Review Article

Designing Opioids That Deter Abuse

Table 3

Opioid analgesic formulations designed to resist or deter abuse which are commercially available or in development.

Name CompanyAgent(s)DescriptionComment

Physical barrier

Remoxy [24]Pain therapeutics and King PharmaceuticalsOxycodone extended releaseHard gelatin capsule containing viscous liquidORADUR technology (extended-release formulation)
Acuracet [25]AcuraOxycodone immediate release and acetaminophenImpediments to snorting and injection (not further described)
Vycavert [26]Hydrocodone immediate release and acetaminophenImpediments to snorting and injection (not further described)
C0L-003 [27]Collegium pharmaceuticalOxycodone sustained releaseMultiparticulate matrix with particles in waxy excipient base
COL-172 [27]Oxycodone sustained releaseMultiparticulate matrix with particles in waxy excipient base
ReXista [28]IntellipharmaceuticsOxycodone sustained releaseNot described
OxyContin [29]PurdueOxycodone controlled releaseResists crushing and dissolving
TQ-1015 [30]Oxycodone extended releaseCrush and tamper resistantSecurel technology
TQ-1017 [31]TheraQuest BiosciencesTramadol extended releaseTransforms into viscous substance when hydrated
TQ1020 [32]Levorphanol extended releaseNot stated
DDS-08B [33]Labopharm/PaladinOxycodone/APAP extended releaseExtended release even if tablet is tampered with
Exalgo [34]Neuromed/CovidienHydromorphone extended releaseOsmotic delivery system (OROS push-pull technology)New formulation
Not named [35]Pisgah LabsHydrocodoneInsoluble at pH ranges in mucosal membranes
ADPREM [36, 37]Egalet (Denmark)MorphineErodible matrix covered by water-impermeable nonerodible shell
Egalet hydrocodone [36]Egalet (Denmark)HydroconeHard matrix

Agonist/Antagonist

Embeda [38]King PharmaceuticalsMorphine/naltrexonePellets of morphine surrounding a hard core of sequestered naltrexoneNaltrexone pellets are 1.0 to 1.7 mm diameter
ALO-01 [39]AlpharmaMorphine extended release with naltrexoneSequestered naltrexone
Oxytrex [40]Albert Einstein College of MedicineOxycodone and ultra-low-dose naltrexoneUltra-low-dose naltrexone
OxyNal or ELI-216 [40]Elite PharmaceuticalsOxycodone-controlled release with naltrexone pelletsPellets release naltrexone only when crushed
Talwin [41]Sanofi-AventisPentazocine and naloxoneNaloxoneNaloxone released if drug administered parenterally
Suboxone Film [42]Reckitt BenckiserBuprenorphine/naloxoneNaloxone

Aversive agents

Acurox with niacin [43]Acura Pharmaceuticals and King PharmaceuticalsOxycodone immediate release 5 and 7.5 mgNiacin; tablets contain a gel-forming ingredient

Prodrug

NRP 290 [44, 45]New River PharmaceuticalsConditional bioreversible derivative of hydrocodoneLysine-modified prodrugNRP 369 is backup for NRP 290