pharmacopeia
GET
/api/v1/drug/rosuvastatin
2D structure
(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
SMILES CC(C)C1=NC(=NC(=C1/C=C/[C@H](C[C@H](CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C
InChIKey BPRHUIZQVSMCRT-VEUZHWNKSA-N

Mechanism of action

Sourced from openFDA

Rosuvastatin is an inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3‑hydroxy‑3‑methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol.

Hydroxymethylglutaryl-CoA Reductase

Indications

Sourced from openFDA
  • Rosuvastatin tablets is indicated: To reduce the risk major adverse cardiovascular (CV) events (CV death, nonfatal myocardial infarction, nonfatal stroke, or an arterial revascularization procedure) in adults without established coronary heart disease who are at increased risk of CV disease based on age, high-sensitivity C-reactive protein (hsCRP) ≥2 mg/L, and at least one additional CV risk factor. As an adjunct to diet to: Reduce low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia.ICD-10: E78.5, I21.9, I63.9

Contraindications

Sourced from openFDA
  • Rosuvastatin tablets is contraindicated in the following conditions: Acute liver failure or decompensated cirrhosis [see Warnings and Precautions ( 5.3 )] . Hypersensitivity to rosuvastatin or any excipients in rosuvastatin tablets.contraindicated

Dosage & administration

Sourced from openFDA

Take orally with or without food, at any time of day. ( 2.1 ) Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating rosuvastatin tablets, and adjust dosage if necessary. ( 2.1 ) Adults : Recommended dosage range is 5 to 40 mg once daily. ( 2.1 ) Pediatric Patients with HeFH : Recommended dosage range is 5 to 10 mg once daily for patients aged 8 to less than 10 years of age, and 5 to 20 mg once daily for patients aged 10 years and older. ( 2.2) Pediatric Patients with HoFH : Recommended dosage is 20 mg once daily for patients aged 7 years and older. ( 2.2 ) Asian Patients : Initiate at 5 mg once daily. Consider risks and benefits of treatment if not adequately controlled at doses up to 20 mg once daily. ( 2.4 ) Patients with Severe Renal Impairment (not on hemodialysis) : Initiate at 5 mg once daily; do not exceed 10 mg once daily. ( 2.5 ) See full prescribing information for rosuvastatin tablets dosage and administration modifications due to drug interactions. ( 2.6 ) 2.1 General Dosage and Administration Information Administer rosuvastatin tablets orally as a single dose at any time of day, with or without food. Swallow the tablets whole. Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating rosuvastatin tablets, and adjust the dosage if necessary. If a dose is missed, advise patients not take an extra dose. Resume treatment with the next dose.

Warnings & precautions

Sourced from openFDA

Myopathy and Rhabdomyolysis : Risk factors include age 65 years or greater, uncontrolled hypothyroidism, renal impairment, concomitant use with certain other drugs, and higher rosuvastatin dosage. Asian patients may be at higher risk for myopathy. Discontinue rosuvastatin if markedly elevated CK levels occur or myopathy is diagnosed or suspected. Temporarily discontinue rosuvastatin in patients experiencing an acute or serious condition at high risk of developing renal failure secondary to rhabdomyolysis. Inform patients of the risk of myopathy and rhabdomyolysis when starting or increasing rosuvastatin dosage. Instruct patients to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. ( 5.1 ) Immune-Mediated Necrotizing Myopathy (IMNM) : Rare reports of IMNM, an autoimmune myopathy, have been reported with statin use. Discontinue rosuvastatin if IMNM is suspected. ( 5.2 ) Hepatic Dysfunction : Increases in serum transaminases have occurred, some persistent. Rare reports of fatal and non-fatal hepatic failure have occurred. Consider testing liver enzymes before initiating therapy and as clinically indicated thereafter. If serious hepatic injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs, promptly discontinue rosuvastatin. ( 5.3 ) 5.1 Myopathy and Rhabdomyolysis Rosuvastatin may cause myopathy [muscle pain, tenderness, or weakness associated with elevated creatine kinase (CK)] and rhabdomyolysis.

Adverse reactions

Sourced from openFDA

The following important adverse reactions are described below and elsewhere in the labeling: Myopathy and Rhabdomyolysis [see Warnings and Precautions ( 5.1 )] Immune-Mediated Necrotizing Myopathy [see Warnings and Precautions ( 5.2 )] Hepatic Dysfunction [see Warnings and Precautions ( 5.3 )] Proteinuria and Hematuria [see Warnings and Precautions ( 5.4 )] Increases in HbA1c and Fasting Serum Glucose Levels [see Warnings and Precautions ( 5.5 )] Most frequent adverse reactions (rate ≥2%) are headache, nausea, myalgia, asthenia, and constipation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Westminster Pharmaceuticals, LLC at 1-844-221-7294 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Adverse reactions reported in ≥2% of patients in placebo-controlled clinical studies and at a rate greater than placebo are shown in Table 2. These studies had a treatment duration of up to 12 weeks.

Use in specific populations

Sourced from openFDA

Pregnancy : May cause fetal harm. ( 8.1 ) Lactation : Breastfeeding not recommended during treatment with rosuvastatin. ( 8.2 ) 8.1 Pregnancy Risk Summary Discontinue rosuvastatin when pregnancy is recognized. Alternatively, consider the ongoing therapeutic needs of the individual patient. Rosuvastatin decreases synthesis of cholesterol and possibly other biologically active substances derived from cholesterol; therefore, rosuvastatin may cause fetal harm when administered to pregnant patients based on the mechanism of action [see Clinical Pharmacology ( 12.1 )] . In addition, treatment of hyperlipidemia is not generally necessary during pregnancy. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hyperlipidemia for most patients. Available data from case series and prospective and retrospective observational cohort studies over decades of use with statins in pregnant women have not identified a drug-associated risk of major congenital malformations. Published data from prospective and retrospective observational cohort studies with rosuvastatin use in pregnant women are insufficient to determine if there is a drug-associated risk of miscarriage (see Data) .

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption In clinical pharmacology studies in man, peak plasma concentrations of rosuvastatin were reached 3 to 5 hours following oral dosing. Both C max and AUC increased in approximate proportion to rosuvastatin dose.

Overdosage

Sourced from openFDA

No specific antidotes for rosuvastatin are known. Hemodialysis does not significantly enhance clearance of rosuvastatin. In the event of overdose, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.

Approval history

Sourced from openFDA
  • Aug 12, 2003NDANDA021366Astrazeneca
  • Jul 19, 2016ANDAANDA079170Aurobindo Pharma Ltd
  • Jul 19, 2016ANDAANDA079172Glenmark Speclt
  • Oct 31, 2016ANDAANDA207752Biocon Pharma
  • Oct 31, 2016ANDAANDA207408Changzhou Pharm
  • Oct 31, 2016ANDAANDA207062Renata
  • Oct 31, 2016ANDAANDA201619Torrent
  • Oct 31, 2016ANDAANDA206434Accord Hlthcare

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
223,850 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue14,3146.4%
  2. 2Nausea12,0715.4%
  3. 3Dyspnoea11,6395.2%
  4. 4Drug Ineffective11,5725.2%
  5. 5Diarrhoea10,9814.9%
  6. 6Pain10,6254.7%
  7. 7Off Label Use10,1794.5%
  8. 8Myalgia9,9234.4%
  9. 9Headache9,8104.4%
  10. 10Dizziness9,0874.1%
  11. 11Arthralgia8,9014.0%
  12. 12Asthenia8,5223.8%
  13. 13Pain In Extremity7,9863.6%
  14. 14Malaise7,8003.5%
  15. 15Fall7,4213.3%

Literature

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Recent PubMed references pinned to Rosuvastatin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 880 ClinicalTrials.gov registrations naming Rosuvastatin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Rosuvastatin. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Rosuvastatin work?
Rosuvastatin is an inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3‑hydroxy‑3‑methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol.
What is Rosuvastatin used for?
According to FDA labeling, Rosuvastatin carries indications including: Rosuvastatin tablets is indicated: To reduce the risk major adverse cardiovascular (CV) events (CV death, nonfatal myocardial infarction, nonfatal stroke, or an arterial revascularization procedure) in adults without established coronary heart disease who are at increased risk of CV disease based on age, high-sensitivity C-reactive protein (hsCRP) ≥2 mg/L, and at least one additional CV risk factor. As an adjunct to diet to: Reduce low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Rosuvastatin?
Rosuvastatin is classified as HMG CoA reductase inhibitors, HMG-CoA Reductase Inhibitor, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Decreased Cholesterol Synthesis.
What are the brand names for Rosuvastatin?
Rosuvastatin is marketed under brand names including Crestor, Ezallor, Roszet.
What are the contraindications for Rosuvastatin?
Rosuvastatin labeling lists contraindications including: Rosuvastatin tablets is contraindicated in the following conditions: Acute liver failure or decompensated cirrhosis [see Warnings and Precautions ( 5.3 )] . Hypersensitivity to rosuvastatin or any excipients in rosuvastatin tablets.. Always consult the full prescribing information and a clinician.
Note. Data for rosuvastatin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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