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PubMed2006

Butorphanol for treatment of intractable pruritus.

Severe chronic itch and intractable pruritus are encountered frequently by dermatologists. Recent data suggest that generalized pruritus may result from an imbalance between the mu and kappa opioid systems, and kappa-agonists have been shown to inhibit pruritus in both animals and human beings. These findings led us to use butorphanol, a commercially available kappa-opioid agonist and mu-opioid antagonist. We present a case series of 5 patients with intractable pruritus associated with inflammatory skin diseases or systemic diseases who demonstrated rapid and marked improvement when treated with intranasal butorphanol. Because of the small, open-label nature of this study, butorphanol should be investigated further in a larger, randomized controlled trial.

Adult↗

PubMed2006

Comparison of butorphanol and thiopentone vs fentanyl and thiopentone for laryngeal mask airway insertion.

STUDY OBJECTIVE: To compare laryngeal mask airway (LMA) insertion conditions using a combination of butorphanol and thiopentone vs fentanyl and thiopentone. DESIGN: Prospective, randomized, and double-blind study. SETTING: Operating theater. PATIENTS: One hundred four females, with American Society of Anesthesiologists grades I and II, diagnosed with carcinoma cervix scheduled for intracavitary implant placement, were recruited into the study. The patients were randomly divided into 2 groups of 52 each. INTERVENTION: Anesthesia was induced with butorphanol (30 microg kg(-1)) and thiopentone in group B and fentanyl (1.5 microg kg(-1)) and thiopentone in group F, followed by LMA insertion. Anesthesia was maintained with O2, N2O, and isoflurane with spontaneous ventilation. MEASUREMENTS: Six variables were noted on a 3-point scale: jaw relaxation (nil/slight/gross), ease of insertion (easy/difficult/impossible), swallowing (nil/slight/gross), coughing/gagging (nil/slight/gross), limb/head movement (nil/slight/gross), and laryngospasm (nil/slight/gross). Postoperatively, sedation score was assessed on a 4-point scale at 1/2 hour, 1 hour, and 2 hours. MAIN RESULTS: The 2 groups were demographically similar. Incidence of full jaw relaxation at first attempt was significantly higher in group B vs F (48 vs 35 patients, P = 0.003). Insertion was easy in 48 vs 37 patients in group B and F, respectively (P = 0.017). The incidence of swallowing, patient movements, and laryngospasm was comparable among the groups. Coughing/gagging was significantly lower in group B (P = 0.008). Significantly more patients were sedated in group B at 1/2 hour (P = 0.010) and 1 hour (P = 0.000). None of the patients were deeply sedated at 1 hour. At 2 hours, all patients were awake. CONCLUSION: The use of butorphanol and thiopentone as induction agents produced excellent LMA insertion conditions compared to fentanyl and thiopentone (98% vs 86% success rate with 92% vs 71% easy insertion).

Adjuvants, Anesthesia↗

PubMed1987

Comparison of intramuscular dezocine with butorphanol and placebo in chronic cancer pain: a method to evaluate analgesia after both single and repeated doses.

Sixty hospitalized subjects with chronic moderate to severe pain as a result of advanced cancer were enrolled in a randomized, parallel, double-blind trial comparing single doses and multiple doses of intramuscular dezocine (10 mg) with butorphanol (2 mg) and placebo. During the initial 6-hour efficacy evaluation, analgesia was measured using verbal and visual scriptors and vital signs, and acute toxicity information was recorded. Subjects with initial pain relief entered the 7-day multidose portion of the trial, and efficacy and toxicity data were recorded daily. After the initial dose the peak analgesia of the active agents was similar, but the duration of analgesia was longer with dezocine. After multiple doses, dezocine was superior to butorphanol in terms of length of treatment. Dezocine had less toxicity than had butorphanol after both single and repeated doses, further suggesting that dezocine may be beneficial in managing chronic cancer pain. The described study design is unique in that it compares the analgesic efficacy and toxicity of several analgesics with placebo after both single and multiple doses in the same subject. This method may prove to be an alternative pain model to evaluate chronic cancer pain.

Adult↗

PubMed2000

Sustained-release butorphanol microparticles.

Various butorphanol-loaded microparticles have been prepared with a biodegradable copolymer P(FAD-SA) of erucic acid dimer (FAD) and sebacic acid (SA) and a copolymer P(CPP-SA) of carboxyphenoxypropane (CPP) and SA using a melt compounding and milling method. Drug release was measured in vitro following incubation of drug-loaded microparticles in water for injection at 37 degrees C. It was found that butorphanol was released in a sustained manner, yielding a cumulative drug release of about 100% over a period of 48 hr. Also, drug release was affected by drug loading and the size of the microparticles; however, it was not significantly influenced by the copolymer composition. Scanning electron microscopic (SEM) results showed that most of the particles were irregular in shape with uneven surfaces. The molecular weights of the copolymers were not changed after this fabrication process. In addition, 20% butorphanol-encapsulated microspheres were prepared with copolymer P(FAD-SA) by spray-drying. The SEM micrograph shows that the particle sizes of the microspheres ranged from 2 to 10 microns, and the external surfaces appear smooth. Moreover, rapid drug release was observed for these microspheres, with more than 92% of the encapsulated drug released within the first 2 hr.

Analgesics, Opioid↗

PubMed1984

Premedication with butorphanol. A comparison with morphine.

A blind comparison was made of butorphanol 2 mg with morphine 10 mg i.m. as the sole premedication in four groups, each of 10 women, undergoing total abdominal hysterectomy. On both subjective and objective grounds, butorphanol was as effective as morphine with the advantage of fewer unwanted side-effects, although one patient complained of hallucinations. No clinically significant antagonism could be demonstrated between butorphanol and fentanyl. One patient gave accurate recall of intraoperative events, which reflects the problem of designing a properly constructed scoring system, based on basic clinical signs, to predict accurately the adequacy of anaesthesia.

Adult↗

PubMed1984

Balanced anesthesia: a comparison of butorphanol and morphine.

We did a retrospective study to compare butorphanol with morphine for use in a balanced anesthetic technique with nitrous oxide, oxygen, and neuromuscular relaxants. Patient records were reviewed for preoperative, intraoperative, and postoperative arterial blood gas values and vital signs; postoperative analgesia, nausea, vomiting, hallucinations, and dysphoria; and patient recall of the procedure. Patients in the butorphanol group proved to have less postoperative respiratory depression as determined by arterial carbon dioxide tension on arrival in the recovery room (42.8 mm Hg vs 51.1 mm Hg). The patients who received butorphanol also had less nausea (8.3% vs 44.4%) and less vomiting (8.3% vs 33.3%) than those given morphine. Neither group had any recall of procedure, hallucination, or dysphoria as determined by postoperative interview.

Adult↗

PubMedDate not supplied

Effects of medetomidine and medetomidine-butorphanol combination on Schirmer tear test 1 readings in dogs.

Medetomidine is a commonly used sedative in veterinary medicine whether administered alone or in combination with an opioid such as butorphanol. There are no previous studies that look at the effects of this drug on sequential Schirmer tear test (STT) 1 readings in dogs, including effects on tear production after reversal of the drug. The present study looked at two groups of 10 dogs each that were sedated with intravenous medetomidine or a combination of medetomidine and butorphanol. All dogs had tear readings taken presedation, 15 min postsedation, and 15 min after reversal of medetomidine with atipamezole. Results revealed that intravenous sedation with medetomidine and medetomidine-butorphanol in dogs with no history of ophthalmic disease and presedation STT 1 readings above 15 mm/min, causes a significant decrease in tear production that is measurable at 15 min postsedation. Readings returned to near presedation values within 15 min postreversal in most cases. It is therefore recommended that all eyes be treated with a tear substitute from the time the sedative is given until at least 15 min after reversal.

Analgesics, Opioid↗

PubMed2004

Cardiopulmonary effects of medetomidine, oxymorphone, or butorphanol in selegiline-treated dogs.

OBJECTIVES: To determine if chronic selegiline HCl administration affects the cardiopulmonary response to medetomidine, oxymorphone, or butorphanol in dogs. STUDY DESIGN: Prospective randomized experimental study. ANIMALS: Twenty-eight adult, random source, hound dogs weighing 21-33 kg. METHODS: Dogs were assigned to the following treatment groups: selegiline + medetomidine (MED; n = 6); placebo + MED (n = 6), selegiline + oxymorphone (OXY; n = 6); placebo + OXY (n = 6); selegiline + butorphanol (BUT; n = 7) or placebo + BUT (n = 6). Nine dogs were treated with two of the three pre-medicants. Dogs were treated with selegiline (1 mg kg(-1) PO, q 24 hours) or placebo for at least 44 days prior to pre-medicant administration. On the day of the experiment, arterial blood for blood gas analysis, blood pressure measurements, ECG, cardiac ultrasound (mM-mode, 2-D, and continuous wave Doppler), and behavioral observations were obtained by blinded observers. An IV injection of MED (750 micro g m(-2)), OXY (0.1 mg kg(-1)) or BUT (0.4 mg kg(-1)) was given. Cardiopulmonary and behavioral data were collected at 1, 2, 5, 15, 30, and 60 minutes after injection. RESULTS: Selegiline did not modify responses to any of the pre-medicant drugs. Medetomidine caused a significant decrease in heart rate (HR), cardiac output (CO), and fractional shortening (FS). Mean arterial pressure (MAP), systemic vascular resistance (SVR), and central venous pressure (CVP) were increased. Level of consciousness and resistance to restraint were both decreased. Oxymorphone did not affect MAP, CO, CVP, or SVR, but RR and PaCO(2) were increased. Level of consciousness and resistance to restraint were decreased. BUT decreased heart rate at 1 and 5 minutes. All other cardiovascular parameters were unchanged. BUT administration was associated with decreased arterial pH and increased PaCO(2). BUT decreased level of consciousness and resistance to restraint. CONCLUSIONS AND CLINICAL RELEVANCE: Although pre-medicants themselves altered cardiopulmonary and behavioral function, selegiline did not affect the response to medetomidine, oxymorphone, or butorphanol in this group of normal dogs.

Animals↗

PubMedDate not supplied

Hemodynamic effects of intravenous midazolam-xylazine-butorphanol in dogs.

The hemodynamic effects of a mixture of midazolam (1.0 mg/kg), xylazine (0.44 mg/kg), and butorphanol (0.1 mg/kg) were evaluated in six adult dogs. The dogs were anesthetized with isoflurane for instrumentation. As the dogs returned to consciousness, baseline values were recorded and the midazolam-xylazine-butorphanol mixture and glycopyrrolate (0.01 mg/kg) were administered intravenously (IV). Hemodynamic data were recorded 3, 10, 20, 30, 40, 50, and 60 minutes after injection. Mean arterial pressure (AP), mean pulmonary arterial pressure (PAP), heart rate (HR), rate-pressure product (RPP), mean pulmonary capillary wedge pressure (PCWP), systemic vascular resistance (SVR), and right ventricular stroke work index (RVSWI) were increased significantly above baseline values. Cardiac output (CO), stroke volume (SV), cardiac index (CI), stroke index (SI), mean central venous pressure (CVP), and left ventricular stroke work index (LVSWI) were decreased significantly below baseline values. When administered IV at the dosages used in this study, midazolam-xylazine-butorphanol-glycopyrrolate induced profound acute alterations in several critical hemodynamic variables.

Animals↗

PubMedDate not supplied

Reversal of oxymorphone sedation by naloxone, nalmefene, and butorphanol.

The effects of naloxone (0.4 mg and 1.2 mg intravenously [IV]), nalmefene (0.03 mg/kg IV) and butorphanol (0.2 mg/kg IV and 0.4 mg/kg IV) on oxymorphone-induced sedation were studied in six dogs over a 4-hour observation period. The same dogs were observed for 4 hours untreated (unsedated control) and with oxymorphone sedation followed by saline solution (sedated control). The reversal drug or saline placebo was administered IV 20 minutes after oxymorphone (4.5 mg IV). Blinded observers evaluated the dogs for positional and attitudinal responses, heart rate, and respiratory rate. Sedated dogs treated with nalmefene most closely resembled unsedated dogs in all observed variables. Naloxone was most effective when administered at the higher dose. Mild renarcotization occurred in two dogs at hour 2, even after the higher naloxone dose. Residual sedation was observed in all dogs treated with 0.4 mg naloxone. Butorphanol resulted in partial reversal of sedation at both dosage levels. However, the degree of sedation was significantly less than that observed in the saline-treated controls, and it appeared that 0.4 mg/kg butorphanol may be clinically useful for opiate reversal in some situations.

Animals↗

PubMedDate not supplied

Cardiorespiratory effects of combined midazolam and butorphanol in isoflurane-anesthetized cats.

The cardiorespiratory effects of midazolam (0.1 mg/kg) and butorphanol (0.4 mg/kg) were evaluated in seven cats. Cats were induced in a chamber, removed and intubated, and maintained with isoflurane in 100% oxygen. Cardiorespiratory data were recorded before and 3, 10, 20, 30, 40, 50, and 60 minutes after intravenous injection of midazolam-butorphanol. Heart rate, mean arterial pressure, and respiration rate were significantly (p < .05) decreased below baseline at various times throughout the study. Tidal volume and minute ventilation were unchanged. End-tidal carbon dioxide was significantly (p < .05) increased above baseline for 30 minutes. Midazolam-butorphanol administered intravenously induced significant alterations in several cardiorespiratory parameters in isoflurane-anesthetized cats.

Adjuvants, Anesthesia↗

PubMedDate not supplied

Determination of the ED50 of isoflurane and evaluation of the isoflurane-sparing effect of butorphanol in cockatoos (Cacatua spp.).

The use of butorphanol as an analgesic in a psittacine species was evaluated by determining its isoflurane-sparing effects. The Effective Dose 50 (ED50) of isoflurane was determined using a bracketing technique based on the purposeful movement elicited by pressure applied to a digit with a hemostat. The ED50 of isoflurane for 11 cockatoos (four greater sulfur crested, three lesser sulfur crested, and four citron crested) was determined to be 1.44 +/- 0.07%. After the administration of 1 mg/kg of butorphanol tartrate intramuscularly (IM), the ED50 was significantly (P < .05) decreased to 1.08 +/- 0.05%. Physiological variables that changed significantly included decreases in heart rate, tidal volume (Vt), inspiratory (Ti) and expiratory times (Te), and an increase in respiratory rate. No complications resulted because of these changes. Based on the results, butorphanol produces an isoflurane-sparing effect in cockatoos and has the potential to be a useful analgesic in psittacines.

Administration, Inhalation↗

PubMed1997

Effect of romifidine and romifidine-butorphanol for sedation in dogs.

The sedative and physiological effects of intravenous romifidine at 120 micrograms/kg were compared with intravenous romifidine (120 micrograms/kg) followed immediately by intravenous butorphanol (0.1 mg/kg) in 18 clinically normal adult beagles in a blinded randomised change-over study. Following the injection of romifidine alone the dogs became recumbent and there was an increase in a subjective score awarded to the degree of sedation. Heart rate and respiratory rate decreased and minor bradyarrhythmias were noted. The romifidine-butorphanol combination produced a significant decrease in the time to the onset of sedation and increase in the sedative effect and duration of action compared with romifidine alone. With the exception of a further decrease in heart rate and respiratory rate, there were no additional side effects following the use of the romifidine-butorphanol combination. The marked sedative effect associated with this combination would appear to be useful in the clinical situation where an increased degree of sedation is required.

Adrenergic alpha-Agonists↗

PubMed1997

Effect of high volume epidural morphine, ketamine and butorphanol on halothane minimum alveolar concentration in ponies.

This study determined the effects of epidurally administered morphine, ketamine and butorphanol on halothane minimum alveolar concentration (MAC) in ponies. Seven ponies were anaesthetised with thiopentone and succinylcholine, intubated and anaesthesia maintained with halothane. Ventilation was controlled and blood pressure was maintained within normal limits. Following the determination of baseline halothane MAC for the pelvic and thoracic limbs the ponies were given morphine (0.1 mg/kg bwt), ketamine (0.8 or 1.2 mg/kg bwt), butorphanol (0.05 mg/kg bwt) or saline, epidurally, to a final volume of 0.15 ml/kg bwt. The halothane MAC for the pelvic and thoracic limbs was redetermined following each treatment. The baseline halothane MAC for the control group was mean +/- s.e. 0.85 +/- 0.02% and no significant change occurred after saline administration. Morphine significantly (P = 0.002) decreased MAC from, mean +/- s.e. 0.90 +/- 0.05% to 0.77 +/- 0.06% in the pelvic limb. Ketamine significantly decreased MAC in the pelvic limb from mean +/- s.e. 0.86 +/- 0.06% to 0.71 +/- 0.04%, and 0.82 +/- 0.03% to 0.71 +/- 0.02%, for the low (P = 0.008) and high dose (P = 0.001), respectively. No significant change in MAC occurred following butorphanol. No treatment reduced halothane MAC for the thoracic limb.

Analgesics↗

PubMed1993

Medetomidine-butorphanol-midazolam for anaesthesia in dogs and its reversal by atipamezole.

The clinical efficacy of a combination of medetomidine, butorphanol and midazolam for anaesthesia in dogs, and its reversal by atipamezole, was evaluated in two experimental groups of four adult beagle dogs and compared with a control group of four dogs receiving only midazolam and butorphanol. The anaesthetic procedure was used for surgical procedures in another group of 14 dogs. After the injection of medetomidine, a rapid loss of coordination followed by mild sedation was observed. Anaesthesia was attained 2 +/- 1 minutes after the administration of butorphanol and midazolam and lasted 82 +/- 5 minutes, the dogs recovered 51 +/- 6 minutes later and there were no side effects. Analgesia and skeletal muscle relaxation were optimal throughout the period of anaesthesia. Statistically significant bradycardia and hypothermia were observed but there were no significant effects on respiratory function. After atipamezole the dogs recovered their normal posture, heart rate and body temperature in less than 20 minutes. In the control group, the short-lived light sedation was accompanied by inadequate analgesia and poor muscle relaxation. In the surgical group, no differences, except in drug requirements, were recorded in comparison with the experimental groups. Good analgesia and muscle relaxation, total absence of side effects and stability in vital body functions were observed. The injection of atipamezole was always effective, devoid of side effects and induced recovery in less than 20 minutes.

Adrenergic alpha-Antagonists↗

PubMed1983

Butorphanol tartrate: an intravenous analgesic for outpatient surgery.

Many surgical procedures in otolaryngology, particularly those in the areas of facial plastic surgery, are best performed under a local anesthetic. The majority of these procedures may be done on an outpatient basis and require an intravenous analgesic of some form. This analgesic must be safe, predictable, easy to administer, have a rapid onset, and provide good amnesia. A short recovery period is imperative. Diazepam has been widely used in the outpatient setting, since it generally fulfills the requirements listed. However, the recovery time is often prolonged and unpleasant for the patient. Butorphanol tartrate, a synthetic narcotic, provides rapid analgesia in an intravenous dose, fulfills the other requirements for an analgesic agent suitable for outpatient use, and has a relatively short duration. Butorphanol tartrate has been used in an intravenous drip form for outpatient surgical procedures for the past 18 months. Its use in 400 cases representing a broad spectrum of facial plastic procedures has been closely monitored in both the operative and postoperative periods and the results tabulated. We have found butorphanol tartrate to be an excellent agent for local anesthetic procedures in the outpatient setting.

Adolescent↗

PubMed1997

Butorphanol (Stadol): a study in problems of current drug information and control.

Butorphanol (Stadol, Bristol-Meyers Squibb, Princeton, NJ) is a synthetically derived opiate. As a nasal spray, it was approved for release in 1991 and was subsequently promoted as a safe treatment for migraine. Since then, there have been numerous reports of problems with butorphanol similar to those of any narcotic, especially dependence-addiction and major psychological disturbances. These problems have been documented by the Food and Drug Administration, but the information can be obtained only through the Freedom of Information Act. The experience with butorphanol indicates the need for physicians to have additional sources of information about drugs than are presently available.

Administration, Inhalation↗

PubMed1991

Epidural morphine with butorphanol for postoperative analgesia after cesarean delivery.

Epidural morphine has been used more and more to provide long-lasting postoperative analgesia after cesarean delivery. However, the incidence of pruritus (20%-93%) and nausea (17%-60%) detract from the usefulness of epidural morphine. The purpose of this study was to evaluate, in 30 patients having epidural anesthesia for cesarean delivery, the analgesic efficacy and side effects when a combination of epidural morphine, a mu-receptor agonist, and butorphanol, a mu-receptor antagonist and kappa-receptor agonist, was administered. After clamping of the umbilical cord, patients received 4 mg epidural morphine with 3 mL of normal saline (group 1), 4 mg epidural morphine with 1 mg butorphanol and 2 mL of normal saline (group 2), or 4 mg epidural morphine with 3 mg butorphanol (group 3). Patients were monitored for 24 h after administration of the study medications. There were no significant differences between the groups in visual analogue pain scores, time to first analgesic request, respiratory rate, or Trieger dot test performance in the 24 h immediately after these epidural injections. There were three patients in group 1 and one patient in group 2 who experienced oxygen saturations less than 90%. (No patients in group 3 developed an oxygen saturation less than 92%.) The patients in group 3 did not require treatment for pruritus or nausea, a response significantly different (P less than 0.001 and P less than 0.05, respectively) from group 1 or group 2.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗