Cholesterol Absorption Inhibitors
It interferes with absorption of cholesterol and phytosterols in small intestine by interfering with a transport protein NPC1L1.
- Decreases absorption of cholesterol
- Decrease delivery of cholesterol to liver
- In turn, decrease production of lipids
- Decrease LDL by 17-18%
- Decrease TG by 6%
- Increase HDL by 1-2%
Not very potent drug. Given only when patient is not responding to other drugs.
a. Absorption –Exetimibe is readily absorbed
b. Metabolized by glucuronidation
c. PPC achieved in 12 hours
d. Half life –undergoes enterohepatic circulation so half life is increased up to 22 hours.
e. Elimination -80% in faeces
f. When co-administered with fibrates, there is increased plasma concentration of this drug.
g. When co-administered with bile acid binding resins, concentration decreases.
1. GIT –can interfere with absorption of lipids -steatorrhea
2. Can produce liver injury
3. Rarely myositis
4. Does not interfere with absorption of fat soluble vitamins
- Precursors of TGs
- Decrease levels of VLDL, TG, and LDL.
- Dose -5 g/day.
- Weight reducing agent that decreases plasma lipid levels.
- Decreases absorption of fatty acids and increases excretion, so plasma levels of lipids are decreased
- Inhibits lipases in stomach, pancreas and intestines and decreases plasma lipid levels.
- Loss of dietary lipids is about 30%
- Loss of weight is about 5-10%
Interfere with absorption of fat soluble vitamins
Interfere with absorption of lipids
Given in a dose of 120 mg, thrice a day. Effect is very slow, and takes about 1-2 months. If there is decrease in weight in those 1-2 months, then continued for 2 years.