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Opioid pharmacology

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https://www.readbyqxmd.com/read/28526162/pharmacologic-considerations-of-anesthetic-agents-in-pediatric-patients-a-comprehensive-review
#1
REVIEW
Alan D Kaye, Charles J Fox, Ira W Padnos, Ken P Ehrhardt, James H Diaz, Elyse M Cornett, Debbie Chandler, Sudipta Sen, Shilpadevi Patil
Acute pain in the pediatric population has important differences in terms of biology, intrapopulation variation, and epidemiology. Discussion as to the pharmacologic considerations of anesthetic agents, such as induction agents, neuromuscular blockers, opioids, local anesthetics, and adjuvant agents, is presented in this article. Special considerations and concerns, such as risk for propofol infusion syndrome and adverse potential side effects of anesthesia agents, are discussed. Anesthesiologists managing pediatric patients need to have a firm understanding of physiologic and pharmacologic differences compared with the adult population...
June 2017: Anesthesiology Clinics
https://www.readbyqxmd.com/read/28526158/revisiting-oxycodone-analgesia-a-review-and-hypothesis
#2
REVIEW
Xiulu Ruan, Ken F Mancuso, Alan D Kaye
Oxycodone, a semisynthetic opioid analgesic, is widely used in clinical practice. Oxycodone and morphine seem to be equally effective and equipotent; however, morphine is 10 times more potent than oxycodone when given epidurally. This article provides an updated review of the basic pharmacology of oxycodone with a special focus on pharmacokinetic/pharmacodynamics properties. The controversy regarding oxycodone-mediated effects for visceral pain via agonism and the possible role of peripheral opioid analgesia are discussed in the present investigation in an attempt to propose a plausible explanation to the perplexing question of oxycodone analgesia...
June 2017: Anesthesiology Clinics
https://www.readbyqxmd.com/read/28526152/pharmacologic-properties-of-novel-local-anesthetic-agents-in-anesthesia-practice
#3
REVIEW
Chih H King, Sascha S Beutler, Alan D Kaye, Richard D Urman
Therapeutic duration of traditional local anesthetics when used in peripheral nerve blocks is normally limited. This article describes novel approaches to extend the duration of peripheral nerve blocks currently available or in development. Three newer approaches on extending the duration of peripheral nerve blocks include site-1 sodium channel blockers, novel local anesthetics delivery systems, and novel adjuvants of local anesthetics. Compared with plain amide-based and ester-based local anesthetics, alternative approaches show significant promise in decreasing postoperative pain, rescue opioid requirement, hospital length-of-stay, and overall health care cost, without compromising the established safety profile of traditional local anesthetics...
June 2017: Anesthesiology Clinics
https://www.readbyqxmd.com/read/28524907/breakthrough-cancer-pain-a-systematic-review-of-pharmacologic-management%C3%A2
#4
Jeannine M Brant, Barbara B Rodgers, Eva Gallagher, Thiruppavai Sundaramurthi
BACKGROUND: Breakthrough cancer pain (BtCP), defined as a transient exacerbation of pain that occurs in conjunction with well-controlled background pain, is a common and burdensome problem in patients with cancer.
. OBJECTIVES: The aim of this systematic review is to identify evidence-based pharmacologic modalities for adequate management of BtCP. 
. METHODS: PubMed and CINAHL® databases were searched to identify literature regarding pharmacologic strategies for BtCP published from January 2006 to June 2016...
June 1, 2017: Clinical Journal of Oncology Nursing
https://www.readbyqxmd.com/read/28524906/chronic-and-refractory-pain-a-systematic-review-of-pharmacologic-management-in-oncology%C3%A2
#5
Jeannine M Brant, Lisa Keller, Karen McLeod, Chao Yeh, Linda H Eaton
BACKGROUND: Chronic and refractory cancer pain are significant issues and can increase patient suffering and compromise quality of life. A variety of evidence-based pharmacologic strategies can be used routinely to control cancer pain. 
. OBJECTIVES: The purpose of this study is to conduct a systematic review of the pharmacologic evidence in the management of chronic and refractory cancer pain. 
. METHODS: The Oncology Nursing Society's Putting Evidence Into Practice pain team conducted a search of 184 systematic reviews, meta-analyses, research studies, and guidelines and classified the evidence into weight-of-evidence categories...
June 1, 2017: Clinical Journal of Oncology Nursing
https://www.readbyqxmd.com/read/28523574/medical-management-of-pain-in-chronic-pancreatitis
#6
REVIEW
Vikesh K Singh, Asbjørn M Drewes
The medical management of pain in chronic pancreatitis continues to pose significant challenges for clinicians caring for these patients. There are increasing data, suggesting that pain in chronic pancreatitis is largely due to peripheral and central sensitization that evolves, over time, as a result of nociceptive afferent associated with chronic inflammation and fibrosis of the pancreas. In many instances, patients rapidly progress to requiring opioid analgesics for the adequate treatment of pain despite the unequivocal risks associated with the long-term use of these drugs...
May 18, 2017: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28521010/prospective-audit-of-a-pathway-for-in-patient-pain-management-of-chronic-abdominal-pain-a-novel-and-cost-effective-strategy
#7
Gopinath Niraj, Sanjay Chaudhri
Background.:  Unexplained abdominal pain is a common cause of hospital admission and utilizes significant resource. Current in-patient pain management of acute exacerbation of chronic abdominal pain is primarily directed at pharmacological and psychological management strategies in this group of complex patients. We adopted a novel approach that proved to be both clinically effective and cost-effective. Design.:  Adult patients admitted to a surgical ward with acute exacerbation of chronic abdominal pain referred to in-patient pain management were prospectively audited over a two-year period at a single tertiary centre...
May 17, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28519244/neonatal-abstinence-syndrome-update-on-diagnostic-and-therapeutic-strategies
#8
Genny Raffaeli, Giacomo Cavallaro, K Karel Allegaert, Enno Diederik Wildschut, Monica Fumagalli, Massimo Agosti, Dick Tibboel, Fabio Mosca
Substance use among pregnant women is a major public health issue. Both prescription opioid use and illicit opioid abuse have increased dramatically in recent years. Prolonged in utero drug exposure may result in neonatal abstinence syndrome (NAS), an acute multisystemic clinical entity that occurs in the first days of life. This syndrome is caused by abrupt discontinuation of fetal exposure to licit or illicit drugs chronically consumed by the mother during pregnancy and transmitted to the fetus through the placenta...
May 18, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28514889/pain-perception-in-nicu-a-pilot-questionnaire
#9
C V Bellieni, M Tei, S Cornacchione, S Di Lucia, V Nardi, A Verrotti, G Buonocore
PURPOSE: Neonatal pain management has made a great step forward over the last several years. Despite the drafting of International guidelines, an under-treatment of neonatal pain is still reported. MATERIALS AND METHODS: Medical and paramedical personnel working in 5 Italian NICUs were asked to complete a questionnaire about pain management. The questionnaire was comprised of three sections: (i) brief explanation of the purpose; (ii) demographic information, including age, profession, religious beliefs, and hospital level; (iii) questionnaire about pain management and prevention...
May 17, 2017: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/28509855/the-hypnotic-anxiolytic-and-antinociceptive-profile-of-a-novel-%C3%A2%C2%B5-opioid-agonist
#10
Guilherme Carneiro Montes, Bianca Nascimento Monteiro da Silva, Bismarck Rezende, Roberto Takashi Sudo, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Angelo da Cunha Pinto, Bárbara Vasconcellos da Silva, Gisele Zapata-Sudo
5'-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 1-12 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 µmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a µ-opioid antagonist...
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28504116/exercise-reverses-pain-related-weight-asymmetry-and-differentially-modulates-trabecular-bone-microarchitecture-in-a-rat-model-of-osteoarthritis
#11
Jim Cormier, Katherine Cone, Janell Lanpher, Abigail Kinens, Terry Henderson, Lucy Liaw, Edward J Bilsky, Tamara King, Clifford J Rosen, Glenn W Stevenson
There is great interest in developing and utilizing non-pharmacological/non-invasive forms of therapy for osteoarthritis (OA) pain including exercise and other physical fitness regimens. AIMS: The present experiments determined the effects of prior wheel running on OA-induced weight asymmetry and trabecular bone microarchitecture. MAIN METHODS: Wheel running included 7 or 21days of prior voluntary access to wheels followed by OA induction, followed by 21days post-OA access to wheels...
May 11, 2017: Life Sciences
https://www.readbyqxmd.com/read/28502978/the-opioid-receptor-triple-agonist-dpi-125-produces-analgesia-with-less-respiratory-depression-and-reduced-abuse-liability
#12
Shou-Pu Yi, Qing-Hong Kong, Yu-Lei Li, Chen-Ling Pan, Jie Yu, Ben-Qiang Cui, Ying-Fei Wang, Guan-Lin Wang, Pei-Lan Zhou, Li-Li Wang, Ze-Hui Gong, Rui-Bin Su, Yue-Hai Shen, Gang Yu, Kwen-Jen Chang
Opioid analgesics remain the first choice for the treatment of moderate to severe pain, but they are also notorious for their respiratory depression and addictive effects. This study focused on the pharmacology of a novel opioid receptor mixed agonist DPI-125 and attempted to elucidate the relationship between the δ-, μ- and κ-receptor potency ratio and respiratory depression and abuse liability. Five diarylmethylpiperazine compounds (DPI-125, DPI-3290, DPI-130, KUST202 and KUST13T02) were selected for this study...
May 15, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#13
Ferenc Zádor, Kornél Király, András Váradi, Mihály Balogh, Ágnes Fehér, Dóra Kocsis, Anna I Erdei, Erzsébet Lackó, Zoltán S Zádori, Sándor Hosztafi, Béla Noszál, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass through the blood-brain barrier. Quaternization of the amine group in these molecules, (e.g. methylnaltrexone) results in negligible CNS penetration. In addition, zwitterionic compounds have been reported to have limited CNS access. The current study, for the first time gives report on the synthesis and the in vitro [competition binding, G-protein activation, isolated mouse vas deferens (MVD) and mouse colon assay] pharmacology of the zwitterionic compound, naltrexone-14-O-sulfate...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28501425/the-effects-of-kratom-on-restraint-stress-induced-analgesia-and-its-mechanisms-of-action
#14
José Luis Vázquez López, Lorenz Schild, Thomas Günther, Stefan Schulz, Hartmud Neurath, Axel Becker
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa and its extracts are called kratom (dried leaves, extract). They contain several alkaloids with an affinity for different opioid receptors. They are used in traditional medicine for the treatment of different diseases, as a substitute by opiate addicts, and to mitigate opioid withdrawal symptoms. Apart from their medical properties, they are used to enhance physical endurance and as a means of overcoming stress. PURPOSE: The aim of this study was to determine the mechanisms underlying the effects of kratom on restraint-stress-induced analgesia which occurs during or following exposure to a stressful or fearful stimulus...
May 10, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28500629/early-prediction-tool-to-identify-the-need-for-pharmacotherapy-in-infants-at-risk-of-neonatal-abstinence-syndrome
#15
Barbara T Isemann, Elaina C Stoeckle, Afshin A Taleghani, Eric W Mueller
OBJECTIVE: To develop a tool to predict the need for pharmacologic treatment of neonatal abstinence syndrome (NAS) within 36 hours from birth in infants at risk for opioid withdrawal. STUDY DESIGN: Retrospective study of infants born at 34 weeks or later gestation with in utero exposure to opioids during two time periods from January 2013 through October 2016. Period 1 was used to develop a predictive tool for validation during Period 2. Birth weight, gestational age, four categories of opioid exposure, and individual scores for 21 withdrawal symptoms from the Modified Finnegan Score at 36 hours of life were recorded...
May 13, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28494108/selective-%C3%AE%C2%BA-opioid-receptor-partial-agonist-hs666-produces-potent-antinociception-without-inducing-aversion-after-i-c-v-administration-in-mice
#16
Mariana Spetea, Shainnel O Eans, Michelle L Ganno, Aquilino Lantero, Michael Mairegger, Lawrence Toll, Helmut Schmidhammer, Jay P McLaughlin
BACKGROUND AND PURPOSE: The κ opioid (KOP) receptor has a central role in modulating neurotransmission in central and peripheral neuronal circuits that subserve pain and other behavioural responses. Although KOP agonists do not produce euphoria or lead to respiratory suppression, they induce dysphoria and sedation. We hypothesized that brain-penetrant KOP receptor ligands possessing biased agonism towards G protein signalling over β-arrestin2 recruitment would produce robust antinociception with fewer liabilities of use...
May 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28492129/codeine-misuse-and-dependence-in-south-africa-perspectives-of-addiction-treatment-providers
#17
Charles D H Parry, Eileen Rich, Marie Claire Van Hout, Paolo Deluca
BACKGROUND: General practitioners are referring patients with codeine-related problems to specialist treatment facilities, but little is known about the addiction treatment providers, the kinds of treatment they provide, and whether training or other interventions are needed to strengthen this sector. OBJECTIVES: To investigate the perspectives of addiction treatment providers regarding treatment for codeine misuse or dependence. METHOD: Twenty addiction treatment providers linked to the South African Community Epidemiology Network on Drug Use and the South African Addiction Medicine Society were contacted telephonically and asked 20 questions...
April 25, 2017: South African Medical Journal, Suid-Afrikaanse Tydskrif Vir Geneeskunde
https://www.readbyqxmd.com/read/28490206/pharmacokinetics-pharmacodynamics-and-pharmacogenetics-associated-with-nonsteroidal-anti-inflammatory-drugs-and-opioids-in-pediatric-cancer-patients
#18
Jonathan Constance, Sarah Campbell, Amit A Somani, Venkata Yellepeddi, Katie Owens, Catherine Sherwin
Advancing appropriate and adequate analgesic pharmacotherapy in pediatric patients with cancer is an area of clinical need. Few studies have been performed to evaluate the selection of an analgesic and appropriate dosing corresponding to analgesic effect among pediatric cancer patients. This review describes information related to pharmacokinetic, pharmacodynamic, and pharmacogenomic (when applicable) considerations for analgesics that are commonly used to manage pain experienced by pediatric patients with cancer...
May 11, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28488910/methadone-induced-neurotoxicity-in-advanced-cancer-a-case-report
#19
Ann M Hoff, Kristopher N Hartwig, Drew A Rosielle
Methadone use as a second-line agent for severe cancer-related pain is increasing in the field of hospice and palliative care. It has a number of qualities that make its use favorable, including lack of known active metabolites and presumed relative safety from adverse effects such as opioid-induced neurotoxicity (OIN). This article describes a case of a patient undergoing treatment of severe cancer-related pain who developed OIN in the setting of oral methadone use. As the use of methadone increases, more research into its pharmacologic and pharmacokinetic properties will be necessary...
May 10, 2017: Journal of Palliative Medicine
https://www.readbyqxmd.com/read/28488805/breastfeeding-considerations-for-mothers-of-infants-with-neonatal-abstinence-syndrome
#20
Amy P Holmes, Holly N Schmidlin, Eliana N Kurzum
Breastfeeding offers many benefits to both mother and baby. Breastfeeding is generally recommended for mothers of infants with neonatal abstinence syndrome (NAS) unless some associated risk outweighs the benefits. Evidence indicates that infants with NAS who receive human milk require less pharmacologic treatment and have shorter hospital lengths of stay. Perhaps the greatest barrier to breastfeeding for women with opioid dependence is the inaccurate and inconsistent information they receive from different sources, including health care professionals...
May 10, 2017: Pharmacotherapy
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