“Rosuvastatin calcium” is the calcium-salt form of rosuvastatin, a synthetic lipid-lowering active Rosuvastatin calcium is the calcium-salt form of rosuvastatin, a synthetic lipid-lowering active pharmaceutical ingredient (API) in the statin class. It is used with diet and lifestyle changes to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol, apolipoprotein B, non-high-density lipoprotein cholesterol, and triglycerides. It may also modestly increase high-density lipoprotein cholesterol.
Rosuvastatin is prescribed for primary hypercholesterolemia, mixed dyslipidemia, familial hypercholesterolemia, and cardiovascular-risk reduction in appropriate patients. The original brand is Crestor, while generic rosuvastatin calcium products are widely available.
Chemical Structure
Rosuvastatin calcium is usually represented as a calcium salt containing two rosuvastatin anions for each calcium ion. Its molecular formula is , and its molecular weight is approximately 1001.1 g/mol.
The active rosuvastatin moiety contains a pyrimidine ring, fluorophenyl group, methylsulfonamide group, and dihydroxyheptenoic acid side chain. The stereochemistry of the hydroxy-acid side chain is important for pharmacological activity. The calcium salt improves the handling and formulation of the API.
Rosuvastatin-Based Medicines
Representative medicines include:
- Crestor tablets.
- Ezallor Sprinkle capsules.
- Roszet tablets containing rosuvastatin and ezetimibe.
- Generic rosuvastatin calcium tablets.
- CRESLIP tablets.
- ROSUCOR tablets.
- ROSULIB tablets.
- PLENANCE tablets.
Brand names and formulations vary by country. Crestor and Ezallor are recognized U.S. products, while several other names are used regionally.
Mechanism of Action
Rosuvastatin selectively and competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A reductase, commonly known as HMG-CoA reductase. This enzyme controls an important early step in hepatic cholesterol synthesis.
By reducing cholesterol production in the liver, rosuvastatin increases hepatic LDL receptors. These receptors remove more LDL particles from the blood, producing a substantial reduction in LDL-C. Rosuvastatin also reduces very-low-density lipoprotein production and may lower triglycerides while modestly increasing HDL-C.
Pharmacokinetics
After oral administration, peak plasma concentrations are usually reached within three to five hours. Approximately 88% of rosuvastatin is reversibly bound to plasma proteins. The drug undergoes limited metabolism, mainly through CYP2C9, and its major metabolite has considerably less activity than the parent compound.
Rosuvastatin Calcium is a substrate of the hepatic OATP1B1 transporter and the BCRP efflux transporter. Drugs that inhibit these transport pathways can substantially increase rosuvastatin exposure. Approximately 90% of an administered dose is eliminated in feces, mainly as unchanged drug. The elimination half-life is approximately 19 hours, supporting once-daily dosing.
Exposure may increase in severe kidney impairment and in some patients of Asian ancestry. Patients with severe renal impairment who are not receiving hemodialysis generally begin with 5 mg once daily, and the dose should not exceed 10 mg daily under current U.S. labeling.
Rosuvastatin Calcium Uses
| Condition | Purpose | Dosage considerations |
|---|---|---|
| Primary hypercholesterolemia | Reduces elevated LDL-C and total cholesterol | Common adult range: 5–40 mg once daily |
| Mixed dyslipidemia | Reduces LDL-C, ApoB, non-HDL-C, and triglycerides | Used with diet and lifestyle changes |
| Heterozygous familial hypercholesterolemia | Treats genetically elevated LDL-C | Dose depends on age and response |
| Homozygous familial hypercholesterolemia | Provides intensive LDL-C reduction | Usually requires specialist supervision |
| Cardiovascular-risk reduction | Helps reduce risk in appropriate patients | Based on individual cardiovascular risk |
| Pediatric HeFH | Treats familial high cholesterol | Approved pediatric age ranges and doses vary |
| Combination therapy | Used with ezetimibe when additional reduction is needed | Available in products such as Roszet |
The adult dosage range is generally 5–40 mg once daily. The 40-mg dose is reserved for patients who have not achieved adequate LDL-C reduction with lower doses and requires careful monitoring because adverse effects may be more frequent.
Side Effects
Common adverse effects include headache, muscle pain, abdominal pain, nausea, weakness, and constipation. Muscle pain is among the most frequently reported statin-related symptoms.
Rarely, rosuvastatin can cause myopathy or rhabdomyolysis. These conditions may involve severe muscle pain, tenderness, weakness, elevated creatine kinase, and, in severe cases, acute kidney injury. Patients should promptly report severe or unexplained muscle symptoms, fever, or dark urine.
Rosuvastatin may increase liver transaminases. Serious liver injury is uncommon, but symptoms such as jaundice, dark urine, persistent fatigue, loss of appetite, or upper-abdominal discomfort require medical evaluation. Small increases in blood glucose and glycated hemoglobin can also occur, particularly in patients already at risk of diabetes.
Drug Interactions
Cyclosporine can markedly increase rosuvastatin exposure and the risk of myopathy. Gemfibrozil may also increase rosuvastatin concentrations and is generally avoided with rosuvastatin. Other fibrates, high-dose niacin, and colchicine may increase the risk of muscle toxicity.
Some HIV and hepatitis C antiviral medicines inhibit transporters such as OATP1B1 and BCRP. Dose restrictions or avoidance may be required. Aluminum- or magnesium-containing antacids can reduce rosuvastatin absorption when taken at the same time; administration should be separated as directed by the product label.
Rosuvastatin may increase the international normalized ratio in patients taking warfarin, particularly when treatment is started, stopped, or adjusted. Additional INR monitoring may therefore be necessary.
Safety Considerations
Rosuvastatin should not be used in patients with a known allergy to the drug or its ingredients. It is generally discontinued when pregnancy is recognized because cholesterol synthesis is important for fetal development and treatment provides no meaningful benefit during pregnancy. Breastfeeding is not recommended during treatment because of the potential for serious effects in nursing infants.
Patients with active liver disease or persistent unexplained increases in liver enzymes require careful evaluation. Liver tests may be obtained before treatment and whenever symptoms suggest hepatic injury.
The risk of muscle toxicity is higher with high doses, advanced age, kidney impairment, untreated hypothyroidism, interacting medicines, and some genetic variants affecting drug transport. Patients should tell their healthcare professional about prior statin intolerance, muscle disorders, thyroid disease, kidney disease, and all medicines or supplements.
Regulatory Status
Crestor received initial U.S. FDA approval in 2003. Rosuvastatin calcium tablets are approved for lipid lowering and several familial hypercholesterolemia indications. Pediatric indications are specified in the relevant product labeling. Generic rosuvastatin calcium tablets, including 5-, 10-, 20-, and 40-mg strengths, are also approved in the United States.
Ezallor Sprinkle and combination products containing rosuvastatin and ezetimibe are also authorized in the United States. Regulatory indications, strengths, age limits, and prescription requirements differ among countries and formulations.
Conclusion
Rosuvastatin calcium is a potent statin API used to lower LDL cholesterol and reduce cardiovascular risk. Its limited metabolism, transporter-based disposition, approximately 19-hour half-life, and once-daily dosing support convenient treatment. Safe use requires attention to kidney and liver function, muscle symptoms, pregnancy, breastfeeding, and drug interactions. Individual dosing should always follow local prescribing information and professional medical advice.
