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Opioid tolerance

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https://www.readbyqxmd.com/read/29158012/a-randomized-double-blind-placebo-controlled-proof-of-concept-study-to-evaluate-samidorphan-in-the-prevention-of-olanzapine-induced-weight-gain-in-healthy-volunteers
#1
Bernard L Silverman, William Martin, Asli Memisoglu, Lauren DiPetrillo, Christoph U Correll, John M Kane
Antipsychotic medications are associated with weight gain and adverse metabolic effects that complicate the treatment and management of schizophrenia. Olanzapine (OLZ) in particular is associated with significant weight gain and adverse metabolic effects. The present Phase 1, proof of concept, multicenter, randomized, double-blind, placebo-controlled study investigated the safety and effect on weight of a combination of OLZ (10mg) and the opioid modulator samidorphan (SAM; 5mg) in comparison to OLZ alone in healthy, male normal weight volunteers...
November 17, 2017: Schizophrenia Research
https://www.readbyqxmd.com/read/29149154/philosophical-issues-and-psychological-variables-that-influence-the-determination-of-opioid-effectiveness-a-narrative-review
#2
Daniel Michael Doleys
BACKGROUND: The prescribing of opioids in the chronic pain setting is often based on the pharmacodynamics, pharmacokinetics, and pharmacogenetics of the drug obtained during development and clinical trials. However, the effectiveness of opioids varies widely and often appears to bear no relationship to the aforementioned variables. The impact of philosophical issues and psychological factors on determining how clinically effective opioid therapy is has often been over looked. OBJECTIVES: This manuscript provides a selective review and narrative summary of the philosophical issues and psychological factors which can influence opioid effectiveness...
November 2017: Pain Physician
https://www.readbyqxmd.com/read/29147587/dexmedetomidine-as-part-of-a-multimodal-analgesic-treatment-regimen-for-opioid-induced-hyperalgesia-in-a-patient-with-significant-opioid-tolerance
#3
Richard K Patch Iii, Jason S Eldrige, Susan M Moeschler, Matthew J Pingree
Acute postoperative pain in patients with opioid tolerance creates a significant management challenge for anesthesiologists and pain medicine physicians. A multimodal approach is key; however other factors can complicate management such as opioid induced hyperalgesia. We present the case of a patient on large amounts of intrathecal opioids for chronic pain syndrome with opioid induced hyperalgesia after an exploratory laparotomy. Dexmedetomidine was utilized successfully as part of a controlled multimodal analgesic plan and should be a consideration for opioid tolerant patients experiencing opioid induced hyperalgesia...
2017: Case Reports in Anesthesiology
https://www.readbyqxmd.com/read/29146238/ccr5-mediates-hiv-1-tat-induced-neuroinflammation-and-influences-morphine-tolerance-dependence-and-reward
#4
Maciej Gonek, Virginia D McLane, David L Stevens, Kumiko Lippold, Hamid I Akbarali, Pamela E Knapp, William L Dewey, Kurt F Hauser, Jason J Paris
The HIV-1 regulatory protein, trans-activator of transcription (Tat), interacts with opioids to potentiate neuroinflammation and neurodegeneration within the CNS. These effects may involve the C-C chemokine receptor type 5 (CCR5); however, the behavioral contribution of CCR5 on Tat/opioid interactions is not known. Using a transgenic murine model that expresses HIV-1 Tat protein in a GFAP-regulated, doxycycline-inducible manner, we assessed morphine tolerance, dependence, and reward. To assess the influence of CCR5 on these effects, mice were pretreated with oral vehicle or the CCR5 antagonist, maraviroc, prior to morphine administration...
November 13, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29145012/the-gut-brain-interaction-in-opioid-tolerance
#5
REVIEW
Hamid I Akbarali, William L Dewey
The prevailing opioid crisis has necessitated the need to understand mechanisms leading to addiction and tolerance, the major contributors to overdose and death and to develop strategies for developing drugs for pain treatment that lack abuse liability and side-effects. Opioids are commonly used for treatment of pain and symptoms of inflammatory bowel disease. The significant effect of opioids in the gut, both acute and chronic, includes persistent constipation and paradoxically may also worsen pain symptoms...
November 13, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29143891/in-search-of-the-ideal-promotility-agent-optimal-use-of-currently-available-promotility-agents-for-nutrition-therapy-of-the-critically-ill-patient
#6
REVIEW
Sarah J Diamond, Endashaw Omer, Laszlo Kiraly
PURPOSE OF REVIEW: Enteral nutrition therapy is essential in the management of critically ill patients. Prokinetic agents have been used successfully to aid in the delivery of nutrition and improve feeding tolerance in patients in the intensive care unit (ICU). The aim of this report is to review the existing promotility agents available for use in the critically ill as well as outline the role of potential investigative drugs in order to provide a guide to the management of this difficult and important clinical dilemma...
November 16, 2017: Current Gastroenterology Reports
https://www.readbyqxmd.com/read/29122372/sufentanil-sublingual-tablet-30mcg-for-moderate-to-severe-acute-pain-in-the-emergency-department
#7
James R Miner, Zubaid Rafique, Harold S Minkowitz, Karen P DiDonato, Pamela P Palmer
BACKGROUND: Pharmacological properties of the sufentanil sublingual tablet 30mcg (SST 30mcg) could offer potential analgesic advantages in settings requiring noninvasive, acute pain management. The feasibility of using SST 30mcg for moderate-to-severe pain management in the emergency department (ED) was evaluated. METHODS: This open-label, multicenter feasibility study included patients aged ≥18years who presented to the ED with moderate-to-severe pain (≥4 on the numeric rating scale of pain intensity (NRS); opioid-tolerant patients were excluded...
October 31, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/29121695/the-effect-of-preoperative-physical-status-on-pain-management-in-total-knee-arthroplasty-patients-receiving-adductor-canal-blockade
#8
Chukwuweike U Gwam, Jaydev B Mistry, Nequesha S Mohamed, Nicole E George, Jennifer I Etcheson, Sana Virani, Ryan Skalsky, Shreya Singh, Nicolas S Piuzzi, Ronald E Delanois
INTRODUCTION: Managing postoperative pain can be challenging for arthroplasty surgeons. While pain control modalities, such as adductor canal blockade (ACB), have been proven effective, the multifactorial nature of pain perception may serve as an obstacle for optimizing pain control. This study assesses the effect of patient pre-operative physical status on patient perception of pain. Specifically, we compared 1) lengths of hospital stay (LOS), 2) pain levels, and 3) opioid consumption in patients receiving total knee arthroplasty (TKA) who presented with an American Society of Anesthesiologists physical status score (ASA) of 2 and 3...
November 9, 2017: Surgical Technology International
https://www.readbyqxmd.com/read/29103572/practical-management-of-the-opioid-tolerant-patient-in-the-perioperative-surgical-home
#9
REVIEW
John-Paul J Pozek, Stephen F Goldberg, Jaime L Baratta, Eric S Schwenk
No abstract text is available yet for this article.
2017: Advances in Anesthesia
https://www.readbyqxmd.com/read/29101087/methadone-as-first-line-opioid-in-cancer-pain-management-a-systematic-review
#10
REVIEW
Sebastiano Mercadante, Eduardo Bruera
AIM: The objective of this review was to assess the existent evidence for the use of methadone as first line therapy in cancer pain management. METHODS: A systematic literature search on MedLine, Embase databases was carried out from each data base, setting up the date to 30 August 2017 Studies were included if methadone was a first line drug as a step 3 of WHO analgesic ladder, or at low doses (step 2), if they were conducted in adult patients with cancer pain, if they contained outcomes on pain and opioid-related adverse effects...
October 31, 2017: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/29098567/oxycodone-naloxone-prolonged-release-a-review-in-severe-chronic-pain
#11
Esther S Kim
Oral oxycodone/naloxone prolonged release (PR) [Targin(®), Targinact(®), Targiniq(®)] is a 12-hourly opioid receptor agonist and opioid receptor antagonist fixed-dose combination product that is approved in countries in the EU for the management of severe pain (adequately manageable only with opioid analgesics) in adults. Oral naloxone prevents oxycodone from binding to μ-receptors in the gastrointestinal (GI) tract, thereby counteracting opioid-induced constipation (OIC). In short-term (5- to 12-week) clinical trials of adults with moderate to severe, chronic pain and OIC (OXN3001, OXN3006, OXN3506), oxycodone/naloxone PR significantly improved OIC while providing noninferior analgesia relative to oxycodone PR; results were consistent between cancer and non-cancer patients in OXN3506...
December 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29097440/desensitization-and-tolerance-of-mu-opioid-receptors-on-pontine-kolliker-fuse-neurons
#12
Erica S Levitt, John T Williams
Acute desensitization of mu opioid receptors is thought to be an initial step in the development of tolerance to opioids. Given the resistance of the respiratory system to develop tolerance, desensitization of neurons in the Kölliker-Fuse (KF), a key area in the respiratory circuit, was examined. The activation of G protein-coupled inwardly rectifying potassium (GIRK) current was measured using whole-cell voltage-clamp recordings from KF and locus coeruleus (LC) neurons contained in acute rat brain slices...
November 2, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29090081/eluxadoline-in-irritable-bowel-syndrome-with-diarrhea-rationale-evidence-and-place-in-therapy
#13
REVIEW
Kenneth Barshop, Kyle Staller
Irritable bowel syndrome (IBS) is the most common gastrointestinal (GI) disorder worldwide, however treatment options for diarrhea-predominant IBS (IBS-D) remain limited. Eluxadoline, a µ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, was recently approved for the treatment of IBS-D. A novel compound first described in 2008, eluxadoline was shown to normalize GI transit, with a subsequent phase I demonstrating its safety and tolerability in healthy adults. In 2016, two randomized, double-blind, placebo-controlled phase III trials studying eluxadoline use at 75 mg and 100 mg twice daily over 26 weeks demonstrated a significant improvement in stool consistency and many global symptoms of IBS...
November 2017: Therapeutic Advances in Chronic Disease
https://www.readbyqxmd.com/read/29071900/-progress-of-researches-on-central-mechanism-of-electroacupuncture-tolerance
#14
Lu-Ying Cui, Ming-Xing Ding
Electroacupuncture (EA) has been demonstrated effective for pain relief. However, repeated application may decline analgesic effect of EA, which is termed EA tolerance, that reduces the clinical efficacy of EA. Therefore, it has attracted attention from researchers in recent years and the progresses include:(1) acute and chronic EA tolerance animal models have been established; (2) cross-tolerance between EA and morphine; (3) Anti-opioid substances, including cholecystokinin, orphanin FQ and angiotensin Ⅱ, have been reported to contribute to EA tolerance; (4) glutamate receptors and transporters, 5-hydroxytryptamine and norepinephrine have been revealed involvement in EA tolerance; (5) cyclic adenosine monophosphate, cyclic guanosine monophosphate and Ca(2+) have been reported to be the second messengers cellularly in EA tolerance...
December 25, 2016: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29062240/a-randomized-phase-iib-study-investigating-oliceridine-trv130-a-novel-%C3%A2%C2%B5-receptor-g-protein-pathway-selective-%C3%AE-gps-modulator-for-the-management-of-moderate-to-severe-acute-pain-following-abdominoplasty
#15
Neil Singla, Harold S Minkowitz, David G Soergel, David A Burt, Ruth Ann Subach, Monica Y Salamea, Michael J Fossler, Franck Skobieranda
BACKGROUND: Oliceridine (TRV130), a novel μ-receptor G-protein pathway selective (μ-GPS) modulator, was designed to improve the therapeutic window of conventional opioids by activating G-protein signaling while causing low β-arrestin recruitment to the μ receptor. This randomized, double-blind, patient-controlled analgesia Phase IIb study was conducted to investigate the efficacy, safety, and tolerability of oliceridine compared with morphine and placebo in patients with moderate to severe pain following abdominoplasty (NCT02335294; oliceridine is an investigational agent not yet approved by the US Food and Drug Administration)...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29056153/oxytocin-tolerance-and-the-dark-side-of-addiction
#16
Cort A Pedersen
Substance use disorders blight the lives of millions of people and inflict a heavy financial burden on society. There is a compelling need for new pharmacological treatments as current drugs have limited efficacy and other major drawbacks. A substantial number of animal and recent clinical studies indicate that the neuropeptide, oxytocin, is a particularly promising therapeutic agent for human addictions, especially alcohol use disorders. In preliminary trials, we found that oxytocin administered by the intranasal route, which produces some neuropeptide penetration into the CNS, potently blocked withdrawal and reduced alcohol consumption in heavy drinkers...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/29056067/-express-usefulness-for-the-combination-of-g-protein-and-%C3%AE-arrestin-biased-ligands-of-%C3%AE-opioid-receptors-prevention-of-antinociceptive-tolerance
#17
Tomohisa Mori, Naoko Kuzumaki, Takamichi Arima, Michiko Narita, Ryunosuke Tateishi, Takashige Kondo, Yusuke Hamada, Hirotsugu Kuwata, Miho Kawata, Mitsuaki Yamazaki, Kazuyuki Sugita, Akinobu Matsuzawa, Kanae Baba, Takayasu Yamauchi, Kimio Higashiyama, Miki Nonaka, Kanako Miyano, Yasuhito Uezono, Minoru Narita
No abstract text is available yet for this article.
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/29054049/individual-variability-in-clinical-effect-and-tolerability-of-opioid-analgesics-importance-of-drug-interactions-and-pharmacogenetics
#18
REVIEW
Vigdis Solhaug, Espen Molden
BACKGROUND: As pain is often a comorbid condition, many patients use opioid analgesics in combination with several other drugs. This implies a generally increased risk of drug interactions, which along with inherent pharmacogenetic variability and other factors may cause differences in therapeutic response of opioids. AIM: To provide an overview of interactions and pharmacogenetic variability of relevance for individual differences in effect and tolerability of opioid analgesics, which physicians and other healthcare professionals should be aware of in clinical practice...
October 17, 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29049115/an-evidence-based-approach-to-the-prescription-opioid-epidemic-in-orthopedic-surgery
#19
REVIEW
Ellen M Soffin, Seth A Waldman, Roberta J Stack, Gregory A Liguori
Orthopedic surgery is associated with significant perioperative pain. Providing adequate analgesia is a critical component of patient care and opioids play a vital role in the acute postoperative setting. However, opioid prescribing for patients undergoing orthopedic procedures has recently been identified as a major contributor to the current opioid epidemic. As opioid usage and related morbidity and mortality continue to rise nationwide, opioid-prescribing practices are under increased scrutiny. Here, we update the evidence base and recommendations behind a set of interventions developed at the Hospital for Special Surgery to address the national epidemic at the local level...
November 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29045243/use-of-ketamine-in-a-multimodal-analgesia-setting-for-rapid-opioid-tapering-in-a-profoundly-opioid-tolerant-patient-a-case-report
#20
Elise M Strickler, Eric S Schwenk, Mitchell J Cohen, Eugene R Viscusi
Opioids are frequently used for the treatment of chronic pain, and patients taking high doses are at increased risk of complications and adverse opioid-related events. Ketamine is appealing as an opioid adjunct because of its lack of respiratory depression and potential prevention of hyperalgesia and central sensitization. We present a case in which a ketamine infusion was utilized over a 7-day period to provide rapid taper of a daily dose of 400 mg of morphine equivalents to less than one-third of that dose on discharge with unchanged pain levels and no symptoms of opioid withdrawal...
October 17, 2017: A & A Case Reports
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