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Indications and Dosage
Oral
Primary hypercholesterolaemia Adult: As adjunctive therapy to diet in patients for whom a statin is considered inappropriate or not well-tolerated: Initially, 3.75 g daily as a single dose or in 2 divided doses. Max: 4.375 g daily. In combination with statins and/or ezetimibe: 2.5-3.75 g daily as a single dose or in 2 divided doses. Max: 3.75 g daily. Oral Adjunct to type 2 diabetes mellitus Adult: In conjunction with diet and exercise: 3.75 g daily as a single dose or in 2 divided doses.
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Administration
Should be taken with food.
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Contraindications
Bowel or biliary obstruction, serum triglyceride concentrations >500 mg/dL, history of hypertriglyceridaemia-induced pancreatitis.
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Special Precautions
Patient with triglyceride levels ≥300 mg/dL; dysphagia or swallowing disorder (particularly when using tab preparations), gastroparesis, severe gastrointestinal motility disorder, inflammatory bowel disease, liver failure, history of major gastrointestinal tract surgery, risk factors for bowel obstruction, CHD, angina pectoris, susceptibility to fat-soluble vitamin deficiencies. Not indicated for use in the treatment of type 1 diabetes or diabetic ketoacidosis. Pregnancy and lactation.
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Adverse Reactions
Significant: Bowel obstruction (e.g. severe abdominal pain, severe constipation), increased triglyceride levels.
Gastrointestinal disorders: Constipation, flatulence, diarrhoea, vomiting, dyspepsia, abdominal pain or distension, nausea, abnormal stools, dysphagia. General disorders and administration site conditions: Asthenia, flu-like symptoms. Injury, poisoning and procedural complications: Accidental injury. Investigations: Increased serum transaminases. Metabolism and nutrition disorders: Hypoglycaemia. Musculoskeletal and connective tissue disorders: Myalgia, back pain. Nervous system disorders: Headache. Respiratory, thoracic and mediastinal disorders: Pharyngitis, rhinitis. Vascular disorders: Hypertension. |
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Patient Counseling Information
Avoid concurrent administration with other medications. If necessary, take colesevelam at least 4 hours before or at least 4 hours after taking other concomitant medications to minimise the risk of a drug interaction.
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Monitoring Parameters
Hypercholesterolaemia: Obtain lipid parameters before starting treatment and then monitor every 4-12 weeks after initiation of treatment and every 3-12 months thereafter. Type 2 diabetes mellitus: Monitor serum glucose.
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Drug Interactions
May reduce the absorption of fat-soluble vitamins A, D, E, and K. May diminish the anticoagulant effect of warfarin. May reduce the exposures of ciclosporin, olmesartan, phenytoin, levothyroxine, oral contraceptives (e.g. norethindrone, ethinylestradiol), glipizide, glimepiride, and glibenclamide. Concurrent use with the extended-release tab of metformin may increase exposure of metformin. May result in increased triglyceride levels with insulin, thiazolidinediones (e.g. pioglitazone), or sulfonylureas.
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Action
Description:
Mechanism of Action: Colesevelam is a nonabsorbable hydrogel that binds with bile acids in the intestine to form a nonabsorbable complex that is excreted in the faeces. This results in increased conversion of cholesterol to bile acids in the liver causing an increased demand for cholesterol in liver cells leading to a compensatory increase in hepatic uptake of circulating LDL-C. Additionally, its mechanism of action for improving glycaemic control in type 2 diabetes mellitus is unknown. Onset: Lipid-lowering effect: Approx 2 weeks. Reduction of HbA1c: 4-6 weeks. Pharmacokinetics: Absorption: Not absorbed from the gastrointestinal tract. Excretion: Via urine (0.05%). |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 160051, Colesevelam. https://pubchem.ncbi.nlm.nih.gov/compound/Colesevelam. Accessed Feb. 23, 2023. |
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Storage
Store between 15-30°C. Protect from moisture.
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MIMS Class
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ATC Classification
C10AC04 - colesevelam ; Belongs to the class of bile acid sequestrants. Used in the treatment of hyperlipidemia.
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References
Anon. Colesevelam. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 09/01/2023. Anon. Colesevelam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 09/01/2023. Buckingham R (ed). Colesevelam Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/01/2023. Cholestagel 625 mg Film-coated Tablets (Neon Healthcare Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 09/01/2023. Joint Formulary Committee. Colesevelam Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/01/2023. Welchol Tablet, Film Coated; Welchol for Suspension (Cosette Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 09/01/2023.
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