Cholestyramine Powder(can) 368.76gm

Manufacturer ASCEND LABORATORIES 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
Category C
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FDA Approved
Aug 1964
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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. Your liver then has to use more cholesterol to make new bile acids, which helps lower the cholesterol in your blood. 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 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

  • Mix the powder with water or other non-carbonated beverages (e.g., fruit juice, milk), or with soft foods (e.g., applesauce, yogurt). Do not take it dry.
  • Take other medications at least 1 hour before or 4-6 hours after cholestyramine to prevent interactions.
  • Maintain a low-cholesterol, low-saturated fat diet as recommended by your doctor.
  • Increase fiber and fluid intake to help manage potential constipation.
  • Regular exercise is beneficial for cholesterol management.

Dosing & Administration

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Adult Dosing

Standard Dose: 4 grams (1 packet or scoopful) 1-2 times daily
Dose Range: 4 - 24 mg

Condition-Specific Dosing:

Hyperlipidemia: Initial: 4 grams once or twice daily. Maintenance: 8-16 grams/day in 1-2 divided doses. Max: 24 grams/day.
Pruritus due to partial biliary obstruction: 4-8 grams/day in 2-3 divided doses. Max: 24 grams/day.
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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: 240 mg/kg/day in 2-3 divided doses, not to exceed 8 grams/day.
Adolescent: Similar to adult dosing, individualized based on weight and condition.
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Dose Adjustments

Renal Impairment:

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

Hepatic Impairment:

Mild: No adjustment needed
Moderate: No adjustment needed
Severe: No adjustment needed

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 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 process upregulates hepatic LDL receptors, leading to increased clearance of LDL-cholesterol from the blood.
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Pharmacokinetics

Absorption:

Bioavailability: 0%
Tmax: Not applicable (not absorbed)
FoodEffect: Can be taken with meals to improve palatability and reduce GI side effects, 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: Feces (as insoluble complex with bile acids)
Unchanged: 100%
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Pharmacodynamics

OnsetOfAction: Within 24-48 hours for bile acid binding; lipid-lowering effects typically seen within 4-7 days.
PeakEffect: Maximum lipid-lowering effect usually observed within 1-3 weeks.
DurationOfAction: Effects persist as long as therapy is continued.

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 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe or persistent constipation
  • Severe stomach pain or bloating
  • Unusual bleeding or bruising
  • Night blindness
  • Bone pain or muscle weakness
  • Dark urine or yellowing of skin/eyes (if used for pruritus, may indicate worsening liver condition)
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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.
If you have a blockage in your biliary tract.

This is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to discuss 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.

To ensure your safety, carefully review all your medications and health conditions with your doctor before taking this drug. Never start, stop, or change the dose of any medication without first consulting your doctor.
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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, ensure that you take 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 recommended to swallow this drug promptly after mixing and avoid holding it in your mouth for an extended period. If you have concerns, discuss them with your doctor.

Maintaining good oral hygiene is crucial; therefore, practice good 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.
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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. Treatment is generally supportive, focusing on relieving constipation and maintaining hydration. Call 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Thyroid hormones (e.g., levothyroxine): Decreased absorption of thyroid hormones. Administer at least 4-6 hours apart.
  • Warfarin: Decreased absorption of warfarin, potentially leading to reduced anticoagulant effect. Monitor INR closely.
  • Digoxin: Decreased absorption of digoxin. Administer at least 4-6 hours apart.
  • Fat-soluble vitamins (A, D, E, K): Decreased absorption. Consider supplementation, especially with long-term use.
  • Folic acid: Decreased absorption. Consider supplementation.
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Moderate Interactions

  • Thiazide diuretics (e.g., hydrochlorothiazide): Decreased absorption. Administer at least 4 hours apart.
  • Beta-blockers (e.g., propranolol): Decreased absorption. Administer at least 4 hours apart.
  • Oral contraceptives: Potential for decreased absorption. Administer at least 4 hours apart.
  • Phenobarbital: Decreased absorption. Administer at least 4 hours apart.
  • Statins (e.g., pravastatin, fluvastatin): Decreased absorption. Administer at least 4 hours apart.
  • Mycophenolate mofetil: Decreased absorption. Avoid concomitant use if possible or separate by several hours.
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Minor Interactions

  • Nonsteroidal anti-inflammatory drugs (NSAIDs): Potential for decreased absorption.
  • Iron supplements: Potential for decreased absorption.

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)

Rationale: To assess baseline liver function, although cholestyramine is not hepatically metabolized.

Timing: Prior to initiation of therapy.

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

Rationale: To assess baseline nutritional status, especially if long-term therapy is anticipated.

Timing: Prior to initiation of therapy.

Prothrombin Time (PT/INR)

Rationale: To assess baseline coagulation, especially if patient is on anticoagulants or at risk for vitamin K deficiency.

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: Individualized based on patient risk factors and guidelines (e.g., LDL-C <100 mg/dL or <70 mg/dL).

Action Threshold: If target levels not met, 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 (e.g., annually or as clinically indicated).

Target: Within normal limits.

Action Threshold: If levels are low, recommend supplementation.

Folic acid levels

Frequency: Periodically, especially with long-term use.

Target: Within normal limits.

Action Threshold: If levels are low, recommend supplementation.

Prothrombin Time (PT/INR)

Frequency: Periodically, especially if patient is on anticoagulants or develops signs of bleeding.

Target: Individualized based on anticoagulant therapy.

Action Threshold: If INR is unstable or prolonged, investigate vitamin K deficiency.

Electrolytes (especially chloride)

Frequency: Periodically, if symptoms of hyperchloremic acidosis develop.

Target: Within normal limits.

Action Threshold: If hyperchloremia or acidosis develops, investigate cause and manage appropriately.

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Symptom Monitoring

  • Constipation
  • Bloating
  • Abdominal pain
  • Nausea
  • Vomiting
  • Heartburn
  • Steatorrhea (fatty stools)
  • Unusual bleeding or bruising (signs of vitamin K deficiency)
  • Night blindness (sign of vitamin A deficiency)
  • Bone pain or weakness (signs of vitamin D deficiency)
  • Muscle weakness or neurological symptoms (signs of vitamin E deficiency)

Special Patient Groups

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Pregnancy

Cholestyramine is not absorbed systemically, so it is generally considered low risk for direct fetal harm. However, it can interfere with the absorption of fat-soluble vitamins (A, D, E, K) and folic acid, which are crucial during pregnancy. Supplementation may be necessary. Use only if clearly needed and benefits outweigh potential risks.

Trimester-Specific Risks:

First Trimester: Potential for vitamin deficiencies if not supplemented.
Second Trimester: Potential for vitamin deficiencies if not supplemented.
Third Trimester: Potential for vitamin deficiencies, especially vitamin K, which could affect neonatal coagulation.
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Lactation

Cholestyramine is not absorbed systemically by the mother, so it is not expected to be excreted into breast milk. However, it can interfere with maternal absorption of fat-soluble vitamins, which could theoretically impact the nutritional content of breast milk. Monitor maternal vitamin status. Generally considered compatible with breastfeeding with appropriate vitamin supplementation.

Infant Risk: Low risk of direct infant exposure. Potential for indirect impact on breast milk vitamin content.
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Pediatric Use

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

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Geriatric Use

No specific dose adjustment is required. Elderly patients may be more susceptible to constipation and its complications (e.g., fecal impaction). Increased fluid and fiber intake is important. Monitor for vitamin deficiencies.

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/soft food before ingestion to prevent esophageal irritation or choking.
  • To minimize GI side effects like constipation, start with a low dose and gradually titrate up. Advise patients to increase fluid and fiber intake.
  • Administer other medications at least 1 hour before or 4-6 hours after cholestyramine to avoid drug interactions due to binding.
  • Long-term use necessitates monitoring and potential supplementation of fat-soluble vitamins (A, D, E, K) and folic acid.
  • Cholestyramine can increase triglyceride levels in some patients; monitor lipid panel regularly, especially triglycerides.
  • It is also used off-label for C. difficile-associated diarrhea (CDAD) due to its ability to bind toxins, though evidence is limited and it's not a primary treatment.
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Alternative Therapies

  • Other Bile Acid Sequestrants: Colestipol, Colesevelam (less GI side effects, fewer drug interactions)
  • Statins (HMG-CoA Reductase Inhibitors): Atorvastatin, Rosuvastatin, Simvastatin (first-line for hyperlipidemia)
  • Ezetimibe (Cholesterol Absorption Inhibitor)
  • PCSK9 Inhibitors: Alirocumab, Evolocumab
  • Fibrates: Gemfibrozil, Fenofibrate (primarily for hypertriglyceridemia)
  • Niacin (Nicotinic Acid)
  • For pruritus: Rifampin, Naltrexone, Ursodeoxycholic acid (for cholestatic pruritus)
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Cost & Coverage

Average Cost: $50 - $200 per 368.76gm can (approx. 42 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 details. 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 information about the medication taken, the amount, and the time it happened.