Colestipol 5gm Granule Packets 30's

Manufacturer GREENSTONE Active Ingredient Colestipol Granules(koe LES ti pole) Pronunciation koe LES ti pole
It is used to lower cholesterol.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 1977
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Colestipol is a medication that helps lower high cholesterol levels in your blood. It works by binding to certain substances in your gut called bile acids, which prevents your body from reabsorbing them. This forces your liver to use more cholesterol to make new bile acids, which helps reduce the amount of 'bad' cholesterol (LDL-C) in your blood.
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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 is essential to follow the instructions carefully to ensure safe and effective use.

Do not take the dry powder form of this medication. Instead, mix it with at least 3 ounces (90 mL) of water or another liquid, and then drink the mixture. After drinking, rinse the glass with more liquid and drink the rinse to ensure you receive the full dose.
You can also mix this medication with soft foods like cereals, soups, or fruits such as applesauce or crushed pineapple. Be sure to follow the instructions you were given on how to mix it properly.

Staying Hydrated

Unless your doctor advises you to limit your fluid intake, drink plenty of non-caffeinated liquids to help your body absorb the medication effectively.

Storing and Disposing of Your Medication

To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding the bathroom.
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 doctor or pharmacist. If you have questions about the best way to dispose of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available 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 continue with 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 low-cholesterol, low-saturated fat diet as recommended by your doctor.
  • Engage in regular physical activity.
  • Maintain a healthy weight.
  • Avoid smoking.
  • Limit alcohol intake.
  • Mix the granules thoroughly with at least 90 mL (3 ounces) of liquid (water, juice, milk, soup) or soft food (applesauce, hot cereal) before taking. Do not take dry granules.
  • Take other medications at least 1 hour before or 4-6 hours after colestipol to prevent interactions.

Dosing & Administration

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Adult Dosing

Standard Dose: 5 grams once or twice daily
Dose Range: 5 - 30 mg

Condition-Specific Dosing:

hyperlipidemia: Initial dose: 5 grams once or twice daily. May increase by 5 grams/day at 1-2 month intervals. Usual maintenance dose: 5-30 grams/day given once or in divided doses. Max dose: 30 grams/day.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established (safety and efficacy not established in pediatric patients, though sometimes used off-label under specialist guidance)
Adolescent: Not established (safety and efficacy not established in pediatric patients, though sometimes used off-label under specialist guidance)
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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 colestipol 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

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. The increased demand for cholesterol in the liver results in an upregulation of hepatic LDL receptors, which increases the clearance of LDL-C from the blood, thereby lowering plasma LDL-C levels.
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Pharmacokinetics

Absorption:

Bioavailability: Negligible (not absorbed)
Tmax: Not applicable (not absorbed)
FoodEffect: Can be taken with or without food, but usually mixed with liquid or food.

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 (as insoluble complex with bile acids)
Unchanged: 100%
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Pharmacodynamics

OnsetOfAction: Within 1-2 weeks for lipid-lowering effects
PeakEffect: Approximately 1 month for maximal LDL-C reduction
DurationOfAction: Continues as long as therapy is maintained

Safety & Warnings

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Side Effects

Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:

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
Trouble swallowing
Unexplained bruising or bleeding

Common 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. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:

Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Heartburn
Stomach cramps
Gas
Muscle or joint pain
* Headache

Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. 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 abdominal pain or bloating
  • Unusual bleeding or bruising (may indicate vitamin K deficiency)
  • Vision changes (may indicate vitamin A deficiency)
  • Muscle weakness or bone pain (may indicate vitamin D deficiency)
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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.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions.
* Any existing health problems, as this medication may interact with them.

To ensure your safety, it is vital 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.
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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. 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, adhere to the 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 products contain phenylalanine. It is also essential to inform your doctor if you are pregnant, planning to become pregnant, or are breast-feeding, as you will need to discuss the potential benefits and risks to both you and your baby.
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Overdose Information

Overdose Symptoms:

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

What to Do:

Contact a poison control center or emergency medical services immediately. Treatment is generally supportive, focusing on managing constipation and maintaining hydration. Call 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Thyroid hormones (e.g., levothyroxine): Reduced absorption
  • Digoxin: Reduced absorption
  • Warfarin: Reduced absorption (potential for altered INR)
  • Fat-soluble vitamins (A, D, E, K): Reduced absorption with long-term use
  • Thiazide diuretics (e.g., hydrochlorothiazide): Reduced absorption
  • Beta-blockers (e.g., propranolol): Reduced absorption
  • Oral contraceptives: Potential for reduced efficacy (though data are mixed)
  • Phenobarbital: Reduced absorption
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Moderate Interactions

  • Statins (e.g., atorvastatin, simvastatin): Reduced absorption if co-administered too closely
  • Fibrates (e.g., gemfibrozil): Reduced absorption if co-administered too closely
  • Nonsteroidal anti-inflammatory drugs (NSAIDs): Potential for reduced absorption
  • Other medications with narrow therapeutic index

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 rule out underlying liver disease and establish baseline, though colestipol is not hepatotoxic.

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 treatment goals (e.g., LDL-C <100 mg/dL or <70 mg/dL).

Action Threshold: If lipid goals are not met, consider dose adjustment or addition of other lipid-lowering agents.

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

Frequency: Periodically, especially with long-term use or in patients with malabsorption.

Target: Within normal limits.

Action Threshold: Supplementation may be required if levels are low.

Prothrombin Time/INR (for patients on warfarin)

Frequency: More frequently when initiating or adjusting colestipol dose.

Target: Therapeutic range for warfarin.

Action Threshold: Adjust warfarin dose as needed.

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Symptom Monitoring

  • Constipation
  • Abdominal discomfort/bloating
  • Nausea
  • Heartburn
  • Steatorrhea (rare, high doses)
  • Symptoms of vitamin deficiency (e.g., easy bruising for Vitamin K, night blindness for Vitamin A)

Special Patient Groups

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Pregnancy

Colestipol is not absorbed systemically, so maternal and fetal exposure is minimal. It is generally considered a safer option for hyperlipidemia management in pregnancy when diet and lifestyle changes are insufficient, especially compared to statins. However, potential for fat-soluble vitamin deficiency exists, which could impact fetal development.

Trimester-Specific Risks:

First Trimester: Low risk due to minimal systemic absorption. Monitor for fat-soluble vitamin deficiencies.
Second Trimester: Low risk. Monitor for fat-soluble vitamin deficiencies.
Third Trimester: Low risk. Monitor for fat-soluble vitamin deficiencies.
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Lactation

Colestipol is not absorbed systemically by the mother, so it is not excreted into breast milk. It is considered compatible with breastfeeding. However, monitor for potential fat-soluble vitamin deficiencies in the mother, which could indirectly affect milk composition.

Infant Risk: Low risk (L2 - Safest, but monitor for potential maternal vitamin deficiencies).
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Use is generally off-label and reserved for severe cases of familial hypercholesterolemia under specialist supervision. Potential for growth retardation due to fat-soluble vitamin malabsorption is a concern with long-term use.

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Geriatric Use

No specific dose adjustment is required. Elderly patients may be more susceptible to constipation and other gastrointestinal side effects. Monitor hydration status and bowel habits closely.

Clinical Information

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Clinical Pearls

  • Colestipol is a non-systemic agent, making it a good option for patients who cannot tolerate or are contraindicated to systemic lipid-lowering agents.
  • The most common side effects are GI-related, particularly constipation. Advise patients to increase fluid intake and dietary fiber.
  • Crucial to counsel patients on the timing of other medications (1 hour before or 4-6 hours after colestipol) to avoid drug interactions.
  • Long-term use may necessitate supplementation of fat-soluble vitamins (A, D, E, K) and folic acid.
  • Granules must be mixed thoroughly with liquid or soft food; never take dry.
  • While effective for LDL-C lowering, colestipol can sometimes increase triglycerides, especially in patients with pre-existing hypertriglyceridemia.
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Alternative Therapies

  • Cholestyramine (another bile acid sequestrant)
  • Colesevelam (another bile acid sequestrant)
  • Statins (HMG-CoA reductase inhibitors)
  • Ezetimibe (cholesterol absorption inhibitor)
  • PCSK9 inhibitors
  • Fibrates (for hypertriglyceridemia, but also affect LDL-C)
  • Niacin (nicotinic acid)
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Cost & Coverage

Average Cost: Not available (highly variable) per 30 packets
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.