Generic Name
Cholestyramine
Brand Names
Choleystyramine, Questran, Prevalite
FDA approval date: February 01, 1996
Classification: Bile Acid Sequestrant
Form: Powder
What is Choleystyramine (Cholestyramine)?
1) Prevalite ® powder is indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein cholesterol) who do not respond adequately to diet. Prevalite ® 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 resin, secondary causes of hypercholesterolemia , should be excluded and a lipid profile performed to assess Total Cholesterol, HDL-C and triglycerides . For individuals with TG less than 400 mg/dL.
Approved To Treat
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Brand Information
Choleystyramine Light (Choleystyramine Light)
1DESCRIPTION
Cholestyramine for Oral Suspension USP Light powder, 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. Cholestyramine resin is not absorbed from the digestive tract. Each 5.718 grams of Cholestyramine for Oral Suspension USP Light powder contain 4 grams of cholestyramine resin. It is represented by the following structural formula:
Representation of structure of main polymeric groups
Inactive Ingredients: mannitol, fructose, sorbitol, aspartame, citric acid, lake pigment 6010 D&C yellow #10 aluminum lake and FD&C yellow #6/sunset yellow FCF AI 15% - 18%, orange flavour, propylene glycol alginate, xanthan gum, pectin, silicon dioxide.
Inactive Ingredients: mannitol, fructose, sorbitol, aspartame, citric acid, lake pigment 6010 D&C yellow #10 aluminum lake and FD&C yellow #6/sunset yellow FCF AI 15% - 18%, orange flavour, propylene glycol alginate, xanthan gum, pectin, silicon dioxide.
2CLINICAL PHARMACOLOGY
Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum.
Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption.
The increased fecal loss of bile acids due to cholestyramine resin administration leads to an increased oxidation of cholesterol to bile acids, a decrease in beta lipoprotein or low density lipoprotein plasma levels and a decrease in serum cholesterol levels. Although in man, cholestyramine resin produces an increase in hepatic synthesis of cholesterol, plasma cholesterol levels fall.
In patients with partial biliary obstruction, the reduction of serum bile acid levels by cholestyramine resin reduces excess bile acids deposited in the dermal tissue with resultant decrease in pruritus.
Clinical Studies
In a large, placebo-controlled, multi-clinic study, LRC-CPPT1 , hypercholesterolemic subjects treated with cholestyramine resin had mean reductions in total and low-density lipoprotein cholesterol (LDL-C) which exceeded those for diet and placebo treatment by 7.2% and 10.4%, respectively. Over the seven year study period the cholestyramine resin 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 resin and 8.6% placebo). The subjects included in the study were men aged 35 to 59 with serum cholesterol levels above 265 mg/dL and no previous history of heart disease. It is not clear to what extent these findings can be extrapolated to females and other segments of the hypercholesterolemic population. (See also PRECAUTIONS, Carcinogenesis, Mutagenesis, Impairment of Fertility.)
In a large, placebo-controlled, multi-clinic study, LRC-CPPT1 , hypercholesterolemic subjects treated with cholestyramine resin had mean reductions in total and low-density lipoprotein cholesterol (LDL-C) which exceeded those for diet and placebo treatment by 7.2% and 10.4%, respectively. Over the seven year study period the cholestyramine resin 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 resin and 8.6% placebo). The subjects included in the study were men aged 35 to 59 with serum cholesterol levels above 265 mg/dL and no previous history of heart disease. It is not clear to what extent these findings can be extrapolated to females and other segments of the hypercholesterolemic population. (See also PRECAUTIONS, Carcinogenesis, Mutagenesis, Impairment of Fertility.)
Two controlled clinical trials have examined the effects of cholestyramine monotherapy upon coronary atherosclerotic lesions using coronary arteriography. In the NHLBI Type II Coronary Intervention Trial
In the St. Thomas Atherosclerosis Regression Study (STARS)3, 90 hypercholesterolemic men with CAD were randomized to three blinded treatments: usual care, lipid-lowering diet and lipid-lowering diet plus cholestyramine resin. After 36 months, follow-up coronary arteriography revealed progression of disease in 46% of usual care patients, 15% of patients on lipid-lowering diet and 12% of those receiving diet plus cholestyramine resin (p<0.02). The mean absolute width of coronary segments decreased in the usual care group, increased slightly (0.003 mm) in the diet group and increased by 0.103 mm in the diet plus cholestyramine group (p<0.05). Thus in these randomized controlled clinical trials using coronary arteriography, cholestyramine resin monotherapy has been demonstrated to slow progression2,3 and promote regression3 of atherosclerotic lesions in the coronary arteries of patients with coronary artery disease.
The effect of intensive lipid-lowering therapy on coronary atherosclerosis has been assessed by arteriography in hyperlipidemic patients. In these randomized, controlled clinical trials, patients were treated for two to four years by either conventional methods (diet, placebo or in some cases low dose resin) or intensive combination therapy using diet plus colestipol (an anion exchange resin with a mechanism of action and an effect similar on serum lipids to that of Cholestyramine for Oral Suspension Light) plus either nicotinic acid or lovastatin. When compared to conventional measures, intensive lipid-lowering combination therapy significantly reduced the frequency of progression and increased the frequency of regression of coronary atherosclerotic lesions in patients with or at risk for coronary artery disease.
3INDICATIONS 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
Prior to initiating therapy with cholestyramine resin, 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 resin 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
Since the goal of treatment is to lower LDL-C, the NCEP4 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.
Cholestyramine resin monotherapy has been demonstrated to retard the rate of progression
2) Cholestyramine for Oral Suspension USP Light powder, is indicated for the relief of pruritus associated with partial biliary obstruction. Cholestyramine resin has been shown to have a variable effect on serum cholesterol in these patients. Patients with primary biliary cirrhosis may exhibit an elevated cholesterol as part of their disease.
4CONTRAINDICATIONS
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.
5WARNINGS
PHENYLKETONURICS:
6ADVERSE 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.
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 a cholestyramine for oral suspension product. 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.
7OVERDOSAGE
Overdosage of cholestyramine resin 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.
8DOSAGE AND ADMINISTRATION
The recommended starting adult dose for Cholestyramine for Oral Suspension USP Light powder is one pouch or one level scoopful (5.718 grams of Cholestyramine for Oral Suspension USP Light powder contains 4 grams of cholestyramine resin) 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. 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 6 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.
Concomitant Therapy
Preliminary evidence suggests that the lipid-lowering effects of cholestyramine 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 therapy. See the PRECAUTIONS, Drug Interactions for recommendations on administering concomitant therapy.
Preliminary evidence suggests that the lipid-lowering effects of cholestyramine 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 therapy. See the PRECAUTIONS, Drug Interactions 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 at least 2 to 6 ounces of water or other noncarbonated beverage of your choice. 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.
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 at least 2 to 6 ounces of water or other noncarbonated beverage of your choice. 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.
9HOW SUPPLIED
Cholestyramine for Oral Suspension USP Light powder orange flavor is available in cartons of sixty 5.718 gram pouches and in jars containing 240.156 grams. Each 5.718 gram dose of Cholestyramine for Oral Suspension USP Light powder contains 4 grams of anhydrous cholestyramine resin.
Pouch: Pale yellow to yellow powder filled in sealed paper foil pouch.
67877-422-60
67877-422-57
Jar: Pale yellow to yellow powder filled in sealed white HDPE jar.
67877-422-24
Storage
Store at 20°C to 25°C (68°F to 77°F) [see USP Controlled Room Temperature].
Store at 20°C to 25°C (68°F to 77°F) [see USP Controlled Room Temperature].
REFERENCES
1. The Lipid Research Clinics Coronary Primary Prevention Trial Results: (I) Reduction in Incidence of Coronary Heart Disease; (II) The Relationship of Reduction in Incidence of Coronary Heart Disease to Cholesterol Lowering. JAMA. 1984; 251:351-374.
1. The Lipid Research Clinics Coronary Primary Prevention Trial Results: (I) Reduction in Incidence of Coronary Heart Disease; (II) The Relationship of Reduction in Incidence of Coronary Heart Disease to Cholesterol Lowering. JAMA. 1984; 251:351-374.
2. Brensike JF, Levy RI, Kelsey SF, et al. Effects of therapy with cholestyramine on progression of coronary arteriosclerosis: results of the NHLBI type II coronary intervention study. Circulation 1984; 69:313-24.
3. Watte, GF, Lewis B, Brunt JNH, Lewis ES, et al. Effects on coronary artery disease of lipid-lowering diet or diet plus cholestyramine, in the St. Thomas Atherosclerosis Regression Study (STARS). Lancet 1992; 339:563-69.
4. National Cholesterol Education Program. Second Report of the Expert panel on Detection,Evaluation and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel II). Circulation 1994 Mar;89 (3):1333-445.
5. The Lipid Research Clinics Investigators. The Lipid Research Clinics Coronary Primary Prevention Trial: Results of 6 Years of Post-Trial Follow-up. Arch Intern Med 1992; 152:1399-1410.
6. Behrman RE et al (eds): Nelson, Textbook of Pediatrics, ed 15. Philadelphia, PA, WB Saunders Company, 1996.
7. Takemoto CK et al (eds): Pediatric Dosage Handbook, ed 3. Cleveland/Akron, OH, Lexi-Comp, Inc., 1996/1997.
To report SUSPECTED ADVERSE REACTIONS, contact Ascend Laboratories, LLC at 1-877-ASC-RX01 (877-272-7901) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Manufactured by:
Alkem Laboratories Ltd.,
INDIA.
Alkem Laboratories Ltd.,
INDIA.
Distributed by:Ascend Laboratories, LLC
339 Jefferson Road,
Parsippany, NJ 07054
339 Jefferson Road,
Parsippany, NJ 07054
Revised: November 2021
PT9076-02
10PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
NDC 67877-422-24
Cholestyramine for Oral Suspension USP Light Powder
4 grams cholestyramine resin USP, per scoopful.
Orange Flavor
Cholestyramine for Oral Suspension USP Light Powder
4 grams cholestyramine resin USP, per scoopful.
Orange Flavor
NDC 67877-422-60
Cholestyramine for Oral Suspension USP Light Powder
4 grams cholestyramine resin USP, per pouch.
Orange Flavor
Cholestyramine for Oral Suspension USP Light Powder
4 grams cholestyramine resin USP, per pouch.
Orange Flavor
NDC 67877-422-57
Cholestyramine for Oral Suspension USP Light Powder
4 grams cholestyramine resin USP, per pouch.
Orange Flavor
