Trade names Lescol, others MedlinePlus a694010 Molar mass 411.466 g/mol | AHFS/Drugs.com Monograph ATC code C10AA04 (WHO) CAS ID 93957-54-1 | |
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Pregnancycategory AU: DUS: X (Contraindicated) Routes ofadministration By mouth (capsules, tablets) | ||
Fluvastatin (INN, trade names Lescol, Canef, Vastin) is a member of the statin drug class, used to treat hypercholesterolemia and to prevent cardiovascular disease.
Contents
Adverse effects
Adverse effects are comparable to other statins. Common are nausea, indigestion, insomnia and headache. Myalgia (muscle pain), and rarely rhabdomyolysis, characteristic side effects for statins, can also occur.
Interactions
Contrary to lovastatin, simvastatin and atorvastatin, fluvastatin has no relevant interactions with drugs that inhibit the liver enzyme CYP3A4, and a generally lower potential for interactions than most other statins. Fluconazole, a potent inhibitor of CYP2C9, does increase fluvastatin levels.
Mechanism of action
Fluvastatin works by blocking the liver enzyme HMG-CoA reductase, which facilitates an important step in cholesterol synthesis.
Pharmacokinetics
The drug is quickly and almost completely (98%) absorbed from the gut. Food intake slows down absorption, but does not decrease it. Due to its first-pass effect, bioavailability is lower: about 24–30% according to different sources. Over 98% of the substance is bound to plasma proteins.
Several cytochrome P450 enzymes (mainly CYP2C9, but also CYP3A4 and CYP2C8) are involved in the metabolism of fluvastatin, which makes is less liable to interactions than most other statins. The main metabolite is inactive and is called "N-desisopropyl propionic acid" in the literature.
93–95% of the drug are excreted via the feces, less than 2% of which in form of the original substance.
Research
Fluvastatin has also been shown to exhibit antiviral activity against hepatitis C virus in a study with 31 patients. This effect has been described as modest, variable, and often short-lived, by the authors.