Cerivastatin, cholesterol-lowering effects

Simons, L.A., Additive effect of plant sterol-ester margarine and cerivastatin in lowering low-density lipoprotein cholesterol in primary hypercholesterolemia. Am. J. Cardiol, 90, 737, 2002. 

In one of our other studies [37], the 6 months therapy with 0,4 mg daily of other HMG-CoA-reductase inhibitor cerivastatin, which is more effective than pravastatin as cholesterol-lowering drug, sharply increased the level of LDL lipohydroperoxides in the blood plasma of patients [37] (Figure 18). At the same time administration of cerivastatin in combination with synthetic antioxidant probucol in daily dose 250 mg did not produce the increase of the LDL lipohydroperoxide level in the plasma during all time of the observation [37] (Figure 18). 

Today, pharmaceutical companies sometimes pull certain medicines from the market even if authorities do not require them to do so. An example is the cholesterol lowering drug cerivastatin, which had side effects similar to other related drags, but its manufacturer decided that these side effects were too cotmnon and stopped selhng the medicine. 

Fibrates are the most effective triglyceride-lowering agents and also raise HDL cholesterol levels. Combination therapy with a fibrate, particularly gemfibrozil, and a statin has been found to increase the risk for myopathy. Of the 31 rhabdomyolysis deaths reported with cerivastatin use, 12 involved concomitant gemfibrozil.25 Therefore, more frequent monitoring, thorough patient education, and consideration of factors that increase the risk as reviewed previously should be considered. 

Other statins include simvastatin (also a lactone prodrug), pravastatin, atorvastatin, and cerivastatin (active form with open ring). The statins are the most important therapeutics for lowering cholesterol levels. Their notable cardiovascular protective effect, however, appears to involve additional actions. 

The ability of statins to lower hsCRP was first described for pravastatin using data accumulated in the Cholesterol and Recurrent Events (CARE) trial. These data were initially highly controversial because they suggested that statins have both hpid-lowering and antiinflammatory effects. However, confirmatory work rapidly showed the effect of statins on hsCRP to be a consistent and important class effect. Studies of atorvastatin, cerivastatin, lovastatin, pravastatin, and simvastatin have shown that, on average, median hsCRP concentrations decline 15% to 25% as early as 6 weeks after initiation of therapy. Importantly the magnitude of LDL cholesterol reduction caused by statin therapy is minimally correlated with the magnitude of hsCRP reduction. ... 

Statins are now amongst the most widely used drugs worldwide. They are highly effective in lowering cholesterol levels, and have been shown to be effective in the primary and secondary prevention of ischaemic heart disease. Statins, however, can cause muscle toxicity, which most commonly manifests as an asymptomatic rise in CPK, and in the most severe cases, can cause rhabdomyolysis and death (Fig. 3) (Laaksonen 2006). Cerivastatin was withdrawn in 2001 because of its propensity to... 

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