Increased drug delivery to the brain by P-glycoprotein inhibition.

  title={Increased drug delivery to the brain by P-glycoprotein inhibition.},
  author={Abul Sadeque and Christoph Wandel and Handan He and Samit N Shah and Alastair J. J. Wood},
  journal={Clinical pharmacology and therapeutics},
  volume={68 3},
BACKGROUND Although the antidiarrheal loperamide is a potent opiate, it does not produce opioid central nervous system effects at usual doses in patients. On the basis of in vitro studies demonstrating that loperamide is a substrate for the adenosine triphosphate-dependent efflux membrane transporter P-glycoprotein, we postulated that inhibition of P-glycoprotein with quinidine would increase entry of loperamide into the central nervous system with resultant respiratory depression. METHODS To… CONTINUE READING


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