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Mellar P. Davis

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date: 24 September 2021

Chapter 12 discusses Buprenorphine, a methylvinyl ketone adduct of theobaine which was developed in the 1960s. It is classified as a partial mu agonist, but some refer to it as an agonist–antagonist. Buprenorphine binds to mu, kappa1, kappa3, and orphan-related ligand-1 (ORL-1) receptors. Interest in buprenorphine has increased because of its relative safety in addiction maintenance therapy, its ‘ceiling’ effect on respiratory depression, and unique anti-hyperalgesic activity, which differs from that of potent mu opioids such as fentanyl or methadone. Buprenorphine has been used extensively to manage cancer pain. The development of a transdermal matrix patch has increased its use for cancer and non-cancer pain in countries where the patch is available.

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