Cholesterol absorption inhibitors
As the name implies, cholesterol absorption inhibitors inhibit the absorption of cholesterol and related phytosterols from the intestine. Ezetimibe is the drug in this class.
Pharmacokinetics
Ezetimibe is rapidly and extensively absorbed following oral administration. It’s is readily absorbed and is highly bound to plasma proteins. It’s primarily metabolized in the small intestine and excreted by the liver and kidneys.
Pharmacodynamics
Ezetimibe reduces blood cholesterol levels by inhibiting the absorption of cholesterol by the small intestine. This leads to a decrease in delivery of intestinal cholesterol to the liver, reducing hepatic cholesterol stores and increasing clearance from the blood.
Pharmacotherapeutics
Ezetimibe may be administered alone or with dietary changes to treat primary hypercholesterolemia and homozygous sitosterolemia (hereditary hyperabsorption of cholesterol and plant sterols). The drug is also used in combination with HMG-CoA reductase inhibitors to treat primary hypercholesterolemia and homozygous familial hypercholesterolemia.
Ezetimibe may also help lower total cholesterol and LDL cholesterol, and increase HDL cholesterol, when maximum-dose HMG-CoA reductase inhibitor therapy has been ineffective.
Warning!
Adverse reactions to cholesterol absorption inhibitors
The most common adverse reactions include:
- fatigue
- abdominal pain and diarrhea
- pharyngitis and sinusitis
- arthralgia
- back pain
- cough.
When these drugs are given with an HMG-CoA reductase inhibitor, the most common adverse reactions are chest pain, dizziness, headache, abdominal pain, diarrhea, pharyngitis, sinusitis, upper respiratory tract infection, arthralgia, back pain, and myalgia.
Drug interactions
- Ezetimibe administered with cholestyramine may lead to decreased effectiveness of ezetimibe.
- Ezetimibe administered with cyclosporine, fenofibrate, or gemfibrozil leads to increased levels of ezetimibe.
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