lovastatin

Lovastatin is a statin medication used to lower low-density lipoprotein (LDL) cholesterol and reduce the risk of cardiovascular events in adults. It is an inhibitor of hepatic HMG-CoA reductase, the enzyme that controls the rate of cholesterol synthesis. By reducing cholesterol production in the liver, lovastatin increases the number of LDL receptors on liver cells, which enhances clearance of LDL-cholesterol from the bloodstream. It can also modestly lower triglycerides and may raise high-density lipoprotein (HDL) cholesterol in some individuals. Lovastatin is available as an immediate-release tablet (Mevacor) and an extended-release tablet (Altoprev).

Indications typically include primary hyperlipidemia or mixed dyslipidemia, and secondary prevention of cardiovascular events in high-risk adults. It may be used in certain cases of familial hypercholesterolemia, often as part of a broader lipid-lowering strategy. The choice between immediate-release and extended-release forms depends on patient needs and tolerance, with dosing generally guided by lipid response and tolerability.

Dosing and administration commonly involve starting at a low dose and titrating to achieve target LDL reduction. Immediate-release lovastatin is usually taken in the evening, with meals to optimize absorption. Extended-release lovastatin is taken once daily in the evening. The drug’s effect on liver enzymes and cholesterol is gradual, requiring several weeks to reach full benefit.

Safety and interactions: adverse effects can include headache, gastrointestinal symptoms, and elevations in liver enzymes or, rarely, myopathy or rhabdomyolysis, especially at higher doses or with interacting drugs. Contraindications include active liver disease, pregnancy, and breastfeeding. Important drug interactions involve strong CYP3A4 inhibitors, certain antibiotics and antifungals, and some lipid medicines such as fibrates. Grapefruit juice can increase lovastatin levels. Regular monitoring of liver function tests and lipid levels is advised, along with assessment for muscle pain or weakness.

History: Lovastatin was the first statin approved for lowering cholesterol, developed by Merck and approved for medical use in 1987, representing a milestone in cardiovascular risk management. It is a natural product originally derived from fungal sources with a structure later optimized for pharmaceutical use.