Rosuvastatin
- Atc Codes:C10AA07
- CAS Codes:147098-20-2#287714-41-4
- PHARMGKB ID:147098-20-2#287714-41-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Crestor; Belgium: Crestor; Bulgaria: Crestor; Cyprus: Crestor; Czech Republic: Crestor; Denmark: Crestor; Estonia: Crestor; Finland: Crestor; France: Crestor; Germany: Crestor, Rosuvastatin; Greece: Crestor; Hungary: Crestor, Visacor; Ireland: Crestor; Italy: Crestor, Provisacor, Simestat; Latvia: Crestor; Lithuania: Crestor; Luxembourg: Crestor; Malta: Crestor; Netherlands: Cirantan, Crestor, Provisacor, Rosuvastatin; Poland: Crestor; Portugal: Crestor, Visacor; Romania: Crestor; Slovakia: Crestor, Rosucard, Rosuvastatin; Slovenia: Crestor; Spain: Crestor; Sweden: Crestor, Visacor; UK: Crestor.
North America
Canada: Crestor; USA: Crestor.
Latin America
Argentina: Astende, Crestor, Rosedex, Rosimol, Rosustatin, Rosuvast, Rosuvastatina, Rovartal, Sinlip; Brazil: Vivacor; Mexico: Crestor.
Asia
Japan: Crestor.
Drug combinations
Chemistry
Rosuvastatin Calcium: [C~22~H~27~FN~3~O~6~S]~2~Ca. Mw: 1001.14. (1) 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, calcium salt (2:1), (3R,5S,6E)-; (2) [S-[R*,S*-(E)]]-7-[4-(4-Fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-6-heptenoic acid, calcium salt (2:1). CAS-147098-20-2; CAS-287714-41-4 (rosuvastatin)(2000).
Pharmacologic Category
Antilipemic Agents; HMG-CoA Reductase Inhibitors. (ATC-Code: C10AA07).
Mechanism of action
Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, rate-limiting enzyme in cholesterol synthesis. This results in compensatory increase in expression of LDL receptors on hepatocyte membranes and stimulation of LDL catabolism.
Therapeutic use
Used with dietary therapy for hyperlipidemias to reduce elevations in total cholesterol (TC), LDL-C, apolipoprotein B, non HDL-C, and triglycerides in primary hypercholesterolemia (elevations of 1 or more components present in Fredrickson type IIa, IIb, and IV hyperlipidemias). Treatment of primary dysbetalipoproteinemia (Fredrickson type III hyperlipidemia). Treatment of homozygous familial hypercholesterolemia. To slow progression of atherosclerosis as adjunct to TC- and LDL-C-lowering diet.
Pregnancy and lactiation implications
Contraindicated in pregnancy. Administer to women of childbearing potential only when conception highly unlikely. Contraindicated in nursing women.
Unlabeled use
Contraindications
Hypersensitivity to rosuvastatin or any component of the formulation. Active liver disease. Unexplained persistent elevations of serum transaminases (>3 times ULN). Pregnancy. Breast-feeding.
Warnings and precautions
Patients receiving HMG-CoA reductase inhibitors developed rhabdomyolysis with acute renal failure and/or myopathy. Temporarily discontinue for elective major surgery, acute medical or surgical conditions, or in any patient experiencing acute or serious condition predisposing to renal failure (e.g. sepsis, hypotension, trauma, uncontrolled seizures). Use caution in renal impairment, inadequately treated hypothyroidism, and patients taking other drugs associated with myopathy (e.g. colchicine); these patients predisposed to myopathy. Use with caution in patients who consume large amounts of ethanol or have history of liver disease. Cyclosporine, and gemfibrozil significantly increase levels of rosuvastatin. Concomitant use of gemfibrozil not recommended. Lopinavir/ritonavir significantly increases levels of rosuvastatin. Use of niacin may increase risk of myopathy when used with rosuvastatin. Rosuvastatin significantly increases INR in patients on warfarin.