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Novel Opioid

Eric S Schwenk, Eugene R Viscusi
No abstract text is available yet for this article.
April 2018: Regional Anesthesia and Pain Medicine
Jeff Lapoint, Seth Meyer, Charles K Yu, Kristi L Koenig, Roneet Lev, Sayone Thihalolipavan, Katherine Staats, Christopher A Kahn
Introduction: Cannabinoid hyperemesis syndrome (CHS) is an entity associated with cannabinoid overuse. CHS typically presents with cyclical vomiting, diffuse abdominal pain, and relief with hot showers. Patients often present to the emergency department (ED) repeatedly and undergo extensive evaluations including laboratory examination, advanced imaging, and in some cases unnecessary procedures. They are exposed to an array of pharmacologic interventions including opioids that not only lack evidence, but may also be harmful...
March 2018: Western Journal of Emergency Medicine
Eva Ceskova, Petr Silhan
In spite of tremendous development in central nervous system research, current treatment is suboptimal, especially in severe mental disorders. In medicine, there are two main methods of improving the health care provided: seeking new treatment procedures and perfecting (optimizing) the existing ones. Optimization of treatment includes not only practical tools such as therapeutic drug monitoring but also implementation of general trends in the clinical practice. New pharmacological options include new more sophisticated forms of monoaminergic drugs, old drugs rediscovered on the base of a better understanding of pathophysiology of mental illnesses, and drugs aimed at new treatment targets...
2018: Neuropsychiatric Disease and Treatment
Johannes M Hugo, Kevin B Rebe, Evan Tsouroulis, Anthony Manion, Glenn de Swart, Helen Struthers, James A McIntyre
Chemsex is the colloquial term used for a specific pattern of drug use that is increasingly common among men who have sex with men (MSM) globally. The recreational substances employed are used specifically in a sexualized context. The reasons for chemsex among MSM are complex. The Anova Health Institute (Anova) provided harm-reduction services in Cape Town, South Africa in 2013 and 2014. This project, known as Tikking the Boxes had two objectives: first to provide direct harm-reduction services to drug-using MSM in Cape Town, South Africa, and second, to reduce HIV and hepatitis B and C transmission among this population...
March 21, 2018: Sexual Health
Marco Scardino, Tiziana D'Amato, Federica Martorelli, Giorgia Fenocchio, Vincenzo Simili, Berardo Di Matteo, Dario Bugada, Elizaveta Kon
BACKGROUND: Currently many TKA protocols rely on multimodal analgesic protocols with patient-controlled analgesia systems that administer opioids through a patient controlled IV infusion pump, in addition to concomitant peripheral nerve blocks and local anesthetics. Although effective, PCA IV opioids do not provide optimal results with fast track rehabilitation protocols. METHODS: The present is a retrospective study comparing the novel sublingual sufentanil PCA system (SSTS) to our standard of care foreseeing continuous femoral nerve block (cFNB) within a multimodal analgesic in a TKA fast-track protocol...
March 20, 2018: Journal of Experimental Orthopaedics
Rita Turnaturi, Carmela Parenti, Orazio Prezzavento, Agostino Marrazzo, Paschalina Pallaki, Zafiroula Georgoussi, Emanuele Amata, Lorella Pasquinucci
The opioid pharmacological profile of cis -(-)- N -normetazocine derivatives is deeply affected by the nature of their N -substituents. Here, our efforts were focused on the synthesis and pharmacological evaluation of novel derivatives of the lead LP1, a multitarget opioid analgesic compound featuring an N -phenylpropanamido substituent. LP1 derivatives 5a - d and 6a - d were characterized by flexible groups at the N -substituent that allow them to reposition themselves relative to cis -(-)- N -normetazocine nucleus, thus producing different pharmacological profiles at the mu, delta and kappa opioid receptors (MOR, DOR and KOR) in in vitro and in vivo assays...
March 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Aleksander H Erga, Ingvild Dalen, Anastasia Ushakova, Janete Chung, Charalampos Tzoulis, Ole Bjørn Tysnes, Guido Alves, Kenn Freddy Pedersen, Jodi Maple-Grødem
Introduction: Impulse control disorders (ICDs) are frequent non-motor symptoms in Parkinson's disease (PD), with potential negative effects on the quality of life and social functioning. ICDs are closely associated with dopaminergic therapy, and genetic polymorphisms in several neurotransmitter pathways may increase the risk of addictive behaviors in PD. However, clinical differentiation between patients at risk and patients without risk of ICDs is still troublesome. The aim of this study was to investigate if genetic polymorphisms across several neurotransmitter pathways were associated with ICD status in patients with PD...
2018: Frontiers in Neurology
Rachel I Anderson, David E Moorman, Howard C Becker
Understanding the neural systems that drive alcohol motivation and are disrupted in alcohol use disorders is of critical importance in developing novel treatments. The dynorphin and orexin/hypocretin neuropeptide systems are particularly relevant with respect to alcohol use and misuse. Both systems are strongly associated with alcohol-seeking behaviors, particularly in cases of high levels of alcohol use as seen in dependence. Furthermore, both systems also play a role in stress and anxiety, indicating that disruption of these systems may underlie long-term homeostatic dysregulation seen in alcohol use disorders...
March 11, 2018: Handbook of Experimental Pharmacology
J V Pergolizzi, R Taylor, J-A LeQuang, R B Raffa
WHAT IS KNOWN AND OBJECTIVE: Menthol has been used as a non-opioid pain reliever since ancient times. A modern understanding of its molecular mechanism of action could form the basis for generating targets for discovery of novel non-opioid analgesic drugs. METHODS: The PubMed database was queried using search words related to menthol, pain and analgesia. The results were limited to relevant preclinical studies and clinical trials and reviews published in English during the past 5 years, which yielded 31 reports...
March 10, 2018: Journal of Clinical Pharmacy and Therapeutics
Patricia Lavand'homme
PURPOSE OF REVIEW: Cesarean section is the most common surgical procedure performed in the world. Postoperative pain management remains a challenge, particularly in a context of enhanced recovery after surgery. Several barriers related to the specific condition of 'postpartum recovery' may prevent application of effective analgesia in this population. The present review focuses on novel approaches of cesarean section postoperative pain assessment, beyond pain-rating intensity, including objective patient-centered recovery parameters...
March 7, 2018: Current Opinion in Anaesthesiology
Jason N Moore, Marc R Gastonguay, Chee M Ng, Susan C Adeniyi-Jones, David E Moody, Wenfang B Fang, Michelle E Ehrlich, Walter K Kraft
Neonatal abstinence syndrome (NAS) is a condition affecting newborns that are exposed to an opioid in utero. In a randomized, controlled trial assessing the efficacy of buprenorphine and morphine in NAS, blood samples were analyzed from a subset of patients receiving buprenorphine along with NAS scores. The data were used to validate and adapt an existing model of buprenorphine in neonates and to identify relationships between buprenorphine or norbuprenorphine pharmacokinetics (PK) and efficacy or safety. The time to NAS stabilization was found to decrease with increasing buprenorphine exposure...
March 8, 2018: Clinical Pharmacology and Therapeutics
Yosuke Sugiyama, Tomoya Kataoka, Yoshihiko Tasaki, Yuki Kondo, Noriko Sato, Taku Naiki, Nobuhiro Sakamoto, Tatsuo Akechi, Kazunori Kimura
Background: Cancer-related neuropathic pain is sometimes unresponsive to multidrug treatment. Novel drugs are required to treat such severe pain without necessitating the use of adjuvant analgesics. Tapentadol is a new drug that has a dual mechanism as both an opioid agonist and noradrenalin reuptake inhibitor. The study objective was to investigate the effectiveness of oral tapentadol for relieving cancer-related neuropathic pain. Methods: A retrospective, single-center, open, non-randomized study was conducted at the Nagoya City University Hospital...
March 1, 2018: Japanese Journal of Clinical Oncology
William B White, Peter Kowey, Ulysses Diva, Mark Sostek, Raj Tummala
BACKGROUND: Naloxegol is a novel selective, peripherally acting μ-opioid receptor antagonist for treating opioid-induced constipation (OIC) in patients with chronic pain syndromes. We analyzed the cardiovascular (CV) safety of naloxegol based on data from its development program prior to approval by the US Food and Drug Administration in 2015. METHODS: Comprehensive CV safety analyses were performed in 4 clinical studies of naloxegol (12.5 and/or 25 mg) in patients with noncancer pain and OIC: two 12-week, double-blind, randomized studies; a 12-week, double-blind, extension study; and a 52-week, randomized, open-label study versus usual care...
January 1, 2018: Journal of Cardiovascular Pharmacology and Therapeutics
Michael P Webb, Erik M Helander, Bethany L Menard, Richard D Urman, Alan D Kaye
Chronic lower back pain is a significant disease that affects nearly 20% of the worldwide population. Along with hindering patients' quality of life, chronic lower back pain is considered to be the second most common cause of disability among Americans. Treating chronic lower back pain is often a challenge for providers, especially in light of our current opioid epidemic. With this epidemic and an increased aging population, there is an imminent need for development of new pharmacologic therapeutic options, which are not only effective but also pose minimal adverse effects to the patient...
2018: Therapeutics and Clinical Risk Management
Bhuvaneshwar Vaidya, Ali Ehsan Sifat, Vardan T Karamyan, Thomas J Abbruscato
Novel neuroprotective therapies are desperately needed to improve neuronal recovery after ischemic stroke and extend the therapeutic window or offset some of the adverse effects of tissue-type plasminogen activator (tPA). These advances could provide a more effective and safe therapeutic regimen for patients with ischemic stroke. The opioid system has gained intense interest over the past fw years and is currently being investigated as a viable target for the pharmacological treatment of stroke. In this review, we focus on different opioid receptors (ORs) and their distribution in the central nervous system (CNS), and the effect of ischemic stroke on their redistribution...
March 1, 2018: Drug Discovery Today
Felipe Vanz, Maíra Assunção Bicca, Vagner Fagnani Linartevichi, Marcelo Giachero, Leandro José Bertoglio, Thereza C Monteiro de Lima
The main κ opioid receptors (κORs) subtypes already described (κ1 ORs and κ2 ORs) are expressed in brain regions involved in aversive memory consolidation, including the dorsal hippocampus (DH). However, the role of DH κORs in consolidation of aversive memories with varied intensity and specificity is still uncertain. The present study aimed to investigate this question using pharmacological agents in rats subjected to a weak, moderate or strong contextual aversive conditioning (CAC) protocol. Antagonizing DH κORs with nor-binaltorphimine (nor-BNI), immediately after, but not 6 h later, a moderate CAC leads to intensified freezing behavior in the re-exposure to the paired context...
February 27, 2018: Neuropharmacology
Margot Roozekrans, Rutger van der Schrier, Leon Aarts, Elise Sarton, Monique van Velzen, Marieke Niesters, Albert Dahan, Erik Olofsen
BACKGROUND: Previous studies integrated opioid benefit and harm into one single function-the utility function-to determine the drug toxicity (respiratory depression) in light of its wanted effect (analgesia). This study further refined the concept of the utility function using the respiratory and analgesic effects of the opioid analgesic alfentanil as example. METHODS: Data from three previous studies in 48 healthy volunteers were combined and reanalyzed using a population pharmacokinetic-pharmacodynamic analysis to create utility probability functions...
March 2, 2018: Anesthesiology
K L Lentine, N N Lam, A S Naik, D A Axelrod, Z Zhang, V R Dharnidharka, G P Hess, D L Segev, R Ouseph, H Randall, T Alhamad, R Devraj, R Gadi, B L Kasiske, D C Brennan, M A Schnitzler
Evolving literature suggests that the epidemic of prescription opioid use affects the transplant population. We examined a novel database wherein national U.S. transplant registry records were linked to a large pharmaceutical claims warehouse (2007 to 2015) to characterize prescription opioid use before and after kidney transplant, and associations (adjusted hazard ratio,95% LCL aHR95% UCL ) with death and graft loss. Among 75,430 eligible patients, 43.1% filled opioids in the year before transplant. Use was more common among recipients who were women, white, unemployed, publicly insured, and with longer pre-transplant dialysis...
March 2, 2018: American Journal of Transplantation
Manuel P Pereira, Sonja Ständer
The prevalence of chronic pruritus (CP) in the general population is high and increases with age. Owing to high rates of comorbidities and polypharmacy in patients aged 65 or older, the clinical management of these patients is challenging. Areas covered: In this review, the authors discuss the available therapy options for patients aged ≥ 65 with CP, including emollients for dry skin, topical therapies, phototherapy and systemic agents for CP of various origins. Expert opinion: For multimorbid patients, topical substances and phototherapy constitute the best initial options...
April 2018: Expert Opinion on Pharmacotherapy
Lauren Folgosa Cooley, Sandra B Barker
The use of canine-assisted therapy (CAT) in healthcare is expanding and the purpose of this review is to highlight its potential use in the surgical patient. While CAT literature to date has detailed widespread benefits in blood pressure control and improving pain, anxiety, and stress, little research has been performed specifically in surgical patients who may benefit significantly from CAT interventions. Critical points highlighted herein are as follows: (1) Hypertension is common and significantly increases morbidity and mortality associated with elective surgery...
February 24, 2018: Alternative Therapies in Health and Medicine
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