Fluvastatin

Substance from the group of statins.

Active principle: competitive, reversible inhibition of HMG-CoA reductase (rate-determining key enzyme in cholesterol synthesis; reduction of endogenous cholesterol synthesis and lowering of total cholesterol and LDL cholesterol levels.

Fully synthetic, lipophilic statin.

Statin with lower potency of max. possible LDL reduction dose-dependent 30 to 44 % and short half-life of 3 hours.

Metabolism of fluvastatin mainly by liver via CYP2C9;

Elimination: only approx. 6% via the kidneys, therefore also applicable in case of renal impairment; mild and moderate renal impairment have no effect on pharmacokinetics; in case of severe renal impairment doses ≥40mg not recommended (no sufficient data available!).

Can also be used in low doses after transplantation under ciclosporin therapy.

Treatment on the basis of and in combination with lifestyle changes (dietary changes, exercise, smoking cessation if necessary) in accordance with guidelines (Mach F et al 2020).

Hypercholesterolemia, (no separate data available for homozygous FH).

Primary prevention

Secondary prevention, with pre-existing cardiovascular disease (CHD, PAD), or a serious event (MI, stroke, TIA).

FH: Children and adolescents from 9 years of age (in heterozygous FH, simultaneous use of nicotinic acid, cholestyramine, fibrates not investigated in children and adolescents).

In children, observe age-dependent maximum doses, treatment and monitoring only by a specialist (see guideline).

Cholesterol and other intermediate products of cholesterol biosynthesis are essential in embryonic and fetal development and necessary for the synthesis of steroids and cell membranes!

Statins are therefore contraindicated during pregnancy and breastfeeding.

The potential risk of damage justifies a break in therapy.

Women and young girls of childbearing age need effective contraception (note interactions!)

For further information see specialist information!

In case of unexpected pregnancy during treatment, see Embryotox Charité

Enzymesystems/carriers and selection of substances with potential for interaction (inhibition), enhancement of effect and risk of serious adverse effects with concomitant treatment with fluvastatin:

CYP2C9

Amiodarone, capecitabine, cotrimoxazole, etravirine, fluconazole, fluvoxamine, ketoconazole, metronidazole, oxandrolone, voriconazole

OATP1B3

Clarithromycin, Ciclosporin, Erythromycin, Roxithromycin, Sacubitril

Also note:

Fibrates and niacin (fluvastatin only with caution!)

Colchicine (use fluvastatin with caution)

Ciclosporin (fluvastatin should only be used with caution in low doses)

Do not use at the same time as fusidic acid, including up to 7 days after the end of treatment.

Warfarin and others (increased effect possible, laboratory control, increased risk of bleeding cannot be ruled out)

Rifampicin (bioavailability of fluvastatin may be limited and dose increase may be necessary).

Oral antidiabetics (sulfonylureas) Possible increase in effect due to fluvastatin.

This information is only a selection! Further interactions must be clarified individually in each case! (for further information see Fachinfo! or databases on drug interactions).

It should also be noted that statins can alter the effect of concomitant medication and this can also result in additional incompatibilities!

Interaction studies have only been carried out in adults.

Do not use in case of:

• Hypersensitivity to the active substance or ingredients.
• active liver disease or persistent elevation of serum transaminases of unknown cause.
• During pregnancy and breastfeeding.
• Muscle diseases, myasthenia, ocular myasthenia, possibly a history of statin or fibrate-induced myopathy/rhabdomyolysis
• History of liver disease; heavy alcohol consumption should only be used with caution!

Hypothyroidism and other predisposing factors for severe myopathy and complications (careful risk/benefit assessment!).

Patients with rare hereditary galactose intolerance, complete lactase deficiency or glucose-galactose malabsorption should not take this
medicinal product.

For further information, see specialist information!

Fluvastatin (generics) 20mg, 40mg, 80mg (retard).

1. Fluvastatin Fachinfo: Fluvastatin ratiopharm 20mg/40mg/Fluvastatinratiopharm 80 mg Retard.
2. Mach F et al (2020). 2019 ESC/EAS Guidelines for the management of dyslipidaemias: lipid modification to reduce cardiovascular risk: The Task Force for the management of dyslipidaemias of the European Society of Cardiology (ESC) and European Atherosclerosis Society (EAS) European Heart Journal 41:111-188 https://doi.org/10.1093/eurheartj/ehz455.