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https://www.readbyqxmd.com/read/28325149/low-dose-naltrexone-in-the-treatment-of-fibromyalgia
#1
Samy K Metyas, Karen Yeter, John Solyman, Daniel Arkfeld
Fibromyalgia is a chronic pain disorder characterized by diffuse musculoskeletal pain, fatigue, sleep disturbance and cognitive impairment. A significant number of fibromyalgia patients do not respond adequately to the current drugs (pregabalin, milnacipran, duloxetine) approved for fibromyalgia treatment by the Food and Drug Administration (FDA). Thus, there is still a need for adjunctive therapies. Naltrexone is an opioid receptor antagonist used to treat alcohol and opioid dependence. It is hypothesized that low dose naltrexone causes transient blockade of opioid receptors centrally resulting in a rebound of endorphin function which may attenuate pain in fibromyalgia...
March 21, 2017: Current Rheumatology Reviews
https://www.readbyqxmd.com/read/28322161/the-use-of-methylphenidate-in-cancer-patients-a-review
#2
Beatrice Andrew, Chong Guan Ng, Nik Ruzyanei Nik Jaafar
BACKGROUND: One of the goals of cancer treatment is symptoms management especially at the end stage. The common symptoms in cancer include pain, fatigue, depression and cognitive dysfunction. The available treatment options for symptom management are limited. Methylphenidate, a psychostimulant, may be of benefit for these patients. In this report, we review the use of methylphenidate for symptoms control in cancer patients. METHOD: Electronic literature search on PubMed was conducted using the following keywords: methylphenidate, cancer, carcinoma, oncology, oncological and tumour...
March 17, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28319053/alternatively-spliced-mu-opioid-receptor-c-termini-impact-the-diverse-actions-of-morphine
#3
Jin Xu, Zhigang Lu, Ankita Narayan, Valerie P Le Rouzic, Mingming Xu, Amanda Hunkele, Taylor G Brown, William F Hoefer, Grace C Rossi, Richard C Rice, Arlene Martínez-Rivera, Anjali M Rajadhyaksha, Luca Cartegni, Daniel L Bassoni, Gavril W Pasternak, Ying-Xian Pan
Extensive 3' alternative splicing of the mu opioid receptor gene OPRM1 creates multiple C-terminal splice variants. However, their behavioral relevance remains unknown. The present study generated 3 mutant mouse models with truncated C termini in 2 different mouse strains, C57BL/6J (B6) and 129/SvEv (129). One mouse truncated all C termini downstream of Oprm1 exon 3 (mE3M mice), while the other two selectively truncated C-terminal tails encoded by either exon 4 (mE4M mice) or exon 7 (mE7M mice). Studies of these mice revealed divergent roles for the C termini in morphine-induced behaviors, highlighting the importance of C-terminal variants in complex morphine actions...
March 20, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28315268/sigma-1-receptor-antagonists-a-new-class-of-neuromodulatory-analgesics
#4
Cristina Sánchez-Fernández, José Manuel Entrena, José Manuel Baeyens, Enrique José Cobos
The sigma-1 receptor is a unique ligand-operated chaperone present in key areas for pain control, in both the peripheral and central nervous system. Sigma-1 receptors interact with a variety of protein targets to modify their function. These targets include several G-protein-coupled receptors such as the μ-opioid receptor, and ion channels such as the N-methyl-D-aspartate receptor (NMDAR). Sigma-1 antagonists modify the chaperoning activity of sigma-1 receptor by increasing opioid signaling and decreasing NMDAR responses, consequently enhancing opioid antinociception and decreasing the sensory hypersensitivity that characterizes pathological pain conditions...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28314949/tolerance-and-cross-tolerance-to-the-antinociceptive-effects-of-oxycodone-and-the-imidazoline-i2-receptor-agonist-phenyzoline-in-adult-male-rats
#5
David A Thorn, Yanan Zhang, Jun-Xu Li
RATIONALE: Emerging evidence suggests the potential utility of combining opioids with imidazoline I2 receptor agonists for chronic pain. However, chronic pain management requires prolonged pharmacotherapy, and the consequence of such combination therapy remains unclear. OBJECTIVE: This study examined the anti-hyperalgesic effect of the opioid oxycodone, the selective I2 receptor agonist phenyzoline, alone and in combination, during prolonged treatment. METHODS: Von Frey filament test was used to examine the anti-hyperalgesic effect of drugs in complete Freund's adjuvant (CFA)-induced inflammatory pain or chronic constriction injury (CCI)-induced neuropathic pain in rats...
March 17, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28314819/depressive-like-behaviors-are-regulated-by-nox1-nadph-oxidase-by-redox-modification-of-nmda-receptor-1
#6
Masakazu Ibi, Junjie Liu, Noriaki Arakawa, Shiho Kitaoka, Ai Kawaji, Ken-Ichi Matsuda, Kazumi Iwata, Misaki Matsumoto, Masato Katsuyama, Kai Zhu, Satoshi Teramukai, Tomoyuki Furuyashiki, Chihiro Yabe-Nishimura
Involvement of reactive oxygen species (ROS) has been suggested in the development of psychiatric disorders. NOX1 is a non-phagocytic form of NADPH oxidase whose expression in the nervous system is negligible compared with other NOX isoforms. However, NOX1-derived ROS increase inflammatory pain and tolerance to opioid analgesia. To clarify the role of NOX1 in the brain, we examined depressive-like behaviors in mice deficient in Nox1 (Nox1(-/Y)). Depressive-like behaviors induced by chronic social defeat stress or administration of corticosterone (CORT) were significantly ameliorated in Nox1(-/Y) Generation of ROS was significantly elevated in the prefrontal cortex (PFC) of mice administrated with CORT, while NOX1 mRNA was up-regulated only in the ventral tegmental area (VTA) among brain areas responsible for emotional behaviors...
March 17, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28303899/the-behavioral-effects-of-the-antidepressant-tianeptine-require-the-mu-opioid-receptor
#7
Benjamin Adam Samuels, Katherine M Nautiyal, Andrew C Kruegel, Marjorie R Levinstein, Valerie M Magalong, Madalee M Gassaway, Steven G Grinnell, Jaena Han, Michael A Ansonoff, John E Pintar, Jonathan A Javitch, Dalibor Sames, René Hen
Depression is a debilitating chronic illness that affects around 350 million people worldwide. Current treatments, such as selective serotonin reuptake inhibitors (SSRIs), are not ideal because only a fraction of patients achieve remission. Tianeptine is an effective antidepressant with a previously unknown mechanism of action. We recently reported that tianeptine is a full agonist at the mu-opioid receptor (MOR). Here we demonstrate that the acute and chronic antidepressant-like behavioral effects of tianeptine in mice require MOR...
March 17, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28301370/debate-are-benzodiazepines-appropriate-treatments-for-patients-with-substance-use-disorders-yes
#8
Tae Woo Park
Benzodiazepines are a controversial treatment for anxiety in patients with substance use disorders. Concerns include risk of addiction, overdose, and diversion. But benzodiazepines are among the most effective and well-tolerated treatments for anxiety, and are safe for the majority of patients who take them. Though not appropriate for all cases, particularly in those with an active opioid use disorder, benzodiazepines should be considered as a treatment for patients with substance use disorders after careful weighing of benefits and harms...
March 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28299720/ketamine-infusion-as-a-counter-measure-for-opioid-tolerance-in-mechanically-ventilated-children-a-pilot-study
#9
Felix Neunhoeffer, Anja Hanser, Martin Esslinger, Vanja Icheva, Matthias Kumpf, Ines Gerbig, Michael Hofbeck, Jörg Michel
BACKGROUND: Drug rotation to prevent opioid tolerance is well recognized in chronic pain management. However, ketamine infusion as a counter measure for opioid tolerance is rarely described in mechanically ventilated children developing tolerance from prolonged opioid infusion. PATIENTS AND METHODS: We performed a retrospective study in a 14-bed medical-surgical-cardiac pediatric intensive care unit. Thirty-two mechanically ventilated children who had developed tolerance from prolonged intravenous infusion of opioids received a continuous intravenous infusion of ketamine as an opioid substitute for more than 2 days, scheduled in a drug rotation protocol...
March 15, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28298572/correction-wang-et-al-t394a-mutation-at-the-%C3%AE-opioid-receptor-blocks-opioid-tolerance-and-increases-vulnerability-to-heroin-self-administration-in-mice
#10
(no author information available yet)
No abstract text is available yet for this article.
March 15, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28296145/synthesis-and-opioid-activity-of-tyr1-z-cf-ch-gly2-and-tyr1-s-r-cf3ch-nh-gly2-leu-enkephalin-fluorinated-pep-tidomimetics
#11
Somnath N Karad, Mohan Pal, Thomas E Prisinzano, Rachel Saylor Crowley, Ryan A Altman
We describe the design, synthesis, and opioid activity of fluoroalkene (Tyr1-ψ[(Z)CF=CH]-Gly2) and trifluoroethylamine (Tyr1-ψ[(S)/(R)-CF3CH-NH]-Gly2) analogs of the endogenous opioid neuropeptide, Leu-enkephalin. The fluoroalkene peptidomimetic exihibited low nanomolar functional activity (5.0 ± 2 nM and 60 ± 15 nM for δ- and μ-opioid receptors, respectively) with a μ/δ-selectivity ratio that mimicked the natural peptide. However, the trifluoroethyl-amine peptidomimetics, irrespective of stereochemistry, did not activate the opioid receptors, which suggest that bulky CF3 substitu-ents are not tolerated at this position...
March 14, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28294636/indirect-treatment-comparison-of-two-non-invasive-patient-controlled-analgesia-treatments-for-acute-post-operative-pain-management
#12
Pablo Katz, Shweta Takyar, Pamela Palmer, Hiltrud Liedgens
OBJECTIVES: To evaluate the relative clinical efficacy, safety, and tolerability associated with two non-invasive patient-controlled analgesia (PCA) treatments, sufentanil sublingual tablet system (SSTS) and fentanyl iontophoretic patient-controlled transdermal system (PCTS). These two treatments have recently been approved in the EU for the management of acute moderate-to-severe post-operative pain in adult patients. METHODS: As no head-to-head trials comparing SSTS and PCTS currently exist, indirect treatment comparison (ITC) analyses were conducted to evaluate SSTS or PCTS versus intravenous (IV) morphine PCA...
March 15, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28292795/primary-care-management-of-opioid-use-disorders-abstinence-methadone-or-buprenorphine-naloxone
#13
REVIEW
Anita Srivastava, Meldon Kahan, Maya Nader
OBJECTIVE: To advise physicians on which treatment options to recommend for specific patient populations: abstinence-based treatment, buprenorphine-naloxone maintenance, or methadone maintenance. SOURCES OF INFORMATION: PubMed was searched and literature was reviewed on the effectiveness, safety, and side effect profiles of abstinence-based treatment, buprenorphine-naloxone treatment, and methadone treatment. Both observational and interventional studies were included...
March 2017: Canadian Family Physician Médecin de Famille Canadien
https://www.readbyqxmd.com/read/28291085/respiratory-effects-of-the-nociceptin-orphanin-fq-peptide-and-opioid-receptor-agonist-cebranopadol-in-healthy-human-volunteers
#14
Albert Dahan, Merel Boom, Elise Sarton, Justin Hay, Geert Jan Groeneveld, Meike Neukirchen, John Bothmer, Leon Aarts, Erik Olofsen
BACKGROUND: Cebranopadol is a novel strong analgesic that coactivates the nociceptin/orphanin FQ receptor and classical opioid receptors. There are indications that activation of the nociceptin/orphanin FQ receptor is related to ceiling in respiratory depression. In this phase 1 clinical trial, we performed a pharmacokinetic-pharmacodynamic study to quantify cebranopadol's respiratory effects. METHODS: Twelve healthy male volunteers received 600 μg oral cebranopadol as a single dose...
April 2017: Anesthesiology
https://www.readbyqxmd.com/read/28288815/rf313-an-orally-bioavailable-neuropeptide-ff-receptor-antagonist-opposes-effects-of-rf-amide-related-peptide-3-and-opioid-induced-hyperalgesia-in-rodents
#15
Khadija Elhabazi, Jean-Paul Humbert, Isabelle Bertin, Raphaelle Quillet, Valérie Utard, Martine Schmitt, Jean-Jacques Bourguignon, Emilie Laboureyras, Meric Ben Boujema, Guy Simonnet, Caroline Ancel, Valérie Simonneaux, Massimiliano Beltramo, Bernard Bucher, Tania Sorg, Hamid Meziane, Elodie Schneider, Benoit Petit-Demoulière, Brigitte Ilien, Frédéric Bihel, Frédéric Simonin
Although opiates represent the most effective analgesics, their use in chronic treatments is associated with numerous side effects including the development of pain hypersensitivity and analgesic tolerance. We recently identified a novel orally active neuropeptide FF (NPFF) receptor antagonist, RF313, which efficiently prevents the development of fentanyl-induced hyperalgesia in rats. In this study, we investigated the properties of this compound into more details. We show that RF313 exhibited a pronounced selectivity for NPFF receptors, antagonist activity at NPFF1 receptor (NPFF1R) subtype both in vitro and in vivo and no major side effects when administered in mice up to 30 mg/kg...
March 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28287359/opioid-prescribing-patterns-and-costs-in-a-large-group-of-patients-in-colombia
#16
Jorge Enrique Machado-Alba, Andres Gaviria-Mendoza, Camila A Vargas-Mosquera, Andrés Felipe Gil-Restrepo, Luis C Romero-Zapata
The potential for development of tolerance and dependence and the risk of side effects of opioids make it necessary to monitor their prescribing patterns in order to decrease the morbidity and mortality associated with their continued use. The objective of this study was to determine prescription patterns of opioid medication in a group of patients through a cross-sectional study on a population database of 3.5 million people. Patients with three months of continuous opioid use were identified. Pharmacological, co-medication and cost variables were analyzed...
March 2017: Journal of Pain & Palliative Care Pharmacotherapy
https://www.readbyqxmd.com/read/28283282/custirsen-in-combination-with-docetaxel-and-prednisone-for-patients-with-metastatic-castration-resistant-prostate-cancer-synergy-trial-a-phase-3-multicentre-open-label-randomised-trial
#17
Kim N Chi, Celestia S Higano, Brent Blumenstein, Jean-Marc Ferrero, James Reeves, Susan Feyerabend, Gwenaelle Gravis, Axel S Merseburger, Arnulf Stenzl, Andries M Bergman, Som D Mukherjee, Pawel Zalewski, Fred Saad, Cindy Jacobs, Martin Gleave, Johann S de Bono
BACKGROUND: Clusterin is a chaperone protein associated with treatment resistance and upregulated by apoptotic stressors such as chemotherapy. Custirsen is a second-generation antisense oligonucleotide that inhibits clusterin production. The aim of the SYNERGY trial was to investigate the effect of custirsen in combination with docetaxel and prednisone on overall survival in patients with metastatic castration-resistant prostate cancer. METHODS: SYNERGY was a phase 3, multicentre, open-label, randomised trial set at 134 study centres in 12 countries...
March 7, 2017: Lancet Oncology
https://www.readbyqxmd.com/read/28282499/non-opioid-medications-for-the-relief-of-chronic-breathlessness-current-evidence
#18
Carlo Barbetta, David C Currow, Miriam J Johnson
To evaluate systematically randomised clinical trials investigating non-opioid medications for the management and treatment of chronic breathlessness. Areas Covered: The evidence for the role of benzodiazepines, anxiolytics, selective serotonin re-uptake inhibitors (SSRIs), tricyclic antidepressants, antihistamines, cannabinoids, nebulized furosemide and herbal-based treatments were critically reviewed. Search of the Clinical Trials Registry (Clinicaltrial.gov) identified ongoing studies expected to generate new data in the near future in several classes of non-opioid medications for their net effect on chronic breathlessness...
March 10, 2017: Expert Review of Respiratory Medicine
https://www.readbyqxmd.com/read/28280384/tapentadol-extended-release-for-the-management-of-chronic-neck-pain
#19
Domenico Billeci, Flaminia Coluzzi
BACKGROUND: The role of opioids in the management of chronic neck pain is still poorly investigated. No data are available on tapentadol extended release (ER). In this article, we present 54 patients with moderate-to-severe chronic neck pain treated with tapentadol ER. PATIENTS AND METHODS: Patients received tapentadol ER 100 mg/day; dosage was then adjusted according to clinical needs. The following parameters were recorded: pain; Douleur Neuropathique 4 score; Neck Disability Index score; range of motion; pain-associated sleep interference; quality of life (Short Form [36] Health Survey); Patient Global Impression of Change (PGIC); Clinician GIC; opioid-related adverse effects; and need for other analgesics...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28276971/new-drugs-for-pain-management-in-advanced-cancer-patients
#20
Sebastiano Mercadante
Advanced cancer patients represent a frail population, often requiring aggressive pain management, particularly in the late stage of disease, when untreated pain is one the most important causes of suffering. Areas covered: In the last decade, a series of new analgesics have been introduced in the market to offer additional options amongst existent drugs. The characteristics of these drugs, their efficacy and tolerability are examined on the basis of existent studies. Expert opinion: Although new analgesic preparations have been developed in recent years, no specific drug has provided a better analgesic performance in comparison with others...
March 5, 2017: Expert Opinion on Pharmacotherapy
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