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nalbuphine subcutáneous

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https://www.readbyqxmd.com/read/25820831/dual-%C3%AE%C2%BA-agonist-%C3%AE-antagonist-opioid-receptor-modulation-reduces-levodopa-induced-dyskinesia-and-corrects-dysregulated-striatal-changes-in-the-nonhuman-primate-model-of-parkinson-disease
#1
Lisa F Potts, Eun S Park, Jong-Min Woo, Bhagya L Dyavar Shetty, Arun Singh, Steven P Braithwaite, Michael Voronkov, Stella M Papa, M Maral Mouradian
OBJECTIVE: Effective medical management of levodopa-induced dyskinesia (LID) remains an unmet need for patients with Parkinson disease (PD). Changes in opioid transmission in the basal ganglia associated with LID suggest a therapeutic opportunity. Here we determined the impact of modulating both mu and kappa opioid receptor signaling using the mixed agonist/antagonist analgesic nalbuphine in reducing LID and its molecular markers in the nonhuman primate model. METHODS: 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated macaques with advanced parkinsonism and reproducible LID received a range of nalbuphine doses or saline subcutaneously as: (1) monotherapy, (2) acute coadministration with levodopa, and (3) chronic coadministration for 1 month...
June 2015: Annals of Neurology
https://www.readbyqxmd.com/read/25693108/nalbuphine-a-non-controlled-opioid-analgesic-and-its-potential-use-in-research-mice
#2
REVIEW
Heather Lyons Narver
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...
March 2015: Lab Animal
https://www.readbyqxmd.com/read/17225166/sex-differences-in-the-potency-of-kappa-opioids-and-mixed-action-opioids-administered-systemically-and-at-the-site-of-inflammation-against-capsaicin-induced-hyperalgesia-in-rats
#3
Lisa M Lomas, Andrew C Barrett, Jolan M Terner, Donald T Lysle, Mitchell J Picker
RATIONALE: Sex differences in the potency of the antinociceptive effects of kappa opioids have been reported in various acute pain models with evidence suggesting that these sex differences are mediated by activity in the N-methyl-D: -aspartate (NMDA) system. OBJECTIVES: The purpose of the present study was to evaluate sex differences in the antihyperalgesic actions of selected kappa and mixed-action opioids in a persistent pain model and determine if the NMDA system modulates these effects in a sexually dimorphic manner...
April 2007: Psychopharmacology
https://www.readbyqxmd.com/read/12906398/the-sedative-and-behavioral-effects-of-nalbuphine-in-dogs
#4
COMPARATIVE STUDY
Patrick A Lester, James S Gaynor, Peter W Hellyer, Khursheed Mama, Ann E Wagner
We compared the degree of sedation and frequency and intensity of adverse behaviors in dogs associated with nalbuphine when combined with acepromazine or xylazine compared with those of acepromazine or xylazine alone. Twenty-four dogs (13 female, 11 male) undergoing routine ovariohysterectomy or castration were randomly assigned to one of four groups. Group NX received 0.5 mg/kg nalbuphine and 0.5 mg/kg xylazine subcutaneously (s.c.). Group X received 0.5 mg/kg xylazine s.c. Group NA received 0.5 mg/kg nalbuphine and 0...
July 2003: Contemporary Topics in Laboratory Animal Science
https://www.readbyqxmd.com/read/12505963/the-analgesic-effect-of-interscalene-block-using-clonidine-as-an-analgesic-for-shoulder-arthroscopy
#5
RANDOMIZED CONTROLLED TRIAL
Henri Iskandar, Antoine Benard, Joelle Ruel-Raymond, Gyslaine Cochard, Bertrand Manaud
UNLABELLED: Used as the sole analgesic, clonidine produces analgesia after central neural blockade and intraarticular injection but not after axillary block. In this study, we sought to determine whether interscalene clonidine induces analgesia for shoulder arthroscopy. Forty patients scheduled for shoulder arthroscopy were prospectively included in this double-blinded study. Using a nerve stimulator technique, an interscalene catheter was inserted. The patients were randomly divided into two groups...
January 2003: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/11472277/efficacy-and-safety-of-patient-controlled-opioid-analgesia-for-acute-postoperative-pain-a-quantitative-systematic-review
#6
B Walder, M Schafer, I Henzi, M R Tramèr
BACKGROUND: The usefulness of intravenous patient-controlled analgesia (PCA) with opioids for postoperative analgesia is not well defined. METHODS: We systematically searched (MEDLINE, EMBASE, Cochrane Library, bibliographies, any language, to January 2000) for randomised trials comparing opioid-based PCA with the same opioid given intramuscularly, intravenously, or subcutaneously. Weighted mean differences (WMD) for continuous data, relative risks (RR) and numbers-needed-to-treat (NNT) for dichotomous data were calculated with 95% confidence intervals (CI) using fixed and random effects models...
August 2001: Acta Anaesthesiologica Scandinavica
https://www.readbyqxmd.com/read/11376971/controlled-release-of-nalbuphine-propionate-from-biodegradable-microspheres-in-vitro-and-in-vivo-studies
#7
S Y Yen, K C Sung, J J Wang, O Yoa-Pu Hu
The objective of this work was to assess the in vitro characteristics, in vivo pharmacokinetics and in vivo pharmacodynamics of nalbuphine propionate (NAP)-loaded microspheres. An oil-in-water solvent evaporation method was used to incorporate NAP into poly (d,l-lactide-co-glycolide) (PLGA)-based microspheres. The morphology of the microspheres were evaluated using scanning electron microscopy which showed a spherical shape with smooth surface. A prolonged in vitro drug release profile was observed, with approximately 71...
June 4, 2001: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/10817460/adverse-effects-on-growth-rates-in-rats-caused-by-buprenorphine-administration
#8
C Jacobson
As a routine postoperative treatment, a single dose of buprenorphine was given to rats at a dose of 0.05 mg/kg subcutaneously. However, some rats developed abnormal secretions around the nose and mouth and some animals died 3-5 days after surgery and analgesic treatment. At autopsy a yellow fibrous mass was found in the stomach and intestines. Observations of animals given buprenorphine revealed an abnormal ingestion of bedding material. This caused a disturbance to normal digestion, with gastric distension, weight loss or decreased growth rate, constipation and occasionally death...
April 2000: Laboratory Animals
https://www.readbyqxmd.com/read/9750795/-conventional-techniques-for-analgesia-opioids-and-non-opioids-indications-adverse-effects-and-monitoring
#9
REVIEW
J X Mazoit
Morphine dosage must be carefully adapted in patients with renal failure or severe liver failure. The i.v. route is used for morphine titration in the post anaesthesia care unit (PACU), or for analgesia in children. Systematic (not on demand) intramuscular or subcutaneous morphine must be administered at intervals not longer than 4 hours. Dosage is best determined after i.v. titration in the PACU. Codeine, administered orally, is metabolised into morphine. Codeine has almost no effect in 7% of Caucasians and at least 15% of Asians...
1998: Annales Françaises D'anesthèsie et de Rèanimation
https://www.readbyqxmd.com/read/8551472/effect-of-labor-analgesia-with-nalbuphine-hydrochloride-on-fetal-response-to-vibroacoustic-stimulation
#10
S Poehlmann, M Pinette, P Stubblefield
OBJECTIVE: To evaluate the effect of labor analgesia with nalbuphine hydrochloride on the fetal response to vibroacoustic stimulation. STUDY DESIGN: The response to fetal acoustic stimulation (FAS) was recorded in 27 laboring patients before analgesia. After analgesia with 5 mg nalbuphine hydrochloride administered subcutaneously, the response to FAS was again recorded. RESULTS: No ominous fetal heart rate (FHR) patterns were observed. FAS reliably increased FHR baseline and long-term FHR variability and produced FHR accelerations...
October 1995: Journal of Reproductive Medicine
https://www.readbyqxmd.com/read/8235791/magnetic-resonance-imaging-of-nalbuphine-induced-myocutaneous-sclerosis
#11
C E Larsen, R G Stiles, S C Davis
Myocutaneous sclerosis is a known complication of intramuscular and subcutaneous injection of narcotics. We have described the MRI findings of this entity with superimposed infection in a patient addicted to intramuscular and subcutaneously administered nalbuphine. The clinical and imaging features of this disorder are sufficiently characteristic to allow confident diagnosis. This is the first report of this disorder due to nalbuphine.
November 1993: Southern Medical Journal
https://www.readbyqxmd.com/read/7510801/palliative-care-in-mexico-coeliac-plexus-block-for-incidental-visceral-pain
#12
G Montejo Rosas, E Bruera
No abstract text is available yet for this article.
1993: Journal of Palliative Care
https://www.readbyqxmd.com/read/6842402/subclasses-of-opioids-based-on-body-temperature-change-in-rats-acute-subcutaneous-administration
#13
E B Geller, C Hawk, S H Keinath, R J Tallarida, M W Adler
Morphine and a number of opioid agonists and agonist-antagonists were injected into rats to examine their effects on body temperature after acute systemic administration. Dose- and time-response curves were constructed for each drug alone and in the presence of the antagonist naloxone. Based on these data, the opioids could be subdivided into several groups. The first group, made up of morphine, heroin, l-methadone, etorphine, fentanyl and levorphanol, caused hyperthermia at lower doses and hypothermia at higher ones...
May 1983: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/6744688/increased-naloxone-potency-induced-by-pretreatment-with-morphine-and-nalbuphine-in-mice
#14
C L Wong, M K Wai
Both morphine and nalbuphine were effective in suppressing the abdominal constriction response induced by intraperitoneal injection of acetic acid in mice. On a weight to weight basis, nalbuphine was more potent than morphine in this test. However, the effect of nalbuphine was more effectively blocked by naloxone. Pretreatment with morphine 2.0 mg/kg subcutaneously did not alter the antinociceptive effect of either morphine or nalbuphine measured 3 h later. However, naloxone was about 1.4-fold more effective in antagonizing the antinociceptive effect of both drugs in morphine-pretreated mice than in saline-pretreated animals...
May 1984: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/6254782/inhibition-of-growth-in-young-mice-treated-with-pentazocine-reversal-by-naltrexone
#15
N M Wassef, A A Smith
One week old mice were injected subcutaneously once daily with d,1-methadone (5 mg/kg), pentazocine, naltrexone, naloxone, nalorphine or nalbuphine, each at 10 mg/kg. The remaining half of each litter was used as control. Only methadone and pentazocine groups showed reduced weight gain after 3 weeks of treatment (P < 0.01). Injection of pentazocine in dosages of 5-20 mg/kg inhibited weight gain and protein synthesis in a dose-related manner. The incorporation of labeled leucine was followed in brain, liver and muscles...
August 29, 1980: European Journal of Pharmacology
https://www.readbyqxmd.com/read/3691617/the-pharmacokinetics-of-intravenous-intramuscular-and-subcutaneous-nalbuphine-in-healthy-subjects
#16
COMPARATIVE STUDY
M W Lo, F H Lee, W L Schary, C C Whitney
The pharmacokinetics of intravenously, intramuscularly, and subcutaneously administered nalbuphine were studied in three parallel groups of 12 healthy volunteers each. The subjects received single doses of 10 mg and 20 mg of nalbuphine separated by a one week washout period. Blood specimens were obtained up to 15 h after dosing for determination of nalbuphine. Mean plasma nalbuphine concentrations 5 min after intravenous administration of 10 or 20 mg were 39 and 73 ng/ml, respectively. The mean maximum plasma concentrations (Cmax) after intramuscular or subcutaneous administration of nalbuphine 10 mg were 29 and 31 ng/ml, respectively...
1987: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/3582496/the-effect-of-nalbuphine-on-gastrointestinal-transit-in-mice
#17
C L Wong
Nalbuphine given subcutaneously (s.c.) inhibited gastrointestinal transit in a dose-dependent manner. Prior s.c. administration of naloxone hydrochloride suppressed the inhibitory effect of nalbuphine on gastrointestinal transit. Naloxone methobromide (naloxone MB), a quaternary compound, was also effective in antagonising this effect of nalbuphine but was less effective than naloxone hydrochloride. Furthermore, prior s.c. administration of Mr 2266 also antagonised the gastrointestinal transit inhibitory action of nalbuphine...
March 17, 1987: European Journal of Pharmacology
https://www.readbyqxmd.com/read/2817464/a-study-of-the-analgesic-interaction-between-intrathecal-morphine-and-subcutaneous-nalbuphine-in-the-rat
#18
C W Loomis, J Penning, B Milne
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...
November 1989: Anesthesiology
https://www.readbyqxmd.com/read/2445439/differential-effects-of-mu-and-kappa-opioid-analgesics-on-cerebral-glucose-utilization-in-the-rat
#19
R J Fanelli, M Szikszay, D R Jasinski, E D London
The autoradiographic 2-deoxy-D-[1-(-14)C]glucose ([14C]2-DG) method was used to map the effects of subcutaneous (s.c.) morphine (8.0 mg/kg), oxymorphone (0.4 mg/kg) and nalbuphine (16.0 mg/kg) on local cerebral glucose utilization (LCGU), an index of local brain function. At the dosages administered, effects of the opioid agonists on LCGU were very restricted. The mu agonists, injected 15 min before [14C]2-DG, decreased LCGU in thalamic nuclei, including some of those which have been implicated in somatosensory processing, and in the dorsal tegmental nucleus...
October 6, 1987: Brain Research
https://www.readbyqxmd.com/read/2175919/pharmacological-profile-of-the-potentiation-of-opioid-analgesia-by-restraint-stress
#20
D J Calcagnetti, S W Fleetwood, S G Holtzman
Morphine-treated rats exposed to restraint stress show potentiated magnitude and duration of analgesia compared to unstressed rats. The present study was performed to assess the pharmacological characteristics of stress-induced potentiation of opioid analgesia. We tested 10 opioids to determine whether restraint stress treatment would potentiate their ability to produce antinociception indexed by the tail-flick assay. We tested full mu, delta and kappa opioid receptor agonists (fentanyl, meperidine, DPDPE, U50488H, ethylketocyclazocine), and mixed agonist/antagonists representing a range of receptor selectivities and intrinsic activities (profadol, buprenorphine, pentazocine, butorphanol and nalbuphine)...
September 1990: Pharmacology, Biochemistry, and Behavior
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