Nancy A. Melville

October 04, 2011

October 4, 2011 (Las Vegas, Nevada) — An immediate-release oxycodone tablet designed to cause various unpleasant sensations when inhaled shows efficacy in preventing the abuse of the drug, according to research presented here at the annual meeting of the American Academy of Pain Management.

Abuse of controlled prescription pain relievers such as oxycodone, particularly through intranasal or intravenous administration, runs high in the United States. In an effort to prevent such abuse, drug companies have been developing formulations that are just as effective for conventional purposes but are unpleasant enough to deter inhalation abuse.

To evaluate an inhalation-abuse deterrent formulation for oxycodone, researchers led by Robert L. Rolleri, PharmD, from King Pharmaceuticals Research and Development, conducted a randomized, double-blind, 2-way crossover company-supported study of 40 participants who were nondependent recreational opioid users.

The participants were randomly assigned to receive two 7.5-mg crushed oxycodone tablets formulated with functional excipients designed create barriers for intranasal abuse or three 5-mg crushed tablets, administered in crossover fashion and separated by 48 hours.

The study's primary endpoints, all assessed by using 100-point visual analog scales (VAS), included maximum effect for drug liking, the effect at 8 hours postdose regarding whether the participant would take the drug again, and their overall drug liking.

The crushed tablets with functional excipients were associated with significantly less favorable responses; for all measures, least-squares mean VAS scores were reduced compared with crushed oxycodone tablets that lacked the deterrent.

Patient Responses to Oxycodone With or Without Deterrent (VAS Score)

Endpoint Oxycodone With Deterrent Oxycodone Without Deterrent P Value
Maximum effect for drug liking 70.8 93.5 .0001
Take drug again 45.9 91.3 .0001
Overall drug liking 47.8 87.4 .0001

No differences between the groups in terms of treatment were seen according to papillary response measures. The participants were 80% male and 75% white and had a mean age of 35.7 ± 10.2 years. One participant was excluded because of postdose vomiting.

The side effects related to inhalation of the drug formulated as an abuse deterrent included rhinorrhea, nasal congestion, nasal discomfort, throat irritation, increased lacrimation, and facial pain and were greater among those taking the new formulation.

The authors conclude that among nondependent recreational opioid users, these results suggest that crushed tablets of immediate-release oxycodone may have a lower intranasal abuse potential with the addition of functional excipients.

Intense Pressure

Although drug companies push ahead with formulations to better deter intranasal abuse, some question the extent of benefit from such strategies.

"There is a lot of work now on making these drugs abuse resistant because prescription drug abuse is such a big problem," said pain medicine specialist William Granger, MD, from Marion General Hospital, Marion, Indiana, who was not involved in the study. "I think all pharmaceutical companies are under intense pressure to mitigate the large amounts of diverted/abused drugs.

"However, if these things all come to pass, why wouldn't someone just swallow the pill as intended?" he asked.

"Supposedly you get a bigger high injecting or snorting these because you get a large quantity instead of slow measured release," he added. "I think this particular study is just one more attempt to do the same, but whether this really helps remains to be seen."

The study was sponsored by King Pharmaceuticals/Pfizer. Dr. Granger has disclosed no relevant financial relationships.

American Academy of Pain Management. Presented September 21, 2011. Abstract #6.


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