Rosuvastatin
Unchecked
Rosuvastatin
Crestor, Ezallor
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Summary
Classes
Pharmacy
Starting dose
10-20 mg PO once daily (5 mg in Asian ancestry, elderly, hypothyroidism, or strong CYP/SLCO1B1 interactions)
Preparations
5, 10, 20, 40 mg tablets
US FDA Max
40 mg/d (rarely needed; 40 mg restricted to patients not at goal on 20 mg)
Pharmacology
Routes
Oral
Onset
LDL lowering at 1 week, max by 4 weeks
Duration
24 hours
Half-life
~19 hours[2]
Bioavailability
~20% (oral; hydrophilic, minimal CYP metabolism, mostly excreted unchanged in bile)[2]
Pregnancy
Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Rosuvastatin is a hydrophilic competitive HMG-CoA reductase inhibitor; per milligram it is the most potent statin in current use, with substantial LDL-lowering at 5-10 mg.0 Minimal CYP3A4 dependence (CYP2C9 minor) reduces drug-drug interactions; transport in and out of hepatocytes is largely via OATP1B1, making SLCO1B1 PGx genotype the most clinically actionable marker for statin-associated myopathy[1].
References
[edit | edit source]- ↑ CPIC Guideline for SLCO1B1, ABCG2, and CYP2C9 and Statin-Associated Musculoskeletal Symptoms, 2022. https://cpicpgx.org/guidelines/cpic-guideline-for-simvastatin-and-slco1b1/
- ↑ 2.0 2.1 FDA Prescribing Information, Crestor (rosuvastatin calcium), AstraZeneca, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021366s039lbl.pdf