P-glycoprotein (Pgp) is a membrane bound transporter involved in the disposition of many endogenous compounds and xenobiotics. Alterations in Pgp expression and activity can significantly affect the disposition of Pgp substrates. Infection and inflammatory stimuli have also been shown to alter drug disposition. However, the specific effects of inflammation on Pgp expression and activity are not well understood. This paper evaluates and summarizes the current literature on the effects of cytokines and inflammation on mRNA and protein expression as well as functional activity of Pgp in whole animal models, primary rodent hepatocytes and human carcinoma cell lines.