Ezetimibe/rosuvastatin

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Combination drug for hyperlipidemia


Ezetimibe/rosuvastatin is a combination drug used to treat hyperlipidemia, a condition characterized by elevated levels of lipids in the blood. This medication combines two active ingredients: ezetimibe and rosuvastatin.

Mechanism of Action

Ezetimibe/rosuvastatin works by targeting different pathways involved in cholesterol metabolism.

Ezetimibe

Ezetimibe is a cholesterol absorption inhibitor. It acts on the small intestine to block the absorption of cholesterol from the diet. By inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) protein, ezetimibe reduces the amount of cholesterol delivered to the liver, leading to a decrease in blood cholesterol levels.

Rosuvastatin

Rosuvastatin is a member of the statin class of drugs, which are HMG-CoA reductase inhibitors. Statins work by inhibiting the enzyme HMG-CoA reductase, which plays a crucial role in the synthesis of cholesterol in the liver. This results in an upregulation of LDL receptors on liver cells, increasing the clearance of low-density lipoprotein (LDL) cholesterol from the bloodstream.

Clinical Use

Ezetimibe/rosuvastatin is primarily prescribed for patients with hypercholesterolemia who require additional lipid-lowering effects beyond what can be achieved with statin therapy alone. It is particularly useful in patients who have not reached their target cholesterol levels with statins alone or who have familial hypercholesterolemia.

Dosage and Administration

The dosage of ezetimibe/rosuvastatin is individualized based on the patient's current cholesterol levels, response to treatment, and risk factors for cardiovascular disease. It is typically administered once daily, with or without food.

Side Effects

Common side effects of ezetimibe/rosuvastatin include muscle pain, headache, and gastrointestinal disturbances. Serious side effects, although rare, can include rhabdomyolysis, liver enzyme abnormalities, and allergic reactions.

Contraindications

Ezetimibe/rosuvastatin is contraindicated in patients with active liver disease, unexplained persistent elevations of serum transaminases, and in women who are pregnant or breastfeeding.

Related Pages

Ezetimibe/rosuvastatin chemical structure
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Contributors: Prab R. Tumpati, MD