Measures and CDS for Safer Opioid Prescribing: a Literature Review
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Addictions and the Brain
9/18/2012 Addictions and the Brain TAAP Conference September 14, 2012 Acknowledgements • La Hacienda Treatment Center • American Society of Addiction Medicine • National Institute of Drug Abuse © 2012 La Hacienda Treatment Center. All rights reserved. 1 9/18/2012 Definition • A primary, progressive biochemical, psychosocial, genetically transmitted chronic disease of relapse who’s hallmarks are denial, loss of control and unmanageability. DSM IV Criteria for dependency: At least 3 of the 7 below 1. Withdrawal 2. Tolerance 3. The substance is taken in larger amounts or over a longer period than was intended. 4. There is a persistent desire or unsuccessful efforts to cut down or control substance use. 5. A great deal of time is spent in activities necessary to obtain the substance, use the substance, or recover from its effects. 6. Important social, occupational, or recreational activities are given up or reduced because of the substance use. 7. The substance use is continued despite knowledge of having a persistent or recurrent physical or psychological problem that is likely to have been caused or exacerbated by the substance. © 2012 La Hacienda Treatment Center. All rights reserved. 2 9/18/2012 Dispute between behavior and disease Present understanding of the Hypothalamus location of the disease hypothesis. © 2012 La Hacienda Treatment Center. All rights reserved. 3 9/18/2012 © 2012 La Hacienda Treatment Center. All rights reserved. 4 9/18/2012 © 2012 La Hacienda Treatment Center. All rights reserved. 5 9/18/2012 Dispute regarding behavior versus disease © 2012 La Hacienda Treatment Center. All rights reserved. 6 9/18/2012 © 2012 La Hacienda Treatment Center. -
Dezocine Exhibits Antihypersensitivity Activities in Neuropathy Through
www.nature.com/scientificreports OPEN Dezocine exhibits antihypersensitivity activities in neuropathy through spinal Received: 09 November 2016 Accepted: 19 January 2017 μ-opioid receptor activation and Published: 23 February 2017 norepinephrine reuptake inhibition Yong-Xiang Wang1, Xiao-Fang Mao1, Teng-Fei Li1, Nian Gong1 & Ma-Zhong Zhang2 Dezocine is the number one opioid painkiller prescribed and sold in China, occupying 44% of the nation’s opioid analgesics market today and far ahead of the gold-standard morphine. We discovered the mechanisms underlying dezocine antihypersensitivity activity and assessed their implications to antihypersensitivity tolerance. Dezocine, given subcutaneously in spinal nerve-ligated neuropathic rats, time- and dose-dependently produced mechanical antiallodynia and thermal antihyperalgesia, significantly increased ipsilateral spinal norepinephrine and serotonin levels, and induced less antiallodynic tolerance than morphine. Its mechanical antiallodynia was partially (40% or 60%) and completely (100%) attenuated by spinal μ-opioid receptor (MOR) antagonism or norepinephrine depletion/α2-adrenoceptor antagonism and combined antagonism of MORs and α2-adenoceptors, respectively. In contrast, antagonism of spinal κ-opioid receptors (KORs) and δ-opioid receptors (DORs) or depletion of spinal serotonin did not significantly alter dezocine antiallodynia. In addition, dezocine- delayed antiallodynic tolerance was accelerated by spinal norepinephrine depletion/α2-adenoceptor antagonism. Thus dezocine produces antihypersensitivity activity through spinal MOR activation and norepinephrine reuptake inhibition (NRI), but apparently not through spinal KOR and DOR activation, serotonin reuptake inhibition or other mechanisms. Our findings reclassify dezocine as the first analgesic of the recently proposed MOR-NRI, and reveal its potential as an alternative to as well as concurrent use with morphine in treating pain. -
(19) United States (12) Patent Application Publication (10) Pub
US 20100227876A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0227876 A1 Rech (43) Pub. Date: Sep. 9, 2010 (54) METHODS OF REDUCING SIDE EFFECTS Publication Classi?cation OF ANALGESICS (51) Int CL A61K 31/485 (2006.01) A61K 31/40 (2006.01) (75) Inventor: Richard H. Rech, Okemos, MI A61K 31/445 (2006-01) (Us) A61K 31/439 (2006.01) (52) US. Cl. ........................ .. 514/282; 514/409; 514/329 (57) ABSTRACT Correspondence Address: The invention provides for compositions and methods of MARSHALL, GERSTEIN & BORUN LLP reducing pain in a subject by administering a combination of 233 SOUTH WACKER DRIVE, 6300 WILLIS mu-opioid receptor agonist, kappal-opioid receptor agonist TOWER and a nonselective opioid receptor antagonist in amounts CHICAGO, IL 60606-6357 (US) effective to reduce pain and ameliorate an adverse side effect of treatment combining opioid-receptor agonists. The inven tion also provides for methods of enhancing an analgesic effect of treatment With an opioid-receptor agonist in a sub (73) Assignee: RECHFENSEN LLP, RidgeWood, ject suffering from pain While reducing an adverse side effect NJ (US) of the treatment. The invention also provides for methods of reducing the hyperalgesic effect of treatment With an opioid receptor agonist in a subject suffering from pain While reduc ing an adverse side effect of the treatment. The invention (21) Appl. No.: 12/399,629 further provides for methods of promoting the additive anal gesia of pain treatment With an opioid-receptor agonist in a subject in need While reducing an adverse side effect of the (22) Filed: Mar. -
A Review of Unique Opioids and Their Conversions
A Review of Unique Opioids and Their Conversions Jacqueline Cleary, PharmD, BCACP Assistant Professor Albany College of Pharmacy and Health Sciences Adjunct Professor SAGE College of Nursing DISCLOSURES • Kaleo • Remitigate, LLC OBJECTIVES • Compare and contrast unique pharmacotherapy options for the treatment of chronic pain including: methadone, buprenoprhine, tapentadol, and tramadol • Select methadone, buprenorphine, tapentadol, or tramadol based on patient specific factors • Apply appropriate opioid conversion strategies to unique opioids • Understand opioid overdose risk surrounding opioid conversions and the use of unique opioids UNIQUE OPIOIDS METHADONE, BUPRENORPHINE, TRAMADOL, TAPENTADOL METHADONE My favorite drug because….? METHADONE- INDICATIONS • FDA labeled indications – (1) chronic pain (2) detoxification Oral soluble tablets for suspension NOT indicated for chronic pain treatment • Initial inpatient detoxification of opioids by a licensed trained provider with methadone and supportive care is appropriate • Methadone maintenance provider must have special credentialing and training as required by state Outpatient prescription must be for pain ONLY and say “for pain” on RX • Continuation of methadone maintenance from outside provider while patient is inpatient for another condition is appropriate http://cdn.atforum.com/wp-content/uploads/SAMHSA-2015-Guidelines-for-OTPs.pdf MECHANISM OF ACTION • Potent µ-opioid agonist • NMDA receptor antagonist • Norepinephrine reuptake inhibitor • Serotonin reuptake inhibitor ADVERSE EVENTS -
Recommendations for Prescribing Analgesia on Discharge Following Surgery Or Acute Injury Information for Health Practitioners Preparing the Patient for Discharge
Recommendations for prescribing analgesia on discharge following surgery or acute injury Information for health practitioners preparing the patient for discharge better health * better care * better value This booklet ‘Recommendations for prescribing analgesia on discharge following surgery or acute injury: Information for health practitioners preparing the patient for discharge’ is designed to be used in conjunction with the patient booklet titled ‘Pain relief medications following surgery and injury: Information for patients preparing for discharge’. Developed by the Analgesia Management Working Group (AMWG) and made available by the Western Australian Medication Safety Group (WAMSG). For more information on the WAMSG or this booklet go to website www.watag.org.au/wamsg Disclaimer: The information contained in this brochure has been produced as a guide only. It is not intended to be comprehensive and does not take the place of professional medical advice from your doctor, nurse or pharmacist. Contents Background 2 Recommendations for prescribing post-operative analgesia for pain following an acute injury or surgery 4 Precautions when prescribing opioids with other medications 6 Recommendations for prescribing discharge analgesia for pain following an acute injury or surgery 8 Paracetamol 8 Non-Steroidal Anti-inflammatory Drugs (NSAIDs) 8 Opioids 8 Communication to the primary care provider 10 Communication with the patient 10 Appendix 1 – Post-operative and post-intervention analgesia discharge checklist 11 Appendix 2 – Discharge analgesic plan 13 References 14 Recommendations for prescribing analgesia on discharge following surgery or acute injury | 1 Background The WA Medication Safety Group (WAMSG) has identified analgesia management post- surgery or acute injury (specifically managing and ceasing opioids), in the transition period from hospital to home, as a priority safety issue for patients and the community. -
Backing Material Packaging Liner
US009314527B2 (12) United States Patent (10) Patent No.: US 9,314,527 B2 Cottrell et al. (45) Date of Patent: *Apr. 19, 2016 (54) TRANSDERMAL DELIVERY PATCH 9/7061 (2013.01); A61K 9/7084 (2013.01); (71) Applicant: Phosphagenics Limited, Clayton, A61 K3I/355 (2013.01); A61K47/24 Victoria (AU) SE7 8E.O. (72) Inventors: Jeremy Cottrell, Caulfield South (AU); ( .01): ( .01): (2013.01) Giacinto Gaetano, South Melbourne (AU); Mahmoud El-Tamimy, Meadow (58) Field of Classification Search Heights (AU); Nicholas Kennedy, None Boronia (AU); Paul David Gavin, See application file for complete search history. Chadstone (AU) (56) References Cited (73) Assignee: Phosphagenics Limited, Victoria (AU) (*) Notice: Subject to any disclaimer, the term of this U.S. PATENT DOCUMENTS patent is extended or adjusted under 35 2,407,823. A 9, 1946 Fieser U.S.C. 154(b) by 0 days. 2.457,932 A 1/1949 Solmssen et al. This patent is Subject to a terminal dis- (Continued) claimer. (21) Appl. No.: 14/550,514 FOREIGN PATENT DOCUMENTS ppl. No.: 9 (22) Filed: Nov. 21, 2014 A 3.3 5.83 (65) Prior Publication Data (Continued) Related U.S. Application Data Gianello et al. Subchronic Oral Toxicity Study of Mixed Tocopheryl (63) Continuation of application No. 14/086,738, filed on Phosphates in Rates, International Journal of Toxicology, 26:475 Nov. 21, 2013, now abandoned, which is a 490; 2007.* continuation of application No. 13/501,500, filed as (Continued) application No. PCT/AU2011/000358 on Mar. 30, 2011, now Pat. No. 8,652,511. Primary Examiner — Robert A Wax (60) Provisional application No. -
Supplemental Information
REVIEW ARTICLE Supplemental Information SEARCH STRATEGIES 7. exp Congenital Abnormalities/ or remifentanil or sufentanil or 8. (defect or cleft or heart defect tapentadol or tramadol or heroin Database: Ovid MEDLINE(R) In- or nalmefene or naloxone or Process and Other Nonindexed or gastroschisis or cryptorchidism or atresia or congenital or clubfoot naltrexone).mp. Citations and Ovid MEDLINE(R), or renal or craniosynostosis or 4. 1 or 2 or 3 1946 to Present hypospadias or malformation or 5. exp pregnancy/or exp pregnancy spina bifida or neural tube defect). outcome/ mp. 1. exp Analgesics, Opioid/ 6. exp teratogenic agent/ 9. 5 or 6 or 7 or 8 2. (opioid* or opiate*).mp. 7. exp congenital disorder/ 10. 4 and 9 3. (alfentanil or alphaprodine or 11. Limit 10 to (English language and 8. (defect or cleft or heart defect buprenorphine or butorphanol humans) or gastroschisis or cryptorchidism or codeine or dezocine or or atresia or congenital or clubfoot dihydrocodeine or fentanyl or Database: Ovid Embase, 1988– or renal or craniosynostosis or hydrocodone or hydromorphone 2016, Week 7 hypospadias or malformation or or levomethadyl or levorphanol spina bifida or neural tube defect). or meperidine or methadone or mp. 1. exp opiate/ morphine or nalbuphine or opium 9. 5 or 6 or 7 or 8 or oxycodone or oxymorphone 2. (opioid* or opiate*).mp. or pentazocine or propoxyphene 10. 4 and 9 3. (alfentanil or alphaprodine or or remifentanil or sufentanil or buprenorphine or butorphanol 11. Limit 10 to (human and English tapentadol or tramadol or heroin or codeine or dezocine or language and (article or book or or nalmefene or naloxone or book series or conference paper dihydrocodeine or fentanyl or “ ” naltrexone).mp. -
(19) United States (12) Patent Application Publication (10) Pub
US 20050181041A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0181041 A1 Goldman (43) Pub. Date: Aug. 18, 2005 (54) METHOD OF PREPARATION OF MIXED Related US. Application Data PHASE CO-CRYSTALS WITH ACTIVE AGENTS (60) Provisional application No. 60/528,232, ?led on Dec. 9, 2003. Provisional application No. 60/559,862, ?led (75) Inventor: David Goldman, Portland, CT (US) on Apr. 6, 2004. Correspondence Address: Publication Classi?cation LEYDIG VOIT & MAYER, LTD (51) Int. Cl.7 ....................... .. A61K 31/56; A61K 38/00; TWO PRUDENTIAL PLAZA, SUITE 4900 A61K 9/64 180 NORTH STETSON AVENUE (52) US. Cl. ............................ .. 424/456; 514/179; 514/2; CHICAGO, IL 60601-6780 (US) 514/221 (73) Assignee: MedCrystalForms, LLC, Hunt Valley, (57) ABSTRACT MD This invention pertains to a method of preparing mixed phase co-crystals of active agents With one or more materials (21) Appl. No.: 11/008,034 that alloWs the modi?cation of the active agent to a neW physical/crystal form With unique properties useful for the delivery of the active agent, as Well as compositions com (22) Filed: Dec. 9, 2004 prising the mixed phase co-crystals. Patent Application Publication Aug. 18, 2005 Sheet 1 0f 8 US 2005/0181041 A1 FIG. 1a 214.70°C z.m."m.n... 206.98°C n..0ao 142 OJ/g as:20m=3: -0.8 -1.0 40 90 1:10 2110 Temperture (°C) FIG. 1b 0.01 as:22“.Km: 217 095 24221.4 39Jmum/Q -0.8 35 155 255 255 Temperture (°C) Patent Application Publication Aug. -
Opioid Receptorsreceptors
OPIOIDOPIOID RECEPTORSRECEPTORS defined or “classical” types of opioid receptor µ,dk and . Alistair Corbett, Sandy McKnight and Graeme Genes encoding for these receptors have been cloned.5, Henderson 6,7,8 More recently, cDNA encoding an “orphan” receptor Dr Alistair Corbett is Lecturer in the School of was identified which has a high degree of homology to Biological and Biomedical Sciences, Glasgow the “classical” opioid receptors; on structural grounds Caledonian University, Cowcaddens Road, this receptor is an opioid receptor and has been named Glasgow G4 0BA, UK. ORL (opioid receptor-like).9 As would be predicted from 1 Dr Sandy McKnight is Associate Director, Parke- their known abilities to couple through pertussis toxin- Davis Neuroscience Research Centre, sensitive G-proteins, all of the cloned opioid receptors Cambridge University Forvie Site, Robinson possess the same general structure of an extracellular Way, Cambridge CB2 2QB, UK. N-terminal region, seven transmembrane domains and Professor Graeme Henderson is Professor of intracellular C-terminal tail structure. There is Pharmacology and Head of Department, pharmacological evidence for subtypes of each Department of Pharmacology, School of Medical receptor and other types of novel, less well- Sciences, University of Bristol, University Walk, characterised opioid receptors,eliz , , , , have also been Bristol BS8 1TD, UK. postulated. Thes -receptor, however, is no longer regarded as an opioid receptor. Introduction Receptor Subtypes Preparations of the opium poppy papaver somniferum m-Receptor subtypes have been used for many hundreds of years to relieve The MOR-1 gene, encoding for one form of them - pain. In 1803, Sertürner isolated a crystalline sample of receptor, shows approximately 50-70% homology to the main constituent alkaloid, morphine, which was later shown to be almost entirely responsible for the the genes encoding for thedk -(DOR-1), -(KOR-1) and orphan (ORL ) receptors. -
Problems of Drug Dependence 1980 Proceedings of the 42Nd Annual Scientific Meeting the Committee on Problems of Drug Dependence
National Institute on Drug Abuse MONOGRAPH SERIES Problems of Drug Dependence 1980 Proceedings of the 42nd Annual Scientific Meeting The Committee on Problems of Drug Dependence, Inc. U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES • Public Health Service • Alcohol, Drug Abuse, and Mental Health Administration Problems of Drug Dependence, 1980 Proceedings of the 42nd Annual Scientific Meeting, The Committee on Problems of Drug Dependence, Inc. Editor: Louis S. Harris, Ph.D. NIDA Research Monograph 34 February 1981 DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service Alcohol, Drug Abuse, and Mental Health Administration National Institute on Drug Abuse Division of Research 5600 Fishers Lane Rockville, Maryland 20857 For sale by the Superintendent of Documents, U.S. Government Printing Office Washington, D.C. 20402 The NIDA Research Monograph series is prepared by the Division of Research of the National Institute on Drug Abuse. Its primary objective is to provide critical reviews of research problem areas and techniques, the content of state-of-the-art conferences, integrative research reviews and significant original research. Its dual publication emphasis is rapid and targeted dissemination to the scientific and professional community. Editorial Advisory Board Avram Goldstein, M.D. Addiction Research Foundation Palo Alto, California Jerome Jaffe, M.D. College of Physicians and Surgeons Columbia University, New York Reese T. Jones, M.D. Langley Porter Neuropsychiatric Institute University of California San Francisco, California William McGlothlin, Ph.D. Deportment of Psychology, UCLA Los Angeles, California Jack Mendelson, M.D. Alcohol and Drug Abuse Research Center Harvard Medical School McLean Hospital Belmont, Massachusetts Helen Nowlis, Ph.D. Office of Drug Education, DHHS Washington, D.C Lee Robins, Ph.D. -
Understanding and Challenging the Drugs: Chemistry and Toxicology
UNDERSTANDING AND CHALLENGING THE DRUGS: CHEMISTRY AND TOXICOLOGY Presenter: • Dr. Jasmine Drake, Graduate Program Director and Assistant Professor, Administration of Justice Department, Barbara Jordan-Mickey Leland School of Public Affairs, Texas Southern University NACDL Training Defending Drug Overdose Homicides in Pennsylvania Penn State Harrisburg, Middletown, PA November 6th, 2019 11:30- 12:45 p.m. Understanding & Challenging the Drugs: Chemistry & Toxicology Dr. Jasmine Drake, Forensic Science Learning Laboratory, Texas Southern University I. Opioid Drug Classifications A. Types of Opioids B. Classic vs. Synthetic C. Toxicology of Opioids 1) How opioids interact with the body 2) Addiction (psychological vs. physiological II. New Classes of Drugs A. Emerging Threats B. Potency III. National Trends in Opioid Overdose Deaths in the U.S. A. Based on State B. Ethnicity C. Drug-Type (prescription vs. fentanyl vs. heroin) IV. Trends of Opioid Overdose Deaths in Philadelphia A. Based on Ethnicity B. Drug Type (prescription vs. fentanyl vs. heroin) V. Legal Considerations to the Opioid Epidemic A. Punitive Measures vs. Rehabilitative Treatment B. Progressive Jurisdictions Nationwide C. New Legal Measures in Philadelphia VI. Toxicology Reports A. What’s in the report? B. Key Aspects of the Tox Report C. Terminology D. Evaluating and Interpreting the data? E. Questions and considerations. VII. Conclusion and Discussion A. Case Specific Examples B. Sample Toxicology Reports The Opioid Epidemic: What labs have to do with it? Ewa King, Ph.D. Associate Director of Health RIDOH State Health Laboratories Analysis. Answers. Action. www.aphl.org Overview • Overdose trends • Opioids and their effects • Analytical testing approaches • Toxicology laboratories Analysis. Answers. Action. -
VHA/Dod CLINICAL PRACTICE GUIDELINE for the MANAGEMENT of POSTOPERATIVE PAIN
VHA/DoD CLINICAL PRACTICE GUIDELINE FOR THE MANAGEMENT OF POSTOPERATIVE PAIN Veterans Health Administration Department of Defense Prepared by: THE MANAGEMENT OF POSTOPERATIVE PAIN Working Group with support from: The Office of Performance and Quality, VHA, Washington, DC & Quality Management Directorate, United States Army MEDCOM VERSION 1.2 JULY 2001/ UPDATE MAY 2002 VHA/DOD CLINICAL PRACTICE GUIDELINE FOR THE MANAGEMENT OF POSTOPERATIVE PAIN TABLE OF CONTENTS Version 1.2 Version 1.2 VHA/DoD Clinical Practice Guideline for the Management of Postoperative Pain TABLE OF CONTENTS INTRODUCTION A. ALGORITHM & ANNOTATIONS • Preoperative Pain Management.....................................................................................................1 • Postoperative Pain Management ...................................................................................................2 B. PAIN ASSESSMENT C. SITE-SPECIFIC PAIN MANAGEMENT • Summary Table: Site-Specific Pain Management Interventions ................................................1 • Head and Neck Surgery..................................................................................................................3 - Ophthalmic Surgery - Craniotomies Surgery - Radical Neck Surgery - Oral-maxillofacial • Thorax (Non-cardiac) Surgery.......................................................................................................9 - Thoracotomy - Mastectomy - Thoracoscopy • Thorax (Cardiac) Surgery............................................................................................................16