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 clinical trial.[5][6]

Buprenorphine/naltrexone
Combination of
BuprenorphineOpioid modulator
NaltrexoneOpioid antagonist
Legal status
Legal status
Identifiers
CAS Number

See also

References
  1. McCann DJ (April 2008). "Potential of buprenorphine/naltrexone in treating polydrug addiction and co-occurring psychiatric disorders". Clinical Pharmacology and Therapeutics. 83 (4): 627–30. doi:10.1038/sj.clpt.6100503. PMID 18212797. S2CID 21165673.
  2. Cordery SF, Taverner A, Ridzwan IE, Guy RH, Delgado-Charro MB, Husbands SM, Bailey CP (July 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): 575–86. doi:10.1111/adb.12020. PMID 23240906. S2CID 18330823.
  3. Falcon E, Maier K, Robinson SA, Hill-Smith TE, Lucki I (March 2015). "Effects of buprenorphine on behavioral tests for antidepressant and anxiolytic drugs in mice". Psychopharmacology. 232 (5): 907–15. doi:10.1007/s00213-014-3723-y. PMC 4326609. PMID 25178815.
  4. Falcon E, Browne CA, Leon RM, Fleites VC, Sweeney R, Kirby LG, Lucki I (August 2016). "Antidepressant-like Effects of Buprenorphine are Mediated by Kappa Opioid Receptors". Neuropsychopharmacology. 41 (9): 2344–51. doi:10.1038/npp.2016.38. PMC 4946065. PMID 26979295.
  5. Almatroudi A, Husbands SM, Bailey CP, Bailey SJ (July 2015). "Combined administration of buprenorphine and naltrexone produces antidepressant-like effects in mice". Journal of Psychopharmacology. 29 (7): 812–21. doi:10.1177/0269881115586937. PMC 5075030. PMID 26045511.
  6. Ling W, Hillhouse MP, Saxon AJ, Mooney LJ, Thomas CM, Ang A, et al. (August 2016). "Buprenorphine + naloxone plus naltrexone for the treatment of cocaine dependence: the Cocaine Use Reduction with Buprenorphine (CURB) study". Addiction. 111 (8): 1416–27. doi:10.1111/add.13375. PMC 4940267. PMID 26948856.
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