Version May 2024
Note: Due to large tablet size, the manufacturer recommends packets of oral suspension for pediatric patients. Overall, with dyslipidemia management, lifestyle changes are recommended to be implemented for at least 6 to 12 months before beginning pharmacotherapy (Ref). Bile acid sequestrant therapy may be considered for LDL/apo B reduction and mild HDL increases but should not be used in pediatric patients with hypertriglyceridemia. Multivitamin supplementation recommended due to potential folic acid and cholecalciferol malabsorption (Ref).
Heterozygous familial hypercholesterolemia: Children ≥10 years and Adolescents: Oral: 3.75 g once daily or in divided doses twice daily.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Children ≥10 years and Adolescents: No adjustment necessary; not absorbed from the GI tract.
Children ≥10 years and Adolescents: No dosage adjustment necessary; not absorbed from the GI tract.
(For additional information see "Colesevelam: Drug information")
Diarrhea associated with bile acid malabsorption (off-label use): Oral: 3.75 g/day in 1 or 2 divided doses (Ref).
Hyperlipidemia (primary), diabetes mellitus (type 2): Oral: 3.75 g/day in 1 or 2 divided doses.
Note: Use may be considered in patients with fasting triglyceride level ≤300 mg/dL who do not meet cholesterol treatment goals with dietary modification and other lipid lowering therapies (eg, maximally tolerated statin and ezetimibe) (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
No dosage adjustments necessary; not absorbed from the gastrointestinal tract.
No dosage adjustments necessary; not absorbed from the gastrointestinal tract.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Actual frequency may be dependent upon indication. Unless otherwise noted, frequency of adverse effects is reported for adult patients.
>10%: Gastrointestinal: Constipation (3% to 11%)
1% to 10%:
Cardiovascular: Cardiovascular toxicity (2%, including myocardial infarction, aortic stenosis, bradycardia), hypertension (2% to 3%)
Central nervous system: Headache (children and adults 4% to 8%), fatigue (children 4%)
Endocrine & metabolic: Hypertriglyceridemia (4% to 5%; >500 mg/dL: <1%; >1,000 mg/dL: <1%), hyperglycemia (3%), hypoglycemia (3%)
Gastrointestinal: Dyspepsia (3% to 8%), diarrhea (4%), nausea (children and adults 3% to 4%), gastroesophageal reflux disease (2%), periodontal abscess (2%), vomiting (children 2%)
Hematologic & oncologic: C-reactive protein increased (3%)
Infection: Influenza (children and adolescents 4%)
Neuromuscular & skeletal: Weakness (4%), back pain (2%), increased creatine phosphokinase (children and adults 2%), myalgia (2%)
Respiratory: Nasopharyngitis (children 5% to 6%), upper respiratory tract infection (children and adults 3% to 5%), flu-like symptoms (children 4%), pharyngitis (3%), rhinitis (children 2%)
<1%, postmarketing, and/or case reports: Abdominal distension, dysphagia, esophageal obstruction, fecal impaction, flatulence, worsening of hemorrhoids, increased serum transaminases, infection, intestinal obstruction, pancreatitis, unstable angina pectoris
History of bowel obstruction; serum TG concentrations of more than 500 mg/dL; history of hypertriglyceridemia-induced pancreatitis.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to colesevelam or any component of the formulation; biliary obstruction
Disease-related concerns:
• Gastrointestinal disease: Use is not recommended in patients with gastroparesis, other severe GI motility disorders, a history of major GI tract surgery, or patients at risk for bowel obstruction. Use tablets with caution in patients with dysphagia or swallowing disorders; use the oral suspension form of colesevelam due to large tablet size and risk for esophageal obstruction. Discontinue if symptoms of bowel obstruction occur (eg, severe abdominal pain, severe constipation).
• Hypertriglyceridemia: Bile acid sequestrants can increase serum triglyceride concentrations; severely elevated triglycerides can cause acute pancreatitis. The manufacturer contraindicates use if triglycerides exceed 500 mg/dL and in patients with a history of hypertriglyceridemia-induced pancreatitis. The American College of Cardiology/American Heart Association recommends avoiding use in patients with baseline fasting triglyceride levels ≥300 mg/dL (ACC/AHA [Grundy 2018]). Use with caution in patients using insulin, thiazolidinediones, or sulfonylureas (may cause increased triglyceride concentrations). Discontinue if symptoms of acute pancreatitis occur (eg, severe abdominal pain with or without nausea and vomiting).
• Patients susceptible to fat-soluble vitamin deficiencies: Use with caution in patients susceptible to fat-soluble vitamin deficiencies. Absorption of fat soluble vitamins A, D, E, and K may be decreased; patients should take vitamins ≥4 hours before colesevelam.
• Phenylketonuria: Some products may contain phenylalanine; use with caution.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
Other warnings/precautions:
• Appropriate use: Primary hyperlipidemia: Has not been studied in types I, III, IV, and V dyslipidemias. Diabetes: Not for use in patients with diabetic ketoacidosis (DKA) or patients with type 1 diabetes mellitus. Unlike adults, colesevelam was not shown to improved glycemic control in pediatric patients 10 to 17 years of age with type 2 diabetes mellitus in clinical trials.
Welchol contains phenylalanine 27 mg per 3.75 gram packet
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Packet, Oral, as hydrochloride:
Welchol: 3.75 g (30 ea) [contains aspartame, propylene glycol alginate]
Welchol: 3.75 g (30 ea [DSC]) [sugar free; contains aspartame]
Generic: 3.75 g (1 ea, 30 ea)
Tablet, Oral, as hydrochloride:
Welchol: 625 mg
Generic: 625 mg
Yes
Pack (Colesevelam HCl Oral)
3.75 g (per each): $22.45 - $22.49
Pack (Welchol Oral)
3.75 g (per each): $32.35
Tablets (Colesevelam HCl Oral)
625 mg (per each): $3.74 - $3.96
Tablets (Welchol Oral)
625 mg (per each): $5.39
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Packet, Oral, as hydrochloride:
Lodalis: 3.75 g (3.75 g) [contains aspartame, propylene glycol alginate]
Tablet, Oral, as hydrochloride:
Lodalis: 625 mg
Generic: 625 mg
Oral:
Granules for oral suspension: Administer with meals. Dissolve in liquid prior to administration (see Preparation for Administration); do not take in dry form (to avoid esophageal distress).
Tablets: Due to tablet size, it is recommended that any patient who has trouble swallowing tablets, including pediatric patients, should avoid use of tablets and use the oral suspension or chewable bars dosage forms. Administer with meal(s) and a liquid.
Granules for oral suspension: Administer with meal(s). Powder is not to be taken in dry form (to avoid esophageal distress).
Tablets: Administer with meal(s) and a liquid. Due to tablet size, it is recommended that any patient who has trouble swallowing tablets should use the oral suspension form.
Store at 25°C (77°F). Excursions permitted to 15°C to 30°C (59°F to 86°F); brief excursions permitted to 40°C (104°F) (tablets only). Protect from moisture.
Management of heterozygous familial hypercholesterolemia (HeFH) who are unable to achieve LDL-C targets despite dietary and lifestyle modification (FDA approved in boys and postmenarchal girls 10 to 17 years of age); management of elevated LDL in primary hyperlipidemia in conjunction with diet and exercise (FDA approved in adults); improve glycemic control in type 2 diabetes mellitus (noninsulin dependent, NIDDM) in conjunction with diet and exercise (FDA approved in adults)
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Amiodarone: Bile Acid Sequestrants may decrease the bioavailability of Amiodarone. Management: Consider alternatives to this combination due to the risk of subtherapeutic amiodarone serum concentrations. If amiodarone is coadministered with colesevelam, administer amiodarone at least 4 hours before colesevelam. Risk D: Consider therapy modification
Chenodiol: Bile Acid Sequestrants may decrease the serum concentration of Chenodiol. Management: Administration of chenodiol 5 hours or more after bile acid sequestrants may reduce the magnitude of this interaction. Monitor for decreased therapeutic effects of chenodiol in patients receiving bile acid sequestrants. Risk D: Consider therapy modification
Cholic Acid: Bile Acid Sequestrants may decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 hour before or 4 to 6 hours after administration of any bile acid-binding products to minimize the potential for a significant interaction. Risk D: Consider therapy modification
Corticosteroids (Oral): Bile Acid Sequestrants may decrease the absorption of Corticosteroids (Oral). Risk C: Monitor therapy
CycloSPORINE (Systemic): Colesevelam may decrease the serum concentration of CycloSPORINE (Systemic). Management: Administer cyclosporine at least 4 hours prior to colesevelam. Monitor for decreased cyclosporine concentrations during concomitant colesevelam therapy. Risk D: Consider therapy modification
Deferasirox: Bile Acid Sequestrants may decrease the serum concentration of Deferasirox. Management: Avoid combination when possible; if the combination must be used, consider a 50% increase in initial deferasirox dose, with monitoring of serum ferritin concentrations and clinical responses to guide further dosing. Risk D: Consider therapy modification
Ethinyl Estradiol-Containing Products: Bile Acid Sequestrants may decrease the serum concentration of Ethinyl Estradiol-Containing Products. Management: Administer ethinyl estradiol-containing products 4 hours prior to the administration of a bile acid sequestrant. Risk D: Consider therapy modification
Ezetimibe: Bile Acid Sequestrants may decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Risk D: Consider therapy modification
Glimepiride: Colesevelam may decrease the serum concentration of Glimepiride. Management: Administer glimepiride at least 4 hours prior to colesevelam. Risk D: Consider therapy modification
GlipiZIDE: Colesevelam may decrease the serum concentration of GlipiZIDE. Management: Administer glipizide at least 4 hours prior to colesevelam. Risk D: Consider therapy modification
GlyBURIDE: Colesevelam may decrease the serum concentration of GlyBURIDE. Management: Administer glyburide at least 4 hours prior to colesevelam. Risk D: Consider therapy modification
Leflunomide: Bile Acid Sequestrants may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Risk D: Consider therapy modification
Lomitapide: Bile Acid Sequestrants may decrease the absorption of Lomitapide. Management: Administer lomitapide at least 4 hours before or after administration of a bile acid sequestrant. Risk D: Consider therapy modification
Loop Diuretics: Bile Acid Sequestrants may decrease the absorption of Loop Diuretics. Risk C: Monitor therapy
Maralixibat: Bile Acid Sequestrants may decrease the serum concentration of Maralixibat. Management: Bile acid sequestrants should be administered either at least 4 hours before, or 4 hours after, maralixibat. Risk D: Consider therapy modification
Methotrexate: Bile Acid Sequestrants may decrease the absorption of Methotrexate. Risk C: Monitor therapy
Multivitamins/Fluoride (with ADE): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Fluoride (with ADE). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Risk D: Consider therapy modification
Multivitamins/Minerals (with ADEK, Folate, Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, bile acid sequestrants may impair the absorption of fat-soluble vitamins. Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Risk D: Consider therapy modification
Multivitamins/Minerals (with AE, No Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with AE, No Iron). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Risk D: Consider therapy modification
Mycophenolate: Bile Acid Sequestrants may decrease the serum concentration of Mycophenolate. Risk X: Avoid combination
Niacin: Bile Acid Sequestrants may decrease the absorption of Niacin. Management: Consider separating the administration times of niacin and bile acid sequestrants by a few hours in order to reduce the potential for decreased efficacy of these agents. Risk D: Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents: Bile Acid Sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Risk C: Monitor therapy
Norethindrone: Colesevelam may decrease the serum concentration of Norethindrone. Management: Oral contraceptives containing ethinyl estradiol and norethindrone should be administered at least 4 hours before colesevelam. Risk D: Consider therapy modification
Obeticholic Acid: Bile Acid Sequestrants may decrease the serum concentration of Obeticholic Acid. Management: Administer obeticholic acid at least 4 hours before or at least 4 hours after the administration of bile acid sequestrants. Risk D: Consider therapy modification
Odevixibat: Bile Acid Sequestrants may decrease the serum concentration of Odevixibat. Management: Bile acid sequestrants should be administered either at least 4 hours before, or 4 hours after, odevixibat. Risk D: Consider therapy modification
Olmesartan: Colesevelam may decrease the serum concentration of Olmesartan. Management: Administer olmesartan at least 4 hours prior to colesevelam. Risk D: Consider therapy modification
Phenytoin: Colesevelam may decrease the serum concentration of Phenytoin. Management: Administer phenytoin at least 4 hours prior to colesevelam. Risk D: Consider therapy modification
Pravastatin: Bile Acid Sequestrants may decrease the serum concentration of Pravastatin. Management: Administer pravastatin at least 1 hour before or 4 hours after administration of bile-acid resins (eg, cholestyramine, colestipol, colesevelam) to minimize the risk for any significant interaction. Risk D: Consider therapy modification
Propranolol: Bile Acid Sequestrants may decrease the serum concentration of Propranolol. Risk C: Monitor therapy
Raloxifene: Bile Acid Sequestrants may decrease the absorption of Raloxifene. Management: Consider separating the doses of raloxifene and bile acid sequestrants by at least 4 hours. Risk D: Consider therapy modification
Taurursodiol: Bile Acid Sequestrants may decrease the absorption of Taurursodiol. Risk X: Avoid combination
Teriflunomide: Bile Acid Sequestrants may decrease the serum concentration of Teriflunomide. Management: Unless using this combination to intentionally enhance teriflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is unlikely to be effective at avoiding the interaction. Risk D: Consider therapy modification
Tetracyclines: Bile Acid Sequestrants may decrease the absorption of Tetracyclines. Risk C: Monitor therapy
Thiazide and Thiazide-Like Diuretics: Bile Acid Sequestrants may decrease the absorption of Thiazide and Thiazide-Like Diuretics. The diuretic response is likewise decreased. Management: Consider separating administraton of bile acid sequestrants and thiazide diuretics by at least 4 hours. Monitor for decreased therapeutic effects of thiazide diuretics if coadministered with a bile acid sequestrant. Risk D: Consider therapy modification
Thyroid Products: Bile Acid Sequestrants may decrease the serum concentration of Thyroid Products. Management: Administer oral thyroid products at least 4 hours prior to or one hour after bile acid sequestrants, or monitor for decreased serum concentrations and clinical effects of oral thyroid products during coadministration. Risk D: Consider therapy modification
Ursodiol: Bile Acid Sequestrants may decrease the serum concentration of Ursodiol. Management: Administer ursodiol 1 hour before or at least 4 to 5 hours after bile acid sequestrants to minimize the potential for any significant interaction. Monitor for decreased therapeutic effects of ursodiol in patients receiving bile acid sequestrants. Risk D: Consider therapy modification
Vitamin D Analogs: Bile Acid Sequestrants may decrease the serum concentration of Vitamin D Analogs. More specifically, bile acid sequestrants may impair absorption of Vitamin D Analogs. Management: Avoid concomitant administration of vitamin D analogs and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the potential risk of interaction. Monitor plasma calcium concentrations. Risk D: Consider therapy modification
Warfarin: Colesevelam may diminish the anticoagulant effect of Warfarin. Risk C: Monitor therapy
Some products may contain phenylalanine.
Colesevelam may reduce the efficacy of oral contraception; consult drug interactions database for detailed information.
Colesevelam is not absorbed systemically following oral administration and maternal use is not expected to result in fetal exposure to the drug.
Lipid concentrations increase during pregnancy as required for normal fetal development. When increases are greater than expected, supervised dietary intervention should be initiated. Bile acid sequestrants are recommended when treatment is needed, and therapy with colesevelam is preferred (Avis 2009; Jacobson 2015).
Colesevelam may interfere with maternal vitamin absorption; therefore, regular supplementation may not be adequate.
Pediatric patients: Fasting lipid profile (including triglycerides; baseline, 4 to 6 weeks after initiation, and then every 6 to 12 months), growth, maturation, number of stools per day (NHLBI 2011)
Adults:
Lipid profile (fasting or nonfasting) should be rechecked 4 to 12 weeks after starting therapy and every 3 to 12 months thereafter (AHA/ACC [Grundy 2018])
Diabetes mellitus, type 2: Serum glucose and HbA1c (at least twice yearly in patients who have stable glycemic control and are meeting treatment goals; quarterly in patients not meeting treatment goals or with therapy change [ADA 2019])
Pediatric: Lipid treatment goals: May vary depending on clinical condition, different clinical practice guidelines, and expert opinion. Refer to clinical practice guidelines for specific treatment goals (AACE [Jellinger 2017]).
Adult:
Diabetes mellitus, type 2: Recommendations for glycemic control in nonpregnant adults with diabetes (ADA 2019):
HbA1c: <7% (a more aggressive [<6.5%] or less aggressive [<8%] HbA1c goal may be targeted based on patient-specific characteristics)
Preprandial capillary blood glucose: 80 to 130 mg/dL (SI: 4.4 to 7.2 mmol/L).
Peak postprandial capillary blood glucose: <180 mg/dL (SI: <10 mmol/L).
Lipid treatment goals: May vary depending on clinical condition, different clinical practice guidelines, and expert opinion. Refer to clinical practice guidelines for specific treatment goals.
Cholesterol is the major precursor of bile acid. Colesevelam binds with bile acids in the intestine to form an insoluble complex that is eliminated in feces. This increased excretion of bile acids results in an increased oxidation of cholesterol to bile acid and a lowering of the serum cholesterol.
Onset of action:
Lipid lowering: Therapeutic: ~2 weeks
Reduction of hemoglobin A1c (Type II diabetes): 4-6 weeks initial onset; 12-18 weeks maximal effect
Absorption: None
Excretion: Urine (0.05%)
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