Colestipol 5gm Granule Packets 90's
It is used to lower cholesterol.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
Aug 1977
DEA Schedule
Not Controlled
Overview
What is this medicine?
Colestipol is a medication used to 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 lower your 'bad' cholesterol (LDL-C). It comes as granules that you mix with liquid or soft food before taking.
How to Use This Medicine
Taking Your Medication Correctly
To use this medication safely and effectively, follow your doctor's instructions and the information provided with your prescription. Take the medication as directed, and be sure to read all accompanying materials carefully.
When taking this medication, do not ingest the dry powder. Instead, mix it with at least 3 ounces (90 mL) of water or another liquid, and then drink the mixture. After consuming the medication, rinse the glass with additional liquid and drink it to ensure you receive the full dose. Alternatively, you can mix the medication with foods like cereals, soups, or fruits such as applesauce or crushed pineapple, following the specific mixing instructions provided to you.
It is essential to stay hydrated while taking this medication, so drink plenty of non-caffeinated liquids unless your doctor advises you to limit your fluid intake.
Storing and Disposing of Your Medication
Store your 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. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your doctor or pharmacist. If you have questions about the proper disposal method, consult 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 make up for a missed dose.
To use this medication safely and effectively, follow your doctor's instructions and the information provided with your prescription. Take the medication as directed, and be sure to read all accompanying materials carefully.
When taking this medication, do not ingest the dry powder. Instead, mix it with at least 3 ounces (90 mL) of water or another liquid, and then drink the mixture. After consuming the medication, rinse the glass with additional liquid and drink it to ensure you receive the full dose. Alternatively, you can mix the medication with foods like cereals, soups, or fruits such as applesauce or crushed pineapple, following the specific mixing instructions provided to you.
It is essential to stay hydrated while taking this medication, so drink plenty of non-caffeinated liquids unless your doctor advises you to limit your fluid intake.
Storing and Disposing of Your Medication
Store your 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. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your doctor or pharmacist. If you have questions about the proper disposal method, consult 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 make up for a missed dose.
Lifestyle & Tips
- Follow a cholesterol-lowering diet as recommended by your doctor (e.g., low in saturated fat and cholesterol).
- Engage in regular physical activity.
- Maintain a healthy weight.
- Avoid smoking.
- Limit alcohol intake.
- Ensure adequate fluid intake to help prevent constipation.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
5 grams once or twice daily, mixed with liquid or food
Dose Range:
5 - 30 mg
Condition-Specific Dosing:
hypercholesterolemia:
Initial: 5 grams once or twice daily. Maintenance: 5 to 30 grams per day, given in 1 to 6 divided doses. Max: 30 grams/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established, but has been used off-label. Dosing typically 10-20 grams/day in divided doses, adjusted based on response and tolerability.
Adolescent:
Not established, but has been used off-label. Dosing typically 10-20 grams/day in divided doses, adjusted based on response and tolerability.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed, as colestipol is not absorbed systemically.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Pharmacology
Mechanism of Action
Colestipol hydrochloride is an insoluble, non-absorbable anion-exchange resin that binds bile acids in the intestine, 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 increased demand for cholesterol in the liver results in an upregulation of hepatic LDL receptors, leading to increased clearance of LDL-cholesterol from the blood.
Pharmacokinetics
Absorption:
Bioavailability:
Negligible (not absorbed)
Tmax:
Not applicable (not absorbed)
FoodEffect:
Should be taken with meals or mixed with liquids/foods.
Distribution:
Vd:
Not applicable (not absorbed)
ProteinBinding:
Not applicable (not absorbed)
CnssPenetration:
No
Elimination:
HalfLife:
Not applicable (not absorbed)
Clearance:
Not applicable (excreted unchanged in feces)
ExcretionRoute:
Fecal
Unchanged:
100%
Pharmacodynamics
OnsetOfAction:
Within 1-2 weeks for lipid-lowering effects
PeakEffect:
Approximately 1 month for maximal lipid-lowering effect
DurationOfAction:
Continues as long as therapy is maintained
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
If you experience any of the following symptoms, call your doctor or seek medical attention immediately, as they may be signs of a severe and potentially life-threatening reaction:
- 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, or swelling of the mouth, face, lips, tongue, or throat
- Difficulty swallowing
- Unexplained bruising or bleeding
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor if you experience any of the following side effects or if they persist or bother you:
- Gastrointestinal issues: constipation, diarrhea, stomach pain, upset stomach, or vomiting
- Heartburn
- Stomach cramps
- Gas
- Muscle or joint pain
- Headache
Reporting Side Effects
This list does not include all possible side effects. 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.
If you experience any of the following symptoms, call your doctor or seek medical attention immediately, as they may be signs of a severe and potentially life-threatening reaction:
- 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, or swelling of the mouth, face, lips, tongue, or throat
- Difficulty swallowing
- Unexplained bruising or bleeding
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor if you experience any of the following side effects or if they persist or bother you:
- Gastrointestinal issues: constipation, diarrhea, stomach pain, upset stomach, or vomiting
- Heartburn
- Stomach cramps
- Gas
- Muscle or joint pain
- Headache
Reporting Side Effects
This list does not include all possible side effects. 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.
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 vision changes (may indicate vitamin A deficiency)
- Bone pain or muscle weakness (may indicate vitamin D deficiency)
- Unexplained fatigue or 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 as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor identify potential interactions between this medication and other substances.
* Any health problems you have, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication is compatible with all your medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor. By sharing this information, you can help your doctor make informed decisions about your treatment and minimize potential risks.
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.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor identify potential interactions between this medication and other substances.
* Any health problems you have, as this medication may interact with certain conditions.
To ensure your safety, it is crucial to verify that this medication is compatible with all your medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor. By sharing this information, you can help your doctor make informed decisions about your treatment and minimize potential risks.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions with your doctor.
To manage your condition effectively, follow the personalized diet and exercise plan recommended by your doctor. If you experience constipation, increasing your fluid intake, engaging in regular physical activity, or adding more fiber to your diet may help alleviate symptoms. However, consult with your doctor before making any changes.
When taking this medication, it is crucial to administer other medications at least 1 hour before or 4 hours after taking this drug to minimize potential interactions.
Long-term use of this medication may lead to low vitamin K levels, increasing the risk of bleeding. If you have concerns or questions, discuss them with your doctor. Additionally, if you have hemorrhoids, inform your doctor, as this medication may exacerbate the condition.
If you have phenylketonuria (PKU), consult with your doctor, as some formulations of this medication may contain phenylalanine.
It is vital to inform your doctor if you are pregnant, planning to become pregnant, or are breast-feeding. Your doctor will help you weigh the benefits and risks of taking this medication during this time, ensuring the best possible outcome for you and your baby.
To manage your condition effectively, follow the personalized diet and exercise plan recommended by your doctor. If you experience constipation, increasing your fluid intake, engaging in regular physical activity, or adding more fiber to your diet may help alleviate symptoms. However, consult with your doctor before making any changes.
When taking this medication, it is crucial to administer other medications at least 1 hour before or 4 hours after taking this drug to minimize potential interactions.
Long-term use of this medication may lead to low vitamin K levels, increasing the risk of bleeding. If you have concerns or questions, discuss them with your doctor. Additionally, if you have hemorrhoids, inform your doctor, as this medication may exacerbate the condition.
If you have phenylketonuria (PKU), consult with your doctor, as some formulations of this medication may contain phenylalanine.
It is vital to inform your doctor if you are pregnant, planning to become pregnant, or are breast-feeding. Your doctor will help you weigh the benefits and risks of taking this medication during this time, ensuring the best possible outcome for you and your baby.
Overdose Information
Overdose Symptoms:
- Severe constipation
- Intestinal obstruction (rare, but possible with very large doses or pre-existing bowel issues)
What to Do:
Contact your doctor or poison control center immediately (Call 1-800-222-1222 in the US). Treatment is generally supportive, focusing on managing constipation and ensuring bowel patency.
Drug Interactions
Major Interactions
- Thyroid hormones (e.g., levothyroxine)
- Warfarin
- Digoxin
- Thiazide diuretics (e.g., hydrochlorothiazide)
- Fat-soluble vitamins (A, D, E, K)
- Mycophenolate mofetil
Moderate Interactions
- Beta-blockers (e.g., propranolol)
- Statins (e.g., pravastatin, fluvastatin)
- Oral contraceptives
- Phenobarbital
- Phenytoin
- Ursodiol
- Folic acid
Minor Interactions
- Other medications that may be affected by altered absorption due to binding.
Monitoring
Baseline Monitoring
Fasting 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, though colestipol is not hepatically metabolized.
Timing: Prior to initiation of therapy
Fat-soluble vitamin levels (A, D, E, K)
Rationale: To assess baseline status, especially if there's concern for malabsorption or prolonged use.
Timing: Prior to initiation of therapy (optional, but recommended for long-term use)
Routine Monitoring
Fasting 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: Failure to achieve target LDL-C, significant increase in triglycerides, or adverse effects.
Fat-soluble vitamin levels (A, D, E, K)
Frequency: Periodically (e.g., annually) for long-term therapy
Target: Normal physiological ranges
Action Threshold: Levels below normal range, requiring supplementation.
Prothrombin Time/INR (for patients on warfarin)
Frequency: More frequently when initiating or discontinuing colestipol
Target: Therapeutic range for warfarin
Action Threshold: INR outside therapeutic range.
Symptom Monitoring
- Constipation
- Abdominal discomfort/pain
- Bloating
- Flatulence
- Nausea
- Heartburn
- Symptoms of fat-soluble vitamin deficiency (e.g., night blindness, easy bruising, bone pain)
Special Patient Groups
Pregnancy
Colestipol is not absorbed systemically, so it is generally considered to have minimal risk to the fetus. However, it can interfere with the absorption of fat-soluble vitamins (A, D, E, K), which are essential for fetal development. Supplementation with fat-soluble vitamins may be necessary. Use only if clearly needed and benefits outweigh potential risks.
Trimester-Specific Risks:
First Trimester:
Low systemic exposure, but potential for vitamin malabsorption.
Second Trimester:
Low systemic exposure, but potential for vitamin malabsorption.
Third Trimester:
Low systemic exposure, but potential for vitamin malabsorption.
Lactation
Colestipol is not absorbed systemically and therefore is not expected to be excreted in breast milk. It is generally considered compatible with breastfeeding. However, monitor for potential vitamin deficiencies in the mother.
Infant Risk:
Low risk to infant.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. However, it has been used off-label in children with familial hypercholesterolemia, often under specialist supervision. Dosing must be individualized, and monitoring for vitamin deficiencies is crucial.
Geriatric Use
No specific dose adjustments are generally needed for elderly patients. However, elderly patients may be more susceptible to gastrointestinal side effects like constipation. Adequate fluid intake and fiber are important. Monitor for potential drug interactions and vitamin deficiencies.
Clinical Information
Clinical Pearls
- Colestipol granules must be mixed thoroughly with at least 90 mL (3 fluid ounces) of water, juice, milk, or other non-carbonated liquid. It can also be mixed with soft foods like applesauce or hot cereals.
- Do not take the granules dry, as they can cause esophageal irritation or choking.
- To minimize GI side effects (constipation, bloating), start with a low dose and gradually titrate upwards. Ensure adequate fluid and fiber intake.
- Administer other medications at least 1 hour before or 4-6 hours after colestipol to prevent interference with their absorption.
- Consider supplementation with fat-soluble vitamins (A, D, E, K) and folic acid, especially with long-term use.
- Colestipol can increase triglyceride levels in some patients; monitor lipid panel closely.
- It is an alternative for patients who cannot tolerate statins or as an add-on therapy for severe hypercholesterolemia.
Alternative Therapies
- Other Bile Acid Sequestrants (e.g., Cholestyramine, Colesevelam)
- Statins (HMG-CoA Reductase Inhibitors)
- Ezetimibe (Cholesterol Absorption Inhibitor)
- PCSK9 Inhibitors (e.g., Alirocumab, Evolocumab)
- Fibrates (e.g., Gemfibrozil, Fenofibrate) - primarily for triglycerides
- Niacin (Nicotinic Acid) - less commonly used due to side effects
Cost & Coverage
Average Cost:
Varies widely, typically $100-$300+ per 90 packets (5gm each)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic), Tier 3 or Non-Formulary (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to discuss them with 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 reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.