THE EFFECTS OF COLESTIPOL TABLETS COMPARED WITH COLESTIPOL GRANULES ON PLASMA-CHOLESTEROL AND OTHER LIPIDS IN MODERATELY HYPERCHOLESTEROLEMIC PATIENTS

The purpose of this study was to investigate and compare the efficacy, safety, and patient acceptability of a new formulation of colestipol, colestipol tablets (T), with those of colestipol granules (G), in a r andomized, double-blind, placebo-controlled, multicenter study, Three hundred and seventeen patients with primary hypercholesterolemia who w ere following a low-fat, low-cholesterol diet (NCEP Step I diet), and had low-density lipoprotein cholesterol (LDL-C) levels greater than or equal to 4.14 mmol/l(160 mg/dl) and less than or equal to 6.46 mmol/l (250 mg/dl) were studied. Study medication was taken twice a day, wit h breakfast and supper, for 8 weeks. The six parallel treatment groups consisted of colestipol tablets 2 g b.i.d. and 8 g b.i.d., matching p lacebo tablets b.i.d., colestipol granules 2 g b.i.d. and 8 g b.i.d., and matching placebo granules b.i.d.. Study endpoints included absolut e change and percentage change from baseline in selected lipid, lipopr otein, and apolipoprotein measurements; LDL-C lowering was the primary efficacy endpoint. Treatment with colestipol tablets and colestipol g ranules resulted in virtually identical, statistically significant (P less than or equal to 0.05) reductions of LDL-C, total cholesterol (TC ), TC/HDL-C, and apolipoprotein B (ape B). Compared with placebo, all active treatments (tablets 4 g/day, tablets 16 g/day, granules 4 g/day , granules 16 g/day) significantly reduced LDL-C (12%, 24%, 12%, 25%, respectively), TC(7%, 15%, 8%, 15%, respectively), TC/HDL-C (8%, 14%, 9%, 15%, respectively) and apo B (12%, 20%, 13%, 22%, respectively). A ll active treatments significantly increased lipoprotein particle AI(L pAI) (5%, 23%, 14%, 18%, respectively). VLDL-C and triglycerides incre ased significantly in the high-dose groups. The proportions of patient s reporting adverse events, largely gastrointestinal-related, were not different among the active treatment groups. The treatments were well -tolerated, and no drug-related serious adverse events were reported. Patients experienced with granule medication prior to this study prefe rred tablets over granules. This study demonstrates that colestipol ta blets are an effective treatment to reduce LDL-C in patients with prim ary hypercholesterolemia, are equivalent to colestipol granules, are w ell-tolerated, and are preferred over granules by patients..