Rosuvastatin is a medication used to regulate blood lipids, belonging to the class of drugs known as statins. Its primary function is to inhibit the synthesis of cholesterol in the liver, thereby reducing low-density lipoprotein cholesterol (LDL-C, known as "bad cholesterol") and total cholesterol levels in the blood. It can also slightly increase high-density lipoprotein cholesterol (HDL-C, known as "good cholesterol") and decrease triglycerides. This medication is commonly used to treat hyperlipidemia and can reduce the risk of cardiovascular diseases such as heart attacks or strokes.
The drug works by selectively inhibiting HMG-CoA reductase (a key enzyme in hepatic cholesterol synthesis), significantly decreasing cholesterol production in the liver and promoting an increase in LDL receptors on the liver surface, which accelerates the metabolism of LDL in the blood. Clinical studies show that rosuvastatin often has a stronger effect in lowering LDL-C compared to other statins, making it suitable for patients with difficult-to-control lipid levels.
The generic name of this medication is "Rosuvastatin Calcium," with the common brand name "CRESTOR®." Different regions may have other brand names, but the generic name "Rosuvastatin" is internationally recognized. The medication is supplied in tablet form, with dosages typically available in 5 mg, 10 mg, 20 mg, and 40 mg strengths.
Rosuvastatin belongs to the class of "HMG-CoA Reductase Inhibitors," which are first-line drugs for treating hyperlipidemia. Its chemical structure confers high selectivity, effectively lowering LDL-C, and it has a relatively long half-life compared to other statins, requiring only once-daily dosing.
This drug is also classified as a "Lipid Metabolism Regulating Agent," primarily acting on lipid metabolic pathways. Its mechanism of action differs from other lipid-lowering drugs such as fibrates or niacin, and it is generally not recommended to combine it with other statins.
The main indications for rosuvastatin include: primary hyperlipidemia (including familial hypercholesterolemia), mixed dyslipidemia (high LDL-C and high triglycerides), and primary and secondary prevention of cardiovascular disease. According to clinical guidelines, it is also suitable for patients who have experienced heart attacks or strokes to reduce future cardiovascular event risks.
Additionally, this medication can be combined with non-pharmacological treatments such as diet control and exercise to achieve better lipid management. In certain cases, physicians may adjust the dosage based on the patient's baseline LDL-C levels and cardiovascular risk to meet LDL-C reduction targets (such as 50% or more).
Common mild side effects include headache, muscle soreness, diarrhea, bloating, or indigestion. These symptoms usually occur early in treatment and may diminish over time. Approximately 2-5% of patients may experience mild elevations in transaminases (liver function tests), but most cases do not require discontinuation of the medication.
Contraindications: Pregnant women or women who may become pregnant should avoid use due to potential fetal abnormalities; patients with severe liver disease, those allergic to the drug components, or those taking contraindicated medications (such as certain antifungals or immunosuppressants) should also avoid use.
The medication carries a black box warning from the U.S. FDA, emphasizing:
Concurrent use with the following medications may increase the risk of side effects:
When taking this medication, avoid excessive intake of grapefruit juice, as it may inhibit hepatic enzymes and increase drug concentration. Alcohol consumption may exacerbate liver metabolism burden; therefore, alcohol intake should be moderate.
The starting dose is usually 10 mg daily. Based on lipid targets and tolerability, the dose can be adjusted up to 40 mg (the maximum recommended dose). It is generally recommended to take the medication at a fixed time, with or without food, as food does not significantly affect absorption. Elderly patients or those with renal impairment should have dosage adjustments, especially if creatinine clearance is below 30 mL/min, with a maximum dose of 20 mg/day.
Blood lipid levels should be checked 4-12 weeks after starting therapy, and cardiovascular risk and side effects should be evaluated every 3-6 months. During treatment, continue diet control and lifestyle modifications, as medication efficacy depends on a low-fat diet for optimal results.
If a dose is missed, and the time until the next dose is less than 6 hours, skip the missed dose and take the next dose as scheduled; do not double dose. If a longer time has passed and the next dose is approaching, take the medication at the scheduled time without extra supplementation.
If medication is missed long-term, leading to treatment interruption, contact your physician immediately to adjust the medication plan. Do not increase the dose on your own to compensate. Abrupt discontinuation of statins may cause lipid rebound; dose adjustments should be supervised by a healthcare professional.
In case of suspected overdose, seek medical attention immediately. Overdose of rosuvastatin may cause severe muscle damage or liver injury. Treatment includes gastric lavage, monitoring of creatine phosphokinase (CPK) and liver function, and hospitalization if severe.
If combined with other drugs that cause muscle toxicity (such as certain antibiotics or antifungals), the risk is higher, requiring urgent management. There is no specific antidote; supportive care includes discontinuing the drug, hydration, and monitoring renal function.
If I occasionally miss a dose of rosuvastatin, how should I handle it?
If the missed dose is close to the next scheduled dose, skip the missed dose and do not double up. If the missed dose is recent, consult your doctor or pharmacist before taking the next dose to avoid overdose-related risks such as liver dysfunction or muscle discomfort.
Is regular liver function testing necessary during long-term rosuvastatin use?
Yes. Rosuvastatin may affect liver function. It is recommended to monitor liver enzymes every 4-8 weeks initially, and if no abnormalities are found, extend to every 6 months. If symptoms such as fatigue or dark urine occur, stop medication and seek medical attention immediately.
Should I restrict certain foods while taking rosuvastatin?
It is advisable to avoid excessive intake of high-fat foods, as they may reduce drug efficacy. Additionally, grapefruit juice may increase drug concentration; daily intake should be limited to 240 mL. A balanced diet combined with medication can enhance lipid-lowering effects.
What interactions should I be aware of when using other lipid-lowering drugs together?
Rosuvastatin combined with amiodarone, cyclosporine, and other drugs may increase muscle toxicity risk, requiring dose adjustments or alternative medications. Always inform your healthcare provider of all prescription drugs, over-the-counter medications, and herbal supplements to prevent interactions.
How can exercise complement medication therapy to improve lipid levels?
Regular aerobic exercise (such as brisk walking or swimming) can enhance drug effects. It is recommended to engage in at least 150 minutes of moderate-intensity exercise weekly. If muscle pain or weakness occurs after exercise, stop and measure CPK levels to prevent muscle damage.
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