Drug-induced cholestasis manifests as an acute self-limiting injury or as a chronic perpetuating injury, resulting in duct loss and cirrhosis. The number of drugs implicated in drug-induced cholestasis grows every year as new drugs are developed and approved. Other agents such as herbals, nutritional supplements, and complementary and alternative medicines are also reported to cause cholestatic liver injury. Recent literature on molecular transporters involved in bile transport has improved our understanding of patterns of drug-induced liver injury and the mechanisms of cholestasis. This article summarizes the probable offending drugs, and the diagnosis and management of drug-induced cholestasis.