Buprenorphine/naltrexone
Combination drug formulation
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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]
| Combination of | |
|---|---|
| Buprenorphine | Opioid modulator |
| Naltrexone | Opioid antagonist |
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