What is ezetimibe, and how does it work (mechanism of action)?
Ezetimibe is an oral drug that is used for
the treatment of
elevated blood cholesterol. The most commonly used class of
drugs for lowering cholesterol levels, the statins, act by preventing the
production of cholesterol by the liver. Ezetimibe has a different mechanism of
action and lowers blood cholesterol by reducing the absorption of cholesterol
from the intestine. It does not affect the absorption of triglycerides or
fat-soluble vitamins. The FDA approved ezetimibe in October 2002.
What brand names are available for ezetimibe?
Zetia
Is ezetimibe available as a generic drug?
GENERIC AVAILABLE: No
Do I need a prescription for ezetimibe?
Yes
What are the side effects of ezetimibe?
The most common side effects of ezetimibe are:
- diarrhea,
- abdominal pain,
- back pain,
- joint pain,
- muscle aches, and
- sinusitis.
Hypersensitivity reactions, including angioedema (swelling of the skin and
underlying tissues of the head and neck that can be life-threatening) and skin
rash rarely occur.
Other important side effects include:
- Nausea,
- pancreatitis,
- muscle damage (myopathy or rhabdomyolysis) and
- hepatitis
What is the dosage for ezetimibe?
The recommended dose of ezetimibe is 10 mg daily. Ezetimibe
can be taken with or without food and at the same time as statin drugs.
Which drugs or supplements interact with ezetimibe?
Cholestyramine (Questran), colestipol (Colestid)
and colesevelam (WelChol), bile acid-binding drugs that may be used to treat
elevated levels of cholesterol, bind to ezetimibe and reduce its absorption from
the intestine by about 50%. Therefore, ezetimibe should be taken at least two
hours before or 4 hours after administration of these drugs. Cyclosporine (Gengraf,
Neoral) increases the levels of ezetimibe while ezetimibe increases levels of
cyclosporine. Combining both drugs may increase side effects of either drug.
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Is ezetimibe safe to take if I’m pregnant or breastfeeding?
There are no adequate studies of ezetimibe in
pregnant
women. Therefore, physicians must weight the benefit of prescribing ezetimibe
during pregnancy against potential but unknown risks.
There are no adequate studies of ezetimibe in women
who are breastfeeding. Therefore, physicians must weight the benefit of prescribing ezetimibe to
nursing women against potential but unknown risks.
What else should I know about ezetimibe?
What preparations of ezetimibe are available?
Tablets, 10 mg
How should I keep ezetimibe stored?
Ezetimibe tablets should be stored between 15-30 C (59-86 F).