Colesevelam 625mg Tablets
It is used to lower cholesterol.It is used to help control blood sugar in people with type 2 diabetes.
Drug Class
Antilipemic agent; Glucose lowering agent
Pharmacologic Class
Bile acid sequestrant
Pregnancy Category
Category B
FDA Approved
Jan 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Colesevelam is a medication used to help lower 'bad' cholesterol (LDL-C) and, in people with type 2 diabetes, to help lower blood sugar. It works by binding to certain substances in your gut called bile acids, which helps your body remove more cholesterol and may also affect how your body handles sugar.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with meals to help your body absorb it properly. It's also essential to follow the diet and exercise plan recommended by your doctor. Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake. Swallow your medication whole with water or another liquid. If you have difficulty swallowing, consult your doctor for guidance.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, avoiding the bathroom. Keep all medications in a safe place, out of 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're unsure 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, with a meal. 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.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with meals to help your body absorb it properly. It's also essential to follow the diet and exercise plan recommended by your doctor. Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake. Swallow your medication whole with water or another liquid. If you have difficulty swallowing, consult your doctor for guidance.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry location, avoiding the bathroom. Keep all medications in a safe place, out of 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're unsure 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, with a meal. 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.
Lifestyle & Tips
- Maintain a healthy diet low in saturated and trans fats, and cholesterol.
- Engage in regular physical activity as recommended by your doctor.
- If you have diabetes, continue to follow your prescribed diet and exercise plan.
- Take this medication with a meal and a glass of water or other liquid to help it go down and reduce stomach upset.
- If you take other medications, especially thyroid hormones, birth control pills, or certain seizure medications, take them at least 4 hours BEFORE or 4 hours AFTER taking colesevelam to ensure they are properly absorbed.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Hyperlipidemia: 6 tablets (3.75 g) once daily or 3 tablets (1.875 g) twice daily. Type 2 Diabetes: 6 tablets (3.75 g) once daily or 3 tablets (1.875 g) twice daily.
Dose Range:
1875 - 3750 mg
Condition-Specific Dosing:
hyperlipidemia:
3.75 g (6 tablets) once daily or 1.875 g (3 tablets) twice daily with meals and liquid.
type2Diabetes:
3.75 g (6 tablets) once daily or 1.875 g (3 tablets) twice daily with meals and liquid.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for routine use; safety and efficacy not established in children <10 years for hyperlipidemia. Not established for type 2 diabetes.
Adolescent:
Not established for routine use; safety and efficacy not established in children <10 years for hyperlipidemia. Not established for type 2 diabetes.
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
Colesevelam is a non-absorbed, polymeric bile acid sequestrant. It 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 increases the synthesis of bile acids from cholesterol in the liver, leading to an upregulation of hepatic LDL receptors and increased clearance of LDL-C from the blood. The mechanism for glucose lowering in type 2 diabetes is not fully understood but may involve effects on bile acid signaling pathways (e.g., FXR, TGR5) or reduced glucose absorption.
Pharmacokinetics
Absorption:
Bioavailability:
Not absorbed
Tmax:
Not applicable (not absorbed)
FoodEffect:
Should be taken with a meal and liquid to aid administration and potentially reduce gastrointestinal 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 excretion (unchanged)
Unchanged:
100%
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects: Within 2 weeks; Glucose-lowering effects: Within 2-4 weeks.
PeakEffect:
Lipid-lowering effects: 4-6 weeks; Glucose-lowering effects: 6-12 weeks.
DurationOfAction:
Maintained with continued therapy.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice 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
Signs of pancreatitis (pancreas problem), such as:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Trouble swallowing
Severe constipation or stomach pain, which may be signs of a severe bowel problem
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. 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
Heartburn
Headache
Nose or throat irritation
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice 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
Signs of pancreatitis (pancreas problem), such as:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Trouble swallowing
Severe constipation or stomach pain, which may be signs of a severe bowel problem
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. 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
Heartburn
Headache
Nose or throat irritation
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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 constipation or worsening of existing constipation.
- Severe abdominal pain or bloating.
- Unusual bleeding or bruising (may indicate vitamin K deficiency).
- Vision problems, especially at night (may indicate vitamin A deficiency).
- Muscle weakness or bone pain (may indicate vitamin D deficiency).
- Persistent nausea or vomiting.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
To ensure safe and effective treatment, inform your doctor about the following:
Any allergies you have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reactions you've experienced.
A history of high triglycerides or pancreatitis caused by elevated triglyceride levels.
Previous bowel blockage or bowel obstruction.
A slow-moving gastrointestinal (GI) tract or any stomach or bowel surgery you've undergone.
If You're Using This Medication for High Blood Sugar:
Inform your doctor if you have a condition characterized by acidic blood.
Note that this medication is not intended for treating type 1 diabetes. If you have type 1 diabetes, do not use this drug.
It's crucial to discuss all your health conditions and medications with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications.
Natural products and vitamins you're taking.
Verify with your doctor that it's safe to take this medication alongside your other drugs and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
To ensure safe and effective treatment, inform your doctor about the following:
Any allergies you have to this medication, its components, or other substances, including foods and drugs. Describe the allergic reactions you've experienced.
A history of high triglycerides or pancreatitis caused by elevated triglyceride levels.
Previous bowel blockage or bowel obstruction.
A slow-moving gastrointestinal (GI) tract or any stomach or bowel surgery you've undergone.
If You're Using This Medication for High Blood Sugar:
Inform your doctor if you have a condition characterized by acidic blood.
Note that this medication is not intended for treating type 1 diabetes. If you have type 1 diabetes, do not use this drug.
It's crucial to discuss all your health conditions and medications with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications.
Natural products and vitamins you're taking.
Verify with your doctor that it's safe to take this medication alongside your other drugs and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
You should be aware that this drug can cause high triglyceride levels. If you have a history of elevated triglyceride levels, notify your doctor promptly.
Regular blood work and laboratory tests are crucial while taking this medication. Adhere to your doctor's instructions regarding the frequency and timing of these tests.
If you have diabetes (high blood sugar), it is vital to monitor your blood sugar levels closely to ensure they remain within a healthy range.
When taking vitamins orally, take them at least 4 hours before taking this drug to minimize potential interactions.
If you are taking other medications, consult your doctor or pharmacist to determine the best schedule for taking them in relation to this drug, as the timing may need to be adjusted.
Note that birth control pills may be less effective in preventing pregnancy if taken simultaneously with this medication. If you are using birth control pills, take them at least 4 hours before taking this drug to maximize their effectiveness.
If you are pregnant, planning to become pregnant, or are breastfeeding, it is crucial to discuss the benefits and risks of this medication with your doctor, considering both your health and the baby's well-being.
You should be aware that this drug can cause high triglyceride levels. If you have a history of elevated triglyceride levels, notify your doctor promptly.
Regular blood work and laboratory tests are crucial while taking this medication. Adhere to your doctor's instructions regarding the frequency and timing of these tests.
If you have diabetes (high blood sugar), it is vital to monitor your blood sugar levels closely to ensure they remain within a healthy range.
When taking vitamins orally, take them at least 4 hours before taking this drug to minimize potential interactions.
If you are taking other medications, consult your doctor or pharmacist to determine the best schedule for taking them in relation to this drug, as the timing may need to be adjusted.
Note that birth control pills may be less effective in preventing pregnancy if taken simultaneously with this medication. If you are using birth control pills, take them at least 4 hours before taking this drug to maximize their effectiveness.
If you are pregnant, planning to become pregnant, or are breastfeeding, it is crucial to discuss the benefits and risks of this medication with your doctor, considering both your health and the baby's well-being.
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 gastrointestinal symptoms.
Drug Interactions
Major Interactions
- Levothyroxine (reduced absorption, administer 4 hours before or after)
- Oral contraceptives containing ethinyl estradiol and norethindrone (reduced absorption, administer 4 hours before or after)
- Phenytoin (reduced absorption, administer 4 hours before or after)
- Warfarin (potential for altered INR, monitor closely)
- Glipizide (reduced absorption, administer 4 hours before or after)
Moderate Interactions
- Fat-soluble vitamins (A, D, E, K) (reduced absorption, consider supplementation or separate administration)
- Other medications with narrow therapeutic index (monitor closely if co-administered, separate dosing)
Minor Interactions
- Other oral medications (general recommendation to separate administration by 4 hours)
Monitoring
Baseline Monitoring
Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess efficacy for hyperlipidemia.
Timing: Prior to initiation of therapy.
HbA1c and Fasting Plasma Glucose
Rationale: To establish baseline glycemic control and assess efficacy for type 2 diabetes.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs)
Rationale: Although not metabolized by the liver, baseline assessment is prudent.
Timing: Prior to initiation of therapy.
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: LDL-C <100 mg/dL (or individualized target); Triglycerides <150 mg/dL.
Action Threshold: If LDL-C target not met, consider dose adjustment or add-on therapy. If triglycerides significantly increase (>500 mg/dL), consider discontinuation or add-on therapy for hypertriglyceridemia.
HbA1c
Frequency: Every 3-6 months.
Target: Individualized target (e.g., <7%).
Action Threshold: If HbA1c target not met, consider dose adjustment or add-on therapy.
Fasting Plasma Glucose
Frequency: Periodically, as clinically indicated.
Target: Individualized target (e.g., 80-130 mg/dL).
Action Threshold: If target not met, consider dose adjustment or add-on therapy.
Symptoms of Fat-Soluble Vitamin Deficiency (e.g., easy bruising, night blindness)
Frequency: Periodically, as clinically indicated.
Target: Not applicable
Action Threshold: If symptoms occur, consider vitamin supplementation and/or re-evaluate colesevelam therapy.
Symptom Monitoring
- Constipation
- Dyspepsia
- Nausea
- Abdominal pain
- Bloating
- Flatulence
- Symptoms of fat-soluble vitamin deficiency (e.g., vision changes, bleeding, bone pain)
Special Patient Groups
Pregnancy
Colesevelam is classified as Pregnancy Category B. Studies in animals have shown no evidence of harm to the fetus. Since colesevelam is not absorbed systemically, maternal and fetal exposure is expected to be minimal. Use during pregnancy should be considered if clearly needed, especially for managing hyperlipidemia or diabetes where benefits outweigh potential risks.
Trimester-Specific Risks:
First Trimester:
Low risk due to minimal systemic absorption.
Second Trimester:
Low risk due to minimal systemic absorption.
Third Trimester:
Low risk due to minimal systemic absorption. Potential for reduced absorption of fat-soluble vitamins, which may be important in late pregnancy; monitor vitamin status if concerns arise.
Lactation
Colesevelam is not absorbed systemically, so it is not expected to be excreted in breast milk. Therefore, it is considered compatible with breastfeeding. However, potential for reduced absorption of fat-soluble vitamins in the mother should be considered.
Infant Risk:
Low risk to the infant.
Pediatric Use
Safety and efficacy have not been established in children younger than 10 years for hyperlipidemia. Not established for type 2 diabetes in pediatric patients. Generally not recommended for routine use in pediatric populations.
Geriatric Use
No specific dosage adjustment is required based on age. However, elderly patients may be more susceptible to gastrointestinal side effects, particularly constipation. Monitor closely for constipation and ensure adequate fluid intake.
Clinical Information
Clinical Pearls
- Colesevelam is a good option for patients who cannot tolerate statins or as an add-on therapy for further LDL-C reduction.
- It can be particularly useful in patients with both hyperlipidemia and type 2 diabetes due to its dual mechanism of action.
- Monitor triglyceride levels, as colesevelam can sometimes cause an increase in triglycerides, especially in patients with pre-existing hypertriglyceridemia.
- Emphasize the importance of timing other medications (especially narrow therapeutic index drugs and fat-soluble vitamins) at least 4 hours before or after colesevelam to prevent malabsorption.
- Advise patients to take with plenty of water to minimize the risk of constipation.
Alternative Therapies
- Statins (e.g., atorvastatin, rosuvastatin, simvastatin) for hyperlipidemia.
- Other bile acid sequestrants (e.g., cholestyramine, colestipol) for hyperlipidemia.
- Ezetimibe for hyperlipidemia.
- PCSK9 inhibitors (e.g., evolocumab, alirocumab) for severe hyperlipidemia.
- Fibrates (e.g., fenofibrate, gemfibrozil) for hypertriglyceridemia.
- Niacin (nicotinic acid) for dyslipidemia.
- Metformin, SGLT2 inhibitors, GLP-1 receptor agonists, DPP-4 inhibitors, sulfonylureas, insulin for type 2 diabetes.
Cost & Coverage
Average Cost:
Varies widely, typically $300-$600+ per 180 tablets (30-day supply of 6 tablets/day)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Brand) / Tier 1 (Generic) depending on insurance plan and formulary.
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 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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.