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Buprenorphine, sold under the brand name Subutex among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain. [18] It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), or as an implant.
Opioid agonist therapy (OAT) is a treatment in which prescribed opioid agonists are given to patients who live with Opioid use disorder (OUD). [1] In the case of methadone maintenance treatment (MMT), methadone is used to treat dependence on heroin or other opioids, and is administered on an ongoing basis.
Buprenorphine-3-glucuronide (B3G) is a major active metabolite of the opioid modulator buprenorphine. [1] It has affinity for the μ-opioid receptor (K i = 4.9 (± 2.7) pM), δ-opioid receptor (K i = 270 nM), and nociceptin receptor (K i = 36 μM), but not for the κ-opioid receptor. [1]
Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a fixed-dose combination medication that includes buprenorphine and naloxone. [3] It is used to treat opioid use disorder , and reduces the mortality of opioid use disorder by 50% (by reducing the risk of overdose on full-agonist opioids such as heroin or fentanyl ).
It has been known since the 1980s that buprenorphine binds to at high affinity and antagonizes the KOR. [15] [16]Through activation of the KOR, dynorphins, opioid peptides that are the endogenous ligands of the KOR and that can, in many regards, be figuratively thought of as functional inverses of the morphine-like, euphoric and stress-inhibiting endorphins, [17] induce dysphoria and stress ...
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Buprenorphine has been shown experimentally (1982–1995) to be effective against severe, refractory depression. [3] [4] Bupropion, when sold under the brand name Wellbutrin is indicated for depression. It is also sold as a smoking cessation drug, under the name Zyban. In Ontario, Canada, smoking cessation drugs are not covered by provincial ...
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