Hyperbilirubinemia may accompany harmful effects such as jaundice, brain 
dysfunction, and pharmacokinetic alterations of drugs. Clinical drugs are the 
important causes of hyperbilirubinemia, especially for patients with certain 
pathologic conditions or with genetic variations. This article reviews 
hyperbilirubinemic pathophysiology with respect to the effects of clinical 
drugs. In addition, this review introduces a new formula that may be utilized to 
estimate the annual occurrences of drug-induced hyperbilirubinemia in a 
hospital. Variations in the genes of UDP-glucuronosyltransferases, organic 
anion-transporting polypeptides and multidrug resistance proteins are the 
predisposing factors for drug-induced hyperbilirubinemia; therefore, their 
genetic and ethnic polymorphisms are discussed.