Rosuvastatin
Crestor | Ezallor
Overview
Rosuvastatin is a potent HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and reduce cardiovascular risk.
Indications
- Primary hyperlipidemia
- Mixed dyslipidemia
- Prevention of cardiovascular events
- Homozygous familial hypercholesterolemia
Contraindications
- Active liver disease
- Pregnancy and breastfeeding
Classification
Mechanism of Action
Competitively inhibits HMG-CoA reductase, reducing hepatic cholesterol synthesis and increasing LDL-receptor-mediated clearance of LDL particles.
Pharmacodynamics
Produces marked reductions in LDL cholesterol and triglycerides with a modest increase in HDL. It is more hydrophilic than most statins and is largely not metabolized by CYP3A4.
Pharmacokinetics
- Absorption
- Peak plasma concentrations reached in about 3-5 hours; absolute bioavailability is roughly 20%.
- Distribution
- Volume of distribution about 134 L; extensive hepatic uptake via OATP1B1.
- Metabolism
- Limited metabolism, mainly by CYP2C9; not significantly metabolized by CYP3A4.
- Excretion
- About 90% eliminated unchanged in feces; the remainder renally.
- Half-life
- Approximately 19 hours
- Bioavailability
- Approximately 20%
- Protein Binding
- Approximately 88%
Dosage
Typical dosage: 5-40 mg once daily
Available Forms
- Tablet
- Capsule
Side Effects
Common
- Headache
- Myalgia
- Nausea
- Constipation
Serious
- Rhabdomyolysis
- Myopathy
- Hepatotoxicity
Rare
- Proteinuria
- Immune-mediated necrotizing myopathy
Drug Interactions
May increase INR; monitor coagulation when starting or changing the statin dose.
Markedly increases rosuvastatin exposure and the risk of myopathy.
Warnings
Pregnancy
Category X
Toxicity
Dose-related myopathy and hepatotoxicity are the principal toxic effects.
Overdose
No specific antidote. Provide supportive care; hemodialysis is not effective at enhancing clearance.
References
Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.