Ezetimibe has no effect on the CYP450 enzymes, therfore it is unlikely to interact with drugs
 metabolized by these enzymes.

Concomittant administration of ezetimibe with cholestyramine decreases the mean area under the
 curve (AUC) of ezetimibe by approximately 55% which may result in lower than expected LDL-C
 reduction.

Ezetimibe dosed at least two hours before or four hours after a bile acid-sequentrantmay decrease
 the changes of this interaction.

There was a 12-fold- increase in total ezetimibe level in a renal transplant patient receiving
cyclosporine, therfore dose monitoring is recommended for patients receiving concomittant ezetimibe
and cyclosporine.

Ezetimibe appears to be generally well tolerated with adverse events being mild and transcient.
The most common adverse events observed are abdominal discomfort, headache, diarrhoea,  
back pain, arthalgia, respiratory infection and fatigue.

Special precautions-

Ezetimbe is not recommended in patients with moderate or severe hepatic insufficiency

When ezetimibe is administered with a statin liver function tests should be peformed at initiation
 of therapy and according to the recommendations of the statin.

Safety and efectiveness of ezetimibe with fibrates have not been established and therfore
co-administration of ezetimibe with fibrates is not recommended untilfurther stsidies are available.

In clinical trials, ezitimibe did not cause a further increase in myopathy or  rhabdomylosis when added
 to statin therapy

Lactation
Pregnancy
Moderate to severe hepatic impairment
Concomittant use with a statin in active liver disease
Unexplained pesistent elevation in transaminases

Special Precautions-
Monitor liver functions if given with statin
Labour and delivery

 

Date of Approval-                             04-04-07 

indication-

Hypercholesterolaemia

Dosage-
The recoomended dose of ezetimibe is 10mg once daily orally, as monotherapy or in combination
 with a satin.
No dosage adjustments are required intheelderly,in patients with mild hepatic insufficiency or renal
 insufficiency
Ezetimibe should be administered either 2 hours before or 4 hours after administration of a bile
sequestrant.

Pharmacology-

Ezetimibe localizes at the brush border of the small intestine where it inhibits the absorption of cholesterol, decreasing the delivery of intestinal cholesterol to the liver. Cholesterol absorption is an active process and entimibe inhibits the protein transporters on small intestinal enterocyte brush  border which bring about the active transport.

This decrease the cholesterol stores within the liver and ultimately increases clearance of cholesterol  from the blood.

It does not inhibit cholesterol synthesis in the liver, as do statins. By their distinct mechanisms of  action , ezetimibe and statins provide complimentary cholesterol  reduction.

Pharmocokinetics-

Following oral administration ezetimibe is rapidly absorbed and extensively               conjugated to a pharmacologically active phenolic glucoronide accounting                          for 80 -90% of drug in plasma  (ezitimibe glucoronide).
Mean peak plasma concentrations occur within 1 to 2 hours for total ezetimibe.             Food has no effect on the extent of absorption so ezetimibe can taken without regards to meals.
The half-life for ezetimibe and ezetimibe -glucoronide is approximately 22 hours.
Approximately 78% is excreted in feces and 11% in urine.

Food has no effect on the extent of absorption so ezetimibe can taken without regards to meals.

Use contraindicated. Observe caution