Buprenorphine: Molecule, Mechanisms, and Magnaminity
Buprenorphine is a Schedule III opioid analgesic approved in 1981 by the FDA for use by injection for acute pain. A sublingual dosage form was later developed and approved for opioid
use disorder, followed by the development of transdermal and buccal formulations specifically indicated for chronic pain severe enough to require daily, around-the-clock, long-term opioid treatment for which alternative treatment options are inadequate. As the formulations were developed, there has been increased confusion and misunderstandings of its pharmacology and clinical utility. This lecture focuses on buprenorphine as a partial μ-opioid receptor agonist and how that has been misinterpreted to imply low efficacy. Discussions will include how a partial agonist does not necessarily translate to partial or inadequate clinical efficacy compared to a traditional full μ-opioid receptor agonist, and the specific pharmacokinetics and pharmacology for the parent compound and each metabolite. Misconceptions regarding conversion to or from buprenorphine will be discussed, including various considerations for elective and emergent surgery in patients receiving buprenorphine chronically as an outpatient for a chronic pain syndrome vs those requiring it for opioid use disorder. Buprenorphine formulation transitions and variable dosage adjustments between formulations will be reviewed with a case-based example and regulatory considerations specific to the false impression that an “X” waiver is required to prescribe or dispense buprenorphine for chronic pain.
PharmD, DAAPM, FCCP, FASHP
Dr. Fudin graduated from Albany College of Pharmacy & Health Sciences with his Bachelors Degree and Pharm.D. He completed an Oncology/Hematology fellowship at SUNY/Upstate Medical Center. He is a Diplomate to the Academy of Integrative Pain Management and a Fellow to the American College of Clinical Pharmacy, the American Society of Health-system Pharmacists, and the Federation of State Medical Board.
Dr. Fudin is a Senior Section Editor for Pain Medicine, Co-Editor-At-Large for Practical Pain Management, Senior Editor for Pain Medicine, and peer reviewer for several professional medical and pharmacy journals. He has participated in developing practice guidelines for use of opioids in chronic noncancer pain and participated in national (US Health and Human Services) and international guideline development for various pain types.
In 2011, he established a Pharmacy Pain Residency Program at the Stratton Veterans Administration Medical Center in Albany NY and was Program Director through 2020. He holds adjunct faculty appointments at several colleges of pharmacy and has been an invited speaker on pain therapeutics nationally and internationally.
He is owner and managing editor for paindr.com and President of Remitigate Therapeutics offering virtual telemedicine pain consultations. He is also the Founder/President of Remitigate, LLC, a software development company that has provided platforms which aid clinicians to enhance opioid safety regarding urine drug screen interpretation and predictability of opioid-induced respiratory depression.
In addition to several guest Podcasts, he is a prolific lecturer, writer with over 350 publications, and researcher on pain management topics.