pressures and bizarre cholangiograms for patients under such anesthesia led us to investigate the specific effects on intrabiliary pressure of morphine sulfate, fentanyl and butorphanol tartrate, each at two different dosage levels. After control measurements were taken, all of the guinea pigs, an animal with a biliary tract much like that of man, were injected with a different drug, dosage level or with 0.9 per cent saline solution, and changes in intrabiliary pressure were recorded every five minutes. Both high and low dosages of morphine and fentanyl produced marked and statistically significant increases in the intrabiliary pressure. In contrast, equianalgesic dosage of butorphanol produced little or no increase. Since two of these drugs can elevate intrabiliary pressure significantly above pretreatment values, it is recommended that dilations of the biliary tract occurring during operative cholangiograms be interpreted with caution.

Animals↗
PubMed1993

[Effects of morphine, buprenorphine and butorphanol on airway dynamics of the rabbit].

An investigation was made on the effects of morphine, buprenorphine, and butorphanol on airway dynamics with special reference to the airway smooth muscle in rabbits. After tracheostomy under anesthesia, the animals were ventilated with a Servo 900B ventilator, and airway resistance (R) and total compliance (C) were measured according to the method of Norlander, and the effect of each drug was examined. Intravenous injection of morphine 0.2 mg.kg-1 increased R significantly at 10 and 20 minutes after its administration in nontreated animals and changed R insignificantly in animals pretreated with intravenous administration of chlorpheniramine 2.5 mg, an antihistaminic. It is considered that the increase in R after the administration of morphine in the nontreated animals is due to histamine release. Buprenorphine 0.8 micrograms.kg-1 and butorphanol 0.1 mg.kg-1 brought no significant changes in R in both nontreated and the chlorpheniramine pretreated animals. C decreased in all the groups including the control group which received mechanical ventilation alone without any drug administration.

Airway Resistance↗
PubMed1994

Evaluation of butorphanol and cyproheptadine for prevention of cisplatin-induced vomiting in dogs.

Cisplatin was administered at a dosage of 50 mg/m2 of body surface to 69 dogs with various neoplasms. Dogs were randomly assigned to receive antiemetics according to 1 of the following 5 protocols: group 1, no antiemetic (control, n = 45 treatments); group 2, 0.4 mg of butorphanol/kg of body weight (n = 52 treatments); group 3, 0.2 mg of butorphanol/kg (n = 19 treatments); group 4, 2 mg of cyproheptadine/kg (n = 48 treatments); and group 5, 1 mg of cyproheptadine/kg (n = 10 treatments). Randomization was performed for each dog prior to each treatment. Butorphanol was administered IM immediately after completion of cisplatin infusion. Cyproheptadine was given orally 12 to 14 hours before and again immediately before cisplatin administration. The proportion of dogs that vomited in group 1 was 40 of 45 (89%). Butorphanol at a dosage of 0.4 mg/kg proved highly effective in preventing cisplatin-induced vomiting, reducing the proportion of dogs that vomited (10/52, 19%) compared with the control group.

Animals↗
PubMed1994

Cardiorespiratory effects of induction and maintenance of anesthesia with ketamine-midazolam combination, with and without prior administration of butorphanol or oxymorphone.

Cardiorespiratory effects of an IV administered bolus of ketamine (7.5 mg/kg of body weight) and midazolam (0.375 mg/kg) followed by IV infusion of ketamine (200 micrograms/kg/min) and midazolam (10 micrograms/kg/min) for 60 minutes was determined in 6 dogs. Ketamine-midazolam combination was administered to dogs on 3 occasions to determine effects of prior administration of IV administered saline solution (1 ml), butorphanol (0.2 mg/kg), or oxymorphone (0.1 mg/kg). The infusion rate of ketamine and midazolam was decreased by 25% for anesthetic maintenance after opioid administration. There were no significant differences in cardiorespiratory variables after saline solution or butorphanol administration; however, oxymorphone caused significant (P < 0.05) increases in mean arterial blood pressure, systemic vascular resistance, and breathing rate. Bolus administration of ketamine-midazolam combination after saline solution caused significant (P < 0.05) increases in heart rate, mean arterial blood pressure, cardiac index, mean pulmonary blood pressure, venous admixture, and significant decreases in stroke index, pulmonary capillary wedge pressure, arterial and mixed venous oxygen tension, arterial oxygen content, and alveolar-arterial oxygen gradient. Opioid administration was associated with significantly (P < 0.05) lower values than was saline administration for heart rate, mean arterial blood pressure, and arterial and mixed venous pH and with higher values for stroke index, pulmonary capillary wedge pressure, and arterial and mixed venous carbon dioxide tension. Prior oxymorphone administration resulted in the highest (P < 0.05) values for mean pulmonary blood pressure, venous admixture, and arterial and mixed venous carbon dioxide tension, and the lowest values for arterial oxygen tension, and arterial and mixed venous pH. Each treatment provided otherwise uncomplicated anesthetic induction, maintenance, and recovery.(ABSTRACT TRUNCATED AT 250 WORDS)

Anesthesia, Intravenous↗
PubMed1996

Comparison of sedative and cardiorespiratory effects of medetomidine and medetomidine-butorphanol combination in dogs.

OBJECTIVE: Sedative, cardiorespiratory, and analgesic effects of intramuscular administration of medetomidine (40 micrograms/kg of body weight)-glycopyrrolate (0.01 mg/kg) and medetomidine (10 micrograms/kg)-butorphanol (0.2 mg/kg)-glycopyrrolate (0.01 mg/kg) combinations were compared. Additional evaluations were done on reversal of medetomidine, using atipamezole (200 micrograms/kg. IV), after 90 minutes of medetomidine-induced sedation. DESIGN: Crossover study, with each dog receiving each drug combination at 1-week intervals. ANIMALS: Six 2-year-old English hound-type dogs. PROCEDURE: Arterial blood pressure, ECG, respiratory rate, tidal volume, minute volume, arterial blood gas tensions, and serum biochemical variables were measured before, during, and after sedation. Analgesia was evaluated by needle prick on the skin and tail clamp. RESULTS: Heart rate decreased significantly from 100 beats/min to < 40 beats/min within 3 minutes of injection of medetomidine and medetomidine and butorphanol (MB). Mean arterial blood pressure in both groups were maintained above 100 mm of Hg throughout the recording period. There was no significant difference between medetomidine and MB in respiratory rate, tidal volume, and minute ventilation. Hypoxemia (PaO2 < 60 mm of Hg) was observed at 10 and 20 minutes in 2 dogs given MB. Atipamezole administration in the dogs given medetomidine significantly increased PaO2, and returned the values to baseline. Needle prick analgesia duration was longer in the medetomidine (80 +/- 7.7 minutes) than MB (56.0 +/- 19.2 minutes) group. Tail pinch analgesia was variable in both groups. Duration of lateral recumbency was longer after medetomidine (90 +/- 0 minutes) than MB (73.5 +/- 19.0 minutes). CONCLUSION: Medetomidine and MB were effective combination for mildly invasive procedures. CLINICAL RELEVANCE: MB induced a shorter period of analgesia and recumbency than did medetomidine.

Analgesics, Opioid↗
PubMed1996

Hemodynamic effects of medetomidine-midazolam-butorphanol and medetomidine-midazolam-buprenorphine combinations and reversibility by atipamezole in dogs.

OBJECTIVE: To characterize the hemodynamic effects of medetomidine (1 mg/m2 of body surface area; dosage, 39 to 46 micrograms/kg of body weight, IM) and midazolam (1 mg/kg of body weight, i.v.) combined with butorphanol (0.1 mg/kg, i.v.), buprenorphine (10 micrograms/kg, i.v.) or saline solution. Reversibility of these effects by atipamezole (2.5 mg/m2; dosage, 97.5 to 115 micrograms/kg, IM) was evaluated. DESIGN: 2 treated groups and 1 control group, without repetition. ANIMALS: 15 clinically normal dogs (3 groups of 5). PROCEDURE: Medetomidine was administered at time 0; midazolam and butorphanol, buprenorphine, or saline solution at time 20; and atipamezole at time 60. Heart rate, systemic and pulmonary arterial pressures, central venous pressure, body temperature, cardiac output, and arterial and mixed venous blood gas tensions and pH were measured. Cardiac index, stroke index, systemic and pulmonary vascular resistances, and left and right stroke work indexes were calculated. RESULTS: Body temperature, heart rate, cardiac index, and stroke index were significantly decrease below baseline values in some groups. Central venous pressure, pulmonary capillary wedge pressure, and systemic vascular resistance were significantly increased above baseline in all groups. Arterial and venous PO2 and pH decreased in all groups and PCO2 increased, but these changes were more pronounced when buprenorphine was administered. Arterial pressure decreased after atipamezole administration. CONCLUSION: The combinations seemed to result in cardiorespiratory depressant effects of similar importance and most of these effects, which are related to medetomidine, were reversed by atipamezole.

Adrenergic alpha-Antagonists↗
PubMed1996

A comparison of N-butylscopolammonium bromide and butorphanol tartrate for analgesia using a balloon model of abdominal pain in ponies.

The analgesic effect of N-butylscopolammonium bromide (0.3 mg/kg) using a balloon-induced model of colic in ponies was evaluated and compared with butorphanol tartrate (0.1 mg/kg). Eight adult ponies were used and each received both treatments during the two different trials. The order in which the treatment was received was randomly assigned. At the start of each trial, moderate abdominal pain was induced by inflation of a balloon placed in the lumen of the caecum. The ponies were evaluated every 5 minutes, and a cumulative pain score (CPS) was assigned. Two baseline measurements were recorded, followed by the administration of one of the two treatments. Assessments were continued for 60 minutes, or until moderate abdominal pain returned. Three ponies out of 8 responded to treatment with butorphanol tartrate, while 6 out of 8 ponies responded to N-butylscopolammonium bromide. There were no statistical differences in the CPS or duration of drug action between treatments.

Abdominal Pain↗
PubMed1976

Intramuscular butorphanol and meperidine in postoperative pain.

Butorphanol, 1, 2, and 4 mg/70 kg, and meperidine, 40 and 80 mg/70 kg, were compared for analgesic activity and side effects in 104 hospitalized postoperative patients. Butorphanol proved to be 30 to 40 times as potent as meperidine on a weight basis. Both medications provided maximum pain relief approximately 1 hr after administration. The most common side effect in all groups was drowsiness.

Adult↗
PubMed1976

Butorphanol: a double-blind comparison with pentazocine in post-operative patients with moderate to severe pain.

A double-blind, randomized trial was conducted with 124 post-operative patients to compare the analgesic activity and possible side-effects of a new synthetic analgesic--butorphanol tartrate (1, 2, and 4 mg)--and pentazocine lactate (30 and 60 mg), adminstered intramuscularly. Butorphanol was determined to be 16 times more potent than pentazocine, on a weight basis. Both medications provided maximum pain relief within one hour after administration, and had comparable durations of action. Drowsiness was the most common side-effect, and it appeared to be dose related in all test groups.

Adult↗
PubMed1994

The effect of selective opioid antagonists on butorphanol-induced feeding.

Butorphanol tartrate (BT) potently stimulates food intake in satiated rats. The opioid receptor profile of BT is complex and is dependent upon the assay and animal species studied. In the present study we utilized three selective opioid antagonists; namely beta-funaltrexamine (beta-FNA), naltrindole (NTI) and norbinaltorphimine (nor-BNI), to probe the opioid receptor profile of BT as an orexigenic agent. Intracerebroventricular administration of nor-BNI (kappa) antagonized the feeding effects of BT (8 mg/kg, s.c.) at doses of 1, 10 and 100 nmol at the 1-2 h time point and decreased feeding at all time points for the 10 nmol dose. After 1 h, the 100 nmol dose of nor-BNI decreased BT-induced feeding by about 72%. In contrast, intraventricular injection of only the highest dose of the selective mu opioid antagonist, beta-FNA (50 nmol), decreased BT-induced feeding. Intraventricular administration of the delta opioid agonist, NTI, failed to alter BT-induced feeding at doses as high as 50 nmol. These data suggest that BT is dependent upon the kappa and perhaps the mu opioid receptors to increase food intake in satiated rats.

Animals↗
PubMed2005

Analgesic effects of intranasal butorphanol tartrate administered via a unit-dose device in the dental impaction pain model: a randomized, double-blind, placebo-controlled, parallel-group study.

BACKGROUND: Butorphanol tartrate (BT) nasal spray is currently marketed as a multidose spray pump product. However, access to excessive amounts of drug in a single bottle (up to 15 doses) creates the potential for misuse, diversion, and abuse. OBJECTIVE: This study evaluated the efficacy and tolerability of a sterile, unpreserved BT nasal spray administered via a unit-dose device in the treatment of moderate to severe pain after dental impaction surgery. METHODS: This was a single-site, single-dose, randomized, double-blind, placebo-controlled, parallel-group pilot study of unit-dose BT nasal spray 1 and 2 mg compared with vehicle in patients who received standard anesthesia and underwent surgery to remove impacted third molars. When patients reported experiencing moderate or severe postoperative pain, they were assigned to receive the respective treatments in a 2:2:1 ratio. Patients rated pain intensity and pain relief and performed other assessments of analgesic efficacy before dosing and at 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 3, 4, and 6 hours after receipt of study medication. They could request rescue medication from 1 hour after the administration of nasal spray. The primary efficacy variables were summed pain intensity difference (SPID) at 2, 4, and 6 hours after administration of study medication and total pain relief at 6 hours (TOTPAR-6). Vital signs, pulse oximetry, and adverse events were monitored on the same schedule as pain assessments. RESULTS: Thirty men and 30 women were enrolled (mean [SD] age, 22.5 [3.8] years; mean body weight, 168 [41.3] lb) and completed the trial. Pain relief was recorded in most patients within 15 minutes of receiving active treatment. A dose response was observed in SPID scores, with the 2-mg dose of BT providing the greatest response compared with placebo (P < 0.05). Overall, 52 (86.7%) patients requested rescue medication: 22 of 24 (91.7%) in the 1-mg group, 19 of 24 (79.2%) in the 2-mg group, and 11 of 12 (91.7%) in the placebo group. The time to use of rescue medication occurred a median of 75 to 110 minutes after nasal spray dosing. The analysis of TOTPAR-6 showed no significant differences overall or in pairwise comparisons. On the global assessment, 58.3% of patients in each of the active-treatment groups and 83.3% of patients in the placebo group evaluated the study drug as "poor." The unit-dose BT nasal spray was well tolerated, with central nervous system adverse effects being most common in the active-treatment groups compared with placebo (P = 0.029). Dizziness occurred in 11 (45.8%) patients who received BT 1 mg, 14 (58.3%) who received BT 2 mg, and 4 (33.3%) who received placebo; for headache, the corresponding numbers were 11 (45.8%), 7 (29.2%), and 2 (16.7%). There were no significant changes from baseline in vital signs, pulse oximetry, reported nasal irritation, or pathology (eg, irritation, epistaxis, ulceration). CONCLUSIONS: In this small pilot study, sterile BT nasal spray administered via a unit-dose device provided effective postsurgical analgesia in approximately half of patients who had undergone surgery to remove impacted third molars. The results are similar to those of previous studies of BT nasal spray administered via multidose pump for postsurgical analgesia in the dental impaction pain model. The outcomes of this study are limited to the population studied.

Administration, Intranasal↗
PubMed2005

Effect of the analgesic butorphanol on activity behaviour in turkeys (Meleagris gallopavo).

During fattening, the bodyweight of modern broad-breasted turkeys increases considerably within a very short space of time. In particular, the breast muscles increase disproportionately. This leads to a disadvantageous distribution in weight, and as a consequence, to a disturbed leg position and skeletal deformations like antitrochanteric degeneration, tibial dyschondroplasia, bending, twisting and rotation of the tibia, osteochondrosis, osteomyelitis, rickets, and epiphyseolysis of the femoral head increases. This cases of degenerative joint disease cause severe pain in humans and there are indications that this is also true for turkeys. The purpose of this study was to determine if behaviour indicative of such pain in turkeys of the B.U.T. Big 6 breeding line could be attenuated by administering a quick-acting analgesic, butorphanol. Twelve pairs of turkeys were tested at the ages of 7 and 12 weeks. One bird in each pair received an analgesic opioid injection, while the other one received a control injection of physiologically balanced saline solution. The time the birds spent putting weight on their legs, i.e., 'walking' and 'standing' and the distance covered by the birds were recorded during the 30 min periods before and after the application of the drug. At week seven the treated birds spent significantly more time putting weight on their legs than control birds. At week 12, the same tendency was observed. No significant differences were found in the distances covered by the animals. It is concluded that fattening turkeys reduce the time they are putting weight on their legs because these behaviours may be associated with pain.

Analgesics, Opioid↗
PubMed2001

Identification of central sites involved in butorphanol-induced feeding in rats.

Butorphanol (BT), a mixed kappa- and mu-opioid receptor agonist, induces vigorous food intake in rats. Peripheral injection of BT seems to increase food intake more effectively than intracerebroventricular administration. To further elucidate the nature of BT's influence on consummatory behavior, we examined which feeding-related brain areas exhibit increased c-Fos immunoreactivity (IR) following subcutaneous injection of 4 mg/kg body weight BT, a dose known to induce a maximal orexigenic response. We also evaluated whether direct administration of BT into the forebrain regions activated by peripheral BT injection affects food intake. Peripheral BT administration induced c-Fos-IR in the hypothalamic paraventricular nucleus (PVN), central nucleus of the amygdala (CeA), and nucleus of the solitary tract (NTS). However, 0.1-30 microg BT infused into the CeA, failed to increase food intake 1, 2, and 4 h after injection. Only the highest dose of BT (30 microg) injected into the PVN increased feeding. These results suggest that the PVN, CeA, and NTS mediate the effects of peripherally-injected BT. The PVN or CeA are probably not the main target sites of immediate BT action.

Amygdala↗
PubMed1997

Transnasal butorphanol in the emergency department management of migraine headache.

Transnasal butorphanol (TNB) is a mixed agonist-antagonist opioid that has recently been released for the treatment of painful conditions. Patients with a history of migraine diagnosed in either of two emergency departments (EDs) with a moderate or severe migraine were eligible for this prospective study. Patients received 1 mg of TNB at time zero and again in 45 minutes if needed. Twenty-five patients were studied. Pain intensity was measured on a 10-cm visual analog scale. Mean pain intensity was significantly decreased at 15 minutes and declined from 7.9 +/- 1 cm initially to 2.5 +/- 3.3 cm at 90 minutes. Sixty percent of the patients required no further treatment. Thirty-six percent experienced side effects, with all but 1 being mild or moderate. Seventy-five percent rated the treatment as good, very good, or excellent, and 71% would prefer to receive TNB for future migraines over other treatment options. TNB offers rapid, effective pain relief to the majority of ED migraine patients.

Administration, Intranasal↗
PubMed2004

Experimental comparison of ketamine with a combination of ketamine, butorphanol and medetomidine for general anaesthesia of the Eurasian badger (Meles meles L.).

The refinement of anaesthetic regimes is central to improving the welfare of captured wildlife. The Eurasian badger (Meles meles) has been the subject of an intensive long-term ecological and epidemiological study at Woodchester Park, Gloucestershire, England. During routine trapping operations (June 21st, 2000-January 23rd, 2001) an experimental trial was conducted on 89 badgers to compare the physiological effects of anaesthesia using ketamine hydrochloride alone, and in conjunction with medetomidine hydrochloride and butorphanol tartrate. The mixture induced a significantly longer period of anaesthesia, and either substantially reduced or eliminated the adverse effects associated with ketamine anaesthesia (e.g., excessive salivation, bouts of sneezing, rough recoveries, and muscle rigidity). In a sub-sample of badgers given the mixture, anaesthesia was reversed using atipamezole hydrochloride. Under ketamine anaesthesia, heart rates were initially significantly higher and respiration rates were consistently higher, than in badgers given the mixture. In all badgers heart rates declined and respiration rates increased during anaesthesia, but the rate of change was greatest in animals given only ketamine. Overall, the mixture provided a more balanced anaesthesia characterised by muscle relaxation and complete unconsciousness.

Anesthesia, General↗