ROSUSTAD 10 Tablet

Treatment of hypercholesterolaemia

Adults, adolescents and children aged 10 years or older with primary hypercholesterolaemia (type Ⅱa including heterozygous familial hypercholesterolaemia) or mixed dyslipidaemia (typeⅡb) 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.

Dosage and Administration

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 starting dose is 5-10mg orally once daily in both statin naïve or patients switched from another HMG CoA reductase inhibitor. The choice of starting dose should take into account the individual patient’s cholesterol level and future cardiovascular risk as well as the potential risk for adverse reactions. A dose adjustment to the next dose level can be made after 4 weeks, if necessary.

See the package insert about the details below:

- Paediatric population

Paediatric use should only be carried out by specialists.

Children and adolescents 10-17 years of age (boys Tanner StageⅡand above, and girls who are at least 1 year post-menarche)

Children younger than 10 years: Rosuvastatin is not recommended for use in children younger than 10 years.

- Use in elderly

- Dosage in patients with renal insufficiency

- Dosage in patients with hepatic impairment.

- Race

- Patients with hypersensitivity to any of the components of the product.

- Patients with active liver disease including unexplained, persistent elevations of serum transaminases and any serum transaminase elevation exceeding 3the upper limit of normal (ULN).

- Patients with severe renal impairment (creatinine clearance<30mL/min).

- Patients with myopathy.

- Pregnancy and lactation and women of childbearing potential not using appropriate contraceptive measures.

- Immune system disorders

Rare: Hypersensitivity reactions including angioedema.

- Endocrine disorders

Common: Diabetes mellitus.

- Nervous system disorders

Common: Headache, dizziness.

- Gastrointestinal disorders

Common: Constipation, nausea, abdominal pain.

Rare: Pancreatitis.

- Skin and subcutaneous tissue disorders

Uncommon: Pruritus. rash and urticaria

- Musculoskeletal, connective tissue and bone disorders

Common: Myalgia

Rare: Myopathy (including myositis) and rhabdomyolysis

- General disorders

Common: Asthenia

- Renal effects: Proteinuria, detected by dipstick testing and mostly tubular in origin, has been observed in patients treated with rosuvastatin.

proteinuria decreases or disappears spontaneously on continued therapy.

- Skeletal muscle effects: A dose-related in CK levels has been observed in patients taking rosuvastatin. The majority of cases were mild, asymptomatic and transient. If CK levels are elevated, treatment should be discontinued.

- Liver effects: As with other HMG-CoA reductase inhibitors, a dose-related increase in transaminases has been observed in a small number of patients taking rosuvastatin; the majority of cases were mild, asymptomatic and transient.

See the package insert about the details below.

- Ciclosporin

- Vitamin K antagonists

- Ezetimibe

- Gemfibrozil and other lipid-lowering products

- Protease inhibitors

- Antacid

- Erythromycin

- Oral contraceptive/hormone replacement therapy (HRT)

- CYP450 enzymes

Contraindicated. (See the package insert about the details.)

- Renal effects. It is recommended that liver function tests should be performed before the initiation of Rosustad 10, and thereafter when clinically indicated.

- Skeletal muscle effects: Very rare cases of rhabdomyolysis have been reported with the use of ezetimibe in combination with HMG-CoA reductase inhibitors. A pharmacodynamic interaction cannot be excluded and caution should be exercised with their combined use.

- Creatine Kinase measurement:

- Liver effects: Rosuvastatin should be used with caution in patients who consume excessive quantities of alcohol and/or have a history of liver disease. It is recommended that liver function tests be carried out prior to, and 3 months following, the initiation of treatment. Rosuvastatin should be discontinued or the dose reduced if the level of serum transaminases is greater than 3 times the upper limit of normal.

- Race: Pharmacokinetic studies show an increase in exposure in Asian subjects compared with Caucasians.

- Lactose Intolerance: Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

- Interstitial lung disease: Exceptional cases of interstitial lung disease have been reported with some statins, especially with long term therapy. If it is suspected a patient has developed interstitial lung disease, statin therapy should be discontinued.

- Diabetes mellitus: Some evidence suggests that statins as a class raise blood glucose and in some patients, at high risk of future diabetes, may produce a level of hyperglycaemia where formal diabetes care is appropriate. Patients at risk should be monitored both clinically and biochemically according to national guidelines.

There have been rare post marketing reports of cognitive impairment (e.g. memory loss, forgetfulness, amnesia, memory impairment. confusion) associated with statin use. These cognitive issues have been reported for all statins. The reports are generally non serious, and reversible upon statin discontinuation, with variable times to symptoms onset (1 day to years) and symptoms resolution) median of 3 weeks). Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors.

Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor for cholesterol. The primary site of action of rosuvastatin is the liver, the target organ for cholesterol lowering.

Rosuvastatin increases the number of hepatic LDL receptors on the cell-surface, enhancing uptake and catabolism of LDL and it inhibits the hepatic synthesis of VLDL, thereby reducing the total number of VLDL and LDL particles.