cholestyramine

INDICATIONS AND USAGE 1) Cholestyramine for oral suspension USP light powder, 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 USP light powder 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 USP light powder 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 ( 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 USP light powder 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 USP light powder 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 USP light powder or adding other lipid-lowering agents in combination with cholestyramine for oral suspension USP light powder 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 premature menopause without estrogen replacement therapy); family history of premature CHD; current cigarette smoking; hypertension; confirmed HDL-C < 35 mg/dL (< 0.91 mmol/L); and diabetes mellitus. Subtract one risk factor if HDL-C is ≥ 60 mg/dL (≥ 1.6 mmol/L). LDL - Cholesterol mg / dL ( mmol / L ) Definite Atherosclerotic Disease * Two or More Other Risk Factors ** Initiation Level Goal NO NO ≥ 190 (≥ 4.9) < 160 (< 4.1) NO YES ≥ 160 (≥ 4.1) < 130 (< 3.4) YES YES OR NO ≥ 130 (≥ 3.4) ≤ 100 ( ≤ 2.6) Cholestyramine for oral suspension USP light powder monotherapy has been demonstrated to retard the rate of progression 2,3 and increase the rate of regression 3 of coronary atherosclerosis. 2) Cholestyramine for oral suspension USP light powder is indicated for the relief of pruritus associated with partial biliary obstruction. Cholestyramine for oral suspension USP light powder has been shown to have a variable effect on serum cholesterol in these patients. Patients with primary biliary cirrhosis …

DOSAGE AND ADMINISTRATION The recommended starting adult dose for cholestyramine for oral suspension USP light powder is one pouch or one level scoopful once or twice a day. The recommended maintenance dose for cholestyramine for oral suspension USP light powder 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 USP light powder as follows: Cholestyramine for oral suspension USP light powder 5.5 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 pouches or scoopfuls of cholestyramine for oral suspension USP light powder (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 USP light powder may be administered in 1 to 6 doses per day. Cholestyramine for oral suspension USP light powder should not be taken in its dry form. Always mix cholestyramine for oral suspension USP light powder 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 USP light powder 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 USP light powder therapy. See the Drug Interactions subsection of the PRECAUTIONS section for recommendations on administering concomitant therapy. PREPARATION The color of cholestyramine for oral suspension USP light powder 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 USP light powder in a glass or cup. Add an amount of water or other non-carbonated beverage of your choice depending on the product being used: Product Formula Amount of Water or other Non - Carbonated Liquid Cholestyramine for oral suspension USP light powder 2 to 6 ounces per dose Stir to a uniform consistency and drink. Cholestyramine for oral suspension USP light powder may also be mixed with highly fluid soups or pulpy fruits with a high moisture content such as applesauce or crushed pineapple.

CONTRAINDICATIONS Cholestyramine for oral suspension USP light powder 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.

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 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 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. To report SUSPECTED ADVERSE REACTIONS, contact Micro Labs USA Inc., at 1-855-839-8195 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Drug Interactions Cholestyramine for oral suspension 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 resin may interfere with the pharmacokinetics of drugs that undergo enterohepatic circulation. The discontinuance of cholestyramine resin 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 resin. Because cholestyramine binds bile acids, cholestyramine resin 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 resin is given for long periods of time, concomitant supplementation with water-miscible (or parenteral) forms of fat-soluble vitamins should be considered. SINCE CHOLESTYRAMINE RESIN 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 RESIN (OR AT AS GREAT AN INTERVAL AS POSSIBLE) TO AVOID IMPEDING THEIR ABSORPTION.

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 is not absorbed from the digestive tract. Four grams of anhydrous cholestyramine resin is contained in 9 grams of Cholestyramine for Oral Suspension USP. Four grams of anhydrous cholestyramine resin is contained in 5 grams of Cholestyramine for Oral Suspension USP, Light. It is represented by the following structural formula: Cholestyramine for Oral Suspension USP contains the following inactive ingredients: acacia, citric acid, D&C Yellow No. 10, FD&C Yellow No. 6, flavor (natural and artificial Orange), polysorbate 80, propylene glycol alginate and sucrose. Cholestyramine for Oral Suspension USP, Light contains the following inactive ingredients: aspartame, citric acid, colloidal silicon dioxide, D&C Yellow No. 10, FD&C Red No. 40, flavor (natural and artificial Orange), maltodextrin, propylene glycol alginate and xanthan gum. cholestrymine

OVERDOSAGE Overdosage with cholestyramine for oral suspension USP light powder 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 Cholestyramine for Oral Suspension USP is a yellow colored orange flavored powder available in HDPE Bottles containing 378 grams and in cartons of sixty 9 gram packets. Four grams of anhydrous cholestyramine resin are contained in 9 grams of Cholestyramine for Oral Suspension USP. The 378 g HDPE Bottle includes a 15 cc scoop. The scoop is not interchangeable with scoops from other products. NDC 49884-465-51 HDPE Bottle, 378 g NDC 49884-465-65 Carton of 60, 9 g packets Cholestyramine for Oral Suspension USP, Light is a cream to pale yellow colored orange flavored powder available in HDPE Bottles containing 210 grams and in cartons of sixty 5 gram packets. Four grams of anhydrous cholestyramine resin are contained in 5 grams of Cholestyramine for Oral Suspension USP, Light. The 210 g HDPE Bottle includes a 9 cc scoop. The scoop is not interchangeable with scoops from other products. NDC 49884-466-50 HDPE Bottle, 210 g NDC 49884-466-65 Carton of 60, 5 g packets Storage Store between 20o to 25oC (68o to 77oF). [See USP Controlled Room Temperature]. Excursions permitted to 15o to 30oC (59o to 86oF).