====== Rosuvastatin (Crestor®) ======

<WRAP right 300px>
<WRAP infobox>
^ Drug Overview | {{ :cardio:lipids:rosuvastatin_structure.svg |}}|
| Drug Class | [[cardio:lipids:start|Statins]] |
| Mechanism | HMG-CoA Reductase Inhibitor |
| Primary Uses | [[cardio:lipids:ascvd|ASCVD Prevention]]; [[cardio:lipids:hyperlipidemia|Hyperlipidemia]] |
| Route | Oral |
| Dose Range | 5–40 mg daily |
| Intensity | Moderate–High |
| LDL Reduction | 45–63% |
| Metabolism | Minimal CYP2C9 |
| Half-life | ~19 hours |
| Elimination | Hepatic (minor renal component) |
| Renal Adjustment | Yes (severe CKD) |
| Black Box Warning | No |
| FDA Approval | 2003 |
</WRAP>
</WRAP>

===== Overview =====

Rosuvastatin is a high-potency [[cardio:lipids:start|statin]] with strong LDL-lowering capability and robust outcome data.

It is one of the most potent statins per milligram and has a lower CYP interaction burden compared to [[cardio:lipids:atorvastatin|Atorvastatin]].

It is frequently selected for high-intensity therapy.

<WRAP clear></WRAP>

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===== Mechanism of Action =====

Primary Target:
  * HMG-CoA reductase (rate-limiting enzyme in hepatic cholesterol synthesis)

Physiologic Effects:
  * ↓ Hepatic cholesterol synthesis
  * ↑ LDL receptor expression
  * ↑ Circulating LDL clearance

Net Effect:
  * Significant LDL reduction
  * Plaque stabilization
  * Reduced cardiovascular events

LDL lowering is dose-dependent.

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===== Indications =====

  * [[cardio:lipids:hyperlipidemia|Hyperlipidemia]]
  * [[cardio:lipids:ascvd|ASCVD prevention]]
  * Secondary prevention after:
      * [[cardio:ischemia:mi|Myocardial Infarction]]
      * [[cardio:ischemia:stroke|Ischemic Stroke]]
      * [[cardio:ischemia:stable_angina|Stable Angina]]

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===== Dosing =====

Moderate-Intensity:
  * 5–10 mg daily

High-Intensity:
  * 20–40 mg daily

Renal Considerations:
  * Start lower doses in severe CKD
  * Avoid 40 mg dose in significant renal impairment

Dose selection is based on ASCVD risk category.

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===== Pharmacokinetic Highlights =====

  * Hydrophilic statin
  * Minimal CYP metabolism (CYP2C9)
  * Lower drug–drug interaction risk compared to [[cardio:lipids:atorvastatin|Atorvastatin]] or [[cardio:lipids:simvastatin|Simvastatin]]
  * Longer half-life (~19 hours)

Hydrophilicity may reduce muscle penetration relative to lipophilic statins.

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===== Adverse Effects =====

Muscle:
  * Myalgias
  * Myositis
  * Rare rhabdomyolysis

Hepatic:
  * Mild ALT elevation

Metabolic:
  * Slight increase in diabetes risk

Risk increases with:
  * High doses
  * Renal impairment
  * Combination with [[cardio:lipids:fibrates:start|Fibrates]] (especially [[cardio:lipids:gemfibrozil|Gemfibrozil]])

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===== Drug Interactions =====

Lower CYP interaction burden.

Caution with:
  * [[cardio:lipids:fibrates:start|Fibrates]]
  * [[cardio:lipids:niacin|Niacin]]
  * Severe renal impairment

Less affected by CYP3A4 inhibitors compared to:
  * [[cardio:lipids:atorvastatin|Atorvastatin]]
  * [[cardio:lipids:simvastatin|Simvastatin]]
  * [[cardio:lipids:lovastatin|Lovastatin]]

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===== Monitoring =====

  * Lipid panel (4–12 weeks after initiation)
  * Baseline liver enzymes
  * Assess for muscle symptoms
  * Renal function in CKD patients

Routine CK monitoring only if symptomatic.

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===== Comparison Within Class =====

Compared to [[cardio:lipids:atorvastatin|Atorvastatin]]:

  * More potent per mg
  * Fewer CYP interactions
  * More hydrophilic

Compared to [[cardio:lipids:pravastatin|Pravastatin]]:

  * Much more potent
  * Greater LDL reduction

Clinical Role:
  * Excellent high-intensity option
  * Preferred in patients on multiple interacting medications

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===== High-Yield Pearls =====

  * Most potent statin per mg
  * High-intensity therapy at 20–40 mg
  * Lower CYP interaction risk
  * Requires caution in severe renal impairment
  * Strong outcome data in secondary prevention

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===== Related =====

  * [[cardio:lipids:start|Statins]]
  * [[cardio:lipids:atorvastatin|Atorvastatin]]
  * [[cardio:lipids:ezetimibe|Ezetimibe]]
  * [[cardio:lipids:pcsk9:start|PCSK9 Inhibitors]]
  * [[cardio:intro:start|Cardiovascular Pharmacology]]