Alpha-methyldopa-induced liver injury was studied in six patients by clinical, biochemical, histologic, and morphometric methods. The patients, all women, developed hepatic injury after long-term therapy lasting 2 to 8 years. Withdrawal of the drug resulted in improvement of the symptoms. Hepatitis with fibrosis and moderate to severe fatty accumulation was seen in most of the liver biopsies at onset of symptoms. Follow-up ranged from 7 to 24.5 months, at the end of which the liver function test results were in the normal range. A second liver biopsy showed significant decrease in fatty infiltration. Three patients showed a decrease in lipid content from moderate to mild or normal and two other patients from severe to moderate. A 73-year-old patient had chronic aggressive hepatitis with massive necrosis of the parenchyma after 8 years of therapy, and follow-up biopsy 12 months later showed cirrhosis. In this study alpha-methyldopa withdrawal resulted in a reduction of lipid and fibrous trabeculae content, possibly caused by alpha-methyldopa-induced derangement of liver function.