Elimination of substances from the brain parenchyma: efflux via perivascular pathways and via the blood–brain barrier

SB Hladky, MA Barrand - Fluids and Barriers of the CNS, 2018 - Springer
This review considers efflux of substances from brain parenchyma quantified as values of
clearances (CL, stated in µL g− 1 min− 1). Total clearance of a substance is the sum of …

Opioids and the blood-brain barrier: a dynamic interaction with consequences on drug disposition in brain

C Chaves, F Remiao, S Cisternino… - Current …, 2017 - ingentaconnect.com
Background: Opioids are widely used in pain management, acting via opioid receptors
and/or Toll-like receptors (TLR) present at the central nervous system (CNS). At the blood …

ADMET Evaluation in Drug Discovery. 13. Development of in Silico Prediction Models for P-Glycoprotein Substrates

D Li, L Chen, Y Li, S Tian, H Sun… - Molecular pharmaceutics, 2014 - ACS Publications
P-glycoprotein (P-gp) actively transports a wide variety of chemically diverse compounds out
of cells. It is highly associated with the ADMET properties of drugs and drug candidates and …

Interaction of drugs of abuse and maintenance treatments with human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2)

N Tournier, L Chevillard, B Megarbane… - International Journal …, 2010 - academic.oup.com
Drug interaction with P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP)
may influence its tissue disposition including blood–brain barrier transport and result in …

Imaging of cyclosporine inhibition of P-glycoprotein activity using 11C-verapamil in the brain: studies of healthy humans

M Muzi, DA Mankoff, JM Link, S Shoner… - Journal of Nuclear …, 2009 - Soc Nuclear Med
The multiple-drug resistance (MDR) transporter P-glycoprotein (P-gp) is highly expressed at
the human blood–brain barrier (BBB). P-gp actively effluxes a wide variety of drugs from the …

Efflux transporters-and cytochrome P-450-mediated interactions between drugs of abuse and antiretrovirals

D Pal, D Kwatra, M Minocha, DK Paturi, B Budda… - Life sciences, 2011 - Elsevier
Multidrug regimens and corresponding drug interactions cause many adverse reactions and
treatment failures. Drug efflux transporters: P-gp, MRP, BCRP in conjunction with …

Oxycodone, an opioid like the others?

N Marie, F Noble - Frontiers in Psychiatry, 2023 - frontiersin.org
The over-prescription of opioid analgesics is a growing problem in the field of addiction,
which has reached epidemic-like proportions in North America. Over the past decade …

The Impact of P-Glycoprotein on Opioid Analgesics: What's the Real Meaning in Pain Management and Palliative Care?

F Coluzzi, MS Scerpa, M Rocco… - International Journal of …, 2022 - mdpi.com
Opioids are widely used in cancer and non-cancer pain management. However, many
transporters at the blood–brain barrier (BBB), such as P-glycoprotein (P-gp, ABCB1/MDR1) …

Differential involvement of P-glycoprotein (ABCB1) in permeability, tissue distribution, and antinociceptive activity of methadone, buprenorphine, and diprenorphine: in …

HE Hassan, AL Myers, A Coop… - Journal of pharmaceutical …, 2009 - Elsevier
Conclusions based on either in vitro or in vivo approach to evaluate the P-gp affinity status of
opioids may be misleading. For example, in vitro studies indicated that fentanyl is a P-gp …

Respiratory toxicity of buprenorphine results from the blockage of P-glycoprotein-mediated efflux of norbuprenorphine at the blood–brain barrier in mice

H Alhaddad, S Cisternino, X Declèves… - Critical care …, 2012 - journals.lww.com
Objectives: Deaths due to asphyxia as well as following acute poisoning with severe
respiratory depression have been attributed to buprenorphine in opioid abusers. However …