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Opioid pharmacology

Maria Elena Giusepponi, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura, Laura Mattioli, Alan Hudson, Eleonora Diamanti, Fabio Del Bello, Mario Giannella, Valerio Mammoli, Corinne Dalila Paoletti, Alessandro Piergentili, Maria Pigini, Wilma Quaglia
Tolerance and dependence associated with chronic opioid exposure result from molecular, cellular, and neural network adaptations. Such adaptations concern opioid and nonopioid systems, including α2-adrenoceptors (α2-ARs) and I1- and I2-imidazoline binding sites (IBS). Agmatine, one of the hypothesized endogenous ligands of IBS, targeting several systems including α2-ARs and IBS, proved to be able to regulate opioid-induced analgesia and to attenuate the development of tolerance and dependence. Interested in the complex pharmacological profile of agmatine and considering the nature of its targets, we evaluated two series of imidazolines, rationally designed to simultaneously interact with I1-/I2-IBS or I1-/I2-IBS/α2-ARs...
October 13, 2016: ACS Medicinal Chemistry Letters
Adele Sandra Budiansky, Michael P Margarson, Naveen Eipe
Increasing numbers of patients with morbid obesity are presenting for surgery, and their acute pain management requires an evidence-based clinical update. The objective of this study was to complete a literature review for acute pain management in morbid obesity and provide an evidence-based clinical update with recommendations. Using standardized search terms, in March 2015, we completed a literature search to determine evidence for different acute pain pharmacologic modalities in morbid obesity. For each modality, the highest level of evidence was ascertained, and recommendations for each pharmacologic modality are presented...
September 19, 2016: Surgery for Obesity and related Diseases: Official Journal of the American Society for Bariatric Surgery
Steffen T Simon, Irene J Higginson, Sara Booth, Richard Harding, Vera Weingärtner, Claudia Bausewein
BACKGROUND: This is an updated version of the original Cochrane review published in Issue 1, 2010, on 'Benzodiazepines for the relief of breathlessness in advanced malignant and non-malignant diseases in adults'. Breathlessness is one of the most common symptoms experienced in the advanced stages of malignant and non-malignant disease. Benzodiazepines are widely used for the relief of breathlessness in advanced diseases and are regularly recommended in the literature. At the time of the previously published Cochrane review, there was no evidence for a beneficial effect of benzodiazepines for the relief of breathlessness in people with advanced cancer and chronic obstructive pulmonary disease (COPD)...
October 20, 2016: Cochrane Database of Systematic Reviews
Amit Agrawal, Veena Asthana, J P Sharma, Vineeta Gupta
BACKGROUND: Subarachnoid block is the preferred technique for providing anesthesia for patients undergoing cesarean section. Various pharmacological agents in added to local anesthetics (LA) modify their original effects in terms of block characteristics and quality of analgesia. However, there is ongoing debate about this practice of using adjuncts with LA. We tested whether addition of lipophilic versus lipophobic opioids to LA gives any clinical benefits to maternal and fetal outcome when used in these patients requiring spinal anesthesia...
September 2016: Anesthesia, Essays and Researches
Chris Maher, Martin Underwood, Rachelle Buchbinder
Non-specific low back pain affects people of all ages and is a leading contributor to disease burden worldwide. Management guidelines endorse triage to identify the rare cases of low back pain that are caused by medically serious pathology, and so require diagnostic work-up or specialist referral, or both. Because non-specific low back pain does not have a known pathoanatomical cause, treatment focuses on reducing pain and its consequences. Management consists of education and reassurance, analgesic medicines, non-pharmacological therapies, and timely review...
October 10, 2016: Lancet
Manuela L Ferreira, Andrew McLachlan
Sciatica is a debilitating condition affecting approximately 25 % of the population. Typically, the patient will complain of lower limb pain that is more severe than pain in the lower back, usually accompanied by numbness and motor weakness. Most international guidelines recommend pharmacological management for the pain relief of sciatica, including paracetamol, non-steroidal anti-inflammatory drugs, opioid analgesics, anticonvulsants, and corticosteroids, among others. However, the evidence for most of these pharmacological options is scarce, and the majority of clinical trials exclude older patients...
October 13, 2016: Drugs & Aging
Maria Jenelyn M Alviar, Tom Hale, Monalisa Dungca
BACKGROUND: This is an updated version of the original Cochrane review published in Issue 12, 2011. Phantom limb pain (PLP) is pain that arises in the missing limb after amputation and can be severe, intractable, and disabling. Various medications have been studied in the treatment of phantom pain. There is currently uncertainty in the optimal pharmacologic management of PLP. OBJECTIVES: This review aimed to summarise the evidence of effectiveness of pharmacologic interventions in treating PLP...
October 14, 2016: Cochrane Database of Systematic Reviews
Joseph C Dort, D Gregory Farwell, Merran Findlay, Gerhard F Huber, Paul Kerr, Melissa A Shea-Budgell, Christian Simon, Jeffrey Uppington, David Zygun, Olle Ljungqvist, Jeffrey Harris
Importance: Head and neck cancers often require complex, labor-intensive surgeries, especially when free flap reconstruction is required. Enhanced recovery is important in this patient population but evidence-based protocols on perioperative care for this population are lacking. Objective: To provide a consensus-based protocol for optimal perioperative care of patients undergoing head and neck cancer surgery with free flap reconstruction. Evidence Review: Following endorsement by the Enhanced Recovery After Surgery (ERAS) Society to develop this protocol, a systematic review was conducted for each topic...
October 13, 2016: JAMA Otolaryngology—Head & Neck Surgery
Marcelina Jasmine Silva, Andrea Rubinstein
Buprenorphine, a semisynthetic thebaine derivative, is a unique opioid, as it has activity at multiple receptors, including mu (partial agonist), kappa (antagonist), OLR-1 (agonist), and delta (antagonist). Because buprenorphine's pharmacology is relatively complex, misconceptions about its actions are common. Most other opioids act solely or predominately as full mu receptor agonists. Common practice at many institutions calls for the cessation of regular buprenorphine use 48-72 hours prior to surgery. This practice is based on three foundational theories that have come from scant data about the properties of buprenorphine: (1) that buprenorphine is only a partial mu agonist and therefore is not a potent analgesic; (2) because buprenorphine has a ceiling effect on respiratory depression, it also has a ceiling effect on analgesia; and (3) that buprenorphine acts as a "blockade" to the analgesic effects of other opiates when coadministered due to its strong binding affinity...
October 13, 2016: Journal of Pain & Palliative Care Pharmacotherapy
Daniel Ayanga, Daryl Shorter, Thomas R Kosten
Opioid Use Disorder (OUD) is a significant public health concern, negatively impacting the medical, psychological, and social domains of an individual's life as well as creating substantial burdens for society. Effective treatment interventions are necessary for reduction of OUD and its consequences. Pharmacotherapy represents a central component of management. Areas Covered: This review focuses on pharmacologic strategies for OUD treatment, discussing both primary as well as adjunctive therapy modalities. We will discuss both medications used during detoxification to treat withdrawal, as well as those used as maintenance therapy...
October 13, 2016: Expert Opinion on Pharmacotherapy
E H Y Yu, D H D Tran, S W Lam, M G Irwin
The unique pharmacology of remifentanil makes it a popular intra-operative analgesic. Short-acting opioids like remifentanil have been associated with acute opioid tolerance and/or opioid-induced hyperalgesia, two phenomena which have different mechanisms and are pharmacologically distinct. Clinical studies show heterogeneity of remifentanil infusion regimens, durations of infusion, maintenance of anaesthesia, cumulative dose of remifentanil and pain measures, which makes it difficult to draw conclusions about the incidence of acute tolerance or hyperalgesia...
November 2016: Anaesthesia
Laura M Best, Leah L Zhao, Tina Scardochio, Paul B S Clarke
RATIONALE: Adult rat 50-kHz vocalizations have been proposed to indicate a positive affective state, putatively revealed by a predominance of trill calls over flat calls. However, short-term exposure to non-sedative doses of the euphorigen morphine suppresses calling, with no discernible shift in trill or flat call prevalence. OBJECTIVES: This study aimed to determine whether morphine acutely increases 50-kHz call rates or alters the relative prevalence of trill or flat calls, after long-term morphine exposure or acute pharmacological pretreatment...
October 11, 2016: Psychopharmacology
Mahboubeh Firouzkouhi Moghadam, Seyed-Sepehr Hashemian, Masoud Pishjoo, Sanaz Ghasemi, Ahmad Hajebi, Alireza Noroozi
BACKGROUND: About 10 million children worldwide live or work on the street. International reports estimate the prevalence of substance use among street children to be between 25% - 90%, which is who were referredntal disorders and high-risk behaviors. OBJECTIVES: The objective of this study was to report the outcomes of assisted withdrawal of opioid-dependent vulnerable children and adolescents who were referred to child and adolescent psychiatric ward of Ali Ebne Abitaleb hospital, an academic hospital in Zahedan city...
August 2016: Iranian Journal of Pediatrics
Maria Claudia Rodríguez, Perla Villamor, Tatiana Castillo
INTRODUCTION: Pain is a disease by itself and it's a public health concern of major implication in children, not just because of the emotional component of the child and his family, but also due to the potential morbidity and mortality involving it. A proper assessment of pain it's a challenge in the pediatric population, due to their lack of understanding and verbalization of hurt. Additionally, a satisfactory treatment of pediatric pain can be arduous due to a lack of clinical knowledge, insufficient pediatric research, and the fear to opioid side effects and addiction...
November 2016: International Journal of Pediatric Otorhinolaryngology
Dario Kringel, Jörn Lötsch
BACKGROUND: The opioid system is involved in the control of pain, reward, addictive behaviors and vegetative effects. Opioids exert their pharmacological actions through the agonistic binding at opioid receptors and variation in the coding genes has been found to modulate opioid receptor expression or signaling. However, a limited selection of functional opioid receptor variants is perceived as insufficient in providing a genetic diagnosis of clinical phenotypes and therefore, unrestricted access to opioid receptor genetics is required...
October 8, 2016: Clinica Chimica Acta; International Journal of Clinical Chemistry
O Prezzavento, E Arena, C Sánchez-Fernández, R Turnaturi, C Parenti, A Marrazzo, R Catalano, E Amata, L Pasquinucci, E J Cobos
cis-N-Substituted N-normetazocine enantiomers possess peculiar pharmacological profiles. Indeed, dextro enantiomers bind with high affinity σ1 receptor while opposite enantiomers bind opioid receptors. In spite of their stereochemistry, cis-N-2-phenylethyl N-normetazocine (phenazocine) enantiomers showed mixed opioid/σ1 receptor profiles and a significant in vivo analgesia. To the best of our knowledge, there is no information available regarding the evaluation of σ1 pharmacological profile in the antinociceptive effects of (+)- and (-)-phenazocine...
September 26, 2016: European Journal of Medicinal Chemistry
G Jeanne, D Purper-Ouakil, H Rigole, N Franc
AIM: There have been significant changes in adolescent consumption habits over the past fifteen years. New molecules have been synthesized, new devices created and a number of products have increased in popularity; and as a result clinicians sometimes lack information. We chose to focus on this population because of its vulnerability, as adolescents show low sensitivity to long-term outcomes of their actions and may be easily influenced by peers as regards experimentation of new drugs...
October 6, 2016: L'Encéphale
Omar S Mabrouk
Parkinson's disease (PD) is a progressive neurodegenerative disorder that compromises multiple neurochemical substrates including dopamine, norepinephrine, serotonin, acetylcholine, and glutamate systems. Loss of these transmitter systems initiates a cascade of neurological deficits beginning with motor function and ending with dementia. Current therapies primarily address the motor symptoms of the disease via dopamine replacement therapy. Exogenous dopamine replacement brings about additional challenges since after years of treatment it almost invariably gives rise to dyskinesia as a side effect...
October 8, 2016: Handbook of Experimental Pharmacology
Adil E Bharucha, Tae Hee Lee
Although pelvic pain is a symptom of several structural anorectal and pelvic disorders (eg, anal fissure, endometriosis, and pelvic inflammatory disease), this comprehensive review will focus on the 3 most common nonstructural, or functional, disorders associated with pelvic pain: functional anorectal pain (ie, levator ani syndrome, unspecified anorectal pain, and proctalgia fugax), interstitial cystitis/bladder pain syndrome, and chronic prostatitis/chronic pelvic pain syndrome. The first 2 conditions occur in both sexes, while the latter occurs only in men...
October 2016: Mayo Clinic Proceedings
Dayong Lee, Chris W Chronister, Wilson A Broussard, Suzanne R Utley-Bobak, Daniel L Schultz, Russell S Vega, Bruce A Goldberger
Fentanyl induces pharmacological effects and abuse liability comparable to other prescription opioids and heroin. A surge in fentanyl-related fatalities has been periodically reported throughout the USA. The University of Florida Forensic Toxicology Laboratory observed a significant increase in fentanyl-related deaths starting in mid-2014. The present report evaluated toxicological findings, demographics of the decedents and circumstances of death in the postmortem cases that were submitted to the laboratory for toxicological analysis from July 2014 to January 2015 and that were tested for fentanyl in biological specimens...
October 2016: Journal of Analytical Toxicology
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