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Drugs that affect bilirubin metabolism
Last reviewed: 04.07.2025
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Medicines can affect any stage of bilirubin metabolism. Such reactions are predictable, reversible, and mild in adults. However, in newborns, increased levels of unconjugated bilirubin in the brain can lead to bilirubin encephalopathy (kernicterus). It is aggravated by drugs such as salicylates or sulfonamides, which compete with bilirubin for binding sites on albumin. In adults with Gilbert's syndrome, chronic active hepatitis, or primary biliary cirrhosis (PBC), drugs that affect bilirubin metabolism increase bilirubinemia.
The bilirubin load on liver cells increases with hemolytic drug reactions. Hemolysis is usually associated with allergic reactions that impair liver cell function. Such reactions may be observed with treatment with sulfonamides, phenacetin, and quinine. These drugs may also cause hemolysis in individuals with G6PD deficiency.
Reactions may develop to drugs that enter the mother's milk. Toxic effects of synthetic vitamin K preparations in newborns may partly be a consequence of increased hemolysis.
Some drugs interfere with the uptake of bilirubin by the hepatocyte and its intracellular transport. These include contrast agents for cholecystography and rifampin. Newborns may have low levels of transport proteins, which causes sensitivity to drugs that compete with bilirubin for space on the transport protein. These drugs will increase kernicterus.
Drugs that affect the tubular excretion of bilirubin, such as sex hormones, can cause cholestasis.
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