Cholestyramine Powder (can) 348.6gm
It is used to lower cholesterol.It is used to treat itching caused by bile duct blockage. It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antilipemic Agent, Bile Acid Sequestrant
Pharmacologic Class
Bile Acid Sequestrant
Pregnancy Category
Category C
FDA Approved
Sep 1973
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cholestyramine is a powder that you mix with water or other liquids and drink. It works in your intestines to bind to certain substances called bile acids. By binding these, it helps your body remove more cholesterol, which can lower your 'bad' cholesterol (LDL) levels. It can also help relieve itching caused by certain liver conditions.
How to Use This Medicine
Taking Your Medication Correctly
To use this medication safely and effectively, follow your doctor's instructions and read all the information provided. Take this medication exactly as directed by your doctor.
Do not take the dry powder directly. Instead, mix it with at least 2 to 6 ounces (60 to 180 mL) of liquid before taking.
After mixing, rinse the cup with more liquid and drink to ensure you get the full dose.
You can also mix this medication with highly fluid soups, applesauce, or crushed pineapple to make it easier to take.
Unless your doctor advises you to limit your fluid intake, be sure to drink extra liquids after each dose.
Consult with your doctor or pharmacist about the best way to take this medication in relation to food.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, avoiding the bathroom.
Keep all medications in a safe location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist or healthcare provider.
Check with your pharmacist for guidance on the best way to dispose of medications. Your area may have drug take-back programs available.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and continue with your regular dosing schedule.
Do not take two doses at the same time or take extra doses to make up for a missed dose.
To use this medication safely and effectively, follow your doctor's instructions and read all the information provided. Take this medication exactly as directed by your doctor.
Do not take the dry powder directly. Instead, mix it with at least 2 to 6 ounces (60 to 180 mL) of liquid before taking.
After mixing, rinse the cup with more liquid and drink to ensure you get the full dose.
You can also mix this medication with highly fluid soups, applesauce, or crushed pineapple to make it easier to take.
Unless your doctor advises you to limit your fluid intake, be sure to drink extra liquids after each dose.
Consult with your doctor or pharmacist about the best way to take this medication in relation to food.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, avoiding the bathroom.
Keep all medications in a safe location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist or healthcare provider.
Check with your pharmacist for guidance on the best way to dispose of medications. Your area may have drug take-back programs available.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and continue with your regular dosing schedule.
Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Maintain a healthy diet low in saturated and trans fats, and cholesterol.
- Engage in regular physical activity.
- If experiencing constipation, increase fluid intake and dietary fiber, unless medically contraindicated.
- Take other medications at least 1 hour before or 4-6 hours after cholestyramine to prevent interactions.
Available Forms & Alternatives
Available Strengths:
- Cholestyramine 4gm Lght Pow Pk 60s
- Cholestyramine Light Powder (can)
- Cholestyramine Powder (can) 378gm
- Cholestyramine 4gm Lght Pow Pk 60s
- Cholestyramine 4gm Packets 60s
- Cholestyramine Powder(can) 368.76gm
- Cholestyramine Powder (can) 348.6gm
- Cholestyramine Powder (can) 378gm
- Cholestyramine Light Powder (can)
Dosing & Administration
Adult Dosing
Standard Dose:
4 g (1 scoop/packet) 1-2 times daily initially, increasing to 4-8 g 2 times daily
Dose Range:
4 - 24 mg
Condition-Specific Dosing:
hyperlipidemia:
4 g 1-2 times daily initially, increasing to 4-8 g 2 times daily. Max 24 g/day in 2-6 divided doses.
pruritus_due_to_partial_biliary_obstruction:
4 g 1-2 times daily initially, may increase to 4 g 3 times daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established, use with caution and individualized
Child:
Hyperlipidemia: 80 mg/kg/day in 2-3 divided doses, not to exceed 4 g/day. Individualize based on response and tolerability. Monitor for vitamin deficiencies.
Adolescent:
Hyperlipidemia: 80 mg/kg/day in 2-3 divided doses, not to exceed 4 g/day or adult dose if higher. Individualize based on response and tolerability. Monitor for vitamin deficiencies.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed as it is not absorbed systemically.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed (used for pruritus in partial biliary obstruction, but not systemically absorbed or metabolized by liver).
Pharmacology
Mechanism of Action
Cholestyramine resin is an anion-exchange resin that binds bile acids in the intestinal lumen, forming an insoluble complex that is excreted in the feces. This interruption of the enterohepatic circulation of bile acids leads to an increased synthesis of bile acids from cholesterol in the liver. This increased demand for cholesterol in the liver results in an upregulation of hepatic LDL receptors, leading to increased clearance of LDL-C from the plasma and a reduction in serum LDL-C levels.
Pharmacokinetics
Absorption:
Bioavailability:
Not absorbed (0%)
Tmax:
Not applicable (not absorbed)
FoodEffect:
Can be taken with or without food, but often taken with meals to improve palatability and reduce GI side effects. Timing relative to other medications is critical.
Distribution:
Vd:
Not applicable (not absorbed)
ProteinBinding:
Not applicable (not absorbed)
CnssPenetration:
No
Elimination:
HalfLife:
Not applicable (not absorbed)
Clearance:
Not applicable (not absorbed)
ExcretionRoute:
Fecal excretion (as insoluble complex with bile acids)
Unchanged:
100%
Pharmacodynamics
OnsetOfAction:
Within 24-48 hours for bile acid binding; lipid-lowering effects typically seen within 4-7 days, maximal effect within 2-3 weeks.
PeakEffect:
2-3 weeks for maximal LDL-C reduction.
DurationOfAction:
Effects persist as long as therapy is continued; bile acid binding is immediate and continuous with dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe constipation or stomach pain, which may be signs of a severe bowel problem
Unexplained bruising or bleeding
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Constipation: Drinking more liquids, exercising regularly, or adding fiber to your diet may help alleviate this symptom. Your doctor may also recommend a stool softener or laxative.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe constipation or stomach pain, which may be signs of a severe bowel problem
Unexplained bruising or bleeding
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Constipation: Drinking more liquids, exercising regularly, or adding fiber to your diet may help alleviate this symptom. Your doctor may also recommend a stool softener or laxative.
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent constipation
- Severe abdominal pain or bloating
- Unusual bleeding or bruising (e.g., nosebleeds, bleeding gums, dark stools)
- Night blindness or vision changes
- Bone pain or muscle weakness
- Yellowing of skin or eyes (jaundice)
- Dark urine or pale stools
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a blockage in your biliary tract.
This is not an exhaustive list of potential interactions. To ensure your safety, it is crucial to discuss all of the following with your doctor and pharmacist:
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
Any health problems you have.
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe to do so. This will help prevent potential interactions and ensure the safe use of this medication.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a blockage in your biliary tract.
This is not an exhaustive list of potential interactions. To ensure your safety, it is crucial to discuss all of the following with your doctor and pharmacist:
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins.
Any health problems you have.
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe to do so. This will help prevent potential interactions and ensure the safe use of this medication.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you have phenylketonuria (PKU), consult with your doctor, as some formulations of this drug may contain phenylalanine.
Regular blood work and laboratory tests should be conducted as directed by your doctor to monitor your condition. When taking other medications, ensure that you administer them at least 1 hour before or 4 hours after taking this drug to minimize potential interactions.
Adhere to the diet and exercise plan recommended by your doctor to optimize the effectiveness of this medication. To avoid dental complications, such as tooth discoloration, it is crucial to avoid holding the mixed drug in your mouth for an extended period or sipping it slowly. If you have concerns, discuss them with your doctor.
Maintaining good oral hygiene is vital; therefore, practice proper dental care and schedule regular dental check-ups. If you are 60 years or older, use this medication with caution, as you may be more susceptible to experiencing side effects.
Although rare, bowel obstruction has been reported in children taking this drug, and in some cases, it has been fatal. If you have questions or concerns, consult with your doctor. Additionally, if you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Regular blood work and laboratory tests should be conducted as directed by your doctor to monitor your condition. When taking other medications, ensure that you administer them at least 1 hour before or 4 hours after taking this drug to minimize potential interactions.
Adhere to the diet and exercise plan recommended by your doctor to optimize the effectiveness of this medication. To avoid dental complications, such as tooth discoloration, it is crucial to avoid holding the mixed drug in your mouth for an extended period or sipping it slowly. If you have concerns, discuss them with your doctor.
Maintaining good oral hygiene is vital; therefore, practice proper dental care and schedule regular dental check-ups. If you are 60 years or older, use this medication with caution, as you may be more susceptible to experiencing side effects.
Although rare, bowel obstruction has been reported in children taking this drug, and in some cases, it has been fatal. If you have questions or concerns, consult with your doctor. Additionally, if you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Severe constipation
- Intestinal obstruction (rare, but possible with very large doses)
- Abdominal distension
What to Do:
Contact a poison control center or emergency medical services immediately. Management is supportive, focusing on maintaining hydration and bowel function. Call 1-800-222-1222.
Drug Interactions
Major Interactions
- Warfarin (decreased absorption, increased INR variability)
- Digoxin (decreased absorption, reduced efficacy)
- Thyroid hormones (e.g., levothyroxine) (decreased absorption, hypothyroidism)
- Fat-soluble vitamins (A, D, E, K) (decreased absorption, potential for deficiency)
- Thiazide diuretics (e.g., hydrochlorothiazide) (decreased absorption)
- Beta-blockers (e.g., propranolol) (decreased absorption)
- Statins (e.g., pravastatin, fluvastatin) (decreased absorption)
- Oral contraceptives (potential for decreased absorption, reduced efficacy)
- Phenobarbital (decreased absorption)
- Ursodiol (decreased absorption)
Moderate Interactions
- Nonsteroidal anti-inflammatory drugs (NSAIDs) (potential for decreased absorption)
- Glipizide (potential for decreased absorption)
- Methotrexate (potential for decreased absorption)
- Mycophenolate mofetil (decreased absorption)
- Valproic acid (potential for decreased absorption)
Minor Interactions
- Iron supplements (potential for decreased absorption)
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess the primary indication for therapy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST, Alk Phos, Bilirubin)
Rationale: To assess baseline liver function, especially if used for pruritus due to partial biliary obstruction.
Timing: Prior to initiation of therapy.
Prothrombin Time (PT/INR)
Rationale: To assess baseline coagulation, especially if patient is on anticoagulants or has risk factors for vitamin K deficiency.
Timing: Prior to initiation of therapy.
Fat-soluble vitamin levels (A, D, E, K)
Rationale: Consider if patient has pre-existing malabsorption or is at high risk for deficiency, as cholestyramine can interfere with their absorption.
Timing: Prior to initiation of therapy (optional, based on clinical judgment).
Routine Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Frequency: Every 4-6 weeks initially, then every 3-6 months once stable.
Target: Individualized based on patient risk factors and treatment goals (e.g., LDL-C <100 mg/dL or <70 mg/dL).
Action Threshold: If lipid goals are not met, consider dose adjustment or addition of other lipid-lowering agents. If triglycerides significantly increase (>400 mg/dL), re-evaluate therapy.
Liver Function Tests (ALT, AST, Alk Phos, Bilirubin)
Frequency: Periodically, especially if used for pruritus or if symptoms of liver dysfunction develop.
Target: Within normal limits.
Action Threshold: Significant elevation may warrant investigation and re-evaluation of therapy.
Prothrombin Time (PT/INR)
Frequency: Regularly, especially if patient is on warfarin or long-term therapy.
Target: Therapeutic range for warfarin (e.g., INR 2.0-3.0).
Action Threshold: Increased INR may indicate vitamin K deficiency; consider vitamin K supplementation.
Fat-soluble vitamin levels (A, D, E, K)
Frequency: Consider periodically (e.g., annually) for long-term therapy, especially in pediatric patients or those with malabsorption.
Target: Within normal limits.
Action Threshold: Deficiency requires supplementation.
Electrolytes (Chloride)
Frequency: Periodically, especially in pediatric patients or those with renal impairment, if hyperchloremic acidosis is a concern.
Target: Within normal limits.
Action Threshold: Elevated chloride may indicate hyperchloremic acidosis.
Symptom Monitoring
- Constipation (most common side effect)
- Abdominal discomfort/pain
- Bloating
- Nausea
- Vomiting
- Steatorrhea (fatty stools)
- Easy bruising or bleeding (signs of vitamin K deficiency)
- Night blindness (sign of vitamin A deficiency)
- Bone pain or weakness (signs of vitamin D deficiency)
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Cholestyramine is not absorbed systemically, so direct fetal exposure is unlikely. However, it can interfere with the absorption of fat-soluble vitamins (A, D, E, K) and folic acid in the mother, which are essential for fetal development. Supplementation of these vitamins may be necessary.
Trimester-Specific Risks:
First Trimester:
Potential for maternal vitamin deficiencies (especially folate) which are critical for early fetal development.
Second Trimester:
Potential for maternal vitamin deficiencies.
Third Trimester:
Potential for maternal vitamin deficiencies, particularly vitamin K, which could affect neonatal coagulation.
Lactation
L3 (Moderately Safe). Cholestyramine is not absorbed by the mother, so it is not excreted into breast milk. However, it can interfere with the absorption of fat-soluble vitamins in the mother, potentially affecting the nutritional content of breast milk. Monitor the infant for signs of vitamin deficiency if maternal intake is compromised. Consider maternal vitamin supplementation.
Infant Risk:
Low direct risk. Indirect risk due to potential for reduced maternal fat-soluble vitamin levels affecting breast milk composition.
Pediatric Use
Use with caution. Long-term use in children may lead to malabsorption of fat-soluble vitamins (A, D, E, K) and folic acid, potentially affecting growth and development. Regular monitoring of vitamin levels and supplementation may be required. Increased risk of constipation.
Geriatric Use
Increased susceptibility to constipation and potential for fecal impaction. May be more prone to vitamin deficiencies due to pre-existing conditions or polypharmacy. Start with lower doses and titrate slowly. Monitor bowel function closely.
Clinical Information
Clinical Pearls
- Always mix the powder thoroughly with at least 2-6 ounces (60-180 mL) of water, juice, or other non-carbonated beverages, or soft foods like applesauce or pureed fruits. Do not take in dry form.
- To minimize gastrointestinal side effects (especially constipation), start with a low dose and gradually increase. Adequate fluid intake is crucial.
- Timing of administration is critical for drug interactions: take other medications at least 1 hour before or 4-6 hours after cholestyramine to prevent binding and reduced absorption.
- Consider vitamin supplementation (especially fat-soluble vitamins A, D, E, K, and folic acid) for patients on long-term therapy, particularly children and pregnant/lactating women.
- Cholestyramine can increase triglyceride levels in some patients; monitor lipid panel regularly. If triglycerides rise significantly, consider alternative lipid-lowering therapy.
- The 'light' formulations contain aspartame and should be avoided in patients with phenylketonuria (PKU).
Alternative Therapies
- Other Bile Acid Sequestrants: Colesevelam, Colestipol (for hyperlipidemia)
- Statins (HMG-CoA Reductase Inhibitors): Atorvastatin, Rosuvastatin, Simvastatin (for hyperlipidemia)
- Ezetimibe (Cholesterol Absorption Inhibitor) (for hyperlipidemia)
- PCSK9 Inhibitors: Alirocumab, Evolocumab (for severe hyperlipidemia)
- Fibrates: Gemfibrozil, Fenofibrate (primarily for hypertriglyceridemia, but also affect LDL-C)
- Niacin (Nicotinic Acid) (for hyperlipidemia)
- For pruritus due to partial biliary obstruction: Rifampin, Ursodiol, Naltrexone, Sertraline.
Cost & Coverage
Average Cost:
Varies widely, typically $50-$200 per 348.6gm can (approx. 42 doses)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic preferred)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.