DRUGS & SUPPLEMENTS
INDICATIONS AND USAGE
1) Cholestyramine® (cholestyramine for oral suspension, USP) 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® (cholestyramine for oral suspension, USP) 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 (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 reduction should occur during the first month of Cholestyramine resin therapy. The therapy should be continued to sustain cholesterol reduction. If adequate cholesterol reduction is not attained, increasing the dosage of Cholestyramine resin or adding other lipid-lowering agents in combination with Cholestyramine resin should be considered.
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 progression2,3 and increase the rate of regression3 of coronary atherosclerosis.
2) Cholestyramine® (cholestyramine for oral suspension, USP) 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.
Cholestyramine® 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.
PHENYLKETONURICS: Cholestyramine® CONTAINS 14.1 mg PHENYLALANINE PER 5.5 GRAM DOSE.
Chronic use of Cholestyramine resin may be associated with increased bleeding tendency due to hypoprothrombinemia associated with Vitamin K deficiency. This will usually respond promptly to parenteral Vitamin K1 and recurrences can be prevented by oral administration of Vitamin K1. Reduction of serum or red cell folate has been reported over long term administration of Cholestyramine resin. Supplementation with folic acid should be considered in these cases.
There is a possibility that prolonged use of Cholestyramine resin, since it is a chloride form of anion exchange resin, may produce hyperchloremic acidosis. This would especially be true in younger and smaller patients where the relative dosage may be higher. Caution should also be exercised in patients with renal insufficiency or volume depletion and in patients receiving concomitant spironolactone.
Cholestyramine resin may produce or worsen pre-existing constipation. The dosage should be increased gradually in patients to minimize the risk of developing fecal impaction. In patients with pre-existing constipation, the starting dose should be 1 packet or 1 scoop once daily for 5 to 7 days, increasing to twice daily with monitoring of constipation and of serum lipoproteins, at least twice, 4 to 6 weeks apart. Increased fluid intake and fiber intake should be encouraged to alleviate constipation and a stool softener may occasionally be indicated. If the initial dose is well tolerated, the dose may be increased as needed by one dose/day with periodic monitoring of serum lipoproteins. If constipation worsens or the desired therapeutic response is not achieved at one to six doses/day, combination therapy or alternate therapy should be considered. Particular effort should be made to avoid constipation in patients with symptomatic coronary artery disease. Constipation associated with Cholestyramine resin may aggravate hemorrhoids.
Information for Patients
Inform your physician if you are pregnant or plan to become pregnant or are breast-feeding. Drink plenty of fluids and mix each 5.5 gram dose of Cholestyramine® (cholestyramine for oral suspension, USP) powder in at least 2 to 3 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.
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% to 17.1% in the cholestyramine-treated group, compared with an increase of 7.9% to 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.
Cholestyramine resin may delay or reduce the absorption of concomitant oral medication such as phenylbutazone, warfarin, thiazide diuretics 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 1 HOUR BEFORE OR 4 TO 6 HOURS AFTER Cholestyramine RESIN (OR AT AS GREAT AN INTERVAL AS POSSIBLE) TO AVOID IMPEDING THEIR ABSORPTION.
Carcinogenesis, Mutagenesis, 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 resin 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-CPPT5 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 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 weighted 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.
Caution should be exercised when Cholestyramine resin is administered to a nursing mother. The possible lack of proper vitamin absorption described in the "Pregnancy" section may have an effect on nursing infants.
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 g/day with dose titration based on response and tolerance.
In calculating pediatric dosages, 80 mg of anhydrous Cholestyramine resin are contained in 110 mg of Cholestyramine®.
The effects of long-term drug administration, as well as its effect in maintaining lowered cholesterol levels in pediatric patients, are unknown. Also see 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, 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 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:
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.
DOSAGE AND ADMINISTRATION
The recommended starting adult dose for Cholestyramine® powder is one packet or one level scoopful (5.5 grams of Cholestyramine® [cholestyramine for oral suspension, USP] powder contain 4 grams of anhydrous Cholestyramine resin) once or twice a day. The recommended maintenance dose for Cholestyramine® (cholestyramine for oral suspension, USP) powder is 2 to 4 packets 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 six packets or scoopfuls of Cholestyramine® (cholestyramine for oral suspension, USP) 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® (cholestyramine for oral suspension, USP) powder may be administered in 1 to 6 doses per day.
Cholestyramine® (cholestyramine for oral suspension, USP) powder should not be taken in its dry form. Always mix the dry powder with water or other fluids before ingesting. See Preparation Instructions.
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 PRECAUTIONS, Drug Interactions for recommendations on administering concomitant therapy.
The color of Cholestyramine® (cholestyramine for oral suspension, USP) 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 packet or one level scoopful of Cholestyramine® (cholestyramine for oral suspension, USP) powder in a glass or cup. Add at least 2 to 3 ounces of water or the beverage of your choice. Stir to a uniform consistency.
Cholestyramine® (cholestyramine for oral suspension, USP) powder may also be mixed with highly fluid soups or pulpy fruits with a high moisture content such as applesauce or crushed pineapple.
Cholestyramine® (cholestyramine for oral suspension, USP) powder is available in cartons of forty-two and sixty single-dose packets and in cans containing 231 grams. 5.5 grams of Cholestyramine® (cholestyramine for oral suspension, USP) powder contain 4 grams of anhydrous Cholestyramine resin.
Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F).
To report SUSPECTED ADVERSE REACTIONS, contact Upsher-Smith Laboratories, LLC at 1-855-899-9180 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
UPSHER-SMITH LABORATORIES, LLC
Maple Grove, MN 55369
(Cholestyramine for Oral Suspension, USP)
4 grams Cholestyramine
resin USP, per scoopful†
Contains 231 g (168 g anhydrous Cholestyramine resin)
42 measured doses
*NutraSweet and the NutraSweet symbol are registered
trademarks of The NutraSweet Company
Cholestyramine pharmaceutical active ingredients containing related brand and generic drugs:
Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.
Cholestyramine available forms, composition, doses:
Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.
Cholestyramine destination | category:
Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.
Cholestyramine Anatomical Therapeutic Chemical codes:
A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.
Cholestyramine pharmaceutical companies:
Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.
Frequently asked QuestionsCan i drive or operate heavy machine after consuming Cholestyramine?
Depending on the reaction of the Cholestyramine after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Cholestyramine not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Cholestyramine addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
ReviewsDrugs.com conducted a study on Cholestyramine, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Cholestyramine consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.
Two visitors reported frequency of useHow often in a day do you take the medicine?
Are you taking the Cholestyramine drug as prescribed by the doctor?
Few medications can be taken 3 times in a day more than prescribed when the doctor's advice mentions the medicine can be taken according to frequency or severity of symptoms. Most times, be very careful and clear about the number of times you are taking the medication. The report of sDrugs.com website users about the frequency of taking the drug Cholestyramine is mentioned below.
One visitor reported dosesWhat is the dose of Cholestyramine drug you are taking?
According to the survey conducted among sDrugs.com website users, the maximum number of people are using the following dose 1-5mg. Few medications come in only one or two doses. Few are specific for adult dose and child dose. The dose of the medicine given to the patient depends on the severity of the symptom/disease. There can be dose adjustments made by the doctor, based on the progression of the disease. Follow-up is important.
One visitor reported age
The information was verified by Dr. Arunabha Ray, MD Pharmacology