Comparative efficacy of once versus twice daily mevinolin in the therapy of familial hypercholesterolemia

Mevinolin, a competitive inhibitor of the rate‐limiting enzyme in cholesterol biosynthesis, is an effective hypocholesterolemic agent in patients with primary hypercholesterolemia when given in a twice‐daily regimen. The present study compares the hypocholesterolemic effects of mevinolin given in a twice‐daily dosage regimen with the same total dosage given either once in the morning or once in the evening in 12 patients with heterozygous familial hypercholesterolemia. Ten patients took a total daily dose of 40 mg of mevinolin and two took 20 mg. On the twice‐daily dosage regimen, plasma concentrations of total cholesterol decreased 29.5% and 35.9% as compared with 21.4% and 26.9% with mevinolin given once in the morning and 27% and 32.2% with the drug given once in the evening. These values are all significantly different from baseline, but differences between the three treatment regimens do not reach statistical significance (P = 0.07 for the twice‐daily versus once‐in‐the‐morning dosage regimens). We conclude that once‐daily administration of mevinolin, particularly in the evening, is an effective hypocholesterolemic regimen in patients with familial hypercholesterolemia. Clinical Pharmacology and Therapeutics (1986) 40, 338–343; doi: 10.1038/clpt.1986.185