ROVISTA Tablet

Treatment of Hypercholesterolemia

The initial recommended dose: 5-10mg orally once daily. If necessary at intervals of at least 4 weeks to next dose level once daily. When initiating therapy or switching from another HMG-CoA reductase inhibitor therapy, the appropriate starting dose should first be utilized and only then titrated according to the patients response and individualized goal of therapy. After initiation or upon titration of Rovista Tablets, lipid levels should be analyzed within 2-4 weeks and the dosage adjusted accordingly.

Prevention of Cardiovascular Events:

The recommended dose used is 20mg once daily.

Homozygous Familial Hypercholesterolemia:

The recommended starting dose is 20mg once daily. Response to therapy should be estimated from preapheresis LDL-C levels.

Pediatric Population:

Pediatric use should only be carried out by specialists.

Children and Adolescents 10-17 years of age:

Asian Origin:

Renal Insufficiency:

Hepatic Insufficiency:

Elderly:

See the package insert about the details.

- patients with hypersensitivity to rosuvastatin or to any of the excipients.

- 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.

- patients receiving concomitant cyclosporin.

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

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

Common:

Diabetes mellitus, headache, dizziness, constipation, nausea, abdominal pain, myalgia, asthenia.

Uncommon:

Pruritus, rash and urticaria.

Rare:

Pancreatitis, hypersensitivity reactions including angioedema, myopathy, rhabdomyolysis, arthralgia, increased hepatic transaminases.

Laboratory Abnormalities:

Proteinuria has been observed in patients treated with rosuvastatin. This finding was more frequent in patients taking rosuvastatin 40mg, when compared to lower doses of rosuvastatin.

Other abnormal laboratory values reported were elevated creatinine phosphokinase, dose related increase in transaminases, hyperglycemia, glutamyl transpeptidase, alkaline phosphatase, bilirubin and thyroid function abnormalities.

See the package insert about the details below.

Rosuvastatin may result in increase risk of myopathy when co-administered with the following:

- Antibacterials (e.g. Daptomycin)

- Antivirals (e.g. Darunavir, Fosamprenavir, Indinavir, Ritonavir, Saquinavir, Nelfinavir)

- Colchicine

- Fibrates

- Nicotinic acid

- Erythromycin

- Tipranavir, Eltrombopag

- Oestrogen, Progestron

- Cyclosporin

- Gemfibrozil

- In patients taking coumarin anticoagulants

- Antacid suspension containing aluminium and magnesium

- Niacin

Contraindicated.

- Hypothyroidism should be managed adequately before starting treatment with statin.

- Statins should be used with caution in patients with predisposing risk factors for myopathy or rhabdomyolysis. The patients should be advised to report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever.

- It should be used with caution in patients who consume substantial quantities of alcohol and/or have a history of chronic liver disease. It is recommended that liver function tests be performed before and at 12 weeks following both the initiation of therapy and any elevation of dose and periodically thereafter.

- Caution should be exercised if rosuvastatin is administered concomitantly with drugs that may decrease the levels or activity of endogenous steroid hormones such as ketoconazole, spironolactone and cimetidine.

- Rosuvastatin therapy should be withheld temporarily in any patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure, secondary to rhabdomyolysis.

- Dose reduction should be considered for patients on Rosuvastatin therapy with unexplained persistent proteinuria and/or hematuria during routine urinalysis testing.

- Caution should be exercised when rosuvastatin is co-administered with protease inhibitors given in combination with ritonavir.

- Long term use of rosuvastatin therapy may report interstitial Lung Disease, presenting features can include Dyspnoea, non-productive cough and detoriation in general health (fatigue, weight loss and fever). It is advisable that the therapy should be discontinued.

- Patients with fasting glucose 5.6-6.0mmol/L, treatment with rosuvastatin has been associated with an increased risk of diabetes mellitus.

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. In in vivo and in vitro studies, rosuvastatin produces its lipid-modifying effects in two ways. First, it increases the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL. Second, rosuvastatin inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.