Colesevelam
Colesevelam Uses, Dosage, Side Effects, Food Interaction and all others data.
Colesevelam is a bile acid sequestrant. Colesevelam is used with exercise and diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in the blood. It works by binding bile acids in the intestine. Bile acids are made when cholesterol is broken down in the body. Removing these bile acids helps to lower blood cholesterol.
Colesevelam is a high capacity bile-acid binding molecule. Colesevelam binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associated with LDL-C) are associated with an increased risk of atherosclerosis in humans. Similarly, decreased levels of high-density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the levels of total-C and LDL-C, and inversely with the level of HDL-C. The combination of colesevelam and an HMG-CoA reductase inhibitor is effective in further lowering serum total-C and LDL-C levels beyond that achieved by either agent alone.
| Trade Name | Colesevelam |
| Availability | Prescription only |
| Generic | Colesevelam |
| Colesevelam Other Names | Colesevelam |
| Related Drugs | Farxiga, Zetia, Praluent, Repatha, atorvastatin, metformin, simvastatin, rosuvastatin, Lipitor, fenofibrate |
| Weight | 3.75g, 625mg |
| Type | Oral powder for reconstitution, oral tablet |
| Protein binding | Not applicable (not hydrolyzed by digestive enzymes and not absorbed). |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Colesevelam is a bile acid sequestrant used to lower LDL-C in adults with hyperlipidemia and pediatric patients with heterozygous familial hypercholesterolemia, and to improve glycemic control in type 2 diabetes.
For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa).
Colesevelam is also used to associated treatment for these conditions: Heterozygous Familial Hypercholesterolemia, Hyperlipidemias, Type 2 Diabetes Mellitus
How Colesevelam works
Colesevelam binds bile acids in the intestine and prevents their reabsorption. Colesevelam is not absorbed itself. The depletion of bile acid causes the upregulation of cholesterol 7-alpha-hydroxylase and conversion of cholesterol to bile acid. this increases the production and activity of hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase in the liver as well as an increase in the number of low density lipoprotein (LDL) receptors. This process clears LDL cholesterol from the blood.
Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol.
Toxicity
Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colesevelam is not absorbed, the risk of systemic toxicity is low. Doses in excess of 4.5 g per day have not been tested.
Food Interaction
- Drink plenty of fluids.
- Take with food.
Colesevelam Cholesterol interaction
[Major] The manufacturer considers the use of colesevelam to be contraindicated in patients with TG levels >500 mg Colesevelam, like other bile acid sequestrants, can increase serum TG concentrations. Lipid parameters, including TG levels and non-HDL-C, should be obtained before starting colesevelam and periodically thereafter. Caution should be exercised when treating patients with TG levels greater than 300 mg Colesevelam should be discontinued if TG levels exceed 500 mg [Moderate] ADJUST DOSING INTERVAL: Bile acid sequestrants and the phosphate binder, sevelamer, can decrease the absorption of fat-soluble vitamins A, D, E, and K. In non-clinical safety studies, rats administered colesevelam at doses greater than 30-fold the projected human clinical dose developed hemorrhage in association with vitamin K deficiency. In a crossover study involving healthy subjects, coadministration of sevelamer with calcitriol resulted in a significant reduction in bioavailability for calcitriol (calcitriol with sevelamer vs calcitriol alone: AUC 137 pg*hColesevelam multivitamins interaction
Oral vitamin supplements should be administered at least 4 hours before colesevelam and either 1 hour before or 4 to 6 hours after other bile acid sequestrants and sevelamer.
Colesevelam Drug Interaction
Moderate: levothyroxine, levothyroxine, cholecalciferol, cholecalciferolUnknown: aspirin, aspirin, apixaban, apixaban, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, metoprolol, metoprolol, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cetirizine, cetirizine
Colesevelam Disease Interaction
Major: diabetic ketoacidosis, gastrointestinal disorders, TGModerate: PKU, malabsorption syndromes
Elimination Route
Not hydrolyzed by digestive enzymes and is not absorbed.
Elimination Route
Excretion: In 16 healthy volunteers, an average of 0.05% of administered radioactivity from a single 14C-labeled colesevelam hydrochloride dose was excreted in the urine.
Innovators Monograph
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