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morphine tolerance

Samuel Obeng, Yunyun Yuan, Abdulmajeed Jali, Dana E Selley, Yan Zhang
Evidence has shown that downstream signaling by mu opioid receptor (MOR) agonists that recruit β-arrestin2 may lead to the development of tolerance. Also, it has been suggested that opioid receptor desensitization and cyclic AMP overshoot contributes to the development of tolerance and occurrence of withdrawal, respectively. Therefore, studies were conducted with 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3-carboxamido)morphinan (NAQ), a MOR selective partial agonist discovered in our laboratory, to characterize its effect on β-arrestin2 recruitment and precipitation of a cyclic AMP overshoot...
March 9, 2018: European Journal of Pharmacology
N Dietis, H Niwa, R Tose, J McDonald, V Ruggieri, M Filaferro, G Vitale, L Micheli, C Ghelardini, S Salvadori, G Calo, R Guerrini, D J Rowbotham, D G Lambert
BACKGROUND AND PURPOSE: Targeting more than one opioid receptor type simultaneously may have analgesic advantages in reduced side effect profile. We have evaluated the mixed MOP (μ, mu) agonist/DOP (δ, delta) antagonist UFP-505 in vitro and in vivo. EXPERIMENTAL APPROACH: We measured receptor density and function in single MOP, DOP and MOP/DOP double expression systems. GTPγ35 S binding, cAMP formation and arrestin recruitment were measured. Antinociceptive activity was measured in vivo using tail withdrawal and paw pressure tests following acute and chronic treatment...
March 10, 2018: British Journal of Pharmacology
Peter Athanasos, Walter Ling, Felix Bochner, Jason M White, Andrew A Somogyi
Objective: Acute pain management in opioid-dependent persons is complicated because of tolerance and opioid-induced hyperalgesia. Very high doses of morphine are ineffective in overcoming opioid-induced hyperalgesia and providing antinociception to methadone-maintained patients in an experimental setting. Whether the same occurs in buprenorphine-maintained subjects is unknown. Design: Randomized double-blind placebo-controlled. Subjects were tested on two occasions, at least five days apart, once with intravenous morphine and once with intravenous saline...
March 5, 2018: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
Wenying Wang, Xiaqing Ma, Limin Luo, Min Huang, Jing Dong, Xiaoli Zhang, Wei Jiang, Tao Xu
BACKGROUND AND PURPOSE: The P2X3 receptor (P2X3R) is a major receptor in the processing of nociceptive information in dorsal root ganglia (DRGs). We investigated the role of the P2X3R and the detailed mechanisms underlying chronic morphine-induced analgesic tolerance in rats. EXPERIMENTAL APPROACHES: Under isoflurane inhalation anaesthesia, intrathecal catheters were implanted in male Sprague-Dawley rats. Repeated intrathecal (i.t.) morphine treatment was used to induce anti-nociceptive tolerance...
March 3, 2018: British Journal of Pharmacology
M R Rajagopal
Context: Morphine and fentanyl had so far been the only available opioids in India in step three of the World Health Organization analgesic ladder. Especially for those not tolerating morphine and particularly for those developing neurotoxicity, an inexpensive alternative was essential. Many years of advocacy by palliative care activists have resulted in methadone being now available for sale in India for pain management. However, the characteristic pharmacokinetics and pharmacodynamics of methadone raise potential issues of safety...
January 2018: Indian Journal of Palliative Care
Kaouthar Beltaief, Mohamed Habib Grissa, Mohamed Amine Msolli, Nasri Bzeouich, Nizar Fredj, Adel Sakma, Hamdi Boubaker, Wahid Bouida, Riadh Boukef, Semir Nouira
Objective: The objective of this study was to compare the analgesic effect and tolerance profile of acupuncture versus intravenous (IV) titrated morphine in patients presenting to the emergency department (ED) with renal colic. Materials and methods: A total of 115 patients were randomized into two groups. Patients in the IV titrated-morphine group (n=61) received 0.1 mg/kg morphine every 5 minutes until pain score dropped by at least 50% of its baseline value. Patients in the acupuncture group (n=54) received an acupuncture session of 30 minutes following a prespecified protocol...
2018: Journal of Pain Research
Fuyuan Wang, Jingjing Meng, Li Zhang, Timothy Johnson, Chi Chen, Sabita Roy
Opioid analgesics are frequently prescribed in the United States and worldwide. However, serious comorbidities, such as dependence, tolerance, immunosuppression and gastrointestinal disorders limit their long-term use. In the current study, a morphine-murine model was used to investigate the role of the gut microbiome and metabolome as a potential mechanism contributing to the negative consequences associated with opioid use. Results reveal a significant shift in the gut microbiome and metabolome within one day following morphine treatment compared to that observed after placebo...
February 26, 2018: Scientific Reports
Yusuke Takagi, Etsuko Aruga
In 2010s, several opioids became available in Japan, including methadone, tapentadol and hydromorphone. Methadone was approved in September 2012 by Japanese regulatory authority. Since methadone is positioned as so-called "step 4 opioid" in Japan, it must be prescribed as alternative opioid switched from another of 60mg/day or greater equivalent dose of oral morphine. Diversity of pharmacokinetics among individuals and various drug interactions require close monitoring of adverse events. In spite of these cautions, unique characteristics such as inhibiting N-methyl-D-aspartate(NMDA)and in- ducing internalization/degradation of mu-delta opioid receptor heterodimers underline the value of methadone in opioid switching...
February 2018: Gan to Kagaku Ryoho. Cancer & Chemotherapy
Patrick Grenier, David Wiercigroch, Mary C Olmstead, Catherine M Cahill
Long-term use of opioid analgesics is limited by tolerance development and undesirable adverse effects. Paradoxically, spinal administration of ultra-low-dose (ULD) G-protein-coupled receptor antagonists attenuates analgesic tolerance. Here, we determined whether systemic ULD α2-adrenergic receptor (AR) antagonists attenuate the development of morphine tolerance, whether these effects extend to the cannabinoid (CB1) receptor system, and if behavioral effects are reflected in changes in opioid-induced spinal gliosis...
February 23, 2018: Behavioural Pharmacology
Sebastiano Mercadante
Breakthrough cancer pain (BTcP) is an episode of severe intensity in patients receiving an adequate treatment with opioids able to provide at least mild analgesia. BTcP is a heterogeneous condition as episodes vary between individuals. The aim of this article is to review the pharmacologic options for the management of BTcP. Areas covered: Recent reviews revealed that transmucosal preparations of fentanyl provided superior and more rapid pain relief as compared to placebo and oral morphine within the first 30 minutes after dosing...
February 26, 2018: Expert Review of Anticancer Therapy
Ram Kandasamy, Cole T Dawson, Tammy N Hilgendorf, Michael M Morgan
The potential of [INCREMENT]-tetrahydrocannabinol (THC) as a treatment for migraine depends on antinociceptive efficacy with repeated administration. Although morphine has good antinociceptive efficacy, repeated administration causes medication overuse headache (MOH) - a condition in which the intensity/frequency of migraine increases. The present study compared the effect of repeated morphine or THC administration on the magnitude and duration of migraine-like pain induced by a microinjection of allyl isothiocyanate (AITC) onto the dura mater of female rats...
February 16, 2018: Behavioural Pharmacology
Mohammad Taghi Mansouri, Bahareh Naghizadeh, Behnam Ghorbanzadeh, Soheila Alboghobeish, Neda Amirgholami, Gholamreza Houshmand, Omar Cauli
Opioid-induced neuroinflammation and the nitric oxide (NO) signal-transduction pathway are involved in the development of opioid analgesic tolerance. The antidepressant venlafaxine (VLF) modulates NO in nervous tissues, and so we investigated its effect on induced tolerance to morphine, neuroinflammation, and oxidative stress in mice. Tolerance to the analgesic effects of morphine were induced by injecting mice with morphine (50 mg/kg) once a day for three consecutive days; the effect of co-administration of VLF (5 or 40 mg/kg) with morphine was similarly tested in a separate group...
February 14, 2018: Experimental Neurology
Nivedita Page
A 23-year-old female presented to our palliative care center with Ewing's sarcoma of the humerus with lung metastases. Pain in her arm was unrelieved by nonsteroidal anti-inflammatory drugs, neuropathic medication as well as morphine. She could not tolerate any further increase in opioid dose but was so distraught due to the pain that she wanted to die. An intravenous lignocaine infusion in a dose of 2 mg/kg was given over an hour for three successive days. This successfully relieved her pain after which she was settled with her original medication...
January 2018: Indian Journal of Palliative Care
Sevasti Gaspari, Immanuel Purushothaman, Valeria Cogliani, Farhana Sakloth, Rachael L Neve, David Howland, Robert H Ring, Elliott M Ross, Li Shen, Venetia Zachariou
Regulator of G protein signaling z1 (RGSz1), a member of the RGS family of proteins, is present in several networks expressing mu opioid receptors (MOPRs). By using genetic mouse models for global or brain region-targeted manipulations of RGSz1 expression, we demonstrated that the suppression of RGSz1 function increases the analgesic efficacy of MOPR agonists in male and female mice and delays the development of morphine tolerance while decreasing the sensitivity to rewarding and locomotor activating effects...
February 12, 2018: Proceedings of the National Academy of Sciences of the United States of America
Andrew D Jung, Vikrom K Dhar, Richard S Hoehn, Sarah J Atkinson, Bobby L Johnson, Teresa Rice, Jonathan R Snyder, Janice F Rafferty, Michael J Edwards, Ian M Paquette
BACKGROUND: Enhanced recovery pathways (ERPs) aim to reduce length of stay without adversely affecting short-term outcomes. High pharmaceutical costs associated with ERP regimens, however, remain a significant barrier to widespread implementation. We hypothesized that ERP would reduce hospital costs following elective colorectal resections despite the use of more expensive pharmaceutical agents. STUDY DESIGN: An ERP was implemented in January 2016 at our institution...
January 4, 2018: Journal of the American College of Surgeons
Viljami Jokinen, Yulia Sidorova, Hanna Viisanen, Ilida Suleymanova, Henna Tiilikainen, Zhilin Li, Tuomas O Lilius, Kert Mätlik, Jenni E Anttila, Mikko Airavaara, Li Tian, Pekka V Rauhala, Eija A Kalso
Development of tolerance is a well known pharmacological characteristic of opioids and a major clinical problem. In addition to the known neuronal mechanisms of opioid tolerance, activation of glia has emerged as a potentially significant new mechanism. We studied activation of microglia and astrocytes in morphine tolerance and opioid-induced hyperalgesia in rats using immunohistochemistry, flow cytometry and RNA sequencing in spinal- and supraspinal regions. Chronic morphine treatment that induced tolerance and hyperalgesia also increased immunoreactivity of spinal microglia in the dorsal and ventral horns...
February 6, 2018: Neuroscience
Erika Brolin, Sofia Zelleroth, Anna Jonsson, Mathias Hallberg, Alfhild Grönbladh, Fred Nyberg
The use of opioid analgesics to treat non-cancer pain has increased over the years. Many chronic pain patients suffer from numerous adverse effects, such as reduced quality of life, development of dependence, and cognitive impairments. Cognitive processes are regulated by several systems, one of which involves growth hormone (GH) and its secondary mediator insulin-like growth factor-1 (IGF-1), but also glutamatergic transmission, including receptors such as the N-methyl-d-aspartate (NMDA)-receptor complex. In the laboratory, repeated injections are commonly used to establish animal models of long-term or chronic drug exposure...
February 5, 2018: Pharmacology, Biochemistry, and Behavior
Robert Hart, Gordon Burns, Susan Smith
Intrathecal opioids (ITOs) are commonly administered as part of a multimodal anaesthetic strategy for a variety of surgical procedures. The evolution of laparoscopic surgical techniques has seen the popularity of ITOs increase as they are effective, well tolerated and lack the cardiovascular side effects associated with epidural infusions. The risk of delayed respiratory depression remains a concern; therefore, high-quality post-operative monitoring is vital. The evidence regarding the practicalities of ITO administration such as opioid dose, type, side effect prevalence and ideal post-operative care arrangements are sparse...
February 2018: British Journal of Pain
Xian-Ping Wu, Rui-Xuan She, Yan-Ping Yang, Zu-Min Xing, Han-Wen Chen, Yi-Wen Zhang
BACKGROUND: Morphine is widely used in clinical practice for a class of analgesic drugs, long-term use of morphine will cause the action of tolerance. MicroRNAs have been reported to be involved in morphine analgesic tolerance.. METHODS: Forty male SD rats were selected and randomly divided into 5 groups: the control group, morphine tolerance group, miR-365 mimic + morphine (miR-365 mimic) group, miR-365 inhibitor + morphine (miR-365 inhibitor) group and miR-365 negative control (NC) + morphine (miR-365 NC) group...
February 7, 2018: Journal of Biomedical Science
Charles P Schaefer, Nathan B Arkwright, Leigh M Jacobs, Chelsea K Jarvis, Kristen C Hunn, Tally M Largent-Milnes, Margaret E Tome, Thomas P Davis
The rates of opioid prescription and use have continued to increase over the last few decades resulting in a greater number of opioid tolerant patients. Treatment of acute pain from surgery and injury is a clinical challenge for these patients. Several pain management strategies including prescribing increased opioids are used clinically with limited success; all currently available strategies have significant limitations. Many opioids are a substrate for p-glycoprotein (p-gp), an efflux transporter at the blood-brain barrier (BBB)...
2018: PloS One
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