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Samuel Obeng, Yunyun Yuan, Abdulmajeed Jali, Dana E Selley, Yan Zhang
Evidence has shown that downstream signaling by mu opioid receptor (MOR) agonists that recruit β-arrestin2 may lead to the development of tolerance. Also, it has been suggested that opioid receptor desensitization and cyclic AMP overshoot contributes to the development of tolerance and occurrence of withdrawal, respectively. Therefore, studies were conducted with 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3-carboxamido)morphinan (NAQ), a MOR selective partial agonist discovered in our laboratory, to characterize its effect on β-arrestin2 recruitment and precipitation of a cyclic AMP overshoot...
March 9, 2018: European Journal of Pharmacology
F Belal, F Ibrahim, Z A Sheribah, H Alaa
In this paper, novel univariate and multivariate regression methods along with model-updating technique were developed and validated for the simultaneous determination of quaternary mixture of imatinib (IMB), gemifloxacin (GMI), nalbuphine (NLP) and naproxen (NAP). The univariate method is extended derivative ratio (EDR) which depends on measuring every drug in the quaternary mixture by using a ternary mixture of the other three drugs as divisor. Peak amplitudes were measured at 294nm, 250nm, 283nm and 239nm within linear concentration ranges of 4...
February 21, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Sarah L Withey, Carol A Paronis, Jack Bergman
Although the clinical application of opioids for pain management is often hindered by undesired behavioral impairment, preclinical assays of antinociception typically do not provide information regarding the behaviorally disruptive effects of opioids that may accompany their antinociceptive effects. To address this, we modified a warm water tail withdrawal procedure to determine concurrently the effects of opioids on tail withdrawal latency (antinociception) and indices of food-maintained operant behavior (rates of responding and reinforcement density) in squirrel monkeys...
February 22, 2018: Journal of Pain: Official Journal of the American Pain Society
Lilian T Nishimura, Adam Auckburally, Juliana Santilli, Beatriz H B Vieira, Debora O Garcia, Cristiane S Honsho, Ewaldo de Mattos-Junior
OBJECTIVE To evaluate cardiopulmonary, sedative, and antinociceptive effects of dexmedetomidine combined with commonly administered opioids in dogs. ANIMALS 8 healthy Beagles. PROCEDURES Dogs were sedated by IM administration of each of 7 treatments. Treatments comprised dexmedetomidine (0.01 mg/kg; Dex) and the same dose of dexmedetomidine plus butorphanol (0.15 mg/kg; Dex-But), meperidine (5 mg/kg; Dex-Mep), methadone (0.5 mg/kg; Dex-Meth), morphine (0.5 mg/kg; Dex-Mor), nalbuphine (0.5 mg/kg; Dex-Nal), or tramadol (5 mg/kg; Dex-Tram)...
March 2018: American Journal of Veterinary Research
P G Genov, V H Timerbaev, A A Grin, O Yu Rebrova
DESIGN: 129 patients scheduled for elective lumbar discectomy in 2010-2013 were enrolled in prospective study. Group K (n=20) underwent general anaesthesia and postoperative analgesia on-demand. Group PMA+SA (n=23) got subarachnoid block and preventive multimodal analgesia (PMA) including ketoprofen, paracetamol and nalbuphine. At PMA group (n=21) general anaesthesia and PMA were used; at PMA+I (n=21) also bupivacaine wound infiltration was administrated; at PlvL4+S (n=20) - depo-corticosteroid was applied locally on affected spinal nerve root; at PMA+IS (n=24) wound infiltration and local corticosteroids were combined...
September 2017: Anesteziologiia i Reanimatologiia
Li Yang, Jinjing Wu, Tao Li
The aim of the present study was to investigate the analgesic effect and safety of the application of different doses of nalbuphine in patient-controlled intravenous analgesia (PCIA) for patients undergoing subtotal gastrectomy. A total of 120 patients, who underwent subtotal gastrectomy at our hospital between May, 2015 and January, 2017 under combined spinal epidural combined anesthesia, were selected. The patients received PCIA after surgery. The patients were randomly divided into four groups, including the morphine (MOP group), nalbuphine 60 mg (N60 group), nalbuphine 80 mg (N80 group) and nalbuphine 100 mg (N100 group)...
February 2018: Experimental and Therapeutic Medicine
Yong Gong, Yang Zhang, Shoujun Tao
The present study evaluated the use of nalbuphine for analgesia after fraction reduction surgery. Eighty lower limb fracture patients needing open reduction and internal fixation were selected in the First People's Hospital of Jingzhou from January 2015 to December 2015. Patients were randomly divided into observation and control groups (with 40 cases in each). After surgery, the patients in the observation group were treated with nalbuphine (2 mg/kg) for patient-controlled intravenous analgesia (PCIA), while sufentanil (2...
January 2018: Experimental and Therapeutic Medicine
Steven G Schauer, Allyson A Arana, Jason F Naylor, Guyon J Hill, Michael D April
BACKGROUND: Previous studies have evaluated prehospital analgesia during combat operations in Iraq and Afghanistan, but were limited to the adult population. However, a significant portion of the casualties of those conflicts were children. We describe the prehospital analgesia administered to wartime pediatric trauma patients. METHODS: We queried the Department of Defense Trauma Registry (DODTR) for all pediatric patients (<18 years of age) admitted to United States and Coalition fixed-facility hospitals in Iraq and Afghanistan from January 2007 to January 2016...
February 7, 2018: Prehospital Emergency Care
Jeremy C Cornelissen, Samuel Obeng, Kenner C Rice, Yan Zhang, S Stevens Negus, Matthew Banks
Receptor theory predicts that fixed-proportion mixtures of a competitive, reversible agonist (e.g. fentanyl) and antagonist (e.g. naltrexone) at a common receptor (e.g. mu opioid receptors; MOR) will result in antagonist proportion-dependent decreases in apparent efficacy of the mixtures and downward shifts in mixture dose-effect functions. The present study tested this hypothesis by evaluating behavioral effects of fixed-proportion fentanyl/naltrexone mixtures in a warm-water tail-withdrawal procedure in rhesus monkeys (n=4)...
January 12, 2018: Journal of Pharmacology and Experimental Therapeutics
Umesh N Prabhakaraiah, Archana B Narayanappa, Shivakumar Gurulingaswamy, Krishna Kempegowda, Kiran A Vijaynagar, Nagarajaiah B Hanumantharayappa, Diwakar S Ramegowda
Background and Aims: Opioids have been favored as adjuvants to local anesthetics during spinal anesthesia. Nalbuphine, a μ-receptor antagonist and ĸ-receptor agonist, seems to be a suitable adjuvant to local anesthetics. The aim of this study was to compare postoperative analgesia and adverse effects of nalbuphine and fentanyl when used as an adjuvant to hyperbaric bupivacaine during spinal anesthesia. Materials and Methods: Sixty patients belonging to the American Society of Anesthesiologists Physical Status I and II were randomly allocated into two groups of thirty each...
October 2017: Anesthesia, Essays and Researches
Jeremy C Cornelissen, Floyd F Steele, Kenner C Rice, Katherine L Nicholson, Matthew L Banks
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...
February 2018: Behavioural Pharmacology
Chaoyi Deng, Xiao Wang, Qianmei Zhu, Yanming Kang, Jinlin Yang, Heng Wang
OBJECTIVES: Nalbuphine is as effective as morphine as a perioperative analgesic but has not been compared directly with sufentanil in clinical trials. The aims of this study were to compare the efficacy and safety of nalbuphine with that of sufentanil in patients undergoing colonoscopy and to determine the optimal doses of nalbuphine in this indication. METHODS: Two hundred and forty consecutive eligible patients aged 18-65 years with an American Society of Anesthesiologists classification of I-II and scheduled for colonoscopy were randomly allocated to receive sufentanil 0...
2017: PloS One
Viviane H Gomes, Renato Ls Oliveira, Juliana Lr Marques, Cassia Mm Coelho, Marta Fa Silva
OBJECTIVE: To compare sedation and effects on heart rate (HR), mean arterial pressure (MAP) and respiratory rate (fR ) of nalbuphine and butorphanol, alone or combined with acepromazine in dogs. STUDY DESIGN: Prospective, randomized experimental trial. ANIMALS: Eight healthy Beagle dogs, aged (mean ± standard deviation) 3.4 ± 0.5 years and weighing 11.0 ± 1.3 kg. METHODS: Each dog was treated four times: physiological saline (1 mL) combined with nalbuphine (0...
January 2018: Veterinary Anaesthesia and Analgesia
Lisa L Wolfe, Pauline Nol, Matthew P McCollum, Travis Mays, Morgan E Wehtje, William R Lance, Mark C Fisher, Michael W Miller
Previous studies demonstrated that nalbuphine, medetomidine, and azaperone (NalMed-A) can effectively immobilize adult elk (Cervus elaphus nelsoni), and be antagonized using naltrexone and atipamezole, with or without tolazoline. To assess duration of tissue residues for this immobilization package, we immobilized 14 captive adult elk with NalMed-A, then euthanized animals and collected tissues 0, 3, 6, 14, 21, or 28 d later. Except for two animals euthanized immediately, all elk were recovered using naltrexone, atipamezole, and tolazoline...
November 17, 2017: Journal of Wildlife Diseases
Yang Zhang, Qi Jiang, Tao Li
This study sought to investigate the analgesic effects of nalbuphine on patients undergoing thoracoscopic lobectomy during the perioperative period, as well as its effects on inflammatory cytokines. We selected 92 patients with early lung cancer who were admitted to Xiangyang No. 1 People's Hospital between January 2016 and December 2016. The patients were randomly divided into control and observation groups (n=46 each). All patients underwent thoracoscopic lobectomy, with those in the observation group receiving intravenous nalbuphine hydrochloride prior to induction (the control group received saline)...
October 2017: Experimental and Therapeutic Medicine
Rajib Hazarika, Samit Parua, Dipika Choudhury, Rajesh Kumar Barooah
AIM: The objective of this study was to assess and compare the analgesic duration of local infiltration of bupivacaine plus magnesium sulfate and ropivacaine plus magnesium sulfate for postoperative analgesia in patients undergoing lumbar laminectomy. STUDY DESIGN: A randomized, prospective, double-blinded single hospital, comparative study. METHODS: Sixty adult patients of the American Society of Anesthesiologists physical Status I and II were randomly allocated into two Groups BM and RM, comprising 30 and 31 patients...
July 2017: Anesthesia, Essays and Researches
Brenda L Kick, Pan Shu, Bo Wen, Duxin Sun, Douglas K Taylor
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...
September 1, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
Shagufta Naaz, Usha Shukla, Swati Srivastava, Erum Ozair, Adil Asghar
INTRODUCTION: Intrathecal opioids when added to local anaesthetics decrease their dosage and provide haemodynamic stability. Nalbuphine is an agonist-antagonist and acts on kappa receptors providing analgesia. AIM: The study aims to compare the analgesic efficacy of fentanyl with that of two doses of nalbuphine when used with injection bupivacaine heavy in spinal anaesthesia. MATERIALS AND METHODS: A randomised, double blinded, prospective study on 90 patients of ASA I and II undergoing lower limb orthopaedic surgery under subarachnoid block was done...
July 2017: Journal of Clinical and Diagnostic Research: JCDR
Yu En Tien, Wen-Chuan Huang, Hui-Yuan Kuo, Lily Tai, Yow-Shieng Uang, Wendy H Chern, Jin-Ding Huang
Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Its short half-life requires frequent injections in clinical practice, resulting in a greater incidence of adverse events. A prodrug of nalbuphine has been developed, dinalbuphine sebacate (DNS), dissolved in a simple oil-based injectable formulation, which could deliver and maintain an effective blood level of nalbuphine. An open-label, prospective, two-period study was performed in healthy volunteers to verify the extended blood concentration profile of nalbuphine...
July 25, 2017: Biopharmaceutics & Drug Disposition
Nazia Nazir, Shruti Jain
INTRODUCTION: Benefits of regional anesthesia can be prolonged by adding adjuvants to local anesthetics. This study was designed to test the efficacy of adding nalbuphine to bupivacaine in supraclavicular brachial plexus blockade using ultrasound (US) guidance. METHODOLOGY: This was a prospective, randomized, double-blind study involving sixty patients of either sex undergoing elective orthopedic procedures of upper limb. In control Group C (n = 30), 30 mL of 0...
April 2017: Anesthesia, Essays and Researches
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