Combining Oxycodone with the Opioid Antagonist Naloxone to Deter from Drug Abuse

OxyContin® is an opioid agonist and a Schedule II controlled substance with an abuse liability similar to morphine. Oxycodone can be abused in a manner similar to other opioid agonists, legal or illicit. This should be considered when prescribing or dispensing OxyContin® in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion. OxyContin® Tablets are a controlled-release oral formulation of oxycodone hydrochloride indicated for the management of moderate to severe pain when a continuous, around-the-clock analgesic is needed for an extended period of time. OxyContin® tablets are NOT intended for use as a pro re nata (PRN) analgesic.

OxyContin® 80 mg and 160 mg tablets are for use in opioid-tolerant patients only. These tablet strengths may cause fatal respiratory depression when administered to patients not previously exposed to opioids. Oxycontin® tablets are to be swallowed whole and are not to be broken, chewed, or crushed. Taking broken, chewed, or crushed OxyContin® tablets leads to rapid release and absorption of a potentially fatal dose of oxycodone.

In order to overcome such disadvantages, Purdue Pharma investigational drug combined the opioid analgesic oxycodone with the opioid antagonist naloxone in the relation of 3.5:1. The company developed this formulation to reduce intravenous abuse, and potentially intranasal abuse, of OxyContin® (oxycodone HCl controlled release) tablets. This is an interim solution in response to reports of intravenous abuse in late 2000. It was assumed to be the most rapid, albeit partial, solution. The company had been pursuing other approaches prior to the naloxone project and is continuing to develop these other new drug candidates. These may have greater potential to deter not only intravenous abuse, but also the more common oral and intranasal abuse after first crushing the tablet. Developing new forms of pain relievers that are safe and effective for patients with pain while being more resistant to abuse is Purdue Pharma's research priority on developing abuse-resistant formulations.

Developing new medications that are safe and effective for patients in pain, and at the same time, resistant to abuse, is a very complex scientific and technical challenge. Prior data of the Worldwide Research and Development at Purdue Pharma recent Phase 1 studies have shown that the absorption or metabolism of naloxone is more variable than expected. Such variability has the potential to compromise pain relief in some patients. However, using lower doses of naloxone may not be sufficient to deter abuse. After reviewing the results of the Company's clinical data, company and FDA officials agreed that additional studies would be needed to fully assess the safety of this drug formulation in patients with pain as well as its potential to deter abuse. Furthermore, naloxone has significant limitations as an abuse deterrent. According to law enforcement sources, the majority of abuse of OxyContin® occurs orally or intranasally after crushing the tablets. The product's prescribing information therefore contains a warning clearly stating that OxyContin® Tablets are not to be swallowed whole and are not to be broken, chewed or crushed. While the oxycodone/naloxone formulation would deter abuse by intravenous injection, and possibly by the intranasal route ("snorting"), orally administered naloxone is, in most cases, rapidly metabolized and eliminated from the body. Therefore, naloxone is unlikely to be an effective deterrent to oral abuse of crushed OxyContin®.

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