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CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › Bile acid sequestrants
colesevelam
C10AC04
Forms & Strengths
- Oral tablet: 625 mg
- Oral suspension powder: 3.75 g/packet
Adult Dosing
- Hyperlipidemia: 3.75 g daily (either 6 tablets once daily or 3 tablets twice daily with a meal) or one 3.75 g packet suspension daily
- Type 2 Diabetes Mellitus: 3.75 g daily administered as 6 tablets once daily or 3 tablets twice daily with a meal
Pediatric Dosing
- Heterozygous familial hypercholesterolemia (Boys and postmenarchal girls aged 10-17 years): 1.875 g daily (3 tablets) up to 3.75 g daily (6 tablets) with a meal
Indications
- Reduction of elevated LDL-C in primary hyperlipidemia as monotherapy or adjunct to statin therapy
- Improvement of glycemic control in adults with type 2 diabetes mellitus
Mechanism of Action
- Non-absorbed, polymeric bile acid sequestrant that binds bile acids in the intestine, preventing their reabsorption
- Increases hepatic conversion of cholesterol to bile acids, reducing total body cholesterol and LDL-C
- Upregulates hepatic LDL receptors
Contraindications
- History of bowel obstruction
- Serum triglyceride levels > 500 mg/dL
- History of hypertriglyceridemia-induced pancreatitis
Adverse Reactions
- Constipation
- Nasopharyngitis
- Dyspepsia
- Myalgia
- Hypertriglyceridemia
- Increased blood triglycerides
Drug Interactions
- Decreases absorption of fat-soluble vitamins (A, D, E, K)
- May decrease bioavailability of co-administered oral medications; administer other drugs at least 1 hour before or 4 hours after colesevelam
- Cyclosporine: decreased exposure (monitor levels)
- Levothyroxine: decreased absorption (separate administration by at least 4 hours)
- Oral contraceptives containing ethinyl estradiol and norethindrone: potential alterations in absorption
Curated Content: Needs Vetting Before Put to Clinical Use