Buprenorphine/naltrexone

Buprenorphine/naltrexone is an experimental combination drug formulation of buprenorphine, a μ-opioid receptor (MOR) weak partial agonist and κ-opioid receptor (KOR) antagonist, and naltrexone, a MOR and KOR silent antagonist, which is under investigation for the potential treatment of psychiatric disorders.[1][2] The combination of the two drugs is thought to result in a selective blockade of the KOR and hence fewer MOR activation-related concerns such as euphoria and opioid dependence. It has been found to produce antidepressant-like effects in mice (similarly to the case of buprenorphine alone or in combination with samidorphan)[3][4] and (at a buprenorphine dosage of 16 mg/day but not 4 mg/day) has recently been found to be effective in the treatment of cocaine dependence in a large (n = 302) human clinical trial.[5][6]

Buprenorphine/naltrexone
Combination of
BuprenorphineOpioid modulator
NaltrexoneOpioid antagonist
Legal status
Legal status
  • US: Schedule III

See also

References
  1. McCann, DJ (2008). "Potential of Buprenorphine/Naltrexone in Treating Polydrug Addiction and Co-occurring Psychiatric Disorders". Clinical Pharmacology & Therapeutics. 83 (4): 627–630. doi:10.1038/sj.clpt.6100503. ISSN 0009-9236. PMID 18212797.
  2. Cordery, Sarah F.; Taverner, Alistair; Ridzwan, Irna E.; Guy, Richard H.; Delgado-Charro, M. Begoña; Husbands, Stephen M.; Bailey, Christopher P. (2014). "A non-rewarding, non-aversive buprenorphine/naltrexone combination attenuates drug-primed reinstatement to cocaine and morphine in rats in a conditioned place preference paradigm" (PDF). Addiction Biology. 19 (4): 575–586. doi:10.1111/adb.12020. ISSN 1355-6215.
  3. Falcon, Edgardo; Maier, Kaitlyn; Robinson, Shivon A.; Hill-Smith, Tiffany E.; Lucki, Irwin (2014). "Effects of buprenorphine on behavioral tests for antidepressant and anxiolytic drugs in mice". Psychopharmacology. 232 (5): 907–915. doi:10.1007/s00213-014-3723-y. ISSN 0033-3158. PMC 4326609. PMID 25178815.
  4. Falcon, Edgardo; Browne, Caroline A; Leon, Rosa M; Fleites, Vanessa C; Sweeney, Rachel; Kirby, Lynn G; Lucki, Irwin (2016). "Antidepressant-Like Effects of Buprenorphine are Mediated by Kappa Opioid Receptors". Neuropsychopharmacology. 41 (9): 2344–2351. doi:10.1038/npp.2016.38. ISSN 0893-133X. PMC 4946065. PMID 26979295.
  5. Almatroudi, A.; Husbands, S. M.; Bailey, C. P.; Bailey, S. J. (2015). "Combined administration of buprenorphine and naltrexone produces antidepressant-like effects in mice". Journal of Psychopharmacology. 29 (7): 812–821. doi:10.1177/0269881115586937. ISSN 0269-8811. PMC 5075030. PMID 26045511.
  6. Ling, Walter; Hillhouse, Maureen P.; Saxon, Andrew J.; Mooney, Larissa J.; Thomas, Christie M.; Ang, Alfonso; Matthews, Abigail G.; Hasson, Albert; Annon, Jeffrey; Sparenborg, Steve; Liu, David S.; McCormack, Jennifer; Church, Sarah; Swafford, William; Drexler, Karen; Schuman, Carolyn; Ross, Stephen; Wiest, Katharina; Korthuis, Philip; Lawson, William; Brigham, Gregory S.; Knox, Patricia C.; Dawes, Michael; Rotrosen, John (2016). "Buprenorphine + Naloxone plus Naltrexone for the Treatment of Cocaine Dependence:The Cocaine Use Reduction with Buprenorphine(CURB)Study". Addiction. 111 (8): 1416–1427. doi:10.1111/add.13375. ISSN 0965-2140. PMC 4940267. PMID 26948856.


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