Colestipol

Chemical formula: C₁₁H₂₈ClN₅O  Molecular mass: 281.198 g/mol  PubChem compound: 62816

Pharmacodynamic properties

Ion exchange resin which lowers plasma cholesterol through binding with bile acids in the intestinal lumen.

Pharmacokinetic properties

Colestipol is not absorbed; its action is limited to the lumen of the gastro-intestinal tract, and it is passed in the faeces. It binds bile acids in the intestinal lumen and causes them to be excreted in the faeces together with the polymer. When the enterohepatic circulation of bile acids is interrupted, cholesterol conversion to bile acids is enhanced and plasma cholesterol levels are thereby lowered.

Preclinical safety data

Both clinical and animal studies with colestipol have provided no evidence of drug related intestinal neospasms. Colestipol is not mutagenic in the Ames test.

Reproduction and teratologic studies in animals gave no evidence of drug toxicity in parents or offspring.

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