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PubMed1994

Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain.

Scatchard analysis of saturation binding data indicated that dissociation constant (KD) of [3H]phorbol 12,13-dibutyrate (PDB) binding to the membrane-bound protein kinase C of rat cortex and midbrain was significantly decreased following systemic repeated administration of morphine (mu-opioid receptor agonist) and butorphanol (mu/delta/kappa-mixed opioid receptor agonist). No change in the receptor density (Bmax) of [3H]PDB binding was found following repeated treatment with morphine and butorphanol. On the other hand, neither the Bmax nor KD values in pons/medulla were altered in these rats. These results suggest that systemic repeated opioid treatment, such as morphine and butorphanol leads to an increased affinity for phorbol ester binding to the membrane-bound protein kinase C in rat cortex and midbrain.

Animals↗
PubMed1995

Ca2+ channel blocker, diltiazem, prevents physical dependence and the enhancement of protein kinase C activity by opioid infusion in rats.

The influence of an L-type Ca2+ channel blocker, diltiazem [(2S-cis)-3-(acetyloxy)-5-[2-(dimethylamino)-ethyl]-2,3-dihydro-2- (4- methoxyphenyl)-1,5-benzothiazepin-4(5H)-one], on the behavioral signs of naloxone (opioid receptor antagonist)-precipitated withdrawal syndrome and the enhancement of protein kinase C activity in the pons/medulla regions of rats rendered dependent on morphine (mu-opioid receptor agonist) or butorphanol (mu/delta/kappa mixed opioid receptor agonist) was investigated. The expression of physical dependence produced by continuous intracerebroventricular (i.c.v.) infusion of morphine (26 nmol/microliters per h) or butorphanol (26 nmol/microliters per h) for 3 days, as evaluated by naloxone (5 mg/kg, i.p.)-precipitated withdrawal signs, was dose dependently attenuated by concomitant infusion of diltiazem (10 and 100 nmol/microliters per h). Furthermore, diltiazem (100 nmol/microliters per h) completely inhibited the enhancement of cytosolic protein kinase C activity in the pons/medulla regions in rats rendered dependent by continuous infusion with morphine or butorphanol. These results suggest that the augmentation of intracellular Ca2+ concentration mediated through L-type Ca2+ channels during continuous opioid infusion leads to the enhancement of cytosolic protein kinase C activity in the pons/medulla region which is intimately involved in the development and/or expression of physical dependence on opioids.

Animals↗
PubMed1988

Effect of some recent analgesics on labor pain and maternal and fetal blood gases and pH.

This study attempts to determine the analgesic properties of nalbuphine, pentazocine and butorphanol during labor and their potential effects on maternal and fetal blood gases and pH. Butorphanol analgesia was superior to either nalbuphine or pentazocine in relieving labor pain. The studied analgesics caused significant maternal respiratory acidosis and fetal metabolic acidosis. These acidotic changes were most marked with pentazocine, moderate with nalbuphine and minimal with butorphanol.

Adult↗
PubMed1987

Butorphanol/diazepam compared to meperidine/diazepam for sedation in oral maxillofacial surgery: a double-blind evaluation.

Butorphanol and meperidine, each combined with titrated diazepam, 10 to 20 mg, were compared in a randomized, double-blind trial for their sedative-analgesic effects. The fifty patients underwent multiple dental extractions under local anesthesia and sedation in an outpatient clinic. Butorphanol was significantly superior to meperidine with respect to the diazepam dose required to achieve the target level of sedation, the total diazepam dose administered, the clinical level of sedation, the surgeon's overall evaluations of effectiveness and of sedation level, and several patient evaluation parameters measured at discharge from the recovery room and at follow-up interview. All study drugs were well tolerated. Butorphanol offers clinical advantages over meperidine when combined with diazepam for sedation analgesia in outpatient oral surgery.

Adolescent↗
PubMed1995

Influence of chronic opioid treatment on low Km GTPase activity in rat brain: evidence for the involvement of G-proteins in opioid tolerance.

To investigate G protein function during the initial state of opioid tolerance, low Km GTPase activity was measured following chronic treatment with morphine (mu agonist) and butorphanol (mu/delta/kappa mixed agonist) in rats. Chronic opioid administration (20 mg/kg, IP) was performed once a day for 7 consecutive days. Under these conditions, antinociceptive tolerance to morphine but not butorphanol was developed. Chronic morphine treatment enhanced basal low Km GTPase activity in the pons/medulla, but not in the cortex and midbrain. On the other hand, chronic butorphanol treatment had no effect on basal low Km GTPase activity. These results suggest that chronic in vivo treatment of rats with mu agonists leads to an increase in the hydrolysis of GTP to GDP, by a basal low Km GTPase activity of G-proteins in the pons/medulla and that an enhancement of GTPase activity in this specific area may contribute to the development of antinociceptive tolerance to mu agonists.

Animals↗
PubMed2000

A protein kinase inhibitor, H-7, blocks naloxone-precipitated changes in dopamine and its metabolites in the brains of opioid-dependent rats.

The influence of an inhibitor of cAMP-dependent protein kinase and protein kinase C, H-7 [1-(5-isoquinolinesulfonyl)-2-methylpiperazine], on naloxone (an opioid receptor antagonist)-precipitated withdrawal signs and changes in levels of dopamine (DA) and its metabolites in morphine- or butorphanol-dependent rats was investigated. Animals were infused continuously with morphine (a mu-opioid receptor agonist) or butorphanol (a mu/delta/kappa mixed opioid receptor agonist) for 3 days. Naloxone precipitated withdrawal syndrome and decreased the levels of DA in the cortex, striatum, and midbrain; 3, 4-dihydroxyphenylacetic acid (DOPAC) in the cortex, striatum, limbic areas, and midbrain; and homovanilic acid (HVA) in the striatum, limbic areas, and midbrain regions. In animals rendered dependent on butorphanol, the results obtained were similar to those of morphine-dependent rats except for the changes in DOPAC levels. Concomitant infusion of H-7 and opioid blocked both the expression of withdrawal signs and the decreases in DA, DOPAC, and HVA levels in a dose-dependent manner. These results suggest that the enhancement of cAMP-dependent protein kinase and/or protein kinase C activity accompanying the increase of DA neuron activity during continuous infusion of opioids leads to an abrupt reduction in levels of DA and its metabolites precipitated by naloxone, which is intimately involved in the expression of physical dependence on opioids.

1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine↗
PubMed1999

A new method for detoxifying opioid-dependent patients.

The purpose of the study was to investigate a new method for detoxifying opioid-dependent patients. Butorphanol is an opiod with mixed agonist-antagonist properties, and is marketed as a nasal spray. Undiluted, it will cause significant physical withdrawal symptoms in a population dependent on opioids. Forty patients dependent on opioids were detoxified using dilute butorphanol spray. The initial concentration was 40% and gradually reduced. This technique was highly successful in keeping this difficult group of patients engaged in the treatment process for a longer period. This time increased the probability of getting these patients involved with postdetoxification services. There was a subset of patients who had chronic pain and were opioid dependent, who had adequate control of pain with butorphanol spray at 10 to 20% concentration. This unique and unusual approach is worthy of open discussion and further scientific studies.

Administration, Intranasal↗
PubMed1985

Opiates and medial hypothalamic knife cuts cause hyperphagia through different mechanisms.

Several experiments were performed to determine whether the hyperphagia caused by medial hypothalamic knife cuts and that induced by opiate agonists are mediated by a common mechanism. In the first set of experiments, male Sprague-Dawley rats were given bilateral parasagittal medial hypothalamic knife cuts or a sham procedure and fed a high-fat Crisco-chow diet. Knife-cut and sham-operated rats were approximately equally sensitive to the suppressive effects of naloxone on food intake. The kappa opiate receptor agonist ketocyclazocine generally increased daytime food intake in sham-operated rats; in contrast, the normal hyperphagia of knife-cut rats was in most cases either unchanged or decreased by ketocyclazocine. In a second set of experiments, neither diet composition nor hypothalamic knife cuts significantly affected the feeding responses to naloxone or the stimulatory effects of the kappa agonist butorphanol tartrate. It was hypothesized that the differential effects of ketocyclazocine in knife-cut and sham-operated rats are a consequence of the sedative effects of the drug combined with the elevated baseline of the knife-cut subjects. This hypothesis was supported by a third experiment, in which ketocyclazocine also reduced nocturnal intake in unoperated rats and butorphanol increased intake. That feeding responses to naloxone and butorphanol were essentially unchanged by hypothalamic knife cuts suggests that the opioid feeding system is independent of the longitudinal feeding inhibitory pathway believed to be involved in knife-cut-induced hyperphagia.

Animals↗
PubMed2005

Combined dieting and stress evoke exaggerated responses to opioids in binge-eating rats.

The authors developed an animal model of binge eating where history of caloric restriction with footshock stress (R + S) causes rats to consume twice the normal amount of palatable food. The authors tested the hypothesis that binge eating is mediated by changes in opioid control of feeding by comparing rats' anorectic and orexigenic responses to naloxone and butorphanol, respectively, and by testing the ability of butorphanol to elicit binge eating of chow when palatable food was absent. Mu/kappa opioid-receptor blockade and activation had exaggerated responses in the R + S rats with naloxone suppressing binge eating to control levels, and although butorphanol did not trigger chow binge eating, it enhanced binge eating of palatable food. These responses in sated normal-weight rats strengthen evidence that reward, over metabolic need, drives binge eating.

Analgesics, Opioid↗
PubMed1998

Pale, soft, and exudative meat in turkeys treated with succinylcholine.

Rapid post-mortem metabolism concomitant with the early onset of rigor mortis can lead to the development of pale, soft, and exudative (PSE) meat. However, a reliable, nonlethal method for induction of this syndrome for the ante-mortem identification of abnormal turkeys has not been identified. The present study was conducted to evaluate the potential use of succinylcholine for inducing PSE meat in susceptible turkeys. Four-week-old Nicholas toms were either uninjected (controls) (n = 44) or injected with succinylcholine and butorphanol (n = 76) in combination. Post-mortem tissue samples were taken from the Pectoralis at 15 min, 2 h, and 4 h, for pH and R-value (the ratio of inosine to adenosine) determination. L*values were evaluated at 4 and 24 h post-mortem and drip loss and cook loss were determined. Means for pH, R-value, L*value, drip loss, and cook loss did not differ due to injection treatment. When Pectoralis were grouped as normal (L* < 53) or pale (L* > 53), pale fillets had lower pH and higher R-values than normal birds by 15 min post-mortem. Decreased water-holding properties were evident as drip loss and cook loss were increased in the pale group. The observed frequency of pale birds was 21.6% in the population, and the occurrence of pale birds was highest in the butorphanol-treated group. These findings suggest that although butorphanol did not affect overall treatment means for the test parameters, more turkeys in the treated group exhibited PSE meat.

Analgesics, Opioid↗
PubMed1995

Pharmacokinetic/dynamic assessment in drug development: application to the investigational opioid mirfentanil.

The safety, pharmacokinetics, and pharmacodynamics of the investigational partial opioid agonist, mirfentanil, were determined in a dose-escalating, Phase 1 study in healthy male volunteers. Hemodynamic, central nervous system, and respiratory monitoring were used for safety assessment. The electroencephalogram (EEG) was evaluated as a surrogate measure of drug effect. Butorphanol was chosen as the control drug. In the mirfentanil group (n = 8) the dose was increased in sequential subjects from 25 micrograms.kg-1.min-1 for 30 min to 450 micrograms.kg-1.min-1 for 15 min, and in the butorphanol group (n = 10) from 2 micrograms.kg-1.min-1 for 30 min to 25 micrograms.kg-1.min-1 for 15 min. In the mirfentanil group, serious side effects were observed at plasma concentrations more than 2000 ng/mL: heart rates exceeded 130 bpm (n = 2), epileptiform EEG potentials (n = 2), and a convulsion (n = 1). The clearance of mirfentanil was high (5.8-7.2 L/min), and the volume of distribution large (247-348 L). The EEG of the subjects receiving mirfentanil showed no changes typical for opioids. Butorphanol however, caused intermittent slowing in the delta and theta ranges. The results of our study define the upper limit of safe plasma concentrations in future mirfentanil studies.

Adult↗
PubMed1999

An examination of the interactions between the antinociceptive effects of morphine and various mu-opioids: the role of intrinsic efficacy and stimulus intensity.

UNLABELLED: We examined the effects of several opioids that vary in intrinsic efficacy at the mu-opioid receptor alone and in combination with morphine in a rat warm water tail withdrawal procedure using 50 degrees C and 52 degrees C water (i.e., low- and high-stimulus intensities). Morphine, levorphanol, dezocine, and buprenorphine produced dose-dependent increases in antinociception using both stimulus intensities. Butorphanol produced maximal levels of antinociception at the low, but not at the high, stimulus intensity, whereas nalbuphine failed to produce antinociception at either stimulus intensity. For cases in which butorphanol and nalbuphine failed to produce antinociception alone, these opioids dose-dependently antagonized the effects of morphine. When levorphanol, dezocine, and buprenorphine were combined with morphine, there was a dose-dependent enhancement of morphine's effects. Similar effects were obtained at the low-stimulus intensity when butorphanol was administered with morphine. In most cases, the effects of these combinations could be predicted by summating the effects of the drugs when administered alone. These results indicate that the level of antinociception produced by an opioid is dependent on the intrinsic efficacy of the drug and the stimulus intensity. Furthermore, the level of antinociception produced by the opioid, not necessarily the opioids' intrinsic efficacy, determines the type of interaction among opioids. IMPLICATIONS: Compared with high-efficacy opioids, lower efficacy opioids produce lower levels of pain relief, especially in situations of moderate to severe pain. When opioids are given in combination, the effects can only be predicted on the basis of the antinociception obtained when the drugs are administered alone.

Analgesics, Opioid↗
PubMed1988

Combined use of detomidine with opiates in the horse.

The effects of administration of one of four opiates (pethidine 1 mg/kg bodyweight (bwt), morphine 0.1 mg/kg bwt, methadone 0.1 mg/kg bwt, and butorphanol 0.05 mg/kg bwt) given intravenously to horses and ponies already sedated with detomidine (10 micrograms/kg bwt) were investigated. Behavioural, cardiovascular and respiratory effects of the combinations were compared with those occurring with detomidine alone. Addition of the opiate increased the apparent sedation and decreased the response of the animal to external stimuli. At doses used, butorphanol produced the most reliable response. Side effects seen were increased ataxia (greatest following methadone and butorphanol) and excitement (usually muzzle tremors and muscle twitching). Following pethidine, generalised excitement was sometimes seen. Marked cardiovascular changes occurred in the first few minutes after morphine or pethidine injection, but within 5 mins cardiovascular changes were minimal. Following morphine or pethidine there was a significant increase in arterial carbon dioxide tension. Fourteen clinical cases were successfully sedated using detomidine/butorphanol combinations.

Animals↗
PubMed1998

Site of opioid action in the human brain: mu and kappa agonists' subjective and cerebral blood flow effects.

OBJECTIVE: Humans experience the subjective effects of mu and kappa opioid agonists differently: mu agonists produce mainly euphoria, while kappa agonists are more likely to produce dysphoria. This study tested the hypothesis that these subjective effects would be associated with anatomically distinct changes in regional cerebral blood flow (CBF) relative to baseline as assessed with single photon emission computed tomography (SPECT). METHOD: Nine nondependent opioid abusers participated in the study. In the first phase of the study, the participants were acclimated to effects of the study drugs. In the second phase they underwent repeat challenges with the study drugs followed by an assessment of CBF with use of the SPECT tracer [99mTc]HMPAO. Medications tested were the prototypic mu agonist hydromorphone, the mixed agonist/antagonist butorphanol (which has a kappa agonist component of activity), and saline placebo. RESULTS: Subjective effects of the drugs were distinctly different. Hydromorphone produced increased ratings of "good effects," while butorphanol led to more "bad effects." Hydromorphone significantly increased regional CBF in the anterior cingulate cortex, both amygdalae, and the thalamus--all structures belonging to the limbic system. Butorphanol caused a less distinct picture of regional CBF increases, mainly in the area of both temporal lobes. CONCLUSIONS: This study demonstrates that opioids with different subjective effects also produce statistically significant patterns of change in regional CBF from baseline, and the regions of statistical significance appear in different brain regions. In addition, these results demonstrate the applicability of SPECT functional neuroimaging in the study of medications with potential abuse liability.

Amygdala↗
PubMed2003

Postoperative analgesia in children undergoing myringotomy and placement equalization tubes in ambulatory surgery.

UNLABELLED: We enrolled 120 children undergoing bilateral myringotomy and tube placement in this prospective, randomized, observer-blinded study. Patients were randomized into one of four groups: Group 1 (control) was plain acetaminophen 10 mg/kg orally, Group 2 was acetaminophen 10 mg/kg with 1 mg/kg of codeine orally, Group 3 was transnasal butorphanol 25 micro g/kg given immediately after the induction of anesthesia, and Group 4 was ketorolac 1 mg/kg given IM immediately after the induction of anesthesia. All children received oral midazolam (0.6 mg/kg) before surgery. A nurse blinded to the analgesic technique used assessed the child's behavior at the induction of anesthesia and in the postanesthesia care unit using a 4-point scale. Analgesic effectiveness was determined by assessing the child's pain at 5-min intervals using a modified 10-point objective pain scale. In the postanesthesia care unit, rescue pain medication was administered for an objective pain scale >or=4 or a behavior score >or=3. Our data suggest that IM ketorolac is a promising analgesic to be used in this surgical population. Time to first rescue analgesic was longest in the ketorolac group, and there was no associated postoperative vomiting or nausea. IM ketorolac given during surgery was the best analgesic regimen for these procedures. IMPLICATIONS: We compared four different analgesics in the management of pain after placement of pressure equalization tubes during myringotomy in children and demonstrated that ketorolac or butorphanol provided superior analgesia when compared with acetaminophen with codeine or plain acetaminophen. Children who received ketorolac versus butorphanol had less vomiting in the 24 h after surgery.

Acetaminophen↗
PubMed1988

[Cardiohemodynamic and respiratory effects of eptazocine, a new analgesic agent, in anesthetized dogs].

Cardiohemodynamic and respiratory effects of eptazocine, a new analgesic agent, were studied and compared with those of pentazocine and butorphanol in anesthetized dogs. Eptazocine (1 mg/kg, i.v.) increased the heart rate (HR), left ventricular dP/dt (LVdP/dt) and cardiac output (CO), and scarcely affected the blood pressure (BP), left ventricular end-diastolic pressure (LVEDP), right atrial pressure, pulmonary arterial pressure (PAP) and pulmonary capillary wedge pressure. On the other hand, eptazocine (3 mg/kg, i.v.) decreased BP, LVdP/dt, CO and LVEDP and did not influence the pulmonary circulation. Pentazocine (1 mg/kg and 3 mg/kg, i.v.) increased BP, LVdP/dt and CO, while HR was not altered. Pentazocine also increased PAP. Butorphanol (0.1 mg/kg and 0.3 mg/kg, i.v.) decreased BP, HR and LVdP/dt, while other hemodynamic parameters were not changed. In spontaneously breathing anesthetized dogs, eptazocine (1 mg/kg and 3 mg/kg, i.v.) caused a decrease of respiratory minute volume. The fall in PO2 and pH, and a rise in PCO2 were simultaneously observed in blood gas analysis. These respiratory depressant effects of eptazocine were short-lasting, and they were less potent than those of pentazocine. Butorphanol scarcely affected the respiration. These results suggest that eptazocine has different cardiohemodynamic effects than other analgesics and produces mild respiratory depression.

Analgesics↗
PubMed1998

The role of glutamate in physical dependence on opioids.

The present review will evaluate the interactions between kappa-opioid receptors and glutamate within the locus coeruleus (LC) during the development of opioid dependence and on expression of withdrawal from dependence on opioids. Hyperactivity of noradrenergic neurons in the LC has been proposed to play a critical role in the physiological and behavioral responses that comprise opioid withdrawal. Several studies indicate that the excitatory amino acid system, in particular, glutamate and its receptors, participate in both the withdrawal-associated increase in LC neuronal activity and the expression of opioid withdrawal behaviors. Most studies on opioid dependence have focused on the prototypical opioid morphine, which produces its physical dependence through agonist actions at the mu-opioid receptor. Butorphanol (Stadol), which exhibits a markedly different profile of opioid receptor activity than does morphine, produces its physical dependence primarily through actions at the kappa-opioid receptor. Studies from our laboratories using a rodent model in which butorphanol administration induces dependence indicate further that the kappa-opioid receptor is an important regulator of glutamate release within the LC. Glutamate exerts actions within the LC that mediate expression of behavioral symptoms of butorphanol withdrawal.

Analgesics, Opioid↗
PubMed2004

Evaluation of the effects of premedication on gastroduodenoscopy in cats.

OBJECTIVE: To evaluate the effects of hydromorphone, hydromorphone and glycopyrrolate, medetomidine, and butorphanol premedication on the difficulty and time required to pass an endoscope into the stomach and duodenum of cats anesthetized with ketamine and isoflurane. DESIGN: Randomized complete block crossover study. ANIMALS: 8 purpose-bred adult female cats. PROCEDURES: Each cat was premedicated and anesthetized 4 times with an interval of at least 7 days between procedures. Cats were premedicated with hydromorphone, hydromorphone and glycopyrrolate, medetomidine, or butorphanol administered IM. Twenty minutes after premedication, sedation was assessed by use of a subjective ordinal scale. Cats received ketamine administered IM, and 10 minutes later a cuffed orotracheal tube was placed and anesthesia maintained with isoflurane. Cats breathed spontaneously throughout the procedure. When end-tidal isoflurane concentration was stable at 1.4% for 15 minutes, endoscopy was begun. The times required to pass the endoscope through the cardiac and pyloric sphincters were recorded, and the difficulty of endoscope passage was scored by use of a subjective ordinal scale. RESULTS: No significant differences in difficulty or time required to pass the endoscope through the cardiac and pyloric sphincters were found among premedicant groups. Premedication with medetomidine resulted in the greatest degree of sedation and longest time to return to sternal recumbency. CONCLUSIONS AND CLINICAL RELEVANCE: Results suggest that hydromorphone, hydromorphone and glycopyrrolate, medetomidine, and butorphanol at the doses tested can be used satisfactorily to premedicate cats prior to general anesthesia for gastroduodenoscopy.

Analgesics↗