Crestor

Crestor (rosuvastatin calcium) is a prescription medication classified as a statin, specifically designed to manage elevated cholesterol levels and associated cardiovascular risks. It functions by inhibiting HMG-CoA reductase, a key enzyme in the hepatic synthesis of cholesterol, thereby reducing low-density lipoprotein (LDL) and triglycerides while increasing high-density lipoprotein (HDL). Clinically proven in extensive trials, Crestor is indicated for primary hyperlipidemia, mixed dyslipidemia, and as an adjunct to diet in homozygous familial hypercholesterolemia. It also plays a critical role in slowing the progression of atherosclerosis and reducing the incidence of major cardiovascular events in appropriately selected patients. Its efficacy and safety profile make it a cornerstone in modern lipid-lowering therapy under physician supervision.

Features

• Active ingredient: Rosuvastatin calcium
• Available in tablet strengths: 5 mg, 10 mg, 20 mg, 40 mg
• Mechanism: Selective and competitive inhibition of HMG-CoA reductase
• Administration: Oral, once daily with or without food
• Bioavailability: Approximately 20%
• Half-life: ~19 hours
• Excretion: Primarily fecal (90%), with minor renal elimination
• Special formulations: None; standard film-coated tablets

Benefits

• Significantly reduces LDL cholesterol levels by up to 52–63% at maximum doses
• Lowers triglyceride concentrations and increases HDL cholesterol, improving overall lipid profile
• Reduces the risk of myocardial infarction, stroke, and arterial revascularization procedures
• Slows the progression of atherosclerosis and promotes plaque stabilization
• Provides cardiovascular risk reduction in patients with elevated hs-CRP without hyperlipidemia
• Well-tolerated with a predictable pharmacokinetic profile in most patient populations

Common use

Crestor is commonly prescribed for the management of dyslipidemias, particularly in adults with primary hyperlipidemia or mixed dyslipidemia who have not achieved target lipid levels through diet and exercise alone. It is also used in pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia. Additionally, Crestor is indicated to reduce the risk of stroke, myocardial infarction, and revascularization in individuals without clinically evident coronary heart disease but with increased risk factors such as age, hypertension, low HDL-C, or a family history of early coronary heart disease. Off-label uses may include combination therapy with other lipid-modifying agents in complex dyslipidemias, though such use requires careful monitoring.

Dosage and direction

The recommended starting dose for most patients is 10 mg or 20 mg orally once daily. Dosage should be individualized based on LDL-C goals, patient response, and tolerability. The maximum approved dose is 40 mg daily, reserved for patients who do not achieve LDL-C goals with 20 mg. For Asian patients or those with predisposing factors for myopathy, a starting dose of 5 mg is recommended. Administration may occur at any time of day, with or without food. Regular lipid panels should be obtained within 2–4 weeks of initiation or dosage adjustment to assess therapeutic response. Dosage adjustments may be necessary in patients with severe renal impairment (CrCl <30 mL/min) who are not on hemodialysis—initiate at 5 mg and do not exceed 10 mg daily.

Precautions

Before initiating Crestor, assess liver function tests (LFTs), as unexplained persistent elevations may require discontinuation. Use with caution in patients who consume substantial quantities of alcohol or have a history of liver disease. Monitor for myopathy and rhabdomyolysis; assess creatine kinase (CK) levels if muscle symptoms occur. Risk of myopathy increases with higher doses and concomitant use of certain medications. Exercise caution in patients with hypothyroidism, renal impairment, or personal/family history of hereditary muscular disorders. Crestor may increase HbA1c and fasting serum glucose levels. Patients should be advised to report any unexplained muscle pain, tenderness, weakness, or brown urine promptly. Not recommended during pregnancy or in nursing mothers.

Contraindications

Crestor is contraindicated in patients with known hypersensitivity to rosuvastatin or any component of the formulation. It is contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases. Use is prohibited during pregnancy and breastfeeding due to potential fetal harm and interference with cholesterol synthesis. Contraindicated in concomitant use with cyclosporine. Not recommended in patients with severe renal impairment (CrCl <30 mL/min) unless on hemodialysis, and even then, dose restrictions apply.

Possible side effect

Common adverse reactions (≥2%) include headache, myalgia, abdominal pain, nausea, and constipation. Less frequently, dizziness, asthenia, and insomnia may occur. Important serious side effects include myopathy, rhabdomyolysis (with renal failure), hepatotoxicity, and increased HbA1c/fasting glucose. Rare events include immune-mediated necrotizing myopathy, memory loss, confusion, and hypersensitivity reactions. Pancreatitis, gynecomastia, and proteinuria have been reported, though often dose-related and reversible. Pediatric patients may experience side effects similar to adults, with additional monitoring for growth and maturation advised.

Drug interaction

Crestor interacts with several drug classes. Concomitant use with cyclosporine is contraindicated. Avoid with gemfibrozil; if used with other fibrates, caution is warranted. Dose limitation to 5 mg Crestor is recommended with ritonavir/lopinavir combination. Antacids containing aluminum and magnesium hydroxide decrease rosuvastatin absorption; administer at least 2 hours apart. Warfarin: monitor INR closely, as rosuvastatin may enhance anticoagulant effect. Erythromycin, oral contraceptives, and certain anti-infectives may alter rosuvastatin concentrations. Niacin (>1 g/day) or other lipid-lowering agents may increase the risk of myopathy.

Missed dose

If a dose is missed, take it as soon as remembered, unless it is nearly time for the next scheduled dose. Do not double the dose to make up for a missed one. Resume the regular dosing schedule. Consistent daily administration is important for maintaining lipid-lowering efficacy, but occasional missed doses are unlikely to significantly impact long-term outcomes. Patients should be educated on adherence strategies to minimize missed doses.

Overdose

There is no specific antidote for Crestor overdose. Suspected overdose should be managed with supportive measures, including monitoring of vital signs and clinical status. Given its extensive protein binding, dialysis is not expected to enhance elimination. Treatment should focus on symptomatic management, particularly monitoring for and treating myopathy or rhabdomyolysis, including hydration and renal function support. Liver function tests and CK levels should be monitored. Contact a poison control center for latest guidance.

Storage

Store Crestor tablets at room temperature, 20–25°C (68–77°F), with excursions permitted between 15–30°C (59–86°F). Keep in the original container, tightly closed, and protect from light and moisture. Do not store in bathrooms or damp areas. Keep out of reach of children and pets. Dispose of unused or expired medication through take-back programs or according to local regulations; do not flush.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or qualified health provider with any questions regarding a medical condition or before starting any new treatment. Do not disregard professional medical advice or delay seeking it because of something you have read here. Individual patient responses to Crestor may vary, and only a healthcare professional can determine the appropriate therapy based on comprehensive clinical evaluation.

Reviews

Clinical trials and post-marketing surveillance demonstrate that Crestor is highly effective in reducing LDL-C and cardiovascular events, with a generally favorable tolerability profile. Many clinicians report predictable efficacy and patient satisfaction when used according to guidelines. Some reviews note the need for careful patient selection and monitoring for muscular and hepatic adverse effects. Long-term studies support its role in primary and secondary prevention of atherosclerotic cardiovascular disease. Patient reviews often highlight significant improvements in lipid panels, though some report muscle-related side effects that may require dosage adjustment or alternative therapy. Overall, it remains a widely trusted option in statin therapy.