Colesevelam 3.75g Pak For Oral Susp
It is used to lower cholesterol.It is used to help control blood sugar in people with type 2 diabetes.
Drug Class
Antilipemic agent, Antidiabetic agent
Pharmacologic Class
Bile acid sequestrant
Pregnancy Category
B
FDA Approved
Oct 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Colesevelam is a medication that helps lower 'bad' cholesterol (LDL-C) and can also help control blood sugar levels in people with type 2 diabetes. It works by binding to certain substances in your gut, preventing them from being absorbed into your body, which then helps your liver remove more cholesterol from your blood and may affect how your body handles sugar.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and adhere to the guidelines. Take your medication with meals to help your body absorb it properly. Additionally, follow the diet and exercise plan recommended by your doctor to maximize the effectiveness of your treatment.
It's also important to stay hydrated by drinking plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake. To take your medication, mix the powder with 1 cup (8 ounces/240 mL) of water, fruit juice, or diet soda. Stir the mixture well and drink it immediately. Do not ingest the dry powder.
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. When your medication is no longer needed or has expired, dispose of it properly. 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're unsure about the best way to dispose of your medication, consult with your pharmacist, who may be aware of drug take-back programs in your area.
What to Do If You Miss a Dose
If you forget to take 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 get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and adhere to the guidelines. Take your medication with meals to help your body absorb it properly. Additionally, follow the diet and exercise plan recommended by your doctor to maximize the effectiveness of your treatment.
It's also important to stay hydrated by drinking plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake. To take your medication, mix the powder with 1 cup (8 ounces/240 mL) of water, fruit juice, or diet soda. Stir the mixture well and drink it immediately. Do not ingest the dry powder.
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. When your medication is no longer needed or has expired, dispose of it properly. 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're unsure about the best way to dispose of your medication, consult with your pharmacist, who may be aware of drug take-back programs in your area.
What to Do If You Miss a Dose
If you forget to take 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 heart-healthy diet low in saturated and trans fats, and cholesterol.
- Engage in regular physical activity as recommended by your doctor.
- If for diabetes, follow a balanced diet and exercise plan as advised by your healthcare provider.
- Ensure adequate fluid intake to help prevent constipation.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For Hyperlipidemia: 3.75 g once daily or 1.875 g twice daily. For Type 2 Diabetes: 3.75 g once daily or 1.875 g twice daily.
Dose Range:
1.875 - 3.75 mg
Condition-Specific Dosing:
Hyperlipidemia:
3.75 g once daily or 1.875 g twice daily with meals.
Type 2 Diabetes:
3.75 g once daily or 1.875 g twice daily with meals.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for general use. For Heterozygous Familial Hypercholesterolemia (HeFH) in boys and postmenarchal girls 10-17 years: 3.75 g once daily.
Adolescent:
For Heterozygous Familial Hypercholesterolemia (HeFH) in boys and postmenarchal girls 10-17 years: 3.75 g once daily.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment needed
Moderate:
No dosage adjustment needed
Severe:
No dosage adjustment needed
Dialysis:
No dosage adjustment needed, as colesevelam is not systemically absorbed.
Hepatic Impairment:
Mild:
No dosage adjustment needed
Moderate:
No dosage adjustment needed
Severe:
No dosage 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 demand for bile acid synthesis in the liver. The liver compensates by increasing the expression of LDL receptors, which leads to increased clearance of LDL-C from the blood. The mechanism by which colesevelam improves glycemic control in type 2 diabetes is not fully understood but may involve effects on glucose absorption, incretin levels, or hepatic glucose production.
Pharmacokinetics
Absorption:
Bioavailability:
Not absorbed systemically
Tmax:
Not applicable (not absorbed)
FoodEffect:
Should be taken with a meal and liquid to optimize efficacy and tolerability.
Distribution:
Vd:
Not applicable (confined to GI tract)
ProteinBinding:
Not applicable (not absorbed)
CnssPenetration:
No
Elimination:
HalfLife:
Not applicable (not absorbed)
Clearance:
Not applicable (not absorbed)
ExcretionRoute:
Fecal (unchanged)
Unchanged:
100%
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects typically observed within 2 weeks; glycemic effects within weeks.
PeakEffect:
Maximum lipid-lowering effects typically achieved by 2-4 weeks; glycemic effects by 4-6 weeks.
DurationOfAction:
Effects persist as long as treatment is continued.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, some individuals may experience severe and potentially life-threatening side effects while taking this medication. If you exhibit 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), including:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Trouble swallowing
Severe constipation or stomach pain, which may indicate a severe bowel problem
Other Possible Side Effects
As with all medications, side effects can occur. While many people experience no side effects or only mild 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 guidance:
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, don't hesitate to reach out to 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 individuals may experience severe and potentially life-threatening side effects while taking this medication. If you exhibit 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), including:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Trouble swallowing
Severe constipation or stomach pain, which may indicate a severe bowel problem
Other Possible Side Effects
As with all medications, side effects can occur. While many people experience no side effects or only mild 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 guidance:
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, don't hesitate to reach out to 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 worsening constipation
- Severe abdominal pain or cramping
- Persistent nausea or vomiting
- Unexplained bleeding or bruising (potential vitamin K deficiency)
- Unusual fatigue or muscle weakness (potential vitamin D deficiency)
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 reaction you experienced, such as symptoms and signs.
If you have high triglyceride levels or a history of pancreatitis caused by elevated triglycerides.
If you have a bowel obstruction or a condition that affects the movement of food through your digestive system (gastrointestinal tract).
If you have a history of stomach or bowel surgery, or if you have a slow-moving gastrointestinal tract.
* If you are using this medication to manage high blood sugar:
+ If you have a condition that causes acidic blood (acidosis).
+ If you have type 1 diabetes. Note: This medication is not intended to treat type 1 diabetes.
It is essential to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. Your doctor and pharmacist need this information to determine if it is safe for you to take this medication with your other medications and health conditions. Do not initiate, stop, or adjust the dose of any medication without consulting your doctor first.
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 reaction you experienced, such as symptoms and signs.
If you have high triglyceride levels or a history of pancreatitis caused by elevated triglycerides.
If you have a bowel obstruction or a condition that affects the movement of food through your digestive system (gastrointestinal tract).
If you have a history of stomach or bowel surgery, or if you have a slow-moving gastrointestinal tract.
* If you are using this medication to manage high blood sugar:
+ If you have a condition that causes acidic blood (acidosis).
+ If you have type 1 diabetes. Note: This medication is not intended to treat type 1 diabetes.
It is essential to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. Your doctor and pharmacist need this information to determine if it is safe for you to take this medication with your other medications and health conditions. Do not initiate, stop, or adjust the dose of any medication without consulting your doctor first.
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.
Regular blood tests and other laboratory assessments 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, administer 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 optimal timing for taking them in relation to this drug, as the timing may need to be adjusted.
Individuals with phenylketonuria (PKU) should discuss this condition with their doctor, as some formulations of this drug may contain phenylalanine.
It is also important to note that birth control pills may be less effective in preventing pregnancy when taken concurrently with this medication. If you are using birth control pills, take them at least 4 hours before taking this drug. Additionally, if you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
You should be aware that this drug can cause high triglyceride levels. If you have a history of elevated triglyceride levels, notify your doctor.
Regular blood tests and other laboratory assessments 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, administer 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 optimal timing for taking them in relation to this drug, as the timing may need to be adjusted.
Individuals with phenylketonuria (PKU) should discuss this condition with their doctor, as some formulations of this drug may contain phenylalanine.
It is also important to note that birth control pills may be less effective in preventing pregnancy when taken concurrently with this medication. If you are using birth control pills, take them at least 4 hours before taking this drug. Additionally, if you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe constipation
- Abdominal distension
- Nausea
- Vomiting
What to Do:
Since colesevelam is not absorbed, systemic toxicity from overdose is unlikely. Management should be supportive, focusing on alleviating gastrointestinal symptoms. Contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention if a large overdose is suspected.
Drug Interactions
Major Interactions
- Levothyroxine (decreased absorption of levothyroxine; administer levothyroxine at least 4 hours prior to colesevelam)
- Oral Contraceptives (ethinyl estradiol, norethindrone - decreased absorption; administer oral contraceptives at least 4 hours prior to colesevelam)
- Phenytoin (decreased absorption; administer phenytoin at least 4 hours prior to colesevelam)
- Warfarin (potential for altered INR; monitor INR closely)
- Sulfonylureas (potential for altered glucose control; monitor blood glucose)
- Olmesartan (decreased absorption; administer olmesartan at least 4 hours prior to colesevelam)
Moderate Interactions
- Fat-soluble vitamins (A, D, E, K - decreased absorption; consider supplementation)
- Other medications with narrow therapeutic index or those that are highly protein-bound (potential for decreased absorption; administer other medications at least 1 hour before or 4 hours after colesevelam)
Monitoring
Baseline Monitoring
Lipid Panel (LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess treatment efficacy for hyperlipidemia.
Timing: Prior to initiation of therapy.
HbA1c and Fasting Plasma Glucose
Rationale: To establish baseline glycemic control and assess treatment efficacy for type 2 diabetes.
Timing: Prior to initiation of therapy (if for diabetes).
Liver Function Tests (ALT, AST)
Rationale: Although not hepatically metabolized, good practice for patients on lipid-lowering therapy.
Timing: Prior to initiation of therapy.
Renal Function (SCr, eGFR)
Rationale: To assess overall patient health, though no dose adjustment needed for renal impairment.
Timing: Prior to initiation of therapy.
Routine Monitoring
Lipid Panel (LDL-C, HDL-C, Triglycerides)
Frequency: Every 4-6 weeks initially, then every 3-6 months or as clinically indicated.
Target: Individualized based on patient risk factors and treatment goals (e.g., LDL-C <100 mg/dL or <70 mg/dL).
Action Threshold: If LDL-C target not met, consider dose adjustment or combination therapy. If triglycerides significantly increase (>500 mg/dL), re-evaluate therapy.
HbA1c and Fasting Plasma Glucose
Frequency: Every 3-6 months (if for diabetes).
Target: Individualized based on patient goals (e.g., HbA1c <7%).
Action Threshold: If glycemic targets not met, consider dose adjustment or addition of other antidiabetic agents.
GI Symptoms (constipation, dyspepsia, abdominal pain)
Frequency: Routinely during follow-up visits.
Target: Absence or minimal symptoms.
Action Threshold: If severe or persistent, consider dose reduction, dietary changes, or discontinuation.
Symptom Monitoring
- Constipation
- Dyspepsia
- Abdominal pain
- Nausea
- Bloating
- Flatulence
- Unusual fatigue or weakness (potential vitamin deficiency)
Special Patient Groups
Pregnancy
Colesevelam is Pregnancy Category B. Studies in animals have shown no evidence of harm to the fetus. Since colesevelam is not systemically absorbed, it is considered to have a low risk of direct fetal harm. However, there is a theoretical concern for maternal malabsorption of fat-soluble vitamins (A, D, E, K), which are crucial for fetal development. Supplementation may be considered.
Trimester-Specific Risks:
First Trimester:
Low direct fetal risk due to lack of systemic absorption. Monitor maternal vitamin status.
Second Trimester:
Low direct fetal risk. Continue to monitor maternal vitamin status.
Third Trimester:
Low direct fetal risk. Monitor maternal vitamin status and potential for constipation.
Lactation
Colesevelam is not systemically absorbed and therefore not expected to be excreted in breast milk. The primary concern is the potential for maternal malabsorption of fat-soluble vitamins, which could indirectly affect the nutritional status of the breastfed infant if maternal stores are depleted. Use with caution, and consider maternal vitamin supplementation.
Infant Risk:
Low direct risk to infant. Indirect risk from potential maternal vitamin deficiency.
Pediatric Use
Approved for use in boys and postmenarchal girls aged 10-17 years with heterozygous familial hypercholesterolemia (HeFH). Safety and efficacy for other indications or in younger children have not been established. Monitor for GI side effects, especially constipation.
Geriatric Use
No specific dosage adjustment is required based on age. However, elderly patients may be more susceptible to the gastrointestinal side effects, particularly constipation. Monitor closely for these effects and ensure adequate fluid intake.
Clinical Information
Clinical Pearls
- Always take colesevelam with a meal and a glass of water or other liquid to improve tolerability and efficacy.
- Space administration of other medications (especially levothyroxine, oral contraceptives, phenytoin, warfarin, and olmesartan) at least 1 hour before or 4 hours after colesevelam to minimize potential for reduced absorption.
- Consider supplementation with fat-soluble vitamins (A, D, E, K) if long-term use is anticipated, especially in patients with pre-existing deficiencies or conditions affecting vitamin absorption.
- Colesevelam can sometimes increase triglyceride levels, particularly in patients with pre-existing hypertriglyceridemia. Monitor triglyceride levels closely.
- It is a good option for patients who cannot tolerate statins or as an add-on therapy for further LDL-C reduction or glycemic control.
Alternative Therapies
- Statins (e.g., Atorvastatin, Rosuvastatin) for hyperlipidemia
- Ezetimibe for hyperlipidemia
- PCSK9 inhibitors (e.g., Alirocumab, Evolocumab) for severe hyperlipidemia
- Fibrates (e.g., Fenofibrate, Gemfibrozil) for hypertriglyceridemia
- Niacin for dyslipidemia
- Other antidiabetic agents (e.g., Metformin, Sulfonylureas, DPP-4 inhibitors, SGLT2 inhibitors, GLP-1 receptor agonists, Insulin) for type 2 diabetes.
Cost & Coverage
Average Cost:
Variable, typically $200-$400 per 30 packets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Brand), Tier 1 (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 details. 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 information about the medication taken, the amount, and the time it happened.