Molecules, Vol. 25, Pages 4009: Synthesis of Potential Haptens with Morphine Skeleton and Determination of Protonation Constants
tafi Vaccination could be a promising alternative warfare against drug addiction and abuse. For this purpose, so-called haptens can be used. These molecules alone do not induce the activation of the immune system, this occurs only when they are attached to an immunogenic carrier protein. Hence obtaining a free amino or carboxylic group during the structural transformation is an important part of the synthesis. Namely, these groups can be used to form the requisite peptide bond between the hapten and the carrier protein. Focusing on this basic principle, six nor-morphine compounds were treated with ethyl acrylate and et...
Source: Molecules - September 1, 2020 Category: Chemistry Authors: Istv án Köteles K ároly Mazák Gerg ő Tóth Bogl árka Tűz S ándor Hosztafi Tags: Article Source Type: research

Heat shock protein 90 inhibitors block the antinociceptive effects of opioids in mouse chemotherapy-induced neuropathy and cancer bone pain models
This study extended from that initial work to test the cancer-related clinical impact of Hsp90 inhibitors on opioid antinociception in cancer-induced bone pain in female BALB/c mice and chemotherapy-induced peripheral neuropathy in male and female CD-1 mice. Mice were treated with Hsp90 inhibitors (17-AAG, KU-32) by the intracerebroventricular, intrathecal, or intraperitoneal routes, and after 24 hours, pain behaviors were evaluated after analgesic drug treatment. Heat shock protein 90 inhibition in the brain or systemically completely blocked morphine and oxymorphone antinociception in chemotherapy-induced peripheral neur...
Source: Pain - July 29, 2020 Category: Anesthesiology Tags: Research Paper Source Type: research

Model-based Meta-analysis to Compare Primary Efficacy-endpoint, Efficacy-time Course, safety, and Tolerability of Opioids Used in the Management of Osteoarthritic Pain in Humans.
CONCLUSIONS: This MBMA provides clinically meaningful insights into the efficacy and safety profiles of oxycodone, oxymorphone, and tramadol. Resultantly, the presented framework analysis can have an impact in the clinic on drug development where it can guide: the optimization of doses of opioids required to manage osteoarthritic pain; the making of precise key decisions for the positioning of new drugs, and; the design more efficient trials. PMID: 32407270 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 13, 2020 Category: Drugs & Pharmacology Authors: Suliman SO, Milavetz G, Salem AK Tags: Curr Drug Metab Source Type: research

IJERPH, Vol. 17, Pages 3251: Prescription Opioid Distribution after the Legalization of Recreational Marijuana in Colorado
We examined the association between the legalization of recreational marijuana and prescription opioid distribution in Colorado. Utah and Maryland, two states that had not legalized recreational marijuana, were selected for comparison. Prescription data reported to the Drug Enforcement Administration for nine opioids used for pain (e.g., fentanyl, morphine, hydrocodone, hydromorphone, oxycodone, oxymorphone) and two primarily for opioid use disorder (OUD, methadone and buprenorphine) from 2007 to 2017 were evaluated. Analysis of the interval pre (2007–2012) versus post (2013–2017) marijuana lega...
Source: International Journal of Environmental Research and Public Health - May 6, 2020 Category: Environmental Health Authors: Amalie K. Kropp Lopez Stephanie D. Nichols Daniel Y. Chung Daniel E. Kaufman Kenneth L. McCall Brian J. Piper Tags: Article Source Type: research

Development of an in vitro system and model-based translational framework to assess haemolysis risk following intravenous abuse of medications containing polyethylene oxide.
Abstract Multiple cases of potentially life-threatening thrombotic microangiopathy (TMA) have resulted from intravenous abuse of medications containing polyethylene oxide (PEO), most often Opana ER (oxymorphone hydrochloride extended release). No validated models are available to assess the risk of TMA with different formulations and extraction methods following intravenous abuse. We have developed an in vitro system that involves passing pooled blood containing the excipient of interest through a syringe needle and assessing haemolysis via haemoglobin release. Haemolysis is induced by high shear stress ca...
Source: Toxicology in Vitro - January 16, 2020 Category: Toxicology Authors: Persich P, Engels GE, van Oeveren W, Galia E, Benay S, Thun S Tags: Toxicol In Vitro Source Type: research

Patterns in opioid prescription in the United States by region and prescribers over a 4-year period.
CONCLUSION: Patterns of prescription per opioid vary considerably per physician specialty and per US region. Although an overall decrease in prescriptions was seen, certain opioids were more frequently prescribed in 2015 than in 2012. PMID: 31850512 [PubMed - in process] (Source: Journal of Opioid Management)
Source: Journal of Opioid Management - December 19, 2019 Category: Addiction Tags: J Opioid Manag Source Type: research

Identification of specific markers for amphetamines synthesized from glycidic acid pre ‐precursors and retrospective search in German profiling database
This article presents experimental proof that APAAN is currently being replaced by other pre‐precursors, such as glycidic acid deriv atives. (Source: Drug Testing and Analysis)
Source: Drug Testing and Analysis - November 26, 2019 Category: Drugs & Pharmacology Authors: Frank M. Hauser, Michael P ütz, Thorsten Rößler, Janneke W. Hulshof Tags: RESEARCH ARTICLE Source Type: research

Tramadol Prescription over a 4-Year Period in the USA
AbstractPurpose of ReviewDeaths associated to tramadol, a synthetic opioid, are rising globally. Herein, we characterize prescription patterns of tramadol relative to other opioids in the USA from 2012 to 2015, by geographic region and physician specialty.Recent FindingsData on opioid was obtained using Truven Health Analytics MarketScan for the years 2012 –2015. Inclusion criteria included subjects living in the USA with ages from 12 to 64 years. Patterns of prescription of tramadol were contrasted with other prescription opioids including hydrocodone, codeine, oxycodone, oxymorphone, methadone, and fentanyl. Between 2...
Source: Current Pain and Headache Reports - August 5, 2019 Category: Neurology Source Type: research

Decline in primary care providers' prescribing of Schedule II opioids following the implementation of federal and state guidelines.
CONCLUSIONS: This study reports the benefit of incorporating federal and state regulations and institutional evidence-based guidelines into primary care practice to decrease the number of Schedule II opioids prescribed. Further preventive measures include selecting alternative treatments to opioids and reducing the rates of opioid nonmedical use and overdose while maintaining access to prescription opioids when indicated. PMID: 31343712 [PubMed - in process] (Source: Journal of Opioid Management)
Source: Journal of Opioid Management - July 27, 2019 Category: Addiction Tags: J Opioid Manag Source Type: research

Changes in Reported Injection Behaviors Following the Public Health Response to an HIV Outbreak Among People Who Inject Drugs: Indiana, 2016
We reported injection behaviors prior to the response and used Fisher ’s exact Chi square tests (P  <  0.05) to assess differences by HIV status. Next, among persons who injected both before (July–December 2014) and after (past 30 days) the response, we (1) reported the proportion of persons who used the SSP to obtain sterile syringes, and assessed differences in SSP use by HIV status using Fis her’s exact Chi square tests; and (2) compared distributive and receptive sharing of injection equipment and disposal of syringes before and after the outbreak response, and assessed statistical differences using McNem...
Source: AIDS and Behavior - July 15, 2019 Category: Infectious Diseases Source Type: research

Side Effect Rates of Opioids in Equianalgesic Doses Via Intravenous Patient-Controlled Analgesia: A Systematic Review and Network Meta-analysis.
CONCLUSIONS: The opiate chosen for treatment most likely has little effect on the incidence of pruritus and nausea/vomiting, although considerable differences exist in terms of better and worse opioids in the presented rankings. Larger differences between drugs were observed with regard to sedation and patient satisfaction, and choosing the appropriate opioid may help to improve PCA in this regard. PMID: 30418234 [PubMed - as supplied by publisher] (Source: Anesthesia and Analgesia)
Source: Anesthesia and Analgesia - November 9, 2018 Category: Anesthesiology Authors: Dinges HC, Otto S, Stay DK, Bäumlein S, Waldmann S, Kranke P, Wulf HF, Eberhart LH Tags: Anesth Analg Source Type: research

Novel Biased Potent Opioid-Like Agonists as Improved Medications to Treat Chronic and Acute Pain
There are no analgesics to ameliorate chronic pain without adverse side-effects (e.g., respiratory depression, gastrointestinal effects, tolerance, dependence), thus forcing patients into a difficult choice of negative impacts on quality of life. Most of the analgesics used for chronic and acute pain are drugs such as oxycodone, morphine, oxymorphone, and codeine. All of these opioids have been subject to misuse; prescription drug abuse is a severe problem worldwide, causing high mortality and greatly increased emergency room visits.Recently, research indicated that the analgesic and side-effects of opioids may be separabl...
Source: NIH OTT Licensing Opportunities - September 18, 2018 Category: Research Authors: ajoyprabhu3 Source Type: research

Scoring the best deal: Quantity discounts and street price variation of diverted oxycodone and oxymorphone
Pharmacoepidemiology and Drug Safety, EarlyView. (Source: Pharmacoepidemiology and Drug Safety)
Source: Pharmacoepidemiology and Drug Safety - May 16, 2018 Category: Drugs & Pharmacology Authors: Jacob A.Lebin , David L.Murphy , Stevan GeoffreySevertson , Gabrielle E.Bau , NabarunDasgupta , Richard C.Dart Source Type: research

Trends in Medical Use of Opioids in the U.S., 2006 –2016
Conclusions With the exception of buprenorphine, used to treat an opioid use disorder, prescription opioid use has been decreasing over the past 5 years in the U.S. Further efforts are needed to continue to optimize the balance between appropriate opioid access for acute pain while minimizing diversion and treating opioid addiction. (Source: American Journal of Preventive Medicine)
Source: American Journal of Preventive Medicine - May 7, 2018 Category: International Medicine & Public Health Source Type: research