Peringatan Keamanan

Generally well-tolerated. May cause gastrointestinal upset (diarrhea, nausea, constipation, gas, abdominal pain), myotoxicity (mypothy, myositis, rhabdomyolysis), and hepatotoxicity.

Fluvastatin

DB01095

small molecule approved

Deskripsi

Fluvastatin is an antilipemic agent that competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Fluvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. It is also the first entirely synthetic HMG-CoA reductase inhibitor and is structurally distinct from the fungal derivatives of this therapeutic class. Fluvastatin is a racemate comprising equimolar amounts of (3R,5S)- and (3S,5R)-fluvastatin.

Struktur Molekul 2D

Berat 411.473
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3 hours
Volume Distribusi * 0.35 L/kg
Klirens (Clearance) * 0.8 L/h/kg * 107 ± 38.1 L/h [Hypercholesterolemia patients receiving a single dose of 20 mg] * 87.8 ± 45 L/h [Hypercholesterolemia patients receiving 20 mg twice daily] * 108 ± 44.7 L/h [Hypercholesterolemia patients receiving 40 mg single] * 64.2 ± 21.1 L/h [Hypercholesterolemia patients receiving 40 mg twice daily]

Absorpsi

Rapidly and almost completely absorbed (> 90%), but undergoes extensive first pass metabolism. Bioavailability is 24% (range 9-50%) when a 10 mg dose is given. The mean relative bioavailability of the extended-release tablet is 29% (range: 9% to 66%) compared to an immediate-release capsule administered under fasting conditions. When given orally, fluvastatin reaches peak concentrations (Tmax) in less than one hour. Taking the extended release tablet with a high-fat meal will delay absorption (Tmax = 6 hours) and increase bioavailability by approximately 50%. However, the maximum concentration of fluvastatin sodium extended-release tablets seen after a high fat meal is less than the peak concentration following a single dose or twice daily dose of the 40 mg fluvastatin capsule.

Metabolisme

Undergoes hepatic metabolism primarily via hydroxylation of the indole ring at the 5- and 6-positions to 5-hydroxy fluvastatin and 6-hydroxy fluvastatin, respectively. N-dealkylation to N-desisopropyl fluvastatin and beta-oxidation of the side chain also occurs. Metabolized primarily by the CYP2C9 isozyme system (75%), and to a lesser extent by CYP3A4 (~20%) and CYP2C8 (~5%). Hydroxylated metabolites retain some pharmcological activity, but are present as conjugates (glucuronides and sulfates) in the blood and are rapidly eliminated via bile into feces. Both enantiomers of fluvastatin are metabolized in a similar manner. Fluvastatin also undergoes glucuronidation via UGT enzymes.

Rute Eliminasi

When orally administered, fluvastatin is primarily excreted in the faces ( ~90%) as metabolites, with less than 2% present as unchanged drug. Approximately 5% was recovered in the urine.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Should be taken consistently in regards to meals.

Interaksi Obat

923 Data
Cyclosporine The serum concentration of Fluvastatin can be increased when it is combined with Cyclosporine.
Acipimox Acipimox may increase the myopathic rhabdomyolysis activities of Fluvastatin.
Bezafibrate Bezafibrate may increase the myopathic rhabdomyolysis activities of Fluvastatin.
Ciprofibrate The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ciprofibrate is combined with Fluvastatin.
Daptomycin The risk or severity of myopathy can be increased when Fluvastatin is combined with Daptomycin.
Gemfibrozil The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Fluvastatin.
Niacin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Fluvastatin.
Pazopanib Fluvastatin may increase the hepatotoxic activities of Pazopanib.
Raltegravir The risk or severity of myopathy and rhabdomyolysis can be increased when Raltegravir is combined with Fluvastatin.
Trabectedin The risk or severity of myopathy and rhabdomyolysis can be increased when Fluvastatin is combined with Trabectedin.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Fluvastatin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Fluvastatin.
Fluconazole The metabolism of Fluvastatin can be decreased when combined with Fluconazole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Fluvastatin.
Colchicine Colchicine may increase the myopathic rhabdomyolysis activities of Fluvastatin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Fluvastatin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Fluvastatin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Fluvastatin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Fluvastatin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Fluvastatin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Fluvastatin.
Amiodarone The metabolism of Fluvastatin can be increased when combined with Amiodarone.
Bosentan The serum concentration of Fluvastatin can be decreased when it is combined with Bosentan.
Danazol The serum concentration of Fluvastatin can be increased when it is combined with Danazol.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Fluvastatin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Fluvastatin.
Colestipol Colestipol can cause a decrease in the absorption of Fluvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Fluvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Fluvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Fluvastatin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Fluvastatin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Fluvastatin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Fluvastatin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Fluvastatin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Fluvastatin.
Zidovudine The metabolism of Fluvastatin can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Fluvastatin can be increased when combined with Lamotrigine.
Ethinylestradiol The metabolism of Fluvastatin can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Fluvastatin can be increased when combined with Testosterone propionate.
Mifepristone The serum concentration of Fluvastatin can be increased when it is combined with Mifepristone.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Fluvastatin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Fluvastatin.
Mirabegron The serum concentration of Fluvastatin can be increased when it is combined with Mirabegron.
Cholestyramine The serum concentration of Fluvastatin can be decreased when it is combined with Cholestyramine.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Fluvastatin.
Fusidic acid The risk or severity of rhabdomyolysis can be increased when Fusidic acid is combined with Fluvastatin.
Phenindione The risk or severity of bleeding can be increased when Fluvastatin is combined with Phenindione.
Tioclomarol The risk or severity of bleeding can be increased when Fluvastatin is combined with Tioclomarol.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Fluvastatin is combined with Ethyl biscoumacetate.
Diphenadione The risk or severity of bleeding can be increased when Fluvastatin is combined with Diphenadione.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Fluvastatin is combined with 4-hydroxycoumarin.
Clorindione The risk or severity of bleeding can be increased when Fluvastatin is combined with Clorindione.
St. John's Wort The serum concentration of Fluvastatin can be decreased when it is combined with St. John's Wort.
Clofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Clofibrate is combined with Fluvastatin.
Fenofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Fenofibrate is combined with Fluvastatin.
Etofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Etofibrate is combined with Fluvastatin.
Simfibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Simfibrate is combined with Fluvastatin.
Ronifibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Ronifibrate is combined with Fluvastatin.
Aluminium clofibrate The risk or severity of myopathy and rhabdomyolysis can be increased when Aluminium clofibrate is combined with Fluvastatin.
Clofibride The risk or severity of myopathy and rhabdomyolysis can be increased when Clofibride is combined with Fluvastatin.
Fenofibric acid The risk or severity of myopathy and rhabdomyolysis can be increased when Fenofibric acid is combined with Fluvastatin.
Imipramine The metabolism of Fluvastatin can be decreased when combined with Imipramine.
Darifenacin The metabolism of Fluvastatin can be decreased when combined with Darifenacin.
Quinine The metabolism of Fluvastatin can be decreased when combined with Quinine.
Fluvoxamine The metabolism of Fluvastatin can be decreased when combined with Fluvoxamine.
Abiraterone The metabolism of Fluvastatin can be decreased when combined with Abiraterone.
Nicardipine The metabolism of Fluvastatin can be decreased when combined with Nicardipine.
Sulfaphenazole The metabolism of Fluvastatin can be decreased when combined with Sulfaphenazole.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Fluvastatin.
Celecoxib The metabolism of Fluvastatin can be decreased when combined with Celecoxib.
Chloroquine The metabolism of Fluvastatin can be decreased when combined with Chloroquine.
Terbinafine The metabolism of Fluvastatin can be decreased when combined with Terbinafine.
Cholecalciferol The metabolism of Fluvastatin can be decreased when combined with Cholecalciferol.
Rucaparib The metabolism of Fluvastatin can be decreased when combined with Rucaparib.
Cimetidine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cimetidine is combined with Fluvastatin.
Tranylcypromine The metabolism of Fluvastatin can be decreased when combined with Tranylcypromine.
Tegaserod The metabolism of Fluvastatin can be decreased when combined with Tegaserod.
Phenylbutyric acid The metabolism of Fluvastatin can be decreased when combined with Phenylbutyric acid.
Ritanserin The metabolism of Fluvastatin can be decreased when combined with Ritanserin.
Rhein The metabolism of Fluvastatin can be decreased when combined with Rhein.
Metoprolol The metabolism of Fluvastatin can be decreased when combined with Metoprolol.
Venlafaxine The metabolism of Fluvastatin can be decreased when combined with Venlafaxine.
Clobazam The serum concentration of Fluvastatin can be increased when it is combined with Clobazam.
Duloxetine The metabolism of Fluvastatin can be decreased when combined with Duloxetine.
Chlorpromazine The metabolism of Fluvastatin can be decreased when combined with Chlorpromazine.
Perhexiline The metabolism of Fluvastatin can be decreased when combined with Perhexiline.
Primaquine The metabolism of Fluvastatin can be decreased when combined with Primaquine.
Panobinostat The metabolism of Fluvastatin can be decreased when combined with Panobinostat.
Vilazodone The metabolism of Fluvastatin can be decreased when combined with Vilazodone.
Lumefantrine The metabolism of Fluvastatin can be decreased when combined with Lumefantrine.
Manidipine The metabolism of Fluvastatin can be decreased when combined with Manidipine.
Rolapitant The metabolism of Fluvastatin can be decreased when combined with Rolapitant.
Asunaprevir The metabolism of Fluvastatin can be decreased when combined with Asunaprevir.
Desipramine The metabolism of Fluvastatin can be decreased when combined with Desipramine.
Dosulepin The metabolism of Fluvastatin can be decreased when combined with Dosulepin.
Lorcaserin The metabolism of Fluvastatin can be decreased when combined with Lorcaserin.
Berotralstat The metabolism of Fluvastatin can be decreased when combined with Berotralstat.
Thioridazine The metabolism of Fluvastatin can be decreased when combined with Thioridazine.
Paroxetine The metabolism of Fluvastatin can be decreased when combined with Paroxetine.
Cinacalcet The metabolism of Fluvastatin can be decreased when combined with Cinacalcet.

Target Protein

3-hydroxy-3-methylglutaryl-coenzyme A reductase HMGCR
Histone deacetylase 2 HDAC2

Referensi & Sumber

Synthesis reference: Gustavo Frenkel, Eyal Gilboa, "Process for the preparation of fluvastatin sodium crystal form XIV." U.S. Patent US20050119342, issued June 02, 2005.
Artikel (PubMed)
  • PMID: 19663817
    Toda T, Eliasson E, Ask B, Inotsume N, Rane A: Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):327-32. doi: 10.1111/j.1742-7843.2009.00453.x. Epub 2009 Aug 6.

Contoh Produk & Brand

Produk: 30 • International brands: 2
Produk
  • Fluvastatin
    Capsule • 20 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin
    Capsule • 40 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin
    Capsule • 40 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin
    Capsule • 20 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin
    Capsule • 40 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin Sodium
    Capsule • 40 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin Sodium
    Capsule • 20 mg/1 • Oral • US • Generic • Approved
  • Fluvastatin Sodium
    Tablet, film coated, extended release • 80 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 30 produk.
International Brands
  • Canef — AstraZeneca
  • Cranoc — Astellas

Sekuens Gen/Protein (FASTA)

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