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Rosuvastatin

Description Indications and Usage Mechanisms of Action Pharmacokinetics Drug Interactions Adverse Effects References
Rosuvastatin
Rosuvastatin structure
CAS No.
287714-41-4
Chemical Name:
Rosuvastatin
Synonyms
CS-111;Rosuvastatin;Rosuvastatin Acid;Rosuvastatin USP/EP/BP;ROSUVASTATIN (ZD 4522);Rosuvastatin Impurity 21;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;(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid;(3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-MethylMethanesulfonaMido)-6-(propan-2-yl)pyriMidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
CBNumber:
CB8793779
Molecular Formula:
C22H28FN3O6S
Formula Weight:
481.54
MOL File:
287714-41-4.mol

Rosuvastatin Properties

Melting point:
161.9 °C
Boiling point:
745.6±70.0 °C(Predicted)
Density 
1.368±0.06 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
pka
4.25±0.10(Predicted)
CAS DataBase Reference
287714-41-4(CAS DataBase Reference)
FDA UNII
413KH5ZJ73
EPA Substance Registry System
6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, (3R,5S,6E)- (287714-41-4)

Rosuvastatin price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 12029 Rosuvastatin ≥98% 287714-41-4 5mg $44 2021-03-22 Buy
Cayman Chemical 12029 Rosuvastatin ≥98% 287714-41-4 10mg $79 2021-03-22 Buy
Cayman Chemical 12029 Rosuvastatin ≥98% 287714-41-4 50mg $264 2021-03-22 Buy
Cayman Chemical 12029 Rosuvastatin ≥98% 287714-41-4 100mg $440 2021-03-22 Buy

Rosuvastatin Chemical Properties,Uses,Production

Description

Known 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 Usage

Rosuvastatin 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 Action

Rosuvastatin 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.

Pharmacokinetics

Large 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.

References

https://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

Uses

Rosuvastatin Calcium is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.

brand name

Crestor (AstraZeneca).

General Description

Rosuvastatin, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-(methyl-methylsulfonyl-amino)-pyrimidin-5-yl]-3,5-dihydroxy-hept-6-enoic acid (Crestor), is oneof the more recently introduced statins in the United States.As with all statins, there is a concern of rhabdomyolysis andas such, the FDA has mandated that a warning about thisside effect, as well as a kidney toxicity warning, be added tothe product label (http://www.fda.gov/CDER/Drug/advisory/crestor_3_2005.htm). This should not come as a surprisebecause of the relationship in the chemical architectureto cerivastatin, which was withdrawn from the market as aresult of its adverse side effects.

Rosuvastatin Preparation Products And Raw materials

Raw materials

Preparation Products


Rosuvastatin Suppliers

Global( 158)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20010 60
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Shanghai Zheyan Biotech Co., Ltd.
18017610038
zheyansh@163.com CHINA 3623 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29960 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 linda@hubeijusheng.com CHINA 28229 58
BOC Sciences
1-631-485-4226
1-631-614-7828 inquiry@bocsci.com United States 19753 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58
CONIER CHEM AND PHARMA LIMITED
86-18523575427
sales@conier.com CHINA 47496 58
Shaanxi Dideu Medichem Co. Ltd
15336106720
029-88380327 1017@dideu.com CHINA 3979 58
Zhuozhou Wenxi import and Export Co., Ltd
+8613111626072 (WhatsApp)
Wechat: +8613111626072 Wickr me: waynehu zzwenxi@126.com CHINA 13187 58

Related Qustion

  • Q:What is rosuvastatin?
  • A:Rosuvastatin is a prescription drug. It comes in the form of a tablet you take by mouth.Rosuvastatin is available as the brand....
  • Oct 10,2019

View Lastest Price from Rosuvastatin manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-10-21 Rosuvastatin
287714-41-4
US $10.00 / ASSAYS 1ASSAYS 99.9% 8000KGS/MONTH Handan Tongyi New Material Technology Co., Ltd
2021-10-20 Rosuvastatin
287714-41-4
US $10.00 / KG 100g 99% 2000MT/Month Wuhan wingroup Pharmaceutical Co., Ltd
2021-08-31 Rosuvastatin
287714-41-4
US $10.00 / Kg/Bag 1Kg/Bag 99%min 5000 Wuhan Monad Medicine Tech Co.,LTD

287714-41-4(Rosuvastatin)Related Search:


  • 7-[4-(4-Fluorophenyl)-6-(1-methylethyl)-2-(methyl-methylsulfonyl-amino)-pyrimidin-5-yl]-3,5-dihydroxy-hept-6-enoic acid
  • Rosuvastatin Acid
  • ROSUVASTATIN-D3 SODIUM SALT
  • (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
  • R-2: TERT-BUTYL-(+) 7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-(N-METHYLSULFONYLAMINO) PYRIMIDINE-5-YL]-(3R, 5S)-DIOXANE-(E)-6-HEPTENATE
  • Rosuvastatin Impurity 21
  • CS-111
  • ROSUVASTATIN (ZD 4522)
  • 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, (3R,5S,6E)-
  • Rosuvastatin USP/EP/BP
  • Rosuvastatin
  • 287714-41-4
  • C22H24D3FN3NaO6S
  • C22H28FN3O6S
  • C22H24FN3O6SD3Na
  • Isotopically Labeled Pharmaceutical Reference Standard
  • API
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