ROSUVASTATIN LUPIN

What it is

Rosuvastatin Lupin contains rosuvastatin calcium in strengths of 5 mg, 10 mg, 20 mg and 40 mg. Rosuvastatin calcium is a HMG-CoA reductase inhibitor for the treatment of dyslipidaemia. It is a fully synthetic competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol.

Approved indications

— Reduction of the risk of nonfatal myocardial infarction in men aged 50 years and older and women aged 60 years and older with no clinically evident cardiovascular disease but with at least two conventional risk factors for cardiovascular disease. — Reduction of the risk of nonfatal stroke in men aged 50 years and older and women aged 60 years and older with no clinically evident cardiovascular disease but with at least two conventional risk factors for cardiovascular disease. — Reduction of the risk of coronary artery revascularisation procedures in men aged 50 years and older and women aged 60 years and older with no clinically evident cardiovascular disease but with at least two conventional risk factors for cardiovascular disease. — Treatment of hypercholesterolaemia, including familial hypercholesterolaemia.

Dosing overview

The recommended starting dose for hypercholesterolaemia is 5 mg or 10 mg once per day in both statin naïve patients and in those switched from another HMG-CoA reductase inhibitor. A dose adjustment can be made after 4 weeks of therapy where necessary. The usual maximum dose is 20 mg once per day. A dose of 40 mg once per day should only be considered in patients who are still at high cardiovascular risk after their response to a dose of 20 mg once per day is assessed, which may particularly apply to patients with familial hypercholesterolaemia. For cardiovascular event prevention, a dose of 20 mg once daily has been found to reduce the risk of major cardiovascular events.

Key safety warnings

Patients with active liver disease including unexplained, persistent elevations of serum transaminases and any serum transaminase elevation exceeding 3 times the upper limit of normal are contraindicated. Liver function tests should be performed before initiation of treatment and periodically thereafter. Patients who develop increased transaminase levels should be monitored until the abnormalities have resolved. Should an increase in ALT or AST of greater than 3 times the upper limit of normal persist, reduction of dose or withdrawal of rosuvastatin is recommended. Rare cases of rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with rosuvastatin and with other drugs in this class. Factors that may predispose patients to myopathy with HMG-CoA reductase inhibitors include advanced age (≥65 years), hypothyroidism, and renal insufficiency. Patients should be advised to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. Rosuvastatin therapy should be discontinued if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected. Fusidic acid must not be co-administered with statins. There have been reports of rhabdomyolysis (including some fatalities) in patients receiving this combination.

Contraindications

Known hypersensitivity to any of the ingredients. Active liver disease including unexplained, persistent elevations of serum transaminases and any serum transaminase elevation exceeding 3 times the upper limit of normal. <cite index index="1-50">Use is contraindicated during pregnancy, in nursing mothers and in women of childbearing potential, unless they are taking adequate contraceptive precautions.</cite> Concomitant use of fusidic acid. The 40 mg dose is contraindicated in patients with predisposing factors for myopathy or rhabdomyolysis, including hypothyroidism, personal or family history of hereditary muscular disorders, previous history of muscular toxicity with another HMG-CoA reductase inhibitor or fibrate, alcohol abuse, severe renal impairment (creatinine clearance less than 30 mL per minute), Asian patients, and concomitant use of fibrates.

Regulatory history

Rosuvastatin Lupin 5 mg, 10 mg, 20 mg and 40 mg tablets were first listed on the Australian Register of Therapeutic Goods on 1 October 2020.