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QuickView for Rosuvastatin (compound)

Name: rosuvastatin
PubChem Compound ID: 10814617
Molecular formula: C30H22Cl2N2
Molecular weight: 481.415 g/mol
Name: rosuvastatin
Name (isomeric): DB01098
Drug Type: small molecule
Rosuvastatin calcium; ZD-4522
Brand: Rosvel, Rovartal, Rosimol, Visacor, Cirantan, Crestor, Rosedex, Rosuvast, Vivacor, Astende, Rosustatin, Provisacor, Cresadex, Razel, Rosumed, Rosuvas, Sinlip, Simestat
Category: HMG-CoA Reductase Inhibitors, Anticholesteremic Agents, Hydroxymethylglutaryl-CoA Reductase Inhibitors
CAS number: 287714-41-4
Indication: Used as an adjunct to dietary therapy to treat primary hypercholesterolemia (heterozygous familial and nonfamilial), mixed dyslipidemia and hypertriglyceridemia. Also indicated for homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering therapies or when other such therapies are not available.
Rosuvastatin is a synthetic, enantiomerically pure antilipemic agent. It is used to lower total cholesterol, low density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apoB), non-high density lipoprotein-cholesterol (non-HDL-C), and trigleride (TG) plasma concentrations while increasing HDL-C concentrations. High LDL-C, low HDL-C and high TG co...
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Mechanism of Action:
Rosuvastatin is a competitive inhibitor of HMG-CoA reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Rosuvastatin acts primarily in the liver. Decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low density lipoprotein (LDL) recepto...
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Absorption: Bioavailability is approximately 20%
Protein binding: 90% bound to plasma proteins (mostly albumin)
Biotransformation: Not extensively metabolized. Only ~10% is excreted as metabolite. Cytochrome P450 (CYP) 2C9 is primarily responsible for the formation of rosuvastatin's major metabolite, N-desmethylrosuvastatin. N-desmethylrosuvastatin has approximately 50% of the pharmacological activity of its parent compound in vitro. Rosuvastatin accounts for greater than 87% of the pharmacologic action. Inhibitors of CYP2C9 increase the AUC by less than 2-fold. This interaction does not appear to be clinically significant.
Route of elimination: Rosuvastatin is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as metabolite. Following oral administration, rosuvastatin and its metabolites are primarily excreted in the feces (90%).
Half Life: 19 hours
Toxicity: Generally well-tolerated. Side effects may include myalgia, constipation, asthenia, abdominal pain, and nausea. Other possible side effects include myotoxicity (myopathy, myositis, rhabdomyolysis) and hepatotoxicity. To avoid toxicity in Asian patients, lower doses should be considered. Pharmacokinetic studies show an approximately two-fold increase in peak plasma concentration and AUC in Asian patients (Philippino, Chinese, Japanese, Korean, Vietnamese, or Asian-Indian descent) compared to Caucasians patients.
Affected organisms: Humans and other mammals
Drug interaction:
CyclosporineCyclosporine may increase the serum concentration of rosuvastatin. Limit rosuvastatin dosing to 5 mg/day and monitor for changes in the therapeutic and adverse effects of rosuvastatin if cyclosporine is initiated, discontinued or dose changed.
ColchicineIncreased risk of rhabdomyolysis with this combination
MagnesiumMagnesium-containing antacids may decrease the absorption of rosuvastatin.
GemfibrozilGemfibrozil may increase the therapeutic and toxic effects of rosuvastatin. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of rosuvastatin if gemfibrozil is initiated, discontinued or dose changed.
FenofibrateMay cause additive myotoxicity. Monitor for symptoms of muscle toxicity during concomitant therapy.
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