Lipiros5 mg

Rosuvastatin calcium is a statin used, as an adjunct to diet, for:

• Primary hyperlipidemia, to reduce elevated LDL-C, total cholesterol, apolipoprotein B, non-HDL-C, and triglycerides, and to increase HDL-C
• Heterozygous familial hypercholesterolemia (HeFH) in adults and children 8 years and older
• Homozygous familial hypercholesterolemia (HoFH) in adults and children 7 years and older, alone or with other lipid-lowering treatments
• Slowing the progression of atherosclerosis, as part of a cholesterol-lowering treatment plan
• Primary prevention of cardiovascular disease in patients without clinically evident coronary heart disease but with an increased risk based on age, hs-CRP, and other risk factors

Contains Lipiros 5 mg as the active ingredient, available as oral tablets in 5 mg, 10 mg, 20 mg, and 40 mg strengths.

Rosuvastatin is a widely used statin medicine, taken to lower LDL ("bad") cholesterol and reduce the risk of heart attack, stroke, and other cardiovascular events, both in patients with established high cholesterol and, in appropriate candidates, as a preventive measure. It works by reducing the liver's own cholesterol production. Like all statins, its main safety concern is a risk of muscle-related side effects (myopathy), which is more likely with certain risk factors, drug interactions, and, notably, in patients of Asian ancestry, who have significantly higher rosuvastatin blood levels than other populations at the same dose and therefore require a lower starting dose.

Therapeutic Class: Lipid-Lowering Agent (Statin)

Rosuvastatin is a substrate of hepatic uptake transporters, including OATP1B1 and BCRP, and pharmacokinetic studies have demonstrated an approximate 2-fold increase in median rosuvastatin exposure in Asian subjects compared with White controls, which is why a lower starting dose (5 mg) is recommended in this population. Certain genetic polymorphisms are also known to significantly increase rosuvastatin exposure, and a lower starting dose is recommended for patients known to have these variants. Chronic alcohol-related liver disease increases rosuvastatin exposure and hepatic injury risk.

• Taken orally, once daily, at any time of day, with or without food
• Take at approximately the same time each day for consistency
• Continue dietary and lifestyle measures alongside this medicine, as part of the overall approach to lowering cholesterol

The following interactions are particularly important, given increased myopathy risk with certain combinations:

• Cyclosporine: significantly increases rosuvastatin exposure; the rosuvastatin dose should not exceed 5 mg once daily if combined.
• Gemfibrozil: significantly increases rosuvastatin exposure and myopathy risk; concomitant use should be avoided if possible, and if necessary, the rosuvastatin dose should not exceed 10 mg once daily.
• Other fibrates, niacin, and colchicine: may independently cause myopathy, and combined use increases the risk of myopathy and rhabdomyolysis.
• Warfarin and other vitamin K antagonists: rosuvastatin can significantly increase INR; obtain an INR before starting rosuvastatin in patients taking these anticoagulants, and monitor regularly during treatment.
• Certain antiviral medicines and darolutamide: require specific rosuvastatin dose caps if combined; discuss all current medicines with your doctor or pharmacist.
• Antacids (aluminium and magnesium hydroxide combinations): can reduce rosuvastatin absorption; separate dosing by at least 2 hours.

Common side effects

• Headache
• Muscle aches (myalgia)
• Nausea, constipation
• Weakness (asthenia)

Serious side effects (require prompt medical attention)

• Myopathy and rhabdomyolysis, including rare reports of immune-mediated necrotizing myopathy (IMNM): unexplained muscle pain, tenderness, or weakness, particularly with fever or unusual fatigue, or dark urine, requires immediate medical attention; discontinue if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected.
• Hepatotoxicity: monitor for signs including yellowing of the skin or eyes, dark urine, or unusual fatigue; liver function testing is performed as clinically indicated.
• Renal effects: proteinuria and haematuria have been observed, generally transient, more frequent with the 40 mg dose; monitor renal function in patients with renal impairment.
• New-onset diabetes mellitus or worsening blood glucose control, a recognized class effect of statins.
• Rare reports of interstitial lung disease with statins generally.

Pregnancy

Rosuvastatin may cause fetal harm, since cholesterol and cholesterol derivatives are essential for normal fetal development; women of childbearing potential should use effective contraception, and rosuvastatin should be discontinued as soon as pregnancy is recognized.

Breastfeeding

Rosuvastatin is present in animal milk and use during breastfeeding is generally not recommended; discuss alternatives with your doctor if breastfeeding is planned.

• Myopathy risk factors: age 65 or older, uncontrolled hypothyroidism, renal impairment, concomitant use of certain interacting drugs, and higher doses all increase myopathy risk; Asian patients may also be at higher risk. Assess these before starting and periodically during treatment.
• Renal impairment: a risk factor for both reduced rosuvastatin clearance and myopathy; monitor and adjust dose as described.
• Hepatic disease and alcohol use: chronic alcohol-related liver disease increases rosuvastatin exposure and hepatic injury risk; use with caution in patients who consume substantial quantities of alcohol.
• Asian ancestry: requires a lower starting dose, given significantly increased rosuvastatin exposure in this population.
• Discuss all other medicines with your doctor or pharmacist before starting, given the significant number of clinically important interactions.

There is no specific antidote or treatment for rosuvastatin overdose; management is generally supportive. Suspected significant overdose should be evaluated by a healthcare professional, with monitoring of liver function and creatine kinase as clinically indicated. Haemodialysis does not significantly enhance rosuvastatin clearance.

Store at controlled room temperature, protected from moisture and light, in the original container.

• Asian patients: Require a lower starting dose (5 mg once daily), given significantly increased rosuvastatin exposure.
• Severe renal impairment (not on haemodialysis): Requires a lower starting dose (5 mg once daily) and a lower maximum dose (10 mg once daily).
• Elderly: Increased risk factor for myopathy; use with caution and appropriate monitoring.
• Children: Established dosing for HeFH (8 years and older) and HoFH (7 years and older); safety and efficacy for primary hyperlipidemia have not been established below age 8.

Rosuvastatin is generally used as ongoing, long-term therapy for cholesterol management and cardiovascular risk reduction, for as long as it is tolerated and clinically beneficial, alongside dietary and lifestyle measures, with periodic monitoring of lipid levels and myopathy symptoms, as directed by the treating physician.

Drug Class: HMG-CoA reductase inhibitor

Rosuvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme the liver uses to synthesize cholesterol. By blocking this enzyme, rosuvastatin reduces the liver's own cholesterol production, which prompts the liver to increase the number of LDL receptors on its surface to draw more LDL cholesterol out of the bloodstream, lowering LDL-C. This same mechanism also modestly raises HDL ("good") cholesterol and lowers triglycerides.

Rosuvastatin is used in children 8 years and older with heterozygous familial hypercholesterolemia (5-20 mg once daily, depending on age) and in children 7 years and older with homozygous familial hypercholesterolemia (20 mg once daily); safety and efficacy for other pediatric indications have not been established.