Rosuvastatin Calcium

Rosuvastatin Calcium blocks the HMG-CoA reductase enzyme, which is required by the body to produce cholesterol. It lowers "bad" cholesterol (LDL) and triglycerides while increasing "good" cholesterol (HDL). It prevents fatty buildup in blood vessels (atherosclerosis), reducing the risk of heart attack and stroke. It is safe for long-term use and widely prescribed worldwide. However, diabetic patients should monitor blood sugar levels, as this medicine may increase them. Do not use if you have liver disease. It can be taken with or without food, but taking it at night after dinner is more effective because cholesterol synthesis is higher during the night.

• Primary Hyperlipidemia: As an adjunct to diet to reduce elevated total-C, LDL-C, ApoB, non-HDL-C and TG, and increase HDL-C. • Mixed Dyslipidemia: As an adjunct to diet to reduce elevated total-C, LDL-C and ApoB. • Hypertriglyceridemia: As an adjunct to diet to reduce triglycerides. • Primary Dysbetalipoproteinemia (Type III Hyperlipoproteinemia): As an adjunct to diet to reduce lipids. • Homozygous Familial Hypercholesterolemia (HoFH): To reduce LDL-C, total-C and ApoB. • Heterozygous Familial Hypercholesterolemia (HeFH) – Children (10–17 years): To reduce elevated total-C, LDL-C and ApoB after failing diet therapy. • Slowing Atherosclerosis Progression: As an adjunct to diet to lower total-C and LDL-C. • Prevention of MI, Stroke & Arterial Revascularization: In patients without CHD but with multiple risk factors.

Statins (HMG-CoA Reductase Inhibitors) – Lipid-lowering Agent, Other Anti-anginal & Anti-ischaemic drugs

HMG-CoA reductase inhibitor

Rosuvastatin Calcium is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methyl glutaryl coenzyme A to mevalonate, a precursor of cholesterol. Rosuvastatin Calcium 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, it inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles. Rosuvastatin Calcium is more potent than other statins and is effective at lower doses.

Rosuvastatin Calcium blocks the HMG-CoA reductase enzyme responsible for cholesterol production in the liver. This reduces cholesterol production and increases the removal of LDL cholesterol from the blood. It lowers total cholesterol, LDL, triglycerides, and increases HDL. This process prevents fatty buildup in blood vessels, reducing the risk of atherosclerosis, heart attack, and stroke. It also reduces apolipoprotein B, an important marker of atherosclerosis.

• Primary Hyperlipidemia: Initial dose 5–10 mg once daily; maximum dose 40 mg once daily. Dose can be increased every 4 weeks. • Mixed Dyslipidemia: Initial dose 5–10 mg once daily; maximum dose 40 mg once daily. Dose should be determined according to the doctor's advice. • Hypertriglyceridemia: Initial dose 5–10 mg once daily; maximum dose 40 mg once daily. Regular lipid profile monitoring is recommended. • Dysbetalipoproteinemia: Initial dose 5–10 mg once daily; maximum dose 40 mg once daily. Use with diet control. • Homozygous Familial Hypercholesterolemia (HoFH): Initial dose 20 mg once daily; maximum dose 40 mg once daily. Preapheresis LDL-C should be assessed. • Very High Cholesterol & High Risk (MI/Stroke): Dose 40 mg once daily; maximum dose 40 mg once daily. For high-risk patients. • Asian Patients: Initial dose 5 mg once daily; maximum dose 20 mg once daily. Start with a lower dose.

Take this medicine in the dose and duration as advised by your doctor. Swallow the tablet whole; do not chew, crush, or break it. It may be taken with or without food, but it is better to take it at a fixed time each day (preferably at night after dinner). Taking it at night is more effective because cholesterol synthesis is higher during the night.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose (within 12 hours), skip the missed dose and continue with your regular schedule. Do not take two doses within 12 hours. Double dosing may increase the risk of side effects.

Common Side Effects (in 5–10% patients): • Headache • Myalgia (Muscle pain) • Constipation • Asthenia (Weakness) • Abdominal pain • Nausea • Diarrhea • Gas or upset stomach Serious Side Effects (Rare – Consult Doctor): • Yellowing of eyes or skin (jaundice) – sign of liver problems • Dark urine – sign of liver problems • Severe stomach pain – sign of liver problems • Repeated or unexplained muscle pain – sign of myopathy • Muscle weakness or fatigue – sign of myopathy • Rhabdomyolysis (muscle breakdown) – rare but serious • Elevated liver enzymes (SGOT/SGPT) • Memory loss (rare) • Increased blood sugar (in diabetic patients)

• Does not usually affect driving ability. • Follow regular exercise and a low-fat diet (e.g., green leafy vegetables, fruits, whole grains). • Diabetic patients should monitor blood sugar regularly, as this medicine may increase blood sugar. • Perform liver function tests (SGOT, SGPT) before starting treatment, at 12 weeks, and regularly thereafter (e.g., every 6 months). • Inform your doctor if you have kidney disease, liver disease, thyroid problems, or diabetes. • Contraindicated during pregnancy and breastfeeding. • A lower starting dose of 5 mg is recommended for Asian patients. • Patients over 65 years have a higher risk of muscle problems; caution is required. • Perform liver function tests 12 weeks after any dose increase. • Discontinue the medicine if creatine kinase (CK) levels rise significantly or if myopathy is suspected. • Temporarily withhold the medicine in cases of sepsis, hypotension, dehydration, major surgery, trauma, severe metabolic/endocrine/electrolyte disorders, or uncontrolled seizures.

• Known hypersensitivity to Rosuvastatin Calcium or any of its components. • Active liver disease (any type of liver disease). • Unexplained persistent elevations in hepatic transaminase levels. • Pregnant women and women who may become pregnant. • Nursing mothers. • Severe renal impairment (caution required in specific cases).

• Cyclosporine: Increases Rosuvastatin exposure. Limit the dose to 5 mg once daily. • Gemfibrozil: Increases Rosuvastatin exposure. Combination should be avoided; if used, limit the dose to 10 mg once daily. • Lopinavir/Ritonavir: Increases Rosuvastatin exposure. Limit the dose to 10 mg once daily. • Atazanavir/Ritonavir: Increases Rosuvastatin exposure. Limit the dose to 10 mg once daily. • Coumarin Anticoagulants (Warfarin): May increase INR. Monitor INR frequently. • Fibrates (Fenofibrate): Increased risk of muscle-related adverse effects. Caution is required; consider dose reduction. • Niacin (Nicotinic Acid): Increased risk of muscle-related adverse effects. Caution is required; consider dose reduction.

Caution is advised when consuming alcohol with Rosuvastatin Calcium. Alcohol may put extra strain on the liver and increase the risk of liver problems. Avoid high-fat foods (e.g., fried, processed foods), as they may reduce the effectiveness of the medicine. Grapefruit juice is safe with Rosuvastatin (compared to other statins), but consume in moderation. A healthy diet (green leafy vegetables, fruits, whole grains) enhances the effectiveness of the medicine.

Rosuvastatin Calcium is highly unsafe during pregnancy (FDA Category X). Studies on pregnant women and animals have shown significant harmful effects to the developing baby. Inform your doctor if you are pregnant, planning pregnancy, or suspect pregnancy, and stop the medicine immediately. Do not use this medicine at any stage of pregnancy. It should be administered to women of childbearing age only when they are highly unlikely to conceive and have been informed of the potential hazards.

Pregnancy Category: X — always consult a doctor before taking during pregnancy.

Rosuvastatin Calcium is unsafe during breastfeeding. It is not known whether Rosuvastatin Calcium is excreted in human milk, but a small amount of another drug in this class does pass into breast milk. Do not use this medicine while breastfeeding. If treatment is essential, it is recommended to stop breastfeeding.

Rosuvastatin Calcium can be used in children 10 to 17 years of age for the treatment of Heterozygous Familial Hypercholesterolemia (HeFH). Initial dose is 5 mg once daily, maximum 20 mg once daily. Data on use in children under 10 years is limited. Dose adjustments should be made at intervals of 4 weeks or more. Consult a pediatrician.

Use with caution in elderly patients. Kidney and liver function may decline with age, so dose adjustment may be necessary. Patients over 65 years have a higher risk of muscle problems, so regular monitoring is recommended.

• Renal Impairment: For patients with severe renal impairment (CrCl <30 mL/min/1.73 m²) who are not on hemodialysis, start with 5 mg once daily and do not exceed 10 mg once daily. No dose adjustment is needed in mild to moderate kidney disease, but caution is required. • Hepatic Impairment: Contraindicated in active liver disease. Use with caution in liver disease; dose adjustment may be needed. Monitor liver enzymes (SGOT, SGPT) regularly.

There is no specific treatment in the event of overdose. In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Hemodialysis does not significantly enhance clearance of Rosuvastatin. Contact a doctor immediately if you take an excessive dose.

Store below 30°C temperature, protected from light and moisture. Keep out of reach of children. Do not use after the expiry date.

Molecular Formula: C₂₂H₂₈FN₃O₆S Molecular Weight: 501.54 g/mol Chemical Name: (3R,5S)-7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-(methylsulfonyl)-5-pyrimidinyl]-3,5-dihydroxy-6-heptenoic acid calcium salt