Background: Various transporters, including efflux transporters and uptake transporters,
play an important role in the pharmacokinetics of drugs. Currently, studies suggest that several
antibiotics also serve as substrates for transporters. In addition, these antibiotics are usually
combined with other drugs to treat diseases, more effectively. Therefore, it is necessary to focus
on the role of transporters in pharmacokinetics and drug-drug interactions of antibiotics.
Methods: This review summarizes the findings of recent studies as well as information retrieved
from several databases (until June 2015): ISI Web of KnowledgeSM (ISI WoK), SciFinder
(Caplus, Medline, Registry, Casreact, Chrmlist, and Chemcasts) and PubMed (indexed for Medline).
Results: The present review provides useful information for the study of transporters in the
pharmacokinetics and drug-drug interactions of antibiotics, and should assist researchers investigating
Conclusion: The drug transporters mediate intestinal absorption, hepatic uptake, and kidney or biliary excretion. It is
necessary to focus on drug-drug interactions when these antibiotics are combined with other chemical substances that
are also the substrates for transporters.