Cerivastatin sodium

Overview

Cerivastatin sodium is a synthetic lipid-lowering agent that belongs to the class of drugs known as statins. Statins are used to lower cholesterol levels in the blood and reduce the risk of cardiovascular disease. Cerivastatin was marketed under the trade names Baycol and Lipobay.

Mechanism of Action

Cerivastatin works by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol in the liver. By blocking this enzyme, cerivastatin effectively reduces the synthesis of cholesterol, leading to a decrease in total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides, while modestly increasing high-density lipoprotein (HDL) cholesterol.

Pharmacokinetics

Cerivastatin is administered orally and is rapidly absorbed from the gastrointestinal tract. It undergoes extensive hepatic metabolism, primarily via the cytochrome P450 enzyme system, particularly CYP2C8 and CYP3A4. The drug has a relatively short elimination half-life of 2-3 hours and is excreted mainly through the biliary route.

Clinical Use

Cerivastatin was used to treat hypercholesterolemia and mixed dyslipidemia. It was particularly effective in lowering LDL cholesterol levels, which are a major risk factor for atherosclerosis and coronary artery disease.

Adverse Effects

Common side effects of cerivastatin included myalgia, headache, nausea, and abdominal pain. However, cerivastatin was associated with a higher risk of rhabdomyolysis, a serious condition characterized by the breakdown of muscle tissue leading to the release of muscle fiber contents into the blood, which can cause kidney damage.

Withdrawal from the Market

Cerivastatin was withdrawn from the market in 2001 due to reports of fatal rhabdomyolysis, particularly when used in combination with other lipid-lowering agents such as gemfibrozil. The risk of rhabdomyolysis was found to be significantly higher with cerivastatin compared to other statins, leading to its withdrawal by the manufacturer.

Conclusion

While cerivastatin was effective in lowering cholesterol levels, its association with severe adverse effects, particularly rhabdomyolysis, led to its withdrawal from the market. This highlights the importance of monitoring for adverse effects in patients taking statins and the need for careful consideration of drug interactions.

See Also

• Statins
• Cholesterol
• Rhabdomyolysis
• HMG-CoA reductase

External Links

• FDA Drug Safety
• World Health Organization