Colestyramine: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Primary hypercholesterolaemia

Adult: Doses are expressed in terms of anhydrous colestyramine. As an adjunct to dietary therapy: Initially, 4 g daily, then increased by 4 g at weekly intervals to 12-24 g daily in 1-4 divided doses. Adjust dose according to dosage requirements and patient's response. Max: 36 g daily. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Child: Optimal dosage for this population has not been established. Doses may be calculated based on body weight, either as a percentage of the adult (70 kg) dose or a dose of 240 mg/kg daily in 2-3 divided doses (Max: 8,000 mg daily). Dosage recommendations may vary among countries or individual products (refer to specific product guidelines).

Oral
Primary prevention of coronary heart disease

Adult: Men aged 35-59 years Doses are expressed in terms of anhydrous colestyramine. In patients with primary hypercholesterolaemia who have not responded to diet and other appropriate measures: Initially, 4 g daily, then increased by 4 g at weekly intervals to 12-24 g daily in 1-4 divided doses. Adjust dose according to dosage requirements and patient's response. Max: 36 g daily. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
Pruritus associated with partial biliary obstruction

Adult: Doses are expressed in terms of anhydrous colestyramine. For relief of pruritus: 4-8 g daily.
Child: Optimal dosage for this population has not been established. Doses may be calculated based on body weight as 240 mg/kg daily in 2-3 divided doses. Max: 8,000 mg daily. Dosage recommendations may vary among countries or individual products (refer to specific product guidelines).

Oral
Diarrhoea

Adult: Doses are expressed in terms of anhydrous colestyramine. For relief of cases associated with Crohn's disease, ileal resection, vagotomy, diabetic vagal neuropathy, and radiation: Initially, 4 g daily, then increased by 4 g at weekly intervals to 12-24 g daily in 1-4 divided doses. Adjust dose according to dosage requirements and patient's response. Max: 36 g daily. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).

Administration

May be taken with or without food. Do not take in the dry form. Mix w/ 150 mL of water or fruit juice, stir to a uniform consistency before taking.

Reconstitution

Mix the powder (containing 4 g of anhydrous colestyramine) with 60-180 mL of water or other noncarbonated liquid (e.g. fruit juice) and stir to a uniform consistency. May also be mixed with skimmed milk, thin soups or pulpy fruits with high moisture content (e.g. applesauce or crushed pineapple).

Contraindications

Complete biliary obstruction.

Special Precautions

Patient with constipation, triglyceride levels of 250-299 mg/dL, volume depletion; susceptibility to fat-soluble vitamin deficiencies. Renal impairment. Children. Pregnancy and lactation.

Adverse Reactions

Significant: May produce or exacerbate constipation; increased bleeding tendencies; hyperchloraemic acidosis (prolonged use, particularly in children); decreased serum folate (particularly in children).
Gastrointestinal disorders: Abdominal discomfort and/or pain, flatulence, nausea, vomiting, diarrhoea, heartburn, dyspepsia, steatorrhoea, irritation in the perianal area, tongue irritation.
Metabolism and nutrition disorders: Anorexia.
Musculoskeletal and connective tissue disorders: Osteoporosis.
Skin and subcutaneous tissue disorders: Rash, skin irritation.
Potentially Fatal: Rarely, intestinal obstruction (particularly in children).

Pregnancy Category (US FDA)

PO: C

Monitoring Parameters

Rule out secondary causes of hypercholesterolaemia (e.g. poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinaemia, obstructive liver disease, other drug therapy, alcoholism) and obtain lipid profile before initiating therapy. Monitor lipid profile during the 1st few months and periodically thereafter.

Drug Interactions

May delay or reduce the absorption of digoxin, tetracycline, benzylpenicillin, thiazide diuretics, phenobarbital, phenylbutazone, warfarin, propranolol, thyroid hormones, estrogens and progestins, and Fe salts. May prevent the absorption of fat-soluble vitamins (e.g. vitamins A, D, E and K). May interfere with the absorption of oral phosphate supplements.

Action

Description:
Mechanism of Action: Colestyramine, a bile acid sequestrant, acts by binding with bile acids in the intestine to form a nonabsorbable complex that is excreted in the faeces, resulting in partial removal of bile acids from the enterohepatic circulation. This action leads to increased oxidation of cholesterol to bile acids and reduced low-density lipoprotein serum levels and serum cholesterol levels.
Synonyms: cholestyramine; cholestyramine resin.
Onset: 21 days (peak effect).
Pharmacokinetics:
Absorption: Not absorbed from the gastrointestinal tract.
Excretion: Via faeces (as an insoluble complex with bile acids).

Storage

Store between 15-30°C.

MIMS Class

Dyslipidaemic Agents

ATC Classification

C10AC01 - colestyramine ; Belongs to the class of bile acid sequestrants. Used in the treatment of hyperlipidemia.

References

Anon. Cholestyramine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/01/2023.

Anon. Colestyramine [Cholestyramine] Resin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/01/2023.

Buckingham R (ed). Colestyramine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/01/2023.

Cholestyramine for Oral Suspension Powder (Chartwell RX, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 20/04/2023.

Joint Formulary Committee. Colestyramine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/01/2023.

Pharmacy Retailing (NZ) Limited Trading as Healthcare Logistics. Questran Lite Oral Suspension data sheet May 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 03/01/2023.

Prevalite Oral Suspension (Upsher-Smith Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/01/2023.

Questran 4 g/Sachet Powder for Oral Suspension (Neon Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 03/01/2023.

Questran Light 4 g/Sachet Powder for Oral Suspension (Neon Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 03/01/2023.

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