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Opioid dose ranges

Travis T Wager, Thomas A Chappie, David Horton, Ramalakshmi Y Chandrasekaran, Brian M Samas, Elizabeth Dunn-Sims, Cathleen Hsu, Nawshaba Nawreen, Michelle A Vanase-Frawley, Rebecca E O'Connor, Christopher Schmidt, Keith Dlugolenski, Nancy C Stratman, Mark J Majchrzak, Bethany L Kormos, David Nguyen, Aarti Sawant-Basak, Andy N Mead
Dopamine receptor antagonism is a compelling molecular target for the treatment of a range of psychiatric disorders, including substance use disorders. From our corporate compound file we identified a structurally unique D3 receptor (D3R) antagonist scaffold, 1. Through a hybrid approach, we merged key pharmacophore elements from 1 and D3 agonist 2 to yield the novel D3R/D2R antagonist PF-4363467 (3). Compound 3 was designed to possess CNS drug-like properties as defined by its CNS MPO desirability score (≥4/6)...
October 7, 2016: ACS Chemical Neuroscience
Rostislav Horacek, Barbora Krnacova, Jan Prasko, Klara Latalova
BACKGROUND: The aim of this study was to examine the impact of somatic illnesses, electrolyte imbalance, red blood cell count, hypotension, and antipsychotic and opioid treatment on the duration of delirium in Central Intensive Care Unit for Surgery. PATIENTS AND METHODS: Patients who were admitted to the Department of Central Intensive Care Unit for Surgery in the University Hospital Olomouc from February 2004 to November 2008 were evaluated using Riker sedation-agitation scale...
2016: Neuropsychiatric Disease and Treatment
S Michael Owens, Gerald T Pollard, James L Howard, Timothy R Fennell, Rodney W Snyder, F Ivy Carroll
JDTic is a potent and selective κ-opioid receptor (KOR) antagonist that reverses U50,488-induced diuresis in rats. It partitions into brain with a duration of action lasting for weeks. In a search for KOR antagonists that do not accumulate in the brain, we compared single doses of five methylated JDTic analogs (RTI-97, -194, -212, -240, and -241) for reversal of U50,488 diuresis and pharmacokinetic (PK) properties. All six compounds showed potent and selective KOR antagonism in a [(35)S]GTPγS binding assay...
October 4, 2016: ACS Chemical Neuroscience
Sebastian Botzenhardt, Asia N Rashed, Ian C K Wong, Stephen Tomlin, Antje Neubert
AIM: Analgesic and anti-inflammatory drugs are frequently prescribed in paediatrics. Prescribing and dosing patterns in hospitalised children are not well known. This study explores analgesic drug utilisation on five paediatric wards and discusses its findings in comparison with World Health Organization (WHO) guidelines. METHOD: A sub-analysis of a prospective, multicentre, observational cohort study was undertaken. Prescription data of children aged up to ≤18 years were collected between October 2008 and December 2009 on paediatric general medical wards in five hospitals in Australia, Germany, the United Kingdom (UK), Hong Kong (HK) and Malaysia...
September 30, 2016: Paediatric Drugs
Diab Fuad Hetta, Montaser A Mohamed, Mohammad Farouk Mohammad
STUDY OBJECTIVE: We hypothesized that oral administration of a single dose of pregabalin 2 hours before modified radical mastectomy (MRM) would produce dose-related reduction in postoperative opioid consumption. DESIGN: Prospective randomized controlled clinical trial. SETTING: Postanesthesia care unit. PATIENTS: One hundred twenty adult women scheduled for unilateral (MRM) with axillary evacuation. INTERVENTIONS: Patients were randomized to receive either, placebo capsule, pregabalin 75 mg, pregabalin 150 mg, or pregabalin 300 mg...
November 2016: Journal of Clinical Anesthesia
Gildasio S De Oliveira, Jane Bialek, R-J Marcus, Robert McCarthy
STUDY OBJECTIVE: Diphenhydramine is an antihistamine with previously demonstrated analgesic and antiemetic properties. However, it is unknown if the beneficial perioperative properties of diphenhydramine can translate to a better quality of postsurgical recovery. The main objective of the current investigation was to investigate dose-ranging effects of diphenhydramine on quality of recovery after surgery. SETTING: Tertiary hospital in the United States. DESIGN: A prospective, randomized, double-blind trial...
November 2016: Journal of Clinical Anesthesia
Abolfazl Firouzian, Afshin Gholipour Baradari, Abbas Alipour, Amir Emami Zeydi, Alieh Zamani Kiasari, Seyed Abdollah Emadi, Behrooz Kheradmand, Kaveh Hadadi
BACKGROUND: Lumbar discectomy is one of the most commonly performed neurosurgical procedures. Many patients experience postoperative pain after lumbar discectomy. This study evaluated the effect of ultra-low-dose naloxone infusion on pain intensity after lumbar discectomy in individuals receiving patient-controlled analgesia (PCA) with morphine. MATERIALS AND METHODS: In a double-blind, randomized, controlled trial, a total of 80 patients scheduled for open discectomy was randomly assigned to receive naloxone (group N) or placebo (group P)...
September 26, 2016: Journal of Neurosurgical Anesthesiology
Maureen V Hill, Michelle L McMahon, Ryland S Stucke, Richard J Barth
OBJECTIVE: To examine opioid prescribing patterns after general surgery procedures and to estimate an ideal number of pills to prescribe. BACKGROUND: Diversion of prescription opioids is a major contributor to the rising mortality from opioid overdoses. Data to inform surgeons on the optimal dose of opioids to prescribe after common general surgical procedures is lacking. METHODS: We evaluated 642 patients undergoing 5 outpatient procedures: partial mastectomy (PM), partial mastectomy with sentinel lymph node biopsy (PM SLNB), laparoscopic cholecystectomy (LC), laparoscopic inguinal hernia repair (LIH), and open inguinal hernia repair (IH)...
September 14, 2016: Annals of Surgery
Sara M Hall, Lindsay LeBaron, Cyf Ramos-Colon, Chaoling Qu, Jennifer Yanhua Xie, Frank Porreca, Josephine Lai, Yeon Sun Lee, Victor J Hruby
Dynorphin A (Dyn A) is a unique endogenous ligand that possesses well-known neuroinhibitory effects via opioid receptors with a preference for the kappa receptor but also neuroexcitatory effects, which cause hyperalgesia. We have shown that the neuroexcitatory effects are mediated through bradykinin (BK) receptors and that intrathecal ( administration of our lead ligand 1, [des-Arg(7)]-Dyn A-(4-11), which shows good binding affinity (IC50 = 150 nM) at the BK receptors, blocks Dyn A-induced hyperalgesia in naïve animals and reverses thermal and tactile hypersensitivities in a dose-dependent manner in nerve-injured animals...
September 27, 2016: ACS Chemical Neuroscience
Mathieu Fontaine, Jacques Latarjet, Jacqueline Payre, Jean-Charles Poupelin, François Ravat
INTRODUCTION: The severe pain related to repeated burn dressing changes at bedside is often difficult to manage. However these dressings can be performed at bedside on spontaneously breathing non-intubated patients using powerful intravenous opioids with a quick onset and a short duration of action such as alfentanil. The purpose of this study is to demonstrate the efficacy and safety of the protocol which is used in our burn unit for pain control during burn dressing changes. PATIENTS AND METHODS: Cohort study began after favorable opinion from local ethic committee has been collected...
September 6, 2016: Burns: Journal of the International Society for Burn Injuries
Haifeng Jiang, Maureen Hillhouse, Jiang Du, Shujun Pan, Ang Alfonso, Jun Wang, Zhirong Zhou, Weijun Yuan, Walter Ling, Min Zhao
The purpose of this study was to investigate the blood levels of methadone in participants receiving methadone for the treatment of opioid dependence. After stabilization on methadone for four weeks, blood samples from 95 participants were collected between treatment weeks 4 and 12, before and after receiving doses of methadone, and its blood levels were measured. A multiple linear regression model was used to examine the association between methadone blood levels and the outcomes of methadone maintenance treatment (MMT)...
September 10, 2016: Neuroscience Bulletin
R Wahba, R Kleinert, M Hellmich, C Kurschat, N Heiermann, G Dieplinger, J Löser, D L Stippel
INTRODUCTION: Postoperative pain management in living kidney donor nephrectomy plays a key role in donor comfort and is important for the further acceptance of living kidney donation in times of organ shortage. Standard pain treatment (SPT) based on opioids is limited due to related side effects. Continuous infusion of local anesthesia (CILA) into the operative field is a promising alternative. The aim of this study was to evaluate whether CILA could reduce the dose of opioids in living kidney donors operated with hand-assisted retroperitoneoscopic donor nephrectomy (HARP)...
July 2016: Transplantation Proceedings
Raquel Ajo, Ana Segura, María-Del-Mar Inda, Beatriz Planelles, Luz Martínez, Guillermina Ferrández, Angel Sánchez, César Margarit, Ana-María Peiró
INTRODUCTION: Long-term opioid therapy has been found to have a strong impact on the hypothalamic-pituitary-gonadal axis that can be manifested clinically by sexual dysfunction (SD). This event is rarely reported and thus unnoticed and undertreated. AIM: To analyze the presence of SD in a large group of patients receiving long-term opioids. METHODS: A descriptive, cross-sectional pilot study of sexual health was conducted for 2 years in 750 consecutive ambulatory patients with chronic non-cancer pain (CNP) receiving opioids for at least 12 months...
September 2016: Journal of Sexual Medicine
Sameer Hassamal, Karen Miotto, Tisha Wang, Andrew J Saxon
BACKGROUND AND OBJECTIVES: Opioids increase the risk for sleep disordered breathing (SDB), but there are few studies examining the prevalence and risk factors for SDB, specifically central sleep apnea (CSA), and obstructive sleep apnea (OSA) in chronic pain patients on opioids as well as methadone maintained patients (MMPs). METHODS: A literature review was conducted in which SDB was confirmed by polysomnography (PSG) in chronic pain patients on opioids as well as patients with a diagnosis of an opioid use disorder or opioid dependence on methadone maintenance treatment (MMT)...
September 2016: American Journal on Addictions
Jacob Hutchins, Ioanna Apostolidou, Sara Shumway, Rosemary Kelly, Qi Wang, Cody Foster, Gabriel Loor
OBJECTIVE: Effective postoperative pain management has been shown to be a positive predictive factor for postoperative recovery following a thoracotomy. The primary objective of this study was to examine the efficacy and safety of continuous paravertebral blockade in managing acute postsurgical pain following unilateral and bilateral single-lung transplantation. DESIGN: The authors conducted a prospective observational trial of patients. SETTING: The study was conducted in an academic university hospital...
May 4, 2016: Journal of Cardiothoracic and Vascular Anesthesia
Ahmad Abdulrahman Almeman, R Ismail, Markus Perola
INTRODUCTION: Methadone is accepted as an alternative therapy in opioid use disorders worldwide. Methadone responsiveness , however, is affected by a range of CYP450 enzymes and OPRM1 polymorphisms. OBJECTIVE: This study sought to detect CYP2B6 and OPRM1 variants and their genotypes, as major contributors to inter-variability in methadone responsiveness and methadone dose requirements. METHODS: We carried out a prospective experimental one-phase pharmacogenetic study in four addiction clinics in Malaysia...
August 10, 2016: Drug Metabolism Letters
Guillermo Alberto Keller, María Cecilia Villa Etchegoyen, Nicolás Fernández, Nancy Mónica Olivera, Patricia Noemí Quiroga, Roberto Alejandro Diez, Guillermo Di Girolamo
: A prolongation of the QTc-interval has been described for several opioids, including pethidine (meperidine). OBJECTIVE: To evaluate in the clinical setting the frequency and risk factors associated with the QT-interval prolongation induced by meperidine. RESEARCH DESIGN AND METHODS: We recruited patients requiring meperidine administration and recorded their medical history and comorbidities predisposing to QT-interval prolongation. Ionograms and electrocardiograms (ECGs) were performed at baseline and during treatment; QT was corrected using the Bazzet, Fridericia, Framinghan, and Hogdes formulas...
August 11, 2016: International Journal of Clinical Pharmacology and Therapeutics
I Elias Veizi, Salim M Hayek, Michael Hanes, Ryan Galica, Sivakanth Katta, Tony Yaksh
BACKGROUND: Intrathecal drug delivery therapy has been used effectively in treating patients with intractable chronic pain. The development of an intrathecal catheter tip granuloma (ICTG) related to delivery of intrathecal opiates is a relatively infrequent, but potentially devastating complication. While there are many morphine-related ICTG cases described, reports of hydromorphone-related ICTG are limited. In addition, studies suggest a strong correlation between the use of higher doses and concentrations of intrathecal opiates and ICTG formation...
October 2016: Neuromodulation: Journal of the International Neuromodulation Society
J C G van Niel, J Schneider, T M Tzschentke
Buprenorphine and the mixed agonists/antagonists nalbuphine and pentazocine, formerly classified as µ-opioid (MOP) receptor antagonists, have more recently been shown to be partial to full agonists of the human MOP receptor. These receptors do not necessarily have to be maximally activated for a full physiological response. Partial agonists can also sufficiently stimulate signaling processes leading to a full analgesic response, as shown by the effectiveness of buprenorphine, nalbuphine and pentazocine in animal pain models and in clinical settings where these drugs induce analgesia with full efficacy without a ceiling effect...
August 9, 2016: Drug Research
Jin Han, Santosh L Saraf, Xu Zhang, Michel Gowhari, Robert E Molokie, Johara Hassan, Chaher Alhandalous, Shivi Jain, Jewel Younge, Taimur Abbasi, Roberto F Machado, Victor R Gordeuk
Pain, the hallmark complication of sickle cell disease (SCD), is largely managed with opioid analgesics in the United States, but comprehensive data regarding the long-term use of opioids in this patient population is lacking. The pain medication prescription records from a cohort of 203 SCD patients were analyzed. Twenty-five percent were not prescribed opioid medications while 47% took only short-acting opioids, 1% took only long-acting opioids, and 27% took a combination of short-acting and long-acting opioids...
July 28, 2016: American Journal of Hematology
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