Fluvastatin

Products

Fluvastatin is commercially available in the form of capsules and sustained-release generic tablets (generics). It has been approved in many countries since 1993. Sales of the original Lescol were discontinued by Novartis in 2018.

Structure and properties

Fluvastatin (C24H26FNO4, Mr = 411.5 g/mol) is present in drugs as fluvastatin sodium, a white or pale yellow to pale reddish-yellow, very hygroscopic, amorphous or crystalline powder that is soluble in water. Fluvastatin is a fluorinated indole derivative and was the first statin to be fully synthesized.

Effects

Fluvastatin (ATC C10AA04) has lipid-lowering properties. It lowers total cholesterol, LDL, apolipoprotein B, triglycerides, and increases HDL. The effects are due to inhibition of endogenous formation of cholesterol by competitive inhibition of the enzyme HMG-CoA reductase.

Indications

  • For the treatment of disorders of lipid metabolism (primary hypercholesterolemia, primary mixed dyslipidemia, heterozygous familial hypercholesterolemia).
  • In adults with coronary artery disease to reduce the risk of repeat coronary revascularization procedure.

Dosage

According to the professional information. The capsules are taken in the evening or before bedtime. The sustained-release tablets are administered once daily at any time of day, regardless of meals.

Contraindications

  • Hypersensitivity
  • Active liver disease
  • Unexplained and persistent elevation of serum transaminases.
  • Pregnancy and lactation

Full precautions can be found in the drug label.

Interactions

Fluvastatin is degraded via several CYP450 isozymes. The contribution of CYP3A4 is considered minor, and therefore drug-drug interactions are unlikely. Fibrates such as bezafibrate may increase fluvastatin concentrations and increase myopathy risk. Other interactions have been described with fluconazole, ciclosporin, ion-exchange resins, and rifampicin, among others.

Adverse effects

The most common possible adverse effects include digestive symptoms such as dyspepsia, abdominal pain, nausea, heartburn, constipation, flatulence, diarrhea, central disturbances such as headache, fatigue, insomnia, dizziness, and elevated liver enzymes. Very rarely, life-threatening disintegration of skeletal muscle (rhabdomyolysis) can develop with statins.