Buprenorphine/naltrexone explained

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]}

See also

• Buprenorphine/samidorphan
• Buprenorphine/naloxone

Notes and References

1. McCann DJ . Potential of buprenorphine/naltrexone in treating polydrug addiction and co-occurring psychiatric disorders . Clinical Pharmacology and Therapeutics . 83 . 4 . 627–30 . April 2008 . 18212797 . 10.1038/sj.clpt.6100503 . 21165673 .
2. Cordery SF, Taverner A, Ridzwan IE, Guy RH, Delgado-Charro MB, Husbands SM, Bailey CP . A non-rewarding, non-aversive buprenorphine/naltrexone combination attenuates drug-primed reinstatement to cocaine and morphine in rats in a conditioned place preference paradigm . Addiction Biology . 19 . 4 . 575–86 . July 2014 . 23240906 . 10.1111/adb.12020 . 18330823 .
3. Falcon E, Maier K, Robinson SA, Hill-Smith TE, Lucki I . Effects of buprenorphine on behavioral tests for antidepressant and anxiolytic drugs in mice . Psychopharmacology . 232 . 5 . 907–15 . March 2015 . 25178815 . 4326609 . 10.1007/s00213-014-3723-y .
4. Falcon E, Browne CA, Leon RM, Fleites VC, Sweeney R, Kirby LG, Lucki I . Antidepressant-like Effects of Buprenorphine are Mediated by Kappa Opioid Receptors . Neuropsychopharmacology . 41 . 9 . 2344–51 . August 2016 . 26979295 . 4946065 . 10.1038/npp.2016.38 .
5. Almatroudi A, Husbands SM, Bailey CP, Bailey SJ . Combined administration of buprenorphine and naltrexone produces antidepressant-like effects in mice . Journal of Psychopharmacology . 29 . 7 . 812–21 . July 2015 . 26045511 . 5075030 . 10.1177/0269881115586937 .
6. Ling W, Hillhouse MP, Saxon AJ, Mooney LJ, Thomas CM, Ang A, Matthews AG, Hasson A, Annon J, Sparenborg S, Liu DS, McCormack J, Church S, Swafford W, Drexler K, Schuman C, Ross S, Wiest K, Korthuis PT, Lawson W, Brigham GS, Knox PC, Dawes M, Rotrosen J . 6 . Buprenorphine + naloxone plus naltrexone for the treatment of cocaine dependence: the Cocaine Use Reduction with Buprenorphine (CURB) study . Addiction . 111 . 8 . 1416–27 . August 2016 . 26948856 . 4940267 . 10.1111/add.13375 .