Crestor: Advanced LDL Cholesterol Reduction Therapy

Crestor

Crestor

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Product dosage: 10mg
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Product dosage: 20mg
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Product dosage: 5mg
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Synonyms

Similar products

Crestor (rosuvastatin calcium) is a prescription medication classified as a statin, specifically developed 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 effectively reducing low-density lipoprotein (LDL) and triglycerides while increasing high-density lipoprotein (HDL). Clinical evidence supports its use in primary and secondary prevention of cardiovascular events, including myocardial infarction and stroke, particularly in high-risk patient populations. Its well-established efficacy profile and generally favorable tolerability make it a cornerstone in modern lipid management strategies.

Features

  • Active ingredient: Rosuvastatin calcium
  • Available in 5mg, 10mg, 20mg, and 40mg tablet strengths
  • Once-daily oral administration
  • Bioavailability of approximately 20%
  • Extensive hepatic metabolism via CYP2C9 and minor CYP2C19 pathways
  • Elimination half-life of approximately 19 hours
  • Manufactured under strict pharmaceutical quality standards

Benefits

  • Significantly reduces LDL cholesterol levels by up to 52–63% at maximum doses
  • Lowers triglyceride concentrations by 10–35%
  • Increases HDL cholesterol by 3–12%
  • Reduces risk of major cardiovascular events in appropriate patient populations
  • Slows progression of atherosclerosis as demonstrated in intravascular ultrasound studies
  • May reduce C-reactive protein levels, indicating anti-inflammatory effects

Common use

Crestor is primarily indicated for the treatment of hypercholesterolemia, including heterozygous familial hypercholesterolemia in patients who haven’t achieved target LDL levels through diet and exercise alone. It’s also approved for homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments. Additionally, Crestor is used in primary prevention for individuals without clinically evident coronary heart disease but with increased risk factors based on age, elevated hs-CRP, and at least one additional cardiovascular risk factor. In secondary prevention, it’s prescribed to reduce the risk of stroke, myocardial infarction, and arterial revascularization procedures in patients with established cardiovascular disease.

Dosage and direction

The recommended starting dose is 10–20 mg once daily, with dosage adjustments based on LDL cholesterol goals and individual patient response. For patients requiring aggressive LDL reduction (>45%), a 20 mg starting dose may be appropriate. The maximum recommended dose is 40 mg daily, reserved for patients who haven’t achieved their LDL goal with 20 mg. Administration should occur at the same time each day, with or without food, though consistency in administration relative to meals is recommended. Dosage adjustment is necessary for patients with renal impairment, Asian patients, and those taking certain concomitant medications. Liver function tests should be performed before initiation and periodically thereafter.

Precautions

Liver function monitoring is essential, with baseline measurement of transaminases before therapy initiation and as clinically indicated thereafter. Patients should report any unexplained muscle pain, tenderness, or weakness immediately, particularly if accompanied by fever or malaise. Blood glucose levels should be monitored, as increases in HbA1c and fasting serum glucose have been reported. Use with caution in patients consuming substantial quantities of alcohol or with history of liver disease. Elderly patients may require dose adjustment due to decreased renal function. Patients should be advised that Crestor is not indicated during pregnancy and adequate contraception should be used in women of childbearing potential.

Contraindications

Crestor is contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases. It is contraindicated during pregnancy and breastfeeding due to potential risk to the fetus and infant. Concomitant use with cyclosporine is prohibited. Hypersensitivity to rosuvastatin calcium or any component of the formulation constitutes an absolute contraindication. The 40 mg dose is contraindicated in patients with predisposing factors for myopathy/rhabdomyolysis, including renal impairment, hypothyroidism, and personal or family history of hereditary muscular disorders.

Possible side effect

Common adverse reactions (≥2%) include headache, myalgia, abdominal pain, nausea, and constipation. Less frequent but clinically significant side effects include elevated creatine kinase, increased liver transaminases, and proteinuria (generally transient and not indicative of renal disease). Serious but rare adverse effects include rhabdomyolysis with renal dysfunction, hepatic failure, and immune-mediated necrotizing myopathy. Diabetes mellitus incidence may increase, particularly in patients with existing risk factors. Cognitive impairment (memory loss, confusion) has been reported, though generally reversible upon discontinuation.

Drug interaction

Significant interactions occur with cyclosporine (contraindicated), gemfibrozil (avoid combination), and other fibrates (use with caution). Concurrent administration with warfarin may potentiate anticoagulant effect, requiring frequent INR monitoring. Protease inhibitors, particularly combination HIV therapies, may increase rosuvastatin exposure. Calcium channel blockers like verapamil and amlodipine may moderately increase rosuvastatin concentrations. Oral contraceptives containing ethinyl estradiol and norgestrel may have increased plasma levels when co-administered with Crestor. Antacids containing aluminum and magnesium hydroxide decrease rosuvastatin absorption if taken simultaneously.

Missed dose

If a dose is missed, it should be taken as soon as remembered, unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take double or extra doses to make up for a missed dose. Consistency in daily administration is important for maintaining stable lipid-lowering effects. If multiple doses are missed, patients should contact their healthcare provider for guidance on resumption of therapy.

Overdose

There is no specific antidote for rosuvastatin overdose. Management should be supportive and symptomatic. Gastric lavage may be considered if performed soon after ingestion. Liver function and creatine kinase levels should be monitored closely. Hemodialysis is unlikely to be beneficial due to high protein binding. Cases of overdose have been reported with doses up to 80 mg without serious clinical consequences, but rhabdomyolysis and hepatic dysfunction are potential concerns with significant overdosage. Medical supervision is recommended for any suspected overdose situation.

Storage

Store at room temperature (20–25°C or 68–77°F), with excursions permitted between 15–30°C (59–86°F). Keep in the original container with the lid tightly closed to protect from moisture and light. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Do not transfer tablets to other containers, as this may affect stability. Properly discard any unused medication after therapy completion or expiration.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Crestor is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual results may vary, and not all patients will experience the same benefits or side effects. Patients should not discontinue or modify their dosage without consulting their physician. The full prescribing information should be reviewed before initiating therapy. Only a healthcare provider can determine if Crestor is appropriate for a specific individual based on their medical history, current condition, and risk factors.

Reviews

Clinical trials demonstrate that 80% of patients achieved LDL cholesterol goals with Crestor therapy. In the JUPITER trial, rosuvastatin 20 mg significantly reduced major cardiovascular events by 44% compared to placebo in patients with elevated hs-CRP. Real-world evidence supports maintained efficacy over 5-year treatment periods with consistent safety profile. Patient satisfaction surveys indicate high adherence rates due to once-daily dosing and generally favorable side effect profile. Healthcare providers report particular effectiveness in high-risk patients requiring aggressive LDL reduction. Long-term extension studies show sustained lipid-lowering effects with maintained safety profile over extended treatment periods.