Colestipol

Since no drug is innocuous, strict attention should be paid to the indications and contraindications, particularly when selecting drugs for chronic long-term use. Colestipol hydrochloride granules are indicated as adjunctive therapy to diet for the reduction of elevated serum total and low-density lipoprotein (LDL) cholesterol in patients with primary hypercholesterolemia (elevated low density lipoproteins [LDL] cholesterol) who do not respond adequately to diet. Generally, colestipol hydrochloride granules have no clinically significant effect on serum triglycerides, but with its use triglyceride levels may be raised in some patients. Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia.

and an effect on serum cholesterol similar to that of colestipol hydrochloride, had reductions in total and low-density lipoprotein cholesterol (LDL-C). Over the seven-year study period the cholestyramine group experienced a 19% reduction (relative to the incidence in the placebo group) in the combined rate of coronary heart disease death plus non-fatal myocardial infarction (cumulative incidences of 7% cholestyramine and 8.6%, placebo). The subjects included in the study were middle-aged men (age 35–59) with serum cholesterol-levels above 265 mg/dL, LDL-C above 175 mg/dL on a moderate cholesterol-lowering diet, and no history of heart disease. It is not clear to what extent these findings can be extrapolated to other segments of the hypercholesterolemic population not studied. Treatment with colestipol hydrochloride results in a significant increase in lipoprotein LpAI.

One dose (1 packet or 1 level teaspoon) of colestipol hydrochloride granules contains 5 grams of colestipol hydrochloride. The recommended daily adult dose is one to six packets or level scoopfuls given once or in divided doses. Treatment should be started with one dose once or twice daily with an increment of one dose/day at one- or two-month intervals. Appropriate use of lipid profiles as per NCEP guidelines including LDL-cholesterol and triglycerides is advised so that optimal, but not excessive doses are used to obtain the desired therapeutic effect on LDL-cholesterol level. If the desired therapeutic effect is not obtained at one to six doses/day with good compliance and acceptable side effects, combined therapy or alternate treatment should be considered. To avoid accidental inhalation or esophageal distress, colestipol hydrochloride granules should not be taken in its dry form.

Colestipol hydrochloride granules are contraindicated in those individuals who have shown hypersensitivity to any of its components.

TO AVOID ACCIDENTAL INHALATION OR ESOPHAGEAL DISTRESS, COLESTIPOL HYDROCHLORIDE GRANULES SHOULD NOT BE TAKEN IN ITS DRY FORM. ALWAYS MIX COLESTIPOL HYDROCHLORIDE GRANULES WITH WATER OR OTHER FLUIDS BEFORE INGESTING.

Gastrointestinal The most common adverse reactions are confined to the gastrointestinal tract. To achieve minimal GI disturbance with an optimal LDL-cholesterol lowering effect, a gradual increase of dosage starting with one dose/day is recommended. Constipation is the major single complaint and at times is severe. Most instances of constipation are mild, transient, and controlled with standard treatment. Increased fluid intake and inclusion of additional dietary fiber should be the first step, a stool softener may be added if needed. Some patients require decreased dosage or discontinuation of therapy. Hemorrhoids may be aggravated. Other, less frequent gastrointestinal complaints consist of abdominal discomfort (abdominal pain and cramping), intestinal gas, (bloating and flatulence), indigestion and heartburn, diarrhea and loose stools, and nausea and vomiting.

Since colestipol hydrochloride is an anion exchange resin, it may have a strong affinity for anions other than the bile acids. In vitro studies have indicated that colestipol hydrochloride binds a number of drugs. Therefore, colestipol hydrochloride granules resin may delay or reduce the absorption of concomitant oral medication. The interval between the administration of colestipol hydrochloride granules and any other medication should be as long as possible. Patients should take other drugs at least one hour before or four hours after colestipol hydrochloride granules to avoid impeding their absorption. Repeated doses of colestipol hydrochloride given prior to a single dose of propranolol in human trials have been reported to decrease propranolol absorption.

Store at controlled room temperature 20° to 25° C (68° to 77° F).