CHOLESTYRAMINE (Page 2 of 4)

Information for Patients

Inform your physician if you are pregnant or plan to become pregnant or are breastfeeding. Drink plenty of fluids and mix each 9 gram dose of Cholestyramine for Oral Suspension USP in at least 2 to 6 ounces of fluid. Mix each 5 gram dose of Cholestyramine for Oral Suspension USP, Light in at least 2 to 6 ounces of fluid before taking. Sipping or holding the resin suspension in the mouth for prolonged periods may lead to changes in the surface of the teeth resulting in discoloration, erosion of enamel or decay; good oral hygiene should be maintained.

Laboratory Tests

Serum cholesterol levels should be determined frequently during the first few months of therapy and periodically thereafter. Serum triglyceride levels should be measured periodically to detect whether significant changes have occurred.

The LRC-CPPT showed a dose-related increase in serum triglycerides of 10.7%–17.1% in the cholestyramine-treated group, compared with an increase of 7.9%–11.7% in the placebo group. Based on the mean values and adjusting for the placebo group, the cholestyramine-treated group showed an increase of 5% over pre-entry levels the first year of the study and an increase of 4.3% the seventh year.

Drug Interactions

Cholestyramine for Oral Suspension USP may delay or reduce the absorption of concomitant oral medication such as phenylbutazone, warfarin, thiazide diuretics (acidic), or propranolol (basic), as well as tetracycline, penicillin G, phenobarbital, thyroid and thyroxine preparations, estrogens and progestins, and digitalis. Interference with the absorption of oral phosphate supplements has been observed with another positively-charged bile acid sequestrant. Cholestyramine may interfere with the pharmacokinetics of drugs that undergo enterohepatic circulation. The discontinuance of Cholestyramine could pose a hazard to health if a potentially toxic drug such as digitalis has been titrated to a maintenance level while the patient was taking Cholestyramine.

Because cholestyramine binds bile acids, Cholestyramine may interfere with normal fat digestion and absorption and thus may prevent absorption of fat-soluble vitamins such as A, D, E and K. When Cholestyramine is given for long periods of time, concomitant supplementation with water-miscible (or parenteral) forms of fat-soluble vitamins should be considered.

SINCE CHOLESTYRAMINE MAY BIND OTHER DRUGS GIVEN CONCURRENTLY, IT IS RECOMMENDED THAT PATIENTS TAKE OTHER DRUGS AT LEAST ONE HOUR BEFORE OR 4 TO 6 HOURS AFTER CHOLESTYRAMINE (OR AT AS GREAT AN INTERVAL AS POSSIBLE) TO AVOID IMPEDING THEIR ABSORPTION.

Carcinogenesis and Mutagenesis and Impairment of Fertility

In studies conducted in rats in which cholestyramine resin was used as a tool to investigate the role of various intestinal factors, such as fat, bile salts and microbial flora, in the development of intestinal tumors induced by potent carcinogens, the incidence of such tumors was observed to be greater in cholestyramine resin-treated rats than in control rats.

The relevance of this laboratory observation from studies in rats to the clinical use of Cholestyramine is not known. In the LRC-CPPT study referred to above, the total incidence of fatal and nonfatal neoplasms was similar in both treatment groups. When the many different categories of tumors are examined, various alimentary system cancers were somewhat more prevalent in the cholestyramine group. The small numbers and the multiple categories prevent conclusions from being drawn. However, in view of the fact that cholestyramine resin is confined to the GI tract and not absorbed, and in light of the animal experiments referred to above, a six-year post-trial follow-up of the LRC-CPPT 5 patient population has been completed (a total of 13.4 years of in-trial plus post-trial follow-up) and revealed no significant difference in the incidence of cause-specific mortality or cancer morbidity between cholestyramine and placebo treated patients.

Pregnancy

Pregnancy Category C

There are no adequate and well controlled studies in pregnant women. The use of Cholestyramine in pregnancy or lactation or by women of childbearing age requires that the potential benefits of drug therapy be weighed against the possible hazards to the mother and child. Cholestyramine is not absorbed systemically, however, it is known to interfere with absorption of fat-soluble vitamins; accordingly, regular prenatal supplementation may not be adequate (see PRECAUTIONS: Drug Interactions).

Nursing Mothers

Caution should be exercised when Cholestyramine is administered to a nursing mother. The possible lack of proper vitamin absorption described in the “Pregnancy”section

Pediatric Use

Although an optimal dosage schedule has not been established, standard texts (6,7) list a usual pediatric dose of 240 mg/kg/day of anhydrous cholestyramine resin in two to three divided doses, normally not to exceed 8 gm/day with dose titration based on response and tolerance.

In calculating pediatric dosages, 44.4 mg of anhydrous cholestyramine resin are contained in 100 mg of Cholestyramine for Oral Suspension USP and 80 mg of anhydrous cholestyramine resin are contained in 100 mg of Cholestyramine for Oral Suspension USP, Light.

The effects of long-term administration, as well as its effect in maintaining lowered cholesterol levels in pediatric patients, are unknown. (Also see ADVERSE REACTIONS.)

ADVERSE REACTIONS

The most common adverse reaction is constipation. When used as a cholesterol-lowering agent predisposing factors for most complaints of constipation are high dose and increased age (more than 60 years old). Most instances of constipation are mild, transient, and controlled with conventional therapy. Some patients require a temporary decrease in dosage or discontinuation of therapy.

Less Frequent Adverse Reactions: Abdominal discomfort and/or pain, flatulence, nausea, vomiting, diarrhea, eructation, anorexia, and steatorrhea, bleeding tendencies due to hypoprothrombinemia (Vitamin K deficiency) as well as Vitamin A (one case of night blindness reported) and D deficiencies, hyperchloremic acidosis in children, osteoporosis, rash and irritation of the skin, tongue and perianal area. Rare reports of intestinal obstruction, including two deaths, have been reported in pediatric patients.

Occasional calcified material has been observed in the biliary tree, including calcification of the gallbladder, in patients to whom cholestyramine resin has been given. However, this may be a manifestation of the liver disease and not drug related.

One patient experienced biliary colic on each of three occasions on which he took cholestyramine resin. One patient diagnosed as acute abdominal symptom complex was found to have a “pasty mass” in the transverse colon on x-ray.

Other events (not necessarily drug related) reported in patients taking cholestyramine resin include:

Gastrointestinal—GI-rectal bleeding, black stools, hemorrhoidal bleeding, bleeding from known duodenal ulcer, dysphagia, hiccups, ulcer attack, sour taste, pancreatitis, rectal pain, diverticulitis.

Laboratory test changes—Liver function abnormalities.

Hematologic—Prolonged prothrombin time, ecchymosis, anemia

Hypersensitivity—Urticaria, asthma, wheezing, shortness of breath.

Musculoskeletal—Backache, muscle and joint pains, arthritis.

Neurologic—Headache, anxiety, vertigo, dizziness, fatigue, tinnitus, syncope, drowsiness, femoral nerve pain, paresthesia.

Eye—Uveitis.

Renal—Hematuria, dysuria, burnt odor to urine, diuresis.

Miscellaneous—Weight loss, weight gain, increased libido, swollen glands, edema, dental bleeding, dental caries, erosion of tooth enamel, tooth discoloration.

OVERDOSAGE

Overdosage with Cholestyramine has been reported in a patient taking 150% of the maximum recommended daily dosage for a period of several weeks. No ill effects were reported. Should an overdosage occur, the chief potential harm would be obstruction of the gastrointestinal tract. The location of such potential obstruction, the degree of obstruction, and the presence or absence of normal gut motility would determine treatment.

DOSAGE AND ADMINISTRATION

The recommended starting adult dose for all cholestyramine for oral suspension powdered products (Cholestyramine for Oral Suspension USP and Cholestyramine for Oral Suspension USP, Light) is one packet or one level scoopful once or twice a day. The recommended maintenance dose for all cholestyramine for oral suspension powdered products is 2 to 4 packets or scoopfuls daily (8-16 grams anhydrous cholestyramine resin) divided into two doses. Four grams of anhydrous cholestyramine resin is contained in each measured dose of Cholestyramine as follows:

Cholestyramine for Oral Suspension USP 9 grams
Cholestyramine for Oral Suspension USP, Light 5 grams

It is recommended that increases in dose be gradual with periodic assessment of lipid/lipoprotein levels at intervals of not less than 4 weeks. The maximum recommended daily dose is six packets or scoopfuls of cholestyramine for oral suspension (24 grams of anhydrous cholestyramine resin). The suggested time of administration is at mealtime but may be modified to avoid interference with absorption of other medications. Although the recommended dosing schedule is twice daily, cholestyramine for oral suspension may be administered in 1–6 doses per day.

Cholestyramine should not be taken in its dry form. Always mix Cholestyramine with water or other fluids before ingesting. See Preparation Instructions.

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