Clinical medicine profile
Cholestyramine
Bile Acid Sequestrant [EPC]
- Route
- See product SmPC
- Schedule
- POM
- ATC
- Not assigned
- PPB status
- registered
Safety essentials
The information most likely to change a prescribing or dispensing decision.
Contraindications
- 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.
Precautions
- Obtain allergy and medication history.
- Adjust for renal/hepatic impairment, pregnancy, lactation, extremes of age and interacting drugs.
- Use the lowest effective dose for the shortest appropriate duration.
- Monitor for expected class adverse effects.
Dosing matrix
Population and organ-function guidance, shown together for faster comparison.
DOSAGE AND ADMINISTRATION The recommended starting adult dose for Cholestyramine for Oral Suspension, USP Light powder is one pouch or one level scoopful (5.7 grams of Cholestyramine for Oral Suspension, USP Light powder contains 4 grams of anhydrous 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. Cholestyramine for Oral Suspension, USP Light powder should not be taken in its dry form. Always mix the dry powder with water or other fluids before ingesting. See Preparation Instructions. 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 3 ounces of water or the beverage of your choice. Stir to a uniform consistency. 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.
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 g/day with dose titration based on response and tolerance. In calculating pediatric dosages, 70.2 mg of anhydrous cholestyramine resin are contained in 100 mg of Cholestyramine for Oral Suspension USP Light. 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 .
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Use, effects & interactions
Indications
- 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 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.
Adverse effects
- 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: 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.
Drug interactions
Open multi-drug checker ↗- Professional use: confirm indication, dose, duration, monitoring and patient counselling points against current Kenya STG / EML and the product SmPC.
- Document allergy status and key interactions.
Mechanism & disposition
Bile sequestering resins binds bile acids in the intestine to form an insoluble complex; which is excreted in the faeces.
Read complete mechanism
Bile sequestering resins binds bile acids in the intestine to form an insoluble complex; which is excreted in the faeces. Mechanism is agent-specific. At receptor, enzyme, ion channel, transporter or microbial target level, the drug alters a physiological or pathological pathway to produce its therapeutic effect. Confirm precise molecular mechanism in current SmPC / pharmacology reference for this INN before high-stakes decisions.
Product-specific
Product-specific
See product SmPC
Pregnancy, lactation & diet
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 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 (see PRECAUTIONS, Drug Interactions ).
Nursing Mothers Caution should be exercised when cholestyramine resin is administered to a nursing mother. The possible lack of proper vitamin absorption described in PRECAUTIONS, Pregnancy may have an effect on nursing infants.
Brands & loaded prices
| Brand | Manufacturer | Pack | Observed price |
|---|---|---|---|
| QUESTRAN LIGHT | Not recorded | 4MG SATCHETS 50*S | KES 6,310.25Daima Chemist price-list reference ↗ Source date not recorded · verify current price |
Sources & review state
Decision support only. Confirm patient-specific decisions against the current product SmPC, Kenya STG/EML, and professional judgement.