Lovastatin

Abstract

Lovastatin is the first of a new class of cholesterol lowering drugs that competitively inhibit HMG-CoA reductase. This new drug decreases cholesterol synthesis and apolipoprotein B concentrations, and increases LDL receptor activity without adverse effects on other products in the cholesterol pathway. In patients with heterozygous familial or polygenic (non-familial) hypercholesterolaemia, oral lovastatin 20 to 40 mg twice daily reduces plasma total cholesterol and LDL-cholesterol concentrations by 25 to 40% over a period of several weeks. Lovastatin also produces decreases in plasma triglyceride and VLDL-cholesterol concentrations, although to a lesser extent. In addition, small though significant increases in HDL-cholesterol concentrations have been observed. Combined administration of lovastatin with other lipid-lowering drugs results in further reductions in plasma total and LDL-cholesterol concentrations beyond those seen with either drug alone. From findings in short term studies, lovastatin appears to be well tolerated with a low incidence of side effects. However, liver function tests and eye examinations for possible lens opacities are advised, and further long term studies in larger groups of patients are necessary before the side effect profile of lovastatin will be clearly established. As would be expected at this relatively early stage of its clinical 'life,' lovastatin has not yet been studied in a manner that would determine its effect on cardiovascular mortality during long term administration. Nevertheless, if the substantial improvements to patients' lipid and lipoprotein profiles observed in short term studies are maintained during long term administration, then lovastatin will have an important role in the pharmacological management of hyperlipidaemia.

The Effect of Statins on Postprandial Lipemia

“…Lovastatin reduces LDL cholesterol concentrations by 25-40% in hypercholesterolemic patients [151][152][153] and decreases plasma TG and VLDL levels in hypertriglyceridemic patients [102,154]. Weintraub et al found that lovastatin exerts a better TG-lowering effect in patients with mildly elevated TG levels (160-240 mg/dl; 1.8 -2.7 mmol/l) rather than at lower levels (<160 mg/dl; 1.8 mmol/) [110].…”

Statins and Bone Formation.

“…Simvastatin and pravastatin are chemical modifications of lovastatin originally derived from a fungal source [3,4,5]. Both lovastatin and simvastatin, administered as pro-drug or lactone forms, differ from the other statins administered as the active or beta-hydroxyacid ( Fig.…”

NMR evaluation of total statin content and HMG-CoA reductase inhibition in red yeast rice (Monascus spp.) food supplements

“…They cause a reversible competitive inhibition of the microsomal hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase; thus, they prevent the reduction of HMG-CoA to mevalonic acid and the formation of cholesterol [2]. The major Monascus metabolite is monacolin K, which is structurally identical to lovastatin, the first statin drug introduced into the market [3,4]. The red yeast rice products that are currently marketed as food supplements differ from the traditional red yeast rice that is sold in Chinese groceries.…”