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PubMed1994

Involvement of kappa-opioid receptors in opioid dependence/withdrawal: studies using butorphanol.

The dependence liability of a class of opioid agonist/antagonist analgesics, e.g. pentazocine, butorphanol, and buprenorphine, is widely recognized. However, the relative involvement of mu-, delta-, and kappa-opioid receptors mediating physical dependence on these compounds is not completely known. In the present study, butorphanol dependence was produced by continuous intracerebroventricular (i.c.v.) infusion of butorphanol (26 nmol/h) for 3 days in male Sprague-Dawley rats. Nor-binaltorphimine, a long-acting kappa-opioid receptor antagonist, and naloxone, a nonspecific antagonist, were administered i.c.v. to precipitate withdrawal in butorphanol-dependent animals, so as to investigate the involvement of central kappa-opioid receptors in opioid dependence. ED50 ratios (naloxone/nor-binaltorphimine) for eliciting withdrawal signs were: teeth-chattering (1.25), yawning (2.13), and ejaculation (0.72). Our data indicate that nor-binaltorphimine precipitated withdrawal behaviors similar to those precipitated by naloxone. It appears that central kappa-opioid receptors may play a major role in the development of butorphanol dependence in rats.

Animals↗

PubMed1993

The opioid receptor binding of dezocine, morphine, fentanyl, butorphanol and nalbuphine.

The ability of morphine, fentanyl, butorphanol, nalbuphine, and dezocine to compete with radiolabeled ligands for binding at the mu1, mu2, kappa1, and delta opioid receptors and the sigma receptor was characterized. In the absence of sodium, the potency of opioid receptor competition at each receptor site was found to be: mu1-fentanyl > butorphanol > morphine > or = dezocine = nalbuphine; mu2-butorphanol > fentanyl > nalbuphine > morphine = dezocine; kappa1-butorphanol > nalbuphine >> morphine > or = dezocine > fentanyl; and delta-butorphanol > nalbuphine > or = dezocine > morphine > fentanyl. For all five compounds, competition at the sigma receptor was weak, with nalbuphine and dezocine having Kis of approximately 0.5 microM and the other opioids having Kis of greater than 1 microM. Since the presence of 100 mM NaCl during the competitive binding decreased the K(i), to varying degrees, of all five opioids at the mu1 and delta receptors and of some of the opioids at the mu2 and kappa1 receptors, the five compounds studied appear to differ in efficacy at the five receptor sites.

Analgesics, Opioid↗

PubMed1990

Discrimination of butorphanol and nalbuphine in opioid-dependent humans.

The purpose of the study was to evaluate the agonist and antagonist stimulus properties of the mixed opioid agonist antagonists butorphanol and nalbuphine in opioid-dependent subjects. Opioid-dependent volunteers (methadone 30 mg/day, PO) were trained in a three-choice drug discrimination procedure to discriminate between the effects of saline (2 ml), hydromorphone (10 mg/70 kg) and naloxone (0.15 mg/70 kg) administered IM. Subjects earned monetary reinforcement for correctly identifying the training drugs by letter code. Other subjective, behavioral and physiological measures were also collected. Hydromorphone and naloxone increased drug-appropriate responses and other characteristic subjective effects measures. Butorphanol and nalbuphine produced increases in naloxone-appropriate discrimination responding and in those subjective effect measures increased by naloxone. Butorphanol produced greater than 80% naloxone-appropriate responding at 1.05 mg/70 kg; nalbuphine produced 100% naloxone-appropriate responding at 2.1 mg/70 kg. Neither butorphanol nor nalbuphine showed opioid agonist-like effects in these subjects maintained at moderate levels of physical dependence. In opioid-dependent subjects, the stimulus effects of butorphanol and nalbuphine are antagonist-like.

Adult↗

PubMed1992

Antinociceptive properties of tiletamine-zolazepam improved by addition of xylazine or butorphanol.

A combination of tiletamine HCl and zolazepam HCl is frequently used as an anesthetic, but little is known about the antinociceptive properties of tiletamine-zolazepam. The antinociceptive properties of tiletamine-zolazepam alone or combined with xylazine or butorphanol were determined in the adult male rate using the tail-flick test. Changes in tail-flick latency were determined at 15, 45, and 75 min after IP drug administration of sterile water, sodium pentobarbital, morphine, tiletamine-zolazepam, xylazine, butorphanol, and tiletamine-zolazepam plus xylazine or butorphanol. Tail-flick latency approximated 100% maximum possible effect (MPE) at 15-75 min postinjection in morphine-treated rats. Tiletamine-zolazepam, xylazine, and butorphanol alone, at any dose utilized, produced less than 50% MPE. However, the combination of tiletamine-zolazepam with butorphanol or xylazine increased tail-flick latency approximately three times greater than tiletamine-zolazepam alone. These results demonstrate that: a) consonant with earlier findings, analgesia and anesthesia are independent states; b) tiletamine-zolazepam is not an effective combination with respect to analgesia; but c) in concert with appropriate drugs, it can exhibit potent antinociceptive properties.

Analgesics↗

PubMed1995

Comparative rewarding properties of morphine and butorphanol.

Because butorphanol (Stadol), a synthetic morphinan compound, has been demonstrated in our laboratories to produce physical dependence and withdrawal symptoms in rats, we have hypothesized that butorphanol has rewarding properties indicative of abuse potential. To test this hypothesis, the effects of equimolar doses of butorphanol tartrate (0.5-5.0 micrograms) and morphine sulfate (0.8-8.0 micrograms) were assessed in inbred Lewis male rats using the conditioned place preference (CPP) paradigm. Unilateral microinjections (1 microl/inj) of saline or opioids were made into the ventral tegmental area (VTA). Microinjections of saline to controls were associated with both sides of modified Skinner boxes, whereas opioid injections were associated only with the white chambers (less preferred side to the naive animals). Opioids were administered alternating with saline in the drug-treated animals on alternating days. During eight conditioning sessions the rats learned to associate light and dark sides of the Skinner boxes with microinjections of opioids or saline, respectively. Although all doses of morphine induced significant preference over saline, only the higher doses of butorphanol (2.0-5.0 micrograms) produced significant conditioned place preference for the sides of the chambers associated with the drugs. These results suggest that, like morphine which is widely abused, butorphanol also has rewarding properties, and, therefore, further investigations regarding its abuse potential are necessary.

Animals↗

PubMed1994

Effectiveness of transnasal butorphanol for the treatment of musculoskeletal pain.

A prospective, open-label study of the effectiveness of transnasal butorphanol in the treatment of pain resulting from musculoskeletal injuries. Twenty-eight patients with strains (n = 20), fractures (n = 6), contusions (n = 1), and stab wounds (n = 1) were included. All patients were examined by an attending level emergency medicine physician and deemed to have pain severe enough to warrant parenteral narcotic analgesia. All patients received an initial 1-mg dose of transnasal butorphanol. Subsequent dosing was flexible depending on response to the initial dose. All patients received pain relief from transnasal butorphanol, and only one requested alternative analgesic medication. Fifty-seven percent (n = 16) of patients noticed at least a little relief of pain within 5 minutes of administration and 93% (n = 26) received at least a little relief within 15 minutes. Seventy-one percent of the patients received a 50% reduction of pain within 60 minutes. No serious side effects were noted, but drowsiness occurred in 82% (n = 23) and dizziness in 54% (n = 15) of the patients. One patient discontinued participation in the study because of nausea. In this limited trial transnasal butorphanol proved to be a rapidly effective opioid analgesic. Further controlled studies comparing transnasal butorphanol with standard parenteral narcotics are needed.

Administration, Intranasal↗

PubMedDate not supplied

Butorphanol for the relief of shivering associated with extradural anesthesia in parturients.

STUDY OBJECTIVE: To assess the efficacy of butorphanol for the relief of shivering following the epidural administration of 2% lidocaine. DESIGN: Randomized, double-blind study. SETTING: Labor and delivery department of a university-affiliated hospital inpatient facility. PATIENTS: Sixty-one healthy labor patients. INTERVENTIONS: Patients who had sustained shivering associated with lidocaine epidural anesthesia were given normal saline or butorphanol 1 mg. Patients were observed for 20 minutes following the administration of a study solution. MEASUREMENTS AND MAIN RESULTS: Shivering ceased within a mean time of 12.9 +/- 3.8 minutes in approximately 81% of the patients who received epidural butorphanol (p < 0.01), while 3% of the patients in the placebo group had no shivering following the administration of epidural saline. No sedation or changes in fetal heart rate were associated with epidural butorphanol. CONCLUSIONS: Epidural butorphanol is effective in the treatment of postepidural shivering associated with epidural lidocaine. Epidural agonist opioids have been reported to be efficacious in the management of postepidural shivering. This study demonstrated that a partial agonist opioid also is effective in the treatment of postepidural shivering.

Adult↗

PubMed2004

The effects of a cold-water stimulus on butorphanol effects in males and females.

Using a crossover, randomized, double-blind, cumulative-dosing procedure, we examined whether a painful stimulus modulated subjective and psychomotor effects of butorphanol in eight male and eight female volunteers. During each session, volunteers received four intravenous injections of either butorphanol (0, 0.5, 1, and 2 mg/70 kg) or saline (placebo) at hourly intervals. Saline and butorphanol were tested in two conditions, forearm immersion 30 min after each injection into either 2 or 37 degrees C water. During the 180-s immersion, volunteers completed a visual analog scale (VAS), psychomotor test, and pain ratings. VAS ratings of "Coasting ('spaced out')", "heavy or sluggish feeling," and "sleepy" were lower in the 2 degrees C than in the 37 degrees C condition during butorphanol administration, but only in females. Modulation by a painful stimulus of sleepy ratings was confined to the third immersion (i.e., a dose effect). The cold-water stimulus significantly decreased butorphanol-induced impairment during the third immersion for males, and females showed a similar trend. Overall, pain ratings were higher in females, and although not significant, males reported a greater degree of analgesia. The differences in pain ratings and degree of analgesia between the sexes are discussed as a possible mechanism for the sex differences in modulatory effects.

Adult↗

PubMed1999

Withdrawal from butorphanol dependence alters binding of [3H]phorbol dibutyrate to protein kinase C, but not of [3H]forskolin to adenylate cyclase.

The time course of autoradiographic binding of major second messengers in the rat brain was studied at 2, 7, and 24 h after withdrawal from butorphanol infusion. [3H]Forskolin and [3H]phorbol 12,13-dibutyrate (PDBu) were used to label adenylate cyclase and protein kinase C (PKC), respectively. Rats were rendered dependent by intracerebroventricular infusion of butorphanol (26 nmol microliter-1 h-1) via osmotic minipumps for 3 days. Withdrawal was initiated by abrupt cessation of the butorphanol infusion. The levels of [3H]forskolin binding were not changed at any time or in any brain area, except for an increase following 7 h of withdrawal in the brainstem only. The levels of [3H]PDBu binding were significantly increased (13-47%) in multiple areas of the rat brain following 7 h of withdrawal from butorphanol infusion. These findings suggest that the phosphoinositide cycle system is more susceptible to alteration during butorphanol dependence than is the adenylate cyclase system in the rat brain.

Adenylyl Cyclases↗

PubMed1998

Butorphanol agonist effects and acute physical dependence in opioid abusers: comparison with morphine.

This study compared the direct effects and acute physical dependence of butorphanol and morphine, opioids with differing actions at mu versus kappa receptors. Six non-dependent heroin-using volunteers were exposed to six conditions in a within-subject, Latin square design using double-blind procedures. In each session, agonist effects of single i.m. injections of butorphanol (3 and 6 mg/70 kg), morphine (15 and 30 mg/70 kg), lorazepam (4 mg/70 kg) or saline were evaluated. Butorphanol and morphine produced effects of comparable magnitude on miosis and reports of 'any drug effect'. Volunteers reported dysphoria, confusion and sedation after butorphanol, subjective effects that overlapped with those of lorazepam, whereas morphine produced euphoria and stimulation. Acute physical dependence (i.e. precipitated withdrawal responses to naloxone 10 mg/70 kg i.m. administered 6 h after each treatment) significantly increased after 30 mg/70 kg morphine but not after butorphanol treatments. These differences in naloxone sensitivity are likely due to differences in opioid receptor (mu versus kappa) activity, affinity and efficacy of these compounds. Pharmacological ramifications of these results are discussed.

Adult↗

PubMed2002

Validation and application of a sensitive assay for butorphanol in human plasma by high-performance liquid chromatography with tandem mass spectrometry detection.

A sensitive and convenient high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) assay for the opioid receptor agonist-antagonist butorphanol in human plasma is described. BC-2605, a cyclopropyl analogue of butorphanol, was employed as an internal standard. Butorphanol was recovered from plasma (84.4 +/- 10.9%) by liquid-liquid extraction. The mobile phase flow-rate was 0.3 ml/min and consisted of methanol-water-formic acid (90:10:0.1, v/v/v). The analytical column (4.6 x 100 mm) was packed with Partisil C(8) (5 microm). The standard curve was linear from 13.7 to 1374 pg/ml (r(2)>0.99). The lower limit of quantitation was 13.7 pg/ml. The assay was specific, accurate (% deviation from nominal concentrations were <15%), precise and reproducible (within- and between-day coefficients of variation <7%). Butorphanol in plasma was stable over 3 freeze/thaw cycles and at room temperature for 1 day. The utility of the assay was demonstrated by following butorphanol plasma concentrations in two healthy subjects for 24 h following a 1 mg intranasal dose.

Adult↗

PubMed1996

Lack of pharmacokinetic interaction between butorphanol nasal spray and cimetidine.

The potential for a pharmacokinetic interaction between butorphanol nasal spray and cimetidine, under steady state conditions, was evaluated in 16 healthy male volunteers. Subjects received either a 1 mg butorphanol nasal spray every 6 h or a 300 mg cimetidine tablet every 6 h on days 1 4, the combination of two compounds every 6 h on days 5-8 and the original treatment as described in the first segment (days 1-4) on days 9-12. Serial blood and urine samples were collected on days 4, 8 and 12, and additional blood samples were taken immediately, prior to the morning dose on days 3, 7 and 11. Based on the analysis of the Cmin samples, the plasma concentrations of cimetidine and butorphanol achieved steady state by the third day of dosing. No statistically significant differences were found in the plasma concentrations of butorphanol or cimetidine (except for t1/2 and MRT) between any of the treatment phases. Butorphanol nasal spray and cimetidine can be co-administered without any adjustment of dosage for either drug.

Administration, Intranasal↗

PubMed2001

Analgesic effect of butorphanol and levomethadone in detomidine sedated horses.

The analgesic potency of butorphanol 25 microg/kg bodyweight (BW) and levomethadone 100 microg/kg BW, administered together with detomidine 10 microg/kg BW, was measured in twelve Warmblood horses in a randomized, blinded cross-over study. Detomidine with saline 10 ml 0.9% was used as placebo. The nociceptive threshold was determined using a constant current and a pneumatic pressure model for somatic pair Detomidine alone and in combination with butorphanol or levomethadone caused a significant temporary increase (P < 0.05) of the nociceptive threshold with a maximum effect within 15 min and a return to baseline levels within 90 min. Butorphanol and levomethadone increased the nociceptive threshold and prolonged the duration of anti-nociception significantly from 15 to 75 min (P < 0.05) after drug administration compared with detomidine alone to both test methods. No significant difference between butorphanol and levomethadone was registered. It is concluded that the addition of butorphanol or levomethadone to detomidine increases the nociceptive threshold to somatic pain and prolongs the analgesic effect of detomidine in the horse.

Analgesics, Opioid↗

PubMed1995

IV compared with brachial plexus infusion of butorphanol for postoperative analgesia.

In a randomized, double-blind, controlled study, we have compared two groups of patients receiving either continuous systemic i.v. or continuous brachial plexus infusion of butorphanol for analgesia after operations on the upper extremities. Twenty-two patients undergoing elective upper extremity surgery were allocated randomly to one of two groups to receive either butorphanol i.v. and saline injected into the brachial plexus sheath (i.v. group) or butorphanol injected into the brachial plexus sheath and saline i.v. (brachial plexus group). After surgery on the upper extremity under continuous axillary brachial plexus block, each patient received a continuous infusion of butorphanol either i.v. or into the brachial plexus sheath at a dose of 83.3 micrograms h-1. Concurrently, a saline infusion was given via the alternate route. Patients rated their pain on a 10-cm visual analogue scale (VAS). VAS scores in the two groups did not differ up to 6 h and 24 h after operation. From 9 h until 24 h after operation, pain scores were significantly higher in the i.v. group than in the brachial plexus group. The VAS score 9 h after operation was 3.3 (SD 2.7) in the i.v. group and 0.6 (0.9) in the brachial plexus group (P < 0.01); 12 h after operation 2.7 (1.8) in the i.v. group and 0.6 (0.9) in the brachial plexus group (P < 0.01); 18 h after operation 1.7 (1.0) in the i.v. group and 0.7 (1.0) in the brachial plexus group (P < 0.05); and 24 h after operation 3.2 (2.4) in the i.v. group and 0.7 (1.2) in the brachial plexus group (P < 0.01). We conclude that continuous injection of butorphanol into the brachial plexus sheath provided superior analgesia compared with continuous i.v. injection.

Adolescent↗

PubMed1996

The effects of transnasal butorphanol on mood and psychomotor functioning in healthy volunteers.

Transnasal butorphanol is effective in relieving migraine and postoperative pain. The extent to which this drug preparation impacts on cognitive and psychomotor performance, as well as mood, has not been examined. Accordingly, the cognitive and psychomotor, subjective, and physiological effects of two clinically relevant doses of transnasal butorphanol (1 and 2 mg) were compared to that of placebo, and a common analgesic drug combination given for pain relief in ambulatory settings, 600 mg of acetaminophen and 60 mg of codeine, in healthy volunteers (n = 10). The larger transnasal butorphanol dose impaired psychomotor performance for up to 2 h, and produced subjective effects for up to 3 h. The smaller dose had no psychomotor-impairing effects, but had subjective effects (including increased ratings of "sleepy"). All three active drug conditions including miosis. These laboratory results suggest that patients should use caution when using the 1-mg dose of transnasal butorphanol, and should curtail certain activities if they administer the 2-mg dose of transnasal butorphanol for analgesia.

Acetaminophen↗

PubMed1982

The enflurane sparing effect of morphine, butorphanol, and nalbuphine.

The potencies of morphine and of the narcotic analgesic agonist-antagonists butorphanol and nalbuphine in terms of their ability to decrease enflurane MAC were studied. Following the determination of control MAC for enflurane in each dog, an intravenous bolus dose of either butorphanol tartrate, nalbuphine hydrochloride, morphine, or placebo was administered and enflurane MAC was redetermined. A higher dose of the same drug was then administered and enflurane MAC was redetermined up to a total of four doses in each animal. The successive doses for morphine and nalbuphine were 0.5, 1.5, 5.0, and 20.0 mg/kg; for butorphanol, 0.1, 0.3, 1.0, and 4.0 mg/kg; lactated Ringer's solution was used as a placebo. Both butorphanol and nalbuphine produced significant reductions of enflurane MAC (11 and 8%, respectively) at their lowest doses. No further reductions were produced by three- to forty-fold larger doses of either agonist-antagonist. Morphine produced a 17% reduction of enflurane MAC at the lowest dose with progressive decreases of enflurane MAC up to 63% at a dose of 5 mg/kg morphine. A fourfold increase in the morphine dose did not further decrease MAC. No change in enflurane MAC occurred in the animals given placebo. It was concluded that there is a "ceiling" to the potency of butorphanol and nalbuphine as anesthetic supplements. There is also a limit to the anesthetic sparing effect of morphine, but it is considerably greater than that of the agonist-antagonist narcotic analgesics.

Anesthetics↗

PubMed2005

Intravenous butorphanol, meperidine, and their combination relieve pain and distress in women in labor.

BACKGROUND: Systemic opioids are commonly administered during labor, but their efficacy has been recently questioned. In addition, laboratory and clinical studies provide a strong rationale for combining mu- and kappa-opioid receptor agonists for analgesia. The authors therefore studied, using validated intensity and affective scales and definitions of effective pain relief, the efficacy of intravenous meperidine, butorphanol, and their combination for labor analgesia. METHODS: Healthy women with singleton term pregnancy requesting analgesia during active labor were studied. Women were randomly assigned to receive 50 mg meperidine, 1 mg butorphanol, or 25 mg meperidine plus 0.5 mg butorphanol (n = 15/group). Pain intensity was assessed using a 0-10 numerical rating scale, and affective magnitude was assessed using a ratiometric descriptive scale before drug administration and between the sixth and seventh uterine contractions after drug administration. RESULTS: All three treatments reduced pain intensity equally. Butorphanol alone did not reduce pain affective magnitude, whereas the other treatments did. There was a significant correlation between reduction in pain intensity and affective magnitude in all groups, with greater reductions in affective magnitude than intensity. Overall, 29% of women exhibited clinically meaningful pain relief, with no difference among groups. Groups did not differ in incidence of opioid-induced adverse effects. CONCLUSIONS: These doses of meperidine and butorphanol do reduce pain intensity and affective magnitude, although a minority of patients achieve meaningful pain relief as defined in multiple patient populations, including laboring women. Combination of these drugs did not improve their therapeutic benefit.

Adult↗

PubMed1979

Comparison of butorphanol and pentazocine as postoperative analgesics.

Sixty patients with moderate or severe postsurgical pain were randomly divided into three equal groups for a double-blind comparison of the analgesic effectiveness of intramuscular butorphanol (2 and 4 mg) and pentazocine (60 mg). The groups were demographically similar. Pain intensity and pain relief were scored at 10, 20, 30, 60, 120, 180, and 240 minutes after administration of the drug. All treatments provided significant analgesic activity (P less than .05) within ten minutes. However, both doses of butorphanol reached their peak effect at 30 minutes, in contrast to 60 minutes for pentazocine. The duration of effect appeared somewhat longer for butorphanol, though this did not achieve statistical significance. Butorphanol (4 mg) had a significantly greater (P less than .05) analgesic effect at ten minutes than pentazocine (60 mg), and both butorphanol treatments (2 and 4 mg) were significantly better than pentazocine, according to many parameters at 20 and 30 minutes. Side effects, chiefly sleepiness and dizziness, were seen in 15% of the patients, with no significant difference between the treatment groups.

Adolescent↗