NDICATIONS AND USAGE
Colesevelam hydrochloride is a bile acid sequestrant indicated as an adjunct to diet and exercise to (1)
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reduce elevated low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia as monotherapy or in combination with a hydroxymethyl-glutaryl-coenzyme A (HMG CoA) reductase inhibitor (statin) (1.1).
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reduce LDL-C levels in boys and postmenarchal girls, 10 to 17 years of age, with heterozygous familial hypercholesterolemia as monotherapy or in combination with a statin after failing an adequate trial of diet therapy.
Important Limitations of Use (1.3): (1)
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Do not use for glycemic control in type 1 diabetes or for treating diabetic ketoacidosis.
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Colesevelam hydrochloride tablets have not been studied in type 2 diabetes in combination with a dipeptidyl peptidase 4 inhibitor.
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Colesevelam hydrochloride has not been studied in Fredrickson Type I, III, IV, and V dyslipidemias.
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Colesevelam hydrochloride has not been studied in children younger than 10 years of age or in pre-menarchal girls.
DOSAGE AND ADMINISTRATION
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Colesevelam hydrochloride tablets: The recommended dose is 6 tablets once daily or 3 tablets twice daily. Colesevelam hydrochloride tablets should be taken with a meal and liquid (2.1, 2.2).
DOSAGE FORMS AND STRENGTHS
Tablets: 625 mg (3) (3)
CONTRAINDICATIONS
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Do not use in patients with a history of bowel obstruction (4)
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Do not use in patients with serum triglyceride (TG) concentrations >500 mg/dL (4)
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Do not use in patients with a history of hypertriglyceridemia-induced pancreatitis (4)
WARNINGS AND PRECAUTIONS
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The effect of colesevelam hydrochloride on cardiovascular morbidity and mortality has not been determined (5.1).
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Colesevelam hydrochloride can increase TG. Marked hypertriglyceridemia can cause acute pancreatitis. The effect of hypertriglyceridemia on the risk of coronary artery disease is uncertain. Monitor lipids, including TG and non-high density lipoprotein cholesterol (non-HDL-C) (5.2).
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Bile acid sequestrants may decrease absorption of fat-soluble vitamins. Use caution in patients susceptible to fat-soluble vitamin deficiencies (5.3).
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Because of its constipating effects, colesevelam hydrochloride is not recommended in patients at risk of bowel obstruction (e.g., patients with gastroparesis, other gastrointestinal motility disorders or a history of major gastrointestinal surgery) (5.4).
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Colesevelam hydrochloride reduces gastrointestinal absorption of some drugs. Administer drugs with a known interaction with colesevelam at least 4 hours prior to colesevelam hydrochloride. Drugs that have not been tested for interaction with colesevelam, especially those with a narrow therapeutic index, should also be administered at least 4 hours prior to colesevelam hydrochloride. Alternatively, monitor drug levels of the co-administered drug (5.5, 7, 12.3).
ADVERSE REACTIONS
In clinical trials, the most common (incidence ≥2% and greater than placebo) adverse reactions with colesevelam hydrochloride included constipation, dyspepsia, and nausea. (6)
Postmarketing reports with concomitant colesevelam hydrochloride administration include: (6)
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Increased seizure activity or decreased phenytoin levels in patients receiving phenytoin. Administer phenytoin 4 hours prior to colesevelam hydrochloride.
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Reduced International Normalized Ratio (INR) in patients receiving warfarin. Monitor INR.
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Elevated thyroid-stimulating hormone (TSH) in patients receiving thyroid hormone replacement therapy. Administer thyroid hormones 4 hours prior to colesevelam hydrochloride.
Other postmarketing reports include bowel obstruction, dysphagia, esophageal obstruction, fecal impaction, hypertriglyceridemia, pancreatitis, and increased transaminases (5.5, 6.2, 7, 12.3). (6)
To report SUSPECTED ADVERSE REACTIONS, contact Glenmark Pharmaceuticals Inc., USA at 1-888-721-7115 or FDA at 1-800-FDA-1088 or https://www.fda.gov/medwatch. (6)
DRUG INTERACTIONS
In drug interaction studies, colesevelam hydrochloride reduced levels of cyclosporine, glimepiride, glipizide, glyburide, levothyroxine, olmesartan medoxomil, and oral contraceptives containing ethinyl estradiol and norethindrone. Colesevelam hydrochloride increased levels of metformin when coadministered with metformin extended release. There have been postmarketing reports of decreases in phenytoin levels in patients receiving phenytoin concomitantly with colesevelam hydrochloride and decreases in INR in patients receiving warfarin concomitantly with colesevelam hydrochloride (5.5, 7, 12.3). (7)
See 17 for PATIENT COUNSELING INFORMATION.
Revised: 5/2018
