The Effect of Cholestyramine on Serum Lipids in Hyperlipidemic Patients

Studies on Dose-Response and Safety

Abstract

Cholestyramine, an antihypercholesterolemic agent having a basic anion exchange characteristic, was studied for its effects on serum lipids and for its safety when administered to Type II hyperlipidemic patients at dose levels of either 8Gm per day (4Gm bid) or 12Gm per day (4Gm tid) for 8 consecutive weeks. A total number of patients treated was 44 consisting of 9 Type IIa receiving 8Gm per day, 19 Type IIa receiving 12Gm per day, 7 Type IIb receiving 8Gm per day, 6 Type IIb receiving 12Gm per day, and 3 who were excluded from the data analysis due to low pretherapy values of serum total cholesteol showing less than 220mg/dl.
An average pretherapy value of serum total cholesterol was 333.1mg/dl among the 41 patients analyzed indicating no significant difference between each Type of patients and dose groups. Cholestyramine was remarkably effective for reducing serum total cholesterol as shown by the Percent Reduction Through Therapy which was 15.0% in Type IIa, 16.3% in Type IIb and 15.4% in overall patients. Cholestyramine also demonstrated an excellent dose-response in non-familial Type IIa and Type IIb while it did not show a clear-cut response in familial Type ha which displayed a less percent reduction than did non-familial Type IIa. Data on other serum lipids indicated that triglyceride was not significantly altered whereas HDL-cholesterol had a tendency to increase.
Adverse reactions included constipation in 5 patients (11.4%) and diarrhea in 1 patient (2.3%). Two patients recovered from severe constipation when cholestyramine was withdrawn while the others were able to continue the therapy without interruption. A transient increases in GOT, GPT, CPK and LDH was seen in some patients with the values reversed to normal as the therapy continued. There were no abnormal values found in urine, hematology and serum biochemistry tests concurrently performed.
These data demonstrate that cholestyramine is highly effective in the treatment of severe hypercholesterolemia including familial hypercholesterolemia and is relatively free from serious adverse reactions.