Cholestyramine
FDA Drug Information • Also known as: Cholestyramine, Cholestyramine Light, Prevalite, Questran
- Brand Names
- Cholestyramine, Cholestyramine Light, Prevalite, Questran
- Drug Class
- Bile Acid Sequestrant [EPC]
- Route
- ORAL
- Dosage Form
- POWDER, FOR SUSPENSION
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
DESCRIPTION Cholestyramine for oral suspension USP, the chloride salt of a basic anion exchange resin, a cholesterol lowering agent, is intended for oral administration. Cholestyramine resin is quite hydrophilic, but insoluble in water. The cholestyramine resin in cholestyramine for oral suspension, USP is not absorbed from the digestive tract. Four grams of anhydrous cholestyramine resin is contained in 9 grams of cholestyramine for oral suspension, USP. It is represented by the following structural formula: Cholestyramine for oral suspension, USP contains the following inactive ingredients: citric acid, d & c yellow # 10 aluminum lake, flavor (natural and artificial orange, natural and artificial vanilla), fd & c yellow # 6 aluminum lake, propylene glycol alginate, sucrose and xanthan gum. Formula
What Is Cholestyramine Used For?
INDICATIONS AND USAGE 1) Cholestyramine for oral suspension is indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet. Cholestyramine for oral suspension may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormality of most concern. 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. Treatment should begin and continue with dietary therapy specific for the type of hyperlipoproteinemia determined prior to initiation of drug therapy. Excess body weight may be an important factor and caloric restriction for weight normalization should be addressed prior to drug therapy in the overweight. Prior to initiating therapy with cholestyramine for oral suspension secondary causes of hypercholesterolemia (e.g., poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease, other drug therapy, alcoholism), should be excluded, and a lipid profile performed to assess Total cholesterol, HDL-C, and triglycerides (TG). For individuals with TG less than 400 mg/dL (< 4.5 mmol/L), LDL-C can be estimated using the following equation:- LDL-C = Total cholesterol – [(TG/5) + HDL-C] For TG levels > 400 mg/dL, this equation is less accurate and LDL-C concentrations should be determined by ultracentrifugation. In hypertriglyceridemic patients, LDL-C may be low or normal despite elevated Total-C. In such cases cholestyramine for oral suspension may not be indicated. Serum cholesterol and triglyceride levels should be determined periodically based on NCEP guidelines to confirm initial and adequate long-term response. A favorable trend in cholesterol reduction should occur during the first month of cholestyramine for oral suspension therapy. The therapy should be continued to sustain cholesterol reduction. If adequate cholesterol reduction is not attained, increasing the dosage of cholestyramine for oral suspension or adding other lipid-lowering agents in combination with cholestyramine for oral suspension should be considered. Since the goal of treatment is to lower LDL-C, the NCEP 4 recommends that LDL-C levels be used to initiate and assess treatment response. If LDL-C levels are not available then Total-C alone may be used to monitor long-term therapy. A lipoprotein analysis (including LDL-C determination) should be carried out once a year. The NCEP treatment guidelines are summarized below. * Coronary heart disease or peripheral vascular disease (including symptomatic carotid artery disease). ** Other risk factors for coronary heart disease (CHD) include: age (males ≥ 45 years; females ≥ 55 years or...
Dosage and Administration
DOSAGE AND ADMINISTRATION The recommended starting adult dose for cholestyramine for oral suspension is one pouch or one level scoopful once or twice a day. The recommended maintenance dose for cholestyramine for oral suspension is 2 to 4 pouches or scoopfuls daily (8 to 16 grams anhydrous cholestyramine resin) divided into two doses. Four grams of anhydrous cholestyramine resin is contained in each measured dose of cholestyramine for oral suspension as follows: Cholestyramine for oral suspension 9 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 pouches 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 to 6 doses per day. Cholestyramine for oral suspension should not be taken in its dry form. Always mix cholestyramine for oral suspension with water or other fluids before ingesting. See Preparation Instructions. Concomitant Therapy Preliminary evidence suggests that the lipid-lowering effects of cholestyramine for oral suspension on total and LDL-cholesterol are enhanced when combined with a HMG-CoA reductase inhibitor, e.g., pravastatin, lovastatin, simvastatin, and fluvastatin. Additive effects on LDL-cholesterol are also seen with combined nicotinic acid /cholestyramine for oral suspension therapy. See the Drug Interactions subsection of the PRECAUTIONS section for recommendations on administering concomitant therapy. PREPARATION The color of cholestyramine for oral suspension may vary somewhat from batch to batch but this variation does not affect the performance of the product. Place the contents of one single-dose pouch or one level scoopful of cholestyramine for oral suspension in a glass or cup. Add an amount of water or other noncarbonated beverage of your choice depending on the product being used: Product Formula Amount of Water or other Non-Carbonated Liquid Cholestyramine for oral suspension 2 to 6 ounces per dose Stir to a uniform consistency and drink. Cholestyramine for oral suspension may also be mixed with highly fluid soups or pulpy fruits with a high moisture content such as applesauce or crushed pineapple.
Side Effects (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 for oral suspension 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 for oral suspension. 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 for oral suspension 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.
Contraindications
CONTRAINDICATIONS Cholestyramine for oral suspension is contraindicated in patients with complete biliary obstruction where bile is not secreted into the intestine and in those individuals who have shown hypersensitivity to any of its components.
Overdosage
OVERDOSAGE Overdosage with cholestyramine for oral suspension 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.
How Supplied
HOW SUPPLIED Cholestyramine for Oral Suspension, USP is available in cans containing 378 grams and in cartons of sixty 9 gram pouches. Four grams of anhydrous cholestyramine resin are contained in 9 grams of cholestyramine for oral suspension, USP. The 378 grams can includes a 15 cc scoop. The scoop is not interchangeable with scoops from other products. NDC 70771-1105-1 Can, 378 grams NDC 70771-1105-2 Carton of 60, 9 grams pouches Storage Store between 20 to 25 C (68 to 77 F). [See USP Controlled Room Temperature]. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.