Heroin and Fentanyl Updates and Pharmacology

Updated: May 25th, 2025

Published: Feb 12th, 2025

Presentation Synopsis

This educational presentation by the Opioid Remediation Collaborative (ORCNM) provides an up-to-date overview of the pharmacological properties, clinical effects, and evolving challenges associated with heroin, fentanyl, and emerging synthetic additives like xylazine. It aims to equip providers with the knowledge needed to better understand drug mechanisms, overdose risk, and implications for treatment, monitoring, and public health response.

Learning Objectives

  • Describe the pharmacokinetics and clinical effects of heroin, including its rapid metabolism, route of administration, and short-lived euphoric effects.

  • Explain how fentanyl became the dominant synthetic opioid in the U.S. drug supply, including factors related to production, potency, and distribution.

  • Compare the potency and receptor binding characteristics of fentanyl and heroin, and understand how these pharmacologic differences impact overdose risk and treatment strategies.

  • Recognize the role of xylazine as an additive in fentanyl products, including its purpose, risks, and emerging clinical challenges such as non-healing wounds and prolonged sedation.

  • Identify the complications fentanyl presents for medication-assisted treatment (MAT), including delayed metabolism, extended detection in urine, and difficulty in initiating therapies like buprenorphine.

  • Understand how variability in formulation and metabolic pathways complicates overdose management and surveillance, necessitating new approaches in care and harm reduction.

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