Full Prescribing Info
Rosuvastatin calcium.
Each Film-Coated Tablet contains: Rosuvastatin calcium 10 mg and 20 mg, respectively.
Pharmacology: Rosuvastatin is a hypolipidaemic agent; it is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate-determining enzyme for cholesterol synthesis. HMG-CoA reductase inhibitors (sometimes called "statins") reduce total cholesterol, low-density lipoprotein (LDL)-cholesterol and very-low-density lipoprotein (VLDL)-cholesterol concentrations in plasma. They also tend to reduce triglycerides and to increase high-density lipoprotein (HDL)-cholesterol concentrations. They are considered to exert their hypocholesterolaemic action by stimulating an increase in LDL-receptors on hepatocyte membranes thereby increasing the clearance of LDL from the circulation.
Pharmacokinetics: Rosuvastatin is absorbed from the gastrointestinal tract and is hydrolyzed to its active ß-hydroxyacid form. Other active metabolites have been detected and a number of inactive metabolites are also formed. Rosuvastatin undergoes extensive first-pass metabolism in the liver, its primary site of action. Less than 5% of the oral dose have been reported to reach the circulation as active metabolites. Both Rosuvastatin and its ß-hydroxyacid metabolites are about 95% bound to plasma proteins. It is mainly excreted in the feces via the bile as metabolites. About 10% to 15% is recovered in the urine, mainly in inactive forms. The half-life of the active metabolite is 1.9 hours.
Used to reduce LDL-cholesterol, apolipoprotein B, and triglycerides, and to increase HDL-cholesterol in the management of hyperlipidaemias, including primary hypercholesterolaemia (type IIa), mixed dyslipidaemia (type IIb), and hypertriglyceridaemia (type IV), as well as in patients with homozygous familial hypercholesterolaemia. It is also used to reduce the progression of atherosclerosis.
Dosage/Direction for Use
Rosuvastatin is given in an initial dose of 5 to 10 mg once daily, at night, depending on plasma-cholesterol concentrations, cardiovascular risk factors, and risk factor for adverse effects, or as prescribed by the physician. The maintenance dose ranges from 5 to 40 mg once daily, although the 40-mg dose is reserved for patients with high cardiovascular risk who do not achieve their target cholesterol concentration at lower doses and who do not have risk factors for adverse effects.
There is no specific treatment in the event of overdose. In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Haemodialysis is unlikely to be of benefit.
Rosuvastatin is contraindicated in patients with active liver disease, including unexplained, persistent elevations of hepatic aminotransferases. It is also contraindicated in pregnant patients as suppression of cholesterol biosynthesis could cause fetal harm.
Special Precautions
Rosuvastatin should not be given to patients with acute liver disease or unexplained persistent raised serum-aminotransferase concentrations. It should be avoided during pregnancy since there is a possibility that it could interfere with fetal sterol synthesis; there have been a few reports of congenital abnormalities associate with HMG-CoA reductase inhibitors. It should be discontinued if marked increases in serum-aminotransferase or creatinine-phosphokinase concentrations occur.
Use In Pregnancy & Lactation
The safety of Rosuvastatin during pregnancy and whilst breast-feeding has not been established. Women of childbearing potential should use appropriate contraceptive measures.
Adverse Reactions
The most common adverse effects of therapy with Rosuvastatin and other HMG-CoA reductase inhibitors are gastrointestinal disturbances. Other adverse effects reported include headache, skin rashes, dizziness, blurred vision and dysgeusia. Reversible increases in serum-aminotransferase concentrations may occur and liver function should be monitored. Myopathy, characterized by myalgia and muscle weakness and associated with increased creatinine phosphokinase concentrations, has been reported, especially in patients taking Rosuvastatin concurrently with immunosuppressive drugs, fibric acid derivatives or nicotinic acid. Rarely, rhabdomyolysis with acute renal failure may develop.
Drug Interactions
The most serious consequence of drug interactions with rosuvastatin and other statins is the development of myopathy or rhabdomyolysis. Drugs that can cause myopathy when given alone increase the risk of myopathy with all statins; these drugs include fibric acid derivatives (fibrates or gemfibrozil), and nicotinic acid. Rosuvastatin undergoes limited metabolism, principally by the cytochrome P450 isoenzyme CYP2C9, and may not have the same interactions with enzyme inhibitors as simvastatin. However, increased plasma-rosuvastatin concentrations have been reported with ciclosporin, HIV-protease inhibitors, and to a lesser extent, with gemfibrozil, and such combinations should be avoided. If they must be given together, lower doses of rosuvastatin should be used.
Store at temperatures not exceeding 30°C.
MIMS Class
Dyslipidaemic Agents
ATC Classification
C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
FC tab 10 mg x 30's. 20 mg x 30's.
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