Inhibitors Of Intestinal Sterol

Absorption
Chemistry & Pharmacokinetics
Ezetimibe : absorbed and conjugated in the
intestine an active glucuronide
Reaching peak blood levels in 12-24 hours
It undergoes enterohepatic circulation
Its half-life is 22 hours
Approximately 80% of the drug is excreted in
feces
Plasma concentration : if its administered with
fibrates
Plasma concentration : if its given with
cholestyramine
Mechanism of Action
Selective inhibitor of intestinal absorption
of cholesterol and phytosterol reduce of
LDL levels
Effective even : absence of dietary
cholesterol
Therapeutic Uses &Dosage
Dosage range : 5 20 mg / d
A single daily dose of 10 mg is used
Average reduction in LDL cholesterol in
primary hypercholesterolemia patient is
about : 18%
HDL cholesterol is increase minimally
Apparently synergistic with reductase
inhibitors
Toxicity
Reversible impaired hepatic function