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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Colesevelam Hcl
Generic Name
Colesevelam Hcl
Active Ingredient
ColesevelamCategory
Other
Salt Form
Hydrochloride
Variants
7
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 625 mg/1 | TABLET, FILM COATED | ORAL | 72789-476 |
| 625 mg/1 | TABLET, FILM COATED | ORAL | 50090-7811 |
| 625 mg/1 | TABLET, FILM COATED | ORAL |
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Colesevelam Hcl, you must consult a qualified healthcare professional.
| 625 mg/1 | TABLET, FILM COATED | ORAL | 72162-1846 |
| 625 mg/1 | TABLET, FILM COATED | ORAL | 63629-8767 |
| 625 mg/1 | TABLET, FILM COATED | ORAL | 71335-2905 |
| 625 mg/1 | TABLET, FILM COATED | ORAL | 50090-4371 |
Detailed information about Colesevelam Hcl
Colesevelam is a non-absorbed, polymeric bile acid sequestrant used to reduce LDL cholesterol in adults and children with primary hyperlipidemia and to improve glycemic control in adults with type 2 diabetes mellitus.
The dosage of Colesevelam is standardized based on the condition being treated, though the total daily dose is often similar for both cholesterol and diabetes management.
When taken with a statin, the lipid-lowering effects are additive. Healthcare providers may adjust the dose based on the patient's tolerance and the specific reduction in LDL-C or HbA1c (hemoglobin A1c) observed during follow-up.
Colesevelam is approved for pediatric patients aged 10 to 17 years with heterozygous familial hypercholesterolemia (HeFH).
Because Colesevelam is not absorbed systemically and is not cleared by the kidneys, no dosage adjustments are necessary for patients with renal impairment (kidney disease). However, patients with end-stage renal disease should be monitored for gastrointestinal side effects.
No dosage adjustments are required for patients with hepatic impairment (liver disease). Since the drug works entirely within the intestinal lumen, the liver's metabolic capacity does not affect the drug's levels. However, patients with underlying biliary obstruction should use this medication with caution.
In clinical trials, no overall differences in safety or effectiveness were observed between patients over 65 and younger patients. Dosage adjustments are generally not required for the elderly, though healthcare providers should be mindful of the increased likelihood of constipation in this population.
Proper administration is critical for both the efficacy and safety of Colesevelam:
If you miss a dose of Colesevelam, take it as soon as you remember with a meal. If it is almost time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at once to make up for a missed one. Consistency is key to maintaining stable cholesterol and blood sugar levels.
Because Colesevelam is not absorbed, a systemic toxic overdose is highly unlikely. However, taking an excessive amount could lead to severe gastrointestinal complications, most notably severe constipation or even a bowel obstruction.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose or stop the medication without medical guidance, as this can lead to a rapid increase in cholesterol or blood sugar levels.
The most frequently reported side effects of Colesevelam are gastrointestinal in nature, which is expected given that the drug remains entirely within the digestive tract.
Colesevelam is generally considered safe due to its lack of systemic absorption, but it is not appropriate for everyone. The most critical safety consideration is the patient's baseline triglyceride level. Because the liver increases production of various lipids to compensate for bile acid loss, Colesevelam can significantly raise triglyceride levels, which may lead to acute pancreatitis.
No FDA black box warnings for Colesevelam.
While there are few absolute contraindications for drug combinations, Colesevelam should never be used in patients with a bowel obstruction. From a drug-interaction standpoint, it should not be taken simultaneously with medications that have a narrow therapeutic index where binding would result in immediate clinical failure, unless a strict 4-hour dosing window is maintained.
Colesevelam is strictly prohibited in the following clinical situations due to the risk of severe adverse outcomes:
Colesevelam is classified as Pregnancy Category B (under the older FDA system). Because Colesevelam is not absorbed systemically, it is not expected to cause direct fetal harm or birth defects. It does not reach the developing fetus through the placenta. However, there is a theoretical risk related to the malabsorption of fat-soluble vitamins, particularly Vitamin K, which is essential for blood clotting in both the mother and the fetus. If a pregnant woman takes Colesevelam, healthcare providers may recommend supplemental vitamins to ensure nutritional requirements are met. Use during pregnancy should only occur if the potential benefit justifies the potential risk to the fetus, and it is often preferred over systemic statins, which are generally contraindicated in pregnancy.
Colesevelam is not absorbed into the mother's bloodstream and, therefore, cannot be excreted into breast milk. There is no known risk to the nursing infant from maternal use of Colesevelam. It is considered one of the safer options for managing high cholesterol in breastfeeding women. However, the mother should be monitored for vitamin levels to ensure the quality of the breast milk remains optimal.
Colesevelam is a non-absorbed, lipid-lowering polymer that binds bile acids in the gastrointestinal tract. Chemically, it is a poly(allylamine hydrochloride) cross-linked with epichlorohydrin and alkylated with 1-bromodecane and (6-bromohexyl)-trimethylammonium bromide. This complex structure gives it a high density of positive charges. Bile acids are negatively charged; therefore, Colesevelam binds them through strong ionic and hydrophobic interactions. By sequestering bile acids, it prevents their reabsorption in the ileum. This forces the liver to upregulate the enzyme cholesterol 7-alpha-hydroxylase, which converts hepatic cholesterol into new bile acids. To replenish the liver's cholesterol stores, the liver increases the number of LDL receptors, which clears LDL-C from the blood.
Common questions about Colesevelam Hcl
Colesevelam is primarily used for two distinct medical purposes: lowering 'bad' LDL cholesterol and improving blood sugar control in adults with type 2 diabetes. For cholesterol, it works by binding bile acids in the intestine, which forces the liver to use up circulating cholesterol to make more bile. For diabetes, it is used alongside diet and exercise to lower HbA1c levels, although the exact way it lowers blood sugar is still being studied. It is often prescribed when other medications like statins or metformin aren't enough on their own. It is unique because it stays in the digestive tract and never enters the bloodstream. Always use this medication exactly as prescribed by your healthcare provider.
The most common side effects of Colesevelam are related to the digestive system because the drug acts entirely within the gut. Constipation is the most frequently reported issue, affecting about 1 in 10 patients. Other common symptoms include indigestion (dyspepsia), nausea, gas, and mild stomach pain. These side effects are often most noticeable when starting the medication and may improve over time. To help manage constipation, doctors often recommend increasing fluid intake and dietary fiber. If you experience severe abdominal pain or stop having bowel movements entirely, you should contact your doctor immediately.
There is no direct chemical interaction between Colesevelam and alcohol because the drug is not absorbed into your blood. However, drinking alcohol can significantly increase your triglyceride levels, which is a type of fat in the blood. Since Colesevelam can also cause triglycerides to rise, combining the two may increase your risk of developing pancreatitis, a serious inflammation of the pancreas. It is generally recommended to limit alcohol consumption while managing high cholesterol or diabetes. You should discuss your specific alcohol habits with your healthcare provider to ensure it is safe for your situation.
Colesevelam is often considered one of the safer options for managing high cholesterol during pregnancy because it is not absorbed into the bloodstream and does not reach the fetus. Unlike statins, which are generally avoided during pregnancy, Colesevelam stays in the mother's digestive tract. However, it can interfere with the absorption of essential fat-soluble vitamins like Vitamin K, which is vital for healthy blood clotting. For this reason, it should only be used during pregnancy if clearly needed and under strict medical supervision. Your doctor may recommend a prenatal vitamin supplement to ensure you and your baby get enough nutrients. Always inform your doctor if you are pregnant or planning to become pregnant before starting this drug.
For cholesterol reduction, Colesevelam begins to work relatively quickly, with noticeable changes in LDL cholesterol levels usually appearing within 2 weeks of starting the medication. The full effect is typically reached after 4 to 6 weeks of consistent daily use. When used for type 2 diabetes, it may take a bit longer to see the full impact on your blood sugar; doctors usually check your HbA1c levels after about 3 months to evaluate its effectiveness. It is important to take the medication every day with meals to achieve these results. If you stop taking it, your cholesterol and blood sugar levels will likely return to their previous levels within a week or two.
While stopping Colesevelam suddenly does not cause a physical withdrawal syndrome like some other medications, it will cause your cholesterol or blood sugar levels to rise back to their original levels. Because the drug works by physically binding bile acids every day, its benefits stop as soon as the drug is no longer in your system. You should not stop taking Colesevelam without first consulting your healthcare provider, as they will need to discuss alternative treatments to keep your metabolic health on track. If you are experiencing bothersome side effects, your doctor might suggest a dose adjustment or a different formulation instead of stopping entirely. Always keep your medical team informed of any changes you wish to make.
If you miss a dose of Colesevelam, you should take it as soon as you remember, provided you can take it with a meal. If it is already almost time for your next scheduled dose, simply skip the missed dose and continue with your regular routine. You should never take two doses at the same time to 'catch up,' as this significantly increases the risk of severe constipation or a bowel blockage. Since the drug needs to be in your gut when you eat to be effective, timing it with your largest meals is the best strategy. If you frequently forget your doses, consider using a pill organizer or a reminder app to stay consistent.
Colesevelam is not generally associated with weight gain. In clinical trials for both high cholesterol and type 2 diabetes, weight change was not a significant side effect compared to patients taking a placebo. In some cases, patients with type 2 diabetes may even see a slight improvement in weight management as their blood sugar becomes better controlled, though Colesevelam is not a weight-loss drug. If you notice significant or rapid weight changes while taking this medication, it is more likely related to other factors, such as diet, exercise, or other medications you may be taking. Discuss any concerns about your weight with your healthcare provider.
Colesevelam can interact with many other medications by binding them in the digestive tract and preventing them from being absorbed into your body. This is especially true for thyroid medications, blood thinners like warfarin, certain blood pressure drugs, and birth control pills. To avoid this, the general rule is to take your other medications at least 4 hours before or 4 hours after you take your Colesevelam dose. This 'dosing window' ensures that the other drugs have enough time to enter your bloodstream before the Colesevelam polymer arrives in your gut. Always provide your doctor with a full list of all prescriptions, over-the-counter drugs, and supplements you take.
Yes, Colesevelam is available as a generic medication in both tablet and oral suspension (powder) forms. The generic version is bioequivalent to the brand-name drug Welchol, meaning it contains the same active ingredient and works the same way in the body. Generic Colesevelam is typically much more affordable than the brand-name version and is covered by most insurance plans. When switching from a brand-name to a generic, the appearance of the tablets or the flavor of the powder may vary slightly, but the clinical effect should remain the same. Talk to your pharmacist or healthcare provider if you have questions about choosing the generic option.
Other drugs with the same active ingredient (Colesevelam)
> Warning: Stop taking Colesevelam and call your doctor immediately if you experience any of these serious symptoms.
No FDA black box warnings for Colesevelam. However, it carries significant warnings regarding its use in patients with high triglycerides and those at risk for bowel obstruction.
Report any unusual symptoms to your healthcare provider. Managing side effects like constipation often involves increasing dietary fiber and fluid intake, but this should only be done under medical supervision.
Before starting Colesevelam and periodically during treatment, healthcare providers will typically order the following tests:
Colesevelam has no known effect on the ability to drive or operate heavy machinery. It does not cause drowsiness or impair cognitive function, as it does not enter the central nervous system.
There is no direct chemical interaction between Colesevelam and alcohol. However, alcohol can significantly raise triglyceride levels. Since Colesevelam also has the potential to raise triglycerides, excessive alcohol consumption can increase the risk of hypertriglyceridemia and pancreatitis. Patients should discuss their alcohol intake with their doctor.
There is no 'withdrawal syndrome' associated with stopping Colesevelam because it is not systemic. However, stopping the medication will result in the loss of its therapeutic effect. Cholesterol levels and blood glucose levels will likely return to their pre-treatment baselines within 1 to 2 weeks of discontinuation. No tapering is required, but patients should always consult their doctor before stopping any chronic medication.
> Important: Discuss all your medical conditions, especially any history of intestinal problems or high triglycerides, with your healthcare provider before starting Colesevelam.
Colesevelam does not typically interfere with common laboratory tests (like electrolytes or CBC). However, its effect on increasing triglycerides is a physiological change that will be reflected in a lipid panel. It may also interfere with the absorption of radiopaque dyes used in certain GI imaging studies if taken on the same day.
For each major interaction, the mechanism is physical adsorption. The Colesevelam polymer has a large surface area with functional groups that can trap other drug molecules. The clinical consequence is reduced bioavailability and lower blood levels of the co-administered drug. The universal management strategy is staggered dosing: take other medications at least 4 hours before or 4 hours after Colesevelam.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, especially those for thyroid, seizures, or birth control.
In these conditions, the healthcare provider must perform a careful risk-benefit analysis:
There is no known cross-sensitivity between Colesevelam and other classes of lipid-lowering drugs like statins or fibrates. However, patients who have had a severe allergic reaction to other bile acid sequestrants (like cholestyramine or colestipol) should use Colesevelam with caution, although their chemical structures are distinct.
> Important: Your healthcare provider will evaluate your complete medical history, including your surgical history and baseline lipid levels, before prescribing Colesevelam.
Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently than younger subjects. However, in general, elderly patients are more prone to constipation. Healthcare providers should monitor bowel habits closely in older adults. There are no specific pharmacokinetic changes in the elderly because the drug is not absorbed.
No dosage adjustment is necessary for patients with renal impairment. Since the drug is not cleared by the kidneys, even patients with severe chronic kidney disease (CKD) or those on dialysis can take the standard dose. The primary concern in this population is the management of fluid intake, as the powder formulation requires mixing with 4-8 ounces of liquid.
No dosage adjustment is required for patients with hepatic impairment. However, Colesevelam should be used with caution in patients with biliary obstruction, as the drug's mechanism relies on the presence of bile acids in the intestine. If bile flow is blocked, the drug will be ineffective and may cause further GI distress.
> Important: Special populations, particularly pregnant women and children, require individualized medical assessment and frequent monitoring of lipid and vitamin levels.
| Parameter | Value |
|---|---|
| Bioavailability | 0% (Not absorbed) |
| Protein Binding | 0% |
| Half-life | N/A (Non-systemic) |
| Tmax | N/A |
| Metabolism | None |
| Excretion | Fecal (Nearly 100%) |
Colesevelam is classified as a Bile Acid Sequestrant. It is considered a 'second-generation' sequestrant because it has a higher affinity for bile acids and better gastrointestinal tolerability compared to 'first-generation' agents like cholestyramine and colestipol. Within the therapeutic area of dyslipidemia, it is often used as a second-line agent after statins or as an add-on therapy for patients who cannot reach their LDL goals on statins alone.