Rosuvastatin

Structural formula
General
Non-proprietary name	Rosuvastatin
other names	(3 R , 5 S , 6 E ) -7- [4- (4-fluorophenyl) -2- (methyl-methylsulfonylamino) -6-propan-2-ylpyrimidin-5-yl] -3,5-dihydroxyhept-6 -enic acid ( IUPAC )
Molecular formula	C 22 H 28 FN 3 O 6 S
External identifiers / databases
CAS number 287714-41-4 147098-20-2 (calcium salt) ECHA InfoCard 100.216.011 PubChem 446157 ChemSpider 393589 DrugBank DB01098 Wikidata Q415159
Drug information
ATC code	C10 AA07
Drug class	Statins
Mechanism of action	HMG-CoA reductase - inhibitor
properties
Molar mass	481.54 g · mol -1
Melting point	≥ 155 ° C (calcium salt)
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances danger H and P phrases H: 351-360D-412 P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Rosuvastatin is a drug from the group of statins that is used as a cholesterol-lowering agent in the treatment of lipid metabolism disorders .

Clinical information

Application areas (indications)

Rosuvastatin is a drug from the group of statins and is used to treat primary hypercholesterolemia or mixed dyslipidemia in addition to diet when these and other therapeutic measures, such as additional exercise, do not bring the desired therapeutic success.

Mechanism of action

Rosuvastatin is an inhibitor of HMG-CoA reductase . This enzyme acts as a catalyst in the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate , which is a limiting step in cholesterol synthesis in the liver.

Studies

Safety studies

There are numerous studies on safety. The side effects profile is the same as for the other statins. However, rhabdomyolysis and kidney failure have already been reported at twice the maximum permitted dose of 40 mg .

ASTEROID study

Here the benefit of intensified rosuvastatin therapy at a dose of 40 mg with regard to atherosclerosis was examined. IVU ( intravascular ultrasound ) showed that rosuvastatin could cause regression of coronary plaques of up to 9%. However, this benefit only appeared below an LDL value of 70 mg / dl. This shows that intensified statin therapy can be useful in CHD patients.

AURORA study

( A study Evaluating the U se of R osuvastatin in patients Requiring O Ngoing R enal dialysis: an A ssessment of survival and cardiovascular events) a randomized, double-blind long-term study to evaluate the effect at a dose of 10 mg rosuvastatin regarding mortality and serious cardiovascular events 2775 patients with end-stage renal disease and chronic hemodialysis (started in 2003, as part of the GALAXY program).

COMETS study

The benefits of rosuvastatin were investigated in a prospective study in metabolic syndrome . This is the COMETS study published in 2005 (A COmparative study with rosuvastatin in subjects with METabolic Syndrome). 10 mg rosuvastatin were compared with 10 and 20 mg atorvastatin for the reduction of LDL cholesterol. According to the results, the LDL cholesterol with 10 mg rosuvastatin was reduced by almost 43%, with 10 mg atorvastatin by almost 37%. The comparison of the 20 milligram doses of both statins showed just under 49% and 42.5% in favor of rosuvastatin. There was also a difference in favor of rosuvastatin when “reaching the European LDL target value of less than 100 mg / dl” and with the parameter “percentage HDL increase”.

In 2005, in contrast to simvastatin , pravastatin , fluvastatin and atorvastatin , there were still no long-term studies that would prove a positive benefit in relation to illnesses or deaths beyond a pure lowering of LDL cholesterol as a surrogate parameter .

CORONA study

In 2007, the results of the CORONA study appeared, in which over 5000 heart failure patients were treated with either 10 mg rosuvastatin or placebo daily for one year. For the primary endpoint (cardiovascular death, non-fatal myocardial infarction, stroke) there was no significant difference in the effect between rosuvastatin and placebo administration.

JUPITER study

A study published in the NEJM in 2008 looked at the question of whether people with elevated levels of C-reactive protein (CRP) but normal cholesterol levels could also benefit from statin therapy. Elevated levels of CRP concentration in the blood provide information about the degree of inflammation and are a predictive parameter for cardiovascular risk. As the results of the study show, both the LDL values and the CRP values ​​could be reduced under rosuvastatin.

GISSI-HF study

The GISSI-HF study published in 2008 examined similarly to CORONA 4574 heart failure patients in a comparison between 10 mg rosuvastatin and placebo. The median observation period here was 3.9 years. Again, there was no difference between rosuvastatin and placebo for the combined endpoint of all-cause mortality and hospitalization for cardiovascular reasons. The overall mortality rate was 29% for rosuvastatin and 28% for placebo; the proportion of patients re-hospitalized or death from cardiovascular causes was 57% for rosuvastatin and 56% for placebo.

Finished medicinal products

• AstraZeneca : Crestor (D, A, CH, USA and others), Provisacor (IT), Zuvamor (ZA)

Crestor has been on the market in Austria (since 2003) and Switzerland, and in Germany since 2009.

Web links

• FDA label from Crestor 2010 (PDF; 1.7 MB)

Individual evidence

1. ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals . 14th edition, 2006, p. 1428, ISBN 978-0-911910-00-1 .
2. ↑ There is not yet a harmonized classification for this substance . A labeling of 7- [4- (4-fluorophenyl) -6- (1-methylethyl) -2- (methyl-methylsulfonyl-amino) -pyrimidin-5-yl] -3.5 is shown, which is derived from a self-classification by the distributor -dihydroxy-hept-6-enoic acid in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on July 12, 2020.
3. ↑ A more common dosage for adult humans is 5 to 10 mg per day
4. ↑ Bengt Fellström et al .: Effect of rosuvastatin on outcomes in chronic haemodialysis patients - design and rationale of the AURORA study Curr Control Trials Cardiovasc Med. 2005 May 23; 6 (1): p. 9; PMID 15910680 ; PMC 1175096 (free full text, PDF).
5. ↑ Anton FH Stalenhoef et al .: A CO mparative study with rosuvastatin in subjects with MET abolic syndromes: results of the COMETS study. In: Eur Heart J . 2005 Dec; 26 (24): pp. 2664-2672, PMID 16143705 ( PDF ; 264 kB).
6. ↑ EMEA summary by Crestor, 2005 (PDF; 109 kB).
7. ↑ J. Kjekshus et al., New England Journal of Medicine , November 29, 2007; 357 (22), pp. 2248-2261.
8. Jump up ↑ Paul M Ridker et al .: Rosuvastatin to Prevent Vascular Events in Men and Women with Elevated C-Reactive Protein NEJM November 9, 2008; doi : 10.1056 / NEJMoa0807646 , PMID 18997196 ( PDF ).
9. ^ GISSI-HF Investigators, The Lancet October 4, 2008; 372 (9645): pp. 1231-1239.

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !