Overview
Ezetimibe/Rosuvastatin is a fixed-dose combination medication used to treat hypercholesterolemia. It combines a cholesterol absorption inhibitor (ezetimibe) with a statin (rosuvastatin) to provide dual mechanisms for lowering LDL cholesterol and other lipid parameters.
Mechanism of Action
Ezetimibe inhibits intestinal cholesterol absorption by blocking the NPC1L1 protein in the small intestine. Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis in the liver, thereby increasing LDL receptor expression and clearance of LDL cholesterol from the bloodstream.
Indications
- Primary hyperlipidemia
- Mixed dyslipidemia
- Homozygous familial hypercholesterolemia
- Heterozygous familial hypercholesterolemia
- Atherosclerotic cardiovascular disease risk reduction
Dosage
Available as ezetimibe 10 mg/rosuvastatin 5 mg, 10 mg, 20 mg, or 40 mg tablets. Usual starting dose: ezetimibe 10 mg/rosuvastatin 10 mg once daily. Dose adjustments based on lipid response and tolerability. Maximum dose: ezetimibe 10 mg/rosuvastatin 40 mg daily.
Contraindications
- Active liver disease
- Unexplained persistent elevations in serum transaminases
- Pregnancy
- Lactation
- Hypersensitivity to any component
- Concomitant use with cyclosporine
Side Effects
- Headache
- Myalgia
- Arthralgia
- Nasopharyngitis
- Upper respiratory tract infection
- Diarrhea
- Nausea
- Increased hepatic transaminases
- Muscle spasms
- Back pain
Interactions
- Cyclosporine (contraindicated)
- Gemfibrozil (increases rosuvastatin exposure)
- Antacids (decrease rosuvastatin absorption)
- Warfarin (monitor INR)
- Protease inhibitors
- Colchicine (increased myopathy risk)
- Other lipid-lowering agents