Rosuvastatin
Unchecked
From Pharmacopedia
More actions
Rosuvastatin
Crestor, Ezallor
Experience
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
Effects
No effects listed yet. Be the first to suggest one.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
Summary
Classes
Common uses
Hyperlipidemia0, Cardiovascular risk reduction0, Atherosclerosis0
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- ↑ 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