Buprenorphine Duration of Action: Mu-opioid Receptor Availability and Pharmacokinetic and Behavioral Indices

@article{Greenwald2007BuprenorphineDO,
  title={Buprenorphine Duration of Action: Mu-opioid Receptor Availability and Pharmacokinetic and Behavioral Indices},
  author={Mark K. Greenwald and Chris Ellyn Johanson and Joshua A. Bueller and Yan Chang and David E. Moody and Michael Kilbourn and Robert A. Koeppe and Jon-Kar Zubieta},
  journal={Biological Psychiatry},
  year={2007},
  volume={61},
  pages={101-110}
}
Buprenorphine Pharmacodynamics and Pharmacokinetics
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This chapter will focus on buprenorphine’s action at mu opioid receptors, and whether the kappa antagonist and/or nociceptin/orphanin partial agonist activity of bup Renorphine produce any effects of clinical relevance, although this has been the focus of some speculation.
Effect of sustained high buprenorphine plasma concentrations on fentanyl-induced respiratory depression: A placebo-controlled crossover study in healthy volunteers and opioid-tolerant patients
TLDR
Results from this proof-of-principle study provide the first clinical evidence that high sustained plasma concentrations of buprenorphine may protect against respiratory depression induced by potent opioids like fentanyl.
Sustained-Release Buprenorphine (RBP-6000) Blocks the Effects of Opioid Challenge With Hydromorphone in Subjects With Opioid Use Disorder
TLDR
It is demonstrated that RBP-6000 at a 300 mg dose provides durable and potent blockade of the subjective effects and reinforcing efficacy of hydromorphone in subjects with moderate or severe opioid use disorder.
Early impact of methadone induction for heroin dependence: differential effects of two dose sequences in a randomized controlled study.
  • M. Greenwald
  • Psychology
    Experimental and clinical psychopharmacology
  • 2006
TLDR
The pharmacodynamic and pharmacokinetic effects of 2 methadone (METH) induction dose sequences were evaluated and provide a procedural template that might be applied safely and effectively with a broader range of treatment-seeking individuals.
Population Pharmacokinetics of a Monthly Buprenorphine Depot Injection for the Treatment of Opioid Use Disorder: A Combined Analysis of Phase II and Phase III Trials
TLDR
The present analysis led to the development of a robust population pharmacokinetic model and confirms the ability of BUP-XR to deliver and maintain therapeutic plasma concentrations over the entire treatment duration.
Metabolic and toxicological considerations of the opioid replacement therapy and analgesic drugs: methadone and buprenorphine
  • D. Moody
  • Biology
    Expert opinion on drug metabolism & toxicology
  • 2013
TLDR
The use and misuse of these drugs contributes to the epidemic in opioid-associated mortalities, and a better understanding of metabolism-, transport- and co-medication-induced changes will contribute to their safer use.
Treating Chronic Pain: An Overview of Clinical Studies Centered on the Buprenorphine Option
TLDR
Although originally designed as an analgesic, buprenorphine has mainly been used for opioid maintenance therapy and only now is increasingly recognized as an effective analgesic with an improved therapeutic index relative to certain potent opioids.
Optimal dose of buprenorphine in opioid use disorder treatment: a review of pharmacodynamic and efficacy data
TLDR
The BUP dose in treatment of OUD should be individualized based on a continuous clinical benefit-risk assessment, as there is currently no consensus regarding optimal dose or dose-range of buprenorphine for treatment of opioid use disorder.
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TLDR
It is suggested that high-dose BUP maintenance produces near-maximal μOR occupation, μOR availability correlates well with plasma levels, and BUP-related opioid symptoms and antagonist blockade exhibit concentration–effect relationships.
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These data suggest that 2 mg buprenorphine is a sub-therapeutic maintenance dose, both bupenorphine 8 mg and naltrexone produce immediate and efficacious opioid blockade, and adequate protection against illicit opioids may be achieved with less-than-daily dosing.
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Early impact of methadone induction for heroin dependence: differential effects of two dose sequences in a randomized controlled study.
  • M. Greenwald
  • Psychology
    Experimental and clinical psychopharmacology
  • 2006
TLDR
The pharmacodynamic and pharmacokinetic effects of 2 methadone (METH) induction dose sequences were evaluated and provide a procedural template that might be applied safely and effectively with a broader range of treatment-seeking individuals.
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TLDR
The long elimination half-life of buprenorphine suggested that increasing the bup Renorphine dose with alternate-day administration may provide an effective, flexible therapy regimen for the treatment of opioid dependence.
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