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  • Dr. J. James Frost

Navigating the Complexities of Opioid Antagonism: A Paradigm Shift in Dose Precision and Imaging

Updated: Dec 12, 2023

The global crisis surrounding opioid drugs underscores the critical need for advancements in the field of opioid antagonism. Among the potent opioids that have emerged as serious threats to public health, fentanyl and carfentanil stand out due to their high affinity for the opiate receptor. This inherent characteristic not only complicates the clinical reversal process but also raises concerns about achieving and maintaining an adequate duration of reversal. It is within this challenging context that I am honored to collaborate with distinguished co-authors — Martin Trøstheim, Marie Eikemo, Jan Haaker, and Siri Leknes — on our latest research endeavor.


Our newly published article, titled "Opioid Antagonism in Humans: A Primer on Optimal Dose and Timing for Central Mu-Opioid Receptor Blockade" represents a significant leap forward in addressing these challenges. Access the complete article [here].


In the pursuit of a comprehensive understanding, our study draws on a rich tapestry of human opioid receptor imaging data. We meticulously examined data from various sources, including my contributions spanning back to the earliest PET studies conducted in the 1980s. The synthesis of this extensive data culminated in the development of a sophisticated pharmacokinetic algorithm. This algorithm serves as a powerful tool for estimating mu, delta, and kappa receptor occupancy based on the dosage of naloxone or naltrexone.


The implications of this research extend far beyond the realm of academia. Our advanced approach to dose calculations offers a promising avenue for improving both clinical applications and research methodologies related to opioid antagonism. By providing enhanced knowledge and predictability regarding dose-antagonism relationships, we aim to revolutionize the strategies employed by clinicians and investigators in the opioid field.

Clinicians grappling with the complexities of opioid reversal now have access to a more refined and informed toolkit. Armed with our pharmacokinetic algorithm, they can tailor interventions with greater precision, optimizing both the dose and timing for central mu-opioid receptor blockade. This level of precision is paramount in a landscape where every moment counts, and the stakes are high.


As we present this pioneering research, we invite a diverse audience of clinicians, researchers, and policymakers to engage with its implications. The collective impact of our findings promises to shape a new era in the understanding and management of opioid antagonism, ultimately contributing to more effective and targeted interventions. In a world grappling with the repercussions of opioid misuse, our commitment to advancing knowledge in this field remains steadfast, driven by the shared goal of fostering a safer and more resilient society.


About BioMolecular Imaging


BioMolecular Imaging (BMI Consultants) is a molecular imaging and clinical trial consultancy owned and operated by Dr. J. James Frost M.D./Ph.D out of Baltimore Maryland. BMI has been involved with clinical, therapeutic & diagnostic imaging focused on Oncology, Brain, Biomarkers, Cardiology and Central Image Interpretations for over 20 years.


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