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To what class of drugs does colesevelam belong?
Bile acid sequesterants
What are the indications associated with colesevelam?
What is unique about colesevelam's chemical structure and its absorption characteristics?
Colesevelam is a large, insoluble cationic polymer (MW 618). It is non-absorbable and remains intact in the GI until it is eliminated in the feces.
What is colesevelam's target MOA?
It binds bile acids in the GI.
How does colesevelam's MOA work to reduce cholesterol in the body?
As bile acid is sequestered in the GI, it decreases the bile acid pool, leading to a compensatory increase in conversion of cholesterol to bile.
The action of what enzyme is ramped up to compensate for the bile-sequestering action of colesevelam?
What are some adverse effects associated with colesevelam?
- Hyperchloremia (as Cl- interacts with cationic groups of colesevelam)
- Hyperchloremic acidosis (as HCO3- is ramped up to compensate for lack of Cl-)
- Abdominal cramps, bloating, dyspepsia
- Drug and food interactions (altered absorption)
True or false?
Colesevelam is safe in both pregnant women and children with a genetic predisposition to hypercholesterolemia.
True - due to its absorption characteristics.