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Blood-Brain Barrier Permeability to Drugs

Blood-Brain Barrier Permeability to Drugs William H Oldendorf Research and Neurology Services, V. A. Wadsworth Hospital Center, Los Angeles, California and Department of Neurology, School of Medicine, University of California, Los Angeles, California To affect central nervous system (CNS) cells directly, a c'.rug must appear in the extracellular fluid (ECF) of theCNS. How much of an administered drug distributes to CNS ECF is determined by a number of interdependent factors. If taken orally, a molecule of drug must survive in the gut lumen, penetrate the intestinal wall, traverse the liver, resist degradation by enzymes in blood plasma and other organs, remain unionized in solution unattached to plasma proteins, and ultimately pene­ trate the blood-brain barrier (BBB ). In this review it is assumed a drug is in the peripheral blood, and only those factors directly related to its entry into brain are discussed. Many of the characteristics ofBBB permeability to drugs referred to in this review have been long established and well described previously in this series (1) and in other reviews (2, 3). These well-established areas will be discussed briefly here but emphasis will be placed on what probably are the most interesting relevant develop­ ments during the past decade: the demonstration http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Annual Review of Pharmacology and Toxicology Annual Reviews

Blood-Brain Barrier Permeability to Drugs

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References (1)

Publisher
Annual Reviews
Copyright
Copyright 1974 Annual Reviews. All rights reserved
Subject
Review Articles
ISSN
0362-1642
eISSN
1545-4304
DOI
10.1146/annurev.pa.14.040174.001323
Publisher site
See Article on Publisher Site

Abstract

William H Oldendorf Research and Neurology Services, V. A. Wadsworth Hospital Center, Los Angeles, California and Department of Neurology, School of Medicine, University of California, Los Angeles, California To affect central nervous system (CNS) cells directly, a c'.rug must appear in the extracellular fluid (ECF) of theCNS. How much of an administered drug distributes to CNS ECF is determined by a number of interdependent factors. If taken orally, a molecule of drug must survive in the gut lumen, penetrate the intestinal wall, traverse the liver, resist degradation by enzymes in blood plasma and other organs, remain unionized in solution unattached to plasma proteins, and ultimately pene­ trate the blood-brain barrier (BBB ). In this review it is assumed a drug is in the peripheral blood, and only those factors directly related to its entry into brain are discussed. Many of the characteristics ofBBB permeability to drugs referred to in this review have been long established and well described previously in this series (1) and in other reviews (2, 3). These well-established areas will be discussed briefly here but emphasis will be placed on what probably are the most interesting relevant develop­ ments during the past decade: the demonstration

Journal

Annual Review of Pharmacology and ToxicologyAnnual Reviews

Published: Apr 1, 1974

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