OBJECTIVES: Pharmaceutical treatment of hypercholesterolemia is recommended in individuals with a LDL-cholesterol level of ≥190 mg/dl and 130-189 mg/dl plus two other coronary heart disease risk factors or a coronary heart disease risk >20 % in ten years. The objective of this study was to assess the cost-effectiveness of pharmaceutical treatments of hypercholesterolemia in Catalonia, Spain. METHODS: Treatments evaluated included 20, 40, and 80 mg/day of lovastatin and fluvastatin, 10, 20, and 40 mg/day of pravastatin, simvastatin and atorvastatin, 12 and 24 g/day of cholestyramine, and 1.2 g/day of gemfibrozil. The cost-effectiveness was evaluated comparing annual treatment costs and the percentage of LDL-cholesterol reduction. Treatment costs included medication, medical visits control measures, and treatment of secondary adverse effects. Wholesale prices in 2002 were used to estimate medication costs. A metanalysis was carried out to estimate effectiveness of different treatments, including all published randomized, double blind clinical trials referred on Medline from 1991 to 2002. RESULTS: The annual cost of medication ranged from 332.98€ for 20 mg/day lovastatin to 1105.17€ for 40 mg/day atorvastatin. The percentage of LDL-cholesterol reduction ranged from 10 % for 12 g/day cholestyramine to 49 % for 80 mg/day atorvastatin. The average cost-effectiveness ratios in terms of € per one per cent of LDL-cholesterol reduced were 11.22€-22.55€ for atorvastatin, 12.00-21.96€ for simvastatin, 13.87-21.64€ for lovastatin, 15.24-24.69€ for fluvastatin, 20.96-41.77€ for pravastatin, 32.61€ for gemfibrozil, and 35.21-45.55€ for cholestyramine. The incremental cost-effectiveness analysis showed that the more efficient cholesterol-lowering therapies were 10 mg/day atorvastatin, 10 mg/day simvastatin, 20 mg/day lovastatin, 20 mg/day fluvastatin, and 20, 40 and 80 mg/day atorvastatin. CONCLUSIONS: Efficient statin therapies detected in this study should be the first election cholesterol-lowering drugs used in patients with hypercholesterolemia in Catalonia.