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Opioid pharmacology

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https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#1
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a -opioid receptor (MOR) agonist/-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
April 20, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29675582/multifunctional-opioid-ligands
#2
Jessica P Anand, Deanna Montgomery
The opioid receptor system plays a major role in the regulation of mood, reward, and pain. The opioid receptors therefore make attractive targets for the treatment of many different conditions, including pain, depression, and addiction. However, stimulation or blockade of any one opioid receptor type often leads to on-target adverse effects that limit the clinical utility of a selective opioid agonist or antagonist. Literature precedent suggests that the opioid receptors do not act in isolation and that interactions among the opioid receptors and between the opioid receptors and other proteins may produce clinically useful targets...
April 20, 2018: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/29672145/trends-in-prescription-pain-medication-use-by-race-ethnicity-among-us-adults-with-noncancer-pain-2000-2015
#3
Jordan M Harrison, Pooja Lagisetty, Brian D Sites, Cui Guo, Matthew A Davis
OBJECTIVES: To examine national trends in the use of various pharmacological pain medication classes by race/ethnicity among the US pain population. METHODS: We used data from the Medical Expenditure Panel Survey to conduct a nationally representative, serial cross-sectional study of the noninstitutionalized US adult population from 2000 to 2015. We identified adults with moderate or severe self-reported pain and excluded individuals with cancer. We used complex survey design to provide national estimates of the percentage of adults with noncancer pain who received prescription pain medications among 4 groups: non-Hispanic White, non-Hispanic Black, Hispanic or Latino, and other...
April 19, 2018: American Journal of Public Health
https://www.readbyqxmd.com/read/29670398/remifentanil-induced-postoperative-hyperalgesia-current-perspectives-on-mechanisms-and-therapeutic-strategies
#4
REVIEW
Cristina Santonocito, Alberto Noto, Claudia Crimi, Filippo Sanfilippo
The use of remifentanil in clinical practice offers several advantages and it is used for a wide range of procedures, ranging from day-surgery anesthesia to more complex procedures. Nonetheless, remifentanil has been consistently linked with development of opioid-induced hyperalgesia (OIH), which is described as a paradoxical increase in sensitivity to painful stimuli that develops after exposure to opioid treatment. The development of OIH may cause several issues, delaying recovery after surgery and preventing timely patient's discharge...
2018: Local and Regional Anesthesia
https://www.readbyqxmd.com/read/29669731/involvement-of-activated-brain-stress-responsive-systems-in-excessive-and-relapse-alcohol-drinking-in-rodent-models-implications-for-therapeutics
#5
Yan Zhou, Mary Jeanne Kreek
Addictive diseases, including addiction to alcohol pose massive public health costs. Addiction is a chronic relapsing disease, caused by both the direct effects induced by drugs and persistent neuroadaptations at several (molecular, cellular and behavioral) levels. These drug-type specific neuro-adaptations are brought on largely by the reinforcing effects of drugs on the central nervous system and environment, including stress. Results from animal experiments have demonstrated important interactions between alcohol and the stress responsive systems...
April 18, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29669397/direct-detection-of-the-psychoactive-substance-mt-45-in-human-tissue-samples-by-probe-electrospray-ionization-tandem-mass-spectrometry
#6
Kiyotaka Usui, Tasuku Murata, Yuji Fujita, Yoshito Kamijo, Tomoki Hanazawa, Tomohiro Yoshizawa, Masato Funayama
Analyses of drugs and poisons in tissue samples are essential in forensic toxicology and pharmacology. However, current procedures for tissue analysis are laborious and time-consuming. Therefore, we assessed the utility of a newly devised probe electrospray ionization (PESI) technique with tandem mass spectrometry (MS/MS) for easy, ultra-rapid drug detection in human tissue samples. Using this system, typical pre-treatment procedures, such as solid-phase extraction, liquid-liquid extraction, deproteinization, or homogenization, can be avoided...
April 18, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29667437/transdermal-buprenorphine-for-moderate-chronic-noncancer-pain-syndromes
#7
Joseph V Pergolizzi, Flaminia Coluzzi, Robert Taylor
Chronic noncancer pain has remained a challenging clinical problem. Opioid analgesics are effective, but they are known to be associated with opioid use disorder and potentially treatment-limiting side effects. Buprenorphine is a Schedule III synthetic opioid in the USA with a chemical structure similar to that of morphine but with a longer duration of action, greater potency, and other unique pharmacological attributes. Its role in treatment of chronic noncancer pain may be broader than currently thought. Areas covered: The pharmacokinetics, pharmacodynamics, clinical efficacy, and safety profile of transdermal buprenorphine in moderate chronic noncancer pain syndromes patients will be discussed...
April 18, 2018: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/29662325/sonic-hedgehog-signaling-in-spinal-cord-contributes-to-morphine-induced-hyperalgesia-and-tolerance-through-upregulating-brain-derived-neurotrophic-factor-expression
#8
Su Liu, Jun-Li Yao, Xin-Xin Wan, Zhi-Jing Song, Shuai Miao, Ye Zhao, Xiu-Li Wang, Yue-Peng Liu
Purpose: Preventing opioid-induced hyperalgesia and tolerance continues to be a major clinical challenge, and the underlying mechanisms of hyperalgesia and tolerance remain elusive. Here, we investigated the role of sonic hedgehog (Shh) signaling in opioid-induced hyperalgesia and tolerance. Methods: Shh signaling expression, behavioral changes, and neurochemical alterations induced by morphine were analyzed in male adult CD-1 mice with repeated administration of morphine...
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29649695/doctor-shopping-of-opioid-analgesics-relative-to-benzodiazepines-a-pharmacoepidemiological-study-among-11-7-million-inhabitants-in-the-french-countries
#9
Camille Ponté, Marion Lepelley, Quentin Boucherie, Michel Mallaret, Maryse Lapeyre Mestre, Vincent Pradel, Joëlle Micallef
BACKGROUND: The abuse of prescription opioids and its subsequent consequences is an important public concern particularly in the USA. The literature on opioid analgesic abuse is scarce. OBJECTIVE: We assess the extent and risk of opioid analgesics abuse relative to benzodiazepines (BZD) using the doctor shopping method, taken into account the pharmacological characteristics (dosage, route of administration, extended or immediate release). METHODS: We used SNIIRAM database covering 11...
April 4, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29649035/pharmacological-characterization-of-levorphanol-a-g-protein-biased-opioid-analgesic
#10
Valerie Le Rouzic, Ankita Narayan, Amanda Hunkle, Gina F Marrone, Zhigang Lu, Susruta Majumdar, Jin Xu, Ying-Xian Pan, Gavril W Pasternak
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs. METHODS: Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays...
April 11, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29644468/-pharmacological-treatment-of-osteoarthritis-related-pain
#11
REVIEW
T A Nees, M Schiltenwolf
Joint pain due to osteoarthritis (OA) is often severe and disabling and affects a large proportion of the aging population impairing daily living and quality of life. Numerous pharmacological treatment approaches are available. Including major OA guidelines this review presents the current evidence of pharmacological therapies in OA-related pain and covers topical, oral and intraarticular treatment approaches. In patients with mild OA topical nonsteroidal antiinflammatory drugs (NSAIDs) can be recommended...
April 11, 2018: Der Schmerz
https://www.readbyqxmd.com/read/29627297/neuropharmacological-effects-of-essential-oil-from-the-leaves-of-croton-conduplicatus-kunth-and-possible-mechanisms-of-action-involved
#12
Raimundo Gonçalves de Oliveira Júnior, Christiane Adrielly Alves Ferraz, Juliane Cabral Silva, Roxana Braga de Andrade Teles, Mariana Gama E Silva, Tâmara Coimbra Diniz, Uiliane Soares Dos Santos, Ana Valéria Vieira de Souza, Carlos Eduardo Pereira Nunes, Marcos José Salvador, Vitor Prates Lorenzo, Lucindo José Quintans Junior, Jackson Roberto Guedes da Silva Almeida
ETHNOPHARMACOLOGICAL RELEVANCE: Croton conduplicatus Kunth (Euphorbiaceae) is a Brazilian aromatic medicinal plant, widely known as "quebra-faca". In folk medicine, its leaves and stem-barks are used as a natural analgesic for the treatment of headaches. AIM OF THE STUDY: In this study, we describe for the first time the neuropharmacological potential of the essential oil obtained from the leaves of Croton conduplicatus (EO) in experimental models of pain, anxiety and insomnia...
April 5, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29622502/chronic-pain-medication-management-of-older-populations-key-points-from-a-national-conference-and-innovative-opportunities-for-pharmacy-practice
#13
Julia Fiona-Maree Gilmartin-Thomas, J Simon Bell, Danny Liew, Carolyn A Arnold, Rachelle Buchbinder, Colin Chapman, Flavia Cicuttini, Malcolm Dobbin, Stephen J Gibson, Melita J Giummarra, Jenny Gowan, Benny Katz, Dan L Lubman, Matthew McCrone, Jennifer Pilgrim, Anneliese Synnot, Eleanor van Dyk, Barbara Workman, John McNeil
OBJECTIVE: Inappropriate use of pain medication has serious consequences for older populations. Experts in the field have noted an increase in opioid prescriptions, and opioid-related hospitalisations and deaths among this vulnerable population. In the pursuit of educating pharmacists, physicians, allied healthcare professionals, researchers, academics and the public facing the challenges of chronic pain medication management, 'The Inaugural Monash University School of Public Health and Preventive Medicine (SPHPM) Best Practice in Chronic Pain Medication Management Day Conference' was held in December 2016 at the Alfred Medical Research and Education Precinct (Melbourne, Australia)...
March 19, 2018: Research in Social & Administrative Pharmacy: RSAP
https://www.readbyqxmd.com/read/29619540/understanding-osteoporotic-pain-and-its-pharmacological-treatment
#14
REVIEW
R Vellucci, R Terenzi, J A Kanis, H G Kress, R D Mediati, J-Y Reginster, R Rizzoli, M L Brandi
Osteoporosis, a disorder that affects millions of people worldwide, is characterized by decreased bone mass and microstructural alterations giving rise to an increased risk of fractures. Osteoporotic fractures can cause acute and chronic pain that mainly affects elderly patients with multiple comorbidities and commonly on different drug regimens. The aim of this paper is to summarize the pathogenesis and systemic treatment of osteoporotic pain. This narrative review summarizes the main pathogenetic aspects of osteoporotic pain and the cornerstones of its treatment...
April 4, 2018: Osteoporosis International
https://www.readbyqxmd.com/read/29616344/novel-pharmacological-nonopioid-therapies-in-chronic-pain
#15
REVIEW
Alan David Kaye, Elyse M Cornett, Brendon Hart, Shilpadevi Patil, Andrew Pham, Matthew Spalitta, Kenneth F Mancuso
PURPOSE OF REVIEW: Opioid use and abuse has led to a worldwide opioid epidemic. And while opioids are clinically useful when appropriately indicated, they are associated with a wide range of dangerous side effects and whether they are effective at treating or eliminating chronic pain is controversial. There has long been a need for the development of nonopioid alternative treatments for patients that live in pain, and until recently, only a few effective treatments were available. Today, there are a wide range of nonopioid treatments available including NSAIDs, acetaminophen, corticosteroids, nerve blocks, SSRIs, neurostimulators, and anticonvulsants...
April 3, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29615715/blocking-interleukin-4-enhances-efficacy-of-vaccines-for-treatment-of-opioid-abuse-and-prevention-of-opioid-overdose
#16
Megan Laudenbach, Federico Baruffaldi, Christine Robinson, Philipp Carter, Davis Seelig, Carly Baehr, Marco Pravetoni
Vaccines offer an option to treat heroin and prescription opioid abuse and prevent fatal overdoses. Opioid vaccines elicit antibodies that block opioid distribution to the brain and reduce opioid-induced behavioral effects and toxicity. The major limitation to the translation of addiction vaccines is that efficacy is observed only in subjects achieving optimal drug-specific serum antibody levels. This study tested whether efficacy of a vaccine against oxycodone is increased by immunomodulators targeting key cytokine signaling pathways involved in B and T cell lymphocyte activation...
April 3, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29614184/neonatal-abstinence-syndrome-advances-in-diagnosis-and-treatment
#17
Elisha M Wachman, Davida M Schiff, Michael Silverstein
Importance: Neonatal abstinence syndrome, which occurs as a result of in utero opioid exposure, affects between 6.0 and 20 newborns per 1000 live US births. There is substantial variability in how neonatal abstinence syndrome is diagnosed and managed. Objective: To summarize key studies examining the diagnosis and management (both pharmacologic and nonpharmacologic) of neonatal abstinence syndrome published during the past 10 years. Evidence Review: PubMed, Web of Science, and CINAHL were searched for articles published between July 1, 2007, and December 31, 2017...
April 3, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29601303/the-opioid-epidemic-and-pregnancy-implications-for-anesthetic-care
#18
Britany L Raymond, Bradley T Kook, Michael G Richardson
PURPOSE OF REVIEW: This review summarizes evolving knowledge regarding adverse maternal, fetal, and neonatal effects of opioid exposure during pregnancy, and current treatment options for opioid use disorder (OUD). Maternal and fetal implications of maternal opioid maintenance with methadone and buprenorphine are described. Finally, acute and chronic pain management strategies in opioid-tolerant parturients are reviewed. RECENT FINDINGS: Opioid use among parturients has risen dramatically, with opioid use during pregnancy as high as 20%...
March 29, 2018: Current Opinion in Anaesthesiology
https://www.readbyqxmd.com/read/29597083/traumatic-brain-injury-and-receipt-of-prescription-opioid-therapy-for-chronic-pain-in-iraq-and-afghanistan-veterans-do-clinical-practice-guidelines-matter
#19
Karen H Seal, Daniel Bertenthal, Deborah E Barnes, Amy L Byers, Carolyn J Gibson, Kristine Yaffe
Clinical practice guidelines admonish against prescribing opioids for individuals with chronic pain and traumatic brain injury (TBI) given increased risk for adverse outcomes, yet no studies have described opioid prescribing patterns in these higher risk patients. Between October 2007 and March 2015, 53,124 Iraq and Afghanistan veterans with chronic pain not prescribed opioids in the previous year were followed for one year after completing a Comprehensive TBI Evaluation (CTBIE) within Department of Veterans Affairs health care facilities...
March 26, 2018: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29596288/management-of-intracranial-pressure-part-i-pharmacologic-interventions
#20
Tara L Sacco, Samantha A Delibert
Dangerous, sustained elevation in intracranial pressure (ICP) is a risk for any patient following severe brain injury. Intracranial pressure elevations that do not respond to initial management are considered refractory to treatment, or rICP. Patients are at significant risk of secondary brain injury and permanent loss of function resulting from rICP. Both nonpharmacologic and pharmacologic interventions are utilized to intervene when a patient experiences either elevation in ICP or rICP. In part 1 of this 2-part series, pharmacologic interventions are discussed...
May 2018: Dimensions of Critical Care Nursing: DCCN
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