ChemicalBook > Product Catalog >API >Circulatory system drugs >Anti-atherosclerotic Drugs >Rosuvastatin

Rosuvastatin

Rosuvastatin Suppliers list
Company Name: Capot Chemical Co.,Ltd.
Tel: +86 (0)571-855 867 18
Email: sales@capotchem.com
Products Intro: Product Name:Rosuvastatin
CAS:287714-41-4
Purity:98% (Min,HPLC) Package:100g;1kg;5kg,10kg,25kg,50kg
Company Name: JIANGXI AIFEIMU TECHNOLOGY CO.,LTD  Gold
Tel:+86-570-6040288, 6040289
Email:sales@afmpharm.com
Products Intro:
Company Name: Capot Chemical Co., Ltd  
Tel:+86 (0) 571 85 58 67 18
Email:sales@capotchem.com
Products Intro:Product Name:Rosuvastatin
CAS:287714-41-4
Purity:98% Package:1G;5G;10G;25G Remarks:Cat No.:16072
Company Name: Chemfun Medical Technology(Shanghai) Co., Ltd.  
Tel:021-67220633 & 021-37212706
Email:chemfun@chemfun.net
Products Intro:Product Name:(3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-MethylMethanesulfonaMido)-6-(propan-2-yl)pyriMidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
CAS:287714-41-4
Purity:99% Package:5KG;1KG
Company Name: LGM Pharma  
Tel:1-(800)-881-8210
Email:inquiries@lgmpharma.com
Products Intro:Product Name:Rosuvastatin
CAS:287714-41-4
Purity:Typically NLT 98%
Rosuvastatin Basic information
Description Indications and Usage Mechanisms of Action Pharmacokinetics Drug Interactions Adverse Effects References
Product Name:Rosuvastatin
Synonyms:ROSUVASTATIN-D3 SODIUM SALT;7-[4-(4-Fluorophenyl)-6-(1-methylethyl)-2-(methyl-methylsulfonyl-amino)-pyrimidin-5-yl]-3,5-dihydroxy-hept-6-enoic acid;Rosuvastatin;Rosuvastatin Acid;(3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-MethylMethanesulfonaMido)-6-(propan-2-yl)pyriMidin-5-yl]-3,5-dihydroxyhept-6-enoic acid;(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid
CAS:287714-41-4
MF:C22H24D3FN3NaO6S
MW:481.54
EINECS:
Product Categories:API;Isotopically Labeled Pharmaceutical Reference Standard
Mol File:287714-41-4.mol
Rosuvastatin Structure
Rosuvastatin Chemical Properties
CAS DataBase Reference287714-41-4(CAS DataBase Reference)
Safety Information
Hazardous Substances Data287714-41-4(Hazardous Substances Data)
MSDS Information
Rosuvastatin Usage And Synthesis
DescriptionKnown as an antilipemic agent, rosuvastatin belongs to the class of medications called statins, which is primarily used in the treatment of dyslipidemia, including high cholesterol and related conditions. It functions by blocking the enzyme that helps make cholesterol in the body, which is effective to improve cholesterol levels by reducing blood total cholesterol and triglyceride levels while raising the good cholesterol, HDL cholesterol levels in combination with a healthy diet and exercise program. It is also applied to treat people with certain inherited cholesterol disorders. Besides, since the high level of cholesterol is related to angiocardiopathy, rosuvastatin is beneficial to prevent people from cardiovascular diseases, which is used to reduce the risk of heart attacks, stroke, and angioplasty for people who have at least 2 risk factors for cardiovascular disease.
Indications and UsageRosuvastatin is a drug against hyperlipidemia, a HMG-CoA reductase inhibitor, successfully developed by British AstraZeneca. Applicable to treat a variety of lipid abnormalities, including primary hypercholesterolemia, mixed lipid abnormalities, simple hypertriglyceridemia, and senile coronary heart disease complicated by hyperlipidemia. Rosuvastatin is currently the statin with the strongest and most comprehensive lipid-lowering effect on the market, reducing LDL cholesterol and improve HDL function better than the world-recognized leader atorvastatin, and with better tolerability, fewer side effects, and unique pharmacokinetic effects.
Mechanisms of ActionRosuvastatin is a selective inhibitor of methylglutaryl coenzyme A reductase (HMG-CoA). The HMG-CoA reductase inhibitor is a rate-limiting enzyme which transforms 3-hydroxy-3-methylglutaryl coenzyme A into a methylpentate-cholesterol precursors. Its main site of action is the liver, reducing cholesterol in its target organ. It can competitively inhibit HMG-CoA in the liver to better reduce fat. It can also effectively promote the transfer of LDL into cells, thus enhancing the clearance of low-density lipoprotein, effectively reducing it. In addition, it can also inhibit platelet aggregation, reducing the body's inflammatory response, and protecting the function of endothelial cells, effectively stabilizing the plaque of coronary heart disease patients and reducing its effects. It increases the number of liver cell surface LDL receptors, promoting its absorption and catabolism, inhibiting hepatic synthesis of VLDL, thereby reducing the total count of VLDL and LDL particles.
For patients with homozygous and heterozygous familial and nonfamilial hypercholesterolemia or mixed dyslipidemia, it can reduce total cholesterol, LDL-C, ApoB, and non-HDL-C levels. It can also reduce TG levels and increase HDL-C levels. For patients with simple hypertriglyceridemia, Rosuvastatin can reduce total cholesterol, LDL-C, VLDL-C, ApoB, non HDL-C, and TG levels, and increase HDL-C levels.
PharmacokineticsLarge liver uptake of orally administered Rosuvastatin, distribution volume around 134 L, and serum concentration peaks after 3-5 hours. Absolute bioavailability is 20%. Plasma protein binding rate (mainly albumin) is about 90%. Approximately 90% of the dose is excreted from feces (including absorbed and unabsorbed active substance) in the original form, with the rest discharged through urine. About 5% in the urine is in original form. Plasma clearance half-life is approximately 19 hours. Clearance half-life does not increase with dosage. The geometric mean of plasma clearance is about 50L/hour (coefficient of variation is 21.7%). As with other HMG-CoA reductase inhibitors, liver uptake of Rosuvastatin involves membrane transporter OATP-C, which is important for the removal of Rosuvastatin from the liver.
Drug Interactions
  • Cyclosporine: In combined usage, the AUC of Rosuvastatin is 7 times higher than that seen in healthy volunteers (using the same dosage). Co-administration does not affect cyclosporine plasma concentration.
  • Vitamin K antagonists: As with other HMG-CoA reductase inhibitors, starting Rosuvastatin or gradually increasing dosage may increase International Normalized Ratio (INR) in patients simultaneously using vitamin K antagonists (such as Warfarin). Discontinuing use or gradually reducing dosage reduces INR. In this case, proper testing of INR is required.
  • Combined administration of iferrate, fenofibrate, other fibrates, and lipid lowering dosages (≥1g/日) of niacin with HMG-CoA reductase inhibitors increases the risk of myopathy, possibly because their individual administration can also cause myopathy.
  • Antacids: Combined administration with antacids containing aluminum magnesium hydroxide can reduce Rosuvastatin plasma levels by about 50%. This affect may be alleviated if the antacid is administered 2 hours later. The clinical significance of this drug interaction has not yet been studied.
  • Erythromycin: Combined administration reduces AUC (0-t) of Rosuvastatin by 20%, and Cmax by 30%. This interaction may be caused by an increase in gastrointestinal motility caused by erythromycin.
  • Oral contraceptives/Hormone Replacement Therapy (HRT): Administration combined with oral contraceptives increased ethinyl estradiol and norethindrone AUC by 26% and 34% respectively. These plasma concentrations should be considered when choosing dosages of oral contraceptives. There is no pharmacokinetic data for subjects who use this product with HRT, so the presence of similar interactions cannot be ruled out. In clinical trials, however, this combination is widespread and well tolerated.
Adverse Effects
  • Adverse reactions are usually mild and transient. Headaches, dizziness, constipation, nausea, abdominal pain, myalgia, and weakness are frequently observed.
  • Dosage-related elevation of creatine kinase (CK) was observed in patients taking Rosuvastatin; most cases were mild, asymptomatic, and transient. If CK levels increase (>5×ULN), treatment should be discontinued.
  • Effects on the liver: a dose-dependent increase of transaminase was observed in a small number of patients taking Rosuvastatin; most cases were mild, asymptomatic, and transient.
Referenceshttps://en.wikipedia.org/wiki/Rosuvastatin
http://www.medicinenet.com/rosuvastatin/article.htm
http://bodyandhealth.canada.com/drug/getdrug/apo-rosuvastatin
https://www.drugbank.ca/drugs/DB01098
UsesRosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.
Rosuvastatin Preparation Products And Raw materials
Tag:Rosuvastatin(287714-41-4) Related Product Information
Phenylacetone Triphenylphosphine Simvastatin PHENYLSELENOL 1,1,3,3-TETRAMETHYLBUTYL ISOCYANIDE TERT-BUTYL ISOCYANIDE Rosuvastatin Atorvastatin Sulfadiazine Lovastatin Atorvastatin calcium Rosuvastatin calcium Basic Violet 1 Methyl acetate Glycolic acid Methyl Fluorocytosine Paraquat dichloride