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Opioid pharmacology

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https://www.readbyqxmd.com/read/29225793/recent-advances-in-acute-pain-management-understanding-the-mechanisms-of-acute-pain-the-prescription-of-opioids-and-the-role-of-multimodal-pain-therapy
#1
REVIEW
Richa Wardhan, Jacques Chelly
In this review, we discuss advances in acute pain management, including the recent report of the joint American Pain Society and American Academy of Pain Medicine task force on the classification of acute pain, the role of psychosocial factors, multimodal pain management, new non-opioid therapy, and the effect of the "opioid epidemic". In this regard, we propose that a fundamental principle in acute pain management is identifying patients who are most at risk and providing an "opioid free anesthesia and postoperative analgesia"...
2017: F1000Research
https://www.readbyqxmd.com/read/29223172/association-between-the-use-of-benzodiazepines-and-opioids-with-the-risk-of-falls-and-hip-fractures-in-older-adults
#2
Manuel E Machado-Duque, Juan Pablo Castaño-Montoya, Diego A Medina-Morales, Alejandro Castro-Rodríguez, Alexandra González-Montoya, Jorge E Machado-Alba
BACKGROUND: To determine the association between the use of opioids and benzodiazepines and the risk of falls with hip fracture in populations older than 65 years in Colombia. METHODS: A case-control study with patients older than 65 years with diagnosis of hip fracture. Two controls were obtained per case. The drugs dispensed in the previous 30 days were identified. Sociodemographic, diagnostic, pharmacological (opioids and benzodiazepines), and polypharmacy variables were analyzed...
December 10, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29219169/pharmacokinetics-and-pharmacodynamics-of-sublingual-sufentanil-for-postoperative-pain-management
#3
REVIEW
T van de Donk, S Ward, R Langford, A Dahan
Achieving successful treatment of postoperative pain remains a challenge. Recently, a sufentanil sublingual tablet system has been developed for treatment of moderate-to-severe postoperative pain. The phenylpiperidine sufentanil is a potent analgesic that rapidly crosses the blood-brain barrier and selectively activates central μ-opioid receptors. The system makes use of a hand-held dispenser system, which contains forty 15-μg sufentanil sublingual micro-tablets. The patient can release one tablet at 20-min intervals using a unique radiofrequency adhesive tag, which is wrapped around the patient's thumb...
December 8, 2017: Anaesthesia
https://www.readbyqxmd.com/read/29219048/sodium-oxybate-therapy-for-the-treatment-of-alcohol-withdrawal-syndrome-and-the-maintenance-of-alcohol-abstinence
#4
Carmen Mannucci, Simona Pichini, Elvira Ventura Spagnolo, Fabrizio Calapai, Sebastiano Gangemi, Michele Navarra, Gioacchino Calapai
BACKGROUND: Gamma-hydroxybutyrate (GHB or sodium oxybate) is both an exogenous and endogenous molecule with neuromodulator properties. In the United States, GHB is an approved drug for the treatment of narcolepsy and narcolepsy with cataplexy in adults. In some European Union countries, sodium oxybate is applied for the treatment of opioid and alcohol withdrawal. OBJECTIVE: The aim of the present review was to describe the state of art of the pre-clinical research and the clinical evidence related to GHB used alone or in combination with other treatments in alcohol withdrawal syndrome and alcohol abstinence maintenance...
December 7, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/29211767/investigating-endogenous-%C3%A2%C2%B5-opioid-receptors-in-human-keratinocytes-as-pharmacological-targets-using-novel-fluorescent-ligand
#5
Cheryl Leong, Christine Neumann, Srinivas Ramasamy, Bhimsen Rout, Lim Yi Wee, Mei Bigliardi-Qi, Paul L Bigliardi
Opioids in skin function during stress response, regeneration, ageing and, particularly in regulating sensation. In chronic pruritus, topical treatment with Naltrexone changes μ-opioid receptor (μ-OR) localization to relieve itch. The molecular mechanisms behind the effects of Naltrexone on μ-OR function in reduction of itching behavior has not been studied. There is an immediate need to understand the endogenous complexity of μ-OR dynamics in normal and pathological skin conditions. Here we evaluate real-time behavior of μ-OR-Endomorphine complexes in the presence of agonist and antagonists...
2017: PloS One
https://www.readbyqxmd.com/read/29207922/effect-of-steady-state-methadone-on-high-fructose-corn-syrup-consumption-in-rats
#6
Stephen Daniels, Mick Pratt, Yan Zhou, Francesco Leri
Patients undergoing methadone maintenance treatment self-report enhanced preferences for, and excessive consumption of, foods rich in sugar. However, it is unclear whether these are direct pharmacological effects of methadone or the consequences of metabolic dysfunctions induced by addiction to illicit opiates. Hence, the current study in drug-naïve male Sprague-Dawley rats explored the effects of steady-state methadone delivered by osmotic mini-pumps (13 days; 0, 10, 30 mg/kg/day) on consumption of rat chow and a palatable, sweet, liquid high fructose corn syrup solution...
December 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29207895/nonpharmacological-management-of-neonatal-abstinence-syndrome-a-review-of-the-literature
#7
Gareth Ryan, Anishnaabe Bimaadiziwin, Joe Dooley, Lianne Gerber Finn, Len Kelly
BACKGROUND: Infants with neonatal abstinence syndrome (NAS) experience withdrawal that occurs as a result of termination of placental opioid supply following delivery. Common symptoms include restlessness, tremors, agitation and gastrointestinal disturbances. Severe NAS is often treated using opioids and/or sedatives. Although commonly employed effectively in neonatal care, there is a lack of published information regarding nonpharmacological management of the NAS infant. OBJECTIVE: The purpose of this review was to summarize the current literature on nonpharmacological management of NAS...
December 5, 2017: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/29202454/fentanyl-related-designer-drugs-w-18-and-w-15-lack-appreciable-opioid-activity-in-vitro-and-in-vivo
#8
Xi-Ping Huang, Tao Che, Thomas J Mangano, Valerie Le Rouzic, Ying-Xian Pan, Michael D Cameron, Michael H Baumann, Gavril W Pasternak, Bryan L Roth
W-18 (4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide) and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide). Here, we describe the comprehensive pharmacological profiles of W-18 and W-15, as examination of their structural features predicted that they might lack opioid activity. We found W-18 and W-15 to be without detectible activity at μ, δ, κ, and nociception opioid receptors in a variety of assays...
November 16, 2017: JCI Insight
https://www.readbyqxmd.com/read/29199028/sex-dependent-influences-of-morphine-and-its-metabolites-on-pain-sensitivity-in-the-rat
#9
H H Doyle, A Z Murphy
Preclinical studies report that the effective dose for morphine is approximately 2-fold higher in females than males. Following systemic administration, morphine is metabolized via Phase II glucuronidation in the liver and brain into two active metabolites: morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G), each possessing distinct pharmacological profiles. M6G binds to μ opioid receptors and acts as a potent analgesic. In contrast, M3G binds to toll-like receptor 4 (TLR4), initiating a neuroinflammatory response that directly opposes the analgesic effects of morphine and M6G...
November 30, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/29198512/understanding-the-role-of-serotonin-in-female-hypoactive-sexual-desire-disorder-and-treatment-options
#10
REVIEW
Harry A Croft
BACKGROUND: The neurobiology of sexual response is driven in part by dopamine and serotonin-the former modulating excitatory pathways and the latter regulating inhibitory pathways. Neurobiological underpinnings of hypoactive sexual desire disorder (HSDD) are seemingly related to overactive serotonin activity that results in underactive dopamine activity. As such, pharmacologic agents that decrease serotonin, increase dopamine, or some combination thereof, have therapeutic potential for HSDD...
December 2017: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29196181/cyclopeptide-dmt-d-lys-p-cf3-phe-phe-asp-nh2-a-novel-g-protein-biased-agonist-of-the-mu-opioid-receptor
#11
Justyna Piekielna-Ciesielska, Federica Ferrari, Girolamo Calo', Anna Janecka
Opioid peptides and alkaloid drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor which belongs to the G protein-coupled receptor (GPCR) family. A new important pharmacological concept in the field of GPCRs is biased agonism. Two mu receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 (F-81), were evaluated in terms of their ability to promote or block mu receptor/G protein and mu receptor/β-arrestin interactions...
November 28, 2017: Peptides
https://www.readbyqxmd.com/read/29191753/melanin-concentrating-hormone-acts-through-hypothalamic-kappa-opioid-system-and-p70s6k-to-stimulate-acute-food-intake
#12
Amparo Romero-Picó, Estrella Sanchez-Rebordelo, Monica Imbernon, David González-Touceda, Cintia Folgueira, Ana Senra, Johan Fernø, Clémence Blouet, Roberto Cabrera, Margriet van Gestel, Roger A Adan, Miguel López, Rafael Maldonado, Ruben Nogueiras, Carlos Diéguez
Melanin-Concentrating Hormone (MCH) is one of the most relevant orexigenic factors specifically located in the lateral hypothalamic area (LHA), with its physiological relevance demonstrated in studies using several genetically manipulated mice models. However, the central mechanisms controlling MCH-induced hyperphagia remain largely uncharacterized. Here, we show that central injection of MCH in mice deficient for kappa opoid receptor (k-OR) failed to stimulate feeding. To determine the hypothalamic area responsible for this MCH/k-OR interaction, we performed virogenetic studies and found that downregulation of k-OR by adeno-associated viruses (shOprk1-AAV) in LHA, but not in other hypothalamic nuclei, was sufficient to block MCH-induced food intake...
December 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29191577/electrical-stimulation-of-the-insular-cortex-as-a-novel-target-for-the-relief-of-refractory-pain-an-experimental-approach-in-rodents
#13
Luiz Fabio Dimov, Elaine Flamia Toniolo, Heloísa Alonso-Matielo, Daniel Ciampi de Andrade, Luis Garcia-Larrea, Gerson Ballester, Manoel Jacobsen Teixeira, Camila Squarzoni Dale
Cortical electrical stimulation (CES) has shown to be an effective therapeutic alternative for neuropathic pain refractory to pharmacological treatment. The primary motor cortex(M1) was the main cortical target used in the vast majority of both invasive and non-invasive studies. Despite positive results M1-based approaches still fail to relieve pain in a significant proportion of individuals. It has been advocated that the direct stimulation of cortical areas directly implicated in the central integration of pain could increase the efficacy of analgesic brain stimulation...
November 27, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29189365/using-integrative-medicine-in-pain-management-an-evaluation-of-current-evidence
#14
REVIEW
Yuan-Chi Lin, Limeng Wan, Robert N Jamison
Complementary medicine therapies are frequently used to treat pain conditions such as headaches and neck, back, and joint pain. Chronic pain, described as pain lasting longer than 3-6 months, can be a debilitating condition that has a significant socioeconomic impact. Pharmacologic approaches are often used for alleviating chronic pain, but recently there has been a reluctance to prescribe opioids for chronic noncancer pain because of concerns about tolerance, dependence, and addiction. As a result, there has been increased interest in integrative medicine strategies to help manage pain and to reduce reliance on prescription opioids to manage pain...
December 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29184439/ultrasound-guided-rectus-sheath-block-caudal-analgesia-or-surgical-site-infiltration-for-pediatric-umbilical-herniorrhaphy-a-prospective-double-blinded-randomized-comparison-of-three-regional-anesthetic-techniques
#15
Lance M Relland, Joseph D Tobias, David Martin, Giorgio Veneziano, Ralph J Beltran, Christopher McKee, Tarun Bhalla
Background: Umbilical hernia repair is a common pediatric surgical procedure. While opioid analgesics are a feasible option and have long been a mainstay in the pharmacological intervention for pain, the effort to improve care and limit opioid-related adverse effects has led to the use of alternative techniques, including regional anesthesia. The current study prospectively compares the analgesic efficacy of three techniques, including caudal epidural blockade, peripheral nerve blockade, and local wound infiltration, in a double-blinded study...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29183228/recommendations-for-buprenorphine-and-methadone-therapy-in-opioid-use-disorder-a-european-consensus
#16
Maurice Dematteis, Marc Auriacombe, Oscar D'Agnone, Lorenzo Somaini, Néstor Szerman, Richard Littlewood, Farrukh Alam, Hannu Alho, Amine Benyamina, Julio Bobes, Jean Pierre Daulouede, Claudio Leonardi, Icro Maremmani, Marta Torrens, Stephan Walcher, Michael Soyka
Management of patients with opioid use disorder (OUD) commonly includes opioid agonist therapy (OAT) as a part of an integrated treatment plan. These interventions are associated with proven benefits to the individual and society. Areas covered: The use of methadone and buprenorphine within an integrated treatment plan in the management of patients with OUD: this work provides consensus recommendation on pharmacotherapy in OUD to assist clinicians with practical decision making in this field. Expert opinion: Pharmacotherapy is recommended as part of an integrated OUD treatment approach with psychosocial interventions, with the goal of reducing risks of illicit opioid use, overdose mortality, infection with HIV or HCV, improving health, psychological and social outcomes...
November 29, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29182997/bioanalytical-methods-for-the-quantification-of-hydromorphone-fentanyl-norfentanyl-morphine-morphine-3%C3%A3-glucuronide-and-morphine-6%C3%A3-glucuronide-in-human-plasma
#17
Peter de Bruijn, Evelien J M Kuip, Mei-Ho Lam, Ron H J Mathijssen, Stijn L W Koolen
The aim of this study was to develop an assay for the quantification of hydromorphone, morphine, fentanyl and the metabolites norfentanyl, morphine-3ß-glucuronide and morphine-6ß-glucuronide in human plasma to support pharmacokinetic studies investigating the large interpatient variability in response to opioid treatment. For the quantitation of hydromorphone, morphine, fentanyl and its metabolite norfentanyl aliquots of 200μL human potassium EDTA plasma were deproteinized with deuterated internal standards in a mixture of acetonitrile and acetone, followed by a liquid-liquid extraction with 4% ammonium hydroxide and ethyl acetate...
November 17, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29180552/neighborhood-socioeconomic-status-and-receipt-of-opioid-medication-for-new-back-pain-diagnosis
#18
Sarah Gebauer, Joanne Salas, Jeffrey F Scherrer
BACKGROUND: Although treatment for new back pain is heavily guideline driven, deviations occur frequently. Neighborhood socioeconomic status (nSES) may contribute to these deviations. OBJECTIVE: Determine whether nSES is associated with type of treatment provided for patients seeking treatment for new back pain in primary care clinics. METHODS: This retrospective cohort was conducted in academic internal and family medicine practices. Data were examined from the Primary Care Patient Data Registry...
November 2017: Journal of the American Board of Family Medicine: JABFM
https://www.readbyqxmd.com/read/29170340/43%C3%A2-management-of-acute-low-back-pain-in-the-ed-a-systematic-review
#19
Jane Ashbrook, Nikos Rodgdakis, Peter Goodwin, Gill Yeowell, Michael Callaghan
STUDY OBJECTIVE: There is no consensus on the management of low back pain in the ED and evidence suggests that these patients are likely to receive unwarranted imaging and inappropriate opioid prescription.The purpose of this study is to review the available literature pertaining to the clinical management of acute low back pain in the ED. METHODS: The Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) and Realist And Meta-narrative Evidence Syntheses: Evolving Standards (RAMESES) guidelines were observed during this review...
December 2017: Emergency Medicine Journal: EMJ
https://www.readbyqxmd.com/read/29162628/etiopathogenesis-and-pharmacological-prevention-of-a-type-2-diabetes-model-in-male-mice
#20
Alberto Loizzo, Santi M Spampinato, Gabriele Campana, Stefano Loizzo
We describe a stress-derived type-2 diabetes model in male mice, and formulate new hypotheses on how the model was induced, how diabetes-like alterations were prevented through specific pharmacological treatments, and how its possible neuroendocrine pathogenesis could be hypothesized. Pregnant females arrived in our laboratory on their 14th day of conceptional age. After birth, control mice never showed any apparent behavioral-metabolic-endocrine alterations. However, application of postnatal stress (brief mother deprivation, plus sham injection, daily from birth to weaning), was followed in adult male mice by two series of diabetes-like alterations...
November 21, 2017: Journal of Pharmacology and Experimental Therapeutics
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