The development of drugs able to prevent and cure bacterial infections is one of the 20th century's major contributions to human longevity and quality of life. Antibacterial agents are among the most commonly prescribed drugs of any kind worldwide. Used appropriately, these drugs are lifesaving. To eliminate an infection as rapidly as possible, a sufficient concentration of the drug(s) chosen must reach the site of infection. Serum/tissue concentration is a result of various parameters such as absorption, excretion, protein binding and metabolic inactivation. Biliary excretion is an important route for the elimination of some drugs and drug metabolites in humans. Thus, drugs with a high bile concentration are indicated for the treatment of gallbladder infectious diseases. We present a review of a large number of antimicrobial agents most commonly used in daily clinical practice, with regard to their biliary excretion.