Rosuvastatin Explained - Everything You Need To Know

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Rosuvastatin is a synthetic lipid-lowering medication belonging to the drug class of statins, also known as HMG-CoA reductase inhibitors.
It is one of the most potent statins used to lower cholesterol levels and prevent cardiovascular complications in susceptible individuals.
Major Indications for rosuvastatin therapy include the following.
For hyperlipidemia and mixed dyslipidemia to reduce blood cholesterol and triglyceride levels.
For the primary prevention of cardiovascular disease in high-risk patients.
And for the secondary prevention in patients with established cardiovascular disease, especially following myocardial infarction.
Rosuvastatin works by inhibiting the enzyme HMG-CoA reductase, which catalyzes the rate limiting step in cholesterol synthesis pathway.
Inhibition of this enzyme results in reduced cholesterol synthesis, primarily in hepatocytes.
Increased LDL receptor expression on liver cells, enhancing clearance of circulating LDL cholesterol from the blood.
Reduction of plasma triglycerides and modest increases in HDL cholesterol.
Statins also exert pleiotropic effects, which are unrelated to their major mechanism of action.
Some of these effects include improved endothelial function, stabilization of atherosclerotic plaques, and reduction of vascular inflammation.
Rosuvastatin is taken orally, typically in the evening or at night, because the synthesis of cholesterol is higher at night.
It has a low oral bioavailability and is highly plasma protein bound.
The drug is primarily metabolized in the liver and excreted unchanged in feces.
A small amount is excreted in urine.
Major Adverse Effects of rosuvastatin include the following.
Musculoskeletal effects such as Myalgia, or muscle pain, myopathy, and very rarely, rhabdomyolysis.
Hepatic effects such as Elevated liver enzyme levels, and rarely, acute liver failure.
Gastrointestinal effects such as nausea, abdominal pain, or diarrhea.
Neurological effects such as headache, dizziness, or memory issues.
Hypersensitivity reactions such as rash, pruritus, or angioedema.
It is important to note that statins are usually well-tolerated by most individuals and only a minority of patients experience these adverse effects.
Contraindications for rosuvastatin therapy include the following.
Hypersensitivity to rosuvastatin or its components.
Active liver disease or unexplained persistent elevations in liver transaminases.
Pregnancy and lactation.
Severe renal impairment.
And concomitant use with cyclosporine, gemfibrozil, or other drugs increasing statin toxicity.

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