Cholestyramine Powder (can) 378gm

Manufacturer EPIC 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; Bile Acid Sequestrant
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Pharmacologic Class
Bile Acid Sequestrant
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Pregnancy 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 powder that you mix with water or other liquids and drink. It works in your intestines to help lower high cholesterol levels by removing bile acids from your body. It can also help relieve itching caused by certain liver problems.
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How to Use This Medicine

Taking Your Medication Correctly

To use this medication properly, follow your doctor's instructions and read all the information provided. It's essential to follow the instructions carefully.

Do not take the dry powder. 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 the medication with highly fluid soups, applesauce, or crushed pineapple if preferred.
Unless your doctor advises you to limit fluid intake, drink extra liquids after each dose.
Consult your doctor or pharmacist for guidance on taking this medication with food.

Storing and Disposing of Your Medication

Store the 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.
If you're unsure about the best way to dispose of your medication, consult your pharmacist. You may also have access to drug take-back programs in your area.

What to Do If You Miss a Dose

If you miss a dose, take it as soon as you remember.
However, if it's 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 make up for the missed one.
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Lifestyle & Tips

  • Follow a diet low in saturated fat and cholesterol as recommended by your doctor.
  • Maintain adequate fluid intake (6-8 glasses of water daily) to help prevent constipation, which is a common side effect.
  • Take other medications at least 1 hour before or 4-6 hours after taking cholestyramine to prevent it from binding to and reducing the absorption of other drugs.
  • Mix the powder thoroughly with at least 2-6 ounces (60-180 mL) of water, juice, applesauce, or other non-carbonated liquid. Do not take the powder dry, as it can cause choking.
  • Do not use carbonated beverages for mixing.

Dosing & Administration

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Adult Dosing

Standard Dose: 4 g once or twice daily
Dose Range: 4 - 24 mg

Condition-Specific Dosing:

hyperlipidemia: Initial: 4 g once or twice daily. Maintenance: 8-16 g/day in 1-2 divided doses. Max: 24 g/day.
pruritusDueToPartialBiliaryObstruction: Initial: 4 g once or twice daily. Maintenance: 8-16 g/day in 1-2 divided doses. Max: 24 g/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established (use with caution, individualized)
Child: Hyperlipidemia (6-12 years): 80 mg/kg/day to 160 mg/kg/day in 2-3 divided doses, not to exceed 8 g/day. Pruritus: 240 mg/kg/day in 3 divided doses.
Adolescent: Hyperlipidemia: 80 mg/kg/day to 160 mg/kg/day in 2-3 divided doses, not to exceed 8 g/day. Pruritus: 240 mg/kg/day in 3 divided doses.
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Dose Adjustments

Renal Impairment:

Mild: No adjustment needed (not systemically absorbed)
Moderate: No adjustment needed (not systemically absorbed)
Severe: No adjustment needed (not systemically absorbed); however, caution with prolonged use or high doses due to potential for hyperchloremic acidosis (rare).
Dialysis: No adjustment needed (not systemically absorbed)

Hepatic Impairment:

Mild: No adjustment needed (not systemically absorbed)
Moderate: No adjustment needed (not systemically absorbed)
Severe: No adjustment needed (not systemically absorbed)

Pharmacology

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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 increases the fecal loss of bile acids, leading to an upregulation of hepatic LDL receptors and increased synthesis of bile acids from cholesterol, thereby lowering plasma LDL-C levels. It also reduces bile acid accumulation in the skin, alleviating pruritus.
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Pharmacokinetics

Absorption:

Bioavailability: Negligible (not absorbed)
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. Food does not affect absorption as it is not absorbed.

Distribution:

Vd: Not applicable (not absorbed)
ProteinBinding: Not applicable (not absorbed)
CnssPenetration: No (not absorbed)

Elimination:

HalfLife: Not applicable (not absorbed)
Clearance: Not applicable (not absorbed)
ExcretionRoute: Fecal (as bile acid complex)
Unchanged: 100% (excreted as complex)
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Pharmacodynamics

OnsetOfAction: Days to weeks for lipid-lowering effect; days for pruritus relief.
PeakEffect: Approximately 1 month for maximal lipid-lowering effect.
DurationOfAction: Effects persist as long as therapy continues.

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 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe or persistent constipation
  • Severe stomach pain or bloating
  • Unusual bleeding or bruising (may indicate vitamin K deficiency)
  • Night blindness or difficulty seeing in dim light (may indicate vitamin A deficiency)
  • Bone pain or muscle weakness (may indicate vitamin D deficiency)
  • Dark urine or yellowing of the skin or eyes (jaundice)
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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 allergic reaction you experienced, including any symptoms that occurred.
If you have a blockage in your biliary tract.

This medication may interact with other medications or health conditions. Therefore, it is crucial to provide your doctor and pharmacist with a comprehensive list of:

All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your existing health problems

Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
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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 contain phenylalanine.

Regular blood work and laboratory tests should be conducted as directed by your doctor to monitor your condition. When taking other medications, administer them at least 1 hour before or 4 hours after taking this drug to avoid potential interactions.

Adhere to the diet and exercise plan recommended by your doctor to maximize the benefits of this medication. To minimize the risk of tooth discoloration, avoid sipping this drug 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 by practicing regular dental care and scheduling frequent dental check-ups. This is particularly important to prevent tooth changes, such as discoloration, associated with this medication.

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, plan to become pregnant, or are 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.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Contact a poison control center immediately or seek emergency medical attention. Management is supportive, focusing on relieving constipation and maintaining hydration. Call 1-800-222-1222.

Drug Interactions

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Contraindicated Interactions

  • Complete biliary obstruction (cholestyramine requires bile in the intestine to work)
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Major Interactions

  • Warfarin (decreased absorption, monitor INR closely)
  • Thyroid hormones (e.g., levothyroxine, decreased absorption)
  • Fat-soluble vitamins (A, D, E, K; decreased absorption, may require supplementation)
  • Digoxin (decreased absorption)
  • 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, though clinical significance varies)
  • Phenobarbital (decreased absorption)
  • Tetracyclines (decreased absorption)
  • NSAIDs (e.g., ibuprofen, naproxen; decreased absorption)
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Moderate Interactions

  • Many acidic drugs and drugs with a high molecular weight or that are highly protein-bound (e.g., methotrexate, furosemide, glipizide, sulfonylureas, spironolactone, clofibrate, penicillin G, phosphate supplements, iron salts). Separate administration times.

Monitoring

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Baseline Monitoring

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

Rationale: To establish baseline lipid levels and assess response to therapy.

Timing: Prior to initiation of therapy.

Liver Function Tests (LFTs)

Rationale: To assess baseline liver function, as cholestyramine is used in liver-related pruritus and can rarely affect LFTs.

Timing: Prior to initiation of therapy.

Fat-soluble Vitamin Levels (A, D, E, K)

Rationale: To assess for pre-existing deficiencies and establish baseline for long-term monitoring, especially in patients with malabsorption or poor nutritional status.

Timing: Consider prior to initiation, especially for long-term use.

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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 expected. Target levels vary by patient risk.

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

Liver Function Tests (LFTs)

Frequency: Periodically (e.g., every 6-12 months) or as clinically indicated.

Target: Within normal limits.

Action Threshold: Significant elevations may warrant investigation and dose adjustment or discontinuation.

Fat-soluble Vitamin Levels (A, D, E, K)

Frequency: Periodically (e.g., annually) with long-term use, or if symptoms of deficiency arise.

Target: Within normal limits.

Action Threshold: If levels are low, consider supplementation.

Electrolytes (especially Chloride)

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

Target: Within normal limits.

Action Threshold: Elevated chloride may indicate hyperchloremic acidosis.

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Symptom Monitoring

  • Constipation (most common side effect)
  • Abdominal pain, bloating, gas, nausea, vomiting
  • Symptoms of fat-soluble vitamin deficiency (e.g., easy bruising/bleeding for Vitamin K, night blindness for Vitamin A, bone pain for Vitamin D, neurological symptoms for Vitamin E)
  • Unusual bleeding or bruising (due to Vitamin K deficiency)
  • Dark urine, yellowing of skin/eyes (if used for pruritus, monitor for worsening liver function)

Special Patient Groups

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Pregnancy

Category C. While not systemically absorbed, cholestyramine can interfere with the absorption of fat-soluble vitamins (A, D, E, K) and folic acid, which are essential for fetal development. Supplementation of these vitamins may be necessary during pregnancy if cholestyramine is used.

Trimester-Specific Risks:

First Trimester: Potential for vitamin deficiencies (especially folate) which are critical in early development. Supplementation may be required.
Second Trimester: Continued risk of maternal fat-soluble vitamin deficiencies. Monitor and supplement as needed.
Third Trimester: Continued risk of maternal fat-soluble vitamin deficiencies, particularly vitamin K, which could impact neonatal coagulation. Supplementation may be necessary.
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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 reduce 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 the mother is on high doses or long-term therapy.

Infant Risk: Low risk of direct exposure. Potential for indirect risk if maternal vitamin deficiencies impact breast milk quality. Monitor infant for adequate growth and signs of vitamin deficiency.
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Pediatric Use

Used in children for familial hypercholesterolemia. Dosing is weight-based and individualized. Close monitoring of growth, development, and fat-soluble vitamin levels is crucial due to the potential for malabsorption. Constipation is a common concern.

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Geriatric Use

Use with caution due to increased susceptibility to constipation and potential for fecal impaction. Start with lower doses and titrate slowly. Monitor for fat-soluble vitamin deficiencies and ensure adequate fluid intake.

Clinical Information

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Clinical Pearls

  • Always mix cholestyramine powder thoroughly with liquid (water, juice, applesauce, etc.) before ingestion. Never take the powder dry, as it can cause esophageal irritation or choking.
  • To minimize gastrointestinal side effects (e.g., constipation, bloating), start with a low dose and gradually increase it. Ensure adequate fluid intake.
  • Space administration of other medications (especially those with narrow therapeutic windows or that are highly protein-bound) at least 1 hour before or 4-6 hours after cholestyramine to prevent drug interactions due to binding.
  • Long-term use may lead to deficiencies of fat-soluble vitamins (A, D, E, K) and folic acid. Supplementation may be necessary.
  • Cholestyramine can sometimes cause an increase in triglyceride levels, especially in patients with pre-existing hypertriglyceridemia. Monitor triglyceride levels closely.
  • While not systemically absorbed, rare cases of hyperchloremic acidosis have been reported, particularly with high doses or in patients with renal impairment.
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Alternative Therapies

  • Statins (HMG-CoA reductase inhibitors) for hyperlipidemia (e.g., atorvastatin, simvastatin)
  • Ezetimibe (cholesterol absorption inhibitor) for hyperlipidemia
  • PCSK9 inhibitors (e.g., evolocumab, alirocumab) for severe hyperlipidemia
  • Fibrates (e.g., gemfibrozil, fenofibrate) for hypertriglyceridemia
  • Niacin (nicotinic acid) for dyslipidemia
  • Rifampin, ursodiol, naltrexone for pruritus associated with cholestasis
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Cost & Coverage

Average Cost: Varies widely, typically $50-$200 per 378g can (approx. 42 doses of 9g)
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (preferred 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 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 happened.