Drug and xenobiotic biotransforrnation in the blood-brain barrier: a neglected issue

作者:Agundez Jose A G*; Jimenez Jimenez Felix J; Alonso Navarro Hortensia; Garcia Martin Elena
来源:Frontiers in Cellular Neuroscience, 2014, 8: 335.
DOI:10.3389/fncel.2014.00335

摘要

Drug biotransformation is a crucial mechanism for facilitating the elimination of chemicals from the organism and for decreasing their pharmacological activity. Published evidence suggests that brain drug metabolism may play a role in the development of adverse drug reactions and in the clinical response to drugs and xenobiotics. The blood-brain barrier (BBB) has been regarded mainly as a physical barrier for drugs and xenobiotics, and little attention has been paid to the BBB as a drug-metabolizing barrier. The presence of drug-metabolizing enzymes in the BBB is likely to have functional implications because local metabolism may inactivate drugs or may modify the drug%26apos;s ability to cross the BBB, thus modifying drug response and the risk of developing adverse drug reactions. In this perspective paper, we discuss the expression of relevant xenobiotic metabolizing enzymes in the brain and in the BBB, and we cover current advances and future directions on the potential role of these BBB drug-metabolizing enzymes as modifiers of drug response.

  • 出版日期2014-10-17