Cholestyramine 4gm Lght Pow Pk 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
Category C
FDA Approved
Jan 1973
DEA Schedule
Not Controlled
Overview
What is this medicine?
Cholestyramine is a medication used to lower high cholesterol levels in the blood and to relieve itching caused by certain liver conditions. It works by binding to bile acids in your intestines, which helps your body remove more 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. Take this medication exactly as directed, and be sure to follow all instructions carefully.
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 the rinse to ensure you receive the full dose. You can also mix this medication with highly fluid soups, applesauce, or crushed pineapple to facilitate ingestion.
After each dose, drink extra liquids 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 of medications, consult with your pharmacist, who can 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 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, and be sure to follow all instructions carefully.
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 the rinse to ensure you receive the full dose. You can also mix this medication with highly fluid soups, applesauce, or crushed pineapple to facilitate ingestion.
After each dose, drink extra liquids 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 of medications, consult with your pharmacist, who can 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 a missed dose.
Lifestyle & Tips
- Follow a low-cholesterol, low-fat diet as recommended by your doctor.
- Engage in regular physical activity.
- Maintain adequate hydration to help prevent constipation.
- Mix the powder thoroughly with water, juice, or other non-carbonated beverages (at least 2-6 ounces) 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.
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 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.
pruritus_due_to_partial_biliary_obstruction:
4 g 1-2 times daily. May increase to 4-8 g/day in 2-3 divided doses. Max: 24 g/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Hyperlipidemia: 240 mg/kg/day in 2-3 divided doses (max 8 g/day). Pruritus: Dosing individualized, often 240 mg/kg/day in 2-3 divided doses.
Adolescent:
Hyperlipidemia: 240 mg/kg/day in 2-3 divided doses (max 8 g/day). Pruritus: Dosing individualized, often 240 mg/kg/day in 2-3 divided doses.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed; not systemically absorbed.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
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, which in turn upregulates hepatic LDL receptors, leading to increased clearance of LDL cholesterol from the blood.
Pharmacokinetics
Absorption:
Bioavailability:
0%
Tmax:
Not applicable (not absorbed)
FoodEffect:
Can be taken with or without food, but usually with meals to minimize GI 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
Unchanged:
100%
Pharmacodynamics
OnsetOfAction:
Within 24-48 hours (for bile acid binding)
PeakEffect:
Several weeks for maximal lipid-lowering effect
DurationOfAction:
Dependent on continued administration
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. Immediately contact your doctor or seek medical attention if you experience any of the following symptoms, which may indicate a serious allergic reaction or other severe side effect:
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 do not experience any side effects or only have mild ones, it is 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 for advice:
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. 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. Immediately contact your doctor or seek medical attention if you experience any of the following symptoms, which may indicate a serious allergic reaction or other severe side effect:
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 do not experience any side effects or only have mild ones, it is 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 for advice:
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. 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
- Unusual bleeding or bruising
- Black, tarry stools
- Severe stomach pain
- Nausea or vomiting that doesn't go away
- Signs of vitamin deficiency (e.g., night blindness, bone pain, muscle weakness)
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 list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing health conditions and other medications.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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 list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing health conditions and other medications.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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, 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 optimize the effectiveness of this medication. To avoid tooth discoloration and other dental changes, 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 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 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, 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 optimize the effectiveness of this medication. To avoid tooth discoloration and other dental changes, 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 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 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)
What to Do:
Contact a poison control center or emergency medical services immediately. For the U.S., call 1-800-222-1222. Treatment is generally supportive, focusing on managing constipation and maintaining hydration.
Drug Interactions
Major Interactions
- Warfarin (decreased absorption, increased risk of bleeding)
- Digoxin (decreased absorption, reduced therapeutic effect)
- Thyroid hormones (e.g., levothyroxine) (decreased absorption)
- Fat-soluble vitamins (A, D, E, K) (decreased absorption, potential for deficiency)
Moderate Interactions
- Thiazide diuretics (e.g., hydrochlorothiazide) (decreased absorption)
- Beta-blockers (e.g., propranolol) (decreased absorption)
- Oral contraceptives (potential for decreased efficacy)
- Phenobarbital (decreased absorption)
- Methotrexate (decreased absorption)
- Mycophenolate mofetil (decreased absorption)
- Ursodiol (decreased absorption)
- Statins (potential for decreased absorption, though less significant than other drugs)
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess treatment efficacy.
Timing: Prior to initiation of therapy
Liver Function Tests (ALT, AST, ALP, Bilirubin)
Rationale: To assess baseline hepatic function and monitor for potential liver enzyme elevations (rare).
Timing: Prior to initiation of therapy
Prothrombin Time (PT) / International Normalized Ratio (INR)
Rationale: To assess baseline coagulation status, especially if patient is at risk for vitamin K deficiency or on anticoagulants.
Timing: Prior to initiation of therapy
Fat-soluble Vitamin Levels (A, D, E, K)
Rationale: To assess baseline levels due to potential for malabsorption.
Timing: Prior to initiation of therapy (consider if long-term use or risk factors)
Routine Monitoring
Lipid Panel
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 lower)
Action Threshold: Failure to achieve target lipid levels, significant increase in triglycerides (cholestyramine can increase TGs)
Liver Function Tests
Frequency: Periodically (e.g., every 6-12 months) or as clinically indicated
Target: Within normal limits
Action Threshold: Significant or persistent elevations
Prothrombin Time (PT) / INR
Frequency: Regularly, especially if on warfarin or long-term therapy
Target: Therapeutic range for warfarin (if applicable); otherwise, within normal limits
Action Threshold: Prolonged PT/elevated INR, signs of bleeding
Fat-soluble Vitamin Levels
Frequency: Periodically (e.g., annually) for long-term therapy or if symptoms of deficiency
Target: Within normal limits
Action Threshold: Evidence of deficiency; consider supplementation
Electrolytes (especially Chloride)
Frequency: Periodically, if high doses or long-term use, to monitor for hyperchloremic acidosis
Target: Within normal limits
Action Threshold: Elevated chloride, decreased bicarbonate
Symptom Monitoring
- Constipation (most common GI side effect)
- Abdominal discomfort, bloating, flatulence, nausea, vomiting
- Unusual bleeding or bruising (signs of vitamin K deficiency)
- Night blindness (signs 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
Pregnancy
Generally considered safe due to lack of systemic absorption, but potential for malabsorption of fat-soluble vitamins (especially vitamin K) and folic acid exists, which could affect the mother and fetus. Supplementation may be necessary.
Trimester-Specific Risks:
First Trimester:
Low systemic risk; monitor for vitamin deficiencies.
Second Trimester:
Low systemic risk; monitor for vitamin deficiencies.
Third Trimester:
Low systemic risk; monitor for vitamin deficiencies, particularly vitamin K, which is crucial for fetal coagulation.
Lactation
Considered safe for use during breastfeeding as it is not absorbed systemically and therefore not excreted in breast milk. However, monitor for potential maternal vitamin deficiencies.
Infant Risk:
Low risk to infant.
Pediatric Use
Used in children for hyperlipidemia and pruritus. Dosing is weight-based. Monitor for growth, development, and fat-soluble vitamin deficiencies, especially with long-term use.
Geriatric Use
Use with caution in elderly patients due to increased risk of constipation and potential for fecal impaction. Start with lower doses and titrate slowly. Monitor hydration status and bowel function closely. Consider potential for polypharmacy and drug interactions.
Clinical Information
Clinical Pearls
- Always mix the powder thoroughly with liquid (water, juice, applesauce, etc.) to prevent esophageal irritation or choking. Do not take dry.
- Advise patients to take other medications at least 1 hour before or 4-6 hours after cholestyramine to minimize drug interactions.
- Constipation is the most common side effect; encourage adequate fluid intake and dietary fiber. Stool softeners or laxatives may be necessary.
- Cholestyramine can increase triglyceride levels in some patients; monitor lipid panel regularly.
- Long-term use may require supplementation of fat-soluble vitamins (A, D, E, K) and folic acid.
- It can be used off-label for C. difficile-associated diarrhea (CDAD) due to its bile acid binding properties, though evidence is limited and it should not replace standard CDAD treatment.
Alternative Therapies
- Other bile acid sequestrants (e.g., colesevelam, colestipol)
- Statins (HMG-CoA reductase inhibitors) for hyperlipidemia
- Ezetimibe (cholesterol absorption inhibitor) for hyperlipidemia
- PCSK9 inhibitors for severe hyperlipidemia
- Fibrates (for hypertriglyceridemia, but not primary LDL-C lowering)
- Niacin (for dyslipidemia, but less commonly used due to side effects)
- Rifampin (for pruritus due to cholestasis, by inducing hepatic enzymes)
- Naltrexone (for pruritus due to cholestasis, opioid antagonist)
Cost & Coverage
Average Cost:
Varies widely, typically $50-$200 per 60 packets (4g each)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 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 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 overdose, including the medication taken, the amount, and the time it occurred.