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The administration of antimicrobial drugs by the intramammary route offers a convenient option for the treatment of bovine mastitis. The goal of antimicrobial treatment is to achieve effective drug concentrations at the site of infection. Drug concentrations must also decrease to safe levels before the milk is harvested for human consumption. The rate of change of drug concentrations in the milk and udder tissues over time is dependent on the physicochemical characteristics of the drug and how these interact with the biological environment, affecting the rate and extent of absorption, distribution and elimination. Studies reported in the literature have identified various pathophysiological and pharmaceutical factors that may influence these processes. This review summarizes current understanding of factors affecting the disposition of drugs following intramammary administration. Areas of incomplete knowledge requiring …