Mechanism of Action
Rosuvastatin inhibits HMG-CoA reductase, the enzyme responsible for converting HMG-CoA to mevalonate, a precursor of cholesterol. By inhibiting this enzyme, rosuvastatin reduces the production of cholesterol in the liver, leading to an increase in the uptake of low-density lipoprotein (LDL) cholesterol from the blood and a decrease in overall cholesterol levels.
Indications
- Hyperlipidemia: To lower elevated LDL cholesterol, total cholesterol, and triglycerides, and to increase high-density lipoprotein (HDL) cholesterol.
- Atherosclerosis: To slow the progression of atherosclerosis in patients with elevated cholesterol levels.
- Primary Prevention of Cardiovascular Events: To reduce the risk of stroke, myocardial infarction, and arterial revascularization procedures in individuals without clinically evident coronary heart disease but with increased risk factors.
Dosage and Administration
- Initial Dose: Typically, 5-10 mg once daily.
- Maintenance Dose: Can be adjusted based on response and tolerability, ranging from 5 mg to 40 mg once daily.
- Administration: Usually taken orally, with or without food. Take the dose at the same time each day for optimal effectiveness.
Side Effects
Common side effects include:
- Headache
- Myalgia (muscle pain)
- Abdominal pain
- Nausea
- Dizziness
- Increased liver enzymes
Serious side effects may include:
- Myopathy (muscle disease) and rhabdomyolysis (severe muscle breakdown)
- Hepatotoxicity (liver damage)
- Increased blood sugar levels and risk of diabetes
Contraindications
Rosuvastatin is contraindicated in patients with:
- Active liver disease or unexplained persistent elevations in serum transaminases.
- Pregnancy and lactation.
- Hypersensitivity to rosuvastatin or any of its components.
Drug Interactions
Rosuvastatin can interact with several other medications, including:
- Cyclosporine: Can increase rosuvastatin levels and the risk of myopathy.
- Gemfibrozil and other fibrates: Can increase the risk of myopathy and rhabdomyolysis.
- Warfarin: Rosuvastatin can increase the anticoagulant effect of warfarin.
- Antacids containing aluminum and magnesium hydroxide: Can decrease the absorption of rosuvastatin.
Monitoring
- Lipid Profile: Regular monitoring of cholesterol and triglyceride levels to assess the effectiveness of therapy.
- Liver Function Tests: Periodic monitoring of liver enzymes to detect potential hepatotoxicity.
- Muscle Symptoms: Patients should be advised to report unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise.
Special Populations
- Elderly: No specific dose adjustment is generally required, but elderly patients may be more susceptible to myopathy.
- Pregnancy and Lactation: Contraindicated due to the potential risk to the fetus and infant.
- Renal Impairment: Dose adjustment is recommended for patients with severe renal impairment (CrCl <30 mL/min).
- Hepatic Impairment: Exercise caution in patients with mild to moderate hepatic impairment.
Conclusion
Rosuvastatin is an effective medication for managing hyperlipidemia and reducing the risk of cardiovascular events. Its use requires careful monitoring for potential side effects, particularly myopathy and hepatotoxicity. Seek advice from a healthcare provider for personalized medical guidance.