What is Rosuvastatin (Crestor®)?
Rosuvastatin is the most potent available statin and can reduce LDL cholesterol by up to 55%. It is sold under the brand name Crestor® and as a generic (e.g. Rosuvastatin-ratiopharm®, Rosuvastatin HEXAL®).
In contrast to Simvastatin and Atorvastatin, Rosuvastatin is mined only minimally via CYP enzymes, which leads to significantly less interaction with other drugs. It is a hydrophilic statin with a preferred absorption into the liver.
The JUPITER study showed that Rosuvastatin significantly reduces cardiovascular events even in patients with normal cholesterol but increased CRP (inflammation marker).
Active Ingredients & Mechanism of Action
Active ingredient: Rosuvastatin (als Calciumsalz)
Rosuvastatin particularly inhibits cholesterol biosynthesis:
Active mechanism:
- Potent inhibition of HMG-CoA reductase of all available statistics
- Low absorption in muscle cells (theoretically less muscle problems)
- Strong Compensatory LDL receptor high regulation
Lipid effect:
- LDL cholesterol: 40–55 % reduction (dose dependent)
- Triglycerides: 15–25 % reduction
- HDL cholesterol: 8–14 % increase
Special features:
- Minimal CYP3A4 metabolism → few interactions
- Mainly unaltered over the liver
- No influence on grapefruit juice
- Intake possible at any time of day
Initiation of action: Significant LDL reduction after 1–2 weeks. Maximum effect after 4 weeks.
Who is it suitable for?
Rosuvastatin is suitable for:
- Adults with primary hypercholesterolemia
- Patients with family hypercholesterinemia (strongly elevated LDL)
- Mixed dyslipidemia
- Primary and secondary prevention of cardiovascular events
- patients with increased hsCRP and cardiovascular risk
Especially recommended at:
- High LDL that needs to be greatly reduced (> 50 %)
- Many accompanying drugs (less interactions)
- If atorvastatin does not work enough
- Familiary hypercholesterolemia
Not suitable:
- Pregnancy and breastfeeding
- Active liver disease
- Heavy kidney failure (at 40 mg)
- Myopathy among stamina in prehistory
Available Dosages
Start dose:
- 5–10 mg once a day
Other dosages:
- 5 mg: start of therapy, especially in Asian patients or increased myopathy risk
- 10 mg: standard dose for most patients
- 20 mg: Stronger reduction required
- 40 mg: maximum dose, only with severe hypercholesterolemia under close-meshed control
Available starches:
- 5 mg, 10 mg, 20 mg, 40 mg film tablets
LDL reduction after dose:
- 5 mg: approx. 38 %
- 10 mg: approx. 43 %
- 20 mg: approx. 48 %
- 40 mg: approx. 53–55 %
Dosis adjustment:
- Heavy kidney failure: max. 20 mg (40 mg contraindicated)
- Asian patients: start with 5 mg (increased exposure)
How to Take
Intake:
- Once a day at any time
- Independent meals
- film tablet with water swallow
Advantages:
- No time retention (other than Simvastatin, which must be taken in the evening)
- No Grapefruit problem (other than Simvastatin and Atorvastatin)
Important notes:
- First laboratory control after 4–12 weeks
- Regular monitoring of liver values, lipid profile and kidney function
- For muscle pain or dark urine: Contact doctor
- thyroid function should be checked before the start of therapy
For forgotten dose: Take the next regular time. Don't take twice.
Contraindications
**Rosuvastatin must not be taken at:* *
- Active liver disease or unexplained transaminase increase
- Pregnancy and breastfeeding
- Heavy kidney failure (only with 40 mg contraindicated)
- Myopathy
- Simultaneous ciclosporin therapy (at all doses)
- hypersensitivity to Rosuvastatin
Preview at:
- Hypothyroidism
- Personal or family muscle disease
- Asian origin (increased plasma level)
- Kidney insufficiency (dose adjustment)
- High alcohol consumption
- Simultaneous fibrate intake
pregnant: Strikt contraindicated. Safe contraception required.
Possible Side Effects
Family (1–10 %):
- Headaches
- Squeeze
- Myalgia (muscle pain)
- Gastrointestinal complaints (ovenipation, nausea)
- Asthenie (smooth)
- Increased liver enzymes
- Diabetes mellitus (lightly increased risk, dose-dependent)
** Occasionally (0.1-1 %):* *
- Skin rash, Pruritus
- Increased CK values
- stomach pain
- Proteinuria (at high doses)
Selten:
- Myopathy, Rhabdomyolysis
- Pancreatitis
- Hepatitis
- Peripheral neuropathy
** In controlled studies, the myopathy rate at Rosuvastatin is comparable to other statistics. The hydrophilic profile protects against muscle cell absorption.
Interactions
Advantage of Rosuvastatin: Minimal CYP3A4 metabolism → significantly less interactions than simvastatin or atorvastatin.
Contraint with:
- Ciclosporin (all cans)
Dosis limit:
- Gemfibrozil: Rosuvastatin max. 20 mg
- Lopinavir/Ritonavir, Atazanavir/Ritonavir: Max. 10 mg
- Regorafenib: Careful
Preview at:
- Anticoagulants (Warfarin, Phenprocoumon) – Control INR
- Fibrates (myopathy risk)
- Fusidic acid – temporarily pause
No relevant interaction with:
- Grapefruit juice (no CYP3A4-substrate)
- Amiodaron, Verapamil, Diltiazem (no dose limitation required as with Simvastatin)
Frequently Asked Questions
Similar Medications
Is Rosuvastatin (Crestor®) right for you?
A licensed doctor will review your information and issue a prescription if suitable. Discreet and secure.
Important Notice
This information does not replace medical advice. If you have questions about your health or the suitability of this medication, please consult a doctor or pharmacist.
Important Safety Information
This service operates under German pharmaceutical law (HWG). For risks and side effects, read the package leaflet and consult your doctor or pharmacist. All medications are dispensed from a licensed pharmacy in Germany.