Indications
Alone or with other agents (HMG-CoA reductase inhibitors)
in the management of dyslipidemias including primary
hypercholesterolemia, homozygous familial hypercholesterolemia,
and homozygous sitosterolemia.
Action
Inhibits absorption of cholesterol in the small intestine.
Therapeutic Effects: Lowering of cholesterol, a
known risk factor for atherosclerosis.
Pharmacokinetics
Absorption: Following absorption, rapidly converted
to ezetimibe-glucaronide, which is active. Bioavailability
is variable.
Distribution: Unknown.
Metabolism and Excretion: Undergoes enterhepatic
recycling, mostly eliminated in feces, minimal renal
excretion.
Half-life: 22 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
PO unknown unknown unknown
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Acute liver
disease or unexplained laboratory evidence of liver disease
(when used with HMG-CoA reductase inhibitor);
Moderate or severe hepatic impairment; Concurrent
use of fibrates; OB: May cause fetal harm by interfering
with cholesterol synthesis and, possibly, biologically active
substances derived from cholesterol; Lactation: Potential
for adverse effects in nursing infant.
Use Cautiously in: Pedi: Children 10 yr (safety
not established).
Adverse Reactions/Side Effects
GI: cholecystitis, cholelithiasis,qliver enzymes (with
HMG-CoA reductase inhibitors), nausea, pancreatitis.
Derm: rash. Misc: ANGIOEDEMA.
Interactions
Drug-Drug: Effects may bepby cholestyramine or
other bile acid sequestrants. Concurrent use of fibrates
mayqlevels and the risk of cholelithiasis. Cyclosporine
mayqlevels. Mayqrisk of rhabdomyolysis
when used with HMG CoA-reductase inhibitors.
Route/Dosage
PO (Adults): 10 mg once daily.
Renal Impairment
PO (Adults): CCr 60 mL/min and concurrent use
with simvastatin—Do not exceed simvastatin dose of
20 mg/day.
Availability (generic available)
Tablets: 10 mg. Cost: $517.89/90. In combination
with: simvastatin (Vytorin); see Appendix B.
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