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At least 19 recordsLinked to original sources

PubMed1989

A comparison of recovery in outpatients receiving fentanyl versus those receiving butorphanol.

The frequency of postanesthesia side effects and times to reach "benchmarks" in the recovery process for IV preinduction doses of 20 micrograms/kg butorphanol, 40 micrograms/kg butorphanol, or a 2 micrograms/kg dose of fentanyl were compared in a double-blinded study involving ambulatory surgical patients. The authors hypothesized that all drugs would perform equally well in all study areas. Sixty ASA physical status I and II women undergoing laparoscopic tubal sterilization were randomly assigned to one of three groups: Group I (n = 20) received 20 micrograms/kg butorphanol as a preinduction agent; Group II (n = 20) received 40 micrograms/kg butorphanol; Group III (n = 20) received 2 micrograms/kg fentanyl. Anesthesia management for all groups was the same. Statistically significant variance was found in time to discharge-ready status and duration of nausea (p less than 0.05) between 40 micrograms/kg butorphanol and 2 micrograms/kg fentanyl, but no significant difference was found between 20 micrograms/kg butorphanol and 2 micrograms/kg fentanyl in these areas. Statistically significant variance was found in duration of dizziness and time to obtain a 10 on the Aldrete Post Anesthesia Recovery Score (APARS) between 40 micrograms/kg butorphanol and 20 micrograms/kg butorphanol and 40 micrograms/kg butorphanol and 2 micrograms/kg fentanyl. From the study, 20 micrograms/kg butorphanol appears to be as suitable as 2 micrograms/kg fentanyl for use as a preinduction narcotic analgesic, whereas 40 micrograms/kg butorphanol appears to be unsuitable due to increased duration of nausea, dizziness, and time to score 10 on APARS and reach discharge-ready status.

Adult↗

PubMed1985

Effects of butorphanol and its metabolites on the levels of monoamines and their metabolites in the rat brain.

The effects of butorphanol and its main metabolites, norbutorphanol and hydroxybutorphanol, on the contents of monoamines and their metabolites in various regions of the rat brain were compared with those of morphine and pentazocine using the HPLC-ECD method. The administrations of morphine and pentazocine increased dopamine turnover in the striatum and hypothalamus in a drug dose-dependent manner. The stimulative effects of butorphanol on the dopamine system were weaker than those of morphine and pentazocine, and there were no dose-dependencies in these effects of butorphanol. Butorphanol, morphine and pentazocine increased 5-HT turnover, but there was no drug dose-dependent effect in the case of butorphanol. These differences for the effects of butorphanol from those of morphine and pentazocine seemed to result from the antagonist-agonist property of butorphanol and from a different manner of interaction with the opioid receptor. The effects of butorphanol on the levels of the norepinephrine system were weak. It was considered that the effects of butorphanol on monoamine turnover were produced by the action of butorphanol itself, because norbutorphanol and hydroxybutorphanol showed little change on the level of monoamines and their metabolites.

3,4-Dihydroxyphenylacetic Acid↗

PubMed1977

Comparison of analgesia by intravenous butorphanol and meperidine in patients with post-operative pain.

Intravenous doses of butorphanol tartrate (0.5 mg, 1.0 mg and 2.0 mg) and meperidine hydrochloride (20 mg and 40 mg) were compared under controlled conditions employing a double blind study design. Informed consent was obtained from all post-operative patients suffering from moderate to severe pain who participated in this study. Approximately 25 patients were included in each group. The data from 125 patients were subjected to statistical analysis. The results indicated that butorphanol is approximately 40 to 50 times more potent than meperidine. In addition, at most of the time intervals, there were no statistically significant differences between the responses to butorphanol 0.5 mg and 1 mg and meperidine 20 mg and 40 mg; but the response to butorphanol 2 mg was significantly (p less than 0.05) better than the low dose of each agent. The low doses of butorphanol (0.5 mg) and meperidine (20 mg) appear to have an effective duration of action of less than two hours. The larger doses (butorphanol 1.0 mg and 2.0 mg and meperidine 40 mg) appeared to produce a two- to four-hour duration of action. The largest butorphanol dose (2.0 mg) appeared to produce the longest duration of action. A comparison of the test groups with respect to the incidence and type of side effects showed that butorphanol 2.0 mg produced a greater incidence of drowsiness (39 per cent). The overall incidence of drowsiness for patients receiving either the 0.5 mg or 1.0 mg dose of butorphanol was 12 per cent, as compared with an 8 per cent overall incidence in the meperidine group. The incidence of other side effects was relatively low in all test groups. No significant differences were noted among the groups with regard to the onset (usually less than or equal to 30 minutes post-therapy) or the duration (usually less than or equal to 2 hours) of side effects. Butorphanol appears to be a safe and effective analgesic for the relief of moderate to severe post-operative pain.

Adult↗

PubMed1991

Post-caesarean section analgesia: a comparison of epidural butorphanol and morphine.

Epidural butorphanol 1, 2 and 4 mg were compared with morphine, 5 mg, for postoperative analgesia in 92 consenting, healthy, term parturients who had undergone Caesarean section under epidural lidocaine anaesthesia in a randomized double-blind study. Postoperative pain was assessed using a visual analogue scale and recorded with heart rate, blood pressure and respiratory rate. The demographic characteristics, and the incidences of primary and repeat Caesarean sections, were not different among the four treatment groups. At 15, 30, 45 and 60 min after treatment the median pain scores following butorphanol were similar and lower than those following morphine (P less than 0.05). Calculated median percentage pain relief values for butorphanol were higher than morphine at each of these times (P less than 0.05). At 90 min and 2 hr the pain scores and pain relief values were similar. Beyond 45 min the number of patients requesting supplemental medication and dropping out of the study increased progressively in both the butorphanol and morphine treated patients. The attrition profiles for butorphanol were different from morphine (P less than 0.01). The median time in the study was greater than 24 hr for morphine, and 3, 2.5 and 4 hr for butorphanol, 1, 2 or 4 mg, respectively. No patient developed a clinically important change in heart rate or blood pressure, and none experienced a decrease in respiratory rate below 12 breaths.min-1. One of 69 patients (1.4 per cent) who received butorphanol developed pruritus compared with ten (43 per cent) of 23 patients who received morphine. The global assessments of the adequacy of analgesia were indistinguishable between morphine and butorphanol. Epidural butorphanol provides safe, effective postoperative analgesia, has a prompt onset, and a limited duration.

Adult↗

PubMed1990

Butorphanol's efficacy at mu and kappa opioid receptors: inferences based on the schedule-controlled behavior of nontolerant and morphine-tolerant rats and on the responding of rats under a drug discrimination procedure.

The purpose of the present investigation was to characterize the mu agonist and kappa antagonist effects of the mixed opioid agonist/antagonist butorphanol. To this end, the effects of butorphanol were examined: 1) alone and in combination with the kappa agonist bremazocine in nontolerant and morphine-tolerant rats responding under a fixed-ratio 30 (FR30) schedule of food presentation, and 2) in rats trained to discriminate 10 mg/kg morphine from saline. Prior to the induction of morphine tolerance, morphine, bremazocine and butorphanol produced dose-dependent decreases in rate of responding under the FR30. In these nontolerant rats, butorphanol failed to antagonize bremazocine's rate-decreasing effects. During the chronic morphine regimen, the dose-effect curve for morphine was shifted to the right of its prechronic position by approximately 0.9 log units, whereas the bremazocine curve was not altered substantially. The butorphanol dose-effect curve, in contrast, was shifted to the right and flattened such that doses which eliminated responding in nontolerant rats, as well as doses approximately 1.0 log unit higher, had no effect on responding. In these morphine-tolerant rats, butorphanol produced a dose-dependent antagonism of bremazocine's rate-decreasing effects. In rats trained to discriminate morphine from saline, butorphanol substituted completely for the morphine stimulus. Unlike morphine, which produced its stimulus effects only at doses that decreased rate of responding, butorphanol substituted for the morphine stimulus at doses that had little or no effect on rate of responding.(ABSTRACT TRUNCATED AT 250 WORDS)

Analgesics↗

PubMed1987

Epidural butorphanol or morphine for the relief of post-cesarean section pain: ventilatory responses to carbon dioxide.

To determine the safety, efficacy, and the ventilatory responses to carbon dioxide (CO2) of epidurally administered butorphanol or morphine, 122 healthy women who underwent cesarean section with epidural anesthesia were studied. Patients were randomly assigned to receive one of four epidural regimens for the relief of postoperative pain: 5 mg morphine (n = 32), 4 mg butorphanol (n = 30), 2 mg butorphanol (n = 29), or 1 mg butorphanol (n = 31). Epidural morphine provided satisfactory analgesia with slow onset and long duration of approximately 21 hr. When butorphanol was administered, analgesia of rapid onset was seen with increasing duration and effectiveness observed with increasing dose; approximately 8 hr when using 4 mg. Sixty-two percent of the patients who received morphine had pruritus. Somnolence was the main side effect encountered in patients who received epidural butorphanol. The ventilatory response to CO2 was depressed after morphine and after 2 and 4 mg butorphanol, but the duration of depression was more prolonged after morphine. It is concluded that epidural butorphanol is effective in providing pain relief after cesarean section with minor side effects. However, patients must be observed closely because of possible respiratory depression.

Butorphanol↗

PubMed1976

The pharmacology of butorphanol, a 3,14-dihydroxymorphinan narcotic antagonist analgesic.

Butorphanol, a new, totally synthetic morphinan, which is chemically related to naloxone, has been demonstrated to have both analgesic and narcotic antagonist properties. In rodent antiwrithing analgesic tests, butorphanol was 4 to 30 times more potent than morphine and dl-pentazocine, respectively. As an antagonist, butorphanol was about equivalent to nalorphine and 30 times more potent than dl-pentazocine. On the basis of the naloxone-induced mouse jumping test and the lack of substitution in withdrawn morphine-dependent mice, it is estimated that the potential for physical dependence of butorphanol will be less than that of dl-pentazocine but greater than that of nalorphine and dl-cyclazocine. Animal data also show that agonistic actions of butorphanol, such as respiratory depression and miosis, reach ceiling effects which are lower than those seen with morphine with an increase in dosage. Thus, butorphanol differed from morphine which exhibited agonist effects in a dose-related manner. Butorphanol showed weak to moderate central depressant properties at doses which were considerably higher (greater than 100 X) than those producing analgesia. Minimal cardiovascular and respiratory effects were seen with butorphanol in conscious dogs.

Analgesics↗

PubMed1978

A double-blind study on the effects of butorphanol compared with morphine in balanced anaesthesia.

In a randomized double-blind trial a total of 50 consenting patients scheduled for elective surgical operations were given multiple intravenous doses of butorphanol tartrate or morphine sulphate in combination with other agents to evaluate and compare the efficacy of these drugs in balanced anaesthesia. Equipotent doses of butorphanol tartrate (mean dose 2.0 mg) or morphine sulphate (10 mg) and thiopentone were employed as induction agents followed by the standardized use of muscle relaxants to facilitate tracheal intubation. Butorphanol tartrate or morphine sulphate were then employed during maintenance of anaesthesia in repeated intravenous doses, averaging butorphanol 4.6 mg and morphine 22.8 mg per patient. Evaluation of anaesthesia showed that induction and course were smooth in 96 per cent of the patients receiving butorphanol tartrate and in 84 per cent of patients receiving morphine sulphate. The analgesic action of butorphanol appeared in every respect to approximate that of morphine sulphate, with negligible side-effects. The data demonstrate that butorphanol is a useful analgesic for use in a balanced anaesthesia technique with a low side-effect incidence.

Adult↗

PubMed1991

The physical dependence liability of butorphanol: a comparative study with morphine.

In these studies, the physical dependence liability of butorphanol, a mixed 'agonist/antagonist' opioid analgesic, was compared to that of morphine. Male, Sprague-Dawley rats received i.c.v. infusions of saline (1 microliter/h), or an equimolar dose of butorphanol or morphine (52.3 nmol/h) for 3 days. The physical dependence liabilities of these two compounds were then compared by assessing both behavioral withdrawal signs and weight loss following naloxone-precipitated withdrawal. Body weight loss was also evaluated following abrupt (cessation of infusion) withdrawal from butorphanol or morphine. In animals receiving i.c.v. infusions of butorphanol or morphine, naloxone administration (5 mg/kg s.c.) induced an equivalent degree of body weight loss compared to saline-treated animals. In addition, the ED50 of naloxone to produce wet shakes, escape behavior, teeth chattering, urination and defecation was equivalent in rats receiving butorphanol or morphine. Infusions of butorphanol or morphine also produced an equivalent degree of weight loss in animals undergoing abrupt withdrawal. These results demonstrate then that a substantial degree of physical dependence had developed in rats which received a large dose of butorphanol.

Animals↗

PubMed1989

Comparative pharmacological and biochemical studies between butorphanol and morphine.

A number of in vivo and in vitro studies were undertaken to compare the pharmacological and biochemical effects of the partial agonist, butorphanol, with that of morphine. Both compounds were equipotent antinociceptive agents in the rat tail withdrawal test. In the acetic acid writhing test butorphanol had approximately 3.5 times the antiwrithing activity on a molar basis than morphine. In a study of the effects of these compounds on body temperature, butorphanol as well as morphine produced hyperthermia after acute dosing. Additionally, butorphanol produced a profound diuresis and decrease in urine osmolality after acute administration. In contrast, morphine produced an antidiuresis throughout most of the study period with no significant changes in urine osmolality from control. Butorphanol administration had no effect on respiratory rate, while morphine markedly decreased respiratory rate. In in vitro radioligand displacement studies, butorphanol was a potent competitor against 3H-DAGO, 3H-DPDPE, and 3H(-)-EKC binding, exhibiting 3, 10, and 30 times more activity, respectively, than morphine. Both compounds were weak inhibitors of 3H-(+)-SKF 10047 binding, yielding IC50 values of in excess of 1 microM. The results indicate that butorphanol has multiple actions on the opioid receptor system, and shares similarities as well as differences in its mechanism(s) of actions with morphine.

Analgesia↗

PubMed1991

Interaction of butorphanol, with monoamine oxidase inhibitor, tranylcypromine.

This investigation examines the possibility of interaction between tranylcypromine and butorphanol in comparison to pethidine. The LD50 of pethidine and butorphanol were determined in mice pretreated with the non-selective monoamine oxidase (MAO) inhibitor, tranylcypromine orally for 8 days or with oral saline solution. Tranylcypromine decreased the LD50 of both pethidine and butorphanol by 78% and 41%, respectively. Anesthetized rabbits with halothane pretreated with tranylcypromine or saline were given pethidine (5 mg/kg i.v.) or butorphanol (0.5, 1 and 2 mg/kg i.v.). Pethidine produced a marked increase in blood pressure in rabbits pretreated with tranylcypromine and did not affect significantly the heart rate. Butorphanol did not affect either blood pressure or heart rate at doses of 0.5 or 1 mg/kg. However, the largest dose of butorphanol (2 mg/kg) produced hypotension and tachycardia in rabbits pretreated with tranylcypromine. Neither pethidine nor butorphanol affected the temperature of anesthetized rabbits pretreated with tranylcypromine or saline.

Animals↗

PubMed1988

Cardiopulmonary effects of nalbuphine hydrochloride and butorphanol tartrate in sheep.

The cardiopulmonary, sedative and analgesic effects of butorphanol tartrate and nalbuphine hydrochloride were evaluated in six adult crossbred Dorset sheep (Ovis aries). The animals were divided randomly into two groups of three. The first group received butorphanol tartrate (0.5mg/Kg s.c.) followed in 3 days by nalbuphine hydrochloride (1 mg/Kg, s.c.). The second group received nalbuphine followed in 3 days by butorphanol. Cardiopulmonary parameters were evaluated at baseline (once the animal had accommodated to restraint); immediately following analgesic administration; and at 15, 30, 60, 90 and 120 minutes after analgesic administration. No significant changes (alpha greater than .05) from baseline were seen in any of the measured cardiopulmonary parameters from either the butorphanol or nalbuphine groups. Butorphanol produced the most dramatic analgesic and sedative effects with onset of both within 15 minutes of administration and peak effects occurring 30 minutes post injection. The degree of analgesia was diminished at 120 minutes while the sedative effect returned to near baseline by 90 minutes. The nalbuphine group also showed an onset of analgesia 15 minutes post injection reaching a peak effect after 30 minutes. However, onset of sedation occurred 30 minutes post injection achieving a peak effect at 60 minutes which was markedly less than that of butorphanol. As in the butorphanol group, analgesia was diminished at 120 minutes.

Analgesia↗

PubMed1977

Double-blind placebo controlled oral analgesic comparison of butorphanol andpentazocine in patients with moderate to severe post-operative pain.

A double-blind, randomized trial was conducted in 120 post-surgical patients to evaluate the oral analgesic activity of butorphanol tartrate (4 mg and 8 mg) and pentazocine HCl (50 mg) as compared to placebo. Both dose of butorphanol as well as pentazocine proved to be significantly (p less than 0-05) more effective than placebo. Butorphanol 4 mg and pentazocine 50 mg were never significantly different from each other, while butorphanol 8 mg was significantly beeter than both butorphanol 4 mg as well as pentazocine 50 mg in several instances, demonstrating a significant dose effect relationship for butorphanol. All of the active treatment provided maximum pain relief within 1 to 2 hours and were effective over 4 hours. In contrast to the other treatments, none of the 8 mg butorphanol patients required remedication during the 4-hour observation period. Generally, the incidence fo side-effects appeared low.

Adolescent↗

PubMed1986

Voluntary respiratory effects of butorphanol and fentanyl following barbiturate induction: a double-blind study.

Thirty-one healthy women undergoing outpatient gynecologic surgery were given either butorphanol or fentanyl following barbiturate induction, and various respiratory parameters were measured at intervals after administration of the study drugs. Both fentanyl and butorphanol caused comparable decrements in tidal volume and other respiratory parameters. However, seven of the 15 patients receiving fentanyl had significant respiratory depression that required assisted ventilation. One of the butorphanol patients experienced a 45-second self-limited respiratory depression. One of three butorphanol patients experiencing side effects required treatment for these effects, compared with seven of nine fentanyl patients who experienced adverse effects. It is concluded that butorphanol and fentanyl have comparable anesthetic effects, but butorphanol is safer in terms of respiratory and adverse effects.

Adolescent↗

PubMed1978

A double-blind comparison of butorphanol and meperidine in labour: maternal pain relief and effect on the newborn.

Butorphanol tartrate 1 mg and 2 mg were compared in 80 normal mothers at term in a double-blind study with meperidine hydrochloride 40 mg and 80 mg for the relief of pain in labour. Butorphanol was found to be as effective as meperidine in relieving pain in labour. The foetal condition, as measured by ECG monitoring, Apgar scores, time to sustained respiration, umbilical venous H+ (pH) and PCO2, and a general nursery survey were comparable for meperidine and butorphanol. No psychomimetic phenomena were seen. Assays indicated that both butorphanol and meperidine crossed the placenta. The mean concentration of butorphanol in neonatal serum was 0.84 times maternal serum at 1.5 to 3.5 hours after intramuscular administration of a single or two successive doses of butorphanol 1 mg or 2 mg to the mother. The mean concentrations for meperidine in neonatal serum was 0.89 times maternal serum at 0.85 to 3.6 hours after intramuscular administration of meperidine 40 mg or 80 mg to the mother. Neither analgesic caused severe depression of the infant except for one meperidine-treated case.

Anesthesia, Obstetrical↗

PubMed1979

Butorphanol and meperidine compared in patients with acute ureteral colic.

Pain relief was evaluated in 81 patients with acute ureteral colic and the confirmed presence of a calculus. A randomized double-blind comparison of intramuscular 2 and 4 mg. butorphanol and 80 mg. meperidine was used. Pain intensity and pain relief were evaluated at half hour and hourly intervals for 4 hours. A 2 mg. dose of butorphanol was found to be analgesically equivalent to 80 mg. meperidine, while a 4 mg. dose of butorphanol was found to be more effective than 80 mg. meperidine and 2 mg. butorphanol. Each patient received up to 2 doses of analgesic medication when necessary. There was no significant difference in the incidence of side effects among treatments. One patient had visual hallucinations after a 2 mg. dose of butorphanol, possibly owing to its antagonistic activity to significant narcotic experience given previously at another hospital. There was no other evidence of toxicity with butorphanol. It was found to be a safe, effective and wall tolerated drug for the treatment of ureteral colic and is recommended in place of narcotics.

Acute Disease↗

PubMed1988

Comparison of intramuscular analgesic activity of butorphanol and morphine in patients with sickle cell disease.

This double-blind study compared the analgesic effects of morphine with those of butorphanol in patients who presented with pain because of sickle cell crisis. Patients were placed at bed rest, administered IV hydration, and randomly assigned on each visit to receive either 2 mg IM butorphanol or 6 mg IM morphine every 30 to 60 minutes as needed to produce a pain intensity of 50 mm or less on the linear analog pain scale until the patient was discharged. Linear analog scale for pain and pain relief, level of alertness, and vital signs were assessed at 60 and 120 minutes after each study drug dose, before additional doses, and at discharge. Eighteen patients (12 men, six women; mean age, 29.3 +/- 7.7 years) were studied. Six received only morphine, six received only butorphanol, and six received each treatment at some time during the study period, resulting in 45 randomizations to treatment. The two therapies did not differ significantly (P greater than .40) with respect to pain or relief of pain scores, level of alertness, or vital signs. The discharge rate was 69.6% and 68.2% with morphine and butorphanol, respectively (P = .92). The incidence of adverse effects was 13% and 23% with morphine and butorphanol, respectively (P = .46). We conclude that morphine and butorphanol are equally effective in the treatment of sickle cell crisis pain.

Adolescent↗

PubMed1991

Transnasal butorphanol: a new method for pain relief in post-cesarean section pain.

This study was undertaken to evaluate the efficacy and the safety of transnasal butorphanol (TNB) compared to intravenous butorphanol (IVB) in 186 patients experiencing moderate to severe post-cesarean section pain. Patients were randomly assigned to five groups in a double-blind fashion: Group I (n = 37) received 2 mg IVB, Group II (n = 38) 2 mg TNB, Group III (n = 36) 1 mg TNB followed by a repeat dose of 1 mg TNB at 60 min, Group IV (n = 38) 0.5 mg TNB followed by a repeat dose of 0.5 mg at 60 min, and Group V (n = 37) received placebo. All administrations were double dummy. Pain intensity and relief were noted and the incidence of side effects was recorded. Remedication with the same study drug was allowed up to 72 h. Onset of analgesia was more rapid in the 2 mg IV group compared to the three TN groups: 5 min vs 15 min, respectively. However, the 2 mg and the 1-1 mg TN groups had a longer duration of analgesia, approximately 4.5 h, compared to 3.0 h for the 2 mg IV group (P less than 0.05). Somnolence was dose related and was the most frequent side effect, and was less frequent when the TN dose was divided into 2 doses administered 1 h apart. Multiple doses of TNB and IVB were safe and clinically acceptable up to 3 days at all doses studied. There were no incidences of nasal mucosa irritation, or cardiovascular or respiratory depression. It is concluded that transnasal butorphanol represents a safe and effective alternative to injectable butorphanol for post-cesarean section pain and offers a better and longer duration of analgesia compared to IV butorphanol. The optimum dose seems to be 2 mg TN butorphanol and it is tolerated better when divided into 1 mg increments, given 1 h apart.

Administration, Intranasal↗