Background: Radiation is the fourth most prevalent type of pollution following the water, air and noise
pollution. It can adversely affect normal bodily functions. Radiation alters the protein and mRNA expression of drugmetabolizing
enzymes and drug transporters and the pharmacokinetic characteristics of drugs, thereby affecting drug
absorption, distribution, metabolism, and excretion. Therefore, it is important to study the pharmacokinetic changes
in drugs under radiation.
Methods: To update data on the effects of ionizing radiation and non-ionizing radiation caused by environmental
pollution or clinical treatments on the protein and mRNA expression of drug-metabolizing enzymes and drug transporters.
Data and information on pharmacokinetic changes in drugs under radiation were analyzed and summarized.
Results: The effect of radiation on cytochrome P450 is still a subject of debate. The widespread belief is that higherdose
radiation increased the expression of CYP1A1 and CYP1B1 of rat, zebrafish or human, CYP1A2, CYP2B1, and
CYP3A1 of rat, and CYP2E1 of mouse or rat, and decreased that of rat’s CYP2C11 and CYP2D1. Radiation increased
the expression of multidrug resistance protein, multidrug resistance-associated protein, and breast cancer
resistance protein. The metabolism of some drugs, as well as the clearance, increased during concurrent chemoradiation
therapy, whereas the half-life, mean residence time, and area under the curve decreased. Changes in the expression
of cytochrome P450 and drug transporters were consistent with the changes in the pharmacokinetics of some
drugs under radiation.
Conclusion: The findings of this review indicated that radiation caused by environmental pollution or clinical treatments
can alter the pharmacokinetic characteristics of drugs. Thus, the pharmacokinetics of drugs should be rechecked
and the optimal dose should be re-evaluated after radiation.