Use of Peripheral μ-Opioid Receptor Antagonists for Treating Opioid-Induced Constipation among US Medicare Beneficiaries from 2014 to 2018

2021 ◽  
Author(s):  
Naveen Premnath ◽  
Andrew Sumarsono ◽  
Ramy Sedhom ◽  
David H. Johnson ◽  
Ishwaria M. Subbiah ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Medicare Beneficiaries ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists ◽  
Μ Opioid Receptor

Transformation of μ-opioid receptor agonists into biologically potent μ-opioid receptor antagonists

2007 ◽  
Vol 15 (3) ◽  
pp. 1237-1251 ◽  
Author(s):  
Tingyou Li ◽  
Yunden Jinsmaa ◽  
Masahiro Nedachi ◽  
Anna Miyazaki ◽  
Yuko Tsuda ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Antagonists ◽  
Receptor Agonists ◽  
Opioid Receptor Antagonists ◽  
Μ Opioid Receptor ◽  
Opioid Receptor Agonists

Antipruritic treatment with systemic μ-opioid receptor antagonists: A review

2010 ◽  
Vol 63 (4) ◽  
pp. 680-688 ◽  
Author(s):  
Ngoc Quan Phan ◽  
Jeffrey D. Bernhard ◽  
Thomas A. Luger ◽  
Sonja Ständer
Keyword(s):  
Opioid Receptor ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists ◽  
Μ Opioid Receptor

scholarly journals Blood–brain barrier: mechanisms governing permeability and interaction with peripherally acting μ-opioid receptor antagonists

2020 ◽  
Vol 45 (9) ◽  
pp. 688-695
Author(s):  
Eugene R Viscusi ◽  
Andrew R Viscusi
Keyword(s):  
Blood Brain Barrier ◽  
Opioid Receptor ◽  
Randomized Clinical Trials ◽  
Brain Barrier ◽  
Receptor Antagonists ◽  
Waste Products ◽  
Blood Brain ◽  
Opioid Receptor Antagonists ◽  
Μ Opioid Receptor ◽  
Bbb Permeability

The blood–brain barrier (BBB) describes the unique properties of endothelial cells (ECs) that line the central nervous system (CNS) microvasculature. The BBB supports CNS homeostasis via EC-associated transport of ions, nutrients, proteins and waste products between the brain and blood. These transport mechanisms also serve as physiological barriers to pathogens, toxins and xenobiotics to prevent them from contacting neural tissue. The mechanisms that govern BBB permeability pose a challenge to drug design for CNS disorders, including pain, but can be exploited to limit the effects of a drug to the periphery, as in the design of the peripherally acting μ-opioid receptor antagonists (PAMORAs) used to treat opioid-induced constipation. Here, we describe BBB physiology, drug properties that affect BBB penetrance and how data from randomized clinical trials of PAMORAs improve our understanding of BBB permeability.

scholarly journals 14β-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and Related Opioids. Further Examples of Pseudoirreversible μ Opioid Receptor Antagonists

2009 ◽  
Vol 52 (21) ◽  
pp. 6926-6930 ◽  
Author(s):  
Nick P.R. Nieland ◽  
David Rennison ◽  
Jillian H. Broadbear ◽  
Lauren Purington ◽  
James H. Woods ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists ◽  
Μ Opioid Receptor
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