2021
DOI: 10.3389/fphar.2021.718811
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Transition From Full Mu Opioid Agonists to Buprenorphine in Opioid Dependent Patients—A Critical Review

Abstract: Methadone, a full opioid agonist at the mu-, kappa-, and delta-receptor, and buprenorphine, a partial agonist at the mu receptor, are first-line medications in opioid maintenance treatment. Transition from methadone to buprenorphine may precipitate withdrawal, and no accepted algorithm for this procedure has been developed. Current treatment strategies recommend transfer from methadone to buprenorphine predominantly in patients at low doses of methadone (30–40 mg/day). There are some reports indicating that tr… Show more

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Cited by 9 publications
(6 citation statements)
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References 67 publications
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“…The transition from higher doses of rac-methadone is possible, as was applied in our centers. Several dosing strategies have been proposed to soften withdrawal symptoms and facilitate transfer, including the use of other opioids or medications and, especially, micro-dosing techniques for buprenorphine, as reported by others, including the transition from the higher to lower dosing protocols [34].…”
Section: Discussionmentioning
confidence: 99%
“…The transition from higher doses of rac-methadone is possible, as was applied in our centers. Several dosing strategies have been proposed to soften withdrawal symptoms and facilitate transfer, including the use of other opioids or medications and, especially, micro-dosing techniques for buprenorphine, as reported by others, including the transition from the higher to lower dosing protocols [34].…”
Section: Discussionmentioning
confidence: 99%
“…The mainstay for the treatment of opioid use disorder has been opioid substitution therapy with either methadone or buprenorphine (sublingual film or long-acting injectable depot buprenorphine [LAIB] preparations) [1]. There are a number of indications for transitioning between these medications including patient preference, greater access to unsupervised dosing in some jurisdictions with buprenorphine and clinical concerns about safety [2,3]. Methadone is a full agonist of the mu opioid receptor while buprenorphine is a partial agonist at the mu receptor; however, buprenorphine has a very high affinity for the mu receptor and can displace other full agonist opioids from the mu receptor resulting in the phenomena commonly known as precipitated withdrawal [4,5].…”
Section: Introductionmentioning
confidence: 99%
“…All 3 medications have different mechanisms of action, which are attributed to their variable receptor-binding affinities. 3,4 Methadone is a full opioid agonist, while buprenorphine is a partial μ-opioid receptor agonist and naltrexone is a μ-opioid receptor antagonist. Higher doses of methadone induce opioid tolerance with reduced effects of the injected drug.…”
mentioning
confidence: 99%