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- W101066613 endingPage "72" @default.
- W101066613 startingPage "63" @default.
- W101066613 abstract "The active multidrug transporter P–glycoprotein (Pgp) influences the pharmacokinetics of drugs at several sites in the body due to its presence in various epithelial and endothelial tissues. As a consequence, the oral bioavailabiliy of drugs may be limited by Pgp, whereas excretion may be increased and distribution changed. The role of Pgp is especially clear at the level of the blood–brain barrier, where it prevents Pgp substrates from entering the brain. Numerous studies have been performed to clarify the role of Pgp in the body, but also to influence its function and thereby alter the distribution kinetics of drugs. This also has implications for the intensity of drug effects of various classes of drugs in the brain, such as centrally acting agents, anticancer drugs, and HIV protease inhibitors. Furthermore, it is highly conceivable that a genetically determined polymorphism(s) of Pgp expression exists and that Pgp expression itself can be induced by drugs or environmental conditions. This may lead to substantial intra– and interindividual differences in the disposition of drugs. The pharmacokinetics of drugs may also be altered by Pgp due to its role in modulating the expression of cytochrome P450 3A4 (CYP 3A4). This complicates prediction of the interaction of drugs that are Pgp substrate and are metabolized by CYP 3A4. The reason why Pgp transports such a substantial number of different drugs is, however, still unclear; it seems that Pgp is a complex regulated system with various binding sites." @default.
- W101066613 created "2016-06-24" @default.
- W101066613 creator A5015382020 @default.
- W101066613 creator A5019235837 @default.
- W101066613 creator A5077531513 @default.
- W101066613 date "2004-01-01" @default.
- W101066613 modified "2023-09-26" @default.
- W101066613 title "Implications of P–glycoprotein for the Transport and Distribution of Drugs into the Brain" @default.
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