Multicenter study to assess the efficacy and tolerability of lovastatin, an HMG-CoA reductase inhibitor, in patients with primary hypercholesterolemia

An open-label multicenter trial was carried out to assess the efficacy and tolerability of lovastatin, an inhibitor of HMG-CoA reductase, in 101 patients with primary hypercholesterolemia (total cholesterol [TC] ≥250 mg/dl, triglycerides [TG] ≤350 mg/dl). After a four-week washout period, patients were treated for 12 weeks with a cholesterol-lowering diet, followed by another four-week period of cholesterol-lowering diet plus placebo. Patients received 20 or 40 mg of lovastatin, depending on TC level (greater or less than 300 mg/dl). The dose could be increased later, up to 80 mg daily, if TC did not fall below 200 mg/dl. At baseline and at weeks 4, 8, and 12, TC, TG, low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C), as well as safety, laboratory variables were determined. An efficacy-tolerability index was used to assess the overall clinical usefulness of the drug. A total score was calculated from specific scoring systems for efficacy, adverse changes in laboratory values, and side effects. Patients were allocated into one of the following five groups according to their total scores: very good, good, regular, poor, or very poor results. At week 12, TC fell 33.6%; TG, 21%; LDL-C, 42%; HDL-C increased 4%; and the atherogenic index LDH/HDL decreased 50%. An abnormal raise in creatine phosphokinase was observed in 8% of patients. Collateral symptoms occurred in 10%. Only one patient dropped out, because of constipation. Eighty-seven percent of patients had efficacy-tolerance scores indicating good or very good results. This study supports the efficacy and good tolerability of lovastatin in patients with primary hypercholesterolemia.