Drug reference

Fluvastatin

Statin · Antihyperlipidemic

Also known as Fluvastatin sodium, Cadaff XL, Dorisin XL, Lescol XL, Nandovar XL

StatinAntihyperlipidemic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

Azole AntifungalsSevereTextbookG&G 14e · p736
Hiv Protease InhibitorSevereTextbookKDT 7e · p637
Hiv Protease InhibitorsSevereTextbookG&G 14e · p736
KetoconazoleSevereTextbookKDT 7e · p637

Mechanism

Fluvastatin is a cholesterol-lowering agent that reversibly inhibits HMG-CoA reductase. This enzyme catalyzes a rate-limiting step in cholesterol biosynthesis. By inhibiting cholesterol biosynthesis in the liver, Fluvastatin reduces serum cholesterol levels, with the liver being its main target.

Indications

Adjunct to diet for primary hypercholesterolaemia or combined (mixed) hyperlipidaemias in patients who have not responded adequately to dietary controlPrevention of cardiovascular events in patients with previous myocardial infarction or unstable anginaAdjunct to diet to prevent cardiovascular events in patients with hypercholesterolaemiaSecondary prevention of coronary events after percutaneous coronary angioplastyHypercholesterolemiaReduction of LDL-C levelsTreat dyslipidemias, especially elevated LDL-C

Dosing

Adult: 80 mg daily by mouth using modified-release medicine (note: this dose form is not appropriate for initial dose titration)
Renal adjustment: Initiate doses above 40 mg daily with caution if eGFR less than 30 mL/minute/1.73 m2
Max dose: 80 mg daily (max. dose 20 mg daily with concomitant elbasvir with grazoprevir)

Pharmacokinetics

Half-life

1 to 4 h

Bioavailability

Undergoes efficient first-pass hepatic uptake by OATP1B1 after oral administration

Protein binding

>95%

Metabolism

Metabolized by CYP2C9

Excretion

Undergoes enterohepatic circulation

Side effects

Common

MyalgiaMuscle sorenessWeakness

Serious

Angioedema
Face oedema
Lupus-like syndrome
Muscle weakness
Sensation abnormal
Vasculitis
Myopathy
Rhabdomyolysis
Hepatotoxicity

Pregnancy & lactation

Lactation

Manufacturer advises avoid; no information available

Drug interactions

Azole Antifungals

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Hiv Protease Inhibitor

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Hiv Protease Inhibitors

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy. For simvastatin, coadministration is contraindicated.

Source: G&G 14e · p736

Ketoconazole

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: KDT 7e · p637

Macrolide Antibiotics

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Source: G&G 14e · p736

Nefazodone

Severe

Textbook

Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.

Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.

Source: G&G 14e · p736

Nicotinic Acid

Severe

Textbook

Increased risk of myopathy and rhabdomyolysis.

A lower dose of statin is advisable when nicotinic acid is given concurrently. Close monitoring for muscle symptoms is essential.

Source: KDT 7e · p637, p640

Clofibrate

Severe

Database

Drug interaction classified as: others

Source: DDInter

Colchicine

Severe

Database

Drug interaction classified as: synergy, metabolism

Source: DDInter

Erythromycin

Severe

Database

Increased risk of myopathy and rhabdomyolysis.

Concomitant use should be avoided or used with extreme caution, especially for statins metabolized by CYP3A4. Dose reduction of the statin and vigilant monitoring for muscle symptoms are necessary.

Source: DDInter

Fenofibrate

Severe

Database

Lower risk of statin myopathy compared to other fibrate-statin combinations.

Fenofibrate is the most suitable fibrate for combining with statins due to its minimal impact on statin metabolism and lower myopathy risk. However, continued vigilance for muscle symptoms is prudent.

Source: DDInter

Gemfibrozil

Severe

Database

Increased plasma concentration of statin hydroxy acids, leading to an increased risk of myopathy (including rhabdomyolysis).

Avoid coadministration. The FDA withdrew approval for statin drug combinations containing fibrates in 2016.

Source: DDInter