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Neurobiologie der Opioidabhängigkeit

Scherbaum N, Bonnet U.

Anaesthesist. 2019 Mar;68(3):179-190. doi: 10.1007/s00101-019-0557-3. German. 

Abstract

https://link.springer.com/article/10.1007%2Fs00101-019-0557-3

Understanding the molecular basis of agonist/antagonist mechanism of human mu opioid receptor through gaussian accelerated molecular dynamics method.

Wang YT, Chan YH.

Sci Rep. 2017 Aug 10;7(1):7828. doi: 10.1038/s41598-017-08224-2.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5552784/

Suppression of Human Natural Killer Cells by Different Classes of Opioids.

Maher DP, Walia D, Heller NM.

Anesth Analg. 2019 Feb 18. doi: 10.1213/ANE.0000000000004058.

Abstract

https://www.ncbi.nlm.nih.gov/pubmed/30801358

Opioid-galanin receptor heteromers mediate the dopaminergic effects of opioids

Ning-Sheng Cai, … , Annabelle M. Belcher, Sergi Ferre 

J Clin Invest. 2019. Published March 26, 2019, doi.org/10.1172/JCI126912. 

https://dm5migu4zj3pb.cloudfront.net/manuscripts/126000/126912/cache/126912.1-20190320224231-covered-253bed37ca4c1ab43d105aefdf7b5536.pdf

NIDA. Opioids without the risk of addiction?

Scientists are working to develop medicines that have the pain-relieving effects of opioids without the high risk of misuse and addiction. Since misuse is linked to the euphoric effects of the drug, investigators led by scientists at NIDA’s intramural labs are studying methadone, a drug used to manage opioid addiction that does not have euphoric effects as strong as many other opioids. (NIDA, USA, 26.03.2019)

https://www.drugabuse.gov/news-events/news-releases/2019/03/opioids-without-risk-addiction

Die pharmakologische Visitenkarte des vierten Opioid-Rezeptors

Pharmakologen aus Jena, Toulouse, St. Louis und Boca Raton sowie Montreal, Seattle und Mountain View konnten das molekulare Verhalten des Nociceptin-Rezeptors sowohl in der Zelle als auch im Organismus detailliert aufklären. Ihre jetzt in Science Signaling veröffentlichte Untersuchung des vierten Opioid-Rezeptors ist eine zentrale Vorarbeit für die Entwicklung und klinische Prüfung neuer Schmerzmittel. (Universitätsklinikum Jena, 26.03.2019)

https://idw-online.de/de/news712866

UNODC. Global SMART Update 2019, Vol. 21 (The non-medical Use of Opioids)

The Global SMART Update is designed to provide regular brief reports on emerging patterns and trends of the global synthetic drug situation. 

The current issue provides insight into the non-medical use of opioids, which presents a significant concern for public health, safety and law enforcement authorities worldwide. In the past years, the non-medical use of potent opioids such as fentanyl and its analogues have been reported mainly from North America, as well as from Asia, Europe and Oceania. Often sold as heroin or prescription medicines, these substances have contributed to the unprecedented number of recent opioid overdose deaths. The non-medical use of tramadol, an opioid analgesic, continues to increase in parts of Africa and the Middle East with reported adverse health effects. The rapidly emerging crisis which has resulted in significant harm to human health and welfare, including fatalities, calls for a coordinated, comprehensive and multidisciplinary response. (UNODC, März 2019)

https://www.unodc.org/documents/scientific/Global_SMART_21_web.pdf

Evaluation of a fentanyl drug checking service for clients of a supervised injection facility, Vancouver, Canada.

Karamouzian M, Dohoo C, Forsting S, McNeil R, Kerr T, Lysyshyn M.

Harm Reduct J. 2018 Sep 10;15(1):46. doi: 10.1186/s12954-018-0252-8.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6131768/

Assessing the 2004-2018 Fentanyl Misusing Issues Reported to an International Range of Adverse Reporting Systems.

Schifano F, Chiappini S, Corkery JM, Guirguis A.

Front Pharmacol. 2019 Feb 1;10:46. doi: 10.3389/fphar.2019.00046. eCollection 2019.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6367955/

Fentanyl Family at the Mu-Opioid Receptor: Uniform Assessment of Binding and Computational Analysis.

Lipiński PFJ, Kosson P, Matalińska J, Roszkowski P, Czarnocki Z, Jarończyk M, Misicka A, Dobrowolski JC, Sadlej J.

Molecules. 2019 Feb 19;24(4). pii: E740. doi: 10.3390/molecules24040740.

https://www.mdpi.com/1420-3049/24/4/740/htm

Assessment of the FDA Risk Evaluation and Mitigation Strategy for Transmucosal Immediate-Release Fentanyl Products.

Rollman JE, Heyward J, Olson L, Lurie P, Sharfstein J, Alexander GC. 

JAMA. 2019;321(7):676–685. doi:10.1001/jama.2019.0235

Abstract

https://jamanetwork.com/journals/jama/article-abstract/2725233

Wie sich Opioide auf die Verkehrstüchtigkeit auswirken

(...) Das Team um Dr. Maren Cecilie Strand von der Abteilung für forensische Wissenschaften der Universitätsklinik Oslo nahm 22 gesunde Freiwillige in eine prospektive Studie auf und ließ sie Methadon (5 bzw. 10 mg), Buprenorphin (0,2 bzw. 0,4 mg sublingual) oder ein Placebo einnehmen. (Medical Tribune, 17.02.2019)

https://www.medical-tribune.de/medizin-und-forschung/artikel/wie-sich-opioide-auf-die-verkehrstuechtigkeit-auswirken/

Review article: Effective management of opioid withdrawal symptoms: A gateway to opioid dependence treatment.

Kosten TR, Baxter LE.

Am J Addict. 2019 Jan 31. doi: 10.1111/ajad.12862. [Epub ahead of print] Review.

https://onlinelibrary.wiley.com/doi/full/10.1111/ajad.12862

Blockade of the human ether a-go-go related gene (hERG) potassium channel by fentanyl.

Tschirhart JN, Li W, Guo J, Zhang S.

Mol Pharmacol. 2019 Jan 21. pii: mol.118.114751. doi: 10.1124/mol.118.114751. 

http://molpharm.aspetjournals.org/content/early/2019/01/21/mol.118.114751.long

Non-Medical Use of Novel Synthetic Opioids: A New Challenge to Public Health.

Lovrecic B, Lovrecic M, Gabrovec B, Carli M, Pacini M, Maremmani AGI, Maremmani I.

Int J Environ Res Public Health. 2019 Jan 9;16(2). pii: E177. doi: 10.3390/ijerph16020177. Review.

https://www.mdpi.com/1660-4601/16/2/177/htm

Opioide: Keine Wirkung ohne Nebenwirkung

Pharmakologen des Universitätsklinikums Jena konnten durch genetische Veränderungen am Opioid-Rezeptor in Mäusen die Entwicklung einer Toleranz gegen Opioide fast komplett unterdrücken. Die schmerzmindernde Wirkung verbesserte sich sogar und hielt auch bei längerer Gabe an, Nebenwirkungen wie Atemdepression und Obstipation sowie Abhängigkeits- und Entzugssymptome blieben jedoch unverändert. Die jetzt in Nature Communications veröffentlichte Studie legt nahe, dass die Toleranzentwicklung von Opioiden über Phosphorylierung und Desensitisierung des Opioid-Rezeptors vermittelt wird. Diese Erkenntnisse können zur Entwicklung verbesserter Opioide genutzt werden. (Universitätsklinikum Jena, 21.01.2019)

https://idw-online.de/de/news709190

Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects. 

Kliewer A, et al. 

Nat. Comm. 2019, DOI: 10.1038/s41467-018-08162-1

https://www.nature.com/articles/s41467-018-08162-1

Notes from the Field: Fentanyl Drug Submissions — United States, 2010–2017. 

Springer YP, Gladden RM, O’Donnell J, Seth P. 

MMWR Morb Mortal Wkly Rep 2019;68:41–43. doi.org/10.15585/mmwr.mm6802a4

https://www.cdc.gov/mmwr/volumes/68/wr/mm6802a4.htm

Fentanyle: Verringerung des Risikos einer berufsbedingten Exposition des Strafverfolgungspersonals

Im Laufe der letzten Jahre gab es einen bedeutenden Anstieg bei der Verfügbarkeit von Fentanylen auf dem Drogenmarkt in Europa als Ergebnis der Massenproduktion in China und das online Vertriebs. 

Berichte über Todesfälle bei Drogenkonsumenten nahmen eben so erheblich zu.
In der Regel werden Fentanyle offen als "legale" Ersatzstoffe für illegale Opioide verkauft und ohne das Wissen der Konsumenten mit Heroin vermischt oder als Heroin und sonstige illegale Opioide verkauft.

In einigen Fällen setzt man sie auch zur Arzneimittelfälschungen ein und in einem geringen Maß werden sie mit anderen illegalen Drogen wie Kokain vermischt oder als solche verkauft. 

Angesichts der zunehmenden verfügbarkeit von vielen Terminen in Europa kann das Strafverfolgungspersonal bei der Ausübung seiner Arbeit darauf stoßen. (Europol, Den Haag, Dezember 2017,  in: Bundesverband der Ärztlichen Leiter Rettungsdienst Deutschland e.V.)

https://www.aelrd.de/index.php/downloads/category/13-medizin?download=111:2018-europol-mitteilung-fentanyle

Frequency, risk factors and symptomatology of iatrogenic withdrawal from opioids and benzodiazepines in critically Ill neonates, children and adults: A systematic review of clinical studies.

Duceppe MA, Perreault MM, Frenette AJ, Burry LD, Rico P, Lavoie A, Gélinas C, Mehta S, Dagenais M, Williamson DR.

J Clin Pharm Ther. 2018 Dec 19. doi: 10.1111/jcpt.12787. 

https://onlinelibrary.wiley.com/doi/full/10.1111/jcpt.12787

Comparison between intravenous morphine versus fentanyl in acute pain relief in drug abusers with acute limb traumatic injury.

Vahedi HSM, Hajebi H, Vahidi E, Nejati A, Saeedi M.

World J Emerg Med. 2019;10(1):27-32. doi: 10.5847/wjem.j.1920-8642.2019.01.004.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264977/

USA. A Visual Journey through Addiction

Why do people start using opioids and why can’t they stop? Through interviews with users and experts, The Ney York Times created a visual presentation of how these drugs can hijack the brain. (New York Times, 18.12.2018)

https://www.nytimes.com/interactive/2018/us/addiction-heroin-opioids.html

USA. Fentanyl in cocaine: The deadly truth of new drugs cocktail (Video)

The US government has warned that a surge in cocaine deaths is being exacerbated by the presence of fentanyl, a synthetic opioid 80-100 times stronger than morphine. (BBC, 26.11.2018, Video, 09:55)

https://www.bbc.com/news/av/world-us-canada-46350497/fentanyl-in-cocaine-the-deadly-truth-of-new-drugs-cocktail

Historical Review: Opiate Addiction and Opioid Receptors.

Wang S.

Cell Transplant. 2018 Nov 13:963689718811060. doi: 10.1177/0963689718811060. 

https://journals.sagepub.com/doi/full/10.1177/0963689718811060

Indien/Fentanyl. PGI doctors fear misuse of opioid stronger than heroin 

CHANDIGARH: North India's most prominent referral drug de-addiction centre at PGIMER has sounded a "red alert" after country's first illicit manufacturing drug unit of fentanyl - one of the most potent opioid prescription drugs - was busted recently at Indore. (Times of India, 20.11.2018)

https://timesofindia.indiatimes.com/city/chandigarh/pgi-doctors-fear-misuse-of-opioid-stronger-than-heroin/articleshow/66701820.cms

Fentanyl: Use & OD Prevention Tips 

Hrsg.: The DOPE Project is a program of the Harm Reduction Coalition and is funded by the San Francisco Department of Public Health to coordinate San Francisco’s response to drug overdose. 2018

https://harmreduction.org/wp-content/uploads/2018/11/DOPE_FentanylUseBrochure.pdf

USA / Sufentanil. FDA Approves Powerful Opioid Despite Fears Of More Overdose Deaths

The drug approved Friday is a 30-microgram pill form of sufentanil, a powerful, 34-year-old opioid commonly used after surgery and in emergency rooms. Each pill, placed under the tongue for quick absorption, would have the same impact as five milligrams of intravenous morphine. Each would come in a plastic applicator that looks like a syringe.

The drug is intended for use within health-care settings and perhaps on the battlefield. It would not be available in retail pharmacies. (atforum, USA, 12.11.2018)

http://atforum.com/2018/11/fda-approves-powerful-opioid-despite-fears-of-more-overdose-deaths/

Desomorphine. How a flesh-eating drug containing paint thinner and phosphorous is causing a global crisis

Desomorphine has been in the news a lot lately. Never heard of it? That’s quite possible. But you may well have heard its street name: “Krokodil”. However you know it, it’s a cheap substitute for heroin that has been widely branded as a “flesh-eating zombie drug” – and it’s bad news. (The Independent, UK, 13.11.2018)

https://www.independent.co.uk/life-style/health-and-families/features/flesh-eating-drug-krokodil-desomorphine-heroin-substitute-russia-a8621641.html

Health, Human Rights: Criminalising pain? Scheduling tramadol would hurt those most in need

This blog post is published ahead of the 41st World Health Organisation's Expert Committee on Drug Dependence (ECDD) meeting, which will critically review tramadol and issue a recommendation on its scheduling for the consideration of the 62nd Session of the Commission on Narcotic Drugs. IDPC has submitted contribution to the ECDD's meeting on the matter. IDPC is of the view that scheduling tramadol is presently unnecessary and would be counter-productive in its effects on public health. (idpc - International Drug Policy Consortium, 29.10.2018)

https://idpc.net/blog/2018/10/criminalising-pain-scheduling-tramadol-would-hurt-those-most-in-need

High Rates of Tramadol Use among Treatment-Seeking Adolescents in Malmö, Sweden: A Study of Hair Analysis of Nonmedical Prescription Opioid Use.

Martin O. Olsson, Agneta Öjehagen, Louise Brådvik, Robert Kronstrand, and Anders Håkansson

Journal of Addiction, vol. 2017, Article ID 6716929, 9 pages, 2017. doi.org/10.1155/2017/6716929.

https://www.hindawi.com/journals/jad/2017/6716929/cta/