Buprenorphine/samidorphan

Buprenorphine/samidorphan (also known as BUP/SAM) is a combination drug used for the treatment of major depressive disorder (MDD). It is a combination of buprenorphine, a partial opioid receptor agonist, and samidorphan, an opioid receptor antagonist.

Pharmacology

The combination of buprenorphine and samidorphan works by modulating the mu-opioid receptor (MOR). Buprenorphine is a partial agonist of the MOR, meaning it activates the receptor but not to its full capacity. This results in a ceiling effect, where increasing doses do not increase the drug's effect after a certain point. Samidorphan, on the other hand, is an antagonist of the MOR, meaning it blocks the receptor and prevents it from being activated.

Clinical Use

Buprenorphine/samidorphan is used in the treatment of MDD. It is typically used when other treatments have not been effective. The combination of buprenorphine and samidorphan has been shown to have a rapid onset of action, often providing relief from depressive symptoms within a week.

Side Effects

Common side effects of buprenorphine/samidorphan include nausea, vomiting, and constipation. More serious side effects can include respiratory depression, especially if the drug is taken in high doses or combined with other depressants.

Regulatory Status

Buprenorphine/samidorphan was approved by the Food and Drug Administration (FDA) in 2021 for the treatment of MDD in adults.

See Also

• Major depressive disorder
• Buprenorphine
• Samidorphan
• Opioid receptor

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