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Enzyme systems have evolved in humans to maintain cellular homeostasis and to facilitate the disposition of xenobiotics. These enzymes possess complementary, and sometimes overlapping, functions, a feature which can set the stage for drug–drug interactions. In this chapter, we provide an overview of the phase I and phase II families of detoxification enzymes, their potential for induction and inhibition,...
There is an increasing appreciation of the role that transport proteins play in the absorption, distribution, and elimination of a wide variety of drugs in clinical use. These transporters can be divided into efflux transporters belonging to the ATP-binding cassette (ABC) family and solute carrier (SLC) family members that mediate the influx or bidirectional movement of drugs across the cell membrane...
The extent of drug metabolism or drug transport-based pharmacokinetic drug–drug interactions is highly variable between individuals. CYP enzymes such as CYP2B6, CYP2C9, CYP2C19, and CYP2D6 and drug efflux and uptake transporters such as ABCB1 and OAT1B1 display genetic polymorphisms (presence of genetic variants in at least 1% of a population) that may result in altered drug metabolism or transport...
Nuclear receptors play a central role on the mechanism of induction-type drug–drug interactions by acting as xenosensing transcription factors. Together, PXR, CAR, FXR, and VDR form a core group of nuclear receptors that regulate the expression of a number of important drug-metabolizing enzymes and drug transporters. In this chapter, the molecular determinants of adaptive response to drug exposure...
Physiologically based pharmacokinetic (PBPK) models of the intestine, liver, and kidney were developed to examine the influence of transporters as well as enzymes on the area under the curve and clearances of drugs and metabolites. Whole body PBPK models were then developed, with the kidney and intestine or the kidney and liver as the organs for excretion and metabolism. From these PBPK models, the...
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