HMG-CoA reductase inhibitors have been used for a decade to lower LDL cholesterol levels and to improve cardiovascular diseases and clinical outcomes. This study was designed to evaluate the clinical efficacy and safety profiles of atorvastatin, a new HMG-CoA reductase inhibitor, in patients with elevated LDL-cholesterolemia.

Eighty three patients who had high 12-hour fasting serum LDL-cholesterol level (≥145 mg/dl and ≤ 250 mg/dl) and serum TG level less than 400 mg/dl were enrolled. After completing an 4 week dietary phase, 50 patients who still had LDL-C ≥145 mg/dl and TG ≤400 mg/dl were assigned to receive atorvastatin 10 mg once daily for 4 weeks. After 4 weeks, the dose was continued for 4 weeks in each individual if serum LDL-cholesterol was maintained below 130 mg/dL. For each individual whose serum LDL-cholesterol was above 130 mg/dL, the dose was doubled (20 mg/day) and administered for 4 weeks. Serum AST, ALT and CPK were also measured in addition to blood chemistry tests for lipid profiles at 4 and 8 weeks for safety assessment.

1) The total study population who completed the whole protocol was composed of 46 patients (23 male, 23 female, mean age 54 years). 2) At 4 weeks, the reduction by mean percent change from the baseline in LDL-cholesterol was -44.8% (from 182.3±3.4 mg/dl to 99.7±2.9 mg/dl). The fixed goal of LDL-cholesterol less than 130 mg/dl was achieved by 95.8%. 3) At 4 weeks, the mean percent change from the baseline in TC, TG, HDL-C, LDL/HDL-C and ApoB were -32.3%, -17.4%, +9.6%, -48.5% and -36.6%, respectively. 4) At 8 weeks, the mean percent change from the baseline in LDL-cholesterol was -43.0% (from 182.3±3.4 mg/dl to 103±2.4 mg/dl). The fixed goal of LDL-cholesterol less than 130 mg/dl was achieved by 91.3% of the whole patients. 5) At 8 weeks, the mean percent change from the baseline in TC, TG, HDL-C, LDL/HDL-C and ApoB were -31.3%, -22.6%, +13.7%, -48.8% and -35.9%, respectively. 6) No serious side effects were observed during the whole period.

Atorvastatin is highly effective and safe in modulating lipid profiles favorably (lower LDL-Cholesterol, lower TG, elevate HDL-Cholesterol), in patients with serum lipid abnormality.