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10 mg: Rosuvastatin, a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor (or statin), is a lipid regulating drug with actions on plasma lipids similar to those of simvastatin (p.1394). It is used to reduce LDL cholesterol, apolipoprotein B, and triglycerides, and to increase HDL-cholesterol in the management of hyperlipidaemias, including primary hypercholesterolemia (type IIa), mixed dyslipidemia (type IIb), and hypertriglyceridaemia (type IV), as well as in patients with homozygous familial hypercholesterolemia. It is also used to reduce the progression of atherosclerosis.
Rosuvastatin is given orally as the calcium salt, although doses are expressed in terms of the base; 10.4 mg of rosuvastatin calcium is equivalent to about 10 mg of base.
The usual initial dose of rosuvastatin is 5 to 10 mg once daily, depending on plasma-cholesterol concentrations, cardiovascular risk factors, and risk factors for adverse effects. 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. Specific dosage recommendations vary; for dosage in renal impairment, see following text.
UK licensed product information recommends an initial dose of 5 to 10 mg once daily; elderly patients, Asians, and those at risk of myopathy should be given the 5 mg dose. The dose may be increased at intervals at 4 weeks, if necessary, to usual maximum of 20 mg once daily. A higher dose of 40 mg once daily may be given under specialist supervision in severe hypercholesterolemia, but should not be given to patients at high risk of myopathy, including those receiving fibrates, and Asian patients; use with ciclosporin is contraindicated.
US licensed product information recommends a usual initial dose of 10 mg once daily. However, a lower initial dose of 5 mg once daily may be adequate and is recommended for patients at risk of myopathy, including Asian patients; patients with marked hypercholesterolemia, such as those with homozygous familial hypercholesterolemia, may be started on 20 mg once daily. The dose should be adjusted after 2 to 4 weeks, to a usual maximum 20 mg once daily; a dose of 40 mg once daily may be necessary in some patients. Patients receiving ciclosporin may be given a maximum of 5 mg once daily, and in those receiving gemfibrozil or ritonavir-boosted lopinavir the maximum dose is 10 mg once daily; dosage increases should be made with caution in Asian patients.
Or as prescribed by the physician.
20 mg: Before treatment initiation, the patient should be placed on a standard cholesterol-lowering diet that should continue during treatment. The dose should be individualised according to the goal of therapy and patient response, using current consensus guidelines.
Rosuvastatin may be given at any time of day, with or without food.
Treatment of hypercholesterolaemia: The recommended start dose is 5 or 10 mg orally once daily in both statin naïve and patients switched from another HMG-CoA reductase inhibitors. The choice of start dose should take into account the individual patient's cholesterol level and future cardiovascular risk as well as the potential risk for adverse reactions (see as follows). A dose adjustment to the next dose level can be made after 4 weeks, if necessary (see Pharmacology: Pharmacodynamics under Actions).
In light of the increased reporting rate of adverse reactions with the 40 mg dose compared to lower doses (see Adverse Reactions), a final titration to the maximum dose of 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 (see Precautions).
Specialist supervision is recommended when the 40 mg dose is initiated.
Prevention of cardiovascular events: In the cardiovascular events risk reduction study, the dose used was 20 mg daily (see Pharmacology: Pharmacodynamics under Actions).
Pediatric population: Pediatric use should only be carried out by specialists.
Children and adolescents 6 to 17 years of age (Tanner Stage <II-V): In children and adolescents with heterozygous familial hypercholesterolaemia, the usual start dose is 5 mg daily.
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.
Titration should be conducted according to the individual response and tolerability in paediatric patients, as recommended by the paediatric treatment recommendations (see Precautions).
Children and adolescents should be placed on standard cholesterol-lowering diet before rosuvastatin treatment initiation; this diet should be continued during rosuvastatin treatment.
Experience in children with homozygous familial hypercholesterolaemia is limited to a small number of children aged between 8 and 17 years.
The 40 mg tablet is not suitable for use in paediatric patients.
Children younger than 6 years: The safety and efficacy of use in children younger than 6 years has not been studied. Therefore, rosuvastatin is not recommended for use in children younger than 6 years.
Elderly: A start does of 5 mg is recommended in patients >70 years (see Precautions). No other dose adjustment is necessary in relation to age.
Renal impairment: No dose adjustment is necessary in patients with mild to moderate renal impairment.
The recommended start dose is 5 mg in patients with moderate renal impairment (creatinine clearance <60 mL/min). The 40 mg dose is contraindicated in patients with moderate renal impairment. The use of rosuvastatin in patients with severe renal impairment is contraindicated for all doses (see Contraindications and Pharmacology: Pharmacokinetics under Actions).
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 (see Pharmacology: Pharmacokinetics under Actions). In these patients, an assessment of renal function should be considered (see Precautions). There is no experience in subjects with Child-Pugh scores above 9.
Rosuvastatin is contraindicated in patients with active liver disease (see Contraindications).
Race: Increased systemic exposure has been seen in Asian subjects (see Contraindications, Precautions, and Pharmacology: Pharmacokinetics under Actions). The recommended start dose is 5 mg for patients of Asian ancestry. The 40 mg dose is contraindicated in these patients.
Genetic polymorphism: Specific types of genetic polymorphism are known that can lead to increased rosuvastatin exposure (see Pharmacology: Pharmacokinetics under Actions). For patients who are known to have such specific types of polymorphisms, a lower daily dose of rosuvastatin is recommended.
Patients with predisposing factors to myopathy: The recommended start dose is 5 mg in patients with predisposing factors to myopathy (see Precautions).
The 40 mg dose is contraindicated in some of these patients (see Contraindications).
Concomitant therapy: Rosuvastatin is a substrate of various transporter proteins (e.g. OATP1B1 and BCRP). The risk of myopathy (including rhabdomyolysis) is increased when rosuvastatin is administered concomitantly with certain medicinal products that may increase the plasma concentration of rosuvastatin due to interactions with these transporter proteins (e.g. ciclosporin and certain protease inhibitors including combinations of ritonavir with atazanavir, lopinavir, and/or tipranavir; see Precautions and Interactions). Whenever possible, alternative medicinal products should be considered, and if necessary, consider temporarily discontinuing rosuvastatin therapy. In situations where co-administration of these medicinal products with rosuvastatin is unavoidable, the benefit and risk of concurrent treatment and rosuvastatin dosing adjustments should be carefully considered (see Interactions).
