Drug Class Description
HMG-CoA reductase inhibitors
Generic Name
Rosuvastatin (as Rosuvastatin Calcium)
Drug Description
Each tablet contains either 5 mg, 10 mg, 20 mg or 40 mg rosuvastatin (as rosuvastatin calcium). Each 5 mg tablet contains 94.88 mg lactose monohydrate.Each 10 mg tablet contains 91.3 mg lactose monohydrate.Each 20 mg tablet contains 182.6 mg lactose monohydrate.Each 40 mg tablet contains 168.32 mg lactose monohydrate.
Presentation
Film-coated tablet.5 mg tablet:Round, yellow coloured tablets, intagliated with 'ZD4522' and '5' on one side and plain on the reverse.10 mg tablet:Round, pink coloured tablets, intagliated with 'ZD4522' and '10' on one side and plain on the reverse.20 mg tablet:Round, pink coloured tablets, intagliated with 'ZD4522' and '20' on one side and plain on the reverse.40 mg tablet:Oval, pink coloured tablets, intagliated with 'ZD4522' on one side and '40' on the reverse.
Indications
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.
Adult Dosage
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.
The recommended start dose is 5 mg or 10 mg orally once daily in both statin naïve or patients switched from another HMG CoA reductase inhibitor. 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 below). A dose adjustment to the next dose level can be made after 4 weeks, if necessary. In light of the increased reporting rate of adverse reactions with the 40 mg dose compared to lower doses, 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. Specialist supervision is recommended when the 40 mg dose is initiated.
Crestor may be given at any time of day, with or without food.
Paediatric use
Safety and efficacy have not been established in children. Paediatric experience is limited to a small number of children (aged 8 years or above) with homozygous familial hypercholesterolaemia. Therefore, Crestor is not recommended for paediatric use at this time.
Use in the elderly
A start dose of 5 mg is recommended in patients >70 years. No other dose adjustment is necessary in relation to age.
Dosage in patients with renal insufficiency
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 of <60 ml/min). The 40 mg dose is contraindicated in patients with moderate renal impairment. The use of Crestor in patients with severe renal impairment is contraindicated for all doses.
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. Crestor is contraindicated in patients with active liver disease.
Race
Increased systemic exposure has been seen in Asian subjects. The recommended start dose is 5 mg for patients of Asian ancestry. The 40 mg dose is contraindicated in these patients.
Dosage in patients with pre-disposing factors to myopathy
The recommended start dose is 5 mg in patients with predisposing factors to myopathy.
The 40 mg dose is contraindicated in some of these patients.
Child Dosage
Safety and efficacy have not been established in children. Paediatric experience is limited to a small number of children (aged 8 years or above) with homozygous familial hypercholesterolaemia. Therefore, Crestor is not recommended for paediatric use at this time.
Elderly Dosage
A start dose of 5 mg is recommended in patients>70 years (See Special Precautions). No other dose adjustment is necessary in relation to age.
Contra Indications
Crestor is contraindicated:- in patients with hypersensitivity to rosuvastatin or to any of the excipients.- in patients with active liver disease including unexplained, persistent elevations of serum transaminases and any serum transaminase elevation exceeding 3 x the upper limit of normal (ULN).- in patients with severe renal impairment (creatinine clearance <30 ml/min).- in patients with myopathy.- in patients receiving concomitant ciclosporin.- during pregnancy and lactation and in women of childbearing potential not using appropriate contraceptive measures.The 40 mg dose is contraindicated in patients with pre-disposing factors for myopathy/rhabdomyolysis. Such factors include:- moderate renal impairment (creatinine clearance < 60 ml/min)- hypothyroidism - personal or family history of hereditary muscular disorders- previous history of muscular toxicity with another HMG-CoA reductase inhibitor or fibrate- alcohol abuse- situations where an increase in plasma levels may occur - Asian patients- concomitant use of fibrates.(See Special Precautions and Interactions)
Special Precautions
Renal Effects
