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Opioid dosing

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https://www.readbyqxmd.com/read/28220474/buprenorphine-for-managing-opioid-withdrawal
#1
REVIEW
Linda Gowing, Robert Ali, Jason M White, Dalitso Mbewe
BACKGROUND: Managed withdrawal is a necessary step prior to drug-free treatment or as the endpoint of substitution treatment. OBJECTIVES: To assess the effects of buprenorphine versus tapered doses of methadone, alpha2-adrenergic agonists, symptomatic medications or placebo, or different buprenorphine regimens for managing opioid withdrawal, in terms of the intensity of the withdrawal syndrome experienced, duration and completion of treatment, and adverse effects...
February 21, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28219988/sex-differences-in-microglia-activity-within-the-periaqueductal-gray-of-the-rat-a-potential-mechanism-driving-the-dimorphic-effects-of-morphine
#2
H H Doyle, L N Eidson, D M Sinkiewicz, A Z Murphy
Although morphine remains the primary drug prescribed for alleviation of severe or persistent pain, both preclinical and clinical studies have shown that females require 2-3 times more morphine than males to produce comparable levels of analgesia. In addition to binding to the neuronal μ opioid receptor (MOR), morphine binds to the innate immune receptor toll-like receptor 4 (TLR4) localized primarily on microglia. Morphine action at TLR4 initiates a neuroinflammatory response that directly opposes the analgesic effects of morphine...
February 20, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28218955/antihyperglycemiac-action-of-diosmin-a-citrus-flavonoid-is-induced-through-endogenous-%C3%AE-endorphin-in-type-i-like-diabetic-rats
#3
Chia-Chen Hsu, Mang Hung Lin, Juei Tang Cheng, Ming Chang Wu
Diosmin is one of the flavonoids contained in citrus and has been demonstrated to improve glucose metabolism in diabetic disorders. However, the mechanism(s) of diosmin in glucose regulation remain obscure. Therefore, we investigated the potential mechanism(s) for the antihyperglycemic action of diosmin in streptozotocin-induced diabetic rats (STZ-diabetic rats). Diosmin lowered hyperglycemia in a dose-dependent manner in STZ-diabetic rats. This action was inhibited by naloxone at a dose sufficient to block opioid receptors...
February 20, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28218838/design-and-synthesis-of-enantiomerically-pure-decahydroquinoxalines-as-potent-and-selective-%C3%AE%C2%BA-opioid-receptor-agonists-with-anti-inflammatory-activity-in-vivo
#4
Michael Soeberdt, Peter Molenveld, Roy P M Storcken, Renaud Bouzanne des Mazery, Geert Jan Sterk, Reshma Autar, Marjon G Bolster, Clemens Wagner, Sebastianus N H Aerts, Frank R van Holst, Anita Wegert, Giovanni Tangherlini, Bastian Frehland, Dirk Schepmann, Dieter Metze, Tobias Lotts, Ulrich Knie, Kun-Yuan Lin, Tai-Yu Huang, Chih-Ching Lai, Sonja Ständer, Bernhard Wünsch, Christoph Abels
In order to develop novel κ agonists restricted to the periphery, a diastereo- and enantioselective synthesis of (4aR,5S,8aS)-configured decahydroquinoxalines 5-8 was developed. Physicochemical and pharmacological properties were fine-tuned by structural modifications in the arylacetamide and amine part of the pharmacophore as well as in the amine part outside the pharmacophore. The decahydroquinoxalines 5-8 show single-digit nanomolar to subnanomolar κ-opioid receptor affinity, full κ agonistic activity in the [(35)S]GTPγS assay, and high selectivity over μ, δ, σ1, and σ2 receptors as well as the PCP binding site of the NMDA receptor...
February 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28216196/hypericum-perforatum-st-john-s-wort-beyond-depression-a-therapeutic-perspective-for-pain-conditions
#5
REVIEW
Nicoletta Galeotti
ETHNOPHARMACOLOGICAL RELEVANCE: Hypericum perforatum L. (Hypericaceae), popularly called St. John's wort (SJW), has a rich historical background being one of the oldest used and most extensively investigated medicinal herbs. Many bioactivities and applications of SJW are listed in popular and in scientific literature, including antibacterial, antiviral, anti-inflammatory. In the last three decades many studies focused on the antidepressant activity of SJW extracts. However, several studies in recent years also described the antinociceptive and analgesic properties of SJW that validate the traditional uses of the plant in pain conditions...
February 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28216062/nalmefene-reduces-reward-anticipation-in-alcohol-dependence-an-experimental-functional-magnetic-resonance-imaging-study
#6
Darren R Quelch, Inge Mick, John McGonigle, Anna C Ramos, Remy S A Flechais, Mark Bolstridge, Eugenii Rabiner, Matthew B Wall, Rexford D Newbould, Björn Steiniger-Brach, Franz van den Berg, Malcolm Boyce, Dorrit Østergaard Nilausen, Lasse Breuning Sluth, Didier Meulien, Christoph von der Goltz, David Nutt, Anne Lingford-Hughes
BACKGROUND: Nalmefene is a µ- and δ-opioid receptor antagonist, κ-opioid receptor partial agonist that has recently been approved in Europe for treating alcohol dependence. It offers a treatment approach for alcohol-dependent individuals with "high-risk drinking levels" to reduce their alcohol consumption. However, the neurobiological mechanism underpinning its effects on alcohol consumption remains to be determined. Using a randomized, double-blind, placebo-controlled, within-subject crossover design we aimed to determine the effect of a single dose of nalmefene on striatal blood oxygen level-dependent (BOLD) signal change during anticipation of monetary reward using the monetary incentive delay task following alcohol challenge...
January 10, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28216001/loperamide-inhibits-sodium-channels-to-alleviate-inflammatory-hyperalgesia
#7
Ying Wu, Beiyan Zou, Lingli Liang, Min Li, Yuan-Xiang Tao, Haibo Yu, Xiaoliang Wang, Min Li
Previous studies demonstrated that Loperamide, originally known as an anti-diarrheal drug, is a promising analgesic agent primarily targeting mu-opioid receptors. However some evidences suggested that non-opioid mechanisms may be contributing to its analgesic effect. In the present study, Loperamide was identified as a Nav1.7 blocker in a pilot screen. In HEK293 cells expressing Nav1.7 sodium channels, Loperamide blocked the resting state of Nav1.7 channels (IC50 = 1.86 ± 0.11 μM) dose-dependently and reversibly...
February 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28215574/the-impact-of-pharmacy-services-on-opioid-prescribing-in-dental%C3%A2-practice
#8
Autumn Stewart, Kelsey J Zborovancik, Kara L Stiely
OBJECTIVES: To compare rates of dental opioid prescribing between periods of full and partial integration of pharmacy services and periods of no integration. METHODS: This observational study used a retrospective chart review of opioid prescriptions written by dental providers practicing in a free dental clinic for the medically underserved over a period of 74 months. Pharmacy services were fully integrated into the practice model for 48 of the 74 months under study...
February 15, 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28214687/gastroprotective-effect-and-mechanism-of-action-of-croton-rhamnifolioides-essential-oil-in-mice
#9
Cinara Soares Vidal, Anita Oliveira Brito Pereira Bezerra Martins, Andressa de Alencar Silva, Maria Rayane Correia de Oliveira, Jaime Ribeiro-Filho, Thaís Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Jackson Roberto Guedes da Silva Almeida, Lucindo Jose Quintans, Irwin Rose Alencar de Menezes
BACKGROUND: Croton rhamnifolioides Pax is a plant species that have been used in the folk medicine to treat ulcers, inflammations and hypertension. However, despite the relevant data obtained from ethnopharmacological studies, the pharmacological properties endorsing the efficacy of this plant to treat ulcer remain to be elucidated. HYPOTHESIS/PURPOSE: The present study aimed to characterize the chemical profile and evaluate the gastroprotective activity of the essential oil obtained from C...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28214095/whether-preventive-low-dose-magnesium-sulphate-infusion-has-an-influence-on-postoperative-pain-perception-and-the-level-of-serum-beta-endorphin-throughout-the-total-abdominal-hysterectomy
#10
K Haryalchi, M Abedinzade, K Khanaki, M M Ghanaie, F M Zadeh
OBJECTIVE: Due to the known role of preventive low dose magnesium sulphate on postoperative pain management, in this randomized, double-blinded, placebo-controlled study, we tried to investigate the possible relationship between low dose intra-operative magnesium sulphate infusion, postoperative analgesia and the level of serum beta-endorphin during total abdominal hysterectomy under general anesthesia. METHODS: Forty women undergoing total abdominal hysterectomy were randomly allocated into 2 groups (20 in each arm)...
February 14, 2017: Revista Española de Anestesiología y Reanimación
https://www.readbyqxmd.com/read/28213891/opioids-and-the-immune-system-friend-or-foe
#11
REVIEW
Lisanne Mirja Plein, Heike L Rittner
Systemically administered opioids are among the most powerful analgesics for treating severe pain. Several negative side-effects (respiratory depression, addiction, nausea, confusion) and the risk of opioid-induced hyperalgesia accompany opioid administration. One other side effect is the potential of opioids to suppress the immune response and thereby to increase the vulnerability for infections. Several studies have investigated the link between opioids and immunosuppression in vitro, in vivo as well as in patients with divergent results: Exogenous opioids such as morphine and fentanyl can impair macrophage and natural killer cell as well as T cell function and weaken the gut barrier in vitro and in animal studies...
February 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28213817/breakthrough-cancer-pain-and-rational-drug-use
#12
Juan Manuel Núñez Olarte
Recent data indicate that there are large disparities in the use of opioid analgesics to control breakthrough cancer pain (BTcP) in Europe and worldwide. While it is clear that affordability is a key factor, it is certainly not the only one, and other factors, such as cultural differences and overall awareness, are undoubtedly responsible. More work remains to be done to overcome barriers in the use of these medications when warranted. When prescribing a medication for BTcP, it must be considered that its time profile is different from chronic persistent pain...
February 18, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28213593/randomised-double-blind-parallel-group-placebo-controlled-study-to-evaluate-the-analgesic-efficacy-and-safety-of-vvz-149-injections-for-postoperative-pain-following-laparoscopic-colorectal-surgery
#13
Srdjan S Nedeljkovic, Darin J Correll, Xiaodong Bao, Natacha Zamor, Jose L Zeballos, Yi Zhang, Mark J Young, Johanna Ledley, Jessica Sorace, Kristen Eng, Carlyle P Hamsher, Rajivan Maniam, Jonathan W Chin, Becky Tsui, Sunyoung Cho, Doo H Lee
INTRODUCTION: In spite of advances in understanding and technology, postoperative pain remains poorly treated for a significant number of patients. In colorectal surgery, the need for developing novel analgesics is especially important. Patients after bowel surgery are assessed for rapid return of bowel function and opioids worsen ileus, nausea and constipation. We describe a prospective, double-blind, parallel group, placebo-controlled randomised controlled trial testing the hypothesis that a novel analgesic drug, VVZ -149, is safe and effective in improving pain compared with providing opioid analgesia alone among adults undergoing laparoscopic colorectal surgery...
February 17, 2017: BMJ Open
https://www.readbyqxmd.com/read/28212204/1-2-4-dibromophenyl-3-6-6-trimethyl-1-5-6-7-tetrahydro-4h-indazol-4-one-a-novel-opioid-receptor-agonist-with-less-accompanying-gastrointestinal-dysfunction-than-morphine
#14
Po-Kuan Chao, Shau-Hua Ueng, Li-Chin Ou, Teng-Kuang Yeh, Wan-Ting Chang, Hsiao-Fu Chang, Shu-Chun Chen, Pao-Luh Tao, Ping-Yee Law, Horace H Loh, Ming-Fu Cheng, Jian-Ying Chuang, Chiung-Tong Chen, Chuan Shih, Shiu-Hwa Yeh
BACKGROUND: The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. METHODS: In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a β-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5)...
February 17, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28210861/the-effects-of-alcoholism-and-smoking-on-advanced-cancer-patients-admitted-to-an-acute-supportive-palliative-care-unit
#15
Sebastiano Mercadante, Claudio Adile, Patrizia Ferrera, Alessandra Casuccio
AIM: The aim of this prospective study was to determine the characteristics and symptom burden of advanced cancer patients with alcoholism problems and smoking, who were referred to an acute palliative/supportive care unit (ASPCU) of a comprehensive cancer center. METHODS: Patients' characteristics, indications for admission, kind of admission, awareness of prognosis, and anticancer treatments were recorded. The Edmonton Symptom Assessment Scale (ESAS) was used to assess physical and psychological symptoms, and the CAGE questionnaire for the diagnosis of alcoholism...
February 16, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/28210635/combined-spinal-epidural-for-vaginal-delivery-in-a-parturient-with-takayasu-s-arteritis
#16
Sean Patrick Clifford, Paul Brian Mick, Brian Matthew Derhake
Takayasu's arteritis is a rare, progressive panendarteritis involving all layers of the arterial wall. This disease includes variable involvement of the aorta and its major branches. The most common complication with this condition is severe, uncontrolled hypertension, often leading to end organ dysfunction. We describe the management of a 27-year-old woman diagnosed with Takayasu's arteritis that presented in labor with intense pain and underwent a combined spinal-epidural for anesthetic management. Per literature review, a combined spinal-epidural technique for planned vaginal delivery has not been described for a laboring Takayasu patient...
October 2016: Journal of Investigative Medicine High Impact Case Reports
https://www.readbyqxmd.com/read/28210502/a-single-perioperative-injection-of-dexamethasone-decreases-nausea-vomiting-and-pain-after-laparoscopic-donor-nephrectomy
#17
Shigeyoshi Yamanaga, Andrew Mark Posselt, Chris Earl Freise, Takaaki Kobayashi, Mehdi Tavakol, Sang-Mo Kang
Background. A single dose of perioperative dexamethasone (8-10 mg) reportedly decreases postoperative nausea, vomiting, and pain but has not been widely used in laparoscopic donor nephrectomy (LDN). Methods. We performed a retrospective cohort study of living donors who underwent LDN between 2013 and 2015. Donors who received a lower dose (4-6 mg)  (n = 70) or a higher dose (8-14 mg) of dexamethasone (n = 100) were compared with 111 donors who did not receive dexamethasone (control). Outcomes and incidence of postoperative nausea, vomiting, and pain within 24 h after LDN were compared before and after propensity-score matching...
2017: Journal of Transplantation
https://www.readbyqxmd.com/read/28202437/oscillation-patterns-are-enhanced-and-firing-threshold-is-lowered-in-medullary-respiratory-neuron-discharges-by-threshold-doses-of-a-%C3%AE-opioid-receptor-agonist
#18
Peter M Lalley, Steve W Mifflin
μ-Opioid receptors are distributed widely in the brainstem respiratory network, and opioids with selectivity for μ-type receptors slow in-vivo respiratory rhythm in lowest effective doses. Several studies have reported μ-opioid receptor effects on the three-phase rhythm of respiratory neurons, but there are until now no reports of opioid effects on oscillatory activity within respiratory discharges. In this study, effects of the μ-opioid receptor agonist fentanyl on spike train discharge properties of several different types of rhythm-modulating medullary respiratory neuron discharges were analyzed...
February 15, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28195856/pharmacoepidemiologic-analyses-of-opioid-use-among-oef-oif-ond-veterans
#19
Teresa J Hudson, Jacob T Painter, Brad Martin, Mark A Austen, James S Williams, John Fortney, Mark D Sullivan, Mark E Edlund
There is a great deal of concern about opioid use in Veterans, particularly those that served in Afghanistan (OEF) and Iraq (OIF and OND). The current study provides a detailed pharmacoepidemiologic analysis of opioid use among OEF/OIF/OND Veterans from FY09 to FY12. Data from three data repositories from the Veterans Health Administration (VHA) were used to describe demographic, clinical, and medication characteristics associated with opioid use among OEF/OIF/OND Veterans and among those with TBI. Logistic regression models were used to identify risks associated with chronic opioid use in FY12...
February 11, 2017: Pain
https://www.readbyqxmd.com/read/28188773/maternal-buprenorphine-treatment-and-fetal-neurobehavioral-development
#20
Lauren M Jansson, Martha Velez, Krystle McConnell, Nancy Spencer, Michelle Tuten, Hendree E Jones, Van L King, Neeraj Gandotra, Lorraine A Milio, Kristin Voegtline, Janet A DiPietro
BACKGROUND: Gestational opioid use/misuse is escalating in the United States, however, little is understood about the fetal effects of medications used to treat maternal opioid use disorders. OBJECTIVE: The purpose of this study was to determine the effect of maternal buprenorphine administration on longitudinal fetal neurobehavioral development. STUDY DESIGN: Forty-nine buprenorphine-maintained women attending a substance use disorder treatment facility with generally uncomplicated pregnancies underwent fetal monitoring for 60 minutes at times of trough and peak maternal buprenorphine levels...
February 7, 2017: American Journal of Obstetrics and Gynecology
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