Rovas

Rosuvastatin calcium.

ROVAS 10 contains Rosuvastatin calcium equivalent to rosuvastatin 10 mg.
ROVAS 20 contains Rosuvastatin calcium equivalent to rosuvastatin 20 mg.

Pharmacology: Pharmacodynamics: Mechanism of action: Rosuvastatin is a selective, competitive inhibitor of 3-hydroxymethylglutaryl-CoA (HMG-CoA) reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonate (an early and rate-limiting step in cholesterol biosynthesis. Rosuvastatin reduces total and low-density lipoprotein (LDL)-cholesterol, apolipoprotien B (apo B), non-high-density lipoprotein (HDL)-cholesterol, and triglyceride concentrations, and increase HDL cholesterol concentration in patients with primary hyperlipidemia or mixed dyslipidemia.
Pharmacokinetics: Rosuvastatin is incompletely absorbed from the gastrointestinal tract, with an absolute bioavailability of about 20%. Peak plasma concentrations occur 5 hours after an oral dose. It is about 90% bound to plasma proteins. Rosuvastatin is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as metabolite. The major metabolite is N-desmethyl rovastatin, which is formed principally by cytochrome P-450 (CYP) isoenzyme 2C9. Rosuvastatin and its metabolites are mainly eliminated in feces about 90% following oral administration. The elimination half-life of rosuvastatin is about 19 hours.

Prevention of Cardiovascular Events: In adult patients with an increased risk of atherosclerotic cardiovascular disease based on the presence of cardiovascular disease risk markers such as an elevated high sensitivity C-reactive protein (hsCRP) level, age, hypertension, low HDL-C, smoking or a family history of premature coronary heart disease. Rosuvastatin is indicated to reduce total mortality and the risk of major cardiovascular events (cardiovascular death, stroke, myocardial infarction, unstable angina or arterial revasculization).
In adult patients with hypercholesterolaemia: Primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia) or mixed dyslipidaemia (type IIb) as an adjunct to diet when response to diet and other non-pharmacological treatments (e.g. exercise, weight reduction) is inadequate.
Homozygous familial hypercholesterolaemia as an adjunct to diet and other lipid lowering treatments (e.g. LDL apheresis) or if such treatments are not appropriate.
Slow or delay the progression of atherosclerosis.
Children and adolescents 6 to 17 years of age: Rosuvastatin is indicated to reduce the total cholesterol, LDL and Apo B in patients with heterozygous familial hypercholesterolaemia (HeFH).

Recommended Dose: The recommended start dose is 5 or 10 mg once daily in both statin naive patients or patients switched from another HMG CoA reductase inhibitor. The choice of starting dose should take into account the individual patients cholesterol level and future cardiovascular risk as well as the potential risk for adverse reactions. A dose adjustment to 20 mg can be made after 2 to 4 weeks, if necessary. A doubling of the dose to 40 mg should only be considered in patients with severe hypercholesterolaemia at high cardiovascular risk (in particular those with familial hypercholesterolaemia), who do not achieve their treatment goal on 20 mg, and in whom routine follow-up will be performed.
Children and adolescents 6 to 17 years of age: In children 6 to 9 years of age with heterozygous familial hypercholesterolaemia, the usual dose range is 5-10 mg orally once daily. Safety and efficacy of doses greater than 10 mg have not been studied in this population.
In children 10 to 17 years of age with heterozygous familial hypercholesterolaemia, the usual dose range is 5-20 mg orally once daily. Safety and efficacy of doses greater than 20 mg have not been studied in this population.
Use in the elderly: No dose adjustment is necessary.
Dosage in patients with renal insufficiency: No dose adjustment is necessary in patients with mild to moderate renal impairment. The use of Rosuvastatin in patients with severe renal impairment is contraindicated.
Dosage in patients with hepatic impairment: There was no increase in systemic exposure to rosuvastatin in subjects with Child-Pugh scores of 7 or below. However, increased systemic exposure has been observed in subjects with Child-Pugh scores of 8 and 9. In these patients an assessment of renal function should be considered. There is no experience in subjects with Child-Pugh scores above 9. Rosuvastatin is contraindicated in patients with active liver disease.
Mode of Administration: ROVAS is administered orally as single dose at any time of day, with or without food.

Overdose and Treatment: There is no specific treatment in the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Liver function and CK levels should be monitored. Heamodialysis is unlikely to be of benefit.

Rosuvastatin is contraindicated in patients with known hypersensitivity to rosuvastatin or any ingredient in the formulation.
Rosuvastatin is contraindicated in patients with active liver disease including unexplained, persistent elevations in hepatic aminotransferase (transaminase) concentrations.
Rosuvastatin is contraindicated in patients with severe renal impairment (creatinine clearance < 30 ml/min).
Rosuvastatin is contraindicated in patients with myopathy.
Rosuvastatin is contraindicated in patients receiving concomitant cyclosporin.
Rosuvastatin is contraindicated during pregnancy and breastfeeding.

Musculoskeletal effects: Myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported in patients receiving statins, including rosuvastatin.
Rosuvastatin should be used with caution in patients with predisposing factors for myopathy (e.g. advanced age [65 years or older], renal impairment, inadequately treated hypothyroidism).
Hepatic effects: Rosuvastatin should be used with caution in patients with a history of liver disease (e.g., chronic alcoholic liver disease) and/or in patients who consume substantial amounts of alcohol.

Pregnancy: Category X. Contraindicated during pregnancy.
Congenital animals and/or skeletal malformations have occurred in animals. There have been reports of infants with malformations have occurred in animals following in utero exposure to HMG-CoA reductase inhibitors.
Lactation: Rosuvastatin is excreted in breast milk. Due to potential for serious adverse reactions in a nursing infant, use while breastfeeding is contraindicated.

Common: Gastrointestinal: Abdominal pain (2.4%), nausea (2.4% to 6.3%).
Musculoskeletal: Myalgia (1.9% to 12.7%).
Neurologic: Asthenia (0.9% to 4.7%), headache (3.1% to 8.5%).
Serious: Endocrine metabolic: Diabetes mellitus (2.8%), high hemoglobin A1c level, impaired fasting glucose.
Gastrointestinal: Pancreatitis.
Hepatic: Increase liver enzymes (1.1%), liver failure.
Musculoskeletal: Autoimmune necrotizing myopathy, statin-associated (rare), disorder of muscle (less than 1%), rhabdomyolysis, rupture of tendon.
Renal: Acute renal failure, hematuria (less than 2%), proteinuria (1.5%).

Concomitant use of rosuvastatin and an antacid containing aluminium hydroxide and magnesium hydroxide decreased rosuvastatin peak plasma concentration and area under the plasma concentration-time curve (AUC) by 50%. The antacid should be administered at least 2 hours after rosuvastatin.
Concomitant use of rosuvastatin and itraconazole increased rosuvastatin peak plasma concentration and AUC by 1.4-fold.
Concomitant use of rosuvastatin and colchicines increases the risk of myopathy, including rhabdomyolysis.
Concomitant use of rosuvastatin and cyclosporine increases plasma rosuvastatin concentration, which may increase the risk of myopathy.
Concomitant use of rosuvastatin and digoxin increased both peak plasma concentration and AUC of digoxin by 4%.
Concomitant use of rosuvastatin and erythromycin decreased rosuvastatin peak plasma concentration and AUC by 30 and 20%, respectively.
Coadministration of rosuvastatin with gemfibrozil increases the risk of myopathy and/or rhabdomyolysis.
Coadministration of rosuvastatin with oral contraceptives increased the AUC for norgestrel and estradiol by approximately 34% and 26%, respectively.

Store below 30°C.

Dyslipidaemic Agents

C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

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