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PubMed1978

Pharmacological effects of a combination of butorphanol and acetaminophen.

Isobolographic analysis was used to study in mice the combined oral analgetic action of butorphanol, a new centrally acting analgetic, and acetaminophen, an antipyretic analgetic. Combinations of butorphanol-acetaminophen exhibited analgetic effects which were greater than were expected from just an additive analgetic action of each drug. Consequently, a significant synergistic effect occurred after the simultaneous oral administration of butorphanol and acetaminophen. Furthermore, oral administration of butorphanol-acetaminophen mixture to conscious dogs at approximately 20 times the recommended human dose resulted in little or no effect on aortic blood pressure and arterial blood pH,pCO2 and pO2. Heart rate was slightly reduced and this resulted in a small increase in the PR interval and a prolongation of the QT interval of the lead II surface electrocardiogram.

Acetaminophen↗

PubMed1993

Double-blind comparison of butorphanol and nalbuphine on the common bile duct by ultrasonography in man.

Butorphanol and nalbuphine, narcotic agonist-antagonists were shown to cause no increase in biliary pressure in contrast to morphine in dogs or men. A non-invasive, ultrasonographic technique confirmed that morphine caused constriction of the common bile duct while placebo caused no effect. To prove the lack of constrictive effect of butorphanol and nalbuphine on the common bile duct, the changes in its diameter were measured following placebo or the two agonist-antagonists by ultrasonography. In a double-blind, randomized study, 17 patients undergoing open cholecystectomy were evaluated. No morphine or opioids were allowed for 12 hours prior to the study. After premedication with midazolam and glycopyrrolate, anesthesia was induced by midazolam, 50 micrograms.kg-1 and thiopental, 3.0-5.0 mg.kg-1. Tracheal intubation was facilitated by succinylcholine 1.0 mg.kg-1 and muscle relaxation was maintained with vecuronium. Anesthesia was maintained with isoflurane or enflurane and nitrous oxide in oxygen. After imaging the common bile duct by ultrasonography, placebo, nalbuphine 0.3 mg.kg-1 or butorphanol 40 micrograms.kg-1 were injected intravenously. The diameter of the common bile duct was measured before and at 4 and 8 minutes after drug administration. One-way analysis of variance and paired t-test were utilized for statistical analysis. P < 0.05 was considered significant. No significant changes in the common bile duct diameter was observed after placebo administration, nor was any change observed after either nalbuphine or butorphanol as compared to the baseline. The comparison of three groups of patients showed no statistically significant difference.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

PubMedDate not supplied

Efficacy of transnasal butorphanol tartrate in postepisiotomy pain: a model to assess analgesia.

Butorphanol tartrate, a synthetically derived opioid agonist-antagonist analgesic, was tested in a large group of postpartum women (N = 76) to assess the safety and analgesic efficacy of a recently approved transnasal preparation of this drug in the relief of postepisiotomy pain. The safety and efficacy of intravenous and intramuscular administration of butorphanol tartrate has been established over 14 years of clinical use. The new nasal spray dosage form offers a similar degree of efficacy with a rapid onset of action. Compared with the injectables and other drugs in this class, transnasal butorphanol has a longer duration of action (4 to 5 hours). In this double-blind, parallel-group, dose-response study, 76 female patients ages 17 to 37 years with moderate to severe postepisiotomy pain were randomly assigned to receive a single dose of transnasal butorphanol (0.25, 0.5, 1, or 2 mg) or placebo. The patients were evaluated for 6 hours. The results of the study indicate that the 1-mg and 2-mg doses were associated with greater efficacy compared with placebo using several markers for efficacy, including the pain relief score and time to remedication. The drug was well tolerated, dizziness and drowsiness being the most frequently reported adverse effects. Adverse effects appeared to be dose related.

Administration, Intranasal↗

PubMedDate not supplied

Intranasal butorphanol-induced apraxia reversed by naloxone.

Intranasal butorphanol is an opioid agonist-antagonist that is effective for the treatment of acute pain. Common adverse effects associated with the agent are somnolence, dizziness, nausea, and vomiting; they are readily reversed with naloxone. A patient developed signs and symptoms consistent with apraxia after a single dose of intranasal butorphanol. She was mentally alert, but she was unable to move or speak despite normal muscle tone and reflex movements. When she attempted to speak she had no voluntary control. At the emergency room she was administered naloxone 2 mg intramuscularly, which resulted in complete reversal of the symptoms in a short time. No other published cases describe these findings with butorphanol. Health care professionals should be aware that patients who are prescribed intranasal butorphanol, even in typical doses, may be at risk for such a reaction. This is important because, unlike the injectable formulation, the intranasal product is primarily used in the outpatient setting.

Administration, Intranasal↗

PubMed1996

[Use of a mix of lidocaine and butorphanol as a caudal epidural anesthesia in a mare].

Loss of rear motor control is the main limiting factor in the use of caudal epidural anesthesia in the horse. In man and laboratory animals, a small dose of an opiate combined with a local anesthetic enhances analgesia without impairing motor function. Thus, the amount of local anesthetic administered may be reduced. Butorphanol is an opiate widely used in horses. It has a good margin of safety and few cardiorespiratory effects. The effects of lidocaine (0.25 mg/kg) and lidocaine-butorphanol (0.25 mg/kg, and 0.04 mg/kg, respectively) were compared in 2 groups of 5 healthy unsedated mares. Horses in each group received either lidocaine or lidocaine-butorphanol in saline solution for a total volume of 0.0165 mg/kg. Epidural injection was performed at the first coccygeal interspace. Each mare was used only once. Cutaneous analgesia was assessed by a response to a pin prick; and visceral analgesia was assessed by response to a noxious stimulus applied to the urethra. Heart rate, respiratory rate, and arterial blood pressure were also measured. Analysis of the results showed an increase in duration of both cutaneous and visceral analgesia in the mares given lidocaine-butorphanol. Cutaneous analgesia increased from 36 +/- 13 to 150 +/- 21 min and visceral analgesia increased from 22 +/- 10 to 162 +/- 16 min. A cranial extension of the cutaneous analgesia was also observed. Cardiorespiratory depression or signs of excitation were not observed. However, these mares demonstrated peculiar walking in the hind limbs, not associated with signs of ataxia or hyperkinesia.

Analgesics, Opioid↗

PubMed1997

Comparison of ketoprofen, oxymorphone hydrochloride, and butorphanol in the treatment of postoperative pain in dogs.

OBJECTIVE: To compare analgesic effects of ketoprofen, oxymorphone hydrochloride, and butorphanol when used to control postoperative pain associated with elective orthopedic surgery in dogs. DESIGN: Prospective randomized clinical trial. ANIMALS: 70 dogs undergoing orthopedic surgery on a hind limb. PROCEDURE: Dogs were randomly assigned to 1 of 4 postoperative analgesic treatment groups: ketoprofen alone, oxymorphone alone, butorphanol alone, or ketoprofen-oxymorphone. Drugs were given IM at the end of anesthesia. Pain score, sedation score, arterial blood pressures, arterial blood gas partial pressures, and plasma cortisol concentration were measured for 12 hours after surgery. If the pain score was > or = 9, supplemental oxymorphone was administered IM. RESULTS: The proportion of dogs that did not require supplemental treatment with oxymorphone was significantly higher for the ketoprofen alone and ketoprofen-oxymorphone groups than for the oxymorphone alone group. During the first hour after surgery, pain score was lower for oxymorphone alone and ketoprofen-oxymorphone groups than for ketoprofen or butorphanol alone groups. Significant differences were not detected among groups in regard to pain score 2 and 3 hours after surgery or in regard to arterial blood pressures at any time. From 4 to 12 hours after surgery, pain score was significantly lower for the ketoprofen alone group than for other groups. Plasma cortisol concentration was significantly higher for the oxymorphone alone group 6 and 8 hours after surgery, compared with other groups. CLINICAL IMPLICATIONS: Except during the first hour after surgery, dogs given ketoprofen alone after elective orthopedic surgery had a greater level of, and longer-lasting, analgesia than did dogs given oxymorphone or butorphanol alone.

Analgesics, Opioid↗

PubMed1975

Butorphanol and pentazocine in patients with severe postoperative pain.

Either butorphanol tartrate (1, 2, or 4 mg) or pentazocine (30 or 60 mg) was given intramuscularly (5 dose groups) to 262 patients, who were scheduled for major operations, if they had severe pain after full awakening in the recovery room, postoperatively under double-blind conditions. There were at least 50 patients in each of the five dosage groups. Pain intensity and relief were scored numerically for each treated patient at 1/2 1, 2, 3 and 4 hr, while under direct surveillance, and the patients were seen again for follow-ups during the first 24 hr postoperatively. Appreciable pain relief developed within 30 min at all dose levels, with a peak analgesic effect apparent at about 1 hr. Satisfactory relief persisted for 4 hr in the majority of patients in each group. With the lowest dose of butorphanol tartrate (1 mg), which gave good pain relief for only 2 to 4 hr, approximately 60% of the patients had to be remedicated within 4 hr. Vital signs were not appreciably affected, but the patients who received the high dose of analgesics (butorphanol tartrate 4 mg or pentazocine lactate 60 mg) were often quite drowsy. The incidence of other side effects was negligible. The relative potency assay showed that butorphanol was approximately 20 times as potent as pentazocine for up to 4 hr.

Adolescent↗

PubMed2001

Tolerance to the analgesic effect of buprenorphine, butorphanol, nalbuphine, and cyclorphan, and cross-tolerance to morphine.

PURPOSE: The increased use of opioids in the chronic treatment of pain, especially with oncologic patients, encourages the search for drugs with potent analgesic activity, but with minimal induced tolerance and cross-tolerance to morphine. METHODS: Four agonist-antagonist opioid derivatives (buprenorphine, butorphanol, nalbuphine, and cyclorphan) were examined. Tolerance to the analgesic effect of the four drugs and their cross-tolerance effects with morphine were evaluated in ICR albino mice by the "hot plate method". Measurements of the analgesic effect were taken before and after chronic treatment (of 14 days duration) with these drugs, as well as morphine. RESULTS: All tested drugs produced tolerance after 14 days of treatment. Chronic treatment with morphine reduced the effects of nalbuphine and cyclorphan, but not those of buprenorphine and butorphanol. After 14 days treatment with buprenorphine and cyclorphan, the analgesic action of morphine was reduced, but this reduction did not occur after butorphanol and nalbuphine treatments. CONCLUSION: Of the four agonist-antagonists tested, butorphanol seems to be least likely to produce cross-tolerance with morphine.

Journal Article↗

PubMedDate not supplied

Butorphanol and morphine: a double-blind comparison of their parenteral analgesic activity.

The analgesic effects of butorphanol tartrate and morphine sulfate were compared in 127 patients judged to have moderate to severe pain following major operations. The study was double-blind, and the drugs were given IM at several dosage levels. Scores for pain intensity and relief, as well as pain-intensity difference, were determined at 30, 60 and 120 minutes after medication, then were analyzed by a parallel-line assay method in a modified computer program. The analysis indicated butorphanol tartrate to be 7 times as potent as morphine sulfate. Peak analgesic effects were obtained at 60 minutes with both drugs. Side effects were minimal in degree and incidence. Neither butorphanol nor morphine induced any changes in blood pressure, pulse rate, or respiratory rate. These data, along with those from studies elsewhere, suggest that butorphanol is a safe, potent, and effective analgesic agents, with probably a low potential for inducing drug dependence.

Adolescent↗

PubMedDate not supplied

Derivatization methodology for the analysis of butorphanol by gas chromatography-mass spectrometry.

Butorphanol is an opioid used as analgesic in humans and other species. In horses, it can cause locomotor stimulation at low doses. This drug is not well chromatographed by GC and so, it is necessary to transform it into a more suitable compound, which can be done by derivatization. The derivatization of a drug is used to impart volatility, masking polar groups to improve the results in gas chromatographic analysis. We have evaluated N,O-bis(trimethylsilyl)- trifluoracetamide (BSTFA)+ 1% trimethylchlorsilane (TMCS) and N-methyl-N-trimethylsilil-trifluoroacetamide (MSTFA) as derivatizing reagents for butorphanol at 30, 60 and 80 degrees C during 15, 30 and 60 min. The effects of dilution of these reagents with toluene and the evaporation before the derivatization were tested. Both reagents can be used for butorphanol derivatization and analysis and the dilution and evaporation steps did not alter the final results. The best derivatization conditions were 15 min at 80 degrees C, although 60 degrees C, although 60 degrees C during 60 min were also suitable.

Acetamides↗

PubMed1980

Double-blind comparison of intravenously injected butorphanol and meperidine in parturients.

One hundred women with moderate-to-very-severe prepartum pain participated in a double-blind study of intravenously injected butorphanol and meperidine that compared the analgesic properties, effect on the process of labor, condition of the newborn and the incidence of side effects associated with the two drugs. Cervical dilation, infant birth weight and Apgar scores were not significantly different between the test groups. The mean fetal heart rate for the butorphanol group was significantly faster than that of the meperidine group. Butorphanol provided significantly more analgesia than meperidine at 30 minutes and one hour after administration, based on pain intensity and pain relief scores. Some side effects, including sedation, dizziness, lightheadedness, nausea, vomiting and pain at the injection site, were reported for both drugs.

Adolescent↗

PubMed1980

Pharmacokinetics of subcutaneous and intramuscular butorphanol in dogs.

Butorphanol tartrate was administered intramuscularly and subcutaneously to adult male and female dogs at a dose of 0.25 mg/kg. No significant absorption lag time and no significant difference bwtween peak intramuscular and subcutaneous serum concentrations were observed. The mean peak serum concentration was 29 ng/ml at mean times of 28 min after subcutaneous administration and 40 min after intramuscular administration. There were no significant differences in the pharmacokinetics of butorphanol in dogs with either route. The serum half-life was 1.62 hr, and the serum clearance was 3.45 liters/kg/hr. The apparent volume of distribution of butorphanol was 7.96 liters/kg. Although considerable inter- and intraanimal variation in Cmax and AUC was observed, there was no significant difference in the area under the serum concentration versus time curves, and the two administration routes were considered bioequivalent.

Animals↗

PubMed1991

Butorphanol compared with fentanyl in general anaesthesia for ambulatory laparoscopy.

Butorphanol was compared with fentanyl as the narcotic component of general anaesthesia for ambulatory laparoscopic surgery. This double-blind, randomized study enrolled 60 healthy women who received equianalgesic doses of fentanyl 1 microgram.kg-1 (F, n = 30) or butorphanol 20 micrograms.kg-1 (B, n = 30) prior to induction of anaesthesia. Tracheal anaesthesia was maintained with nitrous oxide/oxygen, isoflurane, and succinylcholine by infusion. Intraoperatively, patients who received B demonstrated lower pulse rate before and after intubation (P less than 0.05, P less than 0.01) and lower diastolic blood pressure after intubation (P less than 0.01). Anesthesiologists judged the maintenance phase as satisfactory more often with B (P less than 0.05). Postoperatively, there were no differences in analgesic need. No major side-effects occurred in either group. Among minor side-effects, patients who received B reported postoperative sedation more often, 77% vs 37% (P less than 0.01), which occurred during the first 45 min of recovery (P less than 0.05). Discharge times were not different. On the first postoperative day, more subjects who received B were satisfied with their anaesthesia experience (P less than 0.05). Butorphanol 20 micrograms.kg-1 is an acceptable alternative analgesic in general anaesthesia for ambulatory laparoscopy.

Adult↗

PubMed2001

Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans.

RATIONALE: The availability of the highly selective and specific kappa opioid agonist enadoline provides an opportunity to explore the function of kappa receptors in humans and their potential utility as a target for substance abuse pharmacotherapy development. OBJECTIVES: The purpose of this study was to characterize the pharmacodynamic effects of enadoline, a selective kappa agonist, and to compare it with butorphanol, a mixed mu/kappa agonist, and hydromorphone, a mu agonist, in humans. METHODS: Pilot evaluation (n=3) served to establish intramuscular doses of enadoline (20, 40, 80, and 160 microg/70 kg), butorphanol (1.5, 3, 6, and 12 mg/70 kg), and hydromorphone (1.5, 3, and 6 mg/70 kg) of comparable activity. These acute doses were examined under double-blind, placebo-controlled and constrained randomized conditions with a minimum of 72 h between tests in volunteers with polysubstance abuse histories (n=6). Physiological and subject- and observer-rated measures were collected 30 min before and for 4 h after administration. RESULTS: Enadoline significantly increased measures of sedation, confusion and dizziness, produced visual distortions and feelings of depersonalization, and increased urinary output. The highest dose (160 microg/70 kg) was not tolerated and led to psychotomimetic effects. Hydromorphone produced prototypic mu opioid effects including respiratory depression, miosis, and euphoria. Butorphanol was most similar to hydromorphone and shared few effects with enadoline. CONCLUSIONS: These results are discussed with respect to the potential use and safety of kappa agonists for clinical indications.

Adult↗

PubMed1994

Influence of chronic morphine treatment on protein kinase C activity: comparison with butorphanol and implication for opioid tolerance.

The aim of this study was to determine whether chronic opioid treatment could influence the protein kinase C (PKC) activity in the rat brain. Chronic morphine (microns agonist) but not butorphanol (mu/delta/kappa mixed agonist) treatment enhanced cytosolic PKC activity in the pons/medulla, but not in the cytosolic fractions of cortex and midbrain regions. Concomitant administration of the opioid receptor antagonist, naloxone, blocked the PKC upregulation by chronic morphine. Chronic administration of morphine and butorphanol produced no change in the membrane PKC activity. Antinociceptive tolerance to morphine but not to butorphanol was developed under these conditions. These results suggest that chronic morphine administration leads to an upregulation of the cytosolic PKC activity in the pons/medulla through repeated activation of mu opioid receptors and that the PKC upregulation in this specific area may contribute to the morphine tolerance.

Animals↗

PubMed1996

Naloxone-precipitated changes in biogenic amines and their metabolites in various brain regions of butorphanol-dependent rats.

Influence of a naloxone (an opioid receptor antagonist) challenge (5 mg/kg, IP) on levels of biogenic amines and their metabolites in various brain regions of rats infused continuously with butorphanol (a mu/delta/kappa mixed opioid receptor agonist; 26 nmol/microliter/h) or morphine (a mu-opioid receptor agonist; 26 nmol/microliter/h) was investigated using high-performance liquid chromatography with electrochemical detection (HPLC-ED). Naloxone precipitated a withdrawal syndrome and decreased the levels of: dopamine (DA) in the cortex and striatum, 3,4-dihydroxyphenylacetic acid (DOPAC) in the striatum, homovanilic acid (HVA) in the striatum, limbic, midbrain, and pons/medulla regions in butorphanol-dependent rats. However, the levels of norepinephrine (NE), serotonin (5-hydroxytryptamine; 5-HT), and 5-hydroxyindoleacetic acid (5-HIAA) in the regions studied were not affected by naloxone-precipitated withdrawal. In addition, naloxone increased the HVA/DA ratio in the cortex, while this ratio was reduced in the limbic, midbrain, and pons/medulla. The reduction of 5-HIAA/5-HT ratio was also detected in the limbic area. In the animals rendered dependent on morphine, the results obtained were similar to those of butorphanol-dependent rats except for changes of 5-HIAA levels in some brain regions. These results suggest that an alteration of dopaminergic neuron activity following a reduction of DA and its metabolites in specific brain regions (e.g., striatum, limbic, midbrain, and pons/medulla) play an important role in the expression of the opioid withdrawal syndrome.

Animals↗

PubMed1987

Agonist action of the agonist/antagonist analgesic butorphanol on dopamine metabolism in the nucleus accumbens of the rat.

The action of butorphanol, an opiate agonist/antagonist, was studied on dopamine (DA) metabolism in several mesocortical and mesolimbic areas and compared with its effects on the nigrostriatal DA pathway. While butorphanol had a bell-shaped dose-response relationship for elevation of DA metabolites in the striatum, it had no action on DA metabolites in the entorhinal, prefrontal, pyriform and cingulate cortices and in the olfactory tubercle. In all of these areas morphine stimulated dopamine metabolism (except for the entorhinal cortex). In contrast, in the nucleus accumbens, butorphanol increased the levels of dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA) and 3-methoxytyramine (3-MT) with no increase in DA steady state levels. This effect was reversible by both opiate antagonists, naloxone and WIN 44441-3 and appears to be mu-opioid receptor-mediated.

3,4-Dihydroxyphenylacetic Acid↗

PubMed1985

Butorphanol.

Butorphanol (Stadol) is a synthetic agonist-antagonist analgesic from the 14-hydroxymorphinan series. Animal studies display analgesia, antitussive effects, low gastrointestinal activity, limited respiratory depression, some cardiovascular and skeletal muscle actions, diuresis, slight miosis and opiate antagonism. Butorphanol is metabolized in the liver with renal excretion, yielding a half-life of 3-4 h. Pain relief is good to excellent with parenteral administration in 90% of patients with moderate to severe pain. Surgical anesthetic indications involve preoperative and preinduction supplementation, balanced anesthesia and postoperative pain. Side effects are sedation, nausea, elevated pulmonary vascular pressures and rarely CNS excitation. Limited respiratory depression exists. Butorphanol is a potent analgesic agent with a favorable side effect profile.

Anesthesia↗