Fluvastatin !

A lower-potency statin metabolized mainly by CYP2C9 rather than CYP3A4. It lowers LDL moderately.

Updated 2026-11-01

Class: Statins
Enzyme: HMG-CoA reductase
ATC code: C10AA04
WHO Model List of Essential Medicines

HMG-CoA reductaseFluvastatin

The figure shows fluvastatin in the HMG-CoA pocket of the catalytic portion of human HMG-CoA reductase.

Target in 3D: HMG-CoA reductase. PDB structure 1HWI (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Fluvastatin competitively inhibits HMG-CoA reductase in the liver. Lower intracellular cholesterol activates SREBP-2, increases LDL receptors and lowers blood LDL.

Occupies the HMG-CoA pocket of HMG-CoA reductase
Liver cholesterol synthesis falls
More LDL receptors clear LDL from the blood

Pharmacokinetics

Absorption: Oral; capsules and an extended-release tablet exist.
Metabolism: Mainly by CYP2C9 (about 75%), with minor roles for CYP2C8 and CYP3A4; its metabolites are not significantly active.
Elimination: Mostly in feces as metabolites; very little in urine.

Indications

High LDL cholesterol and mixed dyslipidemia Atherosclerosis and dyslipidaemia →
Heterozygous familial hypercholesterolemia, including in children and adolescents Familial hypercholesterolemia →
Secondary prevention of coronary events after percutaneous coronary intervention

Adverse effects

Common

Dyspepsia, abdominal pain
Headache
Muscle aches
Raised liver transaminases

Contraindications

Active liver disease or unexplained persistent transaminase rises
Pregnancy and breastfeeding
Hypersensitivity to a component

Key interactions

Cyclosporine, fluconazole: Raise fluvastatin exposure; the dose is limited.
Gemfibrozil, other fibrates, niacin: Add to the muscle risk.
Warfarin: Prothrombin time is checked when fluvastatin is started, stopped or changed.
Glyburide, phenytoin: Glucose or phenytoin levels are checked when the fluvastatin dose changes.

What is monitored

Lipid panel
Liver enzymes
Creatine kinase if there are muscle symptoms

Administration and safety

Oral; capsules and extended-release tablets are different products, and the prescribed form is checked.
Separated from bile acid resins when both are used.
Capsules (immediate release) are usually taken in the evening.

Nursing care

Before: lipid panel, liver enzymes, interacting drugs (fluconazole, cyclosporine, warfarin).
Ask about muscle pain or weakness.
Check the INR more often in patients on warfarin.
Ask about pregnancy plans.

Pregnancy and breastfeeding

Contraindicated in pregnancy and in women who may become pregnant, and not used while breastfeeding.

Test yourself

Think of the answer, then tap the question to see it.

Which CYP enzyme mainly metabolizes fluvastatin?

CYP2C9 (about 75%), unlike simvastatin, lovastatin and atorvastatin, which depend on CYP3A4.

Which antifungal requires a fluvastatin dose limit?

Fluconazole, which raises fluvastatin exposure.

In which coronary patients was fluvastatin shown to reduce recurrent cardiac events?

In patients with coronary heart disease after a percutaneous coronary intervention (PCI).

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Fluvastatin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - FLUVASTATIN capsule (DailyMed (U.S. National Library of Medicine), 2026); COMPLEX OF THE CATALYTIC PORTION OF HUMAN HMG-COA REDUCTASE WITH FLUVASTATIN (RCSB Protein Data Bank, 2001).

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Representative model, for educational purposes only.