Cholestyramine Light Powder (can)

Manufacturer TAGI PHARMA Active Ingredient Cholestyramine Resin(koe LES teer a meen REZ in) Pronunciation koe LES teer a meen REZ in
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.
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Drug Class
Antilipemic Agent
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Pharmacologic Class
Bile Acid Sequestrant
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Pregnancy Category
Category C
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FDA Approved
Jan 1973
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Cholestyramine is a medication that helps lower high cholesterol levels in your blood. It works by binding to certain substances called bile acids in your intestines, 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 'bad' cholesterol (LDL-C). It can also help relieve itching caused by certain liver conditions.
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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 as directed.

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 to ensure you receive the full dose.
You can also mix this medication with highly fluid soups, applesauce, or crushed pineapple to facilitate ingestion.
Unless your doctor advises you to limit fluid intake, drink extra liquids after each dose to help your body absorb the medication.
Consult your doctor or pharmacist for guidance on taking this medication with food.

Storing and Disposing of Your Medication

To maintain the medication's potency and ensure safety:

Store the medication at room temperature in a dry place, avoiding bathrooms and areas prone to moisture.
Keep all medications in a secure 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.
If you have questions about disposing of medications, consult your pharmacist, who can provide information on drug take-back programs in your area.

Missing a Dose

If you miss a dose, take it as soon as you remember. However:

If the missed dose 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.
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Lifestyle & Tips

  • Maintain a healthy diet low in saturated and trans fats, and cholesterol.
  • Engage in regular physical activity.
  • Mix the powder thoroughly with water or other non-carbonated beverages (e.g., fruit juice, milk, applesauce) before taking. Do not take the powder dry.
  • Take other medications at least 1 hour before or 4-6 hours after cholestyramine to prevent interactions and ensure proper absorption of other drugs.
  • Increase fluid intake and dietary fiber to help prevent or manage constipation, a common side effect.

Dosing & Administration

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Adult Dosing

Standard Dose: 4 g (1 scoop/packet) once or twice daily, mixed with liquid. May increase to 8-16 g/day in 2 divided doses.
Dose Range: 4 - 24 mg

Condition-Specific Dosing:

Primary Hypercholesterolemia: Initial: 4 g once or twice daily. Maintenance: 8-16 g/day in 2 divided doses. Max: 24 g/day.
Pruritus associated with partial biliary obstruction: 4-8 g/day in 2-3 divided doses.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Dosing is individualized based on age, weight, and severity of hypercholesterolemia. Typical starting dose: 80 mg/kg/day in 2-3 divided doses. Max: 240 mg/kg/day or 8 g/day, whichever is less.
Adolescent: Similar to adult dosing, individualized based on response and tolerability. Typical starting dose: 4 g once or twice daily. Max: 24 g/day.
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Dose Adjustments

Renal Impairment:

Mild: No adjustment needed
Moderate: No adjustment needed
Severe: No adjustment needed
Dialysis: No adjustment needed, as cholestyramine is not absorbed systemically.

Hepatic Impairment:

Mild: No adjustment needed
Moderate: No adjustment needed
Severe: Use with caution. While not hepatically metabolized, severe hepatic impairment may predispose to vitamin K deficiency and increased bleeding risk due to malabsorption. Monitor prothrombin time/INR.

Pharmacology

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Mechanism of Action

Cholestyramine resin is an anion-exchange resin that binds bile acids in the intestinal lumen, forming an insoluble complex. This complex is then excreted in the feces, preventing the enterohepatic reabsorption of bile acids. The depletion of the bile acid pool stimulates the hepatic synthesis of bile acids from cholesterol, leading to an upregulation of hepatic LDL receptors. This increases the clearance of LDL-cholesterol from the plasma, thereby lowering serum LDL-C levels.
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Pharmacokinetics

Absorption:

Bioavailability: Not absorbed (0%)
Tmax: Not applicable (not absorbed)
FoodEffect: Can be taken with or without food. Taking with meals may improve palatability and reduce gastrointestinal side effects.

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 bile acid-resin complex)
Unchanged: 100% (as bile acid-resin complex)
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Pharmacodynamics

OnsetOfAction: Within 24-48 hours (for bile acid binding)
PeakEffect: Reduction in LDL-C typically observed within 1 month of therapy initiation.
DurationOfAction: Continues as long as therapy is maintained.
Confidence: High

Safety & Warnings

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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 indicate 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 persist, contact your doctor for guidance:

Constipation: Increasing fluid intake, 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe or persistent constipation
  • Severe stomach pain or bloating
  • Unusual bleeding or bruising
  • Dark urine or yellowing of skin/eyes (jaundice)
  • Muscle weakness or bone pain
  • Night blindness
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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 as a result of the allergy.
If you have a blockage in your biliary tract.

This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other medications and health issues.

Remember, do not start, stop, or modify the dosage of any medication without first consulting your doctor to ensure your safety.
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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 performed as directed by your doctor to monitor your condition. When taking other medications, allow 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 ensure optimal management of your condition. To avoid dental discoloration or other tooth changes, avoid sipping this medication after mixing or holding it in your mouth for an extended period. If you have concerns, discuss them with your doctor.

Maintain good oral hygiene and schedule regular dental check-ups to prevent potential dental issues. If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.

Although rare, bowel obstruction has occurred in children taking this medication, and in some cases, it has been fatal. If you have questions or concerns, consult with your doctor. Additionally, if you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe constipation
  • Intestinal obstruction (rare, but possible with very large doses)

What to Do:

Contact a poison control center or emergency medical services immediately. Management is primarily supportive, focusing on relieving constipation and maintaining hydration. Intestinal obstruction may require medical intervention. Call 1-800-222-1222 (Poison Control).

Drug Interactions

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Major Interactions

  • Warfarin (increased risk of bleeding due to vitamin K malabsorption)
  • Thyroid hormones (e.g., Levothyroxine - reduced absorption)
  • Digoxin (reduced absorption)
  • Fat-soluble vitamins (A, D, E, K - reduced absorption, especially with long-term use)
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Moderate Interactions

  • Thiazide diuretics (e.g., Hydrochlorothiazide - reduced absorption)
  • Beta-blockers (e.g., Propranolol - reduced absorption)
  • Oral contraceptives (reduced absorption of estrogen/progestin components)
  • Phenobarbital (reduced absorption)
  • Ursodiol (reduced absorption)
  • Mycophenolate mofetil (reduced absorption)
  • Methotrexate (reduced absorption)
  • Statins (e.g., Atorvastatin - reduced absorption, though often used together with careful timing)
  • Fibrates (e.g., Gemfibrozil - reduced absorption)
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Minor Interactions

  • Nonsteroidal anti-inflammatory drugs (NSAIDs - potential for reduced absorption of some)

Monitoring

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Baseline Monitoring

Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)

Rationale: To establish baseline lipid levels and assess the need for therapy.

Timing: Prior to initiation of therapy.

Liver Function Tests (ALT, AST, Alk Phos, Bilirubin)

Rationale: To assess baseline hepatic function, although cholestyramine is not hepatically metabolized, it's good practice for lipid-lowering therapy.

Timing: Prior to initiation of therapy.

Prothrombin Time (PT) / International Normalized Ratio (INR)

Rationale: Especially if patient is on warfarin or has pre-existing coagulopathy, due to potential for vitamin K malabsorption.

Timing: Prior to initiation of therapy.

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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 LDL-C based on patient's cardiovascular risk.

Action Threshold: If target LDL-C not achieved, consider dose adjustment or combination therapy. If triglycerides significantly increase (>400 mg/dL), re-evaluate therapy.

Fat-soluble vitamin levels (A, D, E, K)

Frequency: Periodically, especially with long-term use or high doses.

Target: Within normal limits.

Action Threshold: Supplementation may be required if deficiencies are noted.

Prothrombin Time (PT) / International Normalized Ratio (INR)

Frequency: Regularly, especially if on warfarin or with signs of bleeding.

Target: Therapeutic range for warfarin, or within normal limits.

Action Threshold: Adjust warfarin dose or supplement vitamin K if INR is elevated or signs of bleeding occur.

Serum Chloride and Bicarbonate

Frequency: Periodically, especially in patients with renal impairment or on high doses.

Target: Within normal limits.

Action Threshold: Monitor for hyperchloremic acidosis.

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Symptom Monitoring

  • Constipation (most common)
  • Abdominal pain or discomfort
  • Bloating
  • Flatulence
  • Nausea
  • Steatorrhea (fatty stools)
  • Unusual bleeding or bruising (signs of vitamin K deficiency)
  • Muscle weakness or bone pain (signs of vitamin D deficiency)
  • Night blindness (signs of vitamin A deficiency)

Special Patient Groups

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Pregnancy

Category C. 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, which are crucial for fetal development. If used during pregnancy, vitamin supplementation may be necessary. Use only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Risk of vitamin deficiencies (especially folate) important for neural tube development.
Second Trimester: Risk of vitamin deficiencies affecting fetal growth and development.
Third Trimester: Risk of vitamin K deficiency in the mother, potentially affecting neonatal coagulation.
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Lactation

L3 (Moderately Safe). Cholestyramine is not absorbed systemically 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 maternal vitamin status and consider supplementation if needed.

Infant Risk: Low direct risk to infant. Indirect risk from potential maternal vitamin deficiencies affecting milk quality.
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Pediatric Use

Used in children for familial hypercholesterolemia, but dosing must be carefully individualized based on age, weight, and lipid levels. Long-term use requires monitoring for fat-soluble vitamin deficiencies and growth. Constipation is a common concern.

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Geriatric Use

No specific dose adjustment needed based on age. However, elderly patients may be more susceptible to constipation and its complications (e.g., fecal impaction). Ensure adequate fluid and fiber intake. Monitor for vitamin deficiencies and drug interactions, as polypharmacy is common.

Clinical Information

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Clinical Pearls

  • Always mix the powder thoroughly with at least 2-6 ounces of water or other non-carbonated liquid (e.g., fruit juice, milk, applesauce) before ingestion. Do not take the powder dry, as it can cause choking or esophageal irritation.
  • To minimize gastrointestinal side effects (especially constipation), start with a low dose and gradually titrate upwards. Encourage increased fluid and fiber intake.
  • Timing of administration is crucial for drug interactions: administer other medications at least 1 hour before or 4-6 hours after cholestyramine.
  • Cholestyramine can increase triglyceride levels in some patients. Monitor triglycerides, especially if baseline levels are high.
  • Long-term use may necessitate supplementation of fat-soluble vitamins (A, D, E, K) and folic acid.
  • The 'light' formulation contains aspartame and should be used with caution in patients with phenylketonuria (PKU).
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Alternative Therapies

  • Other Bile Acid Sequestrants (e.g., Colestipol, Colesevelam)
  • Statins (HMG-CoA reductase inhibitors - e.g., Atorvastatin, Rosuvastatin)
  • Ezetimibe (Cholesterol absorption inhibitor)
  • PCSK9 Inhibitors (e.g., Alirocumab, Evolocumab)
  • Fibrates (e.g., Gemfibrozil, Fenofibrate - primarily for triglycerides)
  • Niacin (Nicotinic acid - for various lipid abnormalities)
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Cost & Coverage

Average Cost: $50 - $200 per 240g can (approx. 60 doses)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (Generic)
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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 this 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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.