Colestipol 1gm Tablets

Manufacturer ZYDUS Active Ingredient Colestipol Tablets(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
C
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FDA Approved
Mar 1977
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Colestipol is a medication used to lower high cholesterol levels in the blood. It works by binding to bile acids in your gut, which helps your body remove more cholesterol. This can reduce your risk of heart disease.
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How to Use This Medicine

Taking Your Medication Correctly

To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions precisely.

Take your medication as directed by your doctor.
If your dose requires more than one tablet, take one tablet at a time.
Do not lick or wet the tablet before placing it in your mouth.
Swallow the tablet whole with a full glass of water immediately after putting it in your mouth. Do not chew, break, or crush the tablet.
If you have difficulty swallowing, consult your doctor for guidance.

Staying Hydrated

Drink plenty of non-caffeinated fluids 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 place, avoiding storage in a 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 by your doctor or pharmacist. Check with your pharmacist for guidance on the best disposal method or to see if there are any 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.
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Lifestyle & Tips

  • Maintain a low-cholesterol, low-saturated fat diet as recommended by your doctor or dietitian.
  • Engage in regular physical activity.
  • Avoid smoking.
  • Limit alcohol intake.
  • Drink plenty of fluids to help prevent constipation, a common side effect.

Dosing & Administration

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Adult Dosing

Standard Dose: 2 grams once or twice daily, increasing as needed
Dose Range: 2 - 16 mg

Condition-Specific Dosing:

primaryHypercholesterolemia: Initial: 2 grams once or twice daily. Maintenance: 2 to 16 grams per day, given in single or divided doses. Max: 16 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)
Adolescent: Not established (safety and efficacy not established in pediatric patients)
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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

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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. This process requires an increased number of LDL receptors on the surface of liver cells, which in turn increases the catabolism of LDL-C from the plasma, 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 taken 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 (as insoluble complex with bile acids)
Unchanged: 100%
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Pharmacodynamics

OnsetOfAction: Within 2-4 weeks for maximal LDL-C lowering effect
PeakEffect: Within 2-4 weeks
DurationOfAction: Continues as long as therapy is maintained

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
Difficulty swallowing
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 persist, contact your doctor for advice:

Gastrointestinal issues:
+ Constipation
+ Diarrhea
+ Stomach pain
+ Upset stomach
+ Vomiting
Heartburn
Stomach cramps
Gas
Muscle or joint pain
* Headache

This list is not exhaustive, and you may experience other 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe or persistent constipation
  • Severe abdominal pain
  • Unusual bleeding or bruising (if taking warfarin)
  • Symptoms of vitamin deficiency (e.g., night blindness, easy bruising, bone pain)
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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 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 and pharmacist assess potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions.

To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current medications and health conditions. Never start, stop, or adjust 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. 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 other medications, allow 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.

If you have a history of hemorrhoids, inform your doctor, as this medication may exacerbate the condition. In rare cases, the tablet may get stuck in the esophagus after swallowing, causing chest pain or pressure. If this occurs, seek immediate medical attention and do not take another tablet unless advised to do so by your doctor.

If you are pregnant, planning to become pregnant, or breastfeeding, it is crucial to discuss the potential benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe constipation
  • Intestinal obstruction

What to Do:

Treatment is symptomatic and supportive. Ensure adequate hydration and consider laxatives for severe constipation. Call 1-800-222-1222 (Poison Control).

Drug Interactions

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Major Interactions

  • Thyroid hormones (e.g., Levothyroxine)
  • Warfarin
  • Digoxin
  • Thiazide diuretics (e.g., Hydrochlorothiazide)
  • Beta-blockers (e.g., Propranolol)
  • Fat-soluble vitamins (A, D, E, K)
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Moderate Interactions

  • Folic acid
  • Oral contraceptives
  • Phenobarbital
  • Glipizide
  • Ursodiol

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 severity of hypercholesterolemia.

Timing: Prior to initiation of therapy

Liver Function Tests (ALT, AST)

Rationale: To rule out underlying liver disease, although colestipol is not hepatically metabolized.

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 cardiovascular risk guidelines (e.g., LDL-C < 100 mg/dL or < 70 mg/dL)

Action Threshold: If target LDL-C is not achieved, consider dose adjustment or addition of other lipid-lowering agents. 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 or high doses

Target: Normal physiological ranges

Action Threshold: Supplementation may be required if deficiencies are noted.

Prothrombin Time/INR (for patients on warfarin)

Frequency: Regularly, as per warfarin monitoring guidelines

Target: Therapeutic INR range for indication

Action Threshold: Adjust warfarin dose as needed due to potential for reduced absorption.

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Symptom Monitoring

  • Constipation
  • Abdominal pain
  • Bloating
  • Flatulence
  • Nausea
  • Heartburn
  • Steatorrhea (rare, high doses)

Special Patient Groups

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Pregnancy

Category C. While not systemically absorbed, it may interfere with the absorption of fat-soluble vitamins (A, D, E, K) and folic acid, which are important during pregnancy. Use only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for reduced absorption of essential vitamins/folic acid.
Second Trimester: Potential for reduced absorption of essential vitamins/folic acid.
Third Trimester: Potential for reduced absorption of essential vitamins/folic acid.
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Lactation

L3 (Moderately Safe). Not systemically absorbed by the mother, so unlikely to be excreted in breast milk. However, there is a theoretical risk of malabsorption of fat-soluble vitamins in the mother, which could indirectly affect the nutritional content of breast milk. Monitor infant for adequate growth and vitamin status if concerns arise.

Infant Risk: Low; theoretical risk of reduced fat-soluble vitamins in breast milk.
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Pediatric Use

Safety and efficacy have not been established in pediatric patients. Use is generally not recommended unless specifically indicated and benefits outweigh risks, and under close medical supervision.

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Geriatric Use

No specific dose adjustments are required based on age. However, elderly patients may be more susceptible to constipation and other gastrointestinal side effects. Initiate with lower doses and titrate slowly, ensuring adequate fluid intake.

Clinical Information

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Clinical Pearls

  • Colestipol is a powder or tablet that must be mixed with liquid or taken with food to prevent esophageal irritation or choking. Tablets should be swallowed whole.
  • To minimize GI side effects, especially constipation, start with a low dose and gradually increase. Advise patients to increase fluid intake and dietary fiber.
  • Crucially, administer other medications at least 1 hour before or 4-6 hours after colestipol to prevent impaired absorption of other drugs.
  • May increase triglyceride levels in some patients; monitor triglycerides closely.
  • Consider fat-soluble vitamin supplementation (A, D, E, K) for patients on long-term therapy, especially if dietary intake is inadequate or signs of deficiency appear.
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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: Varies widely, typically $50-$200 per 30 tablets (1gm)
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 is 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 it's a good idea to check with your pharmacist. If you have any questions or concerns about this 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 seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened.