What is simvastatin?
Simvastatin is a HMG-CoA reductase inhibitor (stin) and is one of the most commonly prescribed cholesterol cores worldwide. It was known by the groundbreaking 4S study (Scandinavian Simvastatin Survival Study), which for the first time showed a reduction in total mortality by statin therapy.
Simvastatin is available as a generic product from numerous manufacturers (e.g. Simvastatin-ratiopharm®, SimvaHEXAL®, Simvastatin-1 A Pharma®). The original product was Zocor®.
It is taken as a prodrug and converted into active metabolite simvastatic acid in the liver. Simvastatin should preferably be taken in the evening as cholesterol synthesis is highest at night.
Active Ingredients & Mechanism of Action
Active ingredient: Simvastatin
Simvastatin inhibits body’s cholesterol production:
Active mechanism:
- Prodrug: is converted in the liver to active simvastatic acid (betahydroxy acid)
- Competitively inhibits HMG-CoA reductase
- Reduces cholesterol biosynthesis in the liver
- Compensatory high regulation of LDL receptors
- Increased intake of LDL cholesterol from blood
Lipid effect:
- LDL cholesterol: 25–40 % reduction (dose dependent)
- Triglycerides: 10–20 % reduction
- HDL cholesterol: 5-10 % increase
Pleiotropic effects:
- plaque stabilization
- Inflammation inhibition
- Improvement of endothelial function
- Antithrombotic action
Initiation of action: Measurable LDL lowering after 2 weeks. Maximum effect after 4–6 weeks.
Who is it suitable for?
Simvastatin is suitable for:
- Adults with hypercholesterinemia
- Patients with coronary heart disease (secondary prevention)
- diabetics with increased cardiovascular risk
- Primary prevention in high-risk patients
Especially suitable:
- If a moderate LDL lowering (25–40 %) is sufficient
- In patients with long-term good compatibility
- Cost-conscious therapy
Not suitable:
- Pregnancy and breastfeeding
- Active liver disease
- Simultaneous intake of strong CYP3A4 inhibitors
- If an LDL lowering > 40 % is required (better atorvastatin or rosuvastatin)
Available Dosages
Start dose:
- 10–20 mg once a day
Other dosages:
- 10 mg: Light cholesterol increase
- 20 mg: standard dose for most patients
- 40 mg: Stronger reduction required
Maximum balances:
- 80 mg: Only in patients who have had this dose for more than 12 months without muscle problems. New adjustment to 80 mg is NOT recommended (increased myopathy risk).
Available starches:
- 10 mg, 20 mg, 40 mg, 80 mg film tablets
LDL reduction after dose:
- 10 mg: approx. 25–30 %
- 20 mg: approx. 30-35 %
- 40 mg: approx. 35–40 %
Important: If > 40 % LDL lowering is necessary, change to Atorvastatin or Rosuvastatin instead of Simvastatin consider 80 mg.
How to Take
Intake:
- Take ABENDS once a day
- Independent meals
- film tablet with water swallow
Why night? The body's cholesterol synthesis is highest at night. Simvastatin has a short half-life (2–3 hours), so evening intake is important for maximum effect.
Important notes:
- NO large quantities of grapefruit juice (exchange effect!)
- First laboratory control after 4–12 weeks
- Regularly control liver values and lipid profile
- In case of muscle pain, muscle cramps or dark urine: inform immediately doctor
- Alcohol in dimensions
Contraindications
**Simvastatin must not be taken at:* *
- Active liver disease or unexplained transaminase increase
- Pregnancy and breastfeeding
- hypersensitivity to simvastatin
- Simultaneous administration of: Itraconazole, ketoconazole, Posaconazole, HIV protease inhibitors, erythromycin, Clarithromycin, Telithromycin, Nefazodon, Cobicistat, Gemfibrozil, Ciclosporin, Danazole
Preview at:
- Hypothyroidism
- Kidney failure
- High alcohol consumption
- Muscle diseases in history
- Older patients (> 70 years)
- Asian descent (increased myopathy rate)
pregnant: Strikt contraindicated. Safe prevention required.
Possible Side Effects
Family (1–10 %):
- Headaches
- Gastrointestinal complaints (abuse, bloating, diarrhea, constipation)
- Myalgia (muscle pain)
- Increased liver enzymes
- Upper respiratory infections
** Occasionally (0.1-1 %):* *
- Squeeze
- Sleep disorders
- Skin rash
- Indigestion
- Increased blood sugar levels
Selten, but seriously:
- Myopathy (CK > 10 times increased, especially at 80 mg)
- Rhabdomyolysis (several muscle decay – emergency!)
- Hepatitis
- Pancreatitis
80 mg dose: The myopathy rate is significantly higher at 80 mg than at lower doses. Therefore, a new adjustment to 80 mg is no longer recommended.
Interactions
Contrained (increased rhabdomyolysis risk):
- Strong CYP3A4 inhibitors: Itraconazole, ketoconazole, erythromycin, clarthromycin, HIV protease inhibitor
- Gemfibrozil
- Ciclosporin
- Danazole
Dosis limit:
- Amiodaron: Simvastatin max. 20 mg
- Verapamil, Diltiazem: Simvastatin max. 20 mg
- Amlodipine: Simvastatin max. 40 mg
- Lomitapid: Simvastatin max. 40 mg
More interactions:
- Grapefruit juice: CYP3A4 inhibition → raised mirror
- Warfarin: Reinforced coagulation inhibition
- Colchicin: Increased myopathy risk
- Fusidic acid: combination contraindicated
Important: Simvastatin has more interactions than atorvastatin or rosuvastatin, as it is more strongly degraded via CYP3A4.
Frequently Asked Questions
Similar Medications
Is simvastatin 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. Read the package leaflet before use.