Cardiac Medications

Cholesterol and Lipid Lowering Drugs:
Cholesterol Absorption Inhibitors

Cholesterol absorption inhibitors are a new class of cholesterol lowering drugs which
block absorption of cholesterol at the brush border of the intestine without affecting
absorption of triglycerides or fat soluble vitamins. These drugs have the advantage
of not being systemically absorbed and can lower cholesterol by about 20% on their
own. When used in addition to statins they may provide an additional 15% cholesterol
lowering. It is recommended to monitor liver function tests when using a cholesterol
absorption inhibitor and a statin together. Side effects including fatigue, abdominal
pain, diarrhea, muscle and joint pains and coughing are infrequent.

The only currently available cholesterol absorption inhibitor is ezetimibe (Ezetrol“).

Health Canada has recently (Feb. 1, 2005) posted an Advisory for Health Professionals and a Public Advisory on ezetimibe (Ezetrol“) based on a letter from Merck Frosst/Schering Pharmaceuticals highlighting important safety information on ezetimibe (Ezetrol“). The product monograph has been updated to include information from international post-marketing reports of rare, and in some cases serious, adverse events.

Additional reports of myalgia (muscle pains), many accompanied by elevated creatine phosphokinase (CK) values, have been reviewed by Health Canada.

The Warnings, Precautions, and Adverse Events sections are being updated to reflect the occurrence of the following adverse events in patients taking Ezetrol® (ezetimibe) alone or in combination with a statin:

  • myalgia;
  • rhabdomyolysis;
  • hepatitis;
  • acute pancreatitis;
  • thrombocytopenia; and
  • suspected interaction between Ezetrol“ (ezetimibe) and Warfarin

Patients should report to their prescribing physician any unexplained symptoms after initiation of ezetimibe. including:

  • dark urine;
  • abdominal pain (especially if felt on the right side below the ribs);
  • nausea or vomiting;
  • yellowing of the skin or eyes;
  • general itchiness; or pale stools
  • ease of bruising

Liver function tests and CK muscle enzyme should be monitored in patients on ezetimibe. Patients on Warfarin who begin ezetimibe should have their INR monitored more closely.

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  Version 2.0, February 2005
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