Cholestyramine
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]
Disclaimer
WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.
Overview
Cholestyramine is a Bile Acid Sequestrant that is FDA approved for the {{{indicationType}}} of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet. Common adverse reactions include constipation.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Reduction of elevated serum cholesterol
- Dosing information
- Recommended starting adult dose: one packet or one level scoopful once or twice a day.
- Recommended maintenance dose for all: 2 to 4 packets or scoopfuls daily (8-16 grams anhydrous cholestyramine resin) divided into two doses.
- Four grams of anhydrous cholestyramine resin is contained in each measured dose of Cholestyramine as follows:
thumb|none|400px|This image is provided by the National Library of Medicine.
- 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 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 should not be taken in its dry form. Always mix Cholestyramine 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 Drug Interactions subsection of the PRECAUTIONS section for recommendations on administering concomitant therapy.
Preparation
- The color of Cholestyramine 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 in a glass or cup. Add an amount of water or other non-carbonated beverage of your choice depending on the product being used:
thumb|none|400px|This image is provided by the National Library of Medicine.
- Stir to a uniform consistency and drink.
- Cholestyramine may also be mixed with highly fluid soups or pulpy fruits with a high moisture content such as applesauce or crushed pineapple.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information about Off-Label Guideline-Supported Use of Cholestyramine in adult patients.
Non–Guideline-Supported Use
There is limited information about Off-Label Non–Guideline-Supported Use of Cholestyramine in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information about the Pediatric Indications and Dosage.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information about Off-Label Guideline-Supported Use of Cholestyramine in pediatric patients.
Non–Guideline-Supported Use
There is limited information about Off-Label Non–Guideline-Supported Use of Cholestyramine in pediatric patients.
Contraindications
There is limited information regarding Cholestyramine Contraindications in the drug label.
Warnings
PHENYLKETONURICS: CHOLESTYRAMINE for ORAL SUSPENSION USP, LIGHT CONTAINS 14.0 mg PHENYLALANINE PER 5 GRAM DOSE.
PRECAUTIONS
General
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 (at monthly intervals) 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.
Laboratory Tests
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%–17.1% in the cholestyramine-treated group, compared with an increase of 7.9%–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.
Adverse Reactions
Clinical Trials Experience
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 resin. 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.
Postmarketing Experience
There is limited information regarding Cholestyramine Postmarketing Experience in the drug label.
Drug Interactions
There is limited information regarding Cholestyramine Drug Interactions in the drug label.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Cholestyramine in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Cholestyramine in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Cholestyramine during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Cholestyramine in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Cholestyramine in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Cholestyramine in geriatric settings.
Gender
There is no FDA guidance on the use of Cholestyramine with respect to specific gender populations.
Race
There is no FDA guidance on the use of Cholestyramine with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Cholestyramine in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Cholestyramine in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Cholestyramine in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Cholestyramine in patients who are immunocompromised.
Administration and Monitoring
Administration
There is limited information regarding Cholestyramine Administration in the drug label.
Monitoring
There is limited information regarding Cholestyramine Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Cholestyramine and IV administrations.
Overdosage
There is limited information regarding Cholestyramine overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Cholestyramine Pharmacology in the drug label.
Mechanism of Action
There is limited information regarding Cholestyramine Mechanism of Action in the drug label.
Structure
There is limited information regarding Cholestyramine Structure in the drug label.
Pharmacodynamics
There is limited information regarding Cholestyramine Pharmacodynamics in the drug label.
Pharmacokinetics
There is limited information regarding Cholestyramine Pharmacokinetics in the drug label.
Nonclinical Toxicology
There is limited information regarding Cholestyramine Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Cholestyramine Clinical Studies in the drug label.
How Supplied
There is limited information regarding Cholestyramine How Supplied in the drug label.
Storage
There is limited information regarding Cholestyramine Storage in the drug label.
Images
Drug Images
{{#ask: Page Name::Cholestyramine |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
{{#ask: Label Page::Cholestyramine |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
Patient Counseling Information
There is limited information regarding Cholestyramine Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Cholestyramine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Cholestyramine Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Cholestyramine Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.