Rosuvastatin
It 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. Rosuvastatin is a medication belonging to the statin class of drugs, primarily used to lower cholesterol and triglycerides in the blood. By inhibiting the enzyme HMG-CoA reductase, it effectively reduces the production of cholesterol in the liver, leading to a decrease in the levels of low-density lipoprotein (LDL) cholesterol, commonly known as "bad" cholesterol. Additionally, it can slightly increase high-density lipoprotein (HDL) cholesterol, or "good" cholesterol, contributing to improved cardiovascular health.Rosuvastatin is indicated for: -Reducing elevated total cholesterol (total-C), LDL-C, apolipoprotein B (ApoB), and triglycerides (TG) -Increasing HDL-C in patients with primary hyperlipidemia or mixed dyslipidemia -Treatment of hypertriglyceridemia -Primary dysbetalipoproteinemia (Type III hyperlipoproteinemia) -Slowing the progression of atherosclerosis as part of a treatment strategy to lower total-C and LDL-C -Primary prevention of cardiovascular disease (CVD) in patients without clinically evident coronary heart disease but with multiple risk factors for CVD -Primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia) or mixed dyslipidaemia (type IIb), including familial hypercolesterolaemia.
-The usual starting dose is 10-20 mg once daily. -For patients with severe hypercholesterolemia or at high cardiovascular risk, a starting dose of 20-40 mg may be considered. -The maintenance dose ranges from 5-40 mg daily, based on patient response and clinical evaluation. -Doses should be adjusted according to individual patient requirements and response, and periodic lipid level assessments are recommended.
Rosuvastatin is contraindicated in: -Patients with known hypersensitivity to rosuvastatin or any of its components -Active liver disease, including unexplained persistent elevations of serum transaminases -Severe renal impairment (creatinine clearance <30 mL/min) -Pregnant or breastfeeding women, due to potential harm to the fetus or nursing infant -Co-administration with certain drugs like cyclosporine
-Regular liver function tests are recommended before and during treatment. -Caution is advised for patients with a history of liver disease, heavy alcohol use, or severe renal impairment. -Rosuvastatin can increase the risk of myopathy and rhabdomyolysis, especially at higher doses. Promptly report unexplained muscle pain, tenderness, or weakness. -Use caution in patients of Asian descent, as they may have increased plasma concentrations of rosuvastatin.
Common side effects include: -Headache -Nausea -Muscle pain (myalgia) -Abdominal pain -Asthenia (weakness) -Serious but rare side effects: -Myopathy and rhabdomyolysis -Liver enzyme abnormalities -Kidney failure
Rosuvastatin can interact with: -Cyclosporine: Significantly increases rosuvastatin levels. -Warfarin: Can increase the anticoagulant effect. -Gemfibrozil and other fibrates: Increase the risk of myopathy. -Antacids containing aluminum or magnesium: Can reduce the absorption of rosuvastatin. -Ezetimibe: May increase the risk of adverse muscular effects.
