Drug Guide
Rosuvastatin Calcium
Classification
Therapeutic: Lipid-lowering agent
Pharmacological: HMG-CoA reductase inhibitor (statin)
FDA Approved Indications
- Hyperlipidemia
- Homozygous familial hypercholesterolemia
- Prevention of cardiovascular disease
Mechanism of Action
Inhibits HMG-CoA reductase enzyme, leading to decreased cholesterol synthesis in the liver and increased LDL receptor expression, which enhances clearance of LDL cholesterol from the bloodstream.
Dosage and Administration
Adult: Starting dose typically 10-20 mg once daily, with max 40 mg daily. Adjust based on response and tolerability.
Pediatric: Approved for children aged 10-17 for certain lipid disorders; dosing varies.
Geriatric: Start at lower doses due to increased risk of adverse effects, monitor closely.
Renal Impairment: Use with caution; dose adjustments may be necessary.
Hepatic Impairment: Contraindicated in active liver disease; caution in elevated liver enzymes.
Pharmacokinetics
Absorption: Well absorbed after oral administration
Distribution: Bound to plasma proteins (~88%)
Metabolism: Minimal hepatic metabolism, primarily via CYP2C9
Excretion: Excreted mainly in feces (90%), some in urine (10%)
Half Life: Approximately 19 hours
Contraindications
- Active liver disease
- Unexplained persistent elevations of serum transaminases
- Pregnancy and lactation
Precautions
- Monitor liver function and lipid levels periodically
- Use with caution in patients on concomitant medications that can increase risk of myopathy
Adverse Reactions - Common
- Headache (Common)
- Myalgia (Common)
- Abdominal pain (Common)
- Nausea (Common)
Adverse Reactions - Serious
- Rhabdomyolysis (Rare)
- Myopathy progressing to rhabdomyolysis (Rare)
- Hepatotoxicity (Rare)
Drug-Drug Interactions
- Cyclosporine, certain antivirals (like HIV protease inhibitors), fibrates, azole antifungals, and others that increase statin levels.
Drug-Food Interactions
- Grapefruit juice (may increase plasma concentration)
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor lipid panels, liver function tests, and for signs of muscle pain or weakness.
Diagnoses:
- Risk for activity intolerance related to muscle adverse effects
- Impaired skin integrity or injury risk due to myopathy.
Implementation: Administer as prescribed, usually once daily. Educate patient on importance of adherence and monitoring.
Evaluation: Assess lipid level changes, liver enzymes, and muscle symptoms periodically.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report any muscle pain, weakness, or unusual fatigue.
- Avoid excessive alcohol intake.
- Inform healthcare providers of all medications and supplements.
Special Considerations
Black Box Warnings:
- Potential for myopathy and rhabdomyolysis, especially when used with interacting drugs.
- Pregnancy Category X - contraindicated in pregnancy.
Genetic Factors: Genetic variants affecting CYP2C9 may alter drug metabolism.
Lab Test Interference: Might slightly elevate liver enzymes or creatine kinase.
Overdose Management
Signs/Symptoms: Muscle pain, weakness, elevated liver enzymes.
Treatment: Supportive care, hydration, and monitoring; no specific antidote.
Storage and Handling
Storage: Store at room temperature, away from moisture and heat.
Stability: Stable for 2-3 years depending on packaging.