STOP Act Prescribing Limit Faqs
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Opioid Tolerance in Methadone Maintenance Treatment: Comparison
Gutwinski et al. Harm Reduction Journal (2016) 13:7 DOI 10.1186/s12954-016-0095-0 RESEARCH Open Access Opioid tolerance in methadone maintenance treatment: comparison of methadone and levomethadone in long-term treatment Stefan Gutwinski*, Nikola Schoofs, Heiner Stuke, Thomas G. Riemer, Corinde E. Wiers and Felix Bermpohl Abstract Background: This study aimed to investigate the development of opioid tolerance in patients receiving long-term methadone maintenance treatment (MMT). Methods: A region-wide cross-sectional study was performed focusing on dosage and duration of treatment. Differences between racemic methadone and levomethadone were examined. All 20 psychiatric hospitals and all 110 outpatient clinics in Berlin licensed to offer MMT were approached in order to reach patients under MMT fulfilling the DSM IV criteria of opiate dependence. In the study, 720 patients treated with racemic methadone or levomethadone gave information on the dosage of treatment. Out of these, 679 patients indicated the duration of MMT. Results: Treatment with racemic methadone was reported for 370 patients (54.5 %), with levomethadone for 309 patients (45.5 %). Mean duration of MMT was 7.5 years. We found a significant correlation between dosage and duration of treatment, both in a conjoint analysis for the two substances racemic methadone and levomethadone and for each substance separately. These effects remained significant when only patients receiving MMT for 1 year or longer were considered, indicating proceeding tolerance development in long-term treatment. When correlations were compared between racemic methadone and levomethadone, no significant difference was found. Conclusions: Our data show a tolerance development under long-term treatment with both racemic methadone and levomethadone. -
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. -
Nitrous Oxide in Emergency Medicine Í O’ Sullivan, J Benger
214 ANALGESIA Emerg Med J: first published as 10.1136/emj.20.3.214 on 1 May 2003. Downloaded from Nitrous oxide in emergency medicine Í O’ Sullivan, J Benger ............................................................................................................................. Emerg Med J 2003;20:214–217 Safe and predictable analgesia is required for the identify these zones as there is considerable vari- potentially painful or uncomfortable procedures often ation between people. He also emphasised the importance of the patient’s pre-existing beliefs. If undertaken in an emergency department. The volunteers expect to fall asleep while inhaling characteristics of an ideal analgesic agent are safety, 30% N2O then a high proportion do so. An appro- predictability, non-invasive delivery, freedom from side priate physical and psychological environment increases the actions of N2O and may allow lower effects, simplicity of use, and a rapid onset and offset. doses to be more effective. Unlike many other Newer approaches have threatened the widespread use anaesthetic agents, N2O exhibits an acute toler- of nitrous oxide, but despite its long history this simple ance effect, whereby its potency is greater at induction than after a period of “accommoda- gas still has much to offer. tion”. .......................................................................... MECHANISM OF ACTION “I am sure the air in heaven must be this Some writers have suggested that N2O, like wonder-working gas of delight”. volatile anaesthetics, causes non-specific central nervous system depression. Others, such as 4 Robert Southey, Poet (1774 to 1843) Gillman, propose that N2O acts specifically by interacting with the endogenous opioid system. HISTORY N2O is known to act preferentially on areas of the Nitrous oxide (N2O) is the oldest known anaes- brain and spinal cord that are rich in morphine thetic agent. -
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. -
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. -
What Are the Treatments for Heroin Addiction?
How is heroin linked to prescription drug abuse? See page 3. from the director: Research Report Series Heroin is a highly addictive opioid drug, and its use has repercussions that extend far beyond the individual user. The medical and social consequences of drug use—such as hepatitis, HIV/AIDS, fetal effects, crime, violence, and disruptions in family, workplace, and educational environments—have a devastating impact on society and cost billions of dollars each year. Although heroin use in the general population is rather low, the numbers of people starting to use heroin have been steadily rising since 2007.1 This may be due in part to a shift from abuse of prescription pain relievers to heroin as a readily available, cheaper alternative2-5 and the misperception that highly pure heroin is safer than less pure forms because it does not need to be injected. Like many other chronic diseases, addiction can be treated. Medications HEROIN are available to treat heroin addiction while reducing drug cravings and withdrawal symptoms, improving the odds of achieving abstinence. There are now a variety of medications that can be tailored to a person’s recovery needs while taking into account co-occurring What is heroin and health conditions. Medication combined with behavioral therapy is particularly how is it used? effective, offering hope to individuals who suffer from addiction and for those around them. eroin is an illegal, highly addictive drug processed from morphine, a naturally occurring substance extracted from the seed pod of certain varieties The National Institute on Drug Abuse (NIDA) has developed this publication to Hof poppy plants. -
Codeine: the Facts Suzanne Nielsen Bpharm Phd MPS Codeine: Overview 1
Codeine: The facts Suzanne Nielsen BPharm PhD MPS Codeine: overview 1. Codeine use in Australia 2. Characteristics of codeine dependence 3. Identifying codeine dependence 4. Treatment approaches (focus on primary care) 2 Codeine use in Australia Codeine (OTC) Tramadol Tapentadol Dextropropoxyphene Codeine (prescription) Oxycodone Morphine Methadone Hydromorphone Fentanyl Buprenorphine 0 5 10 15 20 Million packs Opioid pack sales (in millions) from: Degenhardt, Gisev, Cama, Nielsen, Larance and Bruno. The extent and predictors of pharmaceutical opioid utilisation in Australia. Pharmacoepidemiology and Drug Safety. (2016) 3 Codeine use in Australia • > 15 million packs OTC and 12 million prescribed • Highest codeine use in remote areas and low income areas 4 Codeine as an analgesic • Weak mu-opioid agonist • Analgesic effect predominantly through its metabolism to morphine via CYP2D6 enzyme • Considerable variable in metabolism between individuals (from poor to ultra-rapid metabolism) • Ultra-rapid metabolism opioid toxicity • Poor metabolism no analgesic effect Kirchheiner J et al. Pharmacokinetics of codeine and its metabolite morphine in ultra-rapid metabolizers due to CYP2D6 duplication.Pharmacogenomics J. 2007 5 Codeine-related harm • Codeine-related deaths increased from 3.5 per million in 2000 to 8.7 per million in 2009 • Trebling of non-OST drug treatment presentations fpr codeine between 2002-2011 • Among people entering methadone and buprenorphine increasing numbers report codeine as the main drug • 2014 – 2.7% of cases (1287 people) • 2015 – 3.5% of cases (1676 people) • 2016 – 4.6% of cases (1562 people*) * missing data from Vic and ACT means actual number likely to be higher (>2000) Roxburgh et al (2015). Medical Journal of Australia. -
Measures and CDS for Safer Opioid Prescribing: a Literature Review
Measures and CDS for Safer Opioid Prescribing: A Literature Review Measures and CDS for Safer Opioid Prescribing: A Literature Review Executive Summary The U.S. opioid epidemic continues to pose significant challenges for patients, families, clinicians, and public health policy. Opioids are responsible for an estimated 315,000 deaths (from 1999 to 2016) and have caused 115 deaths per day.1 In 2017, the U.S. Department of Health and Human Services declared the opioid epidemic a public health crisis.2 The total economic burden of opioid abuse in the United States has been estimated to be $78.5 billion per year.3 Although providing care for chronic opioid users is important, equally vital are efforts to prevent so-called opioid-naïve patients (patients with no history of opioid use) from developing regular opioid use, misuse, or abuse. However, much remains unclear regarding what role clinician prescribing habits play and what duration or dose of opioids may safely be prescribed without promoting long-term use.4,5 In 2013, ECRI Institute convened the Partnership for Health IT Patient Safety, and its component, single-topic-focused workgroups followed. For this subject, the Electronic Health Record Association (EHRA): Measures and Clinical Decision Support (CDS) for Safer Opioid Prescribing workgroup included members from the Healthcare Information and Management Systems Society (HIMSS) EHRA and the Partnership team. The project was oriented towards exploring methods to enable a synergistic cycle of performance measurement and identifying electronic health record (EHR)/health information technology (IT)–enabled approaches to support healthcare organizations’ ability to assess and measure opioid prescribing. -
The Effects of the Morphine Analogue Levorphanol on Leukocytes: Metabolic Effects at Rest and During Phagocytosis
The effects of the morphine analogue levorphanol on leukocytes: Metabolic effects at rest and during phagocytosis Nancy Wurster, … , Penelope Pettis, Sharon Lebow J Clin Invest. 1971;50(5):1091-1099. https://doi.org/10.1172/JCI106580. Studies on bacteria have suggested that morphine-like drugs have effects on the cell membrane. To determine the effect of this class of drugs on a mammalian cell, we selected the rabbit peritoneal exudate granulocyte, which undergoes striking membrane changes during phagocytosis. We examined the effect in vitro of the morphine analogue, levorphanol on phagocytosis and metabolism by granulocytes incubated with and without polystyrene particles or live Escherichia coli. Levorphanol (1 or 2 mmoles/liter) decreased: (a) acylation of lysolecithin or lysophosphatidylethanolamine in the medium (which is stimulated about two-fold during phagocytosis) both at rest (40%) and during phagocytosis (60%); (b) uptake of latex particles and Escherichia coli, as judged by electron microscopy; (c) killing of live Escherichia coli (10-fold); (d) 14 14 + CO2 production from glucose-1- C during phagocytosis by at least 80%; (e) K content of granulocytes (35%); (f) oxidation of linoleate-1-14C by 50%, and its incorporation into triglyceride by more than 80%. However, levorphanol stimulated 2 to 3-fold the incorporation of linoleate-1-14C or palmitate-1-14C into several phospholipids. Glucose uptake, lactate production, and adenosine triphosphate (ATP) content are not affected by the drug. Thus, levorphanol does not appear to exert its effects through generalized metabolic suppression. Removal of levorphanol by twice resuspending the granulocytes completely reverses all inhibition. In line with observations on bacteria, it appears that the complex effects of levorphanol on […] Find the latest version: https://jci.me/106580/pdf The Effects of the Morphine Analogue Levorphanol on Leukocytes METABOLIC EFFECTS AT REST AND DURING PHAGOCYTOSIS NANcY WuRsTE, PETER ELSBACH, ERIc J. -
Global Addiction & EUROPAD Joint Conference Diversion, Misuse and Trafficking of Methadone and Buprenorphine Dart RC
Diversion, misuse and trafficking of methadone and buprenorphine Global Addiction Conference Richard C. Dart, MD, PhD Professor, University of Colorado Prescription Opioid Deaths are Rising Internationally United Kingdom Drug Related Deaths 2001 - 2011 Source: RADARS® System, Denver Health and Hospitals What is the RADARS® System? • History – 2006, Denver Health and Hospital Authority (DHHA) – Multiple pharmaceutical subscribers – Independent program – Denver Public Safety Net Hospital for 150 years – State sanctioned independent authority • Conflict of Interest Statement – None, other than running system for DHHA as noted above. 3 RADARS System Scientific Advisory Board Principal Investigators Substance Abuse Experts • Theodore J. Cicero, PhD • Herbert D. Kleber, MD Washington University at St. Louis Columbia University • Richard C. Dart, MD, PhD • Sidney Schnoll, MD, PhD Denver Health and Hospital Authority Pinney Associates • Hilary Surratt, PhD • George E. Woody, MD Nova Southeastern University University of Pennsylvania • Mark W. Parrino, MPA Epidemiology/Biostatistics American Association for the • Edgar Adams, ScD Treatment of Opioid Dependence Covance Law Enforcement • Nabarun Dasgupta, MPH • John Burke Founder – Epidemico National Association of Drug Diversion Investigators • Alvaro Muñoz, PhD Johns Hopkins University 4 Challenges of Prescription Drug Abuse Surveillance • Clandestine behavior • Geographical variability • Changes rapidly • Multiple age groups • Product specificity – 15 active pharmaceutial ingredients (API) • -
PALEXIA IR Immediate Release Tablets
PALEXIA® IR immediate release tablets Tapentadol (as hydrochloride) (Ta-pen-ta-dol) Consumer Medicine Information (CMI) WARNING Limitations of use PALEXIA® IR should only be used when your doctor decides that other treatment options are not able to effectively manage your pain or you cannot tolerate them. Hazardous and harmful use PALEXIA® IR poses risks of abuse, misuse and addiction which can lead to overdose and death. Your doctor will monitor you regularly during treatment. Life threatening respiratory depression PALEXIA® IR can cause life-threatening or fatal breathing problems (slow, shallow, unusual or no breathing), even when used as recommended. These problems can occur at any time during use, but the risk is higher when first starting PALEXIA® IR and after a dose increase, if you are older, or have an existing problem with your lungs. Your doctor will monitor you and change the dose as appropriate. Use of other medicines while using PALEXIA® IR Using PALEXIA® IR with other medicines that can make you feel drowsy such as sleeping tablets (e.g. benzodiazepines), other pain relievers, antihistamines, antidepressants, antipsychotics, gabapentinoids (e.g. gabapentin and pregabalin), cannabis and alcohol may result in severe drowsiness, decreased awareness, breathing problems, coma and death. Your doctor will minimise the dose and duration of use; and monitor you for signs and symptoms of breathing difficulties and sedation. You must not drink alcohol while using PALEXIA® IR. ® What is in this leaflet Keep this leaflet with the PALEXIA IR has been medicine. You may need to read prescribed for you. it again. This leaflet answers some common questions about Before you take ® ® PALEXIA IR.