What is fluvastatin?
Fluvastatin is a synthetic statin that differs from most other statins due to its unique metabolic path via CYP2C9 (instead of CYP3A4). It is used for the treatment of hypercholesterinemia and for secondary prevention according to coronaarrangioplasty (heart catheter intervention).
Fluvastatin was known as Locol® (as retard tablet: Locol® XL) and is now available as a generic (e.g. Fluvastatin-ratiopharm®). The LIPS study (Lescol Intervention Prevention Study) showed a particular benefit for percutaneous coronary intervention (PCI).
It is one of the less potent statins and is used especially with mild to moderate cholesterol increase or as a statin with favorable interaction profile.
Active Ingredients & Mechanism of Action
Active ingredient: Fluvastatin (als Natriumsalz)
Fluvastatin inhibits cholesterol biosynthesis:
Active mechanism:
- inhibits HMG-CoA reductase
- Full Synthetic Statin (Indol derivative)
- Reduces hepatic cholesterol production
- Compensatory high regulation of LDL receptors
Lipid effect:
- LDL cholesterol: 20–35 % reduction (dose dependent)
- Triglycerides: 10-15 % reduction
- HDL cholesterol: 3-8 % increase
Special features:
- Metabolism via CYP2C9 (not CYP3A4!) → other interactions than Simvastatin/Atorvastatin
- High selectivity for liver cells
- Quick intake into the liver (high first pass effect)
- Retardform (XL) allows constant active mirrors
Initiation of action: LDL lowering measurable after 1–2 weeks. Maximum effect after 4 weeks.
Who is it suitable for?
Fluvastatin is suitable for:
- Adults with hypercholesterinemia
- secondary prevention according to coronary arterial (PTCA/PCI)
- Mixed dyslipidemia
- Patients who need to take CYP3A4 inhibitors
Especially recommended at:
- After cardiac catheter intervention (LIPS study)
- If other statistics are not possible due to CYP3A4 interactions
- Light to moderate cholesterol increase
Not suitable:
- Pregnancy and breastfeeding
- Active liver disease
- If strong LDL lowering (> 35 %) is required
Available Dosages
Standard tablets:
- 20–40 mg once a day
Retard tablets (XL):
- 80 mg once a day (can be taken at any time of day)
Available starches:
- 20 mg, 40 mg capsules
- 80 mg retard tablets (XL)
LDL reduction after dose:
- 20 mg: approx. 20–25 %
- 40 mg: approx. 25–30 %
- 80 mg (XL): approx. 33–35 %
Dosis adjustment:
- Light to medium kidney failure: No adjustment required
- Liver failure: contraindicated with active disease
How to Take
**Standard tablets (20/40 mg):* *
- Take once a day (short half-life)
- Independent meals
- Swallow capsule with water
Retard tablets (80 mg XL):
- Once a day, at any time of day
- Do not divide, chew or crush tablet
- Independent meals
Important notes:
- Laboratory control after 4–12 weeks (Leberwerten, Lipide)
- Report muscle pain to the doctor
- No problem with grapefruit juice (no CYP3A4-substrate)
For forgotten dose: Take the next regular time. Don't take twice.
Contraindications
**Fluvastatin must not be taken at:* *
- Active liver disease or unexplained transaminase increase
- Pregnancy and breastfeeding
- hypersensitivity to fluvastatin
Preview at:
- Kidney failure
- Hypothyroidism
- Muscle diseases in history
- High alcohol consumption
- Simultaneously taking fibrates
- CYP2C9 inhibitors (Fluconazole)
pregnant: Contraindicated. Safe contraception required.
Possible Side Effects
Family (1–10 %):
- Sleep disorders
- Headaches
- Gastrointestinal complaints (dyspepsie, abdominal pain, nausea)
- muscle pain
- Increased liver enzymes
** Occasionally (0.1-1 %):* *
- fatigue
- Squeeze
- Skin rash
- Paresthesia
Selten:
- Myopathy, Rhabdomyolysis
- Hepatitis
- Vasculitis
- Sensitivity reactions
General: Fluvastatin is considered a well-tolerated statin. The myopathy rate is comparable to other statins in therapeutic dose.
Interactions
**CYP2C9 change (not CYP3A4!):* * This means other interactions than Simvastatin or Atorvastatin.
Preview at:
- Fluconazole (CYP2C9 inhibitor → increased fluvastatin level)
- Fibrates (Gemfibrozil) → myopathy risk
- Phenytoin → alternating mirror changes
- Warfarin → INR control (Fluvastatin inhibits CYP2C9 easily)
- Ciclosporin → increased levels of both substances
- Colchicin → myopathy risk
No relevant interaction with:
- Grapefruit juice (no CYP3A4-substrate)
- Erythromycin, Clarithromycin
- Itraconazole, ketoconazole
- Verapamil, Diltiazem, Amiodaron
Advantage: Most CYP3A4-dependent interactions that are problematic in simvastatin and atorvastatin are eliminated in fluvastatin.
Frequently Asked Questions
Similar Medications
Is fluvastatin 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.