Cholestyramine 4gm Packets 60s
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
C
FDA Approved
Jan 1973
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cholestyramine is a medication that helps lower high cholesterol levels in your blood. It works by binding to certain substances (bile acids) in your gut, preventing them from being reabsorbed into your body. This forces your liver to use more cholesterol to make new bile acids, which helps to lower your overall cholesterol.
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. It is essential to take this medication exactly as directed.
When taking this medication, do not ingest the dry powder. Instead, mix it with at least 2 to 6 ounces (60 to 180 mL) of liquid before consumption. After mixing, rinse the cup with additional liquid and drink it to ensure you receive the full dose. You may also combine the medication with highly fluid soups, applesauce, or crushed pineapple if preferred.
To stay hydrated, drink extra liquids after each dose of this medication, unless your doctor advises you to limit your fluid intake. Consult with your doctor or pharmacist to determine the best approach to taking this medication in relation to food.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding storage in a bathroom. Keep all medications in a secure place, 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. If you have questions about the proper disposal method, consult with your pharmacist, who can also inform you about potential drug take-back programs in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to compensate for the missed dose.
To use this medication safely and effectively, follow your doctor's instructions and read all the information provided. It is essential to take this medication exactly as directed.
When taking this medication, do not ingest the dry powder. Instead, mix it with at least 2 to 6 ounces (60 to 180 mL) of liquid before consumption. After mixing, rinse the cup with additional liquid and drink it to ensure you receive the full dose. You may also combine the medication with highly fluid soups, applesauce, or crushed pineapple if preferred.
To stay hydrated, drink extra liquids after each dose of this medication, unless your doctor advises you to limit your fluid intake. Consult with your doctor or pharmacist to determine the best approach to taking this medication in relation to food.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry location, avoiding storage in a bathroom. Keep all medications in a secure place, 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. If you have questions about the proper disposal method, consult with your pharmacist, who can also inform you about potential drug take-back programs in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to compensate for the missed dose.
Lifestyle & Tips
- Maintain a healthy diet low in saturated and trans fats and cholesterol.
- Engage in regular physical activity as recommended by your doctor.
- Ensure adequate fluid intake (6-8 glasses of water daily) to help prevent constipation, a common side effect.
- Follow your doctor's instructions regarding the timing of other medications, as cholestyramine can interfere with their absorption.
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 grams (1 packet) orally 1 to 2 times daily initially, then adjusted based on response.
Dose Range:
4 - 24 mg
Condition-Specific Dosing:
primaryHypercholesterolemia:
Initial: 4 g once or twice daily. Maintenance: 8-16 g/day in 2-4 divided doses. Max: 24 g/day.
pruritusAssociatedWithPartialBiliaryObstruction:
4 g orally 1 to 2 times daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established, use with caution and under specialist guidance. Dosing often based on body surface area (BSA) or weight (e.g., 0.25 g/kg/day divided 2-3 times daily).
Child:
Not established, use with caution and under specialist guidance. Dosing often based on body surface area (BSA) or weight (e.g., 0.25 g/kg/day divided 2-3 times daily).
Adolescent:
Not established, use with caution and under specialist guidance. Dosing often based on body surface area (BSA) or weight (e.25 g/kg/day divided 2-3 times daily).
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed as it is not absorbed.
Moderate:
No adjustment needed as it is not absorbed.
Severe:
No adjustment needed as it is not absorbed.
Dialysis:
No adjustment needed as it is not absorbed.
Hepatic Impairment:
Mild:
No adjustment needed as it is not absorbed.
Moderate:
No adjustment needed as it is not absorbed.
Severe:
No adjustment needed as it is not absorbed.
Pharmacology
Mechanism of Action
Cholestyramine resin is an anion-exchange resin that binds bile acids in the intestine to form an insoluble complex, which is then 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, thereby increasing the number of LDL receptors on the hepatocyte surface and subsequently lowering plasma LDL-cholesterol levels.
Pharmacokinetics
Absorption:
Bioavailability:
Negligible (not absorbed)
Tmax:
Not applicable (not absorbed)
FoodEffect:
Can be taken with meals to improve palatability, but may affect absorption of other drugs if taken concurrently.
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 (as insoluble complex)
Unchanged:
100%
Pharmacodynamics
OnsetOfAction:
Within 24-48 hours (for bile acid binding)
PeakEffect:
Cholesterol lowering effect typically seen within 1-3 weeks.
DurationOfAction:
Continues as long as therapy is maintained.
Confidence:
Medium
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
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 immediate medical attention:
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 symptoms that bother you or do not go away, contact your doctor:
Constipation: Drinking more liquids, exercising, 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, contact your doctor for medical advice. 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 immediate medical attention:
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 symptoms that bother you or do not go away, contact your doctor:
Constipation: Drinking more liquids, exercising, 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, contact your doctor for medical advice. 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 stomach pain or bloating
- Unusual bleeding or bruising (especially if on blood thinners)
- Symptoms of vitamin deficiency (e.g., night blindness, bone pain, easy bruising)
- Dark urine or yellowing of skin/eyes (jaundice, rare)
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 drugs, natural products, and vitamins.
Any health problems you have.
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so. This will help you avoid any potential interactions or complications.
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 drugs, natural products, and vitamins.
Any health problems you have.
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so. This will help you avoid any potential interactions or complications.
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 tests and other laboratory assessments 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 dietary and exercise plan recommended by your doctor to optimize the effectiveness of this medication. To avoid tooth discoloration and other dental changes, 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. Maintain good oral hygiene and schedule regular dental check-ups to prevent complications.
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects. In rare cases, bowel obstruction has occurred in children taking this drug, and in some instances, it has been fatal. If you have questions or concerns, consult with your doctor.
Before taking this medication, inform your doctor if you are pregnant, planning to become pregnant, or breastfeeding. Your doctor will discuss the potential benefits and risks of this medication to you and your baby, allowing you to make an informed decision.
Regular blood tests and other laboratory assessments 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 dietary and exercise plan recommended by your doctor to optimize the effectiveness of this medication. To avoid tooth discoloration and other dental changes, 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. Maintain good oral hygiene and schedule regular dental check-ups to prevent complications.
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects. In rare cases, bowel obstruction has occurred in children taking this drug, and in some instances, it has been fatal. If you have questions or concerns, consult with your doctor.
Before taking this medication, inform your doctor if you are pregnant, planning to become pregnant, or breastfeeding. Your doctor will discuss the potential benefits and risks of this medication to you and your baby, allowing you to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe constipation
- Intestinal obstruction (rare, but possible with very large doses or pre-existing bowel issues)
What to Do:
Contact a poison control center or emergency medical services immediately. Management is supportive, focusing on relieving constipation and maintaining hydration. Call 1-800-222-1222.
Drug Interactions
Major Interactions
- Warfarin (decreased absorption, increased bleeding risk)
- Thyroid hormones (e.g., levothyroxine, decreased absorption)
- Digoxin (decreased absorption)
- Fat-soluble vitamins (A, D, E, K - decreased absorption, potential deficiency)
- Thiazide diuretics (e.g., hydrochlorothiazide, decreased absorption)
- Oral phosphates (e.g., sodium phosphate, decreased absorption)
- Mycophenolate mofetil (decreased absorption)
Moderate Interactions
- Phenobarbital (decreased absorption)
- Tetracyclines (decreased absorption)
- Propranolol (decreased absorption)
- Ursodiol (decreased absorption)
- Statins (potential for additive effect on LDL-C lowering, but also potential for decreased statin absorption if not separated)
- Oral contraceptives (potential for decreased absorption, though clinical significance debated)
Minor Interactions
- Nonsteroidal anti-inflammatory drugs (NSAIDs, 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 treatment.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST, ALP, Bilirubin)
Rationale: To assess baseline hepatic function, as cholestyramine is used in conditions affecting bile flow.
Timing: Prior to initiation of therapy.
Prothrombin Time (PT/INR)
Rationale: If patient is on warfarin or has a history of bleeding disorders, due to potential for vitamin K malabsorption.
Timing: Prior to initiation of therapy.
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: LDL-C reduction of 15-30% is typical; target levels based on patient risk.
Action Threshold: If target LDL-C not achieved or if adverse lipid changes (e.g., significant triglyceride increase) occur.
Fat-soluble Vitamin Levels (A, D, E, K)
Frequency: Periodically (e.g., annually) for patients on long-term therapy, especially if symptoms of deficiency arise.
Target: Within normal reference ranges.
Action Threshold: If levels are low, consider supplementation.
Prothrombin Time (PT/INR)
Frequency: Regularly if patient is on warfarin, especially during initiation or dose changes.
Target: Therapeutic range for warfarin (e.g., INR 2.0-3.0).
Action Threshold: If INR is outside target range, adjust warfarin dose.
Electrolytes (Chloride)
Frequency: Periodically, especially in patients with renal impairment or on high doses, due to potential for hyperchloremic acidosis.
Target: Within normal reference range.
Action Threshold: If elevated chloride, investigate and manage.
Symptom Monitoring
- Constipation (most common, monitor bowel habits)
- Abdominal discomfort, bloating, flatulence, nausea
- Symptoms of fat-soluble vitamin deficiency (e.g., night blindness for Vit A, bone pain for Vit D, easy bruising/bleeding for Vit K)
- Unusual bleeding or bruising (especially if on warfarin)
- Changes in stool consistency or color (e.g., steatorrhea)
Special Patient Groups
Pregnancy
Generally considered safe due to lack of systemic absorption, but potential for interference with maternal fat-soluble vitamin absorption (especially vitamin K) should be considered. Supplementation may be necessary. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
Low risk due to lack of systemic absorption; however, monitor maternal vitamin status.
Second Trimester:
Low risk; monitor maternal vitamin status.
Third Trimester:
Low risk; monitor maternal vitamin status, particularly vitamin K, to prevent potential neonatal coagulopathy.
Lactation
Considered compatible with breastfeeding (L3). Cholestyramine is not absorbed systemically by the mother, so it is not excreted into breast milk. However, maternal fat-soluble vitamin deficiencies could theoretically impact milk quality. Monitor infant for adequate growth and development.
Infant Risk:
Low risk to infant. No direct exposure. Indirect risk from potential maternal vitamin deficiencies.
Pediatric Use
Use in children is generally reserved for severe hypercholesterolemia not responsive to diet, or for pruritus associated with biliary obstruction. Dosing is not well-established and should be individualized under specialist supervision. Long-term use requires careful monitoring for growth and fat-soluble vitamin deficiencies.
Geriatric Use
No specific dose adjustment needed. However, elderly patients may be more susceptible to constipation and its complications (e.g., fecal impaction), and may be on multiple medications, increasing the risk of drug interactions. Monitor closely for GI side effects and drug absorption issues.
Clinical Information
Clinical Pearls
- Always mix cholestyramine powder thoroughly with water, juice, or applesauce before administration to prevent esophageal irritation or choking.
- Administer other medications at least 1 hour before or 4-6 hours after cholestyramine to minimize drug binding and ensure adequate absorption of other drugs.
- Constipation is the most common side effect; advise patients to increase fluid intake and dietary fiber. Stool softeners or laxatives may be necessary.
- Long-term use may lead to deficiencies of fat-soluble vitamins (A, D, E, K) and folic acid. Supplementation may be required.
- Cholestyramine can increase triglyceride levels in some patients, especially those with pre-existing hypertriglyceridemia. Monitor lipid panel carefully.
Alternative Therapies
- Other Bile Acid Sequestrants (e.g., Colestipol, Colesevelam)
- Statins (HMG-CoA Reductase Inhibitors)
- Ezetimibe (Cholesterol Absorption Inhibitor)
- PCSK9 Inhibitors
- Fibrates (for hypertriglyceridemia, but also some LDL-C lowering)
- Niacin (Nicotinic Acid)
Cost & Coverage
Average Cost:
Varies, typically $50-$150 per 60 packets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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 medication taken, the amount, and the time it occurred.