Colestiramina

Colestiramina Uses, Dosage, Side Effects, Food Interaction and all others data.

Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum. Colestiramina resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption.

Colestiramina binds bile in the gastrointestinal tract to prevent its reabsorption. The resin is a strong anion exchange resin, which means that it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer.

Trade Name Colestiramina
Availability Prescription only
Generic Cholestyramine
Cholestyramine Other Names Cholestyramine resin, Colestiramina, Colestyramine
Related Drugs atorvastatin, simvastatin, rosuvastatin, Lipitor, fenofibrate, Crestor, Questran, Prevalite, Cholestyramine Light, Questran Light
Type
Groups Approved, Investigational
Therapeutic Class Bile acid sequestrants
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Colestiramina
Colestiramina

Uses

As an adjunct to dietary therapy & exercise to decrease elevated serum cholesterol in the management of type IIa & type IIb hyperlipoproteinaemia & reduce the risk of atherosclerotic coronary artery disease & MI. Symptomatic control of diarrhoea caused by increased bile acids due to short bowel syndrome. Relief of pruritus associated with partial biliary obstruction.

Colestiramina is also used to associated treatment for these conditions: Atherosclerosis, Primary Hypercholesterolemia, Pruritus

How Colestiramina works

Colestiramina forms a resin that acts as a bile acid sequestrant to limit the reabsorption of bile acids in the gastrointestinal tract. Colestiramina resin is a strong anion exchange resin, allowing it to exchange its chloride anions with anionic bile acids present in the gastrointestinal tract and form a strong resin matrix. Colestiramina consists of a functional group, which is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer, in the anion exchange resin.

Dosage

Colestiramina dosage

Adult: Initially 4 gm 1 to 6 times daily. May be taken with or without food. Do not take in the dry form. Mix with 120-180 ml of water or fruit juice, stir to a uniform consistency before taking.

Side Effects

Constipation, faecal impaction &/or haemorrhoids with or without bleeding, steatorrhoea, hyperchloraemic acidosis, increased urinary calcium excretion, irritation of skin, tongue & perianal area.

Toxicity

Overdose may result in blockage of intestine or stomach.

Precaution

Prolonged use may increase bleeding tendency. Not to be used as monotherapy in patients with hyperlipidaemias associated with hypertriglyceridaemia. Folic acid, vit A & D supplement may be needed in long-term use. Lactation, pregnancy & elderly.

Interaction

Binds & may delay or reduce absorption of thyroid hormones, digitoxin, digoxin, warfarin, Fe salts, chenodiol, phenylbutazone, thiazide diuretics, phenobarb, tetracycline, loperamide, penicillin G, HMG-CoA reductase inhibitors. Admin other drugs 1 hr before or 4-6 hr after cholestyramine.

Food Interaction

  • Take with fluids. Do not take with carbonated fluids.
  • Take with food. Take with a meal unless this interferes with other medications.

Colestiramina multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Bile acid sequestrants and the phosphate binder, sevelamer, can decrease the absorption of fat-soluble vitamins A, D, E, and K.

In non-clinical safety studies, rats administered colesevelam at doses greater than 30-fold the projected human clinical dose developed hemorrhage in association with vitamin K deficiency.

In a crossover study involving healthy subjects, coadministration of sevelamer with calcitriol resulted in a significant reduction in bioavailability for calcitriol (calcitriol with sevelamer vs calcitriol alone: AUC 137 pg*h
Oral vitamin supplements should be administered at least 4 hours before colesevelam and either 1 hour before or 4 to 6 hours after other bile acid sequestrants and sevelamer.

Elimination Route

Not absorbed from the gastrointestinal tract following oral administration.

Half Life

6 minutes

Elimination Route

Colestiramina resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces.

Pregnancy & Breastfeeding use

Pregnancy Category- Not Classified

Contraindication

Complete biliary obstruction.

Innovators Monograph

You find simplified version here Colestiramina

*** Taking medicines without doctor's advice can cause long-term problems.
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