Managing severe pain and abuse potential: the potential impact of a new abuse-deterrent formulation oxycodone/naltrexone extended-release product

Abstract

Proper management of severe pain represents one of the most challenging clinical dilemmas. Two equally important goals must be attained: the humanitarian/medical goal to relieve suffering and the societal/legal goal to not contribute to the drug abuse problem. This is an age-old problem, and the prevailing emphasis placed on one or the other goal has resulted in pendulum swings that have resulted in either undertreatment of pain or the current epidemic of misuse and abuse. In an effort to provide efficacious strong pain relievers (opioids) that are more difficult to abuse by the most dangerous routes of administration, pharmaceutical companies are developing products in which the opioid is manufactured in a formulation that is designed to be tamper resistant. Such a product is known as an abuse-deterrent formulation (ADF). ADF opioid products are designed to deter or resist abuse by making it difficult to tamper with the product and extracting the opioid for inhalation or injection. To date, less than a dozen opioid formulations have been approved by the US Food and Drug Administration to carry specific ADF labeling, but this number will likely increase in the coming years. Most of these products are extended-release formulations.

A Surface-Enhanced Raman Spectral Library of Important Drugs Associated With Point-of-Care and Field Applications

“…Codeine, hydrocodone, and oxycodone are Schedule II drugs usually prescribed in combination with nonsteroidal anti-inflammatory drugs, such as acetaminophen, aspirin, and ibuprofen, to treat varying degrees of pain. Oxycodone, sold as OxyContin, is currently the most abused opioid, and resulted in ~6,000 deaths in 2017 (Hedegaard et al, 2018; Pergolizzi et al, 2018). The SERS of codeine, hydrocodone, and oxycodone are also dominated by similar peaks at 510–530, 620–640, 1,275, 1,435, and 1,595–1,605 cm −1 , and assigned to the same vibrational modes (Figure 2) (Rana et al, 2010).…”

Prescribed drugs containing nitrogen heterocycles: an overview

“…362,363 Oxycodone 336, sold under the brand name OxyContin among others, is an opioid medicine used for handle and alleviating of moderate to severe pain. 364 Oxycodone was rst semi-synthesized in Germany in 1916 from a natural product, thebaine, has been a common drug of abuse. 365 Although the structure of oxycodone is similar to natourios morphine, it has shown better oral bioavailability, making it superior for pain alleviating in some clinical trials.…”

A Brief History of the Opioid Epidemic and Strategies for Pain Medicine

“…The various modified opioids released over the past 20 years, such as tamper-resistant preparation, have had differing levels of success, and are collectively referred to as Risk Evaluation and Mitigation Strategies (REMS); these include Targiniq ® (oxycodone and naloxone), Suboxone ® (buprenorphine/naloxone), reformulated OxyContin ® ER (extended release), among others [ 33 – 37 ]. Presently, fewer than one dozen FDA-approved Abuse-Deterrent Formulations (ADFs) exist, but further development and improvements are ongoing [ 38 ].…”