A comparison among tapentadol tamper‐resistant formulations (TRF) and OxyContin^® (non‐TRF) in prescription opioid abusers

Abstract

Aims To examine whether tamper-resistant formulations (TRFs) of tapentadol hydrochloride ER 50 mg (TAP50) and tapentadol hydrochloride 250 mg (TAP250) could be converted into forms amenable to intranasal (Study 1) or intravenous abuse (Study 2). Design Randomized, repeated-measures study designs were employed. A non-TRF of OxyContin® 40 mg (OXY40) served as a positive control. No drug was taken in either study. Setting The studies took place in an outpatient setting in New York, NY. Participants 25 experienced, healthy extended-release oxycodone abusers participated in each study. Measurements The primary outcome for Study 1 was percentage of participants who indicated they would snort the tampered tablets, while the primary outcome for Study 2 was percent yield of active drug in solution. Other descriptive variables such as time spent manipulating the tablets were also examined to better characterize tampering behaviors. Findings Tampered TRF tablets were less desirable than the tampered OXY40 tablets. Few individuals were willing to snort the TRF particles (TAP50: 24%, TAP250: 16%; OXY40: 100% p<.001). There was less drug extracted from the TAP50 tablet than from the OXY40 tablet (3.5% vs. 37.0%, p=.008), and no samples from the TAP250 tablets contained analyzable solutions of the drug. It took participants longer to tamper with the TAPs (Study 1: TAP50 vs. OXY40, p<.01; TAP250 vs. OXY40, p<.01; Study 2: TAP250 vs. OXY40, p<05). Conclusions Taptentadol TRF tablets were not well-liked by individuals who regularly tampered with extended-release oxycodone tablets. Employing tamper resistant technology may be a promising approach towards reducing the abuse potential of tapentadol ER.

Practical Considerations for the Use of Tapentadol Prolonged Release for the Management of Severe Chronic Pain

“…90 A tamper-resistant formulation of tapentadol PR (which is resistant to crushing and forms a gel when combined with small volumes of liquid) is available in the United States. 91 Although caution is warranted when prescribing tapentadol PR to patients for whom there is a concern about an elevated risk of drug misuse, abuse, addiction, or diversion, 33 results of recent studies indicate a low level of abuse for tapentadol in practice. In a study 92 that evaluated the rates of abuse and diversion of tapentadol IR after its introduction to the US market using data from a US surveillance system (the Researched Abuse, Diversion, and AddictionRelated Surveillance [RADARS] system 93 ), rates of tapentadol IR abuse and diversion were low during the first 24 months after its introduction (Figure 8).…”

Commercial Abuse-Deterrent Dosage Forms: Clinical Status

“…For example, a tamper-resistant formulation of Nucynta® ER was compared against an original non-tamper resistant formulation of Oxycontin® to determine ease of reducing each product's particle size [15]. Crushed products produced from each tablet by experienced abusers using any equipment they desired was ultimately passed through varying sieves for particle size analysis.…”

The ALERRT® instrument: a quantitative measure of the effort required to compromise prescription opioid abuse-deterrent tablets

“…A comparison of two formulations of oxymorphone found that the maximum time participants were willing to spend tampering with the products was approximately 15 minutes (10). In a similar study, participants spent an average of 3 to 7 minutes to manipulate oxycodone or tapentadol for intranasal or intravenous administration even though they were allowed up to 60 minutes (11). The latest report from the Researched Abuse, Diversion and Addiction-Related Surveillance (RADARS) system showed that ease of manipulation was a main factor for a strong preference for IR over ER opioids (12).…”

“…In addition to Category 1 studies that focus on the "output" of the manipulation effort, the ALERRT instrument was developed to capture information about the "input" (time, effort, and resources necessary to convert the product into an abusable form). If the degree of effort required is perceived by drug users to be onerous, it is possible that this property may in and of itself deter abuse (9,11). In this respect, it is important to note that this dimension is not captured in Category 3 clinical studies designed to evaluate the abuse potential of a new drug.…”