Drug updated on 4/17/2024
| Dosage Form | Tablet (oral; 5 mg, 10 mg, 20 mg, 40 mg) |
| Drug Class | HMG Co-A reductase inhibitors (statins) |
| Ongoing and Completed Studies | ClinicalTrials.gov |
Indication
- Indicated to reduce the risk of stroke, myocardial infarction, and arterial revascularization procedures in adults without established coronary heart disease who are at increased risk of cardiovascular (CV) disease based on age, hsCRP ≥2 mg/L, and at least one additional CV risk factor.
- Indicated as an adjunct to diet to reduce LDL-C in adults with primary hyperlipidemia.
- Indicated as an adjunct to diet to reduce low-density lipoprotein cholesterol (LDL-C) and slow the progression of atherosclerosis in adults.
- Indicated as an adjunct to diet to reduce LDL-C in adults and pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia (HeFH).
- Indicated as an adjunct to other LDL-C-lowering therapies, or alone if such treatments are unavailable, to reduce LDL-C in adults and pediatric patients aged 7 years and older with homozygous familial hypercholesterolemia (HoFH).
- Indicated as an adjunct to diet for the treatment of adults with: primary dysbetalipoproteinemia, hypertriglyceridemia.
Summary
- Rosuvastatin (Crestor) is notably effective in lowering LDL-C levels, reducing them by approximately 50%, which aligns with current guidelines for high-intensity statin therapy. It also maintains its efficacy when used in combination with ezetimibe.
- Eleven systematic reviews/meta-analyses were compared to assess the safety and effectiveness of Rosuvastatin against other drugs within the statin class and in combination therapies.
- Rosuvastatin has been associated with similar rates of adverse events as other statins; however, it showed a higher risk of transaminase elevations compared to atorvastatin, indicating potential hepatic side effects.
- Statins, including Rosuvastatin, were linked to increased risks of muscle-related symptoms, liver dysfunction, and minor increases in creatine kinase levels, but these did not significantly outweigh their cardiovascular benefits.
- Genetic polymorphisms such as the ABCG2 421C>A variant have a notable impact on Rosuvastatin pharmacokinetics, suggesting nearly 1.5 times higher drug exposure among carriers of the A allele, emphasizing the potential for personalized medicine approaches based on genetic makeup.
- In primary prevention cohorts, Rosuvastatin's risk of inducing diabetes or cognitive impairment appears low, while being counterbalanced by its efficacy in reducing cardiovascular events.
- For patients suffering from hypertension alongside hyperlipidemia conditions like familial hypercholesterolemia or dysbetalipoproteinemia, this medication, along with antihypertensive agents, displayed a significant reduction in diastolic blood pressure, implying additional benefits outside lipid-lowering.
- Rosuvastatin demonstrated superior efficacy over different types of statins concerning LDL-C reduction according to one study, although some studies suggest no significant differences between various types regarding the incidence of muscle symptoms and liver dysfunction, indicating that adverse effects may be more related to intensity rather than the type itself.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Crestor (rosuvastatin) Prescribing Information. | 2023 | AstraZeneca Pharmaceuticals LP Wilmington, DE |