scholarly journals An Examination of the Complex Pharmacological Properties of the Non-Selective Opioid Receptor Modulator Buprenorphine

2020 ◽  
Author(s):  
Leana Pande ◽  
Brian Piper
Keyword(s):  
Partial Agonist ◽  
Analgesic Efficacy ◽  
Receptor Occupancy ◽  
The United States ◽  
Opioid Use Disorder ◽  
Biologically Active ◽  
Poison Control ◽  
Opioid Use ◽  
Analgesic Effects ◽  
Receptor Modulator

Buprenorphine, an analogue of thebaine, is a Schedule III opioid in the United States used for opioid-use disorder and as an analgesic. Research has shown drugs like buprenorphine have a complicated pharmacology with characteristics that challenge traditional definitions of terms like agonist, antagonist, and efficacy. Buprenorphine has a high affinity for the mu (MOR), delta (DOR), kappa (KOR), and intermediate for the nociceptin opioid receptors (NOR). Buprenorphine is generally described as a partial MOR agonist with limited activity and decreased response at the mu-receptor relative to full agonists. In opioid naïve patients, the drug’s analgesic efficacy is equivalent to a full MOR agonist, despite decreased receptor occupancy and the “ceiling effect” produced from larger doses. Some argue buprenorphine’s effects depend on the endpoint measured, as it functions as a partial agonist for respiratory depression, but a full-agonist for pain. Buprenorphine’s active metabolite, norbuprenorphine, attenuates buprenorphine's analgesic effects due to NOR binding and respiratory depressant effects. The method of administration impacts efficacy and tolerance when administered for analgesia. There have been eleven-thousand reports involving buprenorphine and minors (age < 19) to US poison control centers, the preponderance (89.2%) with children. The consequences of prenatal buprenorphine exposure in experimental animals and humans should continue to be carefully evaluated. In conclusion, buprenorphine’s characterization as only a partial mu-agonist is an oversimplification. Contemporary research shows the traditional explanation of the pharmacology of buprenorphine does not take into account changes to receptor theory, pharmacological terminology, route of administration, and biologically active major metabolites.

Use of Buprenorphine for the Treatment of Opioid Use Disorder

2020 ◽  
pp. 155-168
Author(s):  
Paul J. Fudala ◽  
Anne Cramer Andorn
Keyword(s):  
Opioid Dependence ◽  
Addiction Treatment ◽  
Partial Agonist ◽  
The United States ◽  
Opioid Use Disorder ◽  
Sublingual Administration ◽  
Opioid Use ◽  
The Us ◽  
Monthly Administration ◽  
Drug Addiction Treatment

Buprenorphine is a mu-opioid partial agonist that was first developed as a parenteral analgesic and subsequently as a treatment for opioid dependence. In the United States, the first two products approved by the US Food and Drug Administration (in 2002) for the latter indication were buprenorphine (Subutex) and buprenorphine/naloxone (Suboxone) tablet formulations for sublingual administration. Since that time, additional products for both sublingual and buccal administration have also been approved, as well as a subcutaneous injection for once-monthly administration for the treatment of moderate or severe opioid use disorder (OUD) and a subdermal implant for the maintenance treatment of opioid dependence that delivers buprenorphine over a 6-month period. Under the Drug Addiction Treatment Act of 2000 (DATA 2000), qualified practitioners may apply for waivers to treat opioid dependence/OUD with approved buprenorphine products in any setting in which they are qualified to practice. Like other opioids, buprenorphine has the potential for being misused and abused.

scholarly journals Assessing the Relationships Between COVID-19 Stay-at-Home Orders and Opioid Overdoses in the State of Pennsylvania

2021 ◽  
pp. 002204262110063
Author(s):  
Brian King ◽  
Ruchi Patel ◽  
Andrea Rishworth
Keyword(s):  
Age Groups ◽  
The United States ◽  
Opioid Use Disorder ◽  
Opioid Overdose ◽  
Policy Recommendations ◽  
Opioid Use ◽  
Fentanyl Analogs ◽  
Measure Change ◽  
Using Data ◽  
At Home

COVID-19 is compounding opioid use disorder throughout the United States. While recent commentaries provide useful policy recommendations, few studies examine the intersection of COVID-19 policy responses and patterns of opioid overdose. We examine opioid overdoses prior to and following the Pennsylvania stay-at-home order implemented on April 1, 2020. Using data from the Pennsylvania Overdose Information Network, we measure change in monthly incidents of opioid-related overdose pre- versus post-April 1, and the significance of change by gender, age, race, drug class, and naloxone doses administered. Findings demonstrate statistically significant increases in overdose incidents among both men and women, White and Black groups, and several age groups, most notably the 30–39 and 40–49 ranges, following April 1. Significant increases were observed for overdoses involving heroin, fentanyl, fentanyl analogs or other synthetic opioids, pharmaceutical opioids, and carfentanil. The study emphasizes the need for opioid use to be addressed alongside efforts to mitigate and manage COVID-19 infection.

scholarly journals “It’s way more than just writing a prescription”: A qualitative study of preferences for integrated versus non-integrated treatment models among individuals with opioid use disorder

2021 ◽  
Vol 16 (1) ◽  
Author(s):  
Elizabeth C. Saunders ◽  
Sarah K. Moore ◽  
Olivia Walsh ◽  
Stephen A. Metcalf ◽  
Alan J. Budney ◽  
...  
Keyword(s):  
Qualitative Study ◽  
The United States ◽  
Opioid Use Disorder ◽  
Integrated Treatment ◽  
Medical Setting ◽  
Integrated Models ◽  
Opioid Use ◽  
Medical Settings ◽  
Psychosocial Services ◽  
Treatment Models

Abstract Background Increasingly, treatment for opioid use disorder (OUD) is offered in integrated treatment models addressing both substance use and other health conditions within the same system. This often includes offering medications for OUD in general medical settings. It remains uncertain whether integrated OUD treatment models are preferred to non-integrated models, where treatment is provided within a distinct treatment system. This study aimed to explore preferences for integrated versus non-integrated treatment models among people with OUD and examine what factors may influence preferences. Methods This qualitative study recruited participants (n = 40) through Craigslist advertisements and flyers posted in treatment programs across the United States. Participants were 18 years of age or older and scored a two or higher on the heroin or opioid pain reliever sections of the Tobacco, Alcohol, Prescription Medications, and Other Substances (TAPS) Tool. Each participant completed a demographic survey and a telephone interview. The interviews were coded and content analyzed. Results While some participants preferred receiving OUD treatment from an integrated model in a general medical setting, the majority preferred non-integrated models. Some participants preferred integrated models in theory but expressed concerns about stigma and a lack of psychosocial services. Tradeoffs between integrated and non-integrated models were centered around patient values (desire for anonymity and personalization, fear of consequences), the characteristics of the provider and setting (convenience, perceived treatment effectiveness, access to services), and the patient-provider relationship (disclosure, trust, comfort, stigma). Conclusions Among this sample of primarily White adults, preferences for non-integrated versus integrated OUD treatment were mixed. Perceived benefits of integrated models included convenience, potential for treatment personalization, and opportunity to extend established relationships with medical providers. Recommendations to make integrated treatment more patient-centered include facilitating access to psychosocial services, educating patients on privacy, individualizing treatment, and prioritizing the patient-provider relationship. This sample included very few minorities and thus findings may not be fully generalizable to the larger population of persons with OUD. Nonetheless, results suggest a need for expansion of both OUD treatment in specialty and general medical settings to ensure access to preferred treatment for all.

scholarly journals Discovering Non-Invasive Biomarkers Predictive of Opioid Use Disorder Treatment Response

CNS Spectrums ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 173-173
Author(s):  
Amir Levine ◽  
Kelly Clemenza ◽  
Shira Weiss ◽  
Adam Bisaga ◽  
Erez Eitan ◽  
...  
Keyword(s):  
Treatment Response ◽  
Mononuclear Cells ◽  
Specific Treatment ◽  
The United States ◽  
Opioid Use Disorder ◽  
Response To Treatment ◽  
Post Translational Modification ◽  
Opioid Use ◽  
Peripheral Blood Mononuclear ◽  
Long Term Treatment

AbstractBackgroundOpioid use disorder (OUD) continues to be the driving force behind drug overdoses in the United States, killing nearly 47,000 people in 2018 alone. The increasing presence of deadlier fentanyl analogues in the heroin drug supply are putting users at a greater risk for overdose than ever before. Admissions to treatment programs for OUD have also nearly doubled since 2006, yet relapse rates remain high. In response to these alarming statistics, developing approaches to reduce overdose deaths has become an area of high priority. As it is not yet known which patients are most likely to benefit from a specific treatment, there is a dire need to utilize new molecular tools to guide precision medicine approaches and improve treatment outcomes. Here we describe a proof-of-concept study evaluating plasma-derived extracellular vesicle (EV) signatures and how they differ in patients who responded to two pharmacologically contrasting treatments for OUD: the μOR agonist methadone, and the μOR antagonist naltrexone.MethodsWe obtained blood samples from patients with OUD who remained abstinent from illicit opioids for at least 3 months during treatment with methadone (n=5) and naltrexone (n=5), as well as matched healthy controls (n=5). EVs were isolated from plasma and histones were isolated from peripheral blood mononuclear cells (PBMCs). EVs were then analyzed for lipid and histone post-translational modification (PTM) content using liquid chromatography-mass spectrometry. EV miRNA cargo was determined by RNA sequencing.ResultsWe found one lipid class and six miRNAs that differed significantly between the naltrexone group and the methadone and control groups. We also found that histone H3acK9acK14 was increasingly acetylated in PMBCs from both the methadone and naltrexone groups compared to controls.DiscussionNaltrexone, which is used in treatment of OUD and other substance use disorders as well as disorders of impulse control, was found to have multiple potential corresponding molecular signatures that can be identified after long-term treatment. It remains to be seen if these markers can also be a good predictor for treatment response. In addition, significant gender differences in EV content are found between men and women with OUD, which supports the importance of examining changes in response to treatment in a gender informed way.

Neurofeedback for Opioid Dependent Patients in an Outpatient Setting: A Pilot Feasibility Study

2021 ◽  
Author(s):  
Helena A. Rempala ◽  
Justin A. Barterian
Keyword(s):  
Large Scale ◽  
The United States ◽  
Outpatient Setting ◽  
Opioid Use Disorder ◽  
High Rate ◽  
Treatment Center ◽  
Opioid Use ◽  
Treatment As Usual ◽  
Factors Affecting ◽  
Study Approach

Abstract Background: Neurofeedback (NF) has been described as “probably efficacious” when used in conjunction with other interventions for substance use disorders, including the most recent studies in population of individuals with opioid use disorder. Despite these promising outcomes, the seriousness of the opioid epidemic, and the high rate of relapse even with the most effective medication-assisted maintenance treatments NF continues to be an under-researched treatment modality. This article explores factors that affected the feasibility of adding Alpha/Theta Neurofeedback to treatment as usual for opioid dependence in an outpatient urban treatment center. The study strived to replicate previous research completed in Iran that found benefits of NF for opioid dependence.Methods: Out of approximately two dozen patients eligible for Alpha/Theta NF, about 60% (n=15) agreed to participate; however, only 2 participants completed treatment. The rates of enrollment in response to active treatment were monitored. Results: The 4 factors affecting feasibility were: 1) the time commitment required of participants, 2) ineffectiveness of standard incentives to promote participation, 3) delayed effects of training, and 4) the length and number of treatments required.Conclusion: The findings indicate a large scale study examining the use of NF for the treatment of opioid use disorder in the United States will likely be difficult to accomplish without modification to the traditional randomized control study approach and suggests challenges to the implementation of this treatment in an outpatient setting.

scholarly journals Patient and Clinician Perspectives on Adolescent Opioid Use Disorder Treatment During a Pandemic: One Step Back, but Two Forward? (Preprint)

2020 ◽  
Author(s):  
Samuel W Stull ◽  
Erin R McKnight ◽  
Andrea E Bonny
Keyword(s):  
The United States ◽  
Opioid Use Disorder ◽  
Drop Out ◽  
Mobile Technologies ◽  
Opioid Use ◽  
The Face ◽  
One Step ◽  
Clinician Perspectives ◽  
Receive Treatment

UNSTRUCTURED Opioid use disorder (OUD) is one of the most pressing public health problems in the United States and is highly prevalent among adolescents and young adults (AYAs). However, only a small percentage of AYAs with OUD ever receive treatment. Further, among those that do receive treatment, a substantial proportion of patients continue to struggle with OUD, and many prematurely drop out of treatment. These challenges have only been heightened in the face of the COVID-19 pandemic, but greater utilization of telehealth and mobile technologies by OUD patients may help counter these barriers, which ultimately may improve AYA OUD treatment in the postpandemic period. This viewpoint presents the perspective of a person in OUD recovery using online and mobile technology to support his own OUD recovery combined with thoughts from two clinicians supporting AYAs with OUD. Their perspectives may provide insights to help counter COVID-19–related consequences and offer clues to improving AYA OUD treatment in the long term.

scholarly journals Methadone Distribution Trends from 2017-2019 in the United States

2020 ◽  
Author(s):  
John A. Furst ◽  
Nicholas J. Mynarski ◽  
Kenneth L. McCall ◽  
Brian J. Piper
Keyword(s):  
United States ◽  
Rhode Island ◽  
Distribution Patterns ◽  
The United States ◽  
Opioid Use Disorder ◽  
Primary Objective ◽  
Treatment Programs ◽  
Opioid Use ◽  
Drug Enforcement ◽  
The Us

AbstractObjectiveMethadone is an evidence based treatment for opioid use disorder and is also employed for acute pain. The primary objective of this study was to explore methadone distribution patterns between the years 2017 and 2019 across the United States (US). This study builds upon previous literature that has analyzed prior years of US distribution patterns, and further outlines regional and state specific methadone trends.MethodsThe Drug Enforcement Administration’s Automated Reports and Consolidated Ordering System (ARCOS) was used to acquire the number of narcotic treatment programs (NTPs) per state and methadone distribution weight in grams. Methadone distribution by weight, corrected for state populations, and number of NTPs were compared from 2017 to 2019 between states, within regions, and nationally.ResultsBetween 2017 and 2019, the national distribution of methadone increased 12.30% for NTPs but decreased 34.57% for pain, for a total increase of 2.66%. While all states saw a decrease in distribution for pain, when compared regionally, the Northeast showed a significantly smaller decrease than all other regions. Additionally, the majority of states experienced an increase in distribution for NTPs and most states demonstrated a relatively stable or increasing number of NTPs, with an 11.49% increase in NTPs nationally. The number of NTPs per 100K in 2019 ranged from 2.08 in Rhode Island to 0.00 in Wyoming.ConclusionAlthough methadone distribution for OUD was increasing in the US, there were pronounced regional disparities.

Sign in / Sign up

Export Citation Format

Share Document