Abstract
Most pharmacokinetic studies so far have focused on the role of drug-metabolizing enzymes as the key determinants of drug disposition and their contribution to drug-drug interactions. It has now become clear that transporters are responsible for both the uptake and efflux of drugs in various tissues. Their coordinated expression and activities at the basolateral and apical side of transporting epithelia are critical in determining the extent and direction of drug movement in major organs for drug disposition such as the intestine, liver and kidney. Thus, drug transporters represent an important mechanism by which one drug may alter the pharmacokinetic and pharmacological effects (toxicity and efficacy) of another and lead to drug-drug interactions of clinical importance. This chapter focuses on the major drug transporters mediating the pharmacokinetics of anti-infective agents with special emphasis on their effect on drug disposition, their drug substrate specificities as well as their role in clinically relevant drug-drug interactions.
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Moss, D.M., Siccardi, M., Marzolini, C. (2018). Mechanisms of Drug Interactions II: Transport Proteins. In: Pai, M., Kiser, J., Gubbins, P., Rodvold, K. (eds) Drug Interactions in Infectious Diseases: Mechanisms and Models of Drug Interactions. Infectious Disease. Humana Press, Cham. https://doi.org/10.1007/978-3-319-72422-5_3
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