nalbuphine and Pain

The adjuvant effectiveness of nalbuphine in context of brachial plexus block (BPB) in patients undergoing upper-limb orthopaedic trauma surgery has remained uncertain. The purpose of this meta-analysis was to evaluate the analgesic benefit of mixing nalbuphine into local anaesthetics in BPB for wound pain from upper-limb trauma surgery. Primary outcome was the duration of analgesia. Seventeen trials (1104 patients) were analysed. Patients receiving nalbuphine have an increased weighted mean difference (WMD) 95% confidence interval of the duration of analgesia by 186.91 minutes (133.67 to 240.16) (P < 0.001). Compared to placebo, nalbuphine shorten the onset time of sensory and motor block by WMD of 2.59 (1.27 to 3.92) and 3.06 minutes (1.65 to 4.48) (P < 0.001), respectively. Meanwhile, nalbuphine prolonged the durations of sensory and motor block (P < 0.001). Qualitative and quantitative synthesis revealed no differences with regard to the outcomes related to side-effects. There is moderate-quality evidence that the addition of nalbuphine to local anaesthetics for BPB in patients undergoing upper-limb orthopaedic trauma surgery significantly prolongs the duration of analgesia, while preserving a similar safety-profile compared with local anaesthetics alone. However, these benefits should be further weighed against nalbuphine-related neurological safety in future studies.

Topics: Anesthetics, Local; Humans; Nalbuphine; Orthopedics; Pain; Upper Extremity

Evaluate the efficacy of prophylactic nalbuphine in preventing neuraxial opioid-induced pruritus.. Systematic review and meta-analysis.. Following the PRISMA statement, PubMed, CINAHL, Cochrane and EMBASE were searched for eligible studies.. A total of 17 trials consisting of 1,052 patients were evaluated. Compared to placebo, there is low quality of evidence that nalbuphine was effective in reducing the incidence of pruritus in all patient population (RR, 0.66; 95% CI, 0.52 to 0.83; P = .0004) and obstetrics (RR, 0.81; 95% CI, 0.67 to 0.98; P = .03). We also found moderate quality of evidence that nalbuphine lowered pruritus in non-obstetrics, the number of rescue pruritus therapy and severity of pruritus episodes. However, nalbuphine did not cause sedation and affect pain scores.. Prophylactic nalbuphine decreased the incidence and severity of pruritus without adverse effects on sedation and analgesic effect of opioids.

Topics: Analgesics, Opioid; Female; Humans; Incidence; Nalbuphine; Pain; Pregnancy; Pruritus; Randomized Controlled Trials as Topic

Parenteral potent opioid availability is becoming an issue in acute pain management. Two opioids, nalbuphine and buprenorphine, are available which can be substituted for hydromorphone, fentanyl, and morphine. There are advantages and disadvantages in using these 2 opioids which are discussed, and potential dosing strategies are outlined.

Topics: Analgesics, Opioid; Buprenorphine; Fentanyl; Humans; Hydromorphone; Morphine; Nalbuphine; Pain

Buprenorphine and the mixed agonists/antagonists nalbuphine and pentazocine, formerly classified as µ-opioid (MOP) receptor antagonists, have more recently been shown to be partial to full agonists of the human MOP receptor. These receptors do not necessarily have to be maximally activated for a full physiological response. Partial agonists can also sufficiently stimulate signaling processes leading to a full analgesic response, as shown by the effectiveness of buprenorphine, nalbuphine and pentazocine in animal pain models and in clinical settings where these drugs induce analgesia with full efficacy without a ceiling effect. Submaximal doses of MOP receptor analgesics combined with submaximal doses of buprenorphine, pentazocine, or nalbuphine result in additive to over-additive antinociceptive effects in animal experiments. Only when doses are given that exceed the therapeutic dose range may the antinociceptive effect be reduced to the effect of either opioid alone. The analgesic effects of pentazocine and nalbuphine combined with morphine are reported to be additive or over-additive in various clinical pain conditions. Buprenorphine, which clinically behaves as a full MOP receptor agonist for pain relief, can be combined with full opioid agonists without precipitating withdrawal. Thus, the overall evidence on the analgesic effects of buprenorphine, pentazocine or nalbuphine combined with opioid analgesics under various clinical pain conditions contradicts the consensus that these compounds diminish MOP receptor analgesia when co-administered with a full MOP receptor agonist.

Topics: Analgesics, Opioid; Animals; Buprenorphine; Humans; Nalbuphine; Narcotic Antagonists; Pain; Pentazocine; Receptors, Opioid

Nalbuphine is an inexpensive, non-controlled, opioid analgesic that has been in clinical use for decades. A kappa opioid receptor agonist and mu opioid receptor antagonist, nalbuphine causes fewer adverse effects than other opioid analgesics. The author reviews the characteristics of nalbuphine, analyzes studies of nalbuphine in mice and explores the potential use of nalbuphine to treat pain in research mice. In analgesiometric studies in mice, nalbuphine ameliorates both somatic and visceral pain. Nalbuphine seems to have a broad range of safe doses for subcutaneous administration in mice. Unlike non-steroidal anti-inflammatory drugs, nalbuphine does not antagonize prostaglandins or impede labor in mice. Although additional study is needed before clinical use can be recommended, evidence presented here suggests that nalbuphine might be an effective analgesic for dystocia (or difficult birth) and other painful conditions in research mice.

Topics: Analgesics, Opioid; Animals; Dystocia; Female; Male; Mice; Nalbuphine; Pain; Pregnancy; Receptors, Opioid, kappa

The aim of this study was to examine the effectiveness and safety of prehospital analgesia with nalbuphine and/or paracetamol by paramedics.. In this retrospective trial, following the implementation of a standard-operating-procedure for pain requiring treatment as defined as a score ≥4 on the 0-10 Numeric Rating Scale for pain, all emergency operations in the district of Gütersloh between January 1, 2020, and June 30, 2022, with analgesic administration by paramedics in patients ≥18 years were included in the study. Analgesic agents employed by the paramedics included nalbuphine and/or paracetamol, butylscopolamine for abdominal colic, and esketamine in case of failure of the other analgesics. The primary endpoint was the patients' rating of their pain on the Numeric Rating Scale at the end of the operation. Additional covariates included sex, cause of pain, analgesics used, Numeric Rating Scale at beginning and analgesic-associated complications (reduced level of consciousness, hypotension, desaturation, a- or bradypnea).. A total of 1931 emergency operations (female: N.=1039 [53.8%]) with pain requiring treatment (non-traumatic cause: N.=1106 [57.3%]; initial Numeric Rating Scale: 8.0±1.4). Analgesics applied were nalbuphine + paracetamol (50.6%), paracetamol (38.7%), butylscopolamine (13.4%), nalbuphine (7.7%), and esketamine (4.9%). Mean pain reduction was 4.3±2.3 (nalbuphine + paracetamol: 5.0±2.1; nalbuphine: 4.7±2.3) and paracetamol: 3.3±2.2, respectively. Factors influencing a change in the Numeric Rating Scale were trauma (regression-coefficient: -0.308, 95% CI: -0.496 - -0.119, P=0.0014 vs. non-trauma; nalbuphine [yes vs. no]: regression-coefficient 0.684, 95% CI 0.0774-1.291, P=0.03; nalbuphine + paracetamol: regression-coefficient 0.763, 95% CI 0.227-1.299, P=0.005). At the end of the operation, 49.7% had a Numeric Rating Scale <4, 34.3% had a Numeric Rating Scale 4-5, and 16.0% had a Numeric Rating Scale ≥6. Factors influencing a Numeric Rating Scale <4 at end of use were trauma vs. non-trauma: odds ratio 0.788, 95% CI 0.649-0.957, P=0.02. The Numeric Rating Scale at beginning reported: odds ratios 0.754, 95% CI 0.700-0.812, P<0.0001. Analgesic-associated complications were not observed.. Prehospital analgesia by paramedics with nalbuphine as monotherapy or in combination with paracetamol allows for sufficient analgesia without the occurrence of complications.

Topics: Acetaminophen; Adolescent; Adult; Analgesia; Analgesics; Butylscopolammonium Bromide; Emergency Medical Services; Female; Humans; Male; Nalbuphine; Pain; Paramedics; Retrospective Studies

Mice undergo a variety of procedures that necessitate the use of analgesic agents. Opioids are often essential to successful pain management plans, but most are controlled substances, and their use requires appropriate federal and state registrations. Nalbuphine is a potentially effective opioid analgesic for mice that is not currently classified as a controlled substance. This compound has received little attention as an analgesic for mice, and standard dosage regimens have not been developed. Here we compared the pharmacokinetic profiles of 10 mg/kg nalbuphine in male C57BL/6 mice subcutaneous or intraperitoneal administration. Blood was collected from 3 mice per treatment at 5, 10, 20, and 30 min and 1, 2, 3, 6, 12, and 24 h after administration. Plasma concentrations were measured, and standard pharmacokinetic parameters were calculated. Profile characteristics for each route of administration were similar, with significant differences in plasma concentration at 5 and 30 min and 1 and 3 h. Nalbuphine was absorbed more quickly when administered subcutaneously (Tmax, 5 min) than intraperitoneally (Tmax, 10 min), whereas the drug's half-life was similar between the intraperitoneal (0.94 h) and subcutaneous (1.12 h) routes. The AUC0-tldc and AUC0-inf were higher but the apparent clearance and apparent volume of distribution were lower after subcutaneous administration compared with intraperitoneal dosing. Plasma concentrations were below the level of detection by 12 h. These results suggest that nalbuphine is absorbed in and eliminated quickly from mice, making it a possible candidate for acute pain management.

Topics: Analgesics, Opioid; Animals; Animals, Laboratory; Half-Life; Humans; Injections, Intraperitoneal; Injections, Subcutaneous; Male; Mice; Mice, Inbred C57BL; Nalbuphine; Pain

Nalbuphine, an agonist-antagonist kappa-opioid, produces brief analgesia followed by enhanced pain/hyperalgesia in male postsurgical patients. However, it produces profound analgesia without pain enhancement when co-administration with low dose naloxone. To examine the effect of nalbuphine or nalbuphine plus naloxone on activity in brain regions that may explain these differences, we employed pharmacological magnetic resonance imaging (phMRI) in a double blind cross-over study with 13 healthy male volunteers. In separate imaging sessions subjects were administered nalbuphine (5 mg/70 kg) preceded by either saline (Sal-Nalb) or naloxone 0.4 mg (Nalox-Nalb). Blood oxygen level-dependent (BOLD) activation maps followed by contrast and connectivity analyses revealed marked differences. Sal-Nalb produced significantly increased activity in 60 brain regions and decreased activity in 9; in contrast, Nalox-Nalb activated only 14 regions and deactivated only 3. Nalbuphine, like morphine in a previous study, attenuated activity in the inferior orbital cortex, and, like noxious stimulation, increased activity in temporal cortex, insula, pulvinar, caudate, and pons. Co-administration/pretreatment of naloxone selectively blocked activity in pulvinar, pons and posterior insula. Nalbuphine induced functional connectivity between caudate and regions in the frontal, occipital, temporal, insular, middle cingulate cortices, and putamen; naloxone co-admistration reduced all connectivity to non-significant levels, and, like phMRI measures of morphine, increased activation in other areas (e.g., putamen). Naloxone pretreatment to nalbuphine produced changes in brain activity possess characteristics of both analgesia and algesia; naloxone selectively blocks activity in areas associated with algesia. Given these findings, we suggest that nalbuphine interacts with a pain salience system, which can modulate perceived pain intensity.

Topics: Brain; Brain Mapping; Humans; Infusions, Intravenous; Magnetic Resonance Imaging; Male; Nalbuphine; Naloxone; Nerve Net; Organ Specificity; Oxygen; Pain; Psychophysics; Young Adult

To evaluate the antinociceptive effects and duration of action of nalbuphine HCl administered IM on thermal thresholds in Hispaniolan Amazon parrots (Amazona ventralis).. 14 healthy adult Hispaniolan Amazon parrots of unknown sex.. 3 doses of nalbuphine (12.5, 25, and 50 mg/kg, IM) and saline (0.9% NaCl) solution (control treatment) were evaluated in a blinded complete crossover experimental design by use of foot withdrawal threshold to a noxious thermal stimulus. Baseline data on thermal threshold were generated 1 hour before administration of nalbuphine or saline solution; thermal threshold measurements were obtained 0.5, 1.5, 3, and 6 hours after administration.. Nalbuphine administered IM at 12.5 mg/kg significantly increased the thermal threshold (mean change, 2.4°C), compared with results for the control treatment, and significantly changed thermal threshold for up to 3 hours, compared with baseline results (mean change, 2.6° to 3.8°C). Higher doses of nalbuphine did not significantly change thermal thresholds, compared with results for the control treatment, but had a significant effect, compared with baseline results, for up to 3 and 1.5 hours after administration, respectively.. Nalbuphine administered IM at 12.5 mg/kg significantly increased the foot withdrawal threshold to a thermal noxious stimulus in Hispaniolan Amazon parrots. Higher doses of nalbuphine did not result in significantly increased thermal thresholds or a longer duration of action and would be expected to result in less analgesic effect than lower doses. Further studies are needed to fully evaluate the analgesic effects of nalbuphine in psittacine species.

Topics: Analgesics, Opioid; Animals; Cross-Over Studies; Dose-Response Relationship, Drug; Nalbuphine; Pain; Pain Measurement; Parrots

To assess the pharmacokinetics of nalbuphine HCl after IV and IM administration to Hispaniolan Amazon parrots (Amazona ventralis).. 8 healthy adult Hispaniolan Amazon parrots of unknown sex.. Nalbuphine HCl (12.5 mg/kg) was administered IV and IM to all birds in a complete randomized crossover study design; there was a washout period of 21 days between subsequent administrations. Plasma samples were obtained from blood collected at predetermined time points for measurement of nalbuphine concentration by use of liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters were estimated by use of computer software.. Nalbuphine was rapidly eliminated with a terminal half-life of 0.33 hours and clearance of 69.95 mL/min/kg after IV administration and a half-life of 0.35 hours after IM administration. Volume of distribution was 2.01 L/kg after IV administration. The fraction of the dose absorbed was high (1.03) after IM administration. No adverse effects were detected in the parrots during the study.. In Hispaniolan Amazon parrots, nalbuphine appeared to have good bioavailability after IM administration and was rapidly cleared after IV and IM administration. Safety and analgesic efficacy of various nalbuphine treatment regimens in this species require further investigation to determine the potential for clinical palliation of signs of pain in psittacine species.

Topics: Analgesics, Opioid; Animals; Area Under Curve; Bird Diseases; Cross-Over Studies; Dose-Response Relationship, Drug; Half-Life; Injections, Intramuscular; Injections, Intravenous; Nalbuphine; Pain; Parrots

To determine if the intravenous co-administration of equal volumes of lidocaine and nalbuphine, with undiluted normal saline, prevents injection pain caused by nalbuphine.. Eighty adult patients who were scheduled for minor surgeries under general anesthesia delivered via a laryngeal mask airway (LMA) were enrolled in this prospective, randomized, single-blind clinical trial. In the saline group (control) (n = 40), 1 mL (10 mg) nalbuphine was diluted with 9 mL normal saline. In the lidocaine group (experimental) (n = 40), 1 mL (10 mg) nalbuphine was diluted with 1 mL lidocaine (20 mg). The two respective nalbuphine solutions were injected into the cephalic vein at a rate of 20 mL/minute (0.33 mL/second). Pain scores were categorized into five grades. Pain responses upon intravenous injection of nalbuphine, site of cannulation, size of the catheter, and hemodynamic responses to nalbuphine were also recorded.. Overall, the median pain score of patients in the lidocaine group was lower than that of the saline group (p < 0.001). In addition, the incidence of injection pain was lower in the lidocaine group than the saline group (2.5% vs. 30%, p = 0.001).. A solution of equal volumes of lidocaine and nalbuphine can decrease intravenous nalbuphine-induced injection pain.

Topics: Adult; Female; Humans; Hydrogen-Ion Concentration; Injections, Intravenous; Lidocaine; Male; Middle Aged; Nalbuphine; Pain; Prospective Studies; Single-Blind Method

In patients with common atrial flutter (CAF), radiofrequency ablation (RFA) causes discomfort. Patients undergoing RFA often feel pain which is difficult to control as the mechanisms are unclear.. Inhaled nitrous oxide (N2O) is a potent sedative-analgesic-anxiolytic agent that may relieve anxiety and discomfort during CAF ablation.. In a prospective randomized study, the effect of Inhaled N2O was compared with that of intravenous sedation with Nalbuphine during CAF ablation in 76 patients (64 +/- 13 years, 56 men). We used a 24 pole mapping catheter around the tricuspid annulus and a 8-mm tip ablation catheter for each patient. Forty-two patients (group 1) underwent radiofrequency (RF) application to the cavotricuspid isthmus 5 minutes after the beginning of inhalation of a (50% N2O/50% O2) mixture. Thirty-four patients (group 2), underwent the first RF application 15 minutes after the end of an infusion of Nalbuphine (20 mg delivered over 15 minutes). Ablation-related anxiety and discomfort were assessed using a visual analog scale (VAS) ranging from 0 to 100 mm, with 0 correlating to the statement "no pain at all" and 100 with "the worst possible pain." The VAS score was determined at the end of each application. The number of RF applications (group 1; 10 +/- 8 vs group 2; 11 +/- 6, P = NS) and procedure duration (group 1; 75 +/- 53 minutes vs group 2; 72 +/- 45 minutes, P = NS), were similar for the two groups. N(2)O sedation compared with nalbuphine infusion reduced VAS for anxiety (10 mm +/- 8 vs 58 mm +/- 22, P < 0.05) and for discomfort (18 mm +/- 9 vs 45 mm +/- 34, P < 0.01), respectively. Although there was more frequent vomiting in group 1; 7 of 42 (17%) than in group 2; 3 of 34 (9%), P < 0.05, patients were less likely to have hypotension during the procedure 1 of 42 (2.5%) versus 4 of 34 (12%), P < 0.05, respectively.. Inhalation of a (50% N2O/50% O2) mixture during RF ablation for atrial flutter is a safe and efficient way to reduce anxiety and discomfort caused by RF applications.

Topics: Administration, Inhalation; Analgesics, Opioid; Anesthetics, Inhalation; Anxiety; Atrial Flutter; Catheter Ablation; Conscious Sedation; Drug Combinations; Female; Humans; Infusions, Intravenous; Male; Middle Aged; Nalbuphine; Nitrous Oxide; Pain; Treatment Outcome

To examine the effects of meperidine and nalbuphine on intrapartum fetal heart rate (FHR) tracings using computer analysis.. We studied 28 women with uncomplicated pregnancies in early labor at term with reactive FHR tracings. The women were randomized to receive either meperidine 50 mg or nalbuphine 10 mg intravenously on request. One-hour FHR recordings were obtained before and immediately after administration of the medications.. There were no significant differences in the FHR characteristics of the two groups during the pre-treatment period. Nalbuphine significantly decreased the number of accelerations of 10 beats per minute (17 versus 4, P = .003) and 15 beats per minute (10 versus 1.5, P = .001), time spent in episodes of high variation (35.5 versus 10 minutes, P = .004), long-term variation (47 versus 29.8 milliseconds, P = .002), and short-term variation (8.4 versus 6.4 milliseconds, P = .03). Meperidine had no significant effect on any FHR characteristic.. In the early intrapartum period of normal term pregnancies and at commonly used dosages, nalbuphine had a significant effect on FHR tracings, whereas meperidine had no effect, as determined by computer analysis.

Topics: Adolescent; Adult; Cardiotocography; Female; Heart Rate, Fetal; Humans; Infusions, Intravenous; Meperidine; Nalbuphine; Obstetric Labor Complications; Pain; Pregnancy; Prospective Studies; Signal Processing, Computer-Assisted

A randomized, placebo-controlled, double-blind study was conducted on 66 healthy patients aged 10-61 years undergoing elective ear, nose and throat surgery to assess the incidence and severity of pain associated with intravenous (i.v.) injection of diluted nalbuphine HCl given during induction of general anaesthesia, and to determine the efficacy of adding lignocaine (2 mg mL-1) to nalbuphine to reduce this pain. Injection of saline produced pain of low intensity in 15% of patients and a withdrawal response in 3% of patients. Injection of nalbuphine mixed with lignocaine produced a significantly higher incidence (36%; P < 0.025) and severity (P < 0.025) of pain than saline, but a similar number of responses (6%) to pain. The diluted nalbuphine alone produced the highest incidence (61%) of pain (P < 0.01 vs. saline, P = NS vs. nalbuphine with lignocaine), which was most severe (P < 0.01 vs. saline, P < 0.025 vs. nalbuphine with lignocaine), and caused the highest number (27%) of withdrawal responses (P < 0.01 vs. saline, P < 0.025 vs. nalbuphine with lignocaine). We conclude that diluted nalbuphine 2 mg mL-1 produces pain on i.v. injection into peripheral veins, and that this can be significantly reduced by adding lignocaine 2 mg mL-1 to the solution.

Topics: Adolescent; Adult; Analgesics, Opioid; Anesthetics, Local; Child; Double-Blind Method; Drug Combinations; Female; Humans; Injections, Intravenous; Lidocaine; Lidocaine, Prilocaine Drug Combination; Male; Middle Aged; Nalbuphine; Pain; Prilocaine

Adult patients who had arthroscopic surgery under general anesthesia and requested postoperative pain relief were randomized to receive treatment in a double-blind protocol with 5 mg of intravenous dezocine (20 patients), morphine (22 patients), nalbuphine (18 patients), or saline (24 patients). At 10-min intervals, starting with the first dose of analgesic, patients could choose up to three additional doses of the primary treatment, or choose an alternative analgesic if the primary drug was unsatisfactory. One to four doses of morphine were given as the alternate treatment if the initial treatment was dezocine or nalbuphine, and one to four doses of dezocine were given if the initial treatment was saline or morphine. The proportion of patients treated successfully by the initial treatments (i.e., not requesting alternate treatment), with P value for difference from placebo treatment, were saline 25%, nalbuphine 33% (P = 0.048), morphine 54% (P = 0.04), and dezocine 75% (P = 0.003). Dezocine and morphine are more efficacious than nalbuphine in the management of early postoperative pain. As an alternate analgesic in this study, dezocine required fewer doses to achieve patient satisfaction and was thus more efficacious than morphine. The incidence of treatment-related, adverse effects was different from that of saline or other treatments only for nalbuphine-related pain or burning on injection and dezocine-related facial itching. With respect to analgesic actions and side effects, dezocine seems more like morphine than nalbuphine.

Topics: Adult; Aged; Ambulatory Surgical Procedures; Analgesics; Bridged Bicyclo Compounds, Heterocyclic; Cycloparaffins; Female; Humans; Male; Middle Aged; Morphine; Nalbuphine; Pain; Postoperative Period; Prospective Studies; Tetrahydronaphthalenes

Nalbuphine and meperidine were compared as analgesic components of intravenous conscious sedation in a double-blind, prospective trial of 47 patients undergoing elective oral surgery. Subjects were evaluated for pain intensity, pain relief, anxiety, sedation, recall, and vital signs at systematic observation points intraoperatively and postoperatively. At the conclusion of surgery 83% of patients who had received nalbuphine and 86% of patients treated with meperidine indicated complete pain relief. One observed adverse reaction was attributed to meperidine and another to the sedative component diazepam. No statistically significant differences were observed between nalbuphine and meperidine treatments.

Topics: Adult; Anesthesia, Dental; Anesthesia, Local; Anxiety; Diazepam; Double-Blind Method; Female; Humans; Infusions, Intravenous; Male; Meperidine; Middle Aged; Morphinans; Nalbuphine; Pain; Preanesthetic Medication

The narcotic agonist-antagonist nalbuphine is reported to act as a strong analgesic with only minor respiratory depressant side-effects. Even in the postoperative period, the pain-relieving properties of analgesic drugs are reported to continue if the respiratory side-effects are being antagonized by administering nalbuphine. It was the aim of this study to investigate the analgesic properties of nalbuphine as compared to those of fentanyl, in suppressing the hemodynamic responses due to endotracheal intubation and skin incision. Furthermore, we are interested in studying postoperative analgesia and respiratory depression after using the two drugs during anesthesia.. Forty-one patients undergoing general surgical procedures were randomly assigned to two groups in a double-blind study. The patients were between 18 and 70 years old and belonged to ASA classes I-III. Patients with chronic obstructive pulmonary disease, cerebral vascular disorders, hepatic or renal failure, or those treated with monoamine oxidase inhibitors and tricyclic antidepressants were excluded from the study, as were patients with a drug dependency. All patients were premedicated with 25-50 mg each promethazine and pethidine. Anesthesia was induced with either 60-70 mg nalbuphine or 0.3-0.35 mg fentanyl, 2 mg alcuronium, 0.01 mg/kg flunitrazepam, and 1-2 mg/kg thiopental. All patients were intubated following 1-2 mg/kg succinylcholine. Five minutes following intubation they received another 30-40 mg nalbuphine or 0.15-0.2 mg fentanyl intravenously. Anesthesia was maintained with N2O:O2 2:1, alcuronium, and either nalbuphine or fentanyl and enflurane up to 1 vol.% or halothane up to 0.5 vol.%. Blood pressure, pulse rate, and arterial blood gases were measured at certain intervals.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Adolescent; Adult; Anesthesia, Endotracheal; Blood Pressure; Clinical Trials as Topic; Cognition; Double-Blind Method; Fentanyl; Heart Rate; Hemodynamics; Humans; Middle Aged; Morphinans; Nalbuphine; Pain; Postoperative Period; Respiration

Perioperative pain in children is often inadequately treated, and emergence agitation is common. The purpose of this analysis was to determine whether nalbuphine is suitable for perioperative eye pain and to analyse if it influences the occurrence of emergence delirium/agitation (EDA) in children undergoing ophthalmic surgery in general anaesthesia.. Retrospective cohort analysis of 50 children in preschool age undergoing general anaesthesia for ophthalmic surgery receiving nalbuphine as a postoperative analgesic in a German university hospital from June 2020 to February 2021.Scores and values for pain and EDA were routinely recorded after awakening and during the stay in the recovery room. Data were evaluated retrospectively from the medical records.. Nalbuphine shows a sufficient analgesic effect for pain therapy following ophthalmic surgery in preschool children. Nalbuphine seems to reduce the incidence of EDA in children undergoing ophthalmic surgery.

Topics: Analgesics; Child; Child, Preschool; Emergence Delirium; Female; Humans; Infant; Male; Nalbuphine; Pain; Retrospective Studies

Various approaches using epidural analgesia have been employed for relieving labor pain and promoting spontaneous delivery. We aimed to evaluate the effect of nalbuphine and ropivacaine versus fentanyl and ropivacaine on the duration of delivery in parturients.. Clinical data of 160 full-term primiparous women who received either nalbuphine or fentanyl in combination with ropivacaine infusion for epidural labor analgesia in our hospital from December 2020 to May 2022 were retrospectively analyzed. The participants were divided into two groups based on anesthesia methods: nalbuphine group (NR group, n = 78) received 0.2 mg/mL nalbuphine combined with 0.1% ropivacaine hydrochloride for patient-controlled epidural analgesia (PCEA) and fentanyl group (FR group, n = 82) received 2 ug/mL fentanyl citrate and 0.1% ropivacaine hydrochloride for PCEA. Both groups received an epidural blockade for labor analgesia at lumbar 2-3 interspace. The duration of the first, second, and third stages of labor, the onset of analgesia, and time before delivery (T0), 15 min of analgesia (T1), 30 min of analgesia (T2), full opening of the uterine opening (T3),exerts force during childbirth(T4), heart rate (HR), blood pressure (BP), blood saturation (SpO2), visual analogue pain scale (VAS) score, Ramsay sedation score, and modified Bromage score, and 5 min were recorded at 2 h postpartum (T5). The neonatal Apgar score, neonatal behavioral neurological assessment (NBNA) score, maternal nausea, vomiting, and itchy skin were recorded.. Compared with the FR group, the first stage of labor duration (p < 0.05) and total duration of labor (p < 0.05) were shortened and the onset of analgesia (p < 0.05) was increased in the NR group. NR group had lower incidence of urinary retention than FR group (p < 0.05). The maternal and neonatal investigational parameters and scores had no significant difference between the two groups.. Nalbuphine combined with ropivacaine in epidural block labor has a faster onset of analgesia and has a lower incidence of urinary retention than fentanyl combined with ropivacaine, and nalbuphine shortens the duration of the first and total stages of labor. Both nalbuphine and fentanyl can reduce pain during labor, have little effect on maternal hemodynamics, and have no significant effect on neonatal Apgar or NBNA scores.

Topics: Analgesia, Epidural; Female; Fentanyl; Humans; Infant, Newborn; Nalbuphine; Pain; Pregnancy; Retrospective Studies; Ropivacaine; Urinary Retention

Developing non-addictive and safer opioids for pain management is unmet medical need. Among a number of bioreversible derivatives of Nalbuphine - an equipotent to morphine opioid without serious side effects - NB-33 was identified in silico and confirmed in vivo as a superior analgesic agent. Apart from enhanced pharmacodynamics profile, NB-33 outperformed the parent compound on equimolar bases in cold ethanol tail-flick and mechanical models of pain in rats. With no β-arrestin engagement liability, good stability in simulated gastro-intestinal fluid and slow release of Nalbuphine by plasma NB-33 is being developed as an oral and safer alternative of its parent drug.

Topics: Analgesics; Analgesics, Opioid; Animals; Morphine; Nalbuphine; Pain; Rats

Pain is a noxious stimulus caused due to tissue damage and varies from mild to severe. Nalbuphine (NLB) is an approved, inexpensive, non-controlled, opioid agonist/antagonist analgesic used worldwide in various clinical settings for pain management. The current study aims to formulate NLB loaded solid lipid nanoparticles (SLNs) using solvent injection technology. The morphological and chemical structure of the developed SLNs were characterized using Field Emission Scanning Electron Microscopy (FESEM), Transmission Electron Microscopy (TEM) and Fourier Transformation Infrared Spectroscopy (FTIR). The results revealed from the point prediction confirmation in design expert software was the formulation of NLB-SLNs with an average particle size of (170.07 ± 25.1 nm), encapsulation efficiency (93.6 ± 1.5%) & loading capacity of 26.67%. The in-vitro permeation of developed NLB-SLNs was observed to be 94.18% at 8 h when compared with NLB solution whose maximum permeation was seen within 3 h of application. Efficacy of the formulation was also evaluated using eddy's hot plate method, where the onset of action started within 10 min of administration, and the maximum effect was observed at 1 h. The NLB-SLNs was screened for cytotoxicity in human embryonic kidney cells (HEK-293), and the dosage was considered safe when administered intranasally in animal since no detectable effect to the brain was observed. Biodistribution and gamma scintigraphy study of NLB-SLNs showed the prepared formulation reaching the target site, i.e. brain and was retained. Conclusively, the prepared NLB-SLNs formulation was safe and effective in producing an analgesic effect in vivo.

Topics: Analgesics, Opioid; Animals; Drug Carriers; Drug Delivery Systems; HEK293 Cells; Humans; Lipids; Nalbuphine; Nanoparticles; Pain; Pain Management; Particle Size; Rats; Rats, Sprague-Dawley; Surface Properties

Pain is one of the major symptoms complained about by patients in the prehospital setting, especially in the case of trauma. When there is mountainous topography, as in Switzerland, there may be a time delay between injury and arrival of professional rescuers, in particular on ski slopes. Administration of a safe opioid by first responders may improve overall treatment. We therefore assessed administration of nasal nalbuphine as an analgesic treatment for trauma patients in Switzerland.. This observational cohort study examined 267 patients who were treated with nasal nalbuphine by first responders in six ski resorts in Switzerland. All first responders were instructed to begin treatment by assessing the feasibility of using nalbuphine to treat pain in the patient. A treatment algorithm was developed and distributed to assure that nalbuphine was only administered following a strict protocol. Data regarding pain scores and pain reduction after administration of nalbuphine were collected on-site. Refills were handed out to the first responders with the return of each completed questionnaire.. Nalbuphine provided effective pain relief, with the median level of pain on the numeric rating scale for pain reduced by 3 units on average, from 8 points (p < 0.001). The multivariate regression model showed that pain reduction was more pronounced in patients with higher initial pain levels. Nalbuphine was more effective in adolsecents than in patients aged 20 to 60 years (p = 0.006). No major side effects were observed.. Nasal administration of nalbuphine by first responders is a presumably safe and effective noninvasive pain management strategy for acutely injured patients in the prehospital setting. This may be an alternative, especially in the case of severe pain and prolonged time between arrival of the first responders and arrival of EMS/HEMS personnel on scene.

Topics: Aged; Analgesics, Opioid; Cohort Studies; Emergency Medical Services; Emergency Responders; Female; Humans; Male; Middle Aged; Nalbuphine; Pain; Prospective Studies; Skiing; Switzerland; Wounds and Injuries

Nalbuphine, a partial agonist/antagonist opioid analgesic, is structurally related to morphine. It is equipotent to morphine and has no serious side effects. In the past few decades, studies focusing on morphine metabolism have indicated that one of its sugar-conjugated metabolites, morphine-6-glucuronide, exerts a higher analgesic effect than its parent drug. Considering that nalbuphine is a morphine analog that follows a similar metabolic scheme, nalbuphine glucuronides were synthesized in this study and their potential analgesic effects were assessed. Nalbuphine-3-glucuronide (N3G) and nalbuphine-6-glucuronide (N6G) were synthesized based on Schmidt's glycosylation with OPiv protections on the glycosyl donor. In a pharmacodynamic study, paw pressure and cold-ethanol tail-flick tests were conducted in rats to evaluate the analgesic response after intracisternal and intraperitoneal administrations of nalbuphine, N3G, or N6G. The antinociceptive response was evaluated for each compound by calculating the area under the curve and the duration spent at greater than 50% maximum possible analgesia. In conclusion, intracisternal administration of N6G exhibited a stronger analgesic response than nalbuphine in the pain tests after both cold and mechanical stimuli, but N3G had no obvious effect. Similar to that of morphine, the glucuronide metabolite of nalbuphine at the 6-O-position exerted at least three-fold higher antinociceptive potency and five-fold longer analgesic duration than nalbuphine.

Topics: Analgesics, Opioid; Animals; Dose-Response Relationship, Drug; Glucuronides; Male; Molecular Structure; Pain; Pain Measurement; Pain Threshold; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

μ-Opioid agonists are clinically effective analgesics, but also produce undesirable effects such as sedation and abuse potential that limit their clinical utility. Glutamatergic systems also modulate nociception and N-methyl D-aspartate (NMDA) receptor antagonists have been proposed as one useful adjunct to enhance the therapeutic effects and/or attenuate the undesirable effects of μ-opioid agonists. Whether NMDA antagonists enhance the antiallodynic effects of μ-agonists in preclinical models of thermal hypersensitivity (i.e. capsaicin-induced thermal allodynia) are unknown. The present study determined the behavioral effects of racemic ketamine, (+)-MK-801, (-)-nalbuphine, and (-)-oxycodone alone and in fixed proportion mixtures in assays of capsaicin-induced thermal allodynia and schedule-controlled responding in rhesus monkeys. Ketamine, nalbuphine, and oxycodone produced dose-dependent antiallodynia. MK-801 was inactive up to doses that produced undesirable effects. Ketamine, but not MK-801, enhanced the potency of μ-agonists to decrease rates of operant responding. Ketamine and nalbuphine interactions were additive in both procedures. Ketamine and oxycodone interactions were additive or subadditive depending on the mixture. Furthermore, oxycodone and MK-801 interactions were subadditive on antiallodynia and additive on rate suppression. These results do not support the broad clinical utility of NMDA receptor antagonists as adjuncts to μ-opioid agonists for thermal allodynic pain states.

Topics: Analgesics; Analgesics, Opioid; Animals; Conditioning, Operant; Dizocilpine Maleate; Dose-Response Relationship, Drug; Hyperalgesia; Ketamine; Macaca mulatta; Male; Nalbuphine; Oxycodone; Pain; Pain Measurement; Receptors, N-Methyl-D-Aspartate; Receptors, Opioid, mu; Reinforcement Schedule

To analyze the efficacy and safety of nalbuphine in patients with sedative analgesia in intensive care unit (ICU).. A prospective observation was conducted. The adult patients with mild and moderate analgesia in general ICU of the First Affiliated Hospital of Zhengzhou University from January to November in 2017 were enrolled, and they were divided into nalbuphine group and sufentanil group in proper order. The nabobrown group was given 40 mg nabobrown, the sufentanil group was given 0.1 mg sufentanil, both of which were injected with 50 mL normal saline for continuous intravenous infusion in micro-pump. Infusion speed was checked according to pain level. The analgesic target was critical-care pain observation tool (CPOT) score < 2. The change in hemodynamics of patients in both groups were observed, and CPOT score and Richmond agitation-sedation scale (RASS) score were recorded before and l, 3, 5, 12, 24 hours after administration. The analgesic and sedative effects of two drugs were evaluated.. A total of 141 patients were enrolled, including 71 patients in nalbuphine group and 70 in sufentanil group. There was no significant difference in general data including gender, age, body weight, acute physiology and chronic health evaluation II (APACHE II) or pain source, as well as baseline hemodynamics parameter between the two groups. At 1 hour and 3 hours after administration, nalbuphine had no effect on blood pressure, but the heart rate was decreased slightly, while the heart rate and blood pressure of the sufentanil group were decreased obviously. The two drugs could make the heart rate and blood pressure fluctuate obviously with the time of medication, but there was no statistical difference between the two drugs. The two drugs had no significant effect on pulse oxygen saturation (SpO. Naporphine had a sustained and stable analgesic effect on patients with mild and moderate ICU analgesia. The onset time of naporphine was equivalent to sufentanil, and it had a certain sedative effect and less influence on hemodynamics.

Topics: Analgesia; Humans; Intensive Care Units; Nalbuphine; Pain; Prospective Studies; Sufentanil

The most common manifestation of sickle cell disease (SCD) is painful vaso-occlusive episodes (PVOE), and inappropriate treatment leads to unnecessary suffering and potentially fatal complications. This study describes how French paediatric emergency departments (EDs) manage PVOE and their knowledge, and implementation of the French National Authority for Health recommendations on the management of sickle cell patients.. A questionnaire on managing PVOE was sent to all the 111 French paediatric EDs.. We received responses from 81 (72.9%) of the EDs. Of those who responded to each individual question, 85% said that they had read the national recommendations, 71.6% said they used nalbuphine for moderate PVOE, and 85% used intravenous morphine for severe PVOE. The majority (91.7%) of EDs thought that intravenous morphine provided relief for severe PVOE, but only 30.9% thought that intravenous nalbuphine did. A 50:50 nitrous oxide/oxygen mix was used by 71.3% of departments to relieve procedural pain and by 48% to enhance analgesia when morphine was insufficient for severe pain.. Most French EDs follow the national recommendations for PVOE. Nalbuphine was the most commonly used opioid for moderate PVOE and morphine for severe PVOE. A nitrous oxide/oxygen mixture was widely used for PVOE.

Topics: Adolescent; Analgesics; Anemia, Sickle Cell; Child; Emergency Service, Hospital; France; Guideline Adherence; Humans; Morphine; Nalbuphine; Nitrous Oxide; Pain; Practice Patterns, Physicians'; Surveys and Questionnaires

Anti-nociceptive and anti-inflammatory effects of methanolic extract of Wrightia arborea (MEWA) were examined using different models in rats. MEWA was given to rats orally upto 2000 mg kg(-1) b.wt. for acute toxicity study and observed for 14 days. Anti-nociceptive activity was evaluated in rats against Acetic acid induced writhing (chemically induced pain) and Tail immersion method (thermally induced pain). Acute anti-inflammatory activity of MEWA was also evaluated in Formaline-induced rat paw edema model and Carrageenan-induced hind paw edema model in rats. Results demonstrated that no mortality was found upto single dose of 2000 mg kg(-1) b.wt. in rats even after 14 days observation. In comparison to control group MEWA at 100 and 200 mg kg(-1) b.wt. showed highly significant anti-nociceptive activity against chemically (p < 0.001) as well as thermally (p < 0.05 and p < 0.001) induced pain as compared to standard drugs, indomethacin and nalbufin, respectively. In the formalin test, both the doses of 100 and 200 mg kg(-1) of extract significantly prevented increase in volume of paw edema (p < 0.05 and p < 0.01) both in the neurogenic and inflammatory phases. MEWA (200 and 400 mg kg(-1) p.o.) also significantly prevented increase in volume of paw edema in Carrageenan test (p < 0.05 and p < 0.001). The results suggest that MEWA has significant analgesic and anti-inflammatory potential which may be mediated by central and peripheral mechanism.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Apocynaceae; Disease Models, Animal; Edema; Female; Indomethacin; Inflammation; Male; Methanol; Nalbuphine; Pain; Phytotherapy; Plant Components, Aerial; Plants, Medicinal; Rats; Solvents

To evaluate the effectiveness of topical nalbuphine or oral tramadol in the treatment of corneal pain in dogs.. Fourteen male Beagle dogs.. Dogs were divided into three treatment groups and sedated with dexmedetomidine (5 μ/kg IV). A 4 mm corneal epithelial wound was created in the right eye (OD) of all dogs. Sedation was reversed with atipamazole IM. All dogs received pre/post ophthalmic examinations. Post operatively, Group NB (n = 5) received topical 1% preservative-free nalbuphine OD q8 h and an oral placebo PO q8 h. Group TR (n = 5) received tramadol (4 mg/kg) PO q8 h and topical sterile saline OD q8 h. Group CNTRL (n = 4) received topical sterile saline OD q8 h and an oral placebo q8 h. All dogs received topical 0.3% gentamicin OD TID until healed. Dogs were pain scored using a pain scoring system modified from the University of Melbourne pain scale at 0, 1, 2, 4, and 6 h, then every 6 h by observers masked to treatment, until corneal wounds were healed. Treatment failure was recorded if cumulative pain scores were above a minimum threshold of acceptable pain and rescue analgesia of morphine (1.0 mg/kg IM) was administered subsequently.. Four dogs in Group NB, one dog in Group TR, and two dogs in Group CNTRL required rescue analgesia. There was no significant difference in the incidence of treatment failure between groups (P = 0.184). Mean time to rescue was 9.16 h. All corneal wounds were healed by 84 h.. The results of this study suggest tramadol rather than nalbuphine should be further investigated for the treatment of corneal pain.

Topics: Administration, Ophthalmic; Administration, Oral; Analgesics, Opioid; Animals; Cornea; Corneal Injuries; Dog Diseases; Dogs; Male; Nalbuphine; Pain; Pain Measurement; Pilot Projects; Tramadol

Intrathecal opioids have been shown to be safe and effective for postoperative analgesia in healthy children for spinal surgery. The aim of this study was to evaluate the applicability of intrathecal opioids in severely handicapped children scheduled for spinal surgery.. With hospital ethical committee approval, patients with physical states III and IV of the ASA classification requiring spinal surgery were retrospectively studied. In addition to inhalational anesthesia with sevoflurane or intravenous anesthesia using propofol, morphine 20 microg/kgBW and sufentanil 1.5 microg/kgBW were administered intrathecally before surgery. After surgery an infusion of nalbuphine was started. Need for additional intraoperative and postoperative analgesics, time of extubation, postoperative pain scores and p(a)CO2 values as well as adverse effects were recorded.. A total of 28 patients aged from 2.8 to 18.5 years (median 11.6 years) were studied. Immediate tracheal extubation in the operating room was possible in 17 patients and for 11 patients delayed extubation was elected. All patients were extubated within 24 h except for 1 patient who received massive postoperative transfusions. In 26 out of 28 patients (93%) the combination of intrathecal opioids with postoperative nalbuphine provided adequate analgesia. Observed side effects were post-operative nausea and vomiting (PONV), pruritus and moderate hypoventilation. In two patients a change to intravenous morphine therapy was necessary.. The use of intrathecal opioids for perioperative pain control from spinal fusion in severely handicapped children is feasible. Intrathecal opioids provide adequate postoperative analgesia and allow early extubation without persisting relevant respiratory compromise in most of these patients.

Topics: Adolescent; Analgesia; Analgesics, Opioid; Child; Child, Preschool; Disabled Children; Female; Humans; Injections, Spinal; Kaplan-Meier Estimate; Male; Nalbuphine; Pain; Pain Measurement; Pain, Postoperative; Perioperative Care; Postoperative Nausea and Vomiting; Pruritus; Retrospective Studies; Spine

Analgesics are required to prevent and treat postpartum pain, but breast-feeding may be contraindicated, because data on milk transfer are very limited. The present study was undertaken to quantify the transfer of ketoprofen and nalbuphine in milk. Eighteen patients gave their informed consent to participate and completed the study. Following delivery, they received ketoprofen (100 mg/12 hours) and nalbuphine (0.2 mg/kg/4 hours) as an intravenous bolus over 2 to 3 days for postpartum pain. Milk samples were collected during the 12 hours between the third and fourth ketoprofen administrations. Ketoprofen and nalbuphine concentrations were determined with high-performance liquid chromatography. The mean and maximum ketoprofen milk concentrations were 57+/-37 and 91+/-51 ng/mL, respectively. Assuming a milk volume of 150 mL/kg/day, the mean and maximum doses that a breast-fed neonate would ingest during one day are 8.5+/-5.5 and 13.6+/-7.6 microg/kg/day, respectively, and the relative infant dose is 0.31+/-0.17% of the weight-adjusted maternal daily dose. The mean and maximum nalbuphine milk concentrations were 42+/-26 and 61+/-26 ng/mL, respectively. Assuming a milk volume of 150 mL/kg/day, the mean and maximum doses that a breast-fed neonate would ingest during one day is 7.0+/-3.2 and 9.0+/-3.8 microg/kg/day, and the relative infant dose is 0.59+/-0.27% of the weight-adjusted maternal daily dose. Therefore, breast-feeding is permissible when ketoprofen and/or nalbuphine are administered to the mother to treat postpartum pain.

Topics: Adult; Analgesics, Opioid; Anti-Inflammatory Agents, Non-Steroidal; Female; Humans; Ketoprofen; Milk, Human; Nalbuphine; Pain; Parturition; Postpartum Period

Topics: Analgesics, Opioid; Butorphanol; Contraindications; Humans; Nalbuphine; Narcotic Antagonists; Pain; Patient Selection; Pentazocine

Topics: Acute Disease; Analgesics, Opioid; Humans; Male; Middle Aged; Nalbuphine; Narcotic Antagonists; Pain; Substance Withdrawal Syndrome; Time Factors

The hallmark of sickle cell disease (SCD) is recurrent, painful vaso-occlusive episodes (VOC) and is the most common reason for hospitalization in SCD patients. Narcotics, particularly morphine, along with fluid hydration are standard treatments for painful episodes but have been associated with the development of acute pulmonary events commonly referred to as acute chest syndrome (ACS). The development of ACS is often preceded by acute infections, painful episodes, rib infarction, bone marrow infarction, and fat embolism. Its pathophysiology remains multifactorial and has become the most common reason for early mortality. Previous episodes of ACS increase the likelihood of repeated acute pulmonary events and subsequent pulmonary hypertension. Nalbuphine hydrochloride (Nubain) is an opioid with the pain relieving potency of morphine but has not been studied for its association in the development of ACS or compared with morphine in its efficacy of pain control in the sickle cell population.. We reviewed the medical records retrospectively of patients between the age of 5 and 19 years, admitted for vaso-occlusive crisis to the three children's hospitals in Atlanta between January 1999 and December 2002. A computerized search tool was used to identify patients using the International Classification of Diseases Ninth Revision (ICD-9) diagnosis code 282.60 and 282.62. The final discharge diagnosis of ACS was defined as a new pulmonary infiltrate on chest radiograph after admission and before discharge. We calculated the need for 160 patient admissions for 85% power to detect a difference of approximately 20% in incidence of ACS between the two treatment groups.. There were a total of 37 (21%) episodes of ACS. Of these, 26 (29%) were in the morphine group and 11 (12%) were in the Nubain group (P < 0.01). Patients receiving morphine were more likely to have higher white cell counts on admission (P < 0. 05), and to use continuous infusion for medication administration (49% vs. 3%), P < 0. 001. They also had longer hospital stays than patients who received Nubain (median stay 3 days vs. 4 days, morphine), P < 0. 001.. The development of ACS during painful episodes is multi-factorial, but opioid selection may increase this rate. Patients on Nubain were less likely to develop ACS, and they had shorter hospital stays. These results were confounded by use of continuous analgesia infusion with PCA. However, Nubain may provide an alternative to morphine in the treatment of sickle cell pain episodes. A prospective clinical trial comparing these two analgesics would be a preferable next step.

Topics: Acute Disease; Adolescent; Adult; Analgesics, Opioid; Anemia, Sickle Cell; Child; Child, Preschool; Humans; Length of Stay; Lung Diseases; Morphine; Nalbuphine; Pain

Prehospital analgesia can be safely provided with only three agents: fentanyl, morphine and the mixed-gas nitrous oxide/oxygen. Of these three, fentanyl is by far the best agent for general EMS analgesic therapy by paramedics. However, to initiate prehospital analgesia earlier in the EMS response time frame, EMT's should administer nitrous oxide/oxygen. This protocol can easily be added to the EMT education program or through a continuing education session. All of the other agents discussed have absolutely no role in modern prehospital care.

Topics: Analgesics; Anesthetics, Combined; Butorphanol; Emergency Medical Services; Emergency Medical Technicians; Fentanyl; Humans; Ketorolac; Meperidine; Morphine; Nalbuphine; Nitrous Oxide; Oxygen; Pain

Topics: Analgesics, Opioid; Contraindications; Delayed-Action Preparations; Drug Interactions; Drug Resistance; Female; Humans; Infusions, Intravenous; Middle Aged; Morphine; Nalbuphine; Pain

Significant differences in the potency and effectiveness of opioid analgesics have been reported in subject populations differing in age. Although the relationship between aging and sensitivity to the antinociceptive effects of mu opioids has been examined extensively, relatively few studies have examined this relationship in kappa opioids.. The purpose of the present investigation was to examine the antinociceptive effects of selected kappa and mixed-action opioids in young (3 months) and aged (21 months) male rats.. In a warm-water, tail-withdrawal procedure, rats were restrained and the latencies to remove their tails from 50 degrees C (low temperature) and 55 degrees C (high temperature) water were measured. Selected kappa (U69,593, U50,488) and mixed-action (butorphanol, nalbuphine) opioids were tested alone, and in combination with the high-efficacy, kappa-opioid spiradoline.. All test drugs were more effective (i.e., produced a greater maximal effect) in aged rats than in young rats at both water temperatures. In drug combination tests, U69,593 and U50,488 enhanced the effects of spiradoline under conditions in which they failed to produce high levels of antinociception when administered alone. In contrast, butorphanol and nalbuphine antagonized the effects of spiradoline under conditions in which they failed to produce high levels of antinociception when administered alone.. These data may be taken as evidence that: (1) aged male rats are more sensitive than young male rats to the antinociceptive effects of kappa opioids, (2) U69,593 and U50,488 display agonist activity in the warm-water, tail-withdrawal procedure under some conditions in which they fail to produce antinociceptive effects, and (3) butorphanol and nalbuphine possess only limited agonist activity at the kappa receptor.

Topics: 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; Age Factors; Analgesics; Analgesics, Non-Narcotic; Analgesics, Opioid; Analysis of Variance; Animals; Benzeneacetamides; Butorphanol; Cold Temperature; Dose-Response Relationship, Drug; Drug Synergism; Male; Nalbuphine; Pain; Pain Measurement; Pyrrolidines; Rats; Rats, Inbred F344; Reaction Time; Receptors, Opioid, kappa

To determine if low dose nalbuphine provides an adequate reduction in pain with minimal side effects.. Prospective cohort of 115 patients given nalbuphine by paramedics in Wales and the English borders.. (1) Mean total dose of nalbuphine administered, change in pain score, time to adequate pain relief (score below four), and change in respiratory rate and systolic blood pressure; (2) proportion of patients continuing to suffer moderate to severe pain on arrival at hospital; (3) incidence of adverse events.. Full data were obtained for all patients. The mean total dose of nalbuphine administered was 6.09 mg (range 2.5 to 12.5 mg). This was significantly higher in trauma than ischaemic chest pain patients (7.03 versus 5.13 mg). The mean reduction in pain score was -3.97 (95% CI -4.38 to -3.57, p<0.001). The mean time to adequate pain relief (where this was achieved) was 15.7 minutes (95% CI 13.4 to 17.9 minutes). On arrival at hospital 60% of patients (n=69, 95% CI 50.9 to 68.5%) still met ambulance criteria for analgesia (70.7% of trauma patients and 49.1% with ischaemic chest pain). Systolic blood pressure fell by a mean of -3.67 (95% CI -6.76 to -0.58, p=0.02) and respiratory rate increased by a mean of 1.63 (95% CI 1.08 to 2.17, p<0.001). Two patients complained of nausea (1.74%, 95% CI 0.5 to 6.0%). No other adverse events were reported.. Low dose nalbuphine results in few adverse events, but offers poor pain control for a high proportion of patients.

Topics: Analgesics, Opioid; Clinical Protocols; Cohort Studies; Emergency Medical Services; Humans; Medical Audit; Nalbuphine; Pain; Pain Measurement; Prospective Studies

The aim of this investigation was to determine current opioid use in the Philippines and the reasons why its use is very low. We surveyed 314 doctors in Metro Manila to determine their specialty, possession of narcotics license, and knowledge of opioid use beyond the terminal stage. We found that the majority of respondents possess a narcotics licence. All of them see pain patients in their practice. They agree that opioids should not be reserved for the terminally ill; 235 have prescribed opioids for non-cancer pain. A small minority believes that use of opioids for non-cancer pain can lead to addiction. Opioids that were most easily recalled were morphine, meperidine and nalbuphine. The survey contradicts the national data for opioid use. With an INCB (International Narcotics Control Board) allocation of 87 kilograms annually, less than 15 kilograms are consumed every year. Fentanyl has a 7 gram usage versus a 100 gram INCB allocation. We conclude that actual opioid use in the Philippines is minimal. However, the correlation between survey results and actual usage indicates a strong awareness of the usefulness of opioids but hesitancy in opioid prescription.

Topics: Analgesics, Opioid; Chronic Disease; Fentanyl; Health Knowledge, Attitudes, Practice; Humans; Meperidine; Morphine; Nalbuphine; Pain; Philippines; Physicians; Practice Patterns, Physicians'; Surveys and Questionnaires

The effectiveness of analgesia during sickle cell crisis was examined in this descriptive, exploratory study. Pain scores (using the African-American Oucher and the Adolescent Pediatric Pain Tool) and analgesics administered were examined during a 2-hour observation/interview in the hospital while children/adolescents with sickle cell disease (SCD) experienced a vaso-occlusive episode (VOE). A convenience sample of twenty-one 6- to 16-year olds with SCD was included. Evidence indicated that 15 of the 21 children in the sample were in moderate to severe pain during their interviews, indicating that the analgesics did not effectively control their pain. Most participants (17) had received nalbuphine as the primary analgesic by intravenous infusion drip and/or patient-controlled analgesia pump. Many reasons were identified for the inadequate analgesia. The results suggested that the pain of SCD is very complex, requiring continuous adjustment of comfort measures, especially analgesics. More research is needed to examine pain control in children with SCD.

Topics: Adolescent; Analgesia; Analgesics, Opioid; Anemia, Sickle Cell; Child; Female; Humans; Interviews as Topic; Male; Nalbuphine; Pain; Vascular Diseases

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.. 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.

Topics: Analgesics, Opioid; Animals; Bridged Bicyclo Compounds, Heterocyclic; Buprenorphine; Butorphanol; Cycloparaffins; Dose-Response Relationship, Drug; Drug Combinations; Levorphanol; Morphine; Nalbuphine; Narcotics; Nociceptors; Pain; Physical Stimulation; Rats; Rats, Long-Evans; Receptors, Opioid, mu; Tetrahydronaphthalenes

Topics: Analgesics, Opioid; Drug Resistance; Emergency Medical Services; Humans; Morphine; Nalbuphine; Narcotic Antagonists; Pain; Pain Measurement; Pilot Projects; Randomized Controlled Trials as Topic; Tramadol

Paramedic training and skills have been introduced in the United Kingdom in an attempt to improve prehospital patient care. There is presently little control and quality assurance in this potentially difficult environment and paramedic protocols have not been validated. We studied the use of nalbuphine by paramedics for patients with major injury in West Yorkshire. A case-control study was carried out using two cohorts of patients from the regional Major Trauma Outcome Study (MTOS) database; one group had received prehospital nalbuphine by paramedics (the intervention) and a matched group who had not (the control). Both groups of patients were reviewed by a panel of three consultants and a paramedic to assess which patients received or could have received nalbuphine appropriately. Only 85 patients from a database of 4170 patients received nalbuphine. Fifty-two (61%) patients were thought by the panel to have been given nalbuphine appropriately. The panel also concluded that 21 (18%) of the 115 patient control group could have been administered nalbuphine but did not receive the drug. This study demonstrates inadequate and sometimes inappropriate use of nalbuphine in prehospital trauma care. Quality assurance and audit systems should be implemented to identify and correct these deficiencies.

Topics: Adolescent; Adult; Aged; Analgesics, Opioid; Drug Utilization; Emergency Medical Services; Emergency Medical Technicians; Glasgow Coma Scale; Hemodynamics; Humans; Injury Severity Score; Middle Aged; Nalbuphine; Pain; Quality Control; Retrospective Studies; Wounds and Injuries

To determine the analgesic efficacy of the opioid agonist-antagonist Nubain during midtrimester therapeutic terminations with intra-amniotic PGF2 alpha or i.m. administration of the PGE2 derivative sulprostone.. Following osmotic predilatation with laminaria tents patients were given as a premedication 10 mg Valium, 10 mg Nubain and 0.5 mg atropine i.m. prior to prostaglandin treatment, and sequential doses of Nubain during the uterine contractility period. Patients indicated their own perception of uterine pain on a differential graphic rating scale, and the attending physician also evaluated patients' discomfort on a 5-grade scale.. In 55% of the cases patients experienced only 'mild' or 'moderate' pain. The mean induction-to-abortion interval was short (11.6 +/- 1.3 h). The well known gastrointestinal side-effects of the prostaglandins were avoided.. Nubain proved effective in stabilizing patients' condition during intra-amniotic instillation of prostaglandin, effectively relieved uterine pain during the myometrial contractility period, prevented the occurrence of prostaglandin-related side-effects, and provided simple and good anesthesia during instrumental removal of the already detached but retained placenta.

Topics: Abortion, Therapeutic; Adult; Dinoprost; Female; Humans; Injections, Intramuscular; Nalbuphine; Pain; Pain Measurement; Pregnancy; Pregnancy Trimester, Second; Premedication; Uterus

A questionnaire was sent to principal investigators of NIH-sponsored clinical research in sickle cell disease. Twenty of 21 respondents indicated they used parenteral narcotic analgesics for pain episodes sufficiently severe to warrant hospitalization. Eleven used meperidine; seven, morphine; and one each, nalbuphine, hydromorphone, and acetaminophen with codeine. They gave the agents at frequent, regular intervals or by continuous infusion. A total of 41 of more than 3,500 patients required chronic transfusion for pain control. Complications included meperidine-associated convulsions reported by nine respondents and addiction by six. This information indicates that vigorous pain-control methods are used at institutions having a special interest in providing medical care for children with sickle cell disease.

Topics: Acetaminophen; Analgesics; Anemia, Sickle Cell; Child; Child, Preschool; Codeine; Drug Administration Schedule; Drug Combinations; Humans; Hydromorphone; Infant; Length of Stay; Meperidine; Morphine; Nalbuphine; Pain; Pain Management; Seizures

Painful episodes of sickle cell disease remain a source of frustration to patients and health care providers because of the lack of interventions to prevent or control them. Nalbuphine is a potent semisynthetic agonist/antagonist analgesic. We report our experience using nalbuphine as a treatment for painful episodes of sickle cell disease in children. The efficacy of subcutaneous/intramuscular nalbuphine is compared with intramuscular meperidine by a retrospective review of hospitalizations for sickle cell painful episodes. Nalbuphine is as effective as meperidine for the treatment of these episodes. We conclude that nalbuphine is a feasible and effective analgesic and a reasonable treatment option for patients with sickle cell disease experiencing painful episodes.

Topics: Acute Disease; Adolescent; Adult; Anemia, Sickle Cell; Child; Child, Preschool; Female; Humans; Male; Nalbuphine; Pain

The introduction of nalbuphine to intravenous sedation with midazolam added little to the quality of sedation for short operative procedures. There was a greater tendency for patients who received nalbuphine and midazolam to sleep in the afternoon after treatment compared with those who received only midazolam. Significantly more patients had nausea and vomiting in the midazolam/nalbuphine group than did patients in the midazolam-only group.

Topics: Adolescent; Adult; Anesthesia, Dental; Consumer Behavior; Drug Combinations; Female; Humans; Injections, Intravenous; Male; Memory; Midazolam; Molar, Third; Nalbuphine; Neuroleptanalgesia; Pain; Preanesthetic Medication; Tooth Extraction

Topics: Analgesics, Opioid; Animals; Buprenorphine; Butorphanol; Dose-Response Relationship, Drug; Formaldehyde; Male; Morphine; Nalbuphine; Nociceptors; Pain; Pentazocine; Rats; Rats, Inbred Strains; Sensory Thresholds

Nalbuphine reverses opioid-induced respiratory depression, but the effect on analgesia is unclear. The analgesic interaction between subcutaneous (sc) nalbuphine and intrathecal morphine in conscious, male, Sprague-Dawley rats implanted with chronic intrathecal catheters was investigated. Nalbuphine (10 mg/kg) injected 30 min after intrathecal morphine (4 micrograms) significantly antagonized the effect of morphine in the tail flick test. The antagonism was rapid in onset and persisted beyond the experimental period of 240 min. The magnitude and the duration of the effect were comparable to that observed with sc naloxone (1 mg/kg). In contrast to the results in the tail flick test, nalbuphine enhanced the effect of intrathecal morphine in the noninflamed paw pressure test. Nalbuphine (10 mg/kg) alone had no effect on the time course of tail flick latency but significantly increased paw pressure threshold during the 15-90 min interval after sc injection. Nalbuphine (0.5 mg/kg, sc) alone had no antinociceptive effect in either pain test and did not antagonize the antinociceptive effect of intrathecal morphine (4 micrograms) in the tail flick test. However, sc nalbuphine (0.5 mg/kg), injected 30 min after intrathecal morphine (1.5 micrograms), significantly enhanced the effect of morphine in the paw pressure test compared with intrathecal morphine + sc saline-treated rats. The results indicate a complex analgesic interaction between intrathecal morphine and sc nalbuphine. The net analgesic effect during the interaction was determined by the following: 1) the doses of morphine and nalbuphine; 2) the time after nalbuphine administration; and 3) the nature of the nociceptive stimulus. At lower doses, sc nalbuphine appeared to potentiate the effect of intrathecal morphine in the noninflamed paw pressure test.

Topics: Analgesics; Animals; Drug Interactions; Injections, Spinal; Injections, Subcutaneous; Male; Morphinans; Morphine; Nalbuphine; Pain; Pain Measurement; Rats; Rats, Inbred Strains; Reaction Time; Sensory Thresholds

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.

Topics: Adult; Analgesics; Apgar Score; Butorphanol; Carbon Dioxide; Female; Fetal Blood; Humans; Hydrogen-Ion Concentration; Labor, Obstetric; Nalbuphine; Oxygen; Pain; Pentazocine; Pregnancy

Forty-six patients with moderate to severe pain caused by orthopedic injuries, burns, multiple trauma, or intraabdominal conditions were treated with intravenous (IV) nalbuphine hydrochloride (Nubain; DuPont Pharmaceuticals, Wilmington, DE) by paramedics before arrival at the hospital. Patients who weighed less than 60 kg received 15 mg nalbuphine, and patients weighing greater than 60 kg received 20 mg nalbuphine. Forty-one of 46 patients (89%) experienced pain relief from nalbuphine, with maximum relief occurring within 15 minutes after the administration of the drug. Two addicted patients received no pain relief. There were no untoward side effects following nalbuphine administration, and the patients' heart rates, mean arterial pressures, and respiratory rates remained constant and stable throughout the study period. Repeated assessment of the patient by paramedics in the field was not impaired by nalbuphine treatment. In summary, nalbuphine hydrochloride is a useful and safe analgesic drug for IV use by paramedics in the prehospital setting.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Emergencies; Emergency Medical Technicians; Female; Humans; Male; Middle Aged; Morphinans; Nalbuphine; Pain; Wounds and Injuries

In order to examine the pharmacokinetics and excretion of nalbuphine (Nubain 20) in breast milk, patients suffering from postpartum pain were given a single dose of 20 mg nalbuphine intramuscularly. During a 24-h period, the total amount of nalbuphine excreted in the breast milk was 2.3 micrograms (mean value), which is equivalent to 0.012% of the dosage. The mean milk/plasma quotient was calculated using the AUC from the milk and plasma time curves at 1.2:1. An oral intake of 2.3 micrograms nalbuphine would not show any measurable plasma concentrations in the neonate. Adverse opioid reactions, e.g. respiratory depression are not to be expected even if one assumes a lack of glucuronide production in the neonate.

Topics: Adult; Female; Half-Life; Humans; Injections, Intramuscular; Milk, Human; Morphinans; Nalbuphine; Pain; Postpartum Period; Pregnancy

Topics: Analgesics; Animals; Dose-Response Relationship, Drug; Female; Injections, Spinal; Macaca; Morphinans; Nalbuphine; Pain; Sensory Thresholds

Topics: Adult; Dreams; Humans; Male; Mental Disorders; Morphinans; Nalbuphine; Pain

Topics: Adult; Female; Heart Rate; Humans; Infant, Newborn; Male; Middle Aged; Morphinans; Morphine; Nalbuphine; Nausea; Pain; Postoperative Complications; Respiration

A technique for the management of pain and anxiety during pacemaker implantation, electrophysiologic studies, and related procedures is described. The technique involves the intravenous administration of small amounts of the narcotic agonist-antagonist nalbuphine and the benzodiazepine diazepam. The small amounts of medication used induce relaxation while allowing the patient to interact and cooperate during the procedure. The absence of side effects facilitates outpatient treatment. This method of pain management not only improves the quality of patient care but also encourages earlier hospital discharge.

Topics: Adult; Aged; Anesthesia, Inhalation; Anesthesia, Local; Diazepam; Electrophysiology; Female; Humans; Infusions, Parenteral; Lidocaine; Male; Morphinans; Nalbuphine; Pacemaker, Artificial; Pain; Procaine

Topics: Buprenorphine; Butorphanol; Drug Evaluation; Humans; Nalbuphine; Narcotic Antagonists; Pain; Receptors, Opioid

One hundred twenty-one patients with postpartum pain caused by uterine cramp or episiotomy pain were the subjects of a randomized, double-blind, single-dose study of oral nalbuphine (N), 15 mg (N = 39); codeine (C), 60 mg (N = 42); and placebo (N = 40) for analgesia. Observations were made over 6 hr. There were significant differences for sum of pain intensity differences and total pain relief between the active drugs and placebo but not between N and C. Time to onset of analgesia favored N (mean = 0.65 min) over C (mean = 0.74 min), but the analgetic effect of N diminished more rapidly at this dose. Results were the same for both uterine cramp and episiotomy pain. Adverse effects were of the narcotic type and of the same incidence for the two active drugs. Two new parameters for determining analgetic effect are introduced: number of dropouts per dose and number of subjects with zero analgetic effect.

Topics: Administration, Oral; Adult; Codeine; Double-Blind Method; Drug Evaluation; Episiotomy; Female; Humans; Morphinans; Nalbuphine; Pain; Postpartum Period; Pregnancy; Random Allocation; Uterus

To compare the respiratory depressant and analgesic effects of nalbuphine and morphine, six healthy male subjects were given the drugs as single 0.15-mg/kg doses, and as four successive doses of 0.15 mg/kg. Respiratory depression was monitored by ventilatory and mouth occlusion pressure responses during CO2 rebreathing, while analgesia to experimental pain was tested with the submaximal effort tourniquet ischemia test. When given as single 0.15 mg/kg doses, both drugs significantly increases the threshold and tolerance for experimental pain. The analgesic effect was similar for both drugs at this dosage, as was depression of the ventilatory and occlusion pressure responses to CO2. Morphine administered in multiple doses progressively increased pain tolerance from 30 +/- 13% above control with the first dose of 0.15 mg/kg to 107 +/- 13% above control after the fourth dose (cumulative total 0.60 mg/kg). Nalbuphine produced a 40 +/- 12% increase in pain tolerance with an initial dose of 0.15 mg/kg, but additional increments of nalbuphine did not result in significantly greater analgesia. The increasing morphine dosage was associated with progressive rightward displacements and ultimately decreases in the slope of the CO2 response curves. Nalbuphine produced an initial rightward displacement of the CO2 response curves similar to morphine, but continued administration of the drug did not result in further displacement or changes in slope. These findings demonstrate that nalbuphine, in contrast to morphine, exhibits a ceiling effect for respiratory depression which is paralleled by its limited analgesic effect on experimental pain.

Topics: Adult; Analgesics; Carbon Dioxide; Dose-Response Relationship, Drug; Humans; Male; Morphinans; Morphine; Nalbuphine; Pain; Respiration; Sensory Thresholds; Spirometry

Topics: Analgesics; Butorphanol; Drug Evaluation; Female; Humans; Legislation, Drug; Methods; Morphinans; Nalbuphine; Pain; Pregnancy; United States

Topics: Humans; Morphinans; Nalbuphine; Pain