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Opioid pharmacology

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https://www.readbyqxmd.com/read/28224474/pain-severity-and-pharmacologic-pain-management-among-community-living-older-adults-the-mobilize-boston-study
#1
Ampicha Nawai, Suzanne G Leveille, Robert H Shmerling, Guusje van der Leeuw, Jonathan F Bean
BACKGROUND: Concerns about polypharmacy and medication side effects contribute to undertreatment of geriatric pain. This study examines use and effects of pharmacologic treatment for persistent pain in older adults. METHODS: The MOBILIZE Boston Study included 765 adults aged ≥70 years, living in the Boston area, recruited from 2005 to 2008. We studied 599 participants who reported chronic pain at baseline. Pain severity, measured using the Brief Pain Inventory (BPI) severity subscale, was grouped as very mild (BPI <2), mild (BPI 2-3...
February 21, 2017: Aging Clinical and Experimental Research
https://www.readbyqxmd.com/read/28221178/non-neuraxial-labor-analgesia-options
#2
John C Markley, Mark D Rollins
Although it is the most effective method to treat labor pain, neuraxial analgesia may be undesired, contraindicated, unsuccessful, or unavailable. Providing safe choices for labor pain relief is a central goal of health care providers alike. Consequently, knowledge of the efficacy, clinical implementation, and side effects of various non-neuraxial strategies is needed to provide appropriate options for laboring patients. In addition to nonpharmacologic alternatives, inhaled nitrous oxide and systemic opioids represent two broad classes of non-neuraxial pharmacologic labor analgesia most commonly available...
February 17, 2017: Clinical Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28220108/adaptations-in-basal-and-hypothalamic-pituitary-adrenal-activated-deoxycorticosterone-responses-following-ethanol-self-administration-in-cynomolgus-monkeys
#3
Vanessa A Jimenez, Patrizia Porcu, A Leslie Morrow, Kathleen A Grant
Acute ethanol activates the hypothalamic-pituitary-adrenal (HPA) axis, while long-term exposure results in a blunted neuroendocrine state, particularly with regards to the primary endpoint, cortisol, the primary glucocorticoid produced in the adrenal cortex. However, it is unknown if this dampened neuroendocrine status also influences other adrenocortical steroids. Plasma concentration of the mineralocorticoid and neuroactive steroid precursor deoxycorticosterone (DOC) is altered by pharmacological challenges of the HPA axis in cynomolgus monkeys...
2017: Frontiers in Endocrinology
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/28215164/innovative-opioid-peptides-and-biased-agonism-novel-avenues-for-more-effective-and-safer-analgesics-to-treat-chronic-pain
#5
Andrea Bedini, Santi Mario Spampinato
Chronic pain is a clinically relevant and yet unsolved conditions that is poorly treated with the currently available drugs, thus highlighting the urgent need of innovative analgesics. Although opiates are not very effective in the treatment of inflammatory and neuropathic pain, developing novel opioid receptor peptide agonists, as well as modulating the opioid receptor-mediated responses in a ligand-specific fashion, may represent an innovative and promising strategy to identify more efficacious and safer antalgic drugs...
February 15, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28214687/gastroprotective-effect-and-mechanism-of-action-of-croton-rhamnifolioides-essential-oil-in-mice
#6
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/28214183/-misuse-and-dependence-on-prescription-opioids-prevention-identification-and-treatment
#7
B Rolland, D Bouhassira, N Authier, M Auriacombe, V Martinez, P Polomeni, G Brousse, R Schwan, P Lack, J Bachellier, S Rostaing, P Bendimerad, P Vergne-Salle, M Dematteis, S Perrot
Since the 1990s, the use of prescription opioids has largely spread, which has brought a real progress in the treatment of pain. The long-term use of prescription opioid is sometimes required, and may lead to pharmacological tolerance and withdrawal symptoms, i.e. pharmacological dependence on prescription opioids. Occasionally, this may also lead to misuse of prescription opioids (MPO). MPO preferentially occurs in vulnerable individuals, i.e., those with a young age, history of other addictive or psychiatric disorders, especially anxious and depressive disorders...
February 14, 2017: La Revue de Médecine Interne
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
#8
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/28203347/killing-two-birds-with-one-stone-successful-opioid-monotherapy-in-intractable-migraine-triggered-epilepsy-a-case-series
#9
REVIEW
Iraj Derakhshan
The novel concept explored in this case series is the primacy of headaches in generating seizures in those patients who suffer from migraine-triggered epilepsy. In this series, once the migraine headaches were fully suppressed, via daily scheduled opioid therapy, the seizures also stopped. Seizures returned, however, after the patients stopped the opiate regimen for any reason. The above pharmacological scenario is reminiscent of a similar but naturalistic course of events reported on the salutary effects of ketogenic diet, or changes in life style, in similar cases of migraine-triggered epilepsy...
January 2017: Therapeutic Advances in Chronic Disease
https://www.readbyqxmd.com/read/28199917/desomorphine-krokodil-an-overview-of-its-chemistry-pharmacology-metabolism-toxicology-and-analysis
#10
REVIEW
Diego Hernando Ângulo Florez, Ana Maria Dos Santos Moreira, Pedro Rafael da Silva, Ricardo Brandão, Marcella Matos Cordeiro Borges, Fernando José Malagueño de Santana, Keyller Bastos Borges
BACKGROUND: "Krokodil" or "Crocodile" is an illegal homemade desomorphine drug obtained from chemical reactions of commercial codeine drugs with several other powerful and highly toxic chemical agents increasing its addiction and hallucinogenic effects when compared with other morphine analogues. METHODS: This paper summarizes a complete review about an old drug called desomorphine (Krokodil), presenting its chemistry, pharmacology, metabolism, toxicology and analysis...
January 31, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28192790/systemic-pharmacologic-therapies-for-low-back-pain-a-systematic-review-for-an-american-college-of-physicians-clinical-practice-guideline
#11
Roger Chou, Richard Deyo, Janna Friedly, Andrea Skelly, Melissa Weimer, Rochelle Fu, Tracy Dana, Paul Kraegel, Jessica Griffin, Sara Grusing
Background: A 2007 American College of Physicians guideline addressed pharmacologic options for low back pain. New evidence and medications have now become available. Purpose: To review the current evidence on systemic pharmacologic therapies for acute or chronic nonradicular or radicular low back pain. Data Sources: Ovid MEDLINE (January 2008 through November 2016), Cochrane Central Register of Controlled Trials, Cochrane Database of Systematic Reviews, and reference lists...
February 14, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28192789/noninvasive-treatments-for-acute-subacute-and-chronic-low-back-pain-a-clinical-practice-guideline-from-the-american-college-of-physicians
#12
Amir Qaseem, Timothy J Wilt, Robert M McLean, Mary Ann Forciea
Description: The American College of Physicians (ACP) developed this guideline to present the evidence and provide clinical recommendations on noninvasive treatment of low back pain. Methods: Using the ACP grading system, the committee based these recommendations on a systematic review of randomized, controlled trials and systematic reviews published through April 2015 on noninvasive pharmacologic and nonpharmacologic treatments for low back pain. Updated searches were performed through November 2016...
February 14, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28192197/characterization-of-3-h-oxymorphone-binding-sites-in-mouse-brain-quantitative-autoradiography-in-opioid-receptor-knockout-mice
#13
Ji Hoon Yoo, Anna Borsodi, Géza Tóth, Sándor Benyhe, Robert Gaspar, Audrey Matifas, Brigitte L Kieffer, Athanasios Metaxas, Ian Kitchen, Alexis Bailey
Oxymorphone, one of oxycodone's metabolic products, is a potent opioid receptor agonist which is thought to contribute to the analgesic effect of its parent compound and may have high potential abuse liability. Nonetheless, the in vivo pharmacological binding profile of this drug is still unclear. This study uses mice lacking mu (MOP), kappa (KOP) or delta (DOP) opioid receptors as well as mice lacking all three opioid receptors to provide full characterisation of oxymorphone binding sites in the brain. Saturation binding studies using [(3)H]oxymorphone revealed high affinity binding sites in mouse brain displaying Kd of 1...
February 10, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28188737/genetic-variation-in-the-behavioral-effects-of-buprenorphine-in-female-mice-derived-from-a-murine-model-of-the-oprm1-a118g-polymorphism
#14
Caroline A Browne, Rebecca L Erickson, Julie A Blendy, Irwin Lucki
Pharmacogenetic studies have identified the non-synonymous single nucleotide polymorphism (A118G) in the human mu opioid receptor (MOR) gene (OPRM1) as a critical genetic variant capable of altering the efficacy of opioid therapeutics. To date few studies have explored the potential impact of the OPRM1 A118G polymorphism on the pharmacological effects of buprenorphine (BPN), a potent MOR partial agonist and kappa opioid receptor antagonist, which is approved by the FDA for the treatment of opioid addiction and chronic pain...
February 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28187838/pharmacologic-treatment-of-opioid-addiction-during-pregnancy
#15
REVIEW
Lori Keough, Heidi Collins Fantasia
Opioid addiction during pregnancy presents a treatment challenge to clinicians and women alike. Untreated addiction can lead to poor maternal and fetal health outcomes. Medication-assisted treatment is the standard of care, and methadone is the current drug of choice for treatment. Emerging evidence also supports the use of buprenorphine during pregnancy. Both methadone and buprenorphine have risks and benefits that should be explored before initiating treatment. Clinicians who work in obstetrics and in addiction treatment can collaborate and coordinate treatment to ensure optimal maternal and fetal outcomes...
February 2017: Nursing for Women's Health
https://www.readbyqxmd.com/read/28179123/spinal-or-supraspinal-phosphorylation-deficiency-at-the-mor-c-terminus-does-not-affect-morphine-tolerance-in-vivo
#16
Cherkaouia Kibaly, Hong-Yiou Lin, Horace H Loh, Ping-Yee Law
The development of tolerance to morphine, one of the most potent analgesics, in the management of chronic pain is a significant clinical problem and its mechanisms are poorly understood. Morphine exerts its pharmacological effects via the μ-opioid receptor (MOR). Tolerance is highly connected to G-protein-coupled receptors (GPCR) phosphorylation and desensitization increase. Because morphine desensitization previously has been shown to be MOR phosphorylation- and ß-arrestin2-independent (in contrast to agonists such as fentanyl), we examined the contribution of phosphorylation of the entire C-terminus to the development of antinociceptive tolerance to the partial (morphine) and full (fentanyl) MOR agonists in vivo...
February 4, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28176937/an-integrated-perspective-on-diabetic-alcoholic-and-drug-induced-neuropathy-etiology-and-treatment-in-the-us
#17
REVIEW
Lily Zeng, Doungkamol Alongkronrusmee, Richard M van Rijn
Neuropathic pain (NeuP) is a syndrome that results from damaged nerves and/or aberrant regeneration. Common etiologies of neuropathy include chronic illnesses and medication use. Chronic disorders, such as diabetes and alcoholism, can cause neuronal injury and consequently NeuP. Certain medications with antineoplastic effects also carry an exquisitely high risk for neuropathy. These culprits are a few of many that are fueling the NeuP epidemic, which currently affects 7%-10% of the population. It has been estimated that approximately 10% and 7% of US adults carry a diagnosis of diabetes and alcohol disorder, respectively...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28162575/-123-non-adherence-to-strong-opioids-regime-in-an-advanced-cancer-population-with-pain-pharmacological-pitfalls-or-not
#18
J Canal-Sotelo, N Arraras-Torrelles, J Lopez-Ribes, E Barallat-Gimeno, A Gasol-Cudós, R Gonzalez-Rubio
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28161300/development-and-delivery-of-a-pharmacist-training-program-to-increase-naloxone-access-in-kentucky
#19
Emma Palmer, Steve Hart, Patricia R Freeman
OBJECTIVE: To describe the development and delivery of a comprehensive training program for Kentucky pharmacists to enable dispensation of naloxone per protocol. PRACTICE DESCRIPTION: In May 2015, the Kentucky Board of Pharmacy (KBP) promulgated regulations outlining the requirements for pharmacists to initiate the dispensing of naloxone under a physician-approved protocol. The Advancing Pharmacy Practice in Kentucky Coalition, a partnership between Kentucky's Colleges of Pharmacy, KBP, and state and local pharmacists associations, developed and offered educational programming to fulfill this regulation...
February 1, 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28156584/survivor-pain-experience-at-an-oncology-palliative-care-clinic
#20
Lisa Emond, Ann Wojtaszczyk
: 260 Background: As of January 2014 there are an estimated 14.5 million cancer survivors in the United States. In observational studies of cancer survivors up to 40% report chronic pain. Opioids remain an important and effective treatment for active cancer pain. For survivors, however, we must take into account the paucity of data supporting long term benefits of opioids on pain and functional outcomes, and extensive evidence of potential harms. We present data from our palliative care clinic where we have established a nuanced approach to pain management in this population, which includes risk mitigation, consistent education, emphasis on non-pharmacological and non-opiate medications, and attempts to down-taper opioid analgesics when feasible...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
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